PHARMACOLOGY

Drugs acting on the

endocrine system
KRISTIE KWIN ALLEY FERRER
HACEL HALIMBATEN
SMYLA DAWN INGIA-EN
BERNADETTE JORNACION
 BERNADETTE S. JORNACI ON

CHAPTER 34:

INTRODUCTION TO THE
ENDOCRINE SYSTEM
 ENDOCRINE SYSTEM
it works to maintain internal homeostasis and
to integrate the body’s response to the
external environment.

FUNCTIONS:

Growth and Development

Metabolism
Reproduction
Electrolyte Balance
Energy use in the body.

BERNADETTE S. JORNACION
 Glands
organized groups of specialized cells that secrete hormones,
or chemical messengers, directly into the bloodstream to
communicate within the body.
hormones
is a chemical that is produced within the body.

ALL HORMONES.
are produced in very small amount.
secreted directly into the blood stream.
Travel through the blood to specific receptor sites
throughout the body.
it acts to increase or decrease the normal metabolic
cellular processes when they react with their specific
receptor sites.
and immediately broken down.

BERNADETTE S. JORNACION

BERNADETTE S. JORNACION
 Hypothalamus
it helps to regulate both nervous and endocrine
responses to internal and external stimuli.
“MASTER GLAND”
FUNCTIONS:
body temperature
thirst
hunger
water retention
blood pressure
respiration
reproduction
emotional reactions
BERNADETTE S. JORNACION
 pituitary gland
found in the sella turcica of the brain; produces
hormones, endorphins, and enkephalins and store
two hypothalamic hormones.

Three Lobe of Pituitary Gland:

Anterior Lobe
Posterior Lobe
Intermediate Lobe
 anterior pituitary
lobe of the pituitary gland that produces
stimulating hormones, as well as growth hormones,
prolactin, and melanocyte-stimulating hormone.
known as the body‘s master gland.

SIX MAJOR HORMONES:

GH
Adrenocorticotropic hormone (ACTH)
DIUMAL RHYTHM
Follicle-stimulating hormone response of the hypothalamus
Luteinizing Hormone and the the pituitary gland and
PRL adrenals to wakefulness,
Thyroid stimulating hormone (TSH) sleeping, and light exposure.
posterior lobe of the pituitary that receives
antidiuretic hormone and oxytocin via
pituitary nerve axons from the hypothalamus
and stores them to be released when
stimulated by the hypothalamus.

two hormones:
adh (vasopressin and oxytosin)
 intermediate lobe

LOBE OF THE PITUITARY THAT PRODUCES ENDORPINS AND ENKEPHALINS,

WHICH ARE RELEASED IN RESPONSE TO SERVE PAIN OR STRESS AND OCCUPY
SPECIFIC ENDORPHIN RECEPTOR SITES IN THE BRAINSTEM TO BLOCK THE
PERCEPTION OF PAIN.
 The production and release of
hormones needs to be tightly
regulated within the body.
Hormones are released in small
amount to accomplish what needs to

endocrine be done to maintain homeostasis

within the body.
The fine-tuning and regulation of
regulation hormones release through the
hypothalamus are often regulated by a
series of negative feedback systems:
Other hormones are not controlled in
this fishion but respond to the direct
stimuli.
 HYPOTHALAMIC-PITUITARY AXIS

INTERCONNECTION OF THE HYPOTHALAMUS AND PITUITARY TO REGULATE

THE LEVEL OF CERTAIN ENDOCRINE HORMONES THROUGH A COMPLEX
SERIES OF NEGATIVE FEEDBACK SYSTEMS.

NEGATIVE FEEDBACK SYSTEMS

CONTROL SYSTEM IN WHICH INCREASING LEVELS OF A HORMONE LEAD TO
DECREASED LEVELS OF RELEASING AND STIMULATING HORMONES, LEADING TO
DECREASED HORMONE LEVELS, WHICH STIMULATES THE RELEASE OF RELEASING
ABD STIMULATING HORMONES; ALLOW TIGHT CONTROL OF THE ENDOCRINE SYSTEM.
HYPOTHALAMIC
AND PITUITARY
AGENTS
 Homeostasis
It is the Endocrine System’s main function. This is achieved through a
complex balance of glandular activities that either stimulate or suppress
hormone release.

