NCM106 – MATABERDE – ENDTERM

LEARNING MODULE 1:

PART 1:

DRUGS AFFECTING THE ENDOCRINE SYSTEM

PART 1: Overview of the Endocrine System

Structure and Function of the Endocrine System

- The endocrine system is a regulatory system that

communicates through the use of hormones. It
provides communication within the body and helps
to regulate growth and development, reproduction,
energy use, and electrolyte balance. Hormones released by the hypothalamus:
- Because the endocrine and nervous systems are
1. Gonadotropin Releasing Hormones (GnRH)
tightly intertwined in the regulation of body
2. Corticotropin Releasing Hormones (CRH)
homeostasis, they are often referred to as the
3. Thyroid Releasing Hormone (TRH)
Neuroendocrine System.
4. Prolactin Releasing Hormone (PRH)
5. Growth Hormone Releasing Hormone (GHRF)

Hormones synthesized in hypothalamus and stored in

Posterior Pituitary Gland (Neurohypophysis):

6. ADH- Antidiuretic Hormone

7. Oxytocin

Glands

- The endocrine glands are collections of specialized

cells that produce hormones that cause an effect at
hormone receptor sites. These glands do not have
ducts, so they secrete their hormones directly into
the bloodstream.

Hormones

- A Hormone is a chemical that is produced within the

body, is needed in only small amounts, travels to PITUITARY GLAND
specific receptor sites to cause an increase or
The pituitary is made of three lobes:
decrease in cellular activity and is broken
immediately. I. Anterior Lobe
Hypothalamus - Produces stimulating hormones in response to
hypothalamic situation.
- The hypothalamus is known as the ‘’master gland’’
of the neuroendocrine system and helps to regulate Produces 6 major hormones:
the central and autonomic nervous systems and the
endocrine system to maintain homeostasis. 1. Growth hormone (GH)
2. Adrenocorticotropic Hormone (ACTH)
3. Follicle-Stimulating Hormone (FSH)
4. Luteinizing Hormone (LH)
𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 5. Prolactin (PRL)
Example of negative feedback system:
6. Thyroid Stimulating Hormone (TSH)

➢ When the hypothalamus senses the need for thyroid

hormone, it secretes the releasing factor
Thyrotropin- releasing hormone (TRH) directly into
the anterior pituitary.

➢ In response to the TRH, the anterior pituitary

II. Posterior Lobes
secretes thyroid stimulating hormone (TSH) which
- Stores 2 hormones produced by the hypothalamus. in turn stimulates the thyroid gland to produce
1. ADH (antidiuretic hormone) thyroid hormones.
2. Oxytocin
➢ When the hypothalamus senses the rising levels of
thyroid hormone, it stops secreting TRH, resulting in
III. Immediate Lobe
decreased TSH production and subsequent reduced
- Produces endorphins and enkephalins to modulate thyroid hormone levels.
pain and perception.
➢ The hypothalamus sensing the falling thyroid
hormone secretes TRH again. The negative feedback
Hypothalamic – Pituitary Axis (HPA) system continues in this fashion, maintaining the
- Together, the hypothalamus and the pituitary levels of thyroid hormone within a relatively narrow
function closely to maintain endocrine activity along range of normal.
what is called the hypothalamic- pituitary axis (HPA)
using a series of negative feedback systems.

➢ Two of the anterior pituitary hormones (GH and

PRL) do not have a target to produce hormones
so they cannot be regulated by the same type of
feedback mechanism.

*The hypothalamus responds directly to rising levels of

GH and PRL

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 PART 2:

DRUGS AFFECTING HYPOTHALAMIC HORMONES

- The hypothalamus uses a number of hormones or

factors to either stimulate or inhibit the release of
hormones from the anterior pituitary.

Factors that stimulate the release of hormones:

1. Growth hormone-releasing hormone (GHRH)

2. Thyrotropin-releasing hormone (TRH)
3. Gonadotropin-releasing hormone (GnRH)
4. Corticotropin-releasing hormone (CRH)
5. Prolactin-releasing Hormone (PRLH)

Factors that inhibits the release of hormones:

1. Somatostatin (growth hormone inhibiting

factor)
2. Prolactin-inhibiting factor

DRUGS AFFECTING HYPOTHALAMIC HORMONES

DRUG NAME DOSAGE/ROUTE USUAL INDICATIONS

AGONIST

Goserelin 3.6mg - Used as an

(Zoladex) subcutaneously antineoplastic agent
every 28 d or for treatment of
10.8mg specific hormone
Subcutaneously stimulated cancers
every 3 months

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
Histerelin One implant - Palliative
(Vastas) implanted treatment of AGONISTS
subcutaneously advanced o Goserelin (Zoladex), Histerelin (Vastas),
every mo 12 prostate cancer Leuprolide (Lupron), Nafarelin (Synarel), and
Tesamorelin (Egrifta) are all Gonadotropin-
Leuprolide Prostate cancer: - Used as
releasing hormone (GnRH) analogues.
(Lupron) 1md/d Antineoplastic
subcutaneously or agent ▪ They are structured to really look like GnRH and
various depot for treatment of to work the same.
preparations specific cancers,
Endometriosis: treatment of ▪ GnRH is a hormone released by the
3.75 mg IM once a endometriosis Hypothalamus. It stimulates the anterior pituitary
Month and precocious gland to release FSH & LH which in turn
puberty that stimulates the gonads to release the sex
Preococious results from hormones. In males, testosterone and in females,
puberty: hypothalamic estrogen, and progesterone.
50mcg/kg/d activity
Subcutaneously
▪ Precocious puberty is defined as the early onset
of secondary sexual characteristics. It’s generally,
Nafarelin 400 mcg/d divided - Treatment of
for the girl’s puberty who started earlier than 8
(Synarel) as one spray in left Endometriosis
nostril AM or PM; and precocious years of age and 9 years old for boys. It is
one spray in right puberty associated with pubertal pituitary gonadotropin
nostril AM or PM activation. It may significantly show advanced
Precocious bone age that can result in diminished adult
puberty: height.
1600-1800 mcg/d
Intranasally ▪ More GnRH = More production of FSH = Increased
production of sex hormones = The child will
Tesamorelin 2mg - Reduction of develop precocious puberty
(Egrifta) subcutaneously excessive ▪ If the precocious puberty is hypothalamic in
once a day abdominal fat
origin, it may be caused by a tumor called central
in HIV-infected
precocious puberty.
patients with
lipodystrophy

ANTAGONISTS

Degarelix Initially 240mg by - Treatment of

(Firmagon) subcutaneously Advanced
injection of two prostate cancer
120-mg injections
at separate sites;
maintenance 80mg
subcutaneously
every 28 days

Ganirelix 250 mcg - Inhibition of

(Antagon) subcutaneously on premature
day 2 or 3 of the luteinizing
menstrual hormones urge
in women
undergoing
controlled
▪ The release of GnRH , FSH, and LH is governed by
ovarian
stimulation as negative feedback which means that if there is
part of a fertility too much testosterone or estrogen being
program. produced, the body will send a signal to the brain,
to the hypothalamus.
▪ As a result, hypothalamus will reduce the
production of GnRH which in turn will reduce the
production of FSH & LH.
𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 ▪ There will be a decreased production of
testosterone for males and for females, estrogen
and progesterone. This produce in the reduced
production of the sex hormones.
➢ If we give Nafarelin and Leuprolide continuously,
initially, it will cause an increase in the
production of FSH and LH. But after weeks of
continuous medication, the levels of LH & FSH
will drop because the pituitary gland will stop
responding to the GnRH and Leuprolide. This will
lead to the decrease of the production of
Female/Male sex hormones. That’s how Lupron
works in treating precocious puberty.
ANTAGONISTS
- The primary function of antagonist is they work by
limiting the release of hypothalamic hormones.
➢ If you give Degarelix, it will decrease the amount
of FSH and LH and will therefore decrease the
amount of testosterone. This will slow or stop
the spread of prostate cancer cells that needs
testosterone in order to grow.
➢ Ganirelix works by preventing the rise of LH
which can trigger early ovulation. It will help
delay premature ovulation so more time will
begiven for the egg to mature. Thereby, there
will be high chances of conception.
NAFARELIN (SYNAREL) & LEUPROLIDE (LUPRON)
- They are medications that are used in the treatment
of endometriosis and central precocious puberty.
Therapeutic Actions and Indications:
▪ Not all of the hypothalamic hormones are used as
pharmacologic agents.
▪ A number of hypothalamic releasing hormones
are used for diagnostic purposes only, and others
are used primarily as antineoplastic agents.
o Antineoplastic drugs are medications used
to treat cancer.
▪ Tesamorelin is used to stimulate GH and its
lipolytic effects, helping to decrease the excess
abdominal fat in HIV-infected patients with
lipodystrophy.
Pharmacokinetics:
▪ For the most part, these drugs are absorbed
slowly when given IM, subcutaneously, or in
depot form (a slow-release form of medication.
e.g. Leuprolide (Lupron)
▪ They tend to have very long half-lives of days to
weeks.
▪ Because they are hormones or similar to
hormones, they cross the placenta, and they
cross into breastmilk. Most of them are excreted
in urine.
▪ Nafarelin is given in a nasal form.
Note:
▪ A drug’s time to onset of action, time to peak
effect, and duration of action are all
characteristics defined by PHARMACOKINETICS.
▪ THE HALF-LIFE OF A DRUG is an estimate of the
period of time that it takes for the concentration
or amount in the body of that drug to be
reduced by exactly one half (50%).
Contraindications and Cautions:
• These drugs are contraindicated with known
hypersensitivity to any component of the drug
because of the risk of hypersensitivity reactions
and during pregnancy and lactation because of
the potential adverse effects to fetus or baby.
• Caution should be used with renal impairment
which could interfere with excretion of the drug;
with peripheral disorders which could alter the
absorption of injected drug;
• With rhinitis when using nafarelin - could alter
the absorption of the nasal spray
Adverse Effects:
- Adverse effects are related to the stimulation or
blocking of regular hormone control.
➢ AGONISTS: can lead to increased release of sex
hormones leading to ovarian overstimulation,
flushing, increased temperature and appetite,
and fluid retention.
➢ ANTAGONISTS: can lead to a decrease in
testosterone levels, leading to loss of energy,
decreased sperm count and activity, potential
alterations in secondary sex characteristics, or to
a decrease in female sex hormones, leading to
𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 ➢ HYPOACTIVE PITUITARY - decreased functioning of
lack of menstruation, fluids and electrolyte the pituitary gland and as result, there’s a decreased
changes, insomnia, and irritability in production of hormones.

KEY POINTS: ▪ In order to supply for the missing hormones, we will

• The hypothalamus releases hormones that act as give specific hormones as a replacement therapy.
releasing factors, stimulating the anterior ▪ Agonists - mimic the effect of specific pituitary
pituitary to release specific stimulating factors hormones.
and inhibiting factors that act to stop the
production of specific anterior pituitary DRUGS AFFECTING ANTERIOR PITUITARY HORMONES
hormones.
• Not all of the hypothalamic hormones are DRUG NAME DOSAGE/ROUTE USUAL INDICATIONS
available for pharmacological use. GROWTH HORMONE AGONISTS
• Those that are available are used mostly for:
1. Diagnostic Testing Somatropin Dose Varies - Treatment of
2. Treating Some Forms of Cancer (Nutropin, with each children with growth
3. As Adjuncts in Fertility Programs. Saizen, product, check failure due to lack of
Humatrope) manufacturer’s GH or to chronic
instructions; renal failure;
must be given
subcutaneously - Replacement of GH
PART 3A: or IM in patients with GH
DRUGS AFFECTING ANTERIOR PITUITARY HORMONES deficiency;

- Agents that affect pituitary function are used mainly - Long term
to mimic or antagonize the effects of specific treatment of growth
pituitary hormones. failure in children
- They may be used either as: born small for
1. Replacement therapy for conditions resulting gestational age who
from a hypoactive pituitary or, do not achieve catch-
2. For diagnostic purposes. up growth by 2y of
age;

- Treatment of short
stature associated
with Turner’s
Syndrome or Prader-
Willi’s Syndrome;

- Also approved to
increase protein
production and
growth in various
AIDS-related stress.

Somatropin - Reserved for use in

0.1mg/kg treatment of adults
rDNA
subcutaneously with short bowel
origin
for 4 weeks syndrome who are
(Zorbtive)
receiving specialized
nutritional support.

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 to induce
▪ Growth hormones are also called SOMATROPIN or per week is ovulation in
human growth hormone. unusual females with
▪ Growth hormones stimulate the growth of functioning
essentially all tissues of the body, including the ovaries, for
bones. treatment of
prepubertal
cryptorchidism
➢ SHORT BOWEL SYNDROME- surgery due to a
when there is no
removal of a portion of the small intestine. Some anatomical
children are born with abnormally short small obstruction to
intestine or with part of their bowel missing, which testicular
can cause short bowel syndrome. If you have this, movement
then the body will have less absorption of nutrients.

□ Male hypogonadism- the body does not produce

Therapeutic Actions and Indications: enough testosterone which plays a key role in masculine
▪ In clinical practice, the agents that are used growth and development
purely as a replacement for anterior pituitary - Not applicable to women with low ovarian reserve, this
hormones are those acting as GH-somatropin will not be applicable for them.
and somatropin rDNA origin. Both of these drugs
are produced with use of rDNA technology. □ Prepubertal cryptorchidism- a condition where one or
both the testes fails to descend from the abdomen into the
Pharmacokinetics: scrotum
▪ Somatropin is injected and reaches peak levels
within 7 hours.
▪ It is widely distributed in the highly perfused
tissues, particularly the liver and kidney.
▪ Excretion occurs through urine and feces.
▪ Patients with liver or renal dysfunction may
experience reduced clearance and increased
concentration of the drug.

Contraindications and Cautions:

• Somatropin is contraindicated in the presence
of closed epiphyses or with underlying cranial Chorionic 250 mg - Induction of
Gonadotropin subcutaneously ovulation in
lesions because of the risk of serious
alpha given 1 d after infertile females
complications and with abdominal surgery and
(Ovidrel) last dose of a who have been
acute illness secondary to complications of open- FSH stimulator pretreated with
heart surgery because of potential problems FSH
with healing.
• Must be used with caution in pregnancy and
lactation because of the potential for adverse
effects on the fetus.
- In order to increase the odds of pregnancy the patient
Adverse Effects: will be given some drug like Femara (Letrozole) or
➢ Use of GH - development of antibodies to GH and Clomid, they’re given to grow and mature an egg. In
subsequent signs of inflammation and autoimmune order to induce the ovulation, for the egg cell to pop
type reactions, such as swelling, and joint pain, and out from the graafian follicles, the patient will be given
the endocrine reactions of hypothyroidism and a trigger shot of Chorionic Gonadotropin alpha
insulin resistance. (Ovidrel).

DRUGS AFFECTING OTHER ANTERIOR PITUITARY - This can be used in cycle with timed sexual intercourse
HORMONES with interior insemination or also you need in vitro
fertilization to increase the odds to achieve pregnancy
in each cycle.
Chorionic Dose Varies with - Treatment of
Gonadotropin indication; 4000- male
(Chorex, others) 10000 IU IM one hypogonadism,
to three times

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 Cosyntropin 250 mg - Diagnosis of
(Cortrosyn) subcutaneously adrenal function
given 1 d after
last dose of a
FSH stimulator.

Thyrotropin 0.9mg IM - Adjunctive

alpha followed by treatment for
(Thyrogen) 0.9mg IM in 24H post-radio iodine
ablation of thyroid
tissue in patients
with near total
Thyroidectomy and
well differentiated
thyroid cancer
without metastasis

Short Synacthen test (SST) /

ACTH Stimulation test/
Cosyntropin Test

- Used to determine the ability ▪ Most conditions of GH hypersecretion are treated by

of the adrenal glands to
produce cortisol in response to
ACTH (the pituitary hormone
regulating adrenal cortisol
production).
GROWTH HORMONE ANTAGONISTS
radiation therapy or surgery. Drug therapy for GH
excess can be used for those patients who are not
candidates for surgery or radiation therapy.
▪ The drugs include:
1. Dopamine agonist:
✓ Bromocriptine mesylate (Parlodel)
Prototype drug; (suppresses growth
hormone (GH) secretion in most
patients with acromegaly )
2. Two somatostatin analogues:
✓ Octreotide acetate (Sandostatin)
✓ Lanreotide (Somatuline depot)
3. GH analogue
✓ Pegvisomant (Somavert)

- GH hypersecretion is usually caused by pituitary

GROWTH HORMONE ANTAGONIST
tumors and can occur at anytime of life. This is often
referred to as HYPERPITUITARISM.
Bromocriptine 1.25-2.5 mg/d - Treatment of
mesylate PO Acromegaly in
▪ If hyperpituitarism occurs before the epiphyseal
(Parlodel) patients who are
plates of the long bones fuse, it causes an
not candidates
acceleration in linear skeletal growth, producing for or cannot
GIGANTISM OF 7 TO 8 FEET in height with fairly tolerate other
normal body proportions. therapy, not
recommended
for children <15y

- Also used for the prevention or suppression of

postpartum physiological lactation but not really
recommended because of the side effects

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 Lanreotide Initially 90mg - Long term • GH antagonists should be used cautiously in the
(Somatuline subcutaneously Treatment of presence of any other endocrine disorder (e.g.
depot) every 4 weeks for Acromegaly in diabetes, thyroid dysfunction) that could be
3 months; then patients with exacerbated by the blocking of GH
adjust dose inadequate
based on patient response to or
Adverse Effects:
response who cannot be
➢ Octreotide - Patients with renal dysfunction may
treated with
surgery or accumulate higher levels of octreotide. GI
radiation complaints are not uncommon because of the
Octreotide 100-500mcg - Treatment of drug effects on the GI tract.
subcutaneously Acromegaly in ➢ Lanreotide - associated with changes in blood
adults who are glucose levels and glucose should be followed
not candidates carefully while on the drug.
for or cannot o Octreotide and Lantreotide are
tolerate other somatostatin analogues.
therapy o Somatostatin inhibit the release of
(Sandostatin) TID adjust dose - Treatment of insulin. Insulin moves the blood sugar
in elderly Acromegaly in (glucose) into the cells.
patients adults who are
➢ Bromocriptine is also associated with GI
not candidates
disturbances. Because of its dopamine-blocking
for or cannot
tolerate other effects, it may cause drowsiness and postural
therapy hypotension. It blocks lactation and should not
Pegvisomant 40mg - Treatment of be used by nursing mothers.
(Somavert) subcutaneously Acromegaly in ➢ Pegvisomant may cause pain and inflammation
as a loading adults who are at the injection site (common).
dose, then not candidates ➢ Increased incidence of infection, nausea, and
10mg/d for or cannot diarrhea and changes in liver function may
subcutaneously tolerate other occur.
therapy

Pharmacokinetics:
▪ Octreotide is rapidly absorbed and widely
distributed throughout the body, and it is
metabolized in the tissues with about
30%excreted unchanged in the urine.
▪ Lanreotide forms a depot in the subcutaneous
tissue and is slowly released into the circulation
with a half-life of 25 to 30 days. It is metabolized
in the tissues and excretion is not known.
o If it’s in depot form meaning the
medication will be slowly released to the
body over a number of weeks
▪ Bromocriptine is administered orally and
effectively absorbed from the GI tract. The drug
undergoes extensive first-pass metabolism in the
liver and is primary excreted in the bile.
▪ Pegvisomant is given by
SQ(subcutaneous)injection and is slowly
absorbed, reaching peak effects in 33 to 77 hours,
it also clears from the body at a slow rate, with a
half-life of 6days. The drug is excreted in the urine.
Contraindications and Cautions
• Bromocriptine should not be used during
pregnancy or lactation because of its effects on
the fetus and because it blocks lactation.
PART 3B:
DRUGS AFFECTING POSTERIOR PITUITARY HORMONES
- Produced in the hypothalamus but stored in the
posterior pituitary gland
- The posterior pituitary stores two hormones
produced in the hypothalamus:
1. ANTIDIURETIC HORMONE (ADH, also known as
vasopressin) - ADH possesses antidiuretic,
hemostatic, and vasopressor properties.
• Lack of ADH produces diabetes insipidus (DI),
which is characterized by large amounts of dilute
urine and excessive thirst.
✓ The patient with diabetes insipidus will
pass large amounts of dilute urine up to
8 liters.
✓ They have high level of urinary output
due to low ADH and as a result because
of dehydration and as the patient loses
too much fluid, there will be
hypernatremia.
• When ADH is produced in excess, the condition
is called syndrome of inappropriate antidiuretic
hormone (SIADH).

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 ✓ Low urinary output because of too
much ADH
✓ It will produce dilutional hyponatremia
due to overhydration.
Vasopressin Blockers
- They block the action of Vasopressin or ADH.
- Cause a loss of water through the urine and therefore
increase in serum sodium levels as the water level
decreases.
- Must be given under close supervision to monitor
fluid volume carefully.

➢ Green - synthetic arginine vasopressin

➢ Light blue - vasopressin blockers

DRUGS AFFECTING POSTERIOR PITUITARY HORMONES

Desmopressin Adult: 0.1-0.4 - Treatment of

(DDAVP, Stimate) ml/d PO, IV, neurogenic
subcutaneously, diabetes
intranasal for insipidus, von
diabetes Willebrand’s
insipidus; disease,
0.3mcg/kg IV hemophilia;
over 15-30 min being studied for
for von the treatment
Willebrand’s of chronic
disease; 20mcg autonomic failure
intranasal at
bedtime for - They replace a
nocturnal low level of
2. OXYTOCIN - stimulates milk ejection or “let down” enuresis vasopressin
in lactating women. In pharmacological doses, it can
be used to initiate or improve uterine contractions Pediatric:
in labor. 0.05-0.3 ml/d
intranasal for
diabetes
Therapeutic Actions and Indications:
insipidus. 0.3
mcg/kg IV over
▪ Endogenous hormone- produced or 15-30 min for
synthesized within the organism or system. von
▪ Exogenous hormones- any hormones entering Willebrand’s
the organisms that are not produced by the disease
patient's own endocrine glands.
▪ The synthetic ADH that are given to the patient Conivaptan 20mg IV loading - Treatment of
works the same as the endogenous (Vaprisol) dose over 30min. hypervolemic or
antidiuretic hormone. The job of the ADH is to then 20-40mg by euvolemic
tell the kidneys to keep more water inside the continuous IV hyponatremia in
blood vessels so that the urine will become infusion over hospitalized
more concentrated. 24hrs patients

ADH (antidiuretic hormone)

- a.k.a. AVP (arginine vasopressin)

- Released in response to increases in plasma
osmolarity or decreases in blood volume.
- Produces its antidiuretic activity in the kidneys,
causing the cortical and medullary parts of the
collecting duct to become permeable to water,
thereby increasing water reabsorption and
decreasing urine formation. These activities reduce
plasma osmolarity and increase blood volume.

