PHARMACOLOGY
facilitate the agglomeration of powder into
Definition of Terms
pharmakon (Gk) = drugs logos (Gk)= science
✓ Science that deals with the study of drugs,
their history, sources, physical and chemical
properties and their actions on living organisms.
DRUGS
Droog (Dutch) = dry
✓ Chemical substances that have an effect on
living organisms
✓ In history, dried plants were the greatest
source of drugs, thus the word was applied
MEDICINES
✓ Therapeutic drugs
✓ Drugs that are used in the prevention or
treatment of diseases
3 phases:
1. Pharmaceutic - preparation, use and
dispensing of medicine
2. Pharmacokinetic
3. Pharmacodynamic
Pharmaceutic
✓ Drug in solid form must disintegrate into
small particles to dissolve into a liquid
✓ Tablets are not 100% drug!!!
EXCIPIENTS - substances used in drug
preparation to allow the drug to take on
particular size shape and taste.
Common Excipients for Tablets
> Diluents: essential excipients for tablets to
increase the weight or volume.
> Binders: vital excipients for tablets to
granules.
Coloring agent Flavoring agent
Sweetener or Sweetening agent
BAD CHOICE of excipients = INTOXICATION or
ADVERSE EFFECTS
*Epileptic patients in Australia in the late 1960s
who were taking phenytoin capsules. The
calcium sulphate used as a diluent in the
capsule had been replaced by lactose.
Drugs are both disintegrated and absorbed
faster in acidic fluids.
• Very young and the elderly have less gastric
acidity
Enteric coated drugs RESIST disintegration in
the gastric acid of the stomach
Food in the GI tract may interfere with the
dissolution and absorption of certain drugs
Pharmacotherapeutics
✓Study of how drugs may best be used in the
treatment of illnesses
✓Study of which drug would be most
appropriate or least appropriate to use for a
specific disease; what dose would be required;
etc.
Pharmacognosy
✓ The study of drugs derived from herbal and
other natural (plant and animal) drug sources
✓Studying compositions of natural substances
helps to gain knowledge for developing
synthetic versions
Toxicology
✓Study of poisons and poisonings
✓All drugs have the potential to become toxic. Ex: Imodium

Drug Uses: 4-(4-chlorophenyl)-4-hydroxy-N,N-dimethyl-, -

diphenyl-1-piperidinebutanamide
✓Symptomatic treatment
GENERIC NAME
✓Prevention
✓ Universally accepted name of a drug that
✓ Diagnostic drugs denotes its formularies.
✓Curative ✓Common name; simpler than chemical name.
✓Health maintenance ✓ Written with first letter NOT capitalized.
✓Contraception Ex: Imodium

✓Dosage Forms loperamide HCI

✓Tablets OFFICIAL NAME

✓ Capsules Suppositories ✓ The name under which the drug is listed by

the U.S. Food and Drug Administration.
✓Liquids
The FDA is empowered by federal law to name
✓Creams/Ointments the drug for human use in the U.S.
✓Parenteral Product Packaging BRAND NAME

✓ Ampules ✓ Trade mark; proprietary name.

✓Vials: either single or multiple dose ✓ Is always followed by which indicate that the
name is registered and that its use is restricted
✓Pre-filled syringes
to the owner who is usually the manufacturer.
DRUG NAMES
✓ Written with first letter capitalized.
✓ Chemical name
Ex:
✓ Generic name
✓4-Thia-1-azabicyclo [3.2.0] heptane-2
✓ Official name carboxylic acid, 6-[(aminophenylacetyl) amino]-
3,3-dimethyl-7-oxo-, [2S [2a,5a,63(S*)]]
✓ Brand name
✓ampicillin
CHEMICAL NAME
Ampicillin, USP
✓ It denotes the exact chemical constitution of
the drug and the exact placing of its atoms or ✓Polycillin
molecular placing. PRESCRIPTION DRUGS

✓ Drugs that require an order by a health

professional who is licensed to prescribed
✓ Identified by: "PX only"
NONPRESCRIPTION DRUGS
✓OTC drugs (over-the-counter)
✓Sold without prescription in a pharmacy or
the health section of department or grocery
stores.
ILLEGAL DRUGS
✓ Recreational drugs
✓ Drugs of chemical substances used for non-
therapeutic purposes.
✓ They are obtained illegally or have not
received approval for use by the FDA.
FUNDAMENTAL CONCEPTS OF
PHARMACOLOGY
Pharmacokinetics- deals with a drug's actions
as it moves through the body.
Kinetics= movement
The term pharmacokinetics is derived from the
ancient Greek words:
pharmakon-drug
kinetics - putting in motion
From the moment that a drug enters the body,
the body recognizes it and processes it in a
unique way, according to the individual
characteristics of the drug.
Therefore…
Pharmacokinetics is the study of how the body
reacts to the presence of the drug!
The LADME Scheme
L= Liberation, the release of the drug from it's
dosage form.
A= Absorption, the movement of drug from the
site of administration to the blood circulation.
D= Distribution, the process by which drug
diffuses or is transferred from intravascular
space to extravascular space.
M = Metabolism, the chemical conversion or
transformation of drugs into compounds which
are easier to eliminate.
E= Excretion, the elimination of unchanged drug
or metabolite from the body via renal, biliary, or
pulmonary processes.
LADME processes can be divided into 2 classes:
1. Drug Input
2. Drug output
Input processes
L- Liberation, the release of the drug from its
dosage form.
A- Absorption, the movement of drug
from the site of administration to the
blood circulation.
The term commonly used to describe the rate
and extent of drug input is bioavailability
Drugs administered by intravenous routes
exhibit essentially 10036 bioavailability
Output processes
D- Distribution, the process by which drug
diffuses or is transferred from intravascular
space to extravascular space.
M- Metabolism, the chemical conversion or
transformation of drugs into compounds which
are easier to eliminate.
E- Excretion, the elimination of unchanged drug
or metabolite from the body via renal, biliary, or
pulmonary processes.
Liberation
It is the process in which a pharmaceutical
substance is released from the formulation it is
delivered in. This must occur before the drug
can be absorbed into the body.
Absorption
Drug absorption covers a drug's progress from
the time it's administered, through its passage
to the tissues, until it reaches systemic
circulation.
On a cellular level, drugs are absorbed by
several means-primarily through active or
passive transport.
The lazy way
Passive transport requires NO cellular energy
because diffusion allows the drug to move from
an area of higher concentration to one of lower
concentration.
Small molecules diffuse across membranes and
stops when drug concentration on both sides of
the membrane is equal.
Using muscle
Active transport requires cellular energy to
move the drug from an area of lower
concentration to one of higher concentration.
Absorbs electrolytes, such as sodium and
potassium, as well as some drugs such as
levodopa.
Taking a bite
Pinocytosis is a unique form of active transport
that occurs when a cell engulfs a drug particle.
Pinocytosis is commonly employed to transport
fat-soluble vitamins (A, D, E, & K).
Pinocytosis- Takes in fluids and solute.
Phagocytosis- Takes in larger substances
(bacteria).
Watch the speed limit!
If only a few cells separate the active drug from
the systemic circulation, absorption will occur
rapidly and the drug will quickly reach
therapeutic levels in the body.
Typically, absorption occurs within seconds or
minutes when a drug is administered
sublingually, IV., or by inhalation
**Drugs given under the tongue, I.V., or by
inhalation are quickly absorbed.**
Not so fast
Absorption occurs at a slower rate when drugs
are administered by the oral, I.M., or subQ
routes because the complex membrane systems
of Gl mucosal layers, muscle, and skin delay
drug passage.
At a snail's pace
At the slowest absorption rates, drugs can take
several hours or days to reach peak
concentration levels. A slow rate usually occurs
with rectally administered or sustained-release
drugs.
Not enough time
Other factors can affect how quickly a drug is
absorbed.
For example, most absorption of oral drugs
occurs in the small intestine.
Surgically removed large sections of the small
intestine.
Look to the liver
Drugs absorbed by the small intestine are
transported to the liver before being circulated
to the rest of the body.
The liver may metabolize much of the drug
before it enters the circulation. This mechanism
is referred to as the first-pass effect.
Liver metabolism may inactivate the drug; if so,
the first-pass effect lowers the amount of active
drug released into the systemic circulation.
Therefore, higher drug dosages must be
administered to achieve the desired effect.
Slowed by pain and stress
This may be due to a change in blood flow,
reduced movement through the Gl tract, or
gastric retention triggered by the autonomic
nervous system response to pain.