Drugs Affecting Hypothalamic Hormones

Factors that stimulate the release of hormones are growth hormone-
releasing hormone, thyrotropin-releasing hormone, gonadotropin-
releasing hormone (GnRH), corticotropin-releasing hormone, and
prolactin-releasing hormone.
 Drug Therapy Across the Lifespan

1. For Children
Children who receive any of the hypothalamic or pituitary agents need
to be monitored closely for adverse effects.

2. For Adults
Adults should also be monitored of their electrolytes and blood sugar
levels when receiving any of these agents.

2. For Older Adults

Older adults may be more susceptible to the imbalances associated
with alterations in the endocrine system. Hence, proper administration
techniques should be reviewed.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

ANTAGONISTS
1. Goserelin (Zoladex) - Used as an antineoplastic agent treatment
of specific hormone-stimulated cancers
2. Histrelin (Vantas) - Palliative treatment of advanced prostate
cancer
3. Leuprolide (Lupron) - Used as antineoplastic agent for treatment
of specific cancers, treatment of endometriosis and precocious
puberty that results from hypothalamic activity
4. Nafarelin (Synarel) - Treatment of endometriosis and precocious
puberty
5. Tesamorelin (Egrifta) - Reduction of excessive abdominal fat in
HIV-infected patients with lipodystrophy
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

ANTAGONISTS
1. Degarelix (Firmagon) - Treatment of advanced prostate cancer
2. Ganirelix (Antagon) - Inhibition of premature luteinizing hormone
surge in women undergoing controlled ovarian stimulation as part
of a fertility program

Pharmacokinetics
For the most part, these drugs are absorbed slowly when given IM,
subcutaneously or in depot form. They tend to have very long half-
lives of days to weeks.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

Contraindications and Cautions:

1. 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.
2. Whereas, caution should be used with renal impairment, peripheral
vascular disorders, and with rhinitis when using nafarelin.

Adverse Effects:
Adverse effects associated with these drugs are related to the
stimulation or blocking of regular hormone control. Agonists can lead to
increased release of sex hormones meanwhile, antagonists can lead to a
decrease in testosterone levels.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

GROWTH HORMONE AGONIST

1. Somatropin (Nutropin, Saizen, Humatrope) - Treatment of children
with growth failure due to lack of GH or to chronic renal failure, etc.
2. Somatropin rDNA origin (Zorbtive) - Reserve for use in treatment of
adults with short bowel syndrome who are receiving specialized
nutritional support.

GROWTH HORMONE ANTAGONIST

1. Bromocriptine Mesylate (Parlodel) - Treatment of acromegaly in
patients who are not candidates for or cannot tolerate other therapy
2. Lanreotide (Somatuline Depot) - Long term treatment of
acromegaly in patients with inadequate response to or who cannot
be treated with surgery or radiation
 DRUGS AFFECTING HYPOTHALAMIC HORMONES
GROWTH HORMONE ANTAGONIST
1. Octreotide (Sandostratin) - Treatment of acromegaly in adults who
are not candidates for or cannot tolerate other therapy
2. Pegvisomant (Somavert) - Treatment of acromegaly in adults who
are not candidates for or who cannot tolerate other therapy.
3. Chorionic Gonadotropin - Treatment of male hypogonadism to
induce ovulation in females with functioning ovaries, etc.
4. Chorionic Gonadotropin Alpha - Induction of ovulation in infertile
females who has been pretreated with FSH
5. Cosyntropin - Diagnosis of adrenal function
6. Thyrotropin Alpha - Adjunctive treatment for post radioiodine
ablation of thyroid tissue in patients with near-total thyroidectomy
and well-differentiated thyroid cancer without metastasis.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

Growth Hormone Agonists

The anterior pituitary hormone that is most commonly used
pharmacologically is GH. GH is responsible for lineal skeletal growth,
the growth of internal organs, protein synthesis, and the stimulation of
many other processes that are required for normal growth.

Pharmacokinetics
Somatropin is injected and reaches peak levels within 7 hours.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

Growth Hormone Therapy

GH can be used to treat growth failure caused either by lack of GH or
by renal failure. The child taking this drug will need to have pre therapy
and periodic tests of thyroid function, blood glucose levels, glucose
tolerance tests, and tests for GH antibodies.

Contraindications and Cautions

Somatropin is contraindicated with any known allergy to the drug or
ingredients in the drug to avoid hypersensitivity reactions.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

Adverse Effects
The adverse effects that most often occur when using GH include the
development of antibodies to GH and subsequent signs of
inflammation and autoimmune-type reactions.