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛

Tolvaptan Initially 15mg - Treatment of
(Samsca) PO; titrate to a hypervolemic
maximum of 60 and euvolemic
mg/d PO based hyponatremia
on patient that is resistant
response to correction
with fluid
restriction
Pharmacokinetics:
▪ Desmopressin - is rapidly absorbed and
metabolized; it is excreted in liver and kidneys.
✓ It is available for oral, IV, subcutaneous,
and nasal administration.
▪ Tolvaptan - given orally, readily absorbed, half-
life is 12 hours.
- The half-life of a drug is the time it takes for the
amount of a drug's active substance in your body to
reduce by half.
▪ Conivaptan - given by IV infusion, half-life of the
drug is 5 hours.
Contraindications and Cautions:
• Drugs affecting the posterior pituitary
hormones are contraindicated with any known
allergy to the drug or its components to avoid
potential hypersensitivity reactions or with
severe renal dysfunction which could alter the
effects of the drugs.
• Should not be used during pregnancy because
of the risk of uterine contractions that would
harm the fetus or during lactation because of the
potential adverse effects to the fetus or baby.
- The hormones stored in the posterior lobe are
vasopressin or ADH and oxytocin. If you will give
synthetic vasopressin, you could also tap the release
of oxytocin that it kept from the same gland.
▪ Must be used with caution in patients who
consume large amounts of fluid because of the
increased risk of electrolyte dilution and
hyponatremia.
▪ Such as patients with psychogenic polydipsia. It
is a form of polydipsia characterized by excessive
fluid intake in the absence of physiological stimuli
to drink. The patient will be overly hydrated.
Adverse Effects:
Desmopressin - works just like the endogenous
vasopressin or ADH. Vasopressin stimulates sodium and
water reabsorption.
✓ water intoxication (drowsiness, light-
headedness, headache, coma, convulsions)
related to the shift to water retention and
resulting electrolyte imbalance.
✓ tremor, sweating, vertigo, and headache related
to water retention (a hangover effect),
abdominal cramps, flatulence, nausea, and
vomiting related to the stimulation of GI motility.
✓ local nasal irritation related to nasal
administration.
Conivaptan and Tolvaptan
✓ Polyuria, blood pressure changes,
hyperglycemia, arrhythmias associated
with rapid volume shifts.
✓ Polyuria- a condition where the body
urinates more than usual and passes
excessive or abnormally large amounts of
urine each time you urinate.
✓ Constipation, dry mouth, and thirst
CLINICALLY IMPORTANT DRUG-DRUG INTERACTIONS
➢ Increased risk of antidiuretic effects if desmopressin
is combined with carbamazepine or chlorpropamide.
➢ Tolvaptan and conivaptan should be used with care
with digoxin, angiotensin-converting enzyme
inhibitors, angiotensin receptor blockers, and
potassium-sparing diuretics, all of which could cause
hyperkalemia.
➢ Tolvaptan should not be combined with
telithromycin because of a risk of severe tolvaptan
toxicity.
Key Points:
➢ Posterior Pituitary hormones are produced in
the hypothalamus and stored in the posterior
pituitary. They include oxytocin and ADH.
𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 ➢ Lack of ADH produces diabetes insipidus, which
GMA:
is characterized by large amounts of dilute urine
and excessive thirst. 1. Glucocorticoids
➢ ADH replacement uses an analogue of ADH, 2. Mineralocorticoids.
desmopressin, and can be administered 3. Androgens (similar to male sex hormones)
parenterally or intranasally.
➢ Vasopressin blockers are used to restore sodium
balance in patients with severe hyponatremia.
➢ Fluid balance needs to be monitored when
patients are taking drugs that affect ADH
- There should be strict intake and output monitoring,
strict measurement of daily weight. Take your weight
ideally upon rising up in the morning before
breakfast so that there will be no discrepancies.

PART 4:

ADRENOCORTICAL AGENTS

The Adrenal Glands

- The two adrenal glands are flattened bodies that sit

on top of each kidney. Each gland is made up of an
inner core called the adrenal medulla and an outer
shell called the adrenal cortex.
- Adrenal medulla is a part of the sympathetic nervous
system (SNS). It is a ganglion of neurons that releases
neurotransmitters into circulation when the SNS is
stimulated:
1. Norepinephrine
2. Epinephrine
- The secretion of these neurotransmitters directly
into the bloodstream allows them to act as
hormones, traveling from the adrenal medulla to
react with specific receptor sites throughout the
body.

- The adrenal cortex surrounds the medulla and

consists of three layers of cells, each of which
synthesizes chemically different types of steroid
hormones that exert physiological effects throughout
the body. The adrenal cortex produces three types of
corticosteroids:

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 HORMONES OF THE ADRENAL CORTEX
Glucocorticoids Mineralocorticoids
- Proteins and fats - Retention of sodium by
converted to glucose or the kidneys
broken down for energy - Increased blood volume
(gluconeogenesis) and blood pressure
→Increased blood
glucose □ Sodium and water are
like Mary and the little
□ Gluconeogenesis lamb.
- proteins and fats will be - Everywhere that Mary
converted to glucose or went, the lamb will be
broken down for energy. sure to go.
• Suppression of - Once sodium is Hypothalamic Pituitary Axis (HPA)
Immune system retained, the water is
• Modulates also reabsorbed. - The release of steroid hormones from the Adrenal
inflammation. - The end product is Cortex is affected by the HPA.
- It has hyperglycemic increased blood volume - The corticosteroids will be released by first the
immunosuppressant and and subsequent hypothalamus will secrete the hormone
anti-inflammatory increased in blood corticotropin-releasing hormone and this will
properties. pressure. stimulate the anterior pituitary gland to release
- Due to the strong adrenocorticotropic hormone and will in turn
anti-inflammatory and □ ACTH only minimally stimulate the adrenal cortex to release the
immune suppressive influences aldosterone corticosteroids. This pattern is influenced by sleep
effect of glucocorticoids secretion
wake cycle or the diurnal rhythm. People with regular
in almost all immune
sleep and wake cycle will release the corticotropic
cells, it is indispensable in
releasing hormone at around midnight.
the treatment of
autoimmune - Adrenocorticotropic hormone and corticosteroids
diseases will be released at around 6:00 to 9:00 A.M.
- The peak adrenal response happens around 8:00-
9:00 A.M. Corticosteroids are given during this time
Adrenal Sex Hormones (Androgens) to mimic the normal physiological response.
□ The main sex hormone produce in the adrenal
cortex are androgens.
• Exert effects similar to those of male sex
hormones.
• The adrenal gland may also secrete small
amounts of some estrogens, or female sex
hormones.
• ACTH controls the secretion of adrenal
androgens.
• When secreted in normal amounts, the
adrenal androgens probably have little effect,
but when secreted in excess, as in certain in
born enzyme deficiencies, masculinization
may result.
• This is termed the adrenogenital syndrome.

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛

➢ SHORT-TERM STRESS
- The release of catecholamines (Epinephrine and
norepinephrine) in short-term stress.
- The nerve impulses from the brain from the
hypothalamus travels to the spinal cord and via the
preganglionic sympathetic fibers, it will stimulate
the adrenal medulla to secrete amino-based
hormones, Catecholamines (Epinephrine and
norepinephrine)
- The effects of catecholamines, it will cause all the
system to go up except the GIT and GUT
- With the short-term stress you will be more
organized and focused but the problem is if you are
so stressed then you will become the opposite.
➢ LONG-TERM STRESS
- The hypothalamus will secrete the CRH, it will
stimulate the anterior pituitary gland to release the
ACTH, and this will in turn stimulate the adrenal
cortex to secrete the steroid hormones.
- The actions of the mineralocorticoids are it will
cause retention of sodium and water by kidneys
causing increased blood volume and blood
pressure.
- The glucocorticoids will have hyperglycemic effect.
- That’s why if you’re stressed you are susceptible to
diseases because of the immune suppressant
effect.
ADRENAL EXCESS
- Excessive adrenocortical excretion results in a
disorder called Cushing’s disease or Cushing’s
syndrome.
o They will have both have a rise of cortisol, the
only difference they have is their origin why their
cortisol is high.
bronchogenic
carcinoma is the
most common
type
• Prolonged
Steroid Therapy
ADRENOCORTICAL INSUFFICIENCY (ADDISON’S
DISEASE)
- Occurs when adrenal cortex function is inadequate
to meet the patient’s need for cortical hormones.
Causes:
✓ Autoimmune or idiopathic atrophy
✓ Surgical removal of both adrenal glands
✓ Infection of the adrenal glands (Tuberculosis and
histoplasmosis-most common)
✓ Inadequate secretion of ACTH from the pituitary
gland
✓ Therapeutic use of corticosteroids - the most
common cause of adrenocortical insufficiency
(Porth & Matfin, 2009).
- This happens because the hypothalamus will release
the CRH which will stimulate the anterior pituitary to
release ACTH, and this will stimulate the adrenal
cortex to release corticosteroids.
- When the body senses that there’s falling levels of
corticosteroids, negative feedback will be sent to the
brain.
- Then the hypothalamus will do the process again.
- If you use synthetic corticosteroids the body will
sense that you have enough corticosteroids and
won’t send negative feedback to your brain and
would therefore not do the HPA Axis.
- Because of this phenomenon, the adrenal cortex will
atrophy from lack of stimulation.

• May also result from the sudden cessation of

CUSHING'S DISEASE VS. CUSHING'S SYNDROME
Cushing's Disease Cushing's Syndrome exogenous adrenocortical hormonal therapy.
- Used exclusively to - Refers to the general
describe the state characterized
condition of by excessive levels of PREVENTION:
excessive cortisol cortisol in the blood.
arising from a - Elevated cortisol Patients should receive only short-term steroid therapy
pituitary tumor levels can occur for and must be weaned slowly so the adrenals have time to
secreting the reasons other than a recover and start producing hormones again.
hormone ACTH pituitary tumor,
(corticotrophin) including:
• Tumors of the
adrenal glands
producing
cortisol
• Ectopic
production of
ACTH by
malignancies;

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛

Adrenal Crisis
- Patients who have adrenal insufficiency may do quite
well until they experience a period of extreme stress,
such as a motor vehicle accident, a surgical
procedure, or a massive infection.
- Treated with massive infusion of replacement
steroids, constant monitoring, and life support
procedures.
Steroids to give if the patient will go into adrenal crisis:
ADRENOCORTICAL AGENTS
I. GLUCOCORTICOIDS/ADRENO CORTICOSTEROIDS
Functions:
1. Stimulate an increase in glucose levels for energy.
2. Increase the rate of protein break down and
decrease the rate of protein formation from amino
acids, another way of preserving energy.
Therapeutic Actions and Indications:
1. Enters target cells and bind to cytoplasmic
receptors, initiating many complex reactions that
are responsible for anti-inflammatory and
immunosuppressive effects.
2. Hydrocortisone, cortisone, and prednisone also
have some mineralocorticoid activity and affect
potassium, sodium, and water levels in the body.
• Hydrocortisone and cortisone are listed in
glucocorticoids and mineralocorticoid because these
drugs also exert some mineralocorticoid activity.
Uses:
✓ Addison’s disease, hormone replacement therapy,
cancer therapy
✓ To decrease inflammation—systemic lupus
erythematosus, rheumatoid arthritis, inflammatory
bowel disease, allergic conditions, asthma, chronic
obstructive pulmonary disease, respiratory distress
syndrome in infants.
✓ To suppress graft rejection.
Pharmacokinetics:
▪ Glucocorticoids are absorbed well from many sites.
They are metabolized by natural systems, mostly
within the liver, and are excreted in the urine.
▪ Known to cross the placenta and to enter
breastmilk; they should be used during pregnancy
and lactation only if the benefits to the mother
clearly outweigh the potential risks to the fetus or
neonate.
Contraindications and Cautions:
• Contraindicated in the presence of any known allergy
to any steroid preparations to avoid hypersensitivity
reactions; in the presence of an acute infection,
which could become serious or even fatal if the
immune and inflammatory responses are blocked.
• With lactation because the anti-inflammatory and
immunosuppressive actions could be passed to the
baby
• CAUTION should be used in diabetic patients because
the glucose-elevating effects disrupt glucose control,
with peptic ulcers because steroid use is associated
with ulcers, in pregnancy because of the potential for
adverse effects on the fetus.
Adverse Effects:
✓ Children are at risk for growth retardation associated
with suppression of the hypothalamic-pituitary
system.
✓ Local use: local inflammations and infections,
burning and tingling sensations.
Clinically Important Drug-Drug Interactions:
o Therapeutic and toxic effects increase if
corticosteroids are given with erythromycin,
ketoconazole, or troleandomycin.
𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 Betamethasone Oral, IM, IV, - Management of
o Serum levels and effectiveness may decrease if (Celestone intra-articular, allergic
corticosteroids are given with salicylates, Soluspan) topical intra-articular,
barbiturates, phenytoin, or rifampin. topical, and
Adult: inflammatory
Side Effects:
- 0.6-7.2 mg/d disorders
• Increased risk of new infection, mask development of PO, up to 9 mg/d
infection, and delayed wound healing. IV,
• Osteoporosis, glucose intolerance(hyperglycemia), -0.5-9.0 mg/d IM;
-apply topical
peptic ulcer, gastrointestinal (GI) bleeding
preparation
• Muscle wasting, fluid and electrolyte disturbance, sparingly
Cushing syndrome

Nursing Implications: Pediatric:

- Individualized
1. Monitor fluid balance and potassium and glucose dose based on
levels. severity
2. Warn patient to take as prescribed and not to and response and
discontinue therapy suddenly. monitor closely
3. Assess for underlying infection and decreased wound Cortisone Oral, IM - Replacement
healing. therapy in
4. Daily doses need to increase during stress. Adult adrenal
-25-300mg/d insufficiency,
5. Assess for Cushing symptoms.
po; 20-330mg IM treatment of
6. Check stools for occult blood.
allergic and
7. Advise patients to wear a Medic-Alert bracelet. Pediatric: inflammatory
8. Teach about alternate-day dosing if ordered and -Base disorders
taking medicine before 9 am dose on response,
monitor patient
(Focus with those rows highlighted in green)
closely
ADRENOCORTICAL AGENTS Budesonide Intranasal - Relief of
DRUG NAME DOSAGE/ROUTE USUAL (Rhinocort, symptoms of
(glucocorticoids) INDICATIONS Entocort EC) Adult and seasonal allergic
Beclomethasone Nasal spray, - Blocking pediatric rhinitis with few
(Beconase AQ) respiratory inflammation in (>6y): side effects,
inhalant the respiratory -256mcg/d maintenance
tract given as two treatment
Adult: sprays and PM of asthma, as an
- Two inhalations oral agent for the
(84-168 mcg) t.i.d. Pediatric (12 treatment of
to q.i.d. mo-8y): mild-to-
- For respiratory -0.5-1mg moderate
inhalant; one once daily in two - Crohn’s Disease
inhalation (42-84 divided doses Popular and
mcg) in each using common drug
nostril jet nebulizer
- b.i.d. to q.i.d for
nasal spray

Pediatric (6-12y):
- One or two
inhalations t.i.d. to
q.i.d. for
respiratory
inhalant

Pediatric (>12y):
- One inhalation in
each nostril b.i.d.
to q.i.d for nasal
spray

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
Dexamethasone Oral, IV, IM, - Management of 5-20mg/d PO
(generic) inhalation, allergic and based on response
intranasal, topical
ophthalmic, inflammatory Pediatric:
topical disorders, - 20-240
adrenal mg/d PO, IM, or
Adult and hypofunction subcutaneously;
pediatric: - 100 mg
- Individualized half-strength by
dose based on retention enema
response and for
severity: 21 d;
- 0.75-9mg/d PO, - one applicator
- 8-16 mg/d IM, full daily to b.i.d.
- 0.5-9mg/d IV, intrarectal;
- two to three - apply topical
inhalations per sparingly;
day for inhalation, - 5-20mg/d PO
- one to two based on response
sprays in each
nostril b.i.d. for
nasal spray, Methylprednisol Oral, IV, IM, - Treatment of
- 1 drop (gtt) t.i.d. one intra-articular allergic and
to q.i.d. for inflammatory
ophthalmic Adult: disorders
solutions, apply - 40-120mg/d PO
topical or IM,
preparations - 10-40mg IV
sparingly slowly

Flunisolide Inhalant, - Control of Pediatric:

intranasal Bronchial - Base dose on
Asthma, relief of severity and
Adult: symptoms of response
- 50-200 mcg seasonal and
intranasal b.i.d. allergic rhinitis
- 640 mcg/d via
inhalation
Prednisone Oral - Replacement
(Rayos) therapy for
Pediatric:
Adult: adrenal
- 2mg/d
- 0.1-0.15mg/kg/d insufficiency,
AeroBid,
PO treatment of
- 160 mcg
allergic and
b.i.d. Aerospan
Pediatric: inflammatory
Hydrocortisone Oral, IV, IM, - Replacement - base on disorders
(Cortef) topical, therapy, severity and
ophthalmic, rectal, treatment of response
intra-articular allergic and
Prednisolone Oral, IV, IM, Treatment of
inflammatory
(Omnipred, Pred ophthalmic, allergic and
Adult: disorders
Forte) intra-articular inflammatory
- 100-500 mg
disorders
IM or IV q2-6h,
Adult:
100 mg half-
- 5-60mg/d PO,
strength by
- 4-60mg IM or IV,
retention enema
- 1-2 gtt in
- for 21 d, one
affected eye
applicator
t.i.d to q.i.d.
full daily to b.i.d.
intrarectal;
Pediatric:
- apply topical
- Base dose on
sparingly;
severity

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 and response
Pharmacokinetics:
Triamcinolone Oral, IM, inhalant, - Treatment of
(Kenalog) intra-articular, allergic and ▪ Undergoes hepatic metabolism to inactive forms.
topical inflammatory ▪ Known to cross placenta and enter breast milk so it
disorders, should be avoided during pregnancy and lactation
Adult: management of because of the potential for adverse effects in the
- 4-60mg/d PO, asthma; fetus or baby.
- 2.5-6mg/d IM, - treatment of
- two inhalations adrenal Contraindications and Cautions:
t.i.d to insufficiency • Contraindicated in the presence of any known allergy
q.i.d. when combined
to the drug to avoid hyper-sensitivity reactions.
with
• With severe hypertension, heart failure, or cardiac
mineralocorticoid
disease because of the resultant increased blood
pressure, with lactation due to potential adverse
Pediatric: effects on the baby
- Individualize • Caution in pregnancy because of the potential for
dose based on adverse effects to the fetus.
severity • In the presence of any infection which will alter
and response adrenal response.
• With high sodium intake because severe
(Triesence) Pediatric (6-12y): - Treatment of hypernatremia could occur.
One to two Sympathetic
Inhalation 4 mg by ophthalmia, Adverse Effects:
ocular injection, 1- temporal
4 mg arteritis, uveitis, ✓ Commonly related to the increased fluid volume
intravitreally for visualization seen with sodium and water retention (e.g.
visualization during headache, edema, hypertension, heart failure,
vitrectomy arrhythmias, weakness) and possible hypokalemia.
✓ Skin rash to anaphylaxis

- In Glucocorticoids, most of the medications are used
as replacement therapy in adrenal insufficiency.
II. MINERALOCORTICOIDS
Therapeutic Actions and Indications:
1. Increase sodium reabsorption in renal tubules,
leading to sodium and water retention, and increase
potassium excretion.
Clinically Important Drug-Drug Interactions:
• Decreased effectiveness of salicylates, barbiturates,
hydantoins, rifampin, and anticholinesterases when
combined with mineralocorticoids.
• (These combinations should be avoided if possible,
but if they are necessary the patient should be
monitored closely and the dose increased as
needed.)

DRUG NAME ROUTE/DOSAGE USUAL

➢ Fludrocortisone - powerful mineral corticoid
INDICATIONS
preferred for replacement therapy over cortisone
Cortisone Oral: IM - Replacement
and hydrocortisone, used in combination with
(generic) therapy in
glucocorticoid. Adult: adrenal
➢ Hydrocortisone and cortisone also exert 25-300mg/d PO; insufficiency,
mineralocorticoid effects at high doses; however, this 20-330mg IM treatment of
effect is usually not enough to maintain electrolyte allergic and
balance in adrenal insufficiency. Pediatric: Base inflammatory
dose on disorders
- Indicated (in combination with glucocorticoid) for response,
replacement therapy in primary and secondary monitor patient
adrenal insufficiency. closely
- Also indicated for the treatment of salt-wasting Fludrocortisone Adult: 0.1-0.2 - Used for
adrenogenital syndrome when taken with (generic) md/d PO Replacement
therapy and
appropriate glucocorticoids.
treatment of
salt-losing
adreno genital

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 syndrome with
a
glucocorticoid,
not
recommended
or
children, being
tried for
treatment of
severe
orthostatic
hypotension Key Points:
because
sodium and o The mineralocorticoids stimulate retention of
water sodium and water and excretion of potassium. They
retention are used therapeutically in conjunction with
effects can glucocorticoids to treat adrenal insufficiency.
lead to o Patients receiving mineralocorticoids need to be
increased
evaluated for possible hypokalemia and its
blood pressure
associated cardiac effects and for fluid retention that
Hydrocortisone Oral, IV, IM, - Used for
could exacerbate heart failure and cause electrolyte
(Cortef) topical, replacement
ophthalmic, therapy, imbalances.
rectal, intra- treatment
articular of allergic and
inflammatory
Adult: disorders
20-240md/d PO, - Given to
100-500mg IM or patients with
IV q2-6h, 100mg adrenal
half-strength by Insufficiency
retention enema, when they are
one applicator in a severe
full rectal foam stress so that
QID to BID; apply the patient
topical will not
preparation go adrenal
sparingly crisis. For
example the OVERVIEW
Pediatric: Base patient is sick
dose on so the patient - The thyroid gland is a butterfly-shaped organ located
response and should be in the lower neck, anterior to the trachea.
severity, 20- given - Consists of two lateral lobes connected by an
240mg/d IM or additional isthmus. The gland is about 5 cmlongand3cm wide
subcutaneous, supplements and weighs about 30 g.
100mg of - The blood flow to the thyroid is very high (about 5
half-strength hydrocortisone
mL/min per gram of thyroid tissue), approximately
by retention to prevent
five times the blood flow to the liver. This reflects the
enema. One adrenal crisis
applicator-full high metabolic activity of the thyroid gland.
rectal foam
QID to BID: apply
Topical Hormones produced by the thyroid gland:
preparation
sparingly 1. Thyroxine (T4)
2. Triiodothyronine (T3)
3. Calcitonin.

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 • Thyroid hormone production and release are
THYROID HORMONES
regulated by anterior pituitary hormone called
thyroid stimulating hormone (TSH).
• The thyroid gland produces increased thyroid
hormones in response to increased levels of TSH.

- Thyroid Hormones (T4 and T3) – referred to

collectively as thyroid hormones.
- The primary function of thyroid hormone-control of
cellular metabolic activity.
- Iodine - essential to the thyroid gland for synthesis of
its hormones.
➢ The major use of iodine in the body is by the
thyroid, and the major derangement in iodine
deficiency is alteration of thyroid function.

Calcitonin

- Regulates serum calcium levels

Thyroid Dysfunction:

1. Hypothyroidism - Lack of sufficient levels of thyroid

hormones to maintain anormal metabolism. This
condition occurs in a number of pathophysiological
states:

✓ Absence of thyroid gland

✓ Lack of sufficient iodine in the diet to produce
the needed level of thyroid hormone.
✓ Lack of sufficient functioning thyroid tissue due
to tumor or autoimmune disorders
✓ Lack of TSH due to pituitary disease
✓ Lack of TRH related to a tumor or disorder of the
hypothalamus.

Control:

• The secretion of TSH is regulated by thyrotropin

releasing hormone (TRH).

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 thyroid gland) is an effect of hyperthyroidism
which occurs when the thyroid is overstimulated
by TSH.
➢ Hyperthyroidism may be treated by surgical
removal of the gland or portions of the gland,
treatment with radiation to destroy all parts or
all of the gland, or drug treatment to block the
production of thyroxine in the thyroid gland or
to destroy parts or all of the gland.

Pathophysiology (Hyperthyroidism)
o Over secretion of thyroid
hormones(hyperthyroidism) manifested by a greatly
increased metabolic rate.
o Many of the other characteristics of
hyperthyroidism result from the increased
response to circulating catecholamines
(epinephrine and norepinephrine).
o Over secretion of thyroid hormones is usually
associated with an enlarged thyroid gland known as
a goiter.
o Goiter also commonly occurs with iodine-deficiency.
Pathophysiology: (Hypothyroidism)

Cretinism- Inadequate secretion of thyroid hormone SIGNS AND SYMPTOMS OF THYROID DYSFUNCTION
during fetal and neonatal development Clinical Hypothyroidism Hyperthyroidism
Clinical manifestations: Effects
CNS Depressed: Stimulated:
✓ Stunted physical and mental growth because of Hypoactive Hyperactive reflexes,
general depression of metabolic activity. reflexes, lethargy, anxiety, nervousness,
sleepiness, slow insomnia, tremors,
(in adults) speech, emotional restlessness,
dullness increased basal
✓ lethargy
temperature
✓ slow mentation
CV System Depressed: Stimulated:
✓ generalized slowing of body functions
Bradycardia, Tachycardia,
hypotension, palpitations,
2. Hyperthyroidism- occurs when excessive amounts of anemia, oliguria, increased pulse
thyroid hormones are produced and released into decreased pressure, systolic
the circulation. sensitivity to hypertension,
➢ Grave’s disease is the most common cause of catecholamines increased
hyperthyroidism. Goiter (enlargement of the sensitivity
𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 to catecholamines (THYROID HORMONES)
Skin, hair, Skin is pale, Skin is flushed, warm,
nails coarse, dry, thin, moist, sweating, Therapeutic Actions and Indications:
thickened; puffy hair is - Thyroid replacement hormones increase the
eyes and fine and soft, nails metabolic rate of body tissues, increasing oxygen
eyelids; are soft and thin consumption, respiration, heart rate, growth and
Metabolic Decreased: Lower Increased:
maturation, and the metabolism of fats,
rate body temperature, Overactive cellular
carbohydrates, and protein.
intolerance to metabolism,
cold, decreased low-grade
appetite, higher fever, intolerance to
levels of fat and heat, increased
cholesterol, weight appetite with weight
gain, loss, muscle
hypercortisolemia wasting and
weakness, thyroid
myopathy
Generalized Accumulation of Localized with
Myxedema mucopolysacchari accumulation of
des in the heart, mucopolysaccharides
tongue, and vocal in eyeballs, ocular
chords, periorbital muscles; periorbital
edema, edema, lid lag,
cardiomyopathy, exophthalmos,
hoarseness and periorbital edema
thickened speech
Ovaries Decreased Altered tendency
function: toward
menorrhagia, oligomenorrhea,
habitual abortion, amenorrhea
sterility, decreased
sexual
function
Goiter Rare; simple Diffuse, highly
nontoxic type may vascular, very
occur frequent

o Signs and symptoms of Hypothyroidism are

attributed to hypometabolic rate and for the - All of these are given as replacement therapy in
Hyperthyroidism are hypermetabolic rate. hypothyroidism.
- What usually comes up in local and foreign exam is
THYROID AGENTS levothyroxine (Synthroid).
1. Thyroid Hormones - It must be given on an empty stomach, at least 30
- Used as replacement therapy in minutes before taking breakfast. This medication
hypothyroidism. should not be chewed or crushed. The medicine
2. Antithyroid Agents must be taken with a full glass of water.
- Treatment of Hyperthyroidism. - This medication must not be used during acute
a) Thioamides thyrotoxicosis unless they are used in conjunction
b) Iodine Solutions with antithyroid drugs.

