DRUGS

AFFECTING
THE
ENDOCRINE
SYSTEM
A PRESENTATION BY 2BSN-B GROUP #6
 GROUP MEMBERS:

Dimacutac, Espartero, Gabaldon, Gonzales, Hernandez,

John Lloyd Kate Kylei Franky Merry Joana Kiel
Joyce

Hibaya, Imperial, Ines, Jubelag,

Emaline Caesar Ean Harriet Karylle Heaven Kirk
 Topic Outline:

Hypothalamic and
1 Endocrine system 2 pituitary agents

Thyroid and Parathyroid

3 Adrenocortical agents 4 agents

5 Agents to control blood glucose levels

 1
THE INTRODUCTION OF
ENDOCRINE SYSTEM
 2
HYPOTHALAMIC AND PITUITARY
AGENTS
Pituitary Gland Hypothalamus
Hypothalamus
- is an area of the brain that produces hormones
that control:
 Body temperature
 Heart rate
 Hunger
DRUGS AFFECTING HYPOTHALAMIC
HORMONES

Angonist Antagonist
-corticotropin-releasing hormone -Abarelix
-gonadorelin -Ganirelix
-goserelin -Leuprolide
-sermorelin -Nafarelin
Corticotropin - releasing hormone (CRH)
( generic)
Indication: Diagnosis of cushing's syndrome. Studied for peritumoral brain edema

Mechanism of Action: Stimulates DNA synthesis and replication, and in a functional

adrenal tumor in tissue culture, ACTH inhibits DNA synthesis and replication. ACTH and
cAMP thus appear to direct the adrenal cell toward the differentiated, maximally functional
state.

Side Effects: Nervous problems such as clinical depression, anxiety, sleep disturbances
and anorexia nervosa.

Contraindications: A history of a previous adverse reaction to ACTH. Scleroderma,

osteoporosis, systemic fungal infections, ocular herpes simplex, peptic ulcer and
hypertension.
 Gonadorelin (Factrel)
Indication: Evaluation of functional capacity and response gonadotropes of anterior
pituitary. Gonadotropin releasing hormone.

Mechanism of Action: Induces release of endogenous luteinizing hormone (LH) to produce

this same effect. Gonadorelin, through release of LH has been demonstrated to induce
ovulation of dominant ovarian follicles present on the bovine ovary during the estrous cycle.

Side Effects: hives, difficulty breathing, swelling of your face, lips, tongue, or throat,
flushing (continuing), rapid heartbeat, hardening of skin at the place of injection, itching,
pain, redness or swelling of skin at place of injection, and skin rash

Contraindications: Hypersensitivity to gonadorelin hydrochloride or any of the

components.
 Goserelin (Zoladex)
Indication: Diagnosis of hypothalamic or pituitary dysfunction in short children; evaluation
response to the surgery or irradiation. Treatment of idiopathic growth failure. As an adjunct
to gonadorelin to stimulate ovulation. AIDS associated cachexia(orphan drug uses).
Gonadotropin releasing hormone (GnRH) agonists.

Mechanism of Action: Acts as an inhibitor of pituitary gonadotropin secretion when

administered in the biodegradable formulation.

Side Effects: tingling in your fingers or toes. hair loss, weight gain, joint pain, changes in
blood pressure.

Contraindications: Those patients who have a known hypersensitivity to GnRH, GnRH

agonist analogues or any of the components in ZOLADEX
 Abarelix (Phenaxis)
Indication: Innovation of premature luteinizing hormone surge in women undergoing
controlled ovarian stimulation as part of a fertility program.

Mechanism of Action: Directly suppressing luteinizing hormone (LH) and follicle stimulating
hormone (FSH) secretion and thereby reducing the secretion of testosterone by the testes.

Side Effects: hot flashes; sleep disturbances; breast enlargement or pain; diarrhea or
constipation; swelling; nausea; dizziness; headache

Contraindications: In those patients with a known hypersensitivity to any of the

components in abarelix for injectable suspension.
 Abarelix (Phenaxis)
Indication: Innovation of premature luteinizing hormone surge in women undergoing
controlled ovarian stimulation as part of a fertility program.