More blood, more absorption High fat doesn't help

Increased blood flow to an absorption site High-fat meals and solid foods slow the rate at
improves drug absorption. which contents leave the stomach and enter the
intestines, delaying intestinal absorption of a
More rapid absorption leads to a quicker onset
drug.
of drug action.
Dosage form factors
For example:
Drug formulation (such as tablets, capsules,
L.M. administration can make a difference in
liquids and coatings) affects the drug absorption
the drug absorption rate. Blood flows faster
rate and the time needed to reach peak blood
through the deltoid muscle than through the
concentration levels.
gluteal muscle. The gluteal muscle, however,
can accommodate a larger volume of drug than
the deltoid muscle.
Absorption increase or decrease? • heart

Combining one drug with another drug, or with • liver kidneys

food, can cause interactions that increase or
Lucky lipids
decrease drug absorption, depending on the
substances involved. The ability of a drug to cross a cell membrane
depends on whether the drug is water or lipid
Drug Interactions
(fat) soluble.
Synergism
Lipid-soluble drugs easily cross through cell
. Combined action of two drugs membranes; water-soluble drugs can't. Lipid-
soluble drugs can also cross the blood-brain
Common Examples Sulfa+Trimethoprim - better
barrier and enter the brain.
bacteria killer • Aspirin + Warfarin = spont.
Hemorrhage Captopril+ Nitro = enh. BP control
in CHF

Distribution

It is the process by which the drug is delivered

from the systemic circulation to body tissues
and fluids. Distribution of an absorbed drug
within the body depends on several factors:

• blood flow
Free to work
• solubility
As a drug travels through the body, it comes in
• protein binding contact with proteins such as the plasma
protein albumin.

The drug can remain free or bind to the protein.

The portion of a drug that's bound to a protein

is inactive and can't exert a therapeutic effect.

Only the free, or unbound, portion remains

active. A drug is said to be highly protein-bound
if more than 80% of the drug is bound to
protein.
Quick to the heart
**Only free drugs, not those bound to protein,
After a drug has reached the bloodstream, its can produce a therapeutic effect!!**
distribution in the body depends on blood flow.
The drug is quickly distributed to organs with a
large supply of blood. These organs include the
Metabolism
Drug metabolism, or biotransformation, is the
process by which the body changes a drug from
its dosage form to a more water-soluble form
that can then be excreted.
Drugs can be metabolized in several ways:
• Most drugs are metabolized into inactive
metabolites which are then excreted.
• Other drugs are converted to active
metabolites, which are capable of exerting their
own pharmacologic action.
• Some drugs can be administered as inactive
drugs, called prodrugs, which don’t become
active until they’re metabolized.
Where metabolism happens:
• Majority of drugs are metabolized by enzymes
in the liver.
• It can also occur in the plasma, kidneys, and
membranes of the intestines.
• If the liver is not working right, a drug doesn’t
get metabolized normally.
Conditional considerations
Certain diseases can reduce metabolism. These
include liver diseases such as cirrhosis as well as
heart failure, which reduces circulation to the
liver.
Gene machine
Genetics allows some people to metabolize
drugs rapidly and others to metabolize them
more slowly.
Stress test
Environment, too, can alter drug metabolism.
For example, cigarette smoke may affect the
rate of metabolism of some drugs; a stressful
situation or event, such as prolonged illness,
surgery, or injury, can also change how a person
metabolizes drugs.
The age game
Developmental changes can also affect drug
metabolism.
For instance, infants have immature livers that
reduce the rate of metabolism, and elderly
patients experience a decline in liver size, blood
flow, and enzyme production that also slows
metabolism.
Excretion
Drug excretion refers to the elimination of drugs
from the body.
Most drugs are excreted by the kidneys and
leave the body through urine.
Drugs can also be excreted through the lungs,
exocrine (sweat, salivary, or mammary) glands,
skin, and intestinal tract.
Half-life = half the drug
The time it takes for one-half of the drug to be
eliminated by the body.
Factors that affect a drug's half-life include its
rate of absorption, metabolism, and excretion.
Knowing how long a drug remains in the body
helps determine how frequently it should be
administered.
3 other factors play important roles in a drug's
pharmacokinetics:
• onset of action
•peak concentration
•duration of action
The onset of action refers to the time interval
from when the drug is administered to when its
therapeutic effect actually begins.
Peak performance
As the body absorbs more drug, blood
concentration levels rise.
The peak concentration level is reached when
the absorption rate equals the elimination rate.
Examples:
The onset of action of paracetamol is 0.5 to 2
hours, the time to peak effect 1 to 3 hours and
the duration of action 3 to 4 hours.
captopril
ROUTE ONSET PEAK DURATION
PO 15-60 min 60-90 min 6-12 hr
Sticking around
The duration of action is the length of time the
drug produces its therapeutic effect.
FUNDAMENTAL CONCEPTS OF PHARMACOLOGY
• Factors Influencing Responses to Drugs
•Drugs Legislation Controlled Substances,
Generic Drugs, Orphan Drugs and Over the
Counter Drugs
**No two people react in EXACTLY the same
way to any given drug**
Factors nurses must know:
1. Weight
People who are much heavier may require
larger doses to get a therapeutic effect from a
drug because they have increased tissues to
perfuse and increased receptor sites in some
reactive tissue.
People who weigh less than the norm may
require smaller doses of a drug.
Tetanus Antitoxin is used
for prophylaxis and
treatment of Tetanus.
At risk with infected
wounds, wounds
contaminated with soil or
mud, deep or punctured
wounds.
Subcutaneously or intramuscularly
TETANUS ANTITOXIN 1500 IU, 3000 IU, 20000
IU
Children are the special case in which weight-
based dosing is always required.
Children 26 years: 5 mL
(equivalent to Meptin 25
mcg) once at bedtime or
twice daily (in the morning
and at bedtime) by the oral
route.
Children <Gyears: 0.25 ml/kg
body weight (equivalent to
Meptin 1.25 mg/kg) once at bedtime or twice
daily in the morning and at bedtime) by the oral
route.
2. Age
Children metabolize many drugs differently
than adults do, and they have immature
systems for handling drugs.
Older adults undergo many physical changes
that are a part of the aging process. Their
bodies may respond very differently in all
aspects of pharmacokinetics.
Nurses should monitor the patient closely for anticipated with people of particular cultural
the desired effects. backgrounds because of their genetic makeup.

3. Gender

Physiological differences between men and

women can influence a drug's effect.

When giving IM injections:

•men have more vascular muscles so the effects

of the drug will be seen sooner

•women have more fat cells than men do so

drugs that deposit in fat may be slowly released
and cause effects for a prolonged period.