GROWTH HORMONE ANTAGONISTS

GH hypersecretion is usually caused by pituitary tumors and can occur
at any time of life. This is often referred to as hyperpituitarism.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

Therapeutic Actions and Indications

1. Somatostatin is an inhibitory factor released from the
hypothalamus. It is not used to decrease GH levels, although it does
do that very effectively.
2. Bromocriptine, a semisynthetic ergot alkaloid, is a dopamine
agonist frequently used to treat acromegaly.
3. Lanreotide, which acts like somatostatin, is given as a monthly
depot subcutaneously injection.
4. Pegvisomant is a GH analogue that was approved for the treatment
of acromegaly in patients who do not respond to other therapies.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

Pharmacokinetics

1. Octreotide and Lanreotide must be administered

subcutaneously. Octreotide is rapidly absorbed and widely
distributed throughout the body. Lanreotide forms a depot in
the subcutaneous tissue.
2. Bromocriptine is administered orally and effectively absorbed
from the gastrointestinal (GI) tract.
3. Pegvisomant is given by subcutaneous injection and is slowly
absorbed, reaching peak effects in 33 to 77 hours
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

Contraindications and Cautions

1. Bromocriptine should not be used during pregnancy or lactation.
2. The use of octreotide, lanreotide, and pegvisomant should be
reserved in pregnancy and during lactation.

Adverse Effects
Patients with renal dysfunction may accumulate higher levels of
octreotide.
Octreotide and Lanreotide have also been associated with the
development of acute cholecystitis, cholestatic jaundice, biliary
tract obstruction, and pancreatitis..
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

Adverse Effects
Lanreotide is associated with changes in blood glucose levels
and glucose should be followed carefully while on the drug
Bromocriptine is also associated with GI disturbances because
of its dopamine-blocking effects. It also blocks lactation and
should not be used by nursing mothers.
Pegvisomant may cause pain and inflammation at the injection
site.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

DRUGS AFFECTING OTHER ANTERIOR PITUITARY HORMONES

Drugs that affect GH are the most commonly used drugs
affecting anterior pituitary hormones.
The other anterior pituitary hormones that are available for
pharmacological use include chorionic gonadotropin (Chorex),
chorionic gonadotropin alpha (Ovidrel), cosyntropin (Cortrosyn),
and thyrotropin alpha (Thyrogen).
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

DRUGS AFFECTING POSTERIOR PITUITARY HORMONES

The posterior pituitary stores two hormones produced by the
hypothalamus. These are called Antidiuretic Hormone (ADH) and
Oxytocin.
Oxytocin stimulates milk ejection in lactating women.
ADH possesses antidiuretic, hemostatic, and vasopressin
properties.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

Diabetes insipidus
Diabetes insipidus is characterized by the production of a large
amount of dilute urine containing no glucose.

Syndrome of Inappropriate Antidiuretic Hormone (SIADH)

Syndrome of Inappropriate Antidiuretic Hormone (SIADH) presents
with fluid retention, dilution of the blood and all the blood elements,
serious issues with water balance and fluid volume.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

Therapeutic Actions and Indications

ADH is released in response to increase in plasma osmolarity or
decreases in blood volume.
The vasopressin blockers cause a loss of water through the urine
and therefore increase in serum sodium levels as the water level
decreases
Pharmacokinetics
Desmopressin is rapidly absorbed and metabolized; it is excreted in
the liver and kidneys. It is available for oral, IV subcutaneous, and
nasal administration.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

Pharmacokinetics
Tolvaptan is given orally, is readily absorbed, and has a half-life
of 12 hours.
Conivaptan is given by continuous IV infusion, the half-life of the
drug is 5 hours, and it is excreted in the urine and feces.

Pharmacokinetics
Drugs affecting the anterior pituitary hormones are
contraindicated with any known allergy to the drug or its
component to avoid potential hypersensitivity reactions or with
severe renal dysfunction.
 DRUGS AFFECTING HYPOTHALAMIC HORMONES

Adverse Effects
Desmopressin includes:
Water intoxication
Tremor
Sweating
Vertigo

Tolvaptan and Conivaptan includes:

Rapid volume shifts
Constipation
Dry mouth
Thirst
Adrenocorticals Agents

Chapter 36
 Drugs in Focus: Adrenocortical Agents

Glucocorticoids
• beclomethasone ( Beconase AQ) - Blocking inflammation in the respiratory tract.
• betamethasone ( Celestrone Soluspan) - management of allergic intra-articular topical,
and inflammatory disorders
• budesonide ( Rhinocort, Entocort EC) - relief of symptoms of seasonal and allergic rhinitis
with few side effects, maintenance treatment of asthma, as an oral agent for the treatment
of mild- to-moderate active Crohn's disease.
• flunisolide (generic) - control of bronchial asthma relief of symptoms of
seasonal and allergic rhinitis
Mineralocorticoids
• cortisone (generic) - used for replacement therapy in adrenal insufficiency
treatment of allergic and inflammatory disorders
• fludrocortisone( generic) – used for replacement therapy and treatment of salt losing adreno
genital syndrome with a glucocorticoid, not recommended for children being tried for treatment of
severe orthostatic hypotension because sodium and water retention effects can lead to increase
blood pressure.
Thyroid and Parathyroid
Agents

Chapter 37
 Drugs in Focus: Thyroid Agents
Thyroid Hormones
• levothyroxine - replacement therapy in hypothyroidism suppression of TSH release:
treatment of myxedema coma and thyrotoxicosis.

Antithyroid Agents
Thioamides
• methimazole– treatment of hyperthyroidism

Iodine Solution
• Sodium iodide - treatment of hyperthyroidism; thyroid-blocking in radiation emergencies;
destruction of thyroid tissue in patients who are not candidates for surgical removal of the
gland.
 Drugs in Focus: Parathyroid Agents
Antihypocalcemic agents
• Calcitriol (Rocaltrol)- management of hypocalcemia and reduction of parathormone levels.
parathyroid hormone (Naptara) - maintenance of serum calcium levels in adults with
hypoparathyroidism.

Antihypercalcemic Agents
Bisphosphonates
• etidronate (Didronel) - treatment of paget's disease, postmenopausal osteoporosis,
heterotopic ossification.

Calcitonins
• calcitonin salmon (miacalcin)-treatment of paget's disease, postmenopausal osteoporosis in
conjunctions with vitamin D, and calcium supplements, emergency treatment of hypercalcemia.
 AGENTS TO
CONTROL BLOOD
GLUCOSE LEVELS
Hacel Halimbaten
 IMPORTANCE OF BLOOD GLUCOSE
CONTROL AND IT’S IMPACT ON HEALTH

• Blood glucose control is crucial for

overall health.
• Imbalanced blood glucose levels
impact health significantly.
• Management of blood glucose is
vital for individuals with or without
diabetes.
• Understanding the importance of
blood glucose control is the first step
towards better health.
 NORMAL BLOOD GLUCOSE
LEVELS

Fasting Blood Glucose (measured after

at least 8 hours of fasting):
• For most people: 70-99 mg/dL (3.9-
5.5 mmol/L)

Postprandial (After a meal) Blood

Glucose:
• For most people: Less than 140
mg/dL (7.8 mmol/L) 2 hours after
eating
TYPES OF AGENTS
 LIFESTYLE
MODIFICATIONS
• Diet: Proper meal planning and portion
control to manage carbohydrate intake.
• Exercise: Regular physical activity helps
the body use glucose effectively.
•Regular Meal Timing: Eating meals and
snacks at consistent times throughout the
day can help stabilize blood sugar levels.
• Stress Management: Chronic stress can
lead to elevated blood sugar levels.
•Weight Management: • Maintaining a
healthy weight or losing excess weight
can significantly improve blood sugar
control. Even modest weight loss can lead
to substantial benefits.
 INSULIN THERAPY
•Individuals with type 1 diabetes have a deficiency of insulin and
require insulin therapy. This involves daily insulin injections or the
use of an insulin pump to replace the missing hormone. The goal is
to mimic the body’s natural insulin production.
• In type 2 diabetes, insulin therapy is often used when other
medications or lifestyle changes do not adequately control blood
glucose levels. It may be necessary when the pancreas doesn’t
produce enough insulin or when the body’s cells become resistant
to insulin.
TYPES OF INSULIN

•Rapid-Acting
•Short-Acting
•Intermediate-Acting
•Long-Acting
 RAPID-ACTING INSULIN

• Insulin Lispro (Humalog), Insulin Aspart (NovoLog), Insulin

Glulisine (Apidra): These insulins start working within 15 minutes of
injection and reach their peak effect within 1-2 hours. They are
typically taken just before or after meals to control post-meal blood
sugar spikes.
 SHORT-ACTING INSULIN