➢ Thyrotoxicosis- this is the name given to the clinical

Pharmacologic Therapy for Hypothyroidism: effects experienced with the patient due to an
excessive level of thyroid hormones in the
bloodstream.

Pharmacokinetics:

• Thyroid hormones are well absorbed from the GI

tract and bound to serum proteins.
𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
• Thyroid hormones do not cross the placenta and
seems to have no effect on the fetus. Thyroid
replacement therapy should not be discontinued
during therapy, and the need often becomes
apparent or increases during pregnancy.
• There is an increase in the metabolism during
pregnancy. The need for thyroid hormones becomes
apparent or it increases during pregnancy. The
woman should go back to the doctor so that the
hormones level can be checked, and necessary
adjustments can be done based on the patient’s signs
and symptoms or the laboratory results.
• Enters breast milk in small amounts. Caution should
be used during lactation.
Contraindications and Cautions:
• Should not be used with any known allergy t the
drugs to prevent hypersensitivity reactions.
• Should not be used during acute thyrotoxicosis
(unless used in conjunction with anti-thyroid drugs)
• During acute myocardial infarction (unless
complicated by hypothyroidism)
• Caution should be used during lactation, with hypo-
adrenal conditions.
• Liothyronine and liotrix - have a greater incidence of
cardiac side effects and not recommended for use in
patients with potential cardiac problems or patients
prone to anxiety reactions.
Adverse Effects:
✓ Skin reactions and loss of hair (during first few
months of treatment in children)
✓ Arrhythmias, hypertension (cardiac stimulation)
✓ Anxiety, sleeplessness, headache (CNS)
✓ Difficulty of swallowing with esophageal atresia
(patient must be instructed to take the drug with a
full glass of water to alleviate this effect)
Clinically Important Drug-Drug Interactions
• Decreased drug absorption of thyroid hormones if
they are taken concurrently with cholestyramine
(should be taken 2 hours apart)
• Effectiveness of oral anticoagulants is increased if
they are combined with thyroid hormone (bleeding
time should be checked periodically)
• Decreased effectiveness of digitalis glycosides can
occur when these drugs are combined. (digitalis
levels should be monitored, and increased dose may
be required)
• Theophylline clearance is decreased in hypothyroid
states. As the patient approaches normal thyroid
function the theophylline dose may need to be
adjusted frequently
Pharmacologic Therapy for Hyperthyroidism:
➢ Antithyroid Agents- Drugs used to block the
production of thyroid hormone and to treat
hyperthyroidism. Two forms of pharmacotherapy for
treating hyperthyroidism and controlling excessive
thyroid activity:
a. Thioamides
b. Iodine Solutions
Therapeutic Actions and Indications
1. Thioamides
o Indicated for the treatment of hyperthyroidism
o Lower thyroid hormone levels by preventing the
formation of thyroid hormone in the thyroid cells,
which lowers the serum levels of thyroid hormone.
o They also partially inhibit the conversion of T4 and T3
at the cellular level.
o Thioamides include propylthiouracil (PTU) and
methimazole (Tapazole)
o Both of these drugs can be fatal to a developing fetus
but if the drug is really needed, the preferred drug
during pregnancy is PTU.
o Propylthiouracil (PTU) - preferred drug during
pregnancy.
o Once the thyro toxicity is under control, the dose is
decreased to prevent fetal hypothyroidism.
Antithyroid medications are contraindicated in late
pregnancy because they may produce goiter and
cretinism in the fetus (Cooper, 2005).
o Methimazole (Tapazole)
𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 seen in 10 to 15 days.
2. Iodine Solutions - The effects are
o Low doses of iodine are needed in the body for the short-lived and may
formation of thyroid hormone. High doses block even precipitate further
thyroid enlargement
thyroid function.
and dysfunction. For
o Iodine solutions cause the thyroid cells to become
this reason, iodides are
oversaturated with iodine and stop producing not often used and are
thyroid hormone. In some cases the thyroid cells are used in cases of
actually destroyed. radiation emergencies
o Radioactive iodine (sodiumiodideI131) is taken up
into the thyroid cells which are then destroyed by
beta-radiation given offby the radioactive iodine. Contraindications and Cautions
o The use of sodium iodide is reserved for those • Contraindicated in the presence of any known allergy
patients who are not candidates for surgery, women to antithyroid drugs to prevent hypersensitivity
who cannot become pregnant, and elderly patients reactions.
with such severe, complicating conditions that • During pregnancy because of the adverse effects on
immediate thyroid destruction is needed. Iodine the fetus and the development of cretinism.
solutions include:
• If antithyroid is essential and the mother has been
1. Strong iodine solution (a.k.a. Lugol’s iodine /
informed about the risk of cretinism in the infant,
aqueous iodine, potassium triiodide)
PTU is the drug of choice, but caution should still be
2. Potassium Iodide
used.
Brand names: SSKI, Iosat, Thyrosafe,
• PTU has been associated with severe liver toxicity
Thyroshield
and is no longer recommended for use in children
3. Sodium Iodide I131
because they are more susceptible to the toxic
effects in the liver.
• Use of strong iodine products is contraindicated with
pulmonary edema and pulmonary tuberculosis.

Adverse Effects:

Thioamides

✓ Thyroid suppression: drowsiness, lethargy,

bradycardia, nausea, skin rash, and so on
✓ PTU – associated with nausea, vomiting, GI
complaints, and severe liver toxicity
✓ Methimazole – (drug of choice for patients who are
unable to tolerate PTU or patients with known liver
dysfunction) GI complaints, bone marrow
suppression, so the patient using this drug must have
frequent blood tests to monitor this effect.
You can check for bone marrow suppression by
reviewing the results of the CBC with differential
Pharmacokinetics: Iodine Solutions
THIOMIDES IODINE SOLUTIONS ✓ Common Adverse effect is hypothyroidism; the
- Well absorbed from the - Rapidly absorbed from patient will need to be started on replacement
GI tract and are then the GI tract and widely thyroid hormone to maintain homeostasis.
concentrated in the distributed throughout
✓ Iodism (metallic taste and burning in the mouth, sore
thyroid gland. the body fluids.
teeth and gums, diarrhea, cold symptoms, and
- Onset and duration of - Excretion occurs
PTU varies with each through stomach upset)
patient the urine. ✓ Staining of teeth (Give iodine solution through a
- Methimazole onset of - Potassium iodide and straw to decrease staining of teeth), skin rash and
action: 30-40 minutes, sodium iodide are development of goiter.
peak: 60 minutes taken orally and have a
- Crosses the placenta rapid onset of action, - Sodium iodide (I₁₃₁) is usually reserved for use in
and is found in high which effects within 24 patients who are older than 30 yrs of age because of
ratio in the breast milk hours and peak effects the adverse effects associated with radioactivity.
𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
- It is recommended for a woman to wait for a year
after they were treated with radioactive iodine
before they try to conceive. And woman who are
breastfeeding should not use radioactive iodine or
they can just use formula feeding for their baby.

(RADIOACTIVE IODINE THERAPY)

Nursing Considerations:

▪ Use of an ablative dose of radioactive iodine initially

causes an acute release of thyroid hormone from the
thyroid gland and may cause increased symptoms.
The patient must be observed for signs of thyroid
storm, a life-threatening condition manifested by:
• Cardiac dysrhythmias
• Fever
• Neurologic impairment

▪ Thyroid Storm- also known as thyrotoxic crisis an

acute state of hyperthyroidism where all the signs
and symptoms are exaggerated. It can be life-
threatening but with quick response can be
controlled and managed.
▪ Propranolol (Inderal) is useful in controlling these
symptoms.
▪ The patient is monitored closely until the euthyroid
state is reached. In 3 to 4 weeks, symptoms of
hyperthyroidism subside.
▪ Radioactive iodine is contraindicated during
pregnancy (because it crosses the placenta) and
while breast-feeding (because it is secreted in breast
milk) to prevent hypothyroidism in the fetus (Cooper,
Doherty, Haugen, et al., 2006).
▪ Pregnancy should be postponed for at least 6 months
after treatment.

Clinically Important Drug-Drug Interactions:

Thioamides

• Increased risk of bleeding when PTU is administered

with anticoagulants.
• Changes in serum levels of theophylline, metoprolol,
propranolol, and digitalis may lead to changes in the
effects of the PTU as the patient moves from
hyperthyroid to the euthyroid state.

Iodine Solutions

• Drugs that have a small margin of safety that could

be altered by the change in thyroid function should
be monitored closely. These drugs include;
anticoagulants, theophylline, digoxin, metoprolol
and propranolol.

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
Part 5B: Parathyroid Agents

Anatomic and Physiologic Overview:

- The parathyroid glands are four very small groups

of glandular tissue located on the back of the
thyroid gland.
- Produce PTH, an important regulator of serum
calcium levels.

Structure and Function: PARATHYROID HORMONE

- Some actions of PTH are increased by the presence
➢ The parafollicular cells of the thyroid gland produce
of vitamin D.
the hormone calcitonin.
- Parathormone also tends to lower the blood
➢ Calcitonin responds to high calcium levels to cause
phosphorus level.
lower serum calcium levels and acts to balance the
- The serum level of ionized calcium regulates the
effects of PTH, which works to elevate calcium levels.
output of parathormone.

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛

PARATHYROID DYSFUNCTION AND RELATED
DISORDERS
- Parathyroid dysfunction involves either absence of
PTH (hypoparathyroidism) or overproduction of PTH
(hyperparathyroidism)
➢ Hypoparathyroidism- The absence of PTH results in
a low calcium level (hypocalcemia) and a relatively
rare condition called hypoparathyroidism.
➢ Hyperparathyroidism- The excessive production of
PTH leads to an elevated calcium level
(hypercalcemia) and a condition called Hyperparathy
PARATHYROID AGENTS
ANTIHYPOCALCEMIC AGENTS
- (for the treatment of hypoparathyroidism):
1. Vitamin D- Primary treatment for
hypoparathyroidism + dietary supplements of
calcium if necessary
2. Calcitriol (Rocaltrol) - most commonly used form of
vitamin D.
Role of Vitamin D in Calcium Homeostasis
The actions of Vitamin D are as follows:
1) Enhances calcium absorption from the intestine
2) Facilitates calcium absorption in the kidney
3) Increases bone calcification and mineralization
4) In excess, mobilizes bone calcium and phosphate
- In hypoparathyroidism there is hypocalcemia, if you give
vitamin D it will increase the chance of calcium
absorption
(Parathyroid Hormones)
Two PTH forms available for therapeutic use:
1. Teriparatide (Forteo)- approved to increase bone
mass in postmenopausal women and men with
primary or hypogonadal osteoporosis who are at
high risk for fracture.
2. Parathyroid Hormone (Natpara) – approved to
help control calcium levels in patients with
hypoparathyroidism.
THERAPEUTIC ACTIONS AND INDICATIONS
Vitamin D compounds:
• Act to regulate the absorption of calcium and
phosphate from the small intestine, mineral
resorption in bone, and reabsorption of phosphate
from the renal tubules.
• Functions as a hormone by working along with
calcitonin and PTH.
• Increases serum calcium and decreases serum
phosphorus.
• Indicated for the management of hypocalcemia in
patients undergoing chronic renal dialysis and for
the treatment of hypoparathyroidism□ Why
patients who are having their dialysis needs
Vitamin D? Calcitriol is used in patients with kidney
disease because patients with this disease can’t
make enough of the active form of Vitamin D. this
medication is used to prevent as well as to treat
certain types of of calcium and phosphorus or
parathyroid problems that can happen with long-
term kidney disease or with long-term kidney
dialysis or hypoparathyroidism. Calcitriol is not
given alone but usually accompanied with specific
diet recommendations and sometimes other
medications.
Teriparatide
• Used for the treatment of postmenopausal or
hypogonadal osteoporosis with sustained
systemic glucocorticoid therapy, which could
lead to fractures
Parathyroid hormone is only approved for maintenance
of calcium levels in patients with hypoparathyroidism.
Pharmacokinetics:
Calcitriol
• Well absorbed from the GI tract and widely
distributed throughout the body. It is stored in the
liver, fat muscle, skin, and bones.
• Half life: approx. 5 to 8 hours
• Duration of action: 3-5 days
𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛

Parathyroid Hormone
• Given as a daily subcutaneous injection, reaches
peak levels in 5 to 30 minutes
• Half-life: 3 hours
• Metabolized in the liver and excreted through the
kidneys.
Contraindications and Cautions
• Should be used during pregnancy if the benefit to the
mother clearly outweighs the potential for adverse
effects on the fetus.
• Calcitriol has been associated with hypercalcemia (in
the baby) when used by nursing mothers, therefore
another method of feeding the baby should be used
if these drugs are used during lactation.
• Caution should be used with a history of renal stones
or during lactation when high calcium levels could
cause problems.
• Limited Use of teriparatide and parathyroid hormone
in postmenopausal women who have osteoporosis
because of their association with osteosarcoma.
These patients should also take supplemental
calcium and Vitamin D3, increase weight-bearing
exercise, and decrease risk factors such as smoking
and alcohol consumption.
- Why does the patient need to perform weight -
bearing exercises? Inactivity can cause bone loss.
Active people will tend to keep calcium in their bones
while sedentary people will lose calcium. Sedentary
people’s bones give up their calcium stores that’s
why we encourage our patient to do weight-bearing
exercise.
Adverse Effects:
✓ GI: Metallic taste, nausea, vomiting, dry mouth,
constipation, anorexia
✓ CNS: weakness, headache, somnolence, irritability
✓ Patients with liver or renal dysfunction may have
increased level of the drugs and/or toxic effects
✓ Severe hypocalcemia and hyper calcemia with the
use of parathyroid hormone
ANTIHYPERCALCEMIC AGENTS
- Drugs used to treat PTH excess or hypercalcemia:
- These drugs act on the serum levels of calcium and
do not suppress the parathyroid gland or PTH.
1. Biphosphonates
2. Calcitonin Salmon
Therapeutic Actions and Indications:
Biphosphonates – acts to slowor block bone resorption
(common suffix - dronate)
o etidronate (Didronel)
o ibandronate (Boniva)
o pamidronate (Aredia)
o risedronate (Actonel)
o alendronate (Fosamax)
o zoledranic acid (Zometa)
- Used in the treatment of Paget’s disease, post
menausal osteoporosis in women, and alendronate
is also used to treat osteoporosis in men.
- Paget’s disease- chronic autoimmune inflammatory
disease that leads to an increasein bone resorption.
- Zoledronic Acid is also used to prevent new fractures
in patients with low-trauma hip fractures and to treat
patients with multiple myeloma or documented
bone metastases from solid tumors.
Calcitonins
- CalcitonINs are hormones secreted by the thyroid
gland to balance the effects of PTH.
- Currently, the only calcitonin readily available is
calcitonin salmon.
- Brand names: Calcimar, Fortical, Micalcin
- Inhibits bone resorption, lowers serum calcium levels
in children and patients with Paget’s disease and
increases the excretion of phosphate, calcium, and
sodium from the kidney.
Pharmacokinetics:
Biphosphonates
• Well absorbed from the small intestine and do not
undergo metabolism, excreted relatively unchanged
in the urine, the onset of action is slow and duration
of action is days to weeks.
• Patients with renal dysfunction may experience toxic
levels of the drug and should be evaluated for a dose
reduction.
Calcitonins
• Metabolized in the body tissues to inactive
fragments, which are excreted by the kidneys.
• Crosses the placenta and have been associated with
adverse effects on the fetus in animal studies
Contraindications and Cautions
Biphosphonates
• Contraindicated for the treatment of osteoporosis in
patients with hypocalcemia.
• Fetal toxicity have been associated with these drugs
in animal trials and should not be used during
pregnancy unless the benefit to the mother clearly
outweighs the potential risk to the fetus or neonate
𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 • GI distress if bisphosphonates are combined with
• Alendronate should not be used by nursing mothers
aspirin, this combination should be avoided as
because of potential risk for adverse effects on the
possible.
baby
• Caution should be used in patients with renal Calcitonins
dysfunction which could interfere with excretion of
• There have been no clinically important drug-drug
the drug, or with upper GI disease which could be
interactions reported with the use of calcitonin.
aggravated by the drug

alendronate, ibandronate, risedronate

DRUG USUAL DOSAGE USUAL INDICATIONS
➢ must be taken on arising in the morning, with a NAME
full glass of water, fully 30 minutes before any ANTIHYPOCALCEMIC AGENTS
other food or beverage and then remain upright Calcitriol 0.5-2 mcg/d PO - Management of
for at least 30 minutes to facilitate the delivery of (Rocaltrol) in the morning hypocalcemia and
drug to the stomach. reduction of
➢ should not be given to anyone who is unable to parathormone
levels
remain upright for 30 minutes after taking the
Parathyroi 50 mcg/day Maintenance of
drug because serious esophageal erosion can
d subcutaneously serum
occur.
Hormone , adjust dose to calcium levels in
- Zoledronic acid- Should be used cautiously in aspirin- (Naptara) maintain serum adults
sensitive asthmatic patients. calcium levels with
in the lower hypoparathyroidism
➢ may be given as an IV infusion onceevery2 years range of normal
for osteoporosis. Teriparatid 20 mg Management of
e subcutaneously osteoporosis in
Calcitonins (Forteo) daily postmenopausal
women and men
• Calcitonin salmon should not be used when a patient
with primary
has a known allergy to salmon or fish products.
hypogonadal
• Should be used in pregnancy only if the benefit to the osteoporosis who
mother clearly outweighs the potential risk to the do not respond to
fetus. standard therapy;
treatment of
patients
Adverse Effects:
on sustained
Biphosphonates systemic
glucocorticoid
✓ Headache, nausea, diarrhea therapy
✓ Increase in bone pain in patients with paget’s at high risk for
disease fractures.
✓ Alendronate – esophageal erosion ANTIHYPERCALCEMIC AGENTS
✓ Femoral shaft fractures in long term use of (BIPHOSPHONATES)
bisphosphonates (over 5 years) Alendronate 10 mg/d PO; for (Fosamax)
(Fosamax) males and for 10 mg/d PO; for
Calcitonins postmenopausal males and for
osteopororsis, postmenopausal
✓ Flushing of the face and hands, skin rash, nausea
70 mg PO osteoporosis, 70
and vomiting, urinary frequency, and local every week or mg PO
inflammation at the site of injection 10 mg/d PO for every week or
treatment, 35 10 mg/d PO for
mg PO every treatment, 35
Clinically Important Drug-Drug Interactions:
week or 5 mg/d mg PO every
Biphosphonates PO for week or 5 mg/d
prevention PO for
• Oral absorption of bisphosphonates is decreased if prevention
they are taken concurrently with antacids, calcium Treatment for
products, iron, or multiple vitamins. If these drugs Paget’s
need to be taken, they should be separated by at disease,
least 30 minutes. postmenopausal
•
𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
 lesions in certain
osteoporosis cancer patients,
treatment
and prevention, prevention of
treatment of new fractures in
glucocorticoid- patients with
induced low-trauma hip
osteoporosis, fractures
osteoporosis in
men CALCITONINS
Etidronate 5-10 mg/kg/d Treatment for
Calcitonin Paget’s Treatment for
(Didronel) POfor 6 mo for Paget’s
Salmon disease: Paget’s disease,
Paget’s disease,
(Miacalcin) 50-100 IU/d postmenopaus
disease; 20 postmenopausal
subcutaneous al osteoporosis
mg/kg/d PO for osteoporosis,
or IM in conjunction
2 wk, then 10 heterotopic
Postmenopausa with vitamin D
mg/kg/d PO for ossification
l osteoporosis: and calcium
10 wk for
100 IU/d supplements;
heterotopic
Treatment for emergency
ossification
Paget’s disease, treatment of
Ibandronate 2.5 mg/d PO or Treatment and postmenopausa hypercalcemia
(Boniva) 150 mg PO prevention of
l osteoporosis in
once per month osteoporosis in
conjunction
on the same postmenopausal
with vitamin D
day each women
and calcium
month; 3 mg IV
supplements;
given over
emergency
15-30 s once
treatment
every 3 mo subcutaneous
Pamidronate 30-90 mg IV as Treatment for or IM with
(Aredia) an infusion Paget’s disease, calcium and
postmenopausal vitamin D
osteoporosis in Hypercalcemia:
women, 4-8 IU/kg
hypercalcemia subcutaneous
of or IM q12h
malignancy,
(Fortical) 200 IU/d Treatment of
osteolytic bone
intranasally; Postmenopausa
lesions in cancer alternate l osteoporosis
patients.
nostrils daily in
Risedronate 30 mg/d PO for Treatment of conjunction
(Actonel) 2 mo; reduce symptomatic with
dose in renal Paget’s disease calcium
dysfunction; 5 in patients who supplements
mg/d PO for are at risk for and vitamin D
osteoporosis or complications,
35 mg PO once treatment and
per wk or 150 prevention of
mg PO once osteoporosis
per mo; 35 mg (postmenopausal
PO once per , glucocorticoid
wk for men to related and in
increase bone men)
mass.
Zoledronic 4 mg IV as a Treatment for
Acid single infusion Paget’s disease,
(Zometa, over not less postmenopausal
Reclast) than 15 min osteoporosis in
(given once women,
every 2 y for hypercalcemia of
postmenopausal malignancy,
osteoporosis) osteolytic bone

𝑚𝑘𝑐𝑐, 𝑟𝑛, 𝑚𝑛
Pharmacology
Ms. Palmyra Mataberde | Endterm

Antidiabetic Agents
Corticosteroids
Topic Outline: Increases glucose output and decreases insulin sensitivity.
I. Overview
II. Insulin
III. Oral Antidiabetic drugs Growth Hormone
IV. Glucose elevating drugs causes decreased insulin sensitivity; increases protein
building; increases FFA formation
Overview
Pancreas
Glucagon and Insulin Feedback Loop
The pancreas has the dual function of secreting hormones into
1. Decreased blood sugar -> pancreas release glucagon
blood (endocrine) and secreting enzymes through ducts
-> causes the liver to release glycogen which turns
(exocrine).
into glucose to increase the low blood sugar level
2. Increased blood sugar -> pancreas releases insulin ->
Only about 5% of the pancreas comprises endocrine cells.
causes glucose to enter into the cells to be used or be
These cells are clustered in groups within the pancreas and
saved as glycogen for later (stored mainly in the liver)
look like little islands of cells when examined under a
microscope.
Major classifications of diabetes:
1. Type 1
These groups of pancreatic endocrine cells are known as
2. Type 2
pancreatic islets or more specifically, islets of Langerhans
3. Gestational diabetes
4. Diabetes Mellitus Associated with other conditions or
Alpha Cells
syndromes (ADA, 2009a)
- release glucagon in response to low blood glucose
levels
Type 1 diabetes
Characterized by destruction of beta cells
Beta cells
- release insulin in response to high blood glucose
Risk factors: Combined genetic, immunologic, and possibly
levels and when stimulated by incretins
environmental (eg, viral) factors are thought to contribute to
beta cell destruction.
D cells
- produce somatostatin (growth hormone-inhibiting
Type 2 diabetes
factor) in response to very low blood glucose levels;
occurs more commonly among people who are older than 30
years of age and obese.
Somatostatin
When levels of other pancreatic hormones, such as insulin and
Risk factors: Lifestyle- being obese, sedentary, poor diet (e.g.
glucagon, get too high, somato______ is secreted to maintain
sugary drinks), stress AND genetics
a balance of glucose.
Two main problems related to insulin in type 2 diabetes:
Other Factors Affecting Glucose Control
1. Insulin resistance
Adipocytes or fat cells secretes adiponectin
- refers to a decreased tissue sensitivity to insulin.
This hormone acts to regulate insulin sensitivity, it
2. Impaired Insulin Secretion
decreases the release of glucose from the liver, and protects
the blood vessels from inflammatory changes.
Signs and symptoms of Hypoglycemia and Hyperglycemia

Endocannabinoid system Clinical Effects Hypoglycemia Hyperglycemia

Increases food intake by blocking satiety signals; decreases
adiponectin release; decreases insulin sensitivity; increases fat CNS Headache, Decreased level of
blurred vision, consciousness,
synthesis; alters gastric emptying to promote greater nutrient
diplopia, sluggishness
absorption. drowsiness progressing to
progressing to coma, hypoactive
The SNS through the effects of Catecholamines coma, ataxia, reflexes
Decreases insulin release; increases glucose output from liver hyperactive
and muscles; increases breakdown of fat to free fatty acids reflexes
(FFAs)

VNV| 1
 Neuromuscular Paresthesias, Weakness, lethargy
weakness, 3 Characteristics of Insulin
muscle spasms, • Onset - refers to the length of time before insulin reaches the
twitching bloodstream and begins lowering blood sugar.
progressing to • Peak time - the time during which insulin is at maximum
seizures strength in terms of lowering blood sugar.
• Duration - how long insulin continues to lower blood glucose.
CV Tachycardia, Tachycardia,
palpitations, hypotension
normal to high
blood pressure

Respiratory Rapid, shallow Rapid, deep

respirations respirations
(kussmaul);
acetone- like or
fruity breath

GI Hunger, nausea Nausea, vomiting,

thirst

Other Diaphoresis, cool Dry, warm, flushed

and clammy skin, skin; soft eyeballs Parts of an insulin pen
normal eyeballs

Laboratory Urine glucose Urine glucose

Tests negative, blood strongly positive;
glucose low urine ketone levels
positive; blood
glucose levels high

Onset Sudden; patient Gradual; patient is

appears anxious, slow and sluggish;
drunk; associated associated with
with overdose of lack of insulin,
insulin, missing a increased stress
meal, increased
stress.