Mechanism of Action: Directly suppressing luteinizing hormone (LH) and follicle stimulating
hormone (FSH) secretion and thereby reducing the secretion of testosterone by the testes.

Side Effects: hot flashes; sleep disturbances; breast enlargement or pain; diarrhea or
constipation; swelling; nausea; dizziness; headache

Contraindications: In those patients with a known hypersensitivity to any of the

components in abarelix for injectable suspension.
 Ganirelix (Antagon)
Indication: Inhibition of premature luteinizing hormone surge in women undergoing
controlled ovarian stimulation as part of a fertility program.

Mechanism of Action: Modulates the hypothalamic-pituitary-gonadal axis by causing a

rapid, profound, reversible suppression of endogenous gonadotropins

Side Effects: Acetate Injection include redness or pain at the injection site reactions (pain,
redness, or irritation), headache, mild nausea, stomach pain, tiredness, pelvic pain (similar
to menstrual cramps), or vaginal bleeding.

Contraindications: Known hypersensitivity to Ganirelix Acetate or to any of its components.

 Nafarelin (Synarel)
Indication: Treatment of endometriosis and precocious puberty.

Mechanism of Action: Stimulates the release of the pituitary gonadotropins, luteinizing

hormone (LH) and follicle-stimulating hormone (FSH), resulting in a temporary increase of
gonadal steroidogenesis.

Side Effects: acne, changes in breast size vaginal bleeding (menstruation should stop with
this medication) mood swings, increase in pubic hair, body odor, oily, flaky, or scaly skin,
nasal irritation.

Contraindications: Hypersensitivity, Undiagnosed vaginal bleeding, Pregnancy/breast

feeding, Caution in PCOS and Osteoporosis, Dyslipidemia
Pituitary Gland
The pituitary sits in a depression in the skull
located just below the third ventricle of the
brain; The pituitary has two divisions: the
anterior pituitary (or adenohypophysis) and
posterior pituitary (or neurohypophysis).
Both divisions are under hypothalamic
control. The hypothalamus communicates
with the anterior pituitary by way of release-
regulating factors delivered through a
system of portal blood vessels. In contrast,
communication with the posterior pituitary is
neuronal.
DRUGS AFFECTING ANTERIOR
PITUITARY HORMONES
GROWTH HORMONE AGONIST
- somatropin
- somatropin rDNA origin

GROWTH HORMONE ANTAGONIST

- bromocriptine mesylate
- octreotide acetate
- pegvisomant

DRUGS AFFECTING OTHER ANTERIOR PITUITARY

- chorionic gonadotropin
chorionic gonadotropin alfa
- Corticotropin
- cosyntropin
-menotropins
- thyrotropin alfa
 Somatropin
Growth Hormone Agonist

Nutropin Saizen Humatrope

 Somatropin

Mechanism of Action
Replaces human growth
hormone; stimulates skeletal
growth, growth of internal
organs, and protein synthesis.
 Somatropin
Indications
Treatment of children with growth failure
due to lack of growth hormone (GH) or to
chronic renal failure; replacement of GH in
patients with GH deficiency; long-term
treatment of growth failure in children born
small for gestational age who do not
achieve catch-up growth by 2 yr of age;
treatment of short stature associated with
Turner syndrome or Prader-Willi syndrome;
also approved to increase protein
production and growth in various AIDS-
related states
Contraindications
Contraindicated with any known allergy to the
drug or ingredients in the drug to avoid
hypersensitivity reactions. It is also
contraindicated in the presence of closed
epiphyses or with underlying cranial lesions
because of the risk of serious complications, and
with abdominal surgery and acute illness
secondary to complications of open-heart surgery
because of potential problems with healing. It
should be used with caution in pregnancy and
lactation because of the potential for adverse
effects on the fetus.
 Somatropin