4. Physiological Factors ACE inhibitors did not seem to work in 800

patients who identified themselves as 'black', a
Physiological differences such as diurnal rhythm
doctor would not prescribe the drug to a
of the nervous and endocrine systems, acid-
patient that he or she perceives as being 'black'.
base balance, hydration, and electrolyte
balance can affect the way that a drug works on Capoten (captopril) Vasotec (enalapril)
the body and the way that the body handles the
drug. And in fact some pharmaceutical companies are
now exploring the concept of developing and
5. Pathological Factors marketing heart drugs specifically to black
patients.
Other pathological conditions can change the
basic pharmacokinetics of a drug. Pharmacogenomics is a new area of study that
explores the unique differences in response to
• Gl disorders can affect the absorption of many
drugs that each individual possesses based on
oral drugs
genetic makeup.
• Vascular diseases and low BP alter the
In the future, medical care and drug regimens
distribution of a drug.
could be individually designed based on each
• Liver or kidney diseases affect the way that a person's unique genetic makeup!
drug is biotransformed and excreted and can
7. Immunological Factors
lead to toxic reactions.
People can develop an allergy to a drug. After
6. Genetic Factors
exposure to its proteins, a person can develop
Some people lack certain enzyme systems antibodies to a drug.
necessary for metabolizing a drug, whereas
With future exposure to the same drug, that
others have overactive enzyme systems that
person may experience a full-blown allergic
cause drugs to be broken down more quickly.
reaction.
Predictable differences in the pharmacokinetics
*Sensitivity to a drug can range from mild to
and pharmacodynamic effects of drugs can be
more severe.*
8. Psychological Factors
The patient's attitude about a drug has been
shown to have an effect on how that drug
works.
A drug is more likely to be effective if the
patient thinks it will work than if the patient
believes it will not work. This is called the
placebo effect.
The patient's personality also influences
compliance with the drug regimen. Some
people who believe that they can influence
their health actively seek health care and
willingly follow a prescribed regimen.
Take note:
The nurse is in a position to influence the
patient's attitude about drug effectiveness.
Frequently, the nurse's positive attitude,
combined with additional comfort measures,
can improve the patient's response to a
medication.
When tolerance occurs, the drug no long causes
the same reaction. Therefore, increasingly
larger doses are needed to achieve a
therapeutic effect.
Example: Morphine
Tolerance is a person's diminished response to a
drug, which occurs when the drug is used
repeatedly and the body adapts to the
continued presence of the drug.
Resistance refers to the ability of
microorganisms or cancer cells to withstand the
effects of a drug usually effective against them.
TB is treatable and curable.
TYPES OF DRUG RESISTANT TB
Multidrug-resistant TB (MDR TB) is caused by TB
bacteria that is resistant to at least isoniazid and
rifampin, the two most potent TB drugs. These
drugs are used to treat all persons with TB
disease.

9. Environmental Factors

Some drug effects are enhanced by a quiet,

cool, non-stimulating environment,

Sedating drugs: reducing external stimuli to

decrease tension and stimulation help the drug
be more effective.

Antihypertensives work well during cold, winter
months may become too effective in warmer
environments.
10. Tolerance
The body may develop a tolerance to some
drugs over time.
Tolerance may arise because of increased
biotransformation of the drug, increased
resistance to its effects, or other
pharmacokinetic factors.
Extensively drug-resistant TB (XDR TB) is a rare
type of MDR TB that is resistant to isoniazid and
rifampin, plus any fluoroquinolone and at least
one of three injectable second-line drugs (i.e.,
amikacin, kanamycin, or capreomycin).
Inappropriate management can have life-
threatening results.
Drug-resistant TB should be managed by or in
close consultation with an expert in the disease.

11. Cumulation
If a drug is taken in successive doses at intervals
that are shorter than recommended or if the
body is unable to eliminate a drug properly, the
drug can accumulate in the body, leading to
toxic levels and adverse effects.
12. Interactions
When two or more drugs or substances are
taken together, there is a possibility that an
interaction can occur, causing unanticipated
effects in the body.
Alternative therapies, such as herbal products,
act as drugs in the body and can cause these
same interactions.
Certain foods can interact with drugs in much
the same way.
LEGAL REGULATION OF DRUGS
The FDA regulates the development and sale of
drugs.
Nurses should become familiar with the rules
and regulations in the area in which they
practice.
Other laws have given the FDA control over
monitoring of potentially addictive drugs and
responsibility for monitoring, to some extent,
the sale of drugs that are available without
prescription!
Submit the ff:
• FDA Pregnancy Categories
•Phases of Drug Development
Controlled Substances
The Controlled Substances Act of 1970
established categories for ranking of the abuse
potential of various drugs. This same act gave
control over the coding of drugs and the
enforcement of these codes to the FDA and the
Drug Enforcement Agency (DEA), a part of the
U.S. Department of Justice.
The FDA studies the drugs and determines their
abuse potential; the DEA enforces their control.
Drugs with abuse potential are called controlled
substances.
DEA Schedules of Controlled Substances
Schedule 1 (C-1): High abuse potential and no
accepted medical use (heroin, marijuana, LSD)
Schedule II (C-1): High abuse potential with
severe dependence liability (narcotics,
amphetamines, and barbiturates)
Schedule III (C-III): Less abuse potential than
schedule Il drugs and moderate dependence
liability (nonbarbiturate sedatives,
nonamphetamine stimulants, limited amounts
of certain narcotics)
Schedule IV (C-IV): Less abuse potential than
schedule III and limited dependence liability
(some sedatives, antianxiety agents, and non-
narcotic analgesics)
Schedule V (C-V): Limited abuse potential.
Primarily small amounts of narcotics (codeine)
used as antitussives or antidiarrheals.
Orphan Drugs PHARMA MIDTERMS

These are drugs that have been discovered but

are not financially viable and therefore have not Drugs Affecting the Reproductive System
been "adopted" by any drug company.

They may be useful in treating a rare disease, or

they may have potentially dangerous adverse
effects. Orphan drugs are often abandoned
after preclinical trials or phase I studies.

octreotide (Brand name: Sandostatin LAR) -

Manufactured by Novartis Pharmaceuticals
Corporation

FDA-approved indication: Reduction of growth
hormone and IGF-1 (somatomedin C) in
acromegaly.
isavuconazonium sulfate (Brand name:
Cresemba) – Manufactured by Astellas
FDA-approved indication: Treatment of invasive
aspergillosis in patients 18 years of age and
older.
Over-the-Counter Drugs
These are products that are available without
prescription for self-treatment of a variety of
complaints.
Some of these agents were approved as
prescription drugs but later were found to be
very safe and useful for patients without the
need of a prescription.
 The female ovary stores ova and
produces the sex hormones estrogen
and progesterone.
 The hypothalamus releases GnRH at
puberty to stimulate the anterior pituitary
release of FSH and LH, thus stimulating
the production and release of the sex
hormones. Levels are controlled by a
series of negative feedback systems.
 Female sex hormones prepare the body
for pregnancy and the maintenance of
the pregnancy. If pregnancy does not
occur, the prepared inner lining of the
uterus sloughs off as menstruation in the
menstrual cycle.
 Menopause occurs when the supply of
ova is exhausted and the woman’s body
no longer produces the hormones
estrogen and progesterone.

**Nurses must always include specific questions

about OTC drug use when taking a drug history
and should provide information in all drug-
teaching protocols about avoiding OTC use
while taking prescription drugs.**

- The testes produce sperm in the

seminiferous tubules in response to FSH
stimulation, and testosterone in the
interstitial cells in response to LH
stimulation.
 - Testosterone is responsible for the - To prevent postpartum breast
development of male sex characteristics. engorgement
These characteristics can be maintained
by the androgens from the adrenal gland - To slow bone loss in osteoporosis
once the body has undergone the changes
of puberty. - For palliation in certain cancers that have
known receptor sensitivity
- Andropause, analogous to female
menopause, occurs with age when the - Important for the development of the
production of testosterone declines, with female reproductive system and secondary
sex characteristics
the subsequent loss of testosterone
effects.
- Responsible for the proliferation of the
endometrial lining
Drugs Affecting the Female Reproductive
System - An absence or decrease in estrogen
SEX HORMONES produces the signs and symptoms of
Used to replace hormones that are missing or to menopause in the uterus, vagina, breasts,
act on the control mechanisms of the endocrine and cervix
system to decrease the release of endogenous
hormones. - Produce a wide variety of systemic effects,
Estrogens and the progestins including protecting the heart from
atherosclerosis, retaining calcium in the
Estrogens: estradiol (Estrace, Climara, and bones, and maintaining the secondary
others), conjugated estrogens (Premarin), female sex characteristics
esterified estrogen (Menest), and estropipate
(Ortho-Est, Ogen) They affect the release of pituitary
follicle-stimulating hormone (FSH)
Progestins: drospirenone (Yasmin, Yaz), and luteinizing hormone (LH); cause
etonogestrel (Implanon), levonorgestrel capillary dilation,
(Mirena), medroxyprogesterone (Provera), fluid retention, and protein anabolism
norethindrone (Aygestin), norgestrel (Ovrette), and thin the cervical mucus;
progesterone (Progestasert and others), and conserve calcium and phosphorus
desogestrel (found in many contraceptive and encourage bone formation;
combinations) inhibit ovulation; and prevent
postpartum breast discomfort.
Estrogens and the progestins (the
endogenous female hormone progesterone
and its various
derivatives)