• Regular Insulin (Humulin R, Novolin R): Regular insulin takes about 30

minutes to start working, with peak action occurring 2-3 hours after
injection. It is usually taken 30 minutes before a meal to cover the increase in
blood sugar caused by eating.
 INTERMEDIATE-ACTING INSULIN

• NPH Insulin (Humulin N, Novolin N): NPH insulin has a slower onset (1-2
hours) and lasts for a more extended period (12-16 hours). It provides a
background insulin level and is often used in combination with rapid-acting
insulins.
 LONG-ACTING INSULIN

• Insulin Glargine (Lantus, Basaglar), Insulin Detemir (Levemir),

Insulin Degludec (Tresiba): Long-acting insulins provide a steady
release of insulin over an extended period, typically 24 hours. They
have no pronounced peak, which helps maintain stable blood sugar
levels throughout the day and night.
 ORAL MEDICATIONS

•There are several classes of oral medications, also known as oral

antidiabetic drugs or oral hypoglycemic agents, used to control blood
glucose levels in people with type 2 diabetes. Each class works in a distinct
way to help lower blood sugar levels.
 BIGUANIDES

• Metformin (Glucophage): Metformin is one of the most commonly

prescribed oral medications. It works by reducing the liver’s production of
glucose and improving the body’s sensitivity to insulin. Metformin is often
the first-line treatment for type 2 diabetes.
 SULFONYLUREAS

• Glipizide (Glucotrol), Glyburide (Diabeta), Glimepiride (Amaryl):

Sulfonylureas stimulate the pancreas to release more insulin. They are
typically taken before meals to help lower blood sugar, but they can cause
low blood sugar (hypoglycemia).
 THIAZOLIDINEDIONES
(TZDS)

• Pioglitazone (Actos), Rosiglitazone (Avandia): TZDs improve insulin

sensitivity in muscle and fat tissues. They can be taken alone or in
combination with other diabetes medications.
 ALPHA-GLUCOSIDASE
INHIBITORS

• Acarbose (Precose), Miglitol (Glyset): Alpha-glucosidase inhibitors slow

down the digestion and absorption of carbohydrates, helping to reduce post-
meal blood sugar spikes. They are taken with the first bite of each meal.
 DIPEPTIDYL PEPTIDASE-4
(DPP-4) INHIBITORS

• Sitagliptin (Januvia), Saxagliptin (Onglyza), Linagliptin (Tradjenta): DPP-4

inhibitors increase the levels of incretin hormones, which stimulate the
release of insulin and reduce glucagon production. They are typically taken
once a day.
 BILE ACID
SEQUESTRANTS

• Colesevelam (Welchol): This medication, primarily used to lower

cholesterol, can also help reduce blood glucose levels by binding to bile
acids in the intestines.
 COMBINATION
MEDICATION

• Some oral medications combine two different classes of drugs to provide a

synergistic effect in controlling blood sugar. For example, metformin may be
combined with a sulfonylurea or a DPP-4 inhibitor.
SIDE EFFECTS AND RISKS
 SIDE EFFECTS OF ORAL
MEDICATIONS
• Sulfonylureas and Meglitinides: These
medications can cause hypoglycemia, weight
gain, and, in some cases, digestive issues like
upset stomach.
• Thiazolidinediones (TZDs): TZDs can lead to
weight gain and fluid retention. There may also
be an increased risk of bone fractures and, in rare
cases, liver issues.
• Alpha-Glucosidase Inhibitors: These drugs can
cause digestive problems, including gas, bloating,
and diarrhea.
 SIDE EFFECTS OF ORAL
MEDICATIONS
• DPP-4 Inhibitors: DPP-4 inhibitors are generally
well-tolerated but can cause joint pain or
pancreatitis in rare cases.
• SGLT-2 Inhibitors: These drugs may lead to
urinary tract infections and an increased risk of
genital yeast infections. Dehydration and low
blood pressure are also potential side effects.
• Bile Acid Sequestrants: Digestive side effects
like constipation and abdominal discomfort can
occur.
SIDE EFFECTS OF INSULIN THERAPY

• Hypoglycemia: Too much insulin or mismatched

doses with meals can cause low blood sugar,
leading to dizziness, confusion, and even loss of
consciousness.
• Weight Gain: Some individuals may experience
weight gain when using certain types of insulin.
• Allergic Reactions: While rare, some individuals
may be allergic to insulin.