Insulin
• Insulin is the only Parenteral Antidiabetic agent available for
exogenous replacement of low levels of insulin. Mixing Insulin
• It is used to treat type 1 and type 2 diabetes in adults who
have no response to diet, exercise, and other agents.

Therapeutic Actions and Indications

✓ Promotes the storage of the body’s fuels
✓ Facilitates the transport of various metabolites and ions
across cell membranes, and stimulates the synthesis of
glycogen from glucose, fats from lipids, and of proteins from
amino acids.
✓ Insulin does these things by reacting with specific receptor
sites on the cell

Pharmacokinetics
✓ Insulin is available in various preparations with a range of
peaks and duration of action.
✓ The types of insulin used are determined by the anticipated
eating and exercise activities of any particular patient.
✓ Insulin glargine (Lantus, Toujeo) and insulin Detemir
(Levemir) cannot be mixed in solution with any other drug,
including other insulins.
Inject air into clear > inject air into cloudy > withdraw from
cloudy > withdraw from clear
Contraindications and Cautions
• No contraindications other than episodes of hypoglycemia
(check blood sugar levels before giving insulin)
VNV | 2
• Insulin does not cross the placenta;therefore, it is the drug
of choice for managing diabetes during pregnancy.
• Insulin does not enter breast milk, but it is destroyed in the
GI tract and does not affect the nursing infant.
(Care should be taken during pregnancy and lactation to
monitor glucose levels closely and adjust the insulin dose
accordingly.)
• Patients using inhaled insulin are at risk for impairment
of respiratory function; this route is contraindicated in people
with asthma or COPD and in people with lung cancer or history
of lung cancer.
Adverse Effects
• Most common: hypoglycemia and ketoacidosis (can be
controlled with proper dose adjustments)
• Local reactions at injection sites (can be lessened by rotation
of injection site)
General Rules:
•Never use the same injection spot more than once
consecutively.
•Place the injections 1-2 centimeters apart.
•Never inject close to the navel.
Clinically important drug-drug interactions
❑ Caution should be used when giving a patient stabilized on
insulin any drug that decreases glucose levels (e.g.
monoamine oxidase inhibitors, beta-blockers, salicylates).
✓ Doss adjustments are needed when any of these drugs is
added or removed.
❑ Care should be taken when combining insulin with any
beta-blocker.
• The blocking of the SNS also blocks many of the signs and
symptoms of hypoglycemia, hindering the patient’s ability to
recognize problems.
Nursing Implications
✓ Draw up clear (e.g. regular, lispro, aspart, and
glulisine—short acting) before the cloudy (e.g. NPH) insulin to
prevent contaminating a short- acting insulin with a long acting
insulin.
✓ Inject subcutaneously; aspiration is not necessary.
✓ Avoid massaging the site after injection.
✓ Rotate sites within anatomic area; the abdomen is preferred
for more rapid, even absorption.
✓ Only NPH (Humulin) can be mixed with short-acting
insulins.
✓ Only the short-acting insulins may be administered
intravenously (IV).
✓ Hypoglycemia is the primary drawback in maintaining tight
control of glucose level.
✓ Store unopened vials of insulin in the refrigerator; vial
currently in use should be stored at room temperature for 1
month.
✓ Prefilled syringes should be stored vertically with the needle
pointing up to avoid clogging the needle; gently agitate the
syringe to resuspend the insulin before use. May be stored in
the refrigerator for at least 1 week, perhaps 2 weeks.
Oral antidiabetic drugs and non-insulin injectable agents
Oral antidiabetic Oral:
1. sulfonylureas
2. biguanides
3. meglitinides (glinides)
4. thiazolidinediones (glitazones)
5. alpha-glucosidase inhibitors
6. dipeptidyl peptidase-4 (DPP-4) inhibitors (gliptins)
7. sodium-glucose cotransporter 2 (SGLT-2) inhibitors.
* Used for type 2 diabetes
Sulfonylureas
Therapeutic actions and indications
• Indicated as an adjunct to diet and exercise to lower blood
glucose levels in type 2 diabetes mellitus.
• Stimulate insulin release from the beta cells in the
pancreas. Improves insulin binding to the insulin receptors and
may actually increase the number of insulin receptors.
• They have the off-label use of being an adjunct to insulin
and metformin and improve glucose control in type 2
diabetes.
Pharmacokinetics
✓ Sulfonylureas are rapidly absorbed from the GI tract and
undergo hepatic metabolism. They are excreted in the urine.
✓ Peak effects and duration of effects differ
Contraindications and cautions
✓ Contraindicated in the presence of known allergy to any
sulfonylureas to avoid hypersensitivity reactions
✓ In diabetes complicated by fever, severe infection, severe
trauma, major surgery diabetic Ketoacidosis, severe renal or
hepatic disease, pregnancy or lactation which require tighter
control of glucose levels using insulin.
✓ Contraindicated in Type 1 diabetes who do not have
functioning beta cells and would have no benefit from the
drug
✓ Not for use during pregnancy and lactation
- Insulin should be used if an antidiabetic agent is
needed during pregnancy.
Adverse Effects
• Most common: hypoglycemia
• GI distress: including nausea, vomiting, epigastric discomfort,
heartburn, and anorexia
• Allergic Skin Reactions
• Increased Risk Of Cardiovascular Disease
Clinically important drug-drug interactions
• Caution with beta blockers which may mask the signs of
hypoglycemia,
• Caution with alcohol which can lead to altered glucose levels
when combined with sulfonylureas
• Any drug that acidifies the urine because the excretion of the
sulfonylurea may be decreased.
VNV | 3
 Adverse Effects: vascular effects including hypotension,
First generation Sulfonylureas headache,cerebral ischemia, weakness, heart failure, and
1. chlorpropamide(Diabinese) arrhythmias (diazoxide relaxes arteriolar smooth muscle)
2. tolazamide(generic
3. tolbutamide(generic) Clinically Important drug-drug interactions:
*-mide Diazoxide in combination with thiazide diuretics causes an
increased risk of toxicity because diazoxide is structurally
Second generation Sulfonylureas similar to these diuretics
1. glimepiride(Amaryl)
2. glipizide(Glucotrol) Glucagon
3. glyburide(DiaBeta,Micronase,Glynase PresTab) Pharmacokinetics: Is given parenterally only and is the
*-ide preferred agent for emergency situations, rapidly absorbed
throughout the body and excreted in urine.

Contraindications and Cautions Use of glucagon during

pregnancy should be reserved for those situations in which the
benefits to the mother outweigh any potential risks to the fetus.
Caution should be used during lactation because the drugs
may cause hyperglycemic effects in the baby.

Adverse Effects:
GI upset, nausea, vomiting

Clinically Important drug-drug interactions:

Increased anticoagulation effects when glucagon is combined
Non-insulin injectable agents: with oral anticoagulants.
1. Human Amylin – used both in DM type 1 and type 2
2. Incretin Mimetics - Used to treat type 2 diabetes
3. GLP-1 Agonists - Used to treat type 2 diabetes Therapeutic Actions and Recommendations
Increases the blood glucose level by decreasing insulin
Glucose-Elevating Agents release and accelerating the breakdown of glycogen in the liver
Glucose-elevating agents as the name implies, raise the blood to release glucose.
level of glucose when severe hypoglycemia occurs (<40mg/dl).
Drug Acting on the Female Reproductive
Drug Name Dosage/Route Usual Indications System
Diazoxide Adult and pediatric: Oral management Topic Outline:
(Proglycem, 3-8 mg/kg/d PO in two of hypoglycemia; I. Sex Hormones
Hyperstat) to three divided doses intravenous use II. Estrogen Receptor Modulators
q8-12h for management III. Fertility Drugs
of severe IV. Uterine Motility Drugs
Glucagon Adult and pediatric hypertension to V. Abortifacients
(GlucaGen) (>20kg): 0.5-1mg counteract severe Glossary of Terms
subcutaneous, IM or hypoglycemic
Abortifacients
IV reactions)
Pediatric(<20kg):0.5 - Drugs used to stimulate uterine contractions and
mg, subcutaneous, IM promote evacuation of the uterus to cause abortion or
or IV to empty the uterus after fetal death
Fertility Drugs
- Drugs used to stimulate ovulation and pregnancy in
Diazoxide
women with functioning ovaries who are having
Pharmacokinetics: Given Orally, rapidly absorbed throughout
trouble conceiving
the body and excreted in urine.
Oxytocics
- Drugs that act like the hypothalamic hormone
Contraindications and Cautions: associated with adverse
oxytocin; this stimulates uterine contraction and
effects on the fetus including pulmonary hypertension and
contraction of the lacteal glands in the breast
should not be used during pregnancy
promoting milk ejection
Progestins

VNV | 4
 - The endogenous female hormone progesterone and
its various derivatives, important in maintaining a
pregnancy and supporting many secondary sex
characteristics
I. Sex Hormones
A. Estrogens
Estrogen that are available for use include:
1. estradiol (Estrace, Climara, and others)
2. conjugated estrogens (Premarin)
3. esterified estrogen (Menest)
4. estropipate (Ogen)
Therapeutic Actions and Indications
• Estrogens are important for the development of
secondary sex characteristics and proliferation of
endometrial lining.
• An absence or decrease in estrogen produces the signs and
symptoms of menopause in the uterus, vagina, breasts and
cervix.
• In small doses, estrogens are used for hormone
replacement therapy (HRT) when ovarian activity is
blocked or absent.
• As a palliation for the discomforts of menopause when
many of the beneficial effects of estrogen are lost
• Treatment of and Indications
• To prevent postpartum engorgement as part of
combination contraceptives
• To slow bone loss in osteoporosis
• Palliation in certain cancers that have known receptor
sensitivity
• Estrogens are known to compete with androgen for receptor
sites; this trait makes them beneficial in certain
androgen-dependent prostate cancers
• Systemic effects:
o Protects the heart from atherosclerosis
o Retaining calcium in the bones
o Maintaining the secondary female sex characteristics female
hypogonadism and ovarian failure
Pharmacokinetics
• Well-absorbed through the GI tract and undergo extensive
hepatic metabolism. They are excreted in urine.
• Crosses the placenta and enters breast milk
Contraindications and Cautions
❑ Contraindicated in the presence of any known allergies to
estrogens to avoid hypersensitivity reactions,
❑ In Patients with idiopathic vaginal bleeding, breast
cancer, or any estrogen- dependent cancer (could be
exacerbated by the drug),
❑With a history of thromboembolic disorders including
CVA (cerebrovascular accident),
❑ With heavy smokers because of the increased risk of
thrombus and embolus development,
❑ With hepatic dysfunction because of the effects of
estrogen on liver function
❑ Contraindicated during pregnancy due to the risk of
serious fetal defects
❑ Should be avoided during breastfeeding because of
possible effects on the neonate.
❑ Used cautiously in patients with metabolic bone disease
because of the bone-conserving effect of estrogen which could
exacerbate the disease
❑ With renal insufficiency, which could interfere with the
renal excretion of the drug and increase the risk for potential
adverse effects on fluid and electrolyte balance
❑With hepatic impairment which could alter the metabolism
of the drug and increase the risk for adverse effects, including
those on the liver and GI tract.
Adverse Effects
• GUT:breakthrough bleeding, menstrual irregularities,
dysmenorrhea, amenorrhea, and changes in libido.
• Systemic effects: fluid retention, electrolyte disturbances,
headache, dizziness, mental changes, weight changes, edema
• GI: Nausea, vomiting, abdominal cramps, bloating, colitis
• Potential serious GI effects: acute pancreatitis, cholestatic
jaundice, hepatic adenoma
Clinically important drug-drug interactions
• Smoking while taking estrogens should be strongly
discouraged because the combination with nicotine
increases the risk for development of thrombi and emboli
• Grapefruit juice can inhibit the metabolism of estradiols
leading to increased serum levels.
• St. John’s Wort can affect the metabolism of estrogens and
can make estrogen-containing contraceptives less effective.
This combination should be discouraged.
B. Progestins
Progestins include:
1. drospirenone (Yasmin, Yaz)
2. etonogestrel (Implanon)
3. levonorgestrel (Mirena)
4. medroxyprogesterone (Provera)
5. norethindrone (Aygestin)
6. norgestrel (generic)
7. progesterone (prometrium and others)
8. desogestrel (found in many contraceptive
combinations)
9. ulipristal (Ella)-used as a postcoital contraceptive
Therapeutic Actions and Indications
• Used as contraceptives, most effectively in combination
with estrogens
• Used to treat primary and secondary amenorrhea and
functional uterine bleeding and as part of fertility
programs.
• Useful in treating some cancers with specific receptor
site sensitivity
VNV | 5

Pharmacokinetics
• Well-absorbed, undergo hepatic metabolism and excreted
in urine.
• Known to cross the placenta and breast milk
• Available in several forms: injectables, intrauterine system,
transdermal system, Vaginal Ring, Subdermal Implant.
Contraindications and Cautions
• Contraindications and cautions are similar to those for
estrogens
• Contraindicated with PID (pelvic inflammatory disease),
sexually transmitted diseases, endometriosis, or pelvic
surgery because of the effects of progestins on the
vasculature of the uterus.
• Drospirenone is contraindicated in patients who are at
risk for hyperkalemia due to renal disorders, liver disease,
adrenal dysfunction, or the use of other drugs that can affect
potassium levels because of its anti-mineralocorticoid effects
and the risk of hyperkalemia.
• Should be used with caution in patients with epilepsy,
migraine, headaches, asthma or cardiac or renal
dysfunction because of the potential exacerbation of these
conditions
Adverse Effects
Adverse effects vary with the administration route used
• Dermal patch: systemic effects are the same with estrogen,
local irritation
• Vaginal gel: headache, nervousness, constipation, breast
enlargement, perineal
pain
• Intrauterine systems: abdominal pain, endometriosis,
abortion, PID, and expulsion of intrauterine device
• Vaginal use: local irritation and swelling
Drospirenone: used in combination with contraceptives, has
antimineralocorticoid activity and can block aldosterone,
leading to increased potassium levels
Clinically important drug-drug interactions
• Interaction with barbiturates, carbamazepine, phenytoin,
griseofulvin, penicillins, tetracyclines, or rifampin may
reduce the effectiveness of progestins.
✓ Patients using any of these drugs should use another
method of contraceptive if birth control is needed.
• St. John’s Wort can affect the metabolism of
progestin-containing contraceptives are less effective.
-This combination should be discouraged.
II. Estrogen Receptor Modulators
Two available Estrogen Receptor Modulators:
1. raloxifene (Evista)
2. toremifene (Fareston)
Therapeutic Actions and Indications
Estrogen Receptor Modulators are not hormones but affect
specific estrogen receptor sites to achieve therapeutic effects
of increased bone mass without stimulating the endometrium
and causing other less desirable estrogen effects.
Pharmacokinetics
• Administered orally, Raloxifene is well-absorbed from the GI
tract and is metabolized in the liver. Excretion occurs through
the feces.
• known to cross the placenta and enter into breast
milk.
Contraindications and Cautions
• Cholestyramine reduces the absorption of raloxifene.
• Highly protein bound drugs such as diazepam (valium),
ibuprofen (Motrin), Indomethacin (Indocin), and Naproxen
(Naprosyn), may interfere with binding sites.
• Warfarin taken with raloxifene may decrease the
prothrombin time; patients using this combination should be
monitored closely.
Raloxifene:
❑ In any known allergy to raloxifene to avoid
hypersensitivity reactions
❑ during pregnancy and lactation because of potential
effects on the fetus or neonate
❑ Caution should be used in patients with a history of
venous thrombosis or smoking because of an increased risk
of clot formation if smoking and estrogen are combined
III. Fertility Drugs
• In women with functioning ovaries, fertility drugs increase
follicle development by stimulating FSH and LH to increase
the chances for pregnancy.
• Women receiving fertility drugs need to be monitored for
ovarian overstimulation, need to be aware of multiple births,
and need support and encouragement to deal with the self-
esteem issues associated with infertility.
Pharmacokinetics
Fertility drugs are well absorbed and are treated like
endogenous hormones within the body, undergoing hepatic
metabolism and renal excretion.
Contraindications and Cautions
• contraindicated in the presence of primary ovarian failure
(they only work to stimulate functioning ovaries
• Thyroid or adrenal dysfunction because of the effects on
the hypothalamic-pituitary axis
VNV | 6
• Ovarian cysts, which could be stimulated and become larger
due to the effects of the drugs
• Pregnancy due to potential for serious fetal effects
• Idiopathic uterine bleeding
• Known allergy to any fertility drug to avoid hypersensitivity
reactions.
• Caution should be used in those with thromboembolic
diseases because of the risk of increased thrombus formation,
in women with respiratory diseases because of alterations
in fluid volume and blood flow that could overtax the respiratory
system
Adverse Effects
• Increased risk of multiple births and birth defects
• Ovarian overstimulation (abdominal pain, distention,
ascites, pleural effusion)
• Headache, fluid retention, nausea, bloating, uterine bleeding,
ovarian enlargement, gynecomastia, febrile reactions
IV. Uterine Motility Drugs
stimulate uterine contractions to assist labor (oxytocics) or
induce abortion (abortifacients).
Oxytocics
stimulate contraction of the uterus much like the action of the
hypothalamic hormone oxytocin, which is stored in the
posterior pituitary
Oxytocic Drugs:
1. Methylergonovine (methergine)
2. Oxytocin (Pitocin)
Pharmacokinetics
• Oxytocics are rapidly absorbed after parenteral or oral
administration, metabolized in the liver, and excreted in
the urine and feces. They cross the placenta and enter breast
milk.
• The oxytocics are administered IM or IV, methylergonovine
is administered as such directly after delivery and then
continued in the oral form to promote uterine involution.
Oxytocin is also used in a nasal form to stimulate milk “let
down” in lactating women.
Contraindications and Cautions
❑In the presence of any known allergy to oxytocics
❑cephalopelvic disproportion
❑Unfavorable fetal position
❑Complete uterine atony
✓ Caution should be used in patients with coronary
disease and hypertension and in patients who have had
previous cesarean births
Adverse Effects
• Uterine hypertonicity and spasm, uterine rupture,
postpartum hemorrhage, decreased fetal heart rate
• GI upset, nausea, headache, dizziness
• Oxytocin may cause severe water intoxication with coma
and even maternal death when used for a prolonged period.
Tocolytics
drugs used to slow uterine activity. Drugs that prevent preterm
labor and immature birth by suppressing uterine contractions
(TOCOLYSIS).
Agents used to delay premature uterine activity include:
1. anticonvulsants – ex. magnesium sulfate
2. beta-mimetics – ex. isoxsuprine
3. oxytocin antagonists –ex. atosiban
4. calcium channel inhibitors – ex. nifedipine
5. adrenergic beta-receptor agonists – ex. Ritodrine
✓ atosiban - the only oxytocin receptor antagonist that is
available as a tocolytic today
V. Abortifacients
Abortifacients are drugs that stimulate uterine activity to
cause uterine evacuation. These drugs can be used to
induce abortion in early pregnancy or to promote uterine
evacuation after fetal death.
Abortifacient drugs
1. carboprost (hemabate)
2. dinoprostone (Cervidil, Prepidil Gel, Prostin E2)
3. mifepristone (RU-486, Mifeprex)
Therapeutic Actions and Indications
❑ Stimulates uterine activity, dislodging any implanted
trophoblasts and preventing implantation of any
fertilized egg.
❑ approved for use to terminate pregnancy at 12 to 20
weeks from the date of the last menstrual period.
VNV | 7

Pharmacokinetics
Abortifacients are well absorbed when administered. They are
metabolized in the liver and excreted in the urine.
• Mifepristone
- administered orally and takes 5 to 7 days to produce
the desired effect
• Carboprost
- available as an IM injection, with an onset of 15
minutes and a duration of 2 hours
• Dinoprostone
- given by intravaginal suppository, with an onset of
effects of 10 minutes and a duration of effects of 2
hours
Contraindications and Cautions
• Should not be used with any known allergy to
abortifacients or prostaglandins to avoid hypersensitivity
reactions
• After 20 weeks from the last menstrual period; which
would be too late into the pregnancy for an abortion
• With active pelvic inflammatory disease or acute
cardiovascular, hepatic, renal, or pulmonary disease which
could be exacerbated by the effects of these drugs
• If to be used by a lactating mother, another method of
feeding the baby should be used.
• Caution should be used with any history of asthma,
hypertension, or adrenal disease which could be exacerbated
by the effects of these drugs
• With acute vaginitis or scarred uterus which could be
aggravated by the uterine contraction
Adverse Effects
• Abdominal cramping, heavy uterine bleeding, perforated
uterus, and uterine rupture (all of which are exaggeration of the
desired effects of the drugs)
• Headache, nausea and vomiting, diaphoresis (sweating),
backache and rash
Drugs Acting on the Male Reproductive
System
Topic Outline:
I. Androgens
II. Anabolic Steroids
III. Drugs for treating Penile Erection Dysfunction
I. Androgens
Therapeutic Actions and Indications
✓responsible for the growth and development of male sex
organs
✓maintenance of secondary male sex characteristics.
✓act to increase the retention of nitrogen, sodium, potassium,
and phosphorus and to decrease the urinary excretion of
calcium.
✓ Testosterones increase protein anabolism and decrease
protein catabolism (breakdown).
✓ Increase the production of red blood cells
Pharmacokinetics
• Testosterone is long-acting and is available in several
forms, including depot (deep-slow-release) injections, buccal
systems, topical gels, topical sprays, urethral pellets, and a
dermal patch.
• They are metabolized in the liver and excreted in the
urine.
Selected Drugs
1. danazol (Danocrine) - Blockade of follicle-stimulating
hormone and luteinizing hormone release in women to prevent
ovulation for treatment of endometriosis, prevention heredity
angioedema
2. fluoxymesterone (Androxy)
3. *testosterone (Androderm, Depotestosterone, Striant,
Androgel, Fortesta, Axiron, Natesto, Aveed)
4. methyltestosterone (Testred, Virilon)
Contraindications and Cautions
• With any known allergy to drug or ingredients in the drug
to prevent hypersensitivity reactions
• During pregnancy and lactation because of potential
adverse effect on the neonate
• In the presence of prostate or breast cancer in men (which
could be aggravated by testosterone effects of the drugs)
VNV | 8
• Topical forms: risk of virilization in children who come in
contact with the drug from touching the clothes and skin
of the man using the drug (patient must be advised to cover
all application areas if coming in contact with children and
wash all clothing that has touched the area before children
come in contact with it)
catabolic or tissue-destroying processes, and increase
hemoglobin and red blood cell mass.
❑ Indications for particular anabolic steroid vary
with the drug
❑ Classified as Class III controlled substances.