Therapeutic Actions and Indications

Estrogens 
- Used for hormone replacement therapy
(HRT) when ovarian activity is blocked or
absent INJECTABLES
- Depo-Provera 150 mg
- Used as palliation for the discomforts of medroxyprogesterone, given 1 mL by deep
menopause when many of the beneficial IM injection q3mo
effects of estrogen are lost
Progestins
- To treat female hypogonadism and ovarian - Used as contraceptives, most effectively in
failure  combination with estrogens (Box 

- Used to treat primary and secondary
amenorrhea and functional uterine
bleeding and as part of fertility programs
- Like the estrogens, some progestins are
useful in treating specific cancers with
specific receptor-site sensitivity
- Transform the proliferative endometrium
into a secretory endometrium, inhibit the
secretion of FSH and LH, prevent follicle
maturation and ovulation, inhibit uterine
contractions, and may have some anabolic
and estrogenic effects
When they are used as contraceptives, the
exact
mechanism of action is not known, but it is
thought that circulating progestins and
estrogens “trick” the hypothalamus and
pituitary and prevent the release of
gonadotropin-releasing
hormone (GnRH), FSH, and LH, thus
preventing follicle development and
ovulation.
Pharmacokinetics
- Well absorbed through the GI tract and
undergo extensive hepatic metabolism.
They are excreted in the urine. Estrogens
cross the placenta and enter breast milk.
- NuvaRing, is available as a subdermal
implant that may be left in place for up to 3
years and then must be removed.  could alter the metabolism of the drug and
- The vaginal ring (NuvaRing) is a small
soft, plastic ring that you place inside your
vagina.
- It releases a continuous dose of the
hormones oestrogen and progestogen into
the bloodstream to prevent pregnancy.
Contraceptive patch
- is a small sticky patch that releases
hormones into your body through your skin
to prevent pregnancy
Contraindications and Cautions
Estrogens and Progestins:  They were developed to produce some of the
- Allergies to estrogens  positive effects of estrogen replacement while
- Idiopathic vaginal bleeding, breast cancer,
or any estrogen-dependent cancer
- History of thromboembolic disorders
- Hepatic dysfunction
- Pregnancy
- Breast-feeding
- Metabolic bone disease
- Renal insufficiency
- Hepatic impairment
Estrogens are contraindicated in the
presence of any known allergies to
estrogens to avoid hypersensitivity reactions
and in patients with idiopathic vaginal
bleeding, breast cancer, or any
estrogen-dependent cancer, all of which
could be exacerbated by the drug; with a
history of thromboembolic disorders,
including
cerebrovascular accident, or with heavy
smokers because of the increased risk of
thrombus and embolus development; or with
hepatic dysfunction, because of the effects
of estrogen
on liver function.
contraindicated during pregnancy due to the
risk of serious fetal defects. They should be
avoided during breast-feeding because of
possible effects on the neonate.
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; and with hepatic impairment, which
increase the risk
for the adverse effects, including those on
the liver and gastrointestinal tract.
Estrogen Receptor Modulators
Raloxifene (Evista) and toremifene (Fareston). 
The long-term effects of these two drugs are not
yet known
Therapeutic Actions and Indications
Not hormones but affect specific estrogen
receptor sites, stimulating some and blocking
others. 
limiting the adverse effects.
Pharmacokinetics
Administered orally, raloxifene is well absorbed
from the GI tract and is metabolized in the liver.
Excretion occurs through the feces. It is known
to cross the placenta and enter into breast milk.
Contraindications and Cautions
Allergy to raloxifene to avoid hypersensitivity
reactions and 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 blood clot formation if smoking
and estrogen are combined.
What are nursing considerations for patients
receiving hormones or estrogen receptor
modulators?
FERTILITY DRUGS
Stimulate the female reproductive system
Work either directly to stimulate follicles and
ovulation or stimulate the hypothalamus to
increase FSH and LH levels
leading to ovarian follicular development
and maturation of ova.
Pharmacokinetics
These drugs are well absorbed and are treated
like endogenous hormones within the body,
undergoing hepatic metabolism and renal
excretion.
Injectables and Oral agent (Clomiphene)
Caution should be used in women who are
breast-feeding because of the risk of adverse
effects on the baby and in those with
thromboembolic diseases because of the risk of
increased thrombus formation
UTERINE MOTILITY DRUGS
Stimulate uterine contractions to assist labor
(oxytocics) or induce abortion (abortifacients)
Terbutaline, a beta2-selective adrenergic agonist
- uterine motility agent to relax the
gravid uterus to prolong pregnancy
- reserved for use after 20 weeks of
gestation, when the fetus has a chance
of survival outside of the uterus
- the patient will need to be monitored
for sympathetic stimulation in the rest of
the body
This drug is administered if uterine
contractions
become strong before term to prevent
premature labor and delivery, which could
result in detrimental effects on the neonate,
including death.
Oxytocics
Stimulate contraction of the uterus, much like the
action of the hypothalamic hormone oxytocin,
which is stored in the posterior pituitary. 
ergonovine (Ergotrate),
methylergonovine (Methergine), and oxytocin
(Pitocin, Syntocinon)
Therapeutic Actions and Indications
They are especially effective in the gravid
uterus. Oxytocin, a synthetic form of the
hypothalamic hormone, also stimulates the
lacteal glands in the breast to contract,
promoting milk ejection in lactating women.
Indicated for the prevention and treatment of
uterine atony after delivery. This is important to
prevent postpartum hemorrhage.
Pharmacokinetics
Rapidly absorbed after parenteral or oral
administration, metabolized in the liver, and
excreted in urine and feces. They cross the
placenta and enter breast milk.
Methylergonovine is administered as such
directly after delivery and then continued in the
oral form to promote uterine involution.
Contraindications and Cautions
Presence of any known allergy to oxytocics and
with cephalopelvic disproportion, unfavorable
fetal position, complete uterine atony, or early
pregnancy
which could be compromised by uterine
stimulation.
Abortifacients
Used to evacuate uterine contents via intense
uterine contractions. Carboprost (Hemabate),
dinoprostone (Cervidil, Prepidil Gel, Prostin
E2), and mifepristone (RU-486,
Mifeprex)