Side Effects
• skin thickening at injection site
• injection site pain, redness, swelling, or itching
• headache
• muscle or joint pain
• sore throat, cough, fever, or other signs of infection
• ear pain
• flatulence or large amounts of gas in the intestines or
bowels
• hair loss
Somatropin rDNA origin (Zorbtive)
Growth Hormone Agonist
Somatropin rDNA origin (Zorbtive)

Mechanism of Action
The actions of somatropin on the gut may be
direct or mediated via the local or systemic
production of IGF-1. In human clinical studies
the administration of growth hormone has
been shown to enhance the transmucosal
transport of water, electrolytes, and nutrients
 Somatropin rDNA origin (Zorbtive)
Indications
Reserved for use in treatment of adults with •
short bowel syndrome who are receiving
specialized nutritional support
Contraindications
active malignancy
• acute critical illness due to complications
following open heart or abdominal surgery,
multiple accidental trauma or acute
respiratory failure
• active proliferative or severe non-proliferative
diabetic retinopathy
• hypersensitivity to somatropin or any of the
excipients of Zorbtive. Systemic
hypersensitivity reactions have been reported
with postmarketing use of somatropin
products
Somatropin rDNA origin (Zorbtive)

Side Effects
nausea, vomiting, stomach pain, gas, and injection
site reactions (soreness, redness, rash, skin
bumps, itching, pain, bruising or swelling).
Bromocriptine mesylate (Parlodel)
Growth Hormone Antagonist
Bromocriptine mesylate (Parlodel)

Mechanism of Action
Binds dopamine receptors and inhibits pituitary
prolactin secretion
Bromocriptine mesylate (Parlodel)
Indications
Treatment of acromegaly in patients who
are not candidates for or cannot tolerate
other therapy; not recommended for
children <15 yr
Contraindications
• The drug should be withdrawn in those who
may experience hypertensive disorders of
pregnancy (including eclampsia,
preeclampsia, or pregnancy-induced
hypertension) unless withdrawal of Parlodel is
considered to be medically contraindicated.
• The drug should not be used during the
postpartum period in women with a history of
coronary artery disease and other severe
cardiovascular conditions unless withdrawal
is considered medically contraindicated. If the
drug is used in the postpartum period, the
patient should be observed with caution
Bromocriptine mesylate (Parlodel)

Side Effects
• mild headache
• depression
• dizziness
• spinning sensation
• tired feeling
• drowsiness
• sleep problems (insomnia)
• nausea
Octreotide (Sandostatin)
Growth Hormone Antagonist
Octreotide (Sandostatin)

Mechanism of Action
target somatostatin receptors
 Octreotide (Sandostatin)

Indications Contraindications

Treatment of acromegaly in adults who are Contraindicated in known hypersensitivity to

not candidates for or cannot tolerate other
therapy
octreotide or any excipient. As it inhibits gall
bladder motility, bile acid secretion and bile flow,
worsening of liver disease in patients whose
disease stems from biliary obstruction might be
anticipated..
 Octreotide (Sandostatin)

Side Effects
Nausea, vomiting, loose/oily stools, constipation,
stomach upset, gas, bloating, dizziness, or
headache may occur. Pain and irritation at the
injection site may also occur.
Pegvisomant (Somavert)
Growth Hormone Antagonist
 Pegvisomant (Somavert)

Mechanism of Action
Selectively binds to growth hormone (GH)
receptors on cell surfaces, where it blocks the
binding of endogenous GH, and thus interferes
with GH signal transduction.
 Pegvisomant (Somavert)

Indications Contraindications

Treatment of acromegaly in adults who are patients with a history of hypersensitivity to any
not candidates for or who cannot tolerate of its components
other therapy
 Pegvisomant (Somavert)

Side Effects
• thickening of the skin or a hard lump where you
injected the medicine; easy bruising; or.