• Danazol: Has a black box warning regarding the risk

for thromboembolic events, fetal abnormalities,
hepatitis, and intracranial hypertension

Adverse Effects
• Androgenic Effects
- acne, edema, hirsutism, deepening of the voice, oily
skin and hair, weight gain, decrease in breast size,
and testicular atrophy
• Antiestrogen effects:
- lushing, sweating, vaginitis, nervousness, emotional
lability (in women)
Pharmacokinetics
• Hepatic toxicity
• Anabolic steroids are well-absorbed and widely distributed
- hepatic function test must be monitored before
throughout the body. They are metabolized in the liver and
beginning therapy and every 6 mos. during therapy
excreted in urine.
• Cardiovascular events
• Contraindicated for use during pregnancy because of
- including myocardial infarction (MI) and stroke and
adverse effects on the fetus.
venous embolic events, including deep-vein
thrombosis (DVT) and pulmonary embolism (PE).
-It is not known whether anabolic steroids enter breast milk, but
because of the potential adverse effects another method of
Clinically Significant Drug-Laboratory Test Interferences
feeding the baby should be used if these drugs are needed
• While a patient is taking Androgens, there may be
during lactation
decreased thyroid function as well as increased creatinine and
creatinine clearance, results that are not associated with
Contraindications and Cautions
disease states.
✓ Contraindicated in the presence of any known allergy to
anabolic steroids to prevent hypersensitivity reactions,
These effects can last up to 2 weeks after discontinuation of
✓ During pregnancy and lactation because of potential
therapy.
masculinization in the neonate,
✓ In the presence of liver dysfunction (because these
Testosterone
drugs are metabolized in the liver and are known to cause liver
✓ replacement therapy in hypogonadism
toxicity),
✓ treatment of delayed puberty in male patients
✓ In coronary disease (because of cholesterol-raising effects
✓ certain breast cancers in postmenopausal women.
through effects on the liver and direct effects on the vascular
✓ *testosterone are also used to prevent of postpartum breast
system),
engorgement
✓In prostate or breast cancer in males, which could be
exacerbated by the effects of these drugs
II. Anabolic Steroids
• Anabolic steroids are analogues of testosterone that have
Adverse Effects
been developed to produce the tissue building effects of
In prepubertal males
testosterone with less androgenic effect.
- adverse effects include virilization (phallic
• These drugs all have black box warnings as alerts to the
enlargement, hirsutism, increased skin pigmentation).
potentially serious effects of liver tumors, hepatitis, and blood
lipid level changes that might be associated with increased risk
In Post Pubertal males
of coronary artery disease.
- inhibition of testicular function, gynecomastia,
testicular atrophy, priapism (a painful and continual
Anabolic Steroids include:
erection of the penis), baldness, and change in libido
1. Oxandrolone (oxandrin)
(increased of libido)
2. Oxymetholone (Anadrol-50)
In women
Therapeutic Actions and Recommendations
- hirsutism, hoarseness, deepening of the voice, clitoral
❑ Promote body tissue-building processes, reverse
enlargement, baldness, and menstrual irregularities
VNV | 9
 • Not indicated for use to improve sexual performance in
As with androgens, serum electrolyte changes, liver women
dysfunction (including life- threatening hepatitis), insomnia, and • Caution should be used in patients with the ff. disease
weight gain. conditions because of the risk of exacerbating these
diseases:
Cardiomyopathy, hepatic carcinoma, personality changes, and ▪ bleeding disorders
sexual dysfunction are all associated with the excessive and ▪ coronary artery disease
off-label use of anabolic steroids. ▪ active peptic ulcer
▪ retinitis pigmentosa
Clinically important drug-drug interactions ▪ optic neuropathy
• Because the anabolic steroids affect the liver, there is a ▪ Hypotension
potential for interaction with anticoagulants and a ▪ severe hypertension
potential decreased need for antidiabetic agents, which ▪ congenital prolonged QT interval
may not be metabolized normally. ▪ severe hepatic or renal disorders
• They may alter lipid metabolism and cause a lack of
effectiveness for lipid-lowering agents. Patients should be Clinically important drug-drug interactions
monitored closely and appropriate dose adjustments made. • PDE5 inhibitors cannot be taken in combination with any
organic nitrates or alpha-adrenergic blockers,
III. Drugs for treating Penile Erectile Dysfunction • Possibility of increased vardenafil or tadalafil levels and
Penile erectile dysfunction is a condition in which the corpus effects if PDE5 inhibitors are taken with ketoconazole,
cavernosum does not fill with blood to allow for penile erection. itraconazole, or erythromycin (monitor the patient and
This can result from the aging process and in vascular and reduce dose as needed)
neurovascular conditions.
• Vardenafil and Tadalafil serum levels can increase if
Drugs for treating erectile dysfunction combined with indinavir and ritonavir (limit the dose of
1. Prostaglandin: alprostadil (Caverject, Muse) the PDE5 inhibitor if these drugs are being used).
2. Phosphodiesterase type 5 (PDE5) Receptor Inhibitors:
Antineoplastic Agents
❑ sildenafil (Viagra)
- also available as Revatio for the treatment of Topic Outline:
pulmonary arterial hypertension (PAH) I. Review of the Cell Cycle
❑ Taladafil (Cialis, Adcirca) II. Alkylating agents
III. Antimetabolites
- also used as treatment for PAH in men and women
IV. Antineoplastic Antibiotics
❑ Vardenafil (Levitra) V. Mitotic Inhibitors
*-afil VI. Hormones and hormone modulators
VII. Cancer cell-specific agents
A. Protein Tyrosine Kinase Inhibitors
B. Epidermal Growth Factor Inhibitors
C. Proteasome Inhibitors

I. Review of the Cell Cycle

•The genetic makeup of a particular cell determines the rate at
which that cell can multiply.
• Some cells reproduce very quickly (e.g. cells lining the GIT),
and some reproduce slowly ( e.g. some cells in breast tissue
have a generation time of a few months).
• Regardless of the rate of reproduction, each cell has
approximately the same life cycle.
• The life of a cell, called the cell cycle, consists of four active
phases and a resting phase.

Contraindications and Cautions

• Contraindicated in the presence of any anatomical
obstruction or condition that might predispose to priapism
because the risk could be exacerbated by these drugs
• Cannot be used with penile implants

VNV | 10
 1. G0 or resting phase
✓Cell is stable, it is not making any proteins associated with
cell division and is basically dormant as far as reproduction
goes. Cancer therapy usually works on active, dividing cells,
leaving resting cells fairly untouched.
2. G1 Phase
✓When a cell is stimulated to emerge from the resting
phase, it enters what is called G1 Phase.
✓Lasts from the time of stimulation from the resting phase
until the formation of DNA. During this period the cell
synthesizes
substances needed for DNA formation.
3. S Phase
✓Involves the actual synthesis of DNA, which is an energy
consuming activity.
✓The cell remains in this phase until the amount of cellular
DNA has doubled.
4. G2 Phase
✓ After the cellular DNA has doubled in preparation for
replication, the G2 phase begins.
✓ During this phase the cell produces all of the substances
required for the manufacture of mitotic spindles.
5. M Phase
✓After the cell has produced all of the substances necessary
for formation of a new cell, or daughter cell, it
undergoes cell division. This occurs during the M phase of the
cell cycle.
✓During this phase the cell splits to form two identical
daughter cells, a process called mitosis.
Cancer
✓CANCER is a disease that strikes a person at any age. It
arises from a single abnormal cell that multiplies and grows.
✓The use of the term chemotherapy implies cancer treatment
to most people. However, only one branch of chemotherapy
involves drugs developed to act on and kill or alter human cells
- the antineoplastic agents, which are designed to fight
neoplasms.
✓The goal of cancer chemotherapy is to decrease the size of
the neoplasm so that the human immune system can deal with
it.
Characteristics of Cancer Cells:
1. Anaplasia
- cancer cells lose their normal function
2. Autonomy
- cancer cells develop characteristics that allow them to
grow in an uninhibited way
3. Metastasis
- Cancer cells have the ability to travel to other sites in
the body that are conducive to their growth.
4. Angiogenesis
- cancer cells have the ability to grow new blood
vessels to feed the tumor
Solid Tumors
– may originate in any body organ and may be further divided
into:
❑ carcinomas (tumors that originate in epithelial cells)
example: granular cell tumors of the breast, bronchogenic
tumors arising in cells that line the bronchial tubes, squamous
and basal tumors of the skin
❑ sarcomas (tumor that originate in the mesenchyme and are
made up of embryonic connective tissue cells)
example: osteogenic tumors which form in the primitive cells
of the bone, and rhabdomyosarcomas which occur in striated
muscles.
Hematological Malignancies
– involve the blood-forming organs of the body, bone marrow,
and lymphatic system. These malignancies alter the body’s
ability to produce and regulate the cells found in the blood.
Antineoplastic Drugs
Antineoplastic drugs can work by affecting cell survival or by
boosting the immune system in its effort to combat the
abnormal cells.
Commonly used antineoplastic drugs:
1. Alkylating agents
2. Antimetabolites
3. Antineoplastic Antibiotics
4. Mitotic Inhibitors
5. Hormones and hormone modulators
6. Cancer cell-specific agents
7. Protein tyrosine kinase inhibitors (which target enzymes
specific to the cancer cells)

VNV | 11
Other drugs are used as adjunctive therapy to combat the • GI effects: nausea, vomiting, anorexia, diarrhea, mucous
serious adverse effects that can be associated with membrane deterioration (related to rapidly multiplying cells of
antineoplastic drugs. the GI tract)
• Hepatic toxicity
II. Alkylating Agents • Renal Toxicity
✓Alkylating agents affect cellular RNA, DNA, or other cellular • Alopecia
proteins are cell-cycle nonspecific, and are most effective
against slow-growing tumors. Allopurinol
✓Most useful in the treatment of slow-growing cancers, which All drugs causing cell death can cause a potentially toxic
have many cells in the resting phase. increase in uric acid levels. Allopurinol has been used to
alleviate this problem.
Alkylating agents include the ff. drugs: Rasburicase
❑altretamine (Hexalen) is used to manage uric acid levels in pediatric patients
❑bendamustine (Treanda) receiving antineoplastics resulting in tumor lysis and elevated
❑busulfan (Busulfex, Myleran) * uric acid levels.
❑carboplatin (generic)
❑carmustine (BiCNU, Gliadel) Contraindications and Cautions
❑chlorambucil (Leukeran) * • Alkylating agents that are known to cause hepatic or renal
❑cisplatin (Platinol, Platinol-AQ)* toxicity should be used cautiously with any other drugs that
❑cyclophosphamide* (generic) have similar effects. In addition, drugs that are toxic to the liver
❑dacarbazine (DTIC-Dome) or that act in the liver (e.g. oral anticoagulants).
❑ifosfamide (Ifex)
❑lomustine (CeeNU) ✓Always check for specific drug-drug interactions for each
❑mechlorethamine (Mustargen) agent in a nursing drug guide.
❑melphalan (Alkeran)
❑oxaliplatin (Eloxatin) SELECTED DRUGS
❑procarbazine (Matulane) Busulfan: Features ABCDEF
❑streptozocin (Zanosar) • Alkylating agent
❑temozolomide (Temodar) • Bone marrow suppression s/e
• CML indication
Therapeutic Actions and Indications • Dark skin (hyperpigmentation) s/e
• Alkylating agents produce their cytotoxic effects by reacting • Endrocrine insufficiency (adrenal) s/e
chemically with portions of RNA, DNA, or other cellular • Fibrosis (pulmonary) s/e
proteins, being most potent when they bind with cellular DNA. chlorambucil (Leukeran)
✓Palliative treatment of lymphomas and leukemias including
• Most useful in the treatment of slow growing cancers such Hodgkin disease;
as various lymphomas, leukemias, myelomas; some ovarian, ✓being considered for the treatment of rheumatoid arthritis
testicular, and breast cancers; some pancreatic cancer and other conditions
❑ Special considerations: toxic to liver and bone marrow;
Pharmacokinetics dosing based on bone marrow response
• Alkylating agents vary in their degree of absorption, and little Cisplatin (Platinol-AQ)
is known about their distribution in the tissues. ✓ Combination therapy for metastatic testicular
• They are metabolized in the liver and excreted in urine. or ovarian tumors, advanced bladder cancers
❑ Special considerations: neurotoxic, nephrotoxic, and can
NOTE: cause serious hypersensitivity reactions
A drug’s time to onset of action, time to peak effect, and duration of
action are all characteristics defined by pharmacokinetics. cyclophosphamide (Cytoxan, Neosar)
✓Treatment of lymphoma, myelomas, leukemias, and other
The half-life of a drug is an estimate of the period of time that it takes
cancers in combination with other drugs
for the concentration or amount in the body of that drug to be reduced
by exactly one half (50%).
❑ Special considerations: hemorrhagic cystitis is a
potentially fatal side effect; alopecia is common
Adverse Effects
• Hematological Effects: bone marrow suppression, with III. Antimetabolites
leukopenia, thrombocytopenia, anemia, and pancytopenia, Drugs that have chemical structures similar to those of various
secondary to the effects of the drugs on the rapidly multiplying natural metabolites that are necessary for growth and division
cells of the bone marrow of rapidly growing neoplastic cells and normal cells.

VNV | 12
 Antimetabolites include:
❑capecitabine (Xeloda)
❑cladribine (generic)
❑clofarabine (Clolar)
❑cytarabine (Depocyt, Tarabine PFS)
❑floxuridine (generic)
❑fludarabine (generic)
❑fluororacil (Carac, Efudex, Fluroplex)
❑gemcitabine (Gemzar)
❑mercaptopurine (generic)
❑methotrexate (Rheumatex, Trexall)
❑pemetrexed (Alimta)
❑pentostatin (Nipent)
❑ pralatrexate (Folotyn)
❑thioguanine (generic)
Therapeutic Actions and Indications
• Antimetabolites inhibit DNA production by inhibiting
metabolites needed for the synthesis of DNA in susceptible
cells.
• Antimetabolites are S-phase cell cycle specific and are
used for some leukemias, as well as some GI and basal cell
cancers.
Contraindications and Cautions
❑ Contraindicated for use during pregnancy and lactation
because of the potential for severe effects on the fetus and
Neonate.
❑ Caution is necessary when administering metabolites to any
individual with a known allergy to any of them to prevent
hypersensitivity reactions
❑ With bone marrow suppression (often the index for dosing
and redosing levels)
❑ With renal or hepatic dysfunction (might interfere with the
metabolism or excretion of drugs and often indicates a need to
change the dose; and with known GI ulcerations or ulcerative
diseases that might be exacerbated by the effects of these
drugs.
Adverse Effects
• Hematological Effects: bone marrow suppression, with
leukopenia, thrombocytopenia, anemia, and
pancytopenia, secondary to the effects of the drugs on
the rapidly multiplying cells of the bone marrow
• GI effects: nausea, vomiting, anorexia, diarrhea,
mucous membrane deterioration (related to rapidly
multiplying cells of the GI tract)
• CNS effects: headache, drowsiness, aphasia, fatigue,
malaise, dizziness
• Pulmonary toxicity: interstitial pneumonitis
• Hepatic toxicity
• Renal Toxicity
• Alopecia
Clinically important drug-drug interactions
• Antimetabolites that are known to cause hepatic or renal
toxicity should be used cautiously with any other drugs
that have the same effects. In addition, drugs that are toxic to
the liver or that act in the liver (e.g. oral anticoagulants).
• Always check for specific drug-drug interactions for each
agent in a nursing drug guide.
SELECTED DRUGS
Methotrexate ((Rheumatrex, Trexall)
✓Treatment of leukemias, psoriasis, rheumatoid arthritis, and
choriocarcinomas
❑Special considerations: hypersensitivity reactions can be
severe; liver toxicity and GI complications are common;
monitor for bone marrow suppression and increased
susceptibility to infections; dose pack available for the oral
treatment of psoriasis and rheumatoid arthritis
fluororacil (Carac, Efudex, Fluroplex)
✓Palliative treatment of various GI cancers; topical treatment
of basal cell carcinoma and actinic and solar keratoses
❑ Special considerations: GI toxicity, bone marrow
suppression, alopecia, and skin rash are common; avoid
occlusive dressings with topical forms; wash hands thoroughly
after coming in contact with drug
IV. Antineoplastic Antibiotics
Although selective for bacterial cells, antineoplastic
antibiotics are also toxic to human cells. Because these
drugs tend to be more toxic to cells that are multiplying rapidly,
They are most useful in the treatment of certain cancers.
Antineoplastic antibiotics are toxic to rapidly dividing
cells.
Antineoplastic Antibiotics include:
✓bleomycin (Blenoxane)
✓dactinomycin (Cosmegen)
✓daunorubicin (DaunoXome)
✓doxorubicin (Adriamycin, Doxil)
✓epirubicin (Ellence)
✓idarubicin (Idamycin)
✓mitomycin (Mutamycin)
✓mitoxantrone (Novantrone
✓valrubicin (Valstar)
*-mycin, -bicin
VNV | 13
 Therapeutic Actions and Indications
✓Antineoplastic antibiotics are cytotoxic and interfere with
cellular DNA synthesis by inserting themselves between base
pairs in the DNA. This in turn causes a mutant DNA
molecule leading to cell death.
✓Toxic to rapidly dividing cells
✓Cell-specific, affecting the S phase
Pharmacokinetics
• Not absorbed well from the GI tract, given IV or injected into
specific sites
• Metabolized in the liver and excreted in the urine at various
sites. Many of them have long half-lives (e.g. 45 hours for
idarubicin); more than 5 days for mitoxantrone
Daunorubicin and Doxorubicin
do not cross the blood- brain barrier, but they are widely
distributed in the body and are taken by the heart, lungs,
kidneys, and spleen. This can lead to toxic effects in these
organs.
Contraindications and Cautions
❑ All antineoplastic antibiotics are contraindicated for use
during pregnancy and lactation because of the potential risk
to the neonate and lactation.
❑ Caution is necessary when administering metabolites to
any individual with a known allergy to the antibiotic or any
related antibiotics to prevent hypersensitivity reactions,
- with bone marrow suppression (often the index for
dosing and redosing levels)
- with renal or hepatic dysfunction (which might
interfere with the metabolism or excretion of these
drugs and often indicates a need to change the dose;
and
- with known GI ulcerations or ulcerative diseases
that might be exacerbated by the effects of these
drugs.
❑ Pulmonary problems with bleomycin or mitomycin
❑ Cardiac problems with idarubicin or mitoxantrone
Adverse Effects
• Hematological Effects: bone marrow suppression, with
leukopenia, thrombocytopenia, anemia, and pancytopenia,
secondary to the effects of the drugs on the rapidly multiplying
cells of the bone marrow
• Toxic GI effects: nausea, vomiting, anorexia, diarrhea,
mucous membrane deterioration (related to rapidly multiplying
cells of the GI tract)
• Hepatic toxicity
• Renal Toxicity
• Alopecia
• Specific antineoplastic antibiotics are toxic to the heart and
lungs (refer to previous slide for example)
Dexrazoxane (Zinecard)
a powerful intracellular chelating agent, is a cardioprotective
drug that interferes with the cardiotoxic effects of
doxorubicin. This agent is approved for use to prevent
cardiomyopathy associated with doxorubicin in doses greater
than 300mg/m2 in women with metastatic breast cancer.
Clinically important drug-drug interactions
• Antineoplastic antibiotics that are known to cause hepatic or
renal toxicity should be used cautiously with any other drugs
that have the same effects.
• Drugs that result in toxicity to the heart and lungs should
be used in caution with any other drugs that produce that
particular toxicity.
• Always check for specific drug-drug interactions for each
agent in a nursing drug guide.
SELECTED DRUGS
doxorubicin (Adriamycin, Doxil)
✓Treatment of a number of leukemias and cancers; used to
induce regression; available in a liposomal form for treatment
of AIDS- associated Kaposi sarcoma
❑Special considerations:
- complete alopecia is common; GI toxicity and bone
marrow suppression may occur;
- severe necrosis may occur at sites of local
extravasation— immediate treatment with
corticosteroids, normal saline, and ice may help; if
ulcerations occur, a plastic surgeon should be
called;
- toxicity is dose related—an accurate record of each
dose received is important in determining dose;
severe pulmonary toxicity, alopecia, and GI toxicity
occur
mitomycin (Mutamycin)
✓ Treatment of disseminated adenocarcinoma of the stomach
and pancreas
❑ Special considerations: severe pulmonary toxicity,
alopecia, and injection-site and GI toxicity occur
idarubicin (Idamycin)
✓ Combination therapy for treatment of acute myeloid
leukemia in adults
❑ Special considerations: may cause severe bone marrow
suppression, which regulates dose; associated with cardiac
toxicity, which can be severe;
- GI toxicity and local necrosis with extravasation are
also common;
- severe necrosis may occur at sites of local
extravasation—immediate treatment with
corticosteroids, normal saline, and ice may help; if
ulcerations occur, a plastic surgeon should be called;
- it is essential to monitor heart and bone marrow
function to protect the patient from potentially fatal
adverse effects
VNV | 14
 IV. Mitotic Inhibitors
- Mitotic inhibitors are drugs that kill cells as the
process of mitosis begins. These cell-specific
agents inhibit DNA synthesis.
- Main adverse effects occur with cells that rapidly
multiply (those in the bone marrow, GI tract, and skin)
Mitotic inhibitors include:
1. cabazitaxel (Jevtana)
2. docetaxel (Taxotere)
3. eribulin (Halaven)
4. etoposide (generic)
5. ixabepilone (Ixempra)
6. paclitaxel (Abraxane, Onxol, Taxol)
7. teniposide (Vumon)
8. vinblastine (generic)
9. vincristine (generic)
10.vinorelbine (Navelbine)
* -taxel, -tine
Therapeutic Actions and Indications:
Mitotic inhibitors interfere with the ability of a cell to
divide; they block or alter DNA synthesis, thus causing cell
death.
They work in the M phase of the cell cycle. These drugs are
used for the treatment of a variety of tumors and leukemias
Pharmacokinetics
• Generally given intravenously because they are not
well-absorbed in the GI tract
• They are metabolized in the liver and excreted primarily
in the feces making them safer for use in patients with
renal impairment than the antineoplastics that are cleared
through the kidney.
Contraindications and Cautions
• Contraindicated for use during pregnancy and lactation
because of the potential for severe effects on the fetus and
neonate.
• Caution is necessary when administering these drugs to
anyone with a known allergy to the drug to prevent
hypersensitivity reactions,
• Care is necessary for patients with bone marrow
suppression which is often the index for dosing and redosing
levels,
• With renal or hepatic dysfunction,
• with known GI ulcerations or ulcerative diseases that might
be exacerbated by the effects of these drugs.
Adverse Effects
• Hematological Effects: bone marrow suppression, with
leukopenia, thrombocytopenia, anemia, and pancytopenia,
secondary to the effects of the drugs on the rapidly multiplying
cells of the bone marrow
• GI effects: nausea, vomiting, anorexia, diarrhea, mucous
membrane deterioration (related to rapidly multiplying cells of
the GI tract)
Eribulin
- may prolong QT interval leading to potentially serious
arrhythmias
• Hepatic toxicity
• Renal Toxicity
• Alopecia
• Necrosis and vasculitis if extravasation occurs so it is
necessary
to regularly monitor injection sites and take appropriate action
as needed.
Clinically important drug-drug interactions
Mitotic Inhibitors that are known to be toxic to the liver or the
CNS should be used with care with any drugs known to have
the same adverse effect.
Check specific drug-drug interactions for each
agent in a nursing drug guide.
SELECTED DRUGS
etoposide (Toposar, VePesid)
✓ Treatment of testicular cancers refractory to other agents;
non–small cell lung carcinomas
❑ Special considerations:
- fatigue, GI toxicity, bone marrow depression, and
alopecia are common side effects;
- avoid direct skin contact with the drug;
- use protective clothing and goggles;
- monitor bone marrow function to adjust dose;
- rapid fall in blood pressure can occur during IV
infusion—monitor patient carefully
paclitaxel (Abraxane, Onxol Taxol)
✓ Treatment of advanced ovarian cancer, breast cancer,
non–small cell lung cancer, and AIDS-related Kaposi sarcoma
❑Special considerations:
- anaphylaxis and severe hypersensitivity reactions
have occurred— monitor very closely during
administration
- also monitor for bone marrow suppression;
cardiovascular toxicity and neuropathies have
occurred.
vincristine (Oncovin, Vincasar)
✓ Treatment of acute leukemia, various lymphomas, and
sarcomas
❑ Special considerations:
- extensive CNS effects are common, GI toxicity, local
irritation at injection IV site, and hair loss commonly
occur;
- syndrome of inappropriate secretion of antidiuretic
hormone has been reported—monitor urine output
and arrange for fluid restriction and diuretics as
needed
VNV | 15
 V. Hormones and Hormone Modulators • Hypercalcemia is a contraindication to the use of
• Hormone and Hormonal agents are used to treat toremifene, which is known to increase calcium levels.
specific cancers that respond to hormone stimulation. • Caution is necessary when administering these drugs to
• Several antineoplastic agents are used to block or anyone with a known allergy to the drug to prevent
interfere with these receptor site to prevent growth of hypersensitivity reactions
the cancer and in some situations to actually cause • Care with renal or hepatic dysfunction (might interfere with
death. the metabolism or excretion of drugs and often indicates a
• Some hormones are used to block the release of need to change the dose)
gonadotropic hormones in breast or prostate cancer if • Care is necessary for patients with bone marrow
the tumors are responsive to gonadotropic hormones. suppression which is often the index for dosing and redosing
• Others may block androgen receptor sites directly and levels.
are useful in the treatment of advanced prostate
Cancers Clinically important drug-drug interactions
Increased risk of bleeding if hormones and hormone
Adverse Effects modulators are taken with oral anticoagulants.
▪ Abiraterone (zytiga)
▪ Anastrazole (Arimidex) Care is also necessary when administering these agents
▪ Bicalutamide (Casodex) with any drugs that might increase serum lipid levels.
▪ Degarelix (Firmagon)
▪ Enzalutamide (Xtandi) Adverse Effects
▪ Estramustine (Emcyt) ✓ Adverse effects involve the effects that are seen
▪ Exemestane (Aromasin) when estrogen is blocked or inhibited. Menopause
▪ Flutamide (generic) associated effects include hot flashes, vaginal
▪ Fulvestrant (Faslodex) spotting, vaginal dryness, moodiness, and depression.
▪ Goserelin (Zoladex) ✓ Bone marrow suppression
▪ Histrelin (Vantas) ✓ GI Toxicity
▪ Letrozole (Femara) ✓ Hepatic Dysfunction
▪ Leuprolide (Lupron, Eligard) ✓ Hypercalcemia as the calcium is pulled out of the
▪ Megestrol (Megace) bones without estrogen activity to promote calcium
▪ Mitotane (Lysodren) deposition
▪ Nilutamide (NIlandron) ✓ Increased risk for cardiovascular disease
▪ Tamoxifen (Soltamox) ✓ Increased risk of adrenocortical insufficiency with
▪ Toremifene (Fareston) the use of Abiraterone
▪ Triptorelin pamoate (Trelstar)