Therapeutic Actions and Indications
Stimulate uterine activity, dislodging any
implanted trophoblasts and preventing
implantation of any fertilized egg. 
These drugs are approved for use to terminate
pregnancy at 12 to 20 weeks from the date of
the last menstrual period
Pharmacokinetics
These drugs are well absorbed when
administered. They are metabolized in the liver
and excreted in the urine. Because of their
effects on the uterus, they are used during
pregnancy only to end the pregnancy.
Contraindications and Cautions
With any known allergy to, after 20 weeks from
the last menstrual period, or with active PID or
acute cardiovascular, hepatic, renal, or
pulmonary disease
Caution should be used with any history of
asthma, hypertension,
or adrenal disease
Drugs Affecting the Male Reproductive
System
SEX HORMONES
Androgens  ANABOLIC STEROIDS
Male sex hormones and include testosterone,
which is produced in the testes, and the
androgens, which are produced in the adrenal
glands.  oxandrolone (Oxandrin) and oxymetholone
Testosterone (Duratest, Testoderm, and others),
the primary natural androgen, is the classic
androgen in use today.  Promote body tissue-building processes, reverse
It is used for replacement therapy in cases of
hypogonadism (underdeveloped testes) and to
treat certain breast cancers.
Testosterones are all class III controlled
substances. Other androgens include  danazol
(Danocrine), fluoxymesterone (Androxy), and
methyltestosterone (Testred, Virilon)
Therapeutic Actions and Indications
Responsible for the growth and development of
male sex organs and the maintenance of
secondary sex characteristics
They 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. They also increase
the production of red blood cells.
Because the androgens are forms of
testosterone,
Pharmacokinetics
Long acting and is available in several forms,
including depot (deep, slow-release) injections
and a dermal patch. 
The androgens are well absorbed and widely
distributed throughout the body. They are
metabolized in the liver and excreted in the
urine.
Contraindications and Cautions
With any known allergy to the drug or
ingredients in the drug; during pregnancy and
lactation; and in the presence of prostate or
breast cancer in men
because of potential adverse effects on the
neonate (another method of feeding the baby
should be used if these drugs are needed
during lactation);
Analogues of testosterone that have been
developed to produce the tissue-building effects
of testosterone with less androgenic effect
(Anadrol-50)
Therapeutic Actions and Indications
catabolic or tissue-destroying processes, and
increase hemoglobin and red blood cell mass 
They can be used to treat anemias, certain
cancers, and angioedema
and to promote weight gain and tissue repair in
debilitated patients and protein anabolism in
patients who are receiving long-term
corticosteroid therapy.
Known to be used illegally for the
enhancement of athletic performance by
promoting increased muscle mass, increased
hematocrit, and, theoretically, an increase in
strength and endurance
Pharmacokinetics
Oxandrolone and oxymetholone are available
orally. Like the androgens, the anabolic steroids
are well absorbed and widely distributed
throughout the body. They are metabolized in
the liver and excreted in the urine
Contraindications and Cautions
Any known allergy to anabolic steroids; during
pregnancy and lactation
Digoxin
Nursing consideration
- Obtain vital signs- HEART RATE
- Assess for digitalis toxicity
- Clients checks HR daily before taking
digoxin
- Client eats food rich in potassium
Symptoms of Angina

Presence of liver dysfunction, coronary disease - Angina

or prostate or breast cancer in males  is caused by reduced blood flow to
the heart muscle
 can spread anywhere between the
Drugs affecting the Body System
belly button and the jaw, including to
Cardiovascular System the shoulder, arm, elbow or hand-
usually on the left side.
EFFECTS OF ADRENERGICS AT
RECEPTORS - Antianginal Drugs
ALPHA1- Smooth muscle contraction,  Used to treat Angina Pectoris/Chest
vasoconstriction pain
 Increases blood flow either by
ALPHA2- vasoconstriction of veins, increasing O2 demand by the
vasoconstriction of arteries to heart (limited) myocardium
vasodilation of arteries
Nitrates
BETA1- ↑ HR and force of contraction
 Causes generalized vascular and
BETA2- smooth muscle relaxation coronary vasodilation. Reduces
ischemia but can cause hypotension
DRUGS FOR CARDIAC DISORDERS  Commonly given SL
Cardiac/Digitals Glycosides  Side effects: headaches (common),
hypotension, dizziness, weakness
- Effective in CHF. Used to correct atrial and fairness
fibrillation and atrial flutter.  Isosorbide dinitrate (isordil)
- Digoxin (Lanoxin)  Isosorbide mononitrate (imdur) ISMN
- 3 effects: positive inotropic, negative  Nitroglycerin (transderm-nitro)
chronotropic, negative dromotropic
- Hypokalemia causes digitalis toxicity Beta-blockers
 Manifestation: anorexia, GI  Block beta 1 and 2.
disturbances, bradycardia, PVC,  Decreases the effect of SNS by
headaches, visual illusions, cardiac blocking the action of
dysrhythmias, blurred visions, catecholamines.
confusions, and deliriums  2 groups
Nonselective- decreases PR
and causes bronchoconstriction.
-propranolol (Inderal)
 Side effects: bronchospasm,
behavioral or psychotic response
and impotence (Inderal)
Selective (blocking beta 1)-
decreasing PR but avoiding
bronchoconstriction
-atenolol (Tenormin), metoprolol
(Lopressor)
Side effects: decreases PR and
BP
Calcium Channel Blockers
 Decreases cardiac contractility and
reduces the workload of the heart.
 Effective in variant and classic angina
 Side effects: headaches,
hypotension, dizziness, flushing of
the skin, reflex tachycardia
Antidysrhythmic Drugs
 Fast (Na) channel blockers-
decrease the fast Na influx to the
cardiac cells
 procamide, lidocaine
 Beta-Blockers-decreases
conduction velocity, automaticity and
recovery time
 Most frequently used
 propanol
Renal Drugs: Diuretics
Thiazide and Thiazide-like
 acts on distal convulated renal tubule,
beyond the loop of Henle.
 Not for immediate diurisis
 HPN and peripheral edema
 Promotes Na, CI and water excretion
 Used for client with normal renal
function
 Chlorothiazide, hydrochlorothianized
 Side effects: hyperglycemia,
hypergalcemia, hyperuricemia,
hyperlipidemia
Loop (High-Ceiling) Diuretics
 act on the ascending loop of Henle by
inhibiting chloride transport of Na into
the circulation more potent than
thiazide great saluretic/naturetic
effect
 Side effects: fluid and electrolyte
imbalances (common), orthostatic
hypotension, thrombocytopenia, skin
disturbances and transient deafness
 furosemide (Lasix)
Osmotic Diuretics
 increases the osmolality of the
plasma and fluid in the renal tubules
 used to prevent kidney failure,
decrease ICP and IOP
 potent K wasting diuretic
 do not exposed in low temperature
 Side effects: fluid and electrolyte
imbalances
 Mannitol
Carbonic Anhydrase Inhibitors
 blocks the action of the enzyme
carbonic anhydrase to maintain acid-
base balance
 acetazolamide
 used to decrease IOP in clients with
openangle glaucoma, epilepsy
 dichlorphenamide
Potassium-Sparing Diuretics
 used as mild diuretics or in
combination with other diuretics
 act primarily in the collecting duct
renal tubules to promote Na and
water excretion BUT promotes K
retention
 Side effect: hyperkalemia
 spironolactone (Aldactone)
Hypertension 1. Stress reduction techniques
2. Exercise
3. Salt restriction
4. Decreased alcohol ingestion
5. Weight reduction

Anti-hypertensive Drugs
- can cause insomnia, nightmares,
depression and sexual dysfunction
- Diuretics – first line drugs for mild HPN
- Calcium Channel Blockers
Hypertension (HPN, HTN or HT)
- Symphatolytics /Sympathetic
➢ You can have HPN for years without Depressants
symptoms!!!
1. Beta blockers/ Beta adrenergic
➢ Headaches, SOB, nosebleeds are not blockers
specific  Step 1 anti HPN drugs
 Step 2 in combination with diuretic
➢ Systolic pressure is greater than 140  Anti anginals and anti dysrhythmics
mmHg and diastolic is greater than  vascular resistance is diminished
90mmHg and blood pressure is lowered
 African-american HPN clients do not
➢ Contributing factors: family history,
respond to this medication
hyperlipidemia, african-american
 If given orally, Onset is 30 mins,
background, diabetes, obesity, aging,
duration is 6-12 hours
STRESS, SMOKING and ALCOHOL  If given thru IV the onset is
ingestion, too little K and too much Na immediate, peak is 20 mins, duration
Category is 4 to 10hours
2. Centrally Acting Alpha2
1. Normal < 120, 160 >100 Agonists
2. Prehypertension 120-139, 80-89  decreases sympathetic activity, CO
3. Stage 1 HPN 140-159, 90-99 and serum epinephrine,
4. Stage 2 HPN >160 >100 norepinephrine (result in peripheral
2 types: vascular resistance)
 methyldopa, clonidine
1. Primary or Essential – exact origin is  can cause water and Na retention so
unknown, common type of HPN usually given with ??? drowsiness,
dry mouth and bradycardia,
2. Secondary – various conditions and 3. Alpha-Adrenergic Blockers
medications  promotes vasodilation and
 kidney and thyroid problems decreases BP. Used for clients
 birth control pills, decongestants, with lipid abnormalities. Safe for
illegal drugs and pain relievers diabetic clients.
 terazosin, prazosin
 Orthostatic hypotension