• liver problems--nausea, upper stomach pain,

itching, tired feeling, loss of appetite, dark urine,
clay-colored stools, jaundice (yellowing of the
skin or eyes).
Chorionic Gonadotropin (Chorex, others)
Drugs Affecting Other Anterior Pituitary
Chorionic Gonadotropin (Chorex, others)

Mechanism of Action
It stimulates production of gonadal steroid
hormones by stimulating the interstitial cells
(Leydig cells) of the testis to produce
androgens and the corpus luteum of the ovary
to produce progesterone.
Chorionic Gonadotropin (Chorex, others)

Indications Contraindications

Treatment of male hypogonadism, to • Hypersensitivity to Human Chorionic

induce ovulation in females with functioning Gonadotropin.
ovaries, for treatment of prepubertal • early puberty (also called precocious
puberty); or.
cryptorchidism when there is no anatomical • hormone-related cancer (such as prostate
obstruction to testicular movement cancer).
• a thyroid or adrenal gland disorder.
• an ovarian cyst;
• premature puberty.
Chorionic Gonadotropin (Chorex, others)

Side Effects
• acne.
• changes in emotions or mood.
• facial hair growth.
• headache.
• pain, irritation or inflammation at the injection
site.
• tiredness.
• upset stomach
Chorionic Gonadotropin Alfa (Ovidrel)
Drugs Affecting Other Anterior Pituitary
Chorionic Gonadotropin Alfa (Ovidrel)

Mechanism of Action
Binds to the LH/hCG receptor of the granulosa
and theca cells of the ovary to effect these
changes in the absence of an endogenous LH
surge.
Chorionic Gonadotropin (Chorex, others)

Indications Contraindications

Induction of ovulation in infertile females 1. Prior hypersensitivity to hCG preparations or

who have been pretreated with FSH one of their excipients.
2. Primary ovarian failure.
3. Uncontrolled thyroid or adrenal dysfunction.
4. An uncontrolled organic intracranial lesion
such as a pituitary tumor.
5. Abnormal uterine bleeding of undetermined
origin (see “Selection of Patients”).
6. Ovarian cyst or enlargement of
undetermined origin (see “Selection of
Patients”).
7. Sex hormone dependent tumors of the
reproductive tract and accessory organs.
8. Pregnancy.
Chorionic Gonadotropin (Chorex, others)

Side Effects
Nausea, vomiting, mild abdominal pain/swelling,
headache, and pain/bruising/redness/swelling at
the injection site may occur
 Corticotropin (Acthar)
Drugs Affecting Other Anterior Pituitary
 Corticotropin (Acthar)

Mechanism of Action
Engaged MCRs on the adrenal cortex to
secrete free cortisol at levels slightly above
normal endogenous range. This is thought to
produce an indirect anti-inflammatory effect.
 Corticotropin (Acthar)
Indications
Diagnosis of adrenal function, treatment of
various inflammatory disorders
Contraindications
• for intravenous administration.
• in infants under 2 years of age who have
suspected congenital infections.
• with concomitant administration of live or live
attenuated vaccines in patients receiving
immunosuppressive doses of Acthar Gel.
• in patients with scleroderma, osteoporosis,
systemic fungal infections, ocular herpes
simplex, recent surgery, history of or the
presence of a peptic ulcer, congestive heart
failure, uncontrolled hypertension, primary
adrenocortical insufficiency, adrenocortical
hyperfunction, or sensitivity to proteins of
porcine origin.
 Corticotropin (Acthar)

Side Effects
• increased blood pressure;
• thinning skin, increased sweating;
• fluid retention (swelling in your hands or feet,
puffiness in your face);
• mood changes, irritability;
• increased appetite; or
• weight gain
 Cosyntropin (Cortrosyn)
Drugs Affecting Other Anterior Pituitary
 Cosyntropin (Cortrosyn)

Mechanism of Action
Stimulates the adrenal glands to release the
hormones cortisol and adrenaline.
 Cosyntropin (Cortrosyn)

Indications Contraindications

Diagnosis of adrenal function The only contraindication to CORTROSYN

(cosyntropin) for Injection is a history of a
previous adverse reaction to it. CORTROSYN
(cosyntropin) for Injection exhibits the full
corticosteroidogenic activity of natural ACTH.
 Cosyntropin (Cortrosyn)