Therapeutic Actions and Indications

❑The hormones and hormone modulators used as
antineoplastics are receptor site specific or hormone
specific to block the stimulation of growing cancer cells
that are sensitive to the presence of that hormone.
❑Indicated for the treatment of breast cancer in
postmenopausal women or in other women without ovarian
function.
❑Some drugs are indicated for the treatment of prostatic
cancers that are sensitive to hormone manipulation.
SELECTED DRUGS
Pharmacokinetics
AGONISTS
▪ Readily absorbed from the GI tract, metabolized in the liver,
and excreted in urine Drug Name Usual Indications
▪ Caution must be used with any patient who has hepatic or
renal impairment goserelin Used as an antineoplastic agent for
▪ Hormones and hormone modulators cross the placenta and (Zoladex) treatment of specific hormone-
stimulated cancers
enter into breast milk
Actions: synthetic luteinizing hormone
Contraindications and Cautions that inhibits pituitary release of
• Contraindicated for use during pregnancy and lactation gonadotropic hormones
because of the potential for severe effects on the fetus and
neonate. histerelin Palliative treatment of advanced
VNV | 16
 (Vastas) prostate cancer
Actions: inhibits gonadotropic
secretion; decreases follicle stimulating
hormone and luteinizing hormone levels
and testosterone levels
leuprolide Used as antineoplastic agent for
(Lupron) treatment of specific cancers, treatment
of endometriosis and precocious
puberty that results from hypothalamic
Activity
Actions: a natural luteinizing hormone
that blocks the release of gonadotropic
hormones
ANTAGONISTS
Drug Name Usual Indications
degarelix (Firmagon) Treatment of advanced
prostate cancer
Actions: Degarelix is a
gonadotrophin-releasing
hormone (GnRH)
antagonist for the first-line
treatment of
androgen-dependent
advanced prostate cancer.
letrozole (Femara)
✓ Treatment of advanced breast cancer in postmenopausal
women with disease after antiestrogen therapy; post-surgery
adjunct for postmenopausal women with early hormone
receptor–positive breast cancer.
Actions: prevents the conversion of precursors to
estrogens in all tissues
❑ Special considerations: GI toxicity, bone marrow
depression, alopecia, hot flashes, and central nervous system
(CNS) depression are common effects; discontinue drug at any
sign that the cancer is progressing
tamoxifen (Soltamox)
✓ In combination therapy with surgery to treat breast cancer;
treatment of advanced breast cancer in men and women; first
drug approved for the prevention of breast cancer in women at
high risk for breast cancer
Actions: antiestrogen, competes with estrogen for receptor
sites in target tissues
❑ Special considerations: signs and symptoms of
menopause are common effects; CNS depression, bone
marrow depression, and GI toxicity are also common; can
change visual acuity and cause corneal opacities and
retinopathy— pretherapy and periodic ophthalmic
examinations are indicated
VI. Cancer cell-specific agents
• Cancer cell-specific drugs have been developed to target
processes that occur in cancer cells but not in healthy
cells. This specificity results in fewer toxic effects than with
traditional antineoplastic therapy.
This include:
1. Protein tyrosine kinase inhibitors
2. Epidermal growth factor inhibitors
3. Proteasome inhibitors
A. Protein Tyrosine Kinase Inhibitors
Each drug that has been developed inhibits a very specific
protein kinase and acts on very specific tumors.
They do not affect healthy human cells, so the patients do not
experience the numerous adverse effects associated with
antineoplastic therapy.
Imatinib (Gleevec)
- first approved drug in this class
- given orally and is approved to treat chronic myeloid
leukemia (CML), several GI stromal tumors, various
myeloproliferative disorders, aggressive systemic
mastocytosis, unresectable dermatofibrosarcoma
protuberans
Long term effects: development of new cancers, cardiac
toxicity, bone marrow suppression
Pharmacokinetics: slowly absorbed from the GI tract,
reaching peak levels in 2 to 4 hours. It is extensively
metabolized in the liver, with a half life of 18 and then 40 hours.
* Each of the many kinase Inhibitor is metabolized in the
liver; the absorption and pharmacokinetics vary with
kinase inhibitor.
Adverse Effects: GI upset, muscle cramps, heart failure, fluid
retention, skin rash
*Severe bone marrow suppression, alopecia, severe GI
effects associated with more traditional antineoplastic
therapy do not occur.
✓Several cancer cell-specific drugs prolong the QT interval
and need to be used with caution in patients with cardiac
problem
Available Kinase Inhibitors:
▪ Afatinib (Gilotrif)
▪ Axitinib (Inlyta)
▪ Bosutinib (Bosulif)
▪ Cabozantinib (Cometriq)
▪ Ceretinib (Zykadia)
▪ Crizotinib (Xalkori)
▪ Dabrafenib (Tafinlar)
▪ Everolimus (Afinitor)
▪ Ibrutinib (Imbruvica)
VNV | 17
▪ Idelalisib (Zydeliq) Contraindications and Cautions
▪ imatinib (Gleevec)
▪ Lapatinib (Tykerb)
▪ Nilotinib (Tasigna)
▪ Palbociclib (Ibrance)
▪ Pazopanib (Vorient)
▪ Ponatinib (Iclusig)
▪ Regorafenib (Stivarga)
▪ Ruxolitinib (Jafaki)
▪ Sorafenib (Nexavar)
▪ Sunitinib (Sutent) ❑ All cancer cell-specific agents are in pregnancy
▪ Temsirolimus (Torisel) category D.
▪ Trametinib (Mekinist) ❑ Women in childbearing age should be advised to use
▪ Vemurafenib (Zelboraf) barrier contraceptives.
▪ Ziv-aflibercept (Zaltrap) ❑ It can enter breast milk, and it should be used during
*-nib lactation only if the benefits to the mother clearly
outweighs the risks to the baby.
B. Epidermal Growth Factor Inhibitor ❑ Contraindicated to patients who have or who are at risk
Erlotinib (Tarceva) for prolonged QT intervals (hypokalemia, hypomagnesemia,
- inhibits cell epidermal growth factor receptors. or taking another drug that prolongs the QT interval
- This growth factor is found on normal and cancerous ❑ Caution is necessary when administering these drugs
cells but is more abundant on rapidly growing cells. to anyone with a known hypersensitivity to any component
of the drug being given.
Pharmacokinetics: well absorbed orally from the GI tract,
reaching peak levels in 4 hours. It is metabolized in the liver Clinically Important drug-drug interactions
with a half life of 36 hours. • St. John’s Wort decreases the effectiveness of many of these
drugs (cell cycle-specific agents) and should be avoided.
Adverse Effects: cardiovascular events and pulmonary • It is also important to avoid any other drugs that are known to
toxicity prolong the QT interval.

C. Proteasome Inhibitor
Bortezomib (Velcade)
- used for the treatment of multiple myeloma in Drugs Acting on the Immune System
patients whose disease had progressed after two
Topic Outline:
other standard therapies.
I. Immune Stimulants
- This drug inhibits proteasome in human cells, a
A. Interferons
large protein complex that works to maintain cell
B. Interleukins
homeostasis and protein production. Without it the
C. Colony Stimulating Factors
cell loses homeostasis and dies.
II. Immune Suppressants
- This drug was shown to delay growth in selected
A. Immune Modulators
tumors.
B. T and B cell Suppressors
C. Interleukin Receptor Antagonist
Pharmacokinetics: given IV, reaches peak effects at the end
D. Monoclonal Antibodies
of the infusion. It is metabolized in the liver and has a half-
III. Vaccines
life of 40 to 193 hours.
IV. Immune Sera
Adverse Effects: cardiovascular events and pulmonary
toxicity, peripheral neuropathy, liver and kidney impairment Glossary of Terms
Immune Stimulant
- specific antibodies produced by a single clone of B
cells to react with a very specific antigen

Immune Suppressant
- specific antibodies produced by a single clone of B
cells to react with a very specific antigen

VNV | 18
 Monoclonal Antibodies
- specific antibodies produced by a single clone of B
cells to react with a very specific antigen
Recombinant DNA (rDNA) Technology
- use of bacteria to produce chemicals normally
produced by human cells.
I. Immune Stimulants
A. Interferons
- naturally released from human cells in response to
viral invasion;
- Interferons are substances naturally produced and
released by human cells that have been invaded by
viruses.
- May also be released from cells in response to other
stimuli, such as cytotoxic T cell activity.
Interferons produced by rDNA technology:
1. Alfa-2b (Intron-A)
2. Peginterferon alfa 2-a (Pegasys)
3. Peginterferon alfa 2-b (Peg-Intron)
4. Interferon beta 1-b (Betaseron)
5. Interferon alfa-n3 (Alferon N)
6. Interferon beta-1a (Avonex)
7. Interferon gamma-1b (Actimmune)
*The interferon of choice depends on the condition being
treated.
Interferon alfa-n3 (Alferon N)
- produced by harvesting human leukocytes
Interferon beta-1a (Avonex
- produced from Chinese hamster ovary cells
Interferon gamma-1b (Actimmune)
- produced by Escherichia Coli bacteria
Therapeutic Actions and Recommendations
• Prevent virus particles from replicating inside cells.
• Stimulate interferon receptor sites on noninvaded cells
to produce antiviral proteins, which prevent viruses from
entering the cell.
• Inhibit tumor growth and replication, to stimulate cytotoxic T
cell activity and to enhance the inflammatory response.
• Interferon gamma 1-b also act like an interleukin, stimulating
phagocytes to be more aggressive.
Pharmacokinetics
❑ Generally well-absorbed after subcutaneous or
intramuscular injection.
❑ They have a rapid onset of action and peak within 3 to 8
hours, half-life: 3 to 8 hours, with the exception of interferon
beta-1a which has an onset of action of 12 hours and reaches
peak levels in 48 hours, with a half-life of 10 hours.
❑ Interferons are broken down in the liver and kidneys and
seem to be excreted primarily through the kidneys.
Contraindications and Cautions
• Contraindicated in the presence of known allergy to any
interferon or product components to prevent
hypersensitivity reactions.
• Potentially teratogenic and therefore should not be used
during pregnancy. Use of barrier contraceptives is advised for
women of childbearing age.
• Not known whether drugs cross into breastmilk but because
of the potential adverse effects to the baby, it is advised that
the drugs not be used during lactation unless the benefits to
the mother clearly outweigh any risks to the baby.
• Caution should be used in the presence of known cardiac
disease because hypertension and arrhythmias can occur;
• Caution with myelosuppression because these drugs may
further depress the bone marrow;
• Caution with CNS dysfunction because of the potential for
CNS depression and personality changes
Adverse Effects
• Flu-like syndrome with lethargy, myalgia, arthralgia,
anorexia, nausea
• Headache, dizziness, bone marrow depression, depression
and suicidal ideation, photosensitivity and liver impairment
Clinically Important drug-drug interactions
•There are no reported clinically important drug- drug
interactions with interferon.
B. Interleukins
• Interleukins are synthetic compounds much like interferons;
they communicate between lymphocytes, which stimulate
cellular immunity and inhibit tumor growth.
• Interleukin 2- stimulates cellular immunity by increasing the
activity of natural killer cells, platelets, and cytokines
Interleukin preparations available for use:
aldesleukin (Proleukin)
- produced by rDNA using Escherichia Coli bacteria
Pharmacokinetics: given IV, reaches peak levels in 13
minutes and has a half-life cycle of 85 minutes.
oprelvekin (Neumega)
- newer agent produced by rDNA technology
Pharmacokinetics: Oprelvekin, which is given subcutaneously
reaches peak levels in 3 to 5 hours and has a half-life of 7
to 8 hours.
Adverse Effects: associated with severe hypersensitivity
reactions (patient should be closely watched when beginning
therapy)
Therapeutic Actions and Recommendations
Natural interleukin 2 is produced by various lymphocytes to
activate cellular immunity and inhibit tumor growth by
increasing lymphocyte numbers and their activity.
VNV | 19
 Pharmacokinetics
- Interleukins are rapidly distributed after injection..
- Interleukins are primarily cleared from the body by the
kidneys.
Contraindications and Cautions
• Contraindicated in the presence of any allergy to an
interleukin or Escherichia coli produced product to prevent
hypersensitivity reactions.
• Should not be used during pregnancy because of their
embryocidal and teratogenic effects in animal studies. Use of
barrier contraceptives is recommended for women of
childbearing age.
• It is not clear whether the drugs cross into breastmilk, but it is
recommended not be used during lactation. If they must be
used, another method of feeding the baby must be chosen.
• Caution should be used with renal, liver, or
cardiovascular impairment because of the adverse effects of
the drugs.
Adverse Effects
• Flu-like syndrome with lethargy, myalgia, arthralgia,
anorexia, nausea
• Respiratory difficulties, CNS changes, cardiac arrhythmias
Clinically important drug-drug interactions
There are no reported clinically important drug-drug
interactions with interleukins.
C. Colony-Stimulating Factors
• Colony stimulating factors are glycoproteins that
promote production of white blood cells (mainly
granulocytes such as neutrophils), in response to
infection.
• Administration of exogenous colony stimulating factors
stimulates the stem cells in the bone marrow to produce
more of the particular white blood cells. The new white
blood cells migrate into the blood and fight the infection.
CSF drugs produced by recombinant DNA technology:
1. filgrastim (Neupogen)
2. pegfilgrastim (Neulasta)
3. Tbo-filgrastim
*-grastim
Therapeutic Actions and Indications
✓ Used in patients who are undergoing cancer treatment that
causes low white blood cell counts (neutropenia) and puts the
patient at risk of infection.
✓ Colony stimulating factors tend to reduce the time where
patients are neutropenic.
Filgrastim
Pharmacokinetics:
can be given IV or by subcutaneous injection, reaching peak
levels in 2 hours IV or 9 hours subcutaneously; it has a half-life
of about 220 minutes and a duration of 4 days; its metabolism
and excretion are not known.
Pegfilgrastim
Pharmacokinetics:
is only given by subcutaneous injection with similar onset
but has a much longer half-life, 15 to 80 hours, than filgrastim.
Tbo-Filgrastim
Pharmacokinetics:
is only given subcutaneously, reaches peak levels in 4 to 6
hours and has a half-life of 3.5 Hours.
Sargramostim
Pharmacokinetics:
can be given IV or subcutaneously with a duration of 6 hours
(IV) or 12 hours subcutaneously. It
has a half-life of 1 to 3 hours; its metabolism and excretion
are not known.
Contraindications and Cautions:
✓ contraindicated in neonates because of benzyl alcohol in
the solution and with excessive leukemic myeloid blasts in
the bone marrow or peripheral blood, which could be
worsened by the drug.
✓ Should be used with caution in pregnancy and lactation
because the potential effects on the fetus or neonate are
not known.
✓ should also be used with caution in hepatic or renal
failure which could alter the pharmacokinetics of the drug,
during or immediately after radiation or chemotherapy
because of a potential loss of effectiveness.
Adverse Effects
• GI effects: nausea, vomiting, diarrhea, constipation,
anorexia; Headache, generalized weakness, alopecia and
dermatitis, and generalized pain and bone pain.
*The effects are thought to be associated with the drug effects
on the bone marrow cells and their increased activity.
Clinically important drug-drug interactions
The only reported drug-drug interactions associated with these
drugs is an increase in the myeloproliferative effects of
sargramostim when combined with lithium or
corticosteroids; these combinations should be used with
Caution.
II. Immune Suppressants
Immune suppressants often are used in conjunction with
corticosteroids, which block the inflammatory reaction and
decrease initial damage to cells.
They are especially beneficial in cases of organ
transplantation and in the treatment of autoimmune
diseases.
B-cells: Attacks invaders outside the cells
T-Cells: Attacks invaders inside the cells
VNV | 20
 A. Immune Modulators
Immune modulators block the release of various cytokines
involved in the inflammatory response and activation of
lymphocytes, decreasing immune activity. The result of
blocking these chemicals is immune suppression.
The immune modulators are a relatively new class of
drugs and include:
1. fingolimod (Gilenya)
2. lenalidomide (Revlimid)
3. thalidomide (Thalomid), an old drug with new uses
4. apremilast (Otezla)
5. dimethyl fumarate (Tecfidera)
6. pomalidomide (Pomalyst)
7. teriflunomide (Aubagio).
fingolimod (Gilenya)
Therapeutic Actions and Indications
✓ inhibits the release of lymphocytes from lymph nodes into
the peripheral blood so they cannot migrate to activate immune
and inflammatory reactions.
✓ Fingolimod is the first oral agent for the treatment of
relapsing forms of multiple sclerosis.
Pharmacokinetics:
slowly absorbed from the GI tract, reaching peak levels in 12
to 16 hours. It is metabolized in the liver and excreted
through the kidneys with a half-life of 6 to 9 days.
lenalidomide (Revlimid)
Therapeutic Actions and Indications
✓ inhibit the secretion of proinflammatory cytokines and
increase the secretion of anti-inflammatory cytokines from
monocytes and have varying effects on cell proliferation.
✓ used in treating multiple myeloma and myelodysplastic
syndromes. Thalidomide is also used for treating multiple
myeloma and erythema nodosum leprosum.
Pharmacokinetics:
absorbed quickly from the GI tract, reaching peak levels in
30 to 90 minutes. It is excreted unchanged in the urine with
a half-life of 3 hours.
thalidomide (Thalomid)
Therapeutic Actions and Indications
✓ inhibit the secretion of proinflammatory cytokines and
increase the secretion of anti-inflammatory cytokines from
monocytes and have varying effects on cell proliferation.
Pharmacokinetics:
very slowly absorbed from the GI tract, reaching peak levels
in 3 to 6 hours. The metabolism of thalidomide is not
known; it is excreted in the urine with a half-life 12 to 24
hours.
apremilast (Otezla)
Therapeutic Actions and Indications
✓ used for adults with psoriatic arthritis.
Pharmacokinetics:
absorbed from the GI tract with peak levels reached in 2.5
hours. It is also metabolized in the liver with excretion in
both urine and feces. Apremilast has a half life of 6 to 9
hours.
dimethyl fumarate (Tecfidera)
Therapeutic Actions and Indications
✓used to treat multiple sclerosis
Pharmacokinetics:
absorbed from the GI tract with peak levels occurring within 2
to 2.5 hours. It is metabolized by esterases throughout the
body with the main excretion occurring as CO2 through
the lungs. The half-life of this drug is about an hour.
pomalidomide (Pomalyst)
Therapeutic Actions and Indications
✓ is a thalidomide analog that is used in treating multiple
myeloma.
Pharmacokinetics:
is absorbed from the GI tract, reaching peak levels in 2 to 3
hours. It is metabolized in the liver and excreted in the
urine with a half-life of 7.5 to 9.5 hours.
teriflunomide (Aubagio)
Pharmacokinetics (oral):
reaches peak levels in 1 to 4 hours; it is excreted unchanged
in the bile. Most of the drug is eliminated from the body within
21 days.
Contraindications and Cautions:
also contraindicated with severe hepatic impairment which
could become more severe due to the drug effects.
Contraindications and Cautions
All contraindicated during pregnancy because their effects
on cells can cause serious fetal harm; women of
childbearing age should be advised to use barrier
contraceptives when using this drug, and proof that the
patient is not pregnant needs to be documented in the
chart before beginning therapy and periodically during
therapy.
B. T and B Cell Suppressors
T and B Cell Suppressors available for use:
• abatercept (Orencia)
• alefacept (Amevive)
• azathioprine (Imuran)
• cyclosporine (Sandimmune, Neoral) - most commonly
used
• glatiramir (Copaxone)
• mycophenolate (Cellcept)
• pimecrolimus (Elidel)
• sirolimus (Rapamune)
• tacrolimus (Prograf)
VNV | 21
*-limus
Therapeutic Actions and Indications
T and B cell suppressors are indicated for the prevention and
treatment of specific transplant rejections.
cyclosporine (Sandimmune, Neoral)
Pharmacokinetics:
well absorbed from the GI tract and extensively metabolized
in the liver. It is available as an oral solution that can be
mixed with milk, chocolate milk, or orange juice for ease
of administration.
mycophenolate (Cellcept)
Pharmacokinetics:
readily absorbed and immediately metabolized to its active
metabolite. Most of the metabolized drug is then excreted
in the urine.
azathioprine (Imuran)
Pharmacokinetics:
rapidly absorbed from the GI tract , reaching peak levels in 1 to
2 hours. The drug is catabolized in the liver and red blood
cells.
tacrolimus (Prograf)
Pharmacokinetics:
Rapidly absorbed from the GI tract, reaching peak
levels in 1.5 to 3.5 hours. It is metabolized in the liver and
excreted in the urine.
Contraindications and Cautions
• Contraindicated in the presence of any known allergy to the
drugs or its component to prevent hypersensitivity
• Contraindicated during pregnancy and lactation because of
serious adverse effects on the fetus or neonate.
• Caution should be used with renal or hepatic impairment,
which could interfere with the metabolism or excretion of the
drug.
• Caution should be used in the presence of known
neoplasms, which potentially could spread with immune
system suppression.
Adverse Effects
• Increased risk for infection and development of
neoplasms due to their blocking effect on the immune system.
• Hepatotoxicity, renal toxicity, renal dysfunction, pulmonary
edema
• Headache, tremors, secondary infections such as acne, GI
upset, diarrhea, and hypertension
Clinically important drug-drug interactions
Increased risk of toxicity if combined with other drugs that are
hepatotoxic or nephrotoxic.
C. Interleukin Receptor Antagonist
• Works to block the activity of the interleukins that are
released in an inflammatory or immune response.
anakinra (Kineret)
The only available interleukin receptor antagonist
Therapeutic Actions and Recommendations
✓ Used to reduce the signs and symptoms of moderately
to severely active rheumatoid arthritis in patients 18 years
of age and older who do not respond to the traditional
antirheumatic drugs.
Pharmacokinetics
✓ The recommended dosage is 100mg/d by subcutaneous
injection.
✓ Anakinra is administered by subcutaneous injection and is
absorbed slowly, reaching peak effects in 3 to 7 hours. It is
metabolized in the tissues with a 4- to 6- hour half-life and
is excreted in the urine.
Contraindications and Cautions
✓Anakinra is contraindicated with any known allergy to
Escherichia coli- products or to anakinra itself to prevent
hypersensitivity reactions.
✓ Caution should be used cautiously during pregnancy
and lactation because the drug may cross the placenta and
enter breast milk.
✓ Caution should be used with renal impairment,
immunosuppression, or any active infection because these
could be exacerbated by the drugs.
*There is a risk for infection whenever an interleukin receptor
antagonist is used, and the patient needs to be protected from
exposure to infections and monitored closely after any
invasive procedures.
*Immunizations cannot be given while the patient is on this drug.
Adverse Effects
• Headache, sinusitis, nausea, diarrhea, upper
respiratory and other infections
• Injection site reactions
Clinically important drug-drug interactions
• Patients who are also receiving etanercept (Enbrel) must be
monitored very closely because severe and even
life-threatening infections have occurred.
• Anakinra should not be combined with abatacept
because of the potential for serious infections.
D. Monoclonal Antibodies
✓ Laboratory-produced molecules engineered to serve as
substitute antibodies that can restore, enhance, or mimic
the immune system’s attack on cancer cells.
✓ Designed to bind to antigens that are generally more
numerous on the surface of cancer cells than healthy cells.
*-mab
Therapeutic Actions and Indications
adalimumab , certolizumab, golimumab and infliximab
- antibodies specific for human tumor necrosis factor.
VNV | 22
 - They keep the inflammatory reaction in check by
reacting with and deactivating the free-floating tumor
necrosis factor released by active leukocytes.
- They are used for treating various forms of
arthritis, Crohn’s disease and ulcerative colitis.
basiliximab and daclizumab
- specific to interleukin-2 receptor sites on activated T
lymphocytes
- They react with those sites and block cellular
response to allograft transplants.
trastuzumab
- also reacts with human epidermal growth factor
receptor 2 (HER2), a genetic defect that is seen in
certain metastatic breast cancers.
- - It is used in the treatment of metastatic breast
cancer in tumors that overexpress HER2.
palivizumab
- is specific to the antigenic site on respiratory syncytial
virus (RSV); it inactivates that virus.
- It is used to prevent RSV disease in high-risk
children.
Leronlimab
- an investigational product which is still undergoing
clinical trials for the treatment of Cancer and
Human Immunodeficiency Virus (HIV). Now, it is
also being investigated for use in the treatment of
COVID-19.
- Recently, the Philippine FDA has granted
Compassionate Special Permits (CSP) for
Leronlimab as requested by medical specialists
for the treatment of COVID-19 patients.
- It must be stressed that an approved CSP is not a
Certificate of Product Registration (CPR) or an
Emergency Use Authorization (EUA), hence it is not
an assurance of the product quality, safety, and
efficacy. No product granted with CSP can be
marketed commercially.
casirivimab and imdevimab (Regen-Cov)
• US FDA has authorized the emergency use of REGEN-
COV (casirivimab and imdevimab) co-formulated product
and REGEN-COV (casirivimab and imdevimab) supplied as
individual vials to be administered together, for the
treatment of mild to moderate COVID-19 in adults and
pediatric patients (12 years of age and older weighing at
least 40 kg) with positive results of direct SARS-CoV-2
viral testing, and who are at high risk for progression to
severe COVID-19, including hospitalization or death
Available dosage forms of REGEN-COV:
1. A single vial which contains two antibodies co-formulated in
a 1:1 ratio of casirivimab and imdevimab or
2. Individual antibody solutions in separate vials, which may be
supplied in separate cartons or in a dose pack.
REGEN-COV may be administered by intravenous infusion or
subcutaneous injection.
INTRAVENOUS INFUSION IS STRONGLY RECOMMENDED.
SUBCUTANEOUS INJECTION IS AN ALTERNATIVE ROUTE
OF ADMINISTRATION WHEN INTRAVENOUS INFUSION IS
NOT FEASIBLE AND WOULD LEAD TO DELAY IN
TREATMENT.
Pharmacokinetics
• All of the monoclonal antibodies have to be injected with the
exception of erlotinib (an oral agent)
• Can be given IV, IM, or subcutaneously.
• Rapidly metabolized in the GI tract since monoclonal
antibodies are proteins.
• Processed by the body like naturally occurring antibodies.
Contraindications and Cautions
• Contraindicated in the presence of any known allergy to
the drugs or its component to prevent hypersensitivity.
• In the presence of fluid overload which could be
exacerbated
• Must be used cautiously with fever (treat the fever before
beginning therapy)
• In patients with previous administration of the
monoclonal antibody (serious hypersensitivity reactions can
occur with repeat administration).
• Should not be used during pregnancy and lactation
unless the benefit clearly outweighs the potential risk to the
fetus or neonate.
Adverse Effects
Acute pulmonary edema (dyspnea, chest pain, wheezing),
which is associated with severe fluid retention and cytokine
release syndrome (flu -like symptoms that can progress to third
-spacing of fluids and shock)
Anticipated adverse effects: fever, chills, malaise, myalgia,
nausea, diarrhea, vomiting, and increased susceptibility to
infection and cancer development
Clinically important drug-drug interactions
Use caution and arrange to reduce the dose if a monoclonal
antibody is combined with any immunosuppressant drug
because severe immune suppression with increased infections
and neoplasms can occur.
III. Vaccines
❑ Vaccines are immunizations containing weakened or
altered protein antigens that stimulate the formation of
antibodies against a specific disease.
❑ Vaccines are used to promote active immunity.
VNV | 23