Direct-Acting Arteriolar Vasodilators

Non – pharmacological measures?
  potent antihypertensive drugs, - Lowers abnormal blood lipid levels
relaxing the smooth muscles of - Lipids composed of the ff:
blood vessels causing  1. cholesterol
vasodilation .  2. triglycerides
 Moderate to severe HPN  3. phospholipids
 SE: tachycardia, palpitations, - Classifications:
edema, nasal congestion,  1. chylomicrons
headache, dizziness, GI  2. VLDL
bleeding, lupus-like and  3. LDL
neurologic symptoms  4. HDL – “good”
 hydralazine, minoxidil
HDL
ACE inhibitors - have a higher percentage of protein and
 inhibits formation of angiotensin LESS lipids
II (vasoconstrictor) and blocks - Function: Remove cholesterol from the
the release of aldosterone. bloodstream and deliver it to the liver
 Effective for heart failure irritating - Other lipoproteins are composed mainly
cough, n/v, diarrhea, headache, of cholesterol and triglycerides and
dizziness, fatigue, insomnia, contribute to Atherosclerotic plaque in
hyperkalemia and tachycardia the blood vessels
 Captopril
Coronary artery with atherosclerotic
Angiotensin II Receptor Antagonist plaques. Recent hemorrhage into
(Blockers) the plaque could acutely narrow the
 new group similar to ACE lumen and produce an acute
inhibitors. It blocks the coronary syndrome with ischemia
angiotensin II. and/or infarction of the myocardium.
 losartan, valsartan, telmisartan
Non-pharmacologic Measures:
Peripheral vasodilators 1. Reduce saturated fat and cholesterol
2. Choose lean meat (fish and chicken)
3. Read food label
4. EXERCISE
5. SMOKING – increases LDL,
decreases HDL

ANTILIPIDEMICS
Fats (Lipids)
Bile-Acid Sequestrants
Main function of fats
- Cholestyramine
 provides energy
 first antilipidemic (1959)
 cushions organs
 Binds with bile acids in the
 carries vitamins (A,D,E,K)
intestines and effective in
 insulator
hyperlipidemia 2
 provides taste
- Gritty powder mixed thoroughly in water
Too much fats
or juice
 weight gain
 increased risk of heart disease
ANTILIPIDEMICS
ANTILIPIDEMICS
- colestipol – similar to cholestyramine
- cholestyramine and colestipol are - increases blood flow to the extremities.
effective in lowering cholesterol Effective for vasospasm
- tolazoline, isoxsuprine, prazosin,
Fibrates/Fibric Acid Derivatives Reduces nifedipine, Statins, ACE inhibitor
- clopidogrel, aspirin, cilostazol
 triglyceride and VLDL. Not given (decreases PAD symptoms)
with anticoagulant because it is
highly protein bound. Raynaud’s Dse
 For type 2 and 4 hyperlipidemia  cold exposure or emotional upset
 Not for long-term use clofibrate, trigger the spasm of toes and
fenofibrate fingers
 SE: cardiac dysrhythmias,  Diabetics
angina, thromboembolism and
gallstones

Nicotinic acid/niacin (Vit B 2)

 Reduces VLDL and LDL. With
numerous side effects

Hepatic 3-hydroxy 3 thylglutaryl

coenzyme A (HMG-CoA) reductase Buerger’s Disease
inhibitors or STATINS  Only in smokers
 decreases cholesterol and LDL  Cause poor circulation in feet
(2 weeks) and hands
 first introduced in 1987  May lead to tissue death and
 increases HDL amputation
 have fewer side effects  Gets worse the more you smoke
 should not be discontinued
abruptly pentoxifylline (Trental)
 SE: rhabdomyolysis – muscle  hemorrheologic agent, improves
tenderness/weakness microcirculation and tissue
 lovastatin (first introduced) perfusion. Dilates rigid
 atorvastatin calcium (Lipitor), arteriosclerotic blood vessels.
 simvastatin (Zocor) Derivative of Xanthine group
 Buerger’s Dse (arterial
occlusion)

DRUGS FOR CIRCULATORY

DISORDERS
- anticoagulants – prevent the formation
of clots that inhibit circulation
antiplatelets/antithrombotics –
prevent platelets aggregation (clumping
together of platelets to form a clot)
- thrombolytics/clot buster – attack and
dissolves blood clots that have already
formed
PERIPHERAL VASODILATORS
- Thrombosis – formation of a clot in an
arterial or venous vessel
Causes:
 1. blood stasis (decreased blood
circulation) 2. platelet
aggregation on the blood vessel
wall
Platelet aggregation is part of
the sequence of events
leading to the formation of a
thrombus or clot
3. blood coagulation
DRUGS FOR CIRCULATORY
DISORDERS
- Anticoagulants
 Inhibits clot formation. Do not
dissolve clots but act only to
prevent new clots from forming.
 Used in clients with venous and
arterial vessel disorders
1. Deep Vein Thrombosis
(DVT)
2. Pulmonary Embolism
3. Coronary Thrombosis (MI)
DVT, is a blood clot that forms in a vein
deep in the body.
- Most deep vein clots occur in the lower
leg or thigh.
Thrombophlebitis - If the vein swells
A deep vein thrombosis can break
loose and cause a serious
problem in the lung, called a
pulmonary embolism
Anticoagulants
- Heparin - usually given thru IV. Its
primary use is to prevent venous
thrombosis which can lead to pulmonary
embolism or stroke
- Poorly absorbed thru GI. Given SQ or
IV.
DRUGS FOR CIRCULATORY
DISORDERS
Anticoagulants
 Heparin- usually given thru IV.
Its primary use is to prevent
venous thrombosis which can
lead to pulmonary embolism or
stroke
 Poorly absorbed thru GI. Given
SQ or IV.
 Can decrease the platelet count
(thrombocytopenia).
 Protamine Sulfate is the antidote
if hemorrhage occurs
 Protamine can be anticoagulant
but in the presence of HEPARIN,
it is an antagonist.
 PTT (Partial Thromboplastin Time)
and APTT (Activated Partial
Thromboplastin Time) are two
medical tests which are used to
represent and characterize blood
coagulation
 PTT is the best single screening test
conducted to assess coagulation
disorders.
 APTT It is same as PTT, but
measures effectiveness of Heparin
(more specific than Partial
Thromboplastin Time).
Function:
 PTT
 It is used primarily to probe
unexplained bleeding or clotting.
It may be conducted along with a
prothrombin time (PT)
APTT
 It is a common medical
screening test conducted to
investigate function of the
intrinsic clotting system and
bleeding disorders.
Significance:
PTT
 It evaluates the amount and the
performance of several proteins
called coagulation factors which
are significant part of blood clot
formation. The PTT screening
test helps to assess a person’s
ability to appropriately develop
blood clots.
APPT
 It investigates factors I the obstructed area
(fibrinogen), II
(prothrombin), V, VIII, IX, X, XI
and II
Reference range
- PTT 60-70 seconds
- APTT 30-40 seconds
Oral anticoagulants
 prolongs clotting time and are
monitored by the Prothrombin
Time (PT)
 warfarin (common), dicumarol
 SE: Bleeding (petechiae,
ecchymosis and (hematemesis)
Vitamin K
 antagonist of warfarin overdose
or uncontrollable bleeding. If
Vitamin K fails to control
bleeding then fresh whole blood
or fresh-frozen plasma or
platelets are given
 CLIENT TEACHING:
1. Use soft toothbrush to
prevent gum bleeding
2. No smoking
3. Aspirin should not be taken
4. Report and control bleeding
Antiplatelets
 used to prevent thrombosis in
the arteries by suppressing
platelet aggregation
 Heparin and warfarin prevent
thrombosis in the veins.
 For prophylactic use such as:
1. prevention of MI or stroke
clients with history
2. prevention of repeat MI or
stroke
3. prevention of a stroke for
clients having transient
ischemic attacks (TIAs)
Thromboembolism
 occlusion of an artery or vein
caused by thrombus or embolus
results in ischemia that causes
necrosis of the tissue distal to
 Thrombus or blood clot
disintegrates when thrombolytic
drug is given 4 to 6 hours after
AMI (heart attack)
Difference between a thrombus and an
emboli
- A thrombus is a clot that is stationary
and an emboli is a thrombus that has
broken off and is travelling
Thrombolytics
- dissolved clots that already formed.
- Used for pulmonary embolism, DVT and
thrombotic stroke
- SE: Hemorrhage (major complication),
streptokinase, urokinase, tissue
plasminogen activator (t-PA), reteplase,
Tenecteplase, anisoylated plasminogen
streptokinase activator complex
(APSAC)
Streptokinase
- may cause hypotension and allergy
when first administered
- Anticoagulants and antiplatelet drug  causes drowsiness, dry mouth
increases the risk of bleeding and other anti-cholinergic
- Aminocaproic acid (Amicar) properties (diphenhydramine)
antithrombolytic drug is used to stop  decreases nasal itching and
bleeding
tickling that causes sneezing
Thrombolytics
- dissolved clots that already formed.
Second Generation/ Non-
- Used for pulmonary embolism, DVT and Sedating
thrombolic stroke  causes fewer anti-cholinergic
- SE: Hemorrhage (major complication), effects (loratidine, cetirizine)
- streptokinase, urokinase
Anticholinergic drugs
- inhibit the transmission of
Pharmacology Drugs Affecting the
parasympathetic nerve impulses,
Body System
thereby reducing spasms of smooth
Respiratory System muscles.
- Blocking acetylcholine signals can
Upper Respiratory Infections:
decrease: involuntary muscle
1. Cold- prevalent, caused by movement, digestion, mucus
rhinovirus secretion???
 RHINORRHEA, nasal
Client Teaching
congestion, cough or tussis
2. Acute rhinitis- inflammation of
mucous membranes of the nose.
3. Sinusitis
4. Acute pharyngitis
Drugs for Common Upper
Respiratory Problems Antihistamines
- Antihistamines H1 blockers or H1 - Safety of antihistamines during
antagonist pregnancy and lactation
- compete with histamine for receptor - Give with food
sites preventing histamine - Avoid driving and alcohol
response - Breastfeeding is not recommended
- rapidly absorbed in 15 minutes, - Not recommended for patients with
commonly used as cold remedies narrow angle glaucoma
- can treat allergic rhinitis but not
potent to combat anaphylaxis