Therapeutic Actions and Recommendations
• Vaccines stimulate active immunity in people who are at high
risk for development of a particular disease.
• The vaccine needed for a patient depends on the exposure
that person will have to the pathogen.
• Exposure is usually determined by where the person lives
and his or her travel plans and work or family environment
exposures.
• Vaccines are thought to provide lifelong immunity to the
disease against which the patient is being immunized.
Pharmacokinetics
There is no pharmacokinetic information on these biologicals,
which are treated like endogenous antibodies in the body
Contraindications and Cautions
• Contraindicated in the presence of immune deficiency
because the vaccine could cause disease and the body would
not be able to respond as anticipated if it is in immunodeficient
state
• Contraindicated during pregnancy because of potential
effects to the fetus and on the success of pregnancy
Vaccines not recommended during pregnancy:
❑ Human papillomavirus (HPV) vaccine
❑ Measles, mumps, and rubella (MMR) vaccines)
❑ Live influenza vaccine (nasal flu vaccine) Varicella (chicken
pox) vaccine)
❑ Certain travel vaccines: yellow fever, typhoid fever, and
Japanese encephalitis
Note: these travel vaccines should generally not be given
during pregnancy, unless the healthcare provider determines
that the benefits outweigh the risks. Further doses of the
vaccines, if needed should be given after the pregnancy is
completed.
Limited Data Are Available about the Safety of COVID-19
Vaccines for People Who Are Pregnant
• Based on how these vaccines work in the body, experts
believe they are unlikely to pose a risk for people who are
pregnant. However, there are currently limited data on the
safety of COVID-19 vaccines in pregnant people.
Contraindications and Cautions
• Contraindicated in patients with known allergies to the
components of the vaccine (refer to each individual
component of the vaccine for specifics including eggs, where
some pathogens are cultured)
• Contraindicated in patients who are receiving immune
globulin or who have received blood or blood products
within 3 months because a serious immune reaction could
occur
• Caution should be used any time a vaccine is given to a child
with a history of febrile convulsions or cerebral injury, or
in any condition in which a potential fever can be
dangerous.
• Caution should also be used in the presence of any acute
infection.
Adverse Effects
Adverse effects are associated with the immune or
inflammatory reaction that is being stimulated:
✓ Moderate fever
✓ Rash
✓ Malaise
✓ Chills
✓ Fretfulness
✓ Drowsiness
✓ Anorexia
✓ Vomiting
✓ Irritability
✓ Nodule Formation at the injection site
✓ Severe hypersensitivity reactions
Clinically important drug-drug interactions
Vaccines should not be given with any immunosuppressant
drugs, including corticosteroids, which could alter the body’s
response to the vaccine.
IV. Immune Sera
✓ Passive immunity can be achieved by providing preformed
antibodies to a specific antigen. These antibodies are found in
immune sera, which may contain antibodies to toxins, venins,
bacteria, viruses, or even red blood cell antigenic factors.
✓ The term immune sera is usually used to refer to sera that
contain antibodies to specific bacteria or viruses.
✓ The term antitoxin refers to immune sera that have
antibodies to very specific toxins that might be released by
invading pathogens.
VNV | 24
✓ The term antivenin is used to refer to immune sera that
Bawang (Allium sativum) Popularly known as “garlic”,
have antibodies to venom that might be injected through spider it mainly reduces cholesterol
or snake bites. These drugs are used to provide early in the blood and hence,
treatment following exposure to known antigens. helps cholesterol blood
pressure.
Therapeutic Actions and Indications
• Used to provide passive immunity to a specific antigen, Bayabas (Psidium “Guava” in english. It is
which could be a pathogen, venom, or toxin. guajava) primarily used as an
antiseptic to disinfect
• May be used as prophylaxis against specific diseases
wounds. Also, it can be used
after exposure in patients who are immunosuppressed. as a mouthwash and to treat
• May be used to lessen the severity of a disease after tooth decay and gum
known or suspected exposure. infection.

Pharmacokinetics Lagundi (vitex nedundo) Known in English as the

No pharmacokinetic data are available for these biologicals. “5-leaved chaste tree”. It is
mainly for the relief of
coughs and asthma.
Contraindications and Cautions
• Contraindicated in patients with a history of severe Niyog-niyogan (Quisqualis Is a vine known as “Chinese
reaction to any immune sera or to products similar to the indica L.) honeysuckle '' It is effective
components of the sera to prevent potential serious in the elimination of
hypersensitivity reactions. intestinal worms particularly
• Should be used with caution during pregnancy because of the Ascaris and Trichina.
Only the fried matured
potential risk to the fetus, in patients with a known history of
seeds are medicinal -crack
previous exposure to the immune sera because increased risk and ingest the dried seeds
of hypersensitivity reaction occurs with each use. two hours after eating (5 to 7
seeds for children & 8 to 10
Adverse Effects seeds for adults). If one
• Adverse effects can be attributed either to the effect of dose does not eliminate the
immune sera on the immune system (rash, nausea, vomiting, worms, wait a week before
repeating the dose.
chills, fever) or to allergic reactions (chest tightness, falling
blood pressure, difficulty breathing). Sambong (Blumea English name Blumea
• Local reactions, such as swelling, tenderness, pain, or balsamifera) camphora. A diuretic that
muscle stiffness at the injection site, are very common. helps in the secretion of
urinary stones. It can also be
Clinically Important Drug-Drug Interactions used as an edema.
Caution should be used if these drugs are combined with any
immune suppressant drugs, including corticosteroids. These Tsaang Gubat (Ehretia In folkloric medicine, the
microphylla Lam.) leaves have been used as a
can alter the body’s response to the biologicals.
disinfectant wash during
childbirth, as cure for
diarrhea, as tea for general
good health and because
Tsaang Gubat has such
Alternative and Complementary fluoride content, it is used as
Therapies “Halamang Gamot” a mouth gargle for
preventing tooth decay.
10 Medicinal Plants in the Philippines endorsed by DOH Ulasimang Bato / It is effective in fighting
Akalpuko (Cassia alata) Also known as Pansit-Pansitan arthritis and grout. The
“bayabas-bayabasan” and (Peperomia pellucida) leaves can be eaten fresh
“ringworm bush” in English, (about a cupful) as salad or
this herbal medicine is used like tea. For the decoration,
to treat ringworms and skin boil a cup of clean chopped
fungal infections. leaves in 2 cups of water.
Boil for 15 to 20 minutes.
Strain, let cool and drink a
Ampalaya (Momordica Known as “bitter gourd” or
cup after meals (3 times a
charantia) “bitter melon” in English, it
day).
most known as a treatment
of diabetes (diabetes
mellitus) , for the non-insulin Yerba Buena (Clinopodium Commonly known as
dependent patients. douglasii) Peppermint, this vine is used

VNV | 25
 Precautions
as an analgesic to relieve
body aches and pain. ● Patients who have renal impairment
● History of eighth cranial nerve impairment
-can be taken internally as a ● Patients with myasthenia gravis
decoration or externally by ● Possible fetal damage when given to pregnant and
pounding the leaves and lactating women
applied directly on the
afflicted area.
Side Effects
● Nephrotoxicity (reversible injury) and ototoxicity
(irreversible injury)
● Neuromuscular blockade leading to flaccid paralysis
and fetal respiratory depression; increased risk in
Anti-Infectives patients receiving skeletal muscle relaxants.
Topic Outline: ● Hypersensitivity reactions: urticaria, pruritus.
I. Antibiotics
A. Aminoglycosides Nursing Implications
B. Cephalosporins 1. Evaluate IM and IV sites for reaction, such as
C. Fluoroquinolones abscess and thrombophlebitis by rotating injection
D. Penicillin sites and slowly injecting a dilute solution.
E. Tetracyclines 2. IM injections are frequently painful; forewarn patient.
F. Quinolones and Tetracyclines–Drug Impact on 3. Do not reconstitute ceftriaxone with any calcium
Pregnancies diluents (Ringer solution).
G. Isoniazid 4. Notify health care provider (HCP) if diarrhea occurs –
H. Macrolides can promote development of Clostridium difficile
II. Antiviral Agents infection.
III. Antifungal Agents 5. Monitor renal and hepatic studies throughout therapy.
IV. Antiprotozoal Agents 6. With medications that cause bleeding tendencies,
V. Anthelmintic Agents monitor for bleeding.
7. If GI upset occurs, patients can take medication with
I. Antibiotics food.
8. Teach patient to refrigerate oral suspensions.
9. 9. Instruct patient to report any signs of allergy (e.g.
skin rash, itching, hives.)

A. Aminoglycosides
Action
✓ Narrow-spectrum antibiotics that are primarily effective
against aerobic gram-negative bacteria
✓ Disrupts the cell synthesis of protein; cell kill is dependent
on the concentration of the medication
Uses
● Parenteral use (poorly absorbed orally) for treatment
of serious infections of the tracts; central nervous
(CNS); bone; skin and soft tissue, including burns
● Topically for application to eyes, ears, and skin.
Contraindication
● History of hypersensitivity or toxic reaction with
aminoglycoside antibiotics.
B. Cephalosporins
Action
✓ Each generation has increasing bactericidal activity to
breakdown gram-negative bacteria and anaerobes, as well as
to reach the cerebrospinal fluid
✓ Cephalosporins interfere with bacterial cell wall
synthesis and are considered broad-spectrum. The cell
weakens, swells, bursts, and dies because of increased
osmotic pressure inside the cell. Increased cephalosporin
resistance is caused by production of beta-lactamases.
Uses
Gram-negative and gram-positive bacterial infections; is not
active against viral or fungal infections
Caution
Do not cause with patients with a severe penicillin allergy
(anaphylaxis, hives)
Side Effects
(Very similar to penicillin)
● Hypersensitivity reactions: rash, pruritus, fever
● Anorexia, nausea, flatulence, vomiting, diarrhea
VNV | 26
● Can promote Clostridium difficile infection
● Severe immediate anaphylactic reactions are rare
● Ceftriaxone and cefotetan may cause bleeding
tendencies
● Taking cefotetan or cefazolin and drinking alcohol
may cause a serious disulfiram-like reaction
Nursing Implications
1. Evaluate IM and IV sites for reactions, such as
abscess and thrombophlebitis. Minimize complication
of thrombophlebitis by rotating injection sites and
slowly injecting in a dilute solution.
2. IM injections are frequently painful; forewarn patient
3. Do not reconstitute ceftriaxone with any calcium
diluents (Ringer solution)
4. Notify health care provider (HCP) if diarrhea occurs–
can promote development of Clostridium difficile
infection
5. Monitor renal and hepatic studies throughout therapy
6. With medications that cause bleeding tendencies,
monitor for bleeding
7. If GI upset occurs, patient can take medication with
food
8. Teach patient to refrigerate oral suspensions
9. Instruct patient to report any signs of allergy (e.g.,
skin rash, itching hives)
C. Fluoroquinolones
Action
● Bactericidal; inhibits DNA enzyme that interferes with
replication; is considered broad negative and some
gram-positive bacteria, but not against anaerobic
infections.
Uses
● Respiratory, urinary, GI, bone, joint, skin, and
soft-tissue infections
● Preferred drug for treatment of inhaled arthrax
Contraindications and Precautions
● Hypersensitivity, history of myasthenia gravis
● Children younger than age 18 years (systemic
treatment should be avoided)
● Pregnancy
Side Effects
● Gi upset – nausea, vomiting, diarrhea, abdominal
pain.
● Dizziness, headache, restlessness.
● Patients older than 60 years, patiens taking
glucocorticoids, and patients who have undergone a
heart, liver, or kidney transplantation are at higher risk
for tendonitis and tendon rupture.
● Photosensitivity reactions: patients should avoid
sunlight ang sunlamps.
● Avoid moxifloxacin in patients with prolonged QT
interval and hypokalemia.
Nursing Implications
1. Teach patient to avoid antacids, iron supplements =m
and milk and dairy products for at least 6 hours after
taking medication; encourage adequate fluid intake.
2. Teach patient to report any tendon pain or
inflammation.
3. Ciprofloxacinm, norfloxacin and ofloxacin can
increase warfarin levels – monitor prothrombin (PT)
time in patients taking warfarin.
4. Administer IV fluoroquinolone medications over 60
mins.
5. All oral medication dosing can be done with or without
food, except for norfloxacin, which needs to be
administered on an empty stomach.
6. Monitor for prolonged QT interval in cardiac patients
taking antidysrhythmic medications.
7. Teach patients to wear sunscreen and protective
clothing when in sunlight.
D. Penicillin (PCN)
Action
✓ Bactericidal; disrupts and weakens the cell wall, leading to
cell lysis and death
Uses
Based on type of penicillin, treatment of infections caused by
bacteria types
Narrow spectrum that are penicillinase sensitive
- Penicillin G (Bicillin), penicillin V
Narrow spectrum penicillinase resistant
(antistaphylococcal penicillins)
- Nafcillin, oxacillin, dicloxacillin
Broad-spectrum (aminopenicillins)
- Ampicillin, amoxicillin, amoxicillin/clavulanate
(Augmentin)
Extended- spectrum penicillins (antipseudomonal
penicillins)
- ticarcillin/clavulanate (Timentin),
piperacillin/tazobactam (Zosyn)
Contraindications and Precautions
● Hypersensitivity or any history of allergic reaction to
penicillin
● Caution in patients with allergy to cephalosporin,
depending on severity of allergy response
Side Effects
● Allergic response (all types) - rash, itching, hives,
anaphylaxis
● With ticarcillin - sodium overload (heart failure), and
bleeding as a result of the interference with platelet
function
VNV | 27
 Nursing Implications
1. Instruct patient to check label with regard to
administering with food
2. Instruct patient to wear medication-alert bracelet if
allergic to penicillin
3. Monitor renal and cardiac function and electrolyte
levels to avoid toxic levels
4. Monitor patient for 30 minutes when given
parenterally; administer epinephrine if anaphylaxis
occurs
5. Collect any laboratory culture specimens before
initiating penicillin therapy
6. Do not mix aminoglycosides with penicillin in the
same IV infusion–deactivates the aminoglycoside
7. Monitor for circulatory overload and bleeding
tendencies when patient receives
ticarcillin/clavulanate
E. Tetracyclines
Action
● Are bacteriostatic, broad-spectrum antibiotics that
suppress bacterial growth by inhibiting protein
synthesis. Inhibit growth of both gram negative and
gram-positive bacteria.
Uses
● Rickettsial diseases (Rocky Mountain spotted fever,
typhus, Q fever)
● Chlamydia infections, peptic ulcer disease
(helicobacter pylori infection)
● Acne, Mycoplasma pneumoniae, Lyme DIsease,
periodontal disease
● Brucellosis, cholera, anthrax Precautions
● May exacerbate kidney impairment.
● Do not give to children younger than age 8 years or
pregnant women.
● May cause staining of developing teeth.
Side Effects
● Alteration of vaginal and intestinal flora resulting in
diarrhea and GI upset
● Photosensitivity, superinfection (Clostridium difficile)
Nursing Implications
1. Monitor carefully for diarrhea; it may indicate a
superinfection of bowel (Clostridium difficile or
Staphylococci).
2. Check dose and rate when delivering intravenously.
3. Take on an empty stomach; antacids, milk products,
and iron supplements should not be consumed until at
least 2 hours after dose was taken.
4. To avoid discoloration of permanent teeth, do not
administer to pregnant women or children younger
than age 8 years.
5. Use a straw in liquid preparations.
6. Wear sunscreen and protective clothing.
F. Quinolones and Tetracyclines–Drug Impact on
Pregnancies
FDA Pregnancy Risk Categories
Category A
- Remote risk of fetal harm
Category B
- Slightly more risk than category A
Category C
- Greater risk than category B
Category D
- Proven risk of fetal harm; labeled as warning
Category X
- Proven risk of fetal harm; label as contraindicated
Contraindications
● Women who are pregnant need to take cautious
approach to drug therapy during pregnancy. The
health care provider is responsible for ordering
medications that are safe and appropriate for the
ever-changing physiologic dynamics during
pregnancy
● Contraindicated medications can cause detrimental
changes in the mother, fetus, and fetal environment
● Quinolones (category C) and tetracyclines (category
D) are not routinely used during pregnancy
Nursing Implications
1. Evaluate patients level of understanding about her
physiologic, mental, and emotional conditions
2. Teach patient to call the prenatal clinic or physicians
office before using any over the counter medications
3. The patient should not take any medications that have
not been specifically approved or prescribed by her
health care provider
4. Advise patient to avoid all alcoholic beverages during
the term of the pregnancy
5. Advise patient to report any unusual signs or
symptoms of reactions to the treatment plan
Think of the mnemonic MCAT to remember other
antibiotics contraindicated in pregnancy
M - Metronidazole
- contraindicated in first trimester; category B- second
and third trimester
C - Chloramphenicol
- Category C
A - Aminoglycoside
- Category C
T - Tetracycline
- Category D
VNV | 28
 G. Isoniazid Contraindications and Precautions
Action ● Liver dysfunction
● Bacteriostatic to “resting organisms” and bactericidal ● Avoid macrolides in patients with preexisting QT
to actively dividing organisms. Interferes with prolongation,and in those taking drugs that can
biosynthesis of bacterial protein, nucleic acid, and increase erythromycin levels (e.g. verapamil,
lipids. diltiazem, HIV protease inhibitors, and azole
Uses antifungal drugs).
● Treatment of active and latent tuberculosis
● Preventive in high-risk persons (e.g. those with a Side Effects
positive tuberculosis [TB] skin test or exposure) ● Diarrhea nausea, vomiting, abdominal pain.
● High levels of all forms of erythromycin can prolong
Contraindications the QT interval, thereby posing a risk of potentially
● History of isoniazid-associated hypersensitivity fatal cardiac dysrhythmias.
reaction.
● Alcoholics and patients with preexisting liver problems Nursing Implications
● When used to treat active TB, it must be used with 1. Take medication 1 hour before or 2 hours after food or
another antitubercular agent. antacids.
2. Aluminum and magnesium antacids reduce the rate of
Side Effects absorption but not extent.
● Dose-related peripheral neuropathy, clumsiness, 3. Observe for development of signs of superinfection
unsteadiness, muscle ache 4. Instruct patient to take prescribed course of therapy,
● Epigastric distress jaundice, drug-induced hepatitis although symptoms may improve or disappear.
5. IV preparations are infused slowly over 60 minutes.
Nursing Implications 6. Patients taking erythromycin and all of its forms –
1. Teach patient to take orally on an empty stomach 1 monitor warfarin levels and watch for prolonged QT
hour before or 2 hours after meals. interval.
2. Depletes vitamin B6 (pyridoxine) and will need
supplementation during treatment.
3. Peripheral neuritis, the most common adverse effect, Anti-In ammatory, Antiarthritis, and
is preceded by paresthesias (e.g. numbness, tingling, Related Agents
burning, pain) of the feet and hands.
Topic Outline:
4. Teach patients to reduce or eliminate consumption of
I. Salicylates
alcohol to reduce the risk of hepatotoxicity.
II. Nonsteroidal Anti-Inflammatory Drugs
5. Anti Tuberculosis treatment always involves two or
III. Related Agent (Acetaminophen)
more medications; INH is often combined with
IV. Anti-arthritis Agents
rifampin.
V. Anti-Rheumatic Drugs
H. Microlides Glossary of Terms
Action Analgesic
● Broad-spectrum antibiotic that binds with ribosome al ● compound with pain-blocking properties, capable of
receptor sites in susceptible organisms to inhibit producing analgesis
bacterial protein synthesis.
Anti-inflammatory agents
Uses ● drugs that block the effects of the inflammatory
There are 3 main drugs: response
➔ Erythromycin
➔ Azithromycin Antipyretic
➔ Clarithromycin ● blocking fever, often by direct effects of the
inflammatory response
● Treats upper respiratory tract, ear, and skin infections;
syphilis (for penicillin-sensitive patients); cholera; and Chrysotherapy
chancroid. ● treatment with gold salts, gold is taken up by
● Azithromycin is drug of choice for Chlamydia macrophages which then inhibit phagocytosis; it is
trachomatis reserved for use in patients who are unresponsive to
conventional therapy

VNV | 29
 Inflammatory response
● the body’s nonspecific response to cell injury,
resulting in pain, swelling, heat, and redness in the
affected area
Nonsteroidal Anti-inflammatory drugs (NSAIDs)
● drugs that block prostaglandin synthesis and act as
anti-inflammatory, antipyretic, and analgesic
Salicylates
● salicylic acid compounds, used as anti-inflammatory,
antipyretic, and analgesic agents; they block the
prostaglandin system
Salicylism
● syndrome associated with high levels of
salicylates-dizziness, ringing in the ears, difficulty
hearing, nausea, vomiting, diarrhea, mental
confusion, and lassitude
I. Salicylates
✓ Salicylates are popular anti-inflammatory agents
not only because of their ability to block the inflammatory
response, but also because of their antipyretic (fever-blocking)
and analgesic (pain-blocking) properties.
✓ Salicylates are some of the oldest anti- inflammatory drugs
used. They were extracted from willow bark, poplar trees, and
other plants by ancient people to treat fever, pain, and what we
now call inflammation.
✓ Generally available without prescription and are
relatively nontoxic when used as directed.
Selected Drugs
✓ aspirin
✓ balsalazide
✓ choline magnesium trisalicylate
✓ diflunisal
✓ mesalamine
✓ olsalazine
✓ salsalate
✓ sodium thiosalicylate
Therapeutic Actions and Indications
• Inhibits the synthesis of prostaglandin, an important
mediator of the inflammatory reaction.
• Indicated for the treatment of mild to moderate pain, fever,
and numerous inflammatory conditions, including
rheumatoid arthritis and osteoarthritis.
Pharmacokinetics
• Readily absorbed directly from the stomach, reaching levels
within 5 to 30 minutes. They are metabolized in the liver and
excreted in the urine with a half life of 15 minutes to 12 hours,
depending on the salicylate.
• Salicylates don’t cross the placenta and enter breast milk;
they are not indicated during pregnancy and lactation because
of the potential adverse effects on the neonate and associated
bleeding risks for the mother.
Contraindications and Cautions
• Contraindicated in the presence of known allergy to
salicylates, other nonsteroidal anti- inflammatory drugs
(NSAIDs)
• Bleeding abnormalities because of the changes in platelet
aggregation associated with these drugs
• Impaired renal function because the drug is excreted in
urine
• Chicken pox or influenza because of the risk of Reye’s
syndrome in children and teenagers
• Surgery or other invasive procedures scheduled within
one week because of the increased
risk of bleeding
• Pregnancy or lactation because of the potential adverse
effects on the neonate or mother.
Adverse Effects
• Adverse effects may be the result of direct drug effects on the
stomach (nausea, dyspepsia, heartburn, epigastric, discomfort)
and on clotting system (blood loss and bleeding abnormalities)
• Salicylism can occur with high levels of aspirin: dizziness,
ringing in the ears, difficulty hearing, nausea, vomiting,
diarrhea, mental confusion, and lassitude can occur.
• Acute Salicylate toxicity may occur at doses of 20 to 25 g or
4g in children.
• Signs of salicylate toxicity: hyperpnea, tachypnea,
hemorrhage, excitement, confusion, pulmonary edema,
convulsions, tetany, metabolic acidosis, fever, coma,
cardiovascular, renal, and respiratory collapse.
Clinically Important Drug-Drug Interactions
Interacts with many other drugs. The list of interacting drugs in
each drug monograph in a nursing drug guide should be
consulted and the prescriber consulted before adding or
removing a salicylate from any drug regimen.
II. Nonsteroidal Anti-Inflammatory Drugs (NSAIDS)
NSAIDs provide strong anti-inflammatory and analgesic
effects without the adverse effects associated with the
Corticosteroids.
VNV | 30
Linked to an increased risk of CV events and death
as well as increased bleeding in the GI tract.
This group of drugs include:
1. Propionic acids (e.g. ibuprofen, naproxen)
2. Acetic acids (e.g. diclofenac, indomethacin)
3. Fenamates (e.g. mefenamic acid)
4. Oxicam derivatives (e.g. meloxicam)
5. Cyclooxygenase-2 (COX-2) inhibitors (e.g. celecoxib)
Related agent: acetaminophen (Tylenol)
Therapeutic Actions and Indications
● The anti-inflammatory, analgesic, and antipyretic
effects of the NSAIDs are largely related to
inhibition of prostaglandin synthesis.
● NSAIDs block two enzymes, known as COX-1 and
COX2. COX-1 is present in all tissues and seems to
be involved in many body functions, including blood
clotting, protecting the stomach lining, and
maintaining sodium and water balance in the kidney.
● COX-1 turns arachidonic acid into prostaglandins as
needed in a variety of tissues.
● COX-2 is active at sites of trauma or injury when more
prostaglandins are needed, but it does not seem to be
involved in the other tissue functions. By interfering
with this part of the inflammatory reaction, NSAIDs
block inflammation before all the signs and symptoms
can develop.
● Most NSAIDs also block various other functions of the
prostaglandins, including protection of the stomach
lining, regulation of blood clotting, and water and salt
balance in the kidney.
● The COX-2 inhibitors are thought to act only at
sites of trauma and injury to block the
inflammatory reaction more specifically. The
adverse effects associated with most NSAIDs are
related to blocking of both enzymes and changes
in the functions that they influence---GI integrity,
blood clotting, and sodium and water balance.
● The COX-2 inhibitors are designed to affect only the
activity of COX-2, the enzyme that becomes active in
response to trauma and injury. They do not interfere
with COX-1, which is needed for normal functioning of
these systems. Consequently, these drugs should not
have the associated adverse effects seen when both
COX-1 and COX-2 are inhibited. Experience has
shown that the COX-2 inhibitors still have some effect
on these other functions, and patients should still be
evaluated for GI effects, changes in bleeding time,
and water retention. Recent studies suggest that they
may block some protective responses in the body,
such as vasodilation and inhibited platelet clumping,
which is protective if vessel narrowing, or blockage
occurs; blocking this effect could lead to CV problems.
● The NSAIDs are indicated for relief of the signs
and symptoms of rheumatoid arthritis and
osteoarthritis, for relief of mild to moderate pain,
for treatment of primary dysmenorrhea, and for
fever reduction.
Pharmacokinetics
The NSAIDs are rapidly absorbed from the GI tract, reaching
peak levels in 1 to 3 hours. They are metabolized in the liver
and excreted in the urine.
NSAIDs cross the placenta and cross into breast milk.
Therefore, they are not recommended during pregnancy and
lactation because of the potential adverse effects on the fetus
or neonate.
Contraindications and Cautions
● Contraindicated in the presence of allergy to any
NSAID or salicylate, and celecoxib is also
contraindicated in the presence of allergy to
sulfonamides.
● CV dysfunction or hypertension because of the
varying effects of the prostaglandins
● In patients with peptic ulcer or known GI bleeding
because of the potential to exacerbate the GI
bleeding
● During pregnancy or lactation because of potential
adverse effects on the neonate or mother.
● Caution should be used with renal or hepatic
dysfunction, which could alter the metabolism and
excretion of these drugs
● Caution should be used with any other known
allergies, which indicate increased sensitivity.
Adverse Effects
● GI: nausea, dyspepsia, GI pain, constipation,
diarrhea, or flatulence, GI bleeding (often is a cause
of discontinuation of the drug)
● CNS: Potential Headache, dizziness, somnolence,
and fatigue
● HEMA: Bleeding, platelet inhibition, hypertension, and
even bone marrow depression has been reported with
chronic use and probably are related to the blocking
of prostaglandin activity.
● Rash and mouth sores may occur, and anaphylactoid
reactions ranging up to fatal anaphylactic shock in
cases of severe hypersensitivity.
Clinically important Drug-Drug Interactions
● Decreased diuretic effect when NSAIDs are taken
with loop diuretics.
● Potential for decreased antihypertensive effect of
beta-clockers if combined with NSAIDs
● Lithium toxicity, especially when combined with
ibuprofen. Patients who receive these combinations
should be monitored closely, and appropriate dose
adjustments should be made by the prescriber.
VNV | 31
 III. Acetaminophen
● Acetaminophen (Tylenol) is used to treat moderate to
mild pain and fever and often is used in place of
NSAIDs or salicylates.
● widely available OTC and is found in many
combination products.
● Can be extremely toxic, causes severe liver toxicity
that can lead to death when taken high doses.
● most frequently used drug for managing pain and
ever in children.
Therapeutic Actions and Indications
• Acetaminophen acts directly on the thermoregulatory
cells in the hypothalamus to cause sweating and
vasodilation; this in turn causes the release of heat and
lowers fever.
• Indicated for the treatment of pain and fever associated with a
variety of conditions, including influenza; for the prophylaxis of
children receiving diphtheria-pertussis-tetanus immunizations
(aspirin may mask Reye syndrome in children); and for the
relief of musculoskeletal pain associated with arthritis.
Pharmacokinetics
• Rapidly absorbed from the GI tract, reaching peak levels in
0.5 to 2 hours. It is extensively metabolized in the liver and
excreted in the urine, with a half-life of about 2 hours.
• Caution should be used in patients with hepatic or renal
impairment, which could interfere with metabolism and
excretion of the drug, leading to toxic levels.
• Acetaminophen crosses the placenta and enters breast
milk; it should be used cautiously during pregnancy or
lactation because of the potential adverse effects on the fetus
or neonate.
Contraindications and Cautions
• Contraindicated in the presence of allergy to
acetaminophen because of the risk of hypersensitivity
reactions.
• Must be used cautiously in pregnancy or lactation
because of the potential for adverse effects on the fetus or
baby
• Use with caution in patients with hepatic dysfunction or
chronic alcoholism because of the associated toxic effects on
the liver.
Adverse Effects
• Headache, hemolytic anemia, renal dysfunction, skin rash,
and fever.
• Hepatotoxicity with chronic use and overdose is related
to direct toxic effects on the liver. When overdose occurs,
acetylcysteine can be used as an antidote. Life support
measures may also be necessary.
Clinically Important Drug-Drug Interactions
• Increased risk of bleeding with oral anticoagulants
because of effects on the liver;
• Toxicity with chronic ethanol ingestion because of toxic
effects on the liver;
• Hepatotoxicity with barbiturates, carbamazepine,
hydantoins, or rifampin. These combinations should be
avoided, but if they must be used, appropriate dose adjustment
be made and the patient should be monitored closely.
IV. Antiarthritis Agents
• Arthritis is a potentially debilitating inflammatory process in
joints causing pain and bone deformities.
• Antiarthritis drugs include Gold compounds, which
are used to prevent and suppress arthritis in selected patients
with rheumatoid arthritis.
Selected Drugs:
1. auranofin (Ridaura)
2. gold sodium thiomalate (Aurolate)
Gold Compounds
Some patients with rheumatic inflammatory conditions do not
respond to the usual anti- inflammatory therapies, and their
conditions worsen despite weeks or months of standard
pharmacological treatment. Some of these patients respond to
treatment with gold salts, also known as chrysotherapy.
Pharmacokinetics
• Absorbed at varying rates, depending on their route of
administration.
• Widely distributed throughout the body but seem to
concentrate in the hypothalamic- pituitary-adrenocortical
system and in the adrenal and renal cortices. Gold salts
are excreted in urine and feces.
• Gold compounds cross the placenta and into breast milk.
They have shown to be teratogenic in animal studies and
should not be used during pregnancy and lactation. Other
methods of feeding the baby should be used and barrier
contraceptives are recommended to women of
childbearing age if gold therapy is needed.
Contraindications and Cautions
Gold salts can be quite toxic and are contraindicated in the
presence of any known allergy to gold, severe diabetes,
congestive heart failure, severe debilitation, renal or hepatic
impairment, hypertension, blood dyscrasias, recent radiation
treatment, history of toxic levels of heavy metals, and
pregnancy or lactation.
Adverse Effects
• Adverse effects are probably related to their deposition in the
tissues and effects at that local level: stomatitis, glossitis,
gingivitis, pharyngitis, laryngitis, colitis, diarrhea, and other GI
inflammation
• Gold bronchitis, interstitial pneumonitis
• Bone marrow depression
• Vaginitis and nephrotic syndrome
• Dermatitis, pruritus, and exfoliative dermatitis
• Allergic reactions ranging from flushing, fainting, and
dizziness to anaphylactic shock
VNV | 32
 Clinically Important Drug-Drug Interactions
NSAIDs should not be combined with penicillamine,
antimalarials, cytotoxic drugs, or immunosuppressive
agents other than low-dose corticosteroids because of the
potential for severe toxicity.
V. Disease-Modifying Antirheumatic Drugs
Other antiarthritis called disease-modifying antirheumatic drugs
(DMARDs) are available for treating arthritis and aggressively
affect the process of inflammation.
Many rheumatologists are selecting DMARDs early in the
diagnoses before damage to the joints has occurred, because
they alter the course of the inflammatory process.
Two types of DMARDs:
A. Tumor Necrosis Factor Blockers (TNF)
B. Other Disease-Modifying Antirheumatic Drugs
Tumor Necrosis Factor Blockers:
1. adalimumab (Humira)
2. certolizumab (Cimzia)
3. etanercept (Enbrel)
4. golimumab (Simponi)
5. infliximab (Remicade)
*-mab
Therapeutic Actions and Indications
✓ TNF blockers act to decrease the local effects of TNF, a
locally released cytokine that can cause the death of tumor
cells and stimulate a wide range of proinflammatory activities.
The actions of this cytokine when inflammation occurs within a
joint capsule can lead to the destruction of bone and the
malformation of joints that is associated with arthritis.
Drugs that block that action of TNF slow the inflammatory
response and the joint damage associated with arthritis.
Drugs that block that action of TNF slow the inflammatory
response and the joint damage associated with it.
TNF blockers are indicated for the treatment of the disease
conditions:
1. rheumatoid arthritis
2. polyarticular juvenile arthritis
3. psoriatic arthritis
4. plaque psoriasis
5. ankylosing spondylitis
Adalimumab, certolizumab, and infliximab are also used in
Crohn’s disease and ulcerative colitis.
Pharmacokinetics
• TNF blockers must be given subcutaneously with the
exception of infliximab which is given IV. They have a slow
onset, usually peaking in 48-72 hours.
• Primarily excreted in the tissues and have very long half-lives
ranging from 115 hours to 2 weeks.
• TNF blockers cross the placenta and enter breast milk,
so use in pregnancy and breastfeeding should be
discouraged.
Contraindications and Cautions
• Cannot be used in anyone with acute infection, cancer,
sepsis, tuberculosis, hepatitis, myelosuppression, or
demyelinating disorders because they block the body’s
immune/inflammatory response and serious reactions
could occur.
• Etanercept cannot be used with a history of allergy to
Chinese hamster ovary products because it is made from
these products.
• Should not be used during pregnancy and lactation
because of potential effects on the fetus or neonate.
• Caution should be used with renal or hepatic disorders,
heart failure, and latex allergies to prevent adverse
reactions.
Adverse Effects
• TNF blockers come with black box warning about the risk of
serious to fatal infections and the development of lymphomas
and other cancers. Patients need to be screened and
monitored accordingly.
• Demyelinating disorders including multiples sclerosis and
various neuritis conditions.
• Myocardial Infarction (MI), heart failure, and hypotension
• Irritation at the site of injection
Clinically Important Drug-Drug Interactions
Use of any other immune suppressant drugs with TNF
blockers increases the risk of serious infections and
cancer. Live vaccines should not be given while on these
drugs.
Other Disease-Modifying Antirheumatic Drugs
Drugs used when patients do not respond to conventional
therapy:
1. anakinra (Kineret)
2. leflunomide (Arava)
3. tofacitinib (Xeljanz)
4. penicillamine (Depen)
Drugs used to directly decrease pain in joints affected by
arthritis:
1. hyaluronidase derivative (Synvisc)
2. sodium hyaluronate (Hyalgan)
Additional drugs used to modify the disease process in
rheumatoid arthritis:
1. Antineoplastic drugs methotrexate and
cyclophosphamide
2. T cell suppressor abatercept (Orencia)
3. Immune Modulators cyclophosphorine A and
azathioprine
VNV | 33
The Internet as a Drug Information
There are various indexing databases available through
Resource the Internet, including:
Topic Outline: 1. Adis International
I. Evaluating Information on the Internet 2. CINAHL
II. Internet Sources of Information 3. PubMed
A. Primary 4. OVID
B. Secondary 5. Web of Science
C. Tertiary 6. Embase International Pharmaceutical Abstracts
7. Google Scholar
Evaluating Information on the Internet 8. Clin-Alert
Due to the unregulated nature of the Internet, it is of utmost 9. Iowa Drug Information Service.
importance to critically evaluate information obtained by this The majority of these resources require a subscription;
method. PubMed and Google
Scholar do not.
Ten Key Questions to Ask When Evaluating a Website
Tertiary Resources
Tertiary resources, a summary of primary resources, are
abundant on the Internet. The difficulty in determining which
sources to utilize often arises due to the significant amount of
information retrieved following an Internet search engine query.
As with print versions of tertiary resources (i.e., textbooks or
review articles), online resources are only as reliable as the
information they are based on.

Whenever using information found on a Web site, it is

critical to locate the date of the last update. This will
eliminate the possibility of basing a decision on outdated
evidence.

Select Open-Access Drug Information Sources Available

via the Internet

Internet Sources of Information

Primary Resources
• Primary resources include published meta-analyses,
randomized controlled trials, observational trials, and case
reports. The information obtained from this literature is the
basis for evidence-based practice.
• Primary resources are generally the most up-to-date
information available. Practitioners have the opportunity to
review the information and form their own opinion of what the
evidence supports. On the other hand, practitioners must be
proficient in interpreting and evaluating the strength of medical
literature. Additionally, decisions should not be based on a
single piece of evidence, but rather on a compilation of all
available evidence.

Secondary Resources
Secondary resources direct one to primary resources. Many
secondary resources such as MEDLINE/PubMed provide
bibliographic and/or abstract Information.

VNV | 34

Current Trends and Clinical Alerts in
Nursing Pharmacology
Topic Outline:
I. Technological Advances to Prevent Medication Errors
II. Performing Medication Reconciliation
III. Controlled Substances
Technological Advances to Prevent Medication Errors
1. Computerized physician order entry (CPOE)
• A system that allows prescribers to electronically enter orders
for medications, thus eliminating the need for written orders.
• CPOE increases the accuracy and legibility of
medication orders; the potential for the integration of clinical
decision support; and the optimization of prescriber, nurse, and
pharmacist time (Agrawal, 2009).
• Decision support software integrated into a CPOE system
can allow for the automatic checking of drug allergies, dosage
indications, baseline laboratory results, and potential drug
interactions.
• When a prescriber enters an order through CPOE, the
information about the order will then transmit to the pharmacy
and ultimately to the MAR.
2. Electronic barcodes on medication labels and
packaging
A patient’s MAR (medication administration record) is entered
into the hospital’s information system and encoded into the
patient’s wristband, which is accessible to the nurse through a
handheld device. When administering a medication, the nurse
scans the patient’s medical record number on the wristband,
and the bar code on the drug. The computer processes the
scanned information, charts it, and updates the patient’s MAR
record appropriately (Poon et al., 2010).
3. Automated medication dispensing systems (AMDS)
Provide electronic automated control of all medications,
including narcotics. Each nurse accessing the system has a
unique access code.
The nurse will enter the patient’s name, the medication, the
dosage, and the route of administration. The system will then
open either the patient’s individual drawer or the narcotic
drawer to dispense the specific medication.
If the patient’s electronic health record is linked to the AMDS,
the medication and the nurse who accessed the system will be
linked to the patient’s electronic record.
Performing Medication Reconciliation
Medication reconciliation is a process in which medications are
“reconciled” at all points of entry and exit to/from a health care
entity. Medication reconciliation requires patients to provide a
list of all the medications they are currently taking (including
herbals and over-the-counter drugs). The prescriber is then to
assess those medications and decide if they are to be
continued upon Hospitalization.
Medication reconciliation was designed to ensure that there
are no discrepancies between what the patient was taking at
home and in the hospital. Medication reconciliation is to occur
at entry into the facility, upon transfer from surgery, or into or
out of the intensive care unit and at discharge.
High-Alert Medications
• “High-alert” medications have been identified as those that,
because of their potentially toxic nature, require special care
when prescribing, dispensing, and/ or administering.
• High-alert medications are not necessarily involved in more
errors than other drugs; however, the potential for patient harm
is higher.
• Medication errors also result from the fact that there are large
numbers of drugs that have similarities in spelling and/or
pronunciation (i.e., look-alike or sound-alike names).
• Several acronyms have been created to refer to these drugs,
including SALAD (sound- alike, look-alike drugs) and LASA
VNV | 35
(look-alike, sound-alike). Mix-ups between such drugs are
Pharmacodynamics vs. Pharmacokinetics
most dangerous when two drugs from very different therapeutic
classes have similar names. This can result in patient effects Topic Outline:
that are grossly different from those intended as part of the I. Pharmacodynamics
drug therapy II. Pharmacokinetics
III.Institutional Policies and Guidelines on Safe Drug
Administration
Pharmacodynamics
✓ the study of the interactions between the chemical
components of living systems and the foreign chemicals,
including drugs that enter systems.
✓ When a new chemical enters the system, multiple changes
in and interferences with cell functioning may occur. To avoid
such problems, drug development works to provide the most
effective and least toxic chemicals for the therapeutic use.

Drug usually work in one of four ways:

1. To replace or act as substitutes for missing chemicals
2. To increase or stimulate certain cellular activities
3. To depress or slow cellular activities
Controlled Substances 4. To interfere with the functioning of foreign cells, such as
invading microorganisms orneoplasms leading to cell death

Pharmacokinetics
involves the study of absorption, distribution, metabolism
(biotransformation), and excretion of drugs.

In clinical practice, pharmacokinetic considerations

include the ff:
1. onset of drug action:
- how long it will take to see the beginning of the
therapeutic effect
2. drug half-life, timing of the peak effect:
how long will it take to see the maximum effect of the drugs
3. duration of drug effects
- how long the patient will experience the drug effects)
4. metabolism or the biotransformation of the drugs
5. site of excretion

Institutional Policies and Guidelines on Safe Drug

Administration
Disclaimer: Every healthcare institution has a different set of
policies. Always review the hospital protocol before
✓ Drugs with abuse potential are called controlled administering medications.
substances. The prescription, distribution, storage, and use of
these drugs are closely monitored by the DEA to decrease
substance abuse of prescribed medications. Each prescriber
has a DEA number, which allows the DEA to monitor
prescription patterns and possible abuse.
✓ A nurse should be familiar with not only the DEA guidelines
for controlled substances but also the local
policies and procedures, which might be even more rigorous.

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 Guidelines for Safe Medication Administration -
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Goodluck ^-^

Safety Considerations
1. Plan medication administration to avoid disruption:
a. Dispense medication in a quiet area.
b. Avoid conversation with others.
c. Follow agency’s no-interruption zone policy.
2. Prepare medications for ONE patient at a time.
3. Follow the SEVEN RIGHTS of medication preparation.
4. Check that the medication has not expired.
5. Perform hand hygiene.
6. Check room for additional precautions (e.g. Contact
precautions, droplet precautions)
7. Introduce yourself to patient.
8. Confirm patient ID using two patient identifiers (e.g., name
and date of birth) AND check against MAR.
9. Check allergy band for any allergies and ask patient about
type and severity of reaction.
10. Complete necessary focused assessments, lab values,
and/or vital signs, and document on MAR.
11. Provide patient education as necessary.
12. If a patient questions or expresses concern regarding a
medication, stop and do not administer.

VNV | 37