Antihistamines
Nasal Decongestants
First Generation - Sympathomimetic amines
 - stimulates the alpha adrenergic
receptors to produce vascular
constriction of the capillaries within
nasal mucosa
- frequent use can cause Rebound
Nasal Congestion
Systemic Decongestants
- Alpha-adrenergic agonist
- relieve nasal congestion for a
longer period
- ephedrine, phenylephrine, neo-
synephrine, phenylpropanolamine
- Side effects: increases BP and
blood sugar, jittery and restless
Intranasal Glucocorticoids
- effective for treating allergic rhinitis
(rhinorrhea, sneezing and
congestion)
- beclomethasone, budesonide,
dexamethasone can cause dryness
of the nasal mucosa for short-term
use only
Antitussive
- act on cough-control center to
suppress the cough reflex
- used for nonproductive and
irritating cough (dextromethorphan)
- 3 types: narcotic, non narcotic,
combination
 Narcotic can cause physical
dependence/tolerance
Classification (Antitussive)
Narcotic/opioid antitussive
 Codeine
 Hydrocodone
Non-narcotic/non-opioid
antitussive
 Dextromethorphan
 Benzonatate
 Diphenhydramine
Expectorants
- loosens bronchial secretions
(Guaifenesin)
- HYDRATION is the best
expectorant
Sinusitis
- Systemic or nasal decongestant
- Acetaminophen
- Fluids and Rest
- Antibiotic for severe sinusitis
Acute Pharyngitis
- Antibiotics (except for viral
pharyngitis)
- Saline gargles
- Lozenges
- Fluids
- Acetaminophen
EFFECTS OF ADRENERGICS AT
RECEPTORS
- ALPHA1 - ↑ force of heart
contraction, vasoconstriction, ↑BP,
dilates pupils, ↓secretion
- ALPHA2 – inhibits release of
norepi, dilates blood vessels, ↓ BP,
mediate arteriolar and venous
constriction
- BETA1 - ↑HR and force of
contraction
- BETA2 – dilates bronchioles, GI
and uterine relaxation
2 Major Categories of Lower
Respiratory Tract Disorders:
1. Chronic Obstructive
Pulmonary Disease (COPD)
 Chronic bronchitis,
Bronchiectasis, Emphysema
and Asthma
2. Restrictive Pulmonary Disease
 Pulmonary edema and
fibrosis, pneumonitis, Lung
tumors, Thoracic deformities
Chronic Bronchitis
- bronchial inflammation and
excessive mucus secretion
Bronchiectasis
- Abnormal dilatation of the bronchi
and bronchioles
Emphysema
- Loss of fiber and elastin network in
the alveoli
- Enlarged alveoli
Bronchial Asthma
- Characterized by periods of
bronchospasm or
bronchoconstriction, wheezing,
mucus secretion and dyspnea
Chemical mediators:
- Histamines
- Cytokines
- Serotonin
- Eosinophil chemotactic factor of
anaphylaxis (ECF-A)
- Leukotrienes
Drugs for Acute and Chronic Lower
Respiratory Disorders
Sympathomimetics: Alpha-and
Beta2-Adrenergic Agonists
- increases cAMP, causing dilation of
the bronchioles
albuterol (Ventolin) – selective
beta2 drug, effective for treatment
and control of asthma with long
duration of action
metaproterenol – has some beta1
effect but used as beta2, for long-
term asthma treatment, frequently
administered by inhalation
isoproterenol
- stimulates both beta1 and beta2
receptors, administered by
inhalation or IV
epinephrine
- alpha1, beta 1 and beta 2 agonist.
Given SQ in acute bronchospasm
caused by anaphylaxis. Elevates
BP.
- SE: Epinephrine - tremors,
dizziness, HPN, tachycardia,
palpitations
Beta2 adrenergic
- tremors, headaches, nervousness,
increase PR and palpitations.
- May increase blood sugar level
Methylxanthine (Xanthine)
Derivatives
- Aminophylline, theophylline and
caffeine
- Stimulates CNS and respiration,
dilates coronary and pulmonary
vessels and causes diuresis
Increases cAMP
 Theophylline Toxicity with
serum concentration
>20mcg/ml
 SE: hyperglycemia,
decreased clotting time,
leukocytosis
- Side effects of Aminophylline
(commonly use) dizziness, flushing,
hypotension, bradycardia and
palpitations
Leukotriene Receptor Antagonist and
Synthesis Inhibitors
 - effective in reducing the
inflammatory symptoms of asthma,
not used for acute asthma attack.
- Zafirlukast, Zileuton and
Montelukast
Glucocorticoids
- has anti-inflammatory action
- given if asthma is unresponsive to
bronchodilator therapy
- have synergistic effect if given with
beta2 agonist
- MDI inhaler, tablet (prednisone),
- IV (dexamethasone,
hydrocortisone)
- should be taken with food
- SE: fluid retention, skin thinning,
increased blood sugar and impaired
immune response
Cromolyn and Nedocromil
- for prophylactic treatment of
asthma, taken daily
- only inhibits the release of
histamine
- SE: cough and bad taste
(common), rebound bronchospasm
Mucolytics
- liquefy and loosens thick mucous
secretions (acetylcysteine)
- bronchodilator should be given
5mins before mucolytic
- SE: nausea and vomiting, stomatitis
and runny nose
Antimicrobials
- used if an infection results from
retained mucus secretions
Drugs Affecting the Body System
Gastrointestinal System
GI SYSTEM
 Oral Cavity – starts the digestive
process. AMYLASE
 Esophagus – peristaltic process of
contraction begins and end in the
lower large intestine
 Stomach – holds 1000-2000mL of
gastric contents
4 cells:
1. chief – pepsin
2. parietal – HCl acid
3. gastrin-producing cells
4. mucus- producing cells
 Small intestine – most of the
digestive contents where absorbed
 Large intestine – accepts
undigested material
VOMITING/EMESIS
2 major cerebral centers:
1. CTZ receives impulses from drug
toxins, vestibular center in the ear
2. Vomiting center – odor, smell and
taste
Nonpharmacologic Measures?
- Tea, Gatorade and Pedialyte
- Crackers and dry toast
- Intravenous Fluids
NONPRESCRIPTION ANTIEMETICS
Selected Antihistamine
- frequently used to prevent motion
sickness. Minimal effect.
- should be taken 30 minutes before
travel
- dimenhydrinate (Dramamine)
- meclizine HCl (Bonamine)
- dipenhydramine HCl
PRESCRIPTION ANTIEMETICS
  antihistamines –hydroxyzine,
promethazine (Phenergan)
 anticholinergics - scopolamine
*dopamine antagonists –
phenothiazine, promethazine
 benzodiazepines – lorazepam
(Ativan)
 serotonin antagonists – ondansetron
 glucocorticoids – dexamethasone,
methylprednisolone
 cannabinoids – cannabinoid
dronabinol
 miscellaneous – metoclopramide
(Plasil), trimethobenzamide
EMETICS
- to induce vomiting
- Vomiting should not be induced if
caustic substances have been
ingested
- Vomiting should also be avoided if
petroleum distillates are ingested
- Activated charcoal is given when
emesis is contraindicated. Odorless,
tasteless, non-toxic
IPECAC
- Acts directly on the gastric mucosa
- Ipecac should be taken with a full glass
of water or other fluid
- If vomiting does not occur in 20 to 30
minutes, repeat the dose.
- SE: cardiotoxicity
Causes of Diarrhea:
- Food
- Bacteria or virus
- Drug Reaction
- Laxative Abuse
- Stress and Anxiety
- Inflammatory Bowel Disease
Types of IBD include:
Ulcerative colitis
 causes long-lasting inflammation
and sores (ulcers) in the innermost
lining of your large intestine (colon)
and rectum.
Crohn's disease
 characterized by inflammation of the
lining of your digestive tract, which
often spreads deep into affected
tissues.
OPIATES AND OPIATE-RELATED
AGENTS
- Opiates decreases peristalsis
- Constipation is a common side-effect
- Duration of Action: 2 hours
- Should not be taken with alcohol and
sedatives
diphenoxyalate (Lomotil)
loperamide (Imodium)
SOMATOSTATIN ANALOG
- Inhibits gastric acid, pepsinogen,
gastrin, cholecystokinin, and serotonin
secretions and intestinal fluid
- Decreases smooth-muscle contractility
- for severe diarrhea resulting from
metastatic cancer
octreotide (Sandostatin)
ADSORBENTS
- Coats the wall of the GI tract and
adsorbing the bacteria and toxins that
cause the diarrhea
kaolin-pectin (Kaopectate)
bismuth salts (Pepto-Bismol)
Activated charcoal
MISCELLANEOUS
- furazolidones
- lactobacillus
- parapectolin
CONSTIPATION
Causes of Constipation:
- Fecal Impaction
- Chronic Laxative Use
- Neurologic Disorders
- Ignoring the urge
- Lack of Exercise
- Selected drugs
LAXATIVES
 promote a soft stool
Catarthics
 result in a soft to watery stool with
some cramping
Purgatives
 are “harsh” catarthics
- Not indicated for client with severe
abdominal pain, intestinal obstruction,
symptoms of appendicitis
OSMOTIC/SALINE LAXATIVES
- Pull water in the colon and increase
water in the feces to increase bulk,
which stimulates peristalsis.
sodium salts (Phospho-Soda)
lactulose (Duphalac)
- Client should have good renal function
- Contraindicated with CHF
STIMULANT /CONTACT LAXATIVES
- Increase peristalsis by irritating
sensory nerve endings in the intestinal
mucosa Can be used as bowel
preparation
bisacodyl (Dulcolax) – F and E
imbalance
senna (Senokot) – can damage
nerves
Castor Oil – stimulates uterine
contraction
SE: nausea, abdominal cramping,
weakness, reddish brown urine
BULK FORMING LAXATIVES
- Promote large, soft stools by absorbing
water into the intestine, increasing
fecal bulk and peristalsis. Non
absorbable c
alcium polycarbophil
fiber granules pysllium hydrophilic
mucilloid (Metamucil)
- Drink plenty of fluids
EMOLLIENTS OR STOOL SOFTENERS
- Decreases straining during defecation.
PREVENT CONSTIPATION
- Lowers surface tension and promoting
water accumulation in the intestine and
the stool
docusate calcium (Surfak)
docusate potassium (Dialose)
docusate sodium (Colace)
SE: n/v, diarrhea, abdominal cramping
NURSING INTERVENTIONS
- Monitor I and O
- Encourage client to increase fluid
intake
- Remind client that the drugs are not for
long-term use
- Advise client to eat food rich in fiber
Nonpharmacologic Measures
- Avoid alcohol and tobacco
- Loose weight
- Avoid hot, spicy and greasy food
- NSAID and glucocorticoids should be
taken with food
ANTACIDS
- neutralizes HCl and reducing pepsin
activity. Does not coat the ulcer.
- 1 to 3 hrs. after meal and bedtime.
- Systemic Antacid
 sodium bicarbonate (Alka-Seltzer)
 calcium carbonate (Tums)
- Non-Systemic Anatacid
 aluminum hydroxide - constipation
 magnesium hydroxide – diarrhea
 Maalox, Simethicone
HISTAMINE 2 BLOCKERS
 - For gastric and duodenal ulcers.
Prevents gastric acid reflux in the
esophagus.

HISTAMINE 2 BLOCKERS
- For gastric and duodenal ulcers.
Prevents gastric acid reflux in the
esophagus.
- Blocks H2 receptors of the parietal
cells
cimetidine (Tagamet)
ranitidine (Zantac)
famotidine (Pepsid)

PROTON PUMP INHIBITORS

- Suppresses gastric acid secretion
- 90% greater than H2 blockers Blocks
the final step in acid Production.
Before meals
omeprazole (Prilosec)
pantoprazole (Protonix)
esomeprazole (Nexium)

PEPSIN INHIBITOR
- Non-absorbable and combines with
protein to form viscous substance that
covers the ulcer
- Does not neutralize and decrease acid
secretion
- Before meals and at bedtime
sucralfate (Carafate)

PROSTAGLANDIN ANALOGUE
ANTIULCER DRUG Misoprostol
- Synthetic prostaglandin analogue,
used to prevent and treat peptic ulcer
- Recommended for patients with
NSAID therapy
- Suppress gastric acid secretion and
increase cytoprotective mucus in the
GI Tract
- Contraindicated during pregnancy and
for women of child-bearing ag