Side Effects
• hives,
• difficulty breathing,
• swelling of your face, lips, tongue, or throat,
• itching,
• red, swollen, blistered, or peeling skin with or
without fever,
• wheeze,
• tightness in the chest or throat,
• difficulty swallowing or talking
 Menotropins (Pergonal)
Drugs Affecting Other Anterior Pituitary
 Menotropins (Pergonal)

Mechanism of Action
facilitating the production and maturation of
follicles (which contain eggs) in the ovaries or
induce ovulation (egg production) in a woman
 Menotropins (Pergonal)

Indications Contraindications

Used as fertility drug to stimulate ovulation If you have a tumor of the hypothalamus or
and spermatogenesis pituitary gland (in the brain). If you have a cyst in
the ovaries. If you have vaginal bleeding due to
an unknown reason. If you have womb cancer.
 Cosyntropin (Cortrosyn)

Side Effects
• Abdominal or stomach pain (severe)
• bloating (moderate to severe)
• decreased amount of urine.
• feeling of indigestion.
• nausea, vomiting, or diarrhea (continuing or
severe)
• pelvic pain (severe)
• shortness of breath.
• weight gain (rapid)
 Thyrotropin alfa (Thyrogen)
Drugs Affecting Other Anterior Pituitary
 Thyrotropin alfa (Thyrogen)

Mechanism of Action
Stimulates iodine uptake and organification,
and synthesis and release of thyroglobulin,
triiodothyronine (T3) and thyroxine (T4). In
patients with well-differentiated thyroid cancer,
a near total or total thyroidectomy is
performed.
 Thyrotropin alfa (Thyrogen)

Indications Contraindications

Adjunctive treatment for post-radioiodine Contraindicated in lactating women

ablation of thyroid tissue in patients with because RAI concentrates in the breast
near-total thyroidectomy and well- tissue and increases the risk of radiation
differentiated thyroid cancer without breast toxicity (refer to the therapeutic RAI
metastasis Prescribing Information).
 Thyrotropin alfa (Thyrogen)

Side Effects
• hives,
• difficulty breathing,
• swelling of your face, lips, tongue, or throat,
• itching,
• red, swollen, blistered, or peeling skin with or
without fever,
• wheezing,
• unusual hoarseness,
• weakness on one side of the body
 DRUGS AFFECTING
POSTERIOR PITUITARY HORMONES

Desmopressin (DDAVP,
Stimate)
 Desmopressin (DDAVP, Stimate)

Mechanism of Action
By mimicking the actions of endogenous ADH,
desmopressin acts as a selective agonist of
V2 receptors expressed in the renal collecting
duct (CD) to increase water re-absorption and
reduce urine production.
 Desmopressin (DDAVP, Stimate)

Indications Contraindications

Treatment of neurogenic diabetes Contraindicated in patients with moderate

insipidus, von Willebrand disease, to severe renal impairment (defined as a
hemophilia; being studied for the treatment creatinine clearance below 50ml/min).
of chronic autonomic failure DDAVP (desmopressin acetate tablets) is
contraindicated in patients with
hyponatremia or a history of hyponatremia.
Desmopressin (DDAVP, Stimate)

Side Effects
• Confusion.
• convulsions.
• decreased urine output.
• dizziness.
• fast or irregular
heartbeat.
• headache.
• increased thirst.
• muscle pain or cramps
 3
ADRONOCORTICAL AGENTS
 The Adrenal Glands
Adrenal glands, also known as suprarenal glands, are small,
triangular-shaped glands located on top of both kidneys, that
produce hormones that help regulate your metabolism, immune
system, blood pressure, response to stress and other essential
functions. Each gland is made of an inner core called the Adrenal
Medulla and an outer shell called Adrenal Cortex.

Adrenal Medulla
The adrenal medulla, the inner part of an adrenal gland, controls
hormones that initiate the flight or fight response. The main
hormones secreted by the adrenal medulla include epinephrine
(adrenaline) and norepinephrine (noradrenaline), which have
similar functions.

Adrenal Cortex
The adrenal cortex is the outer part of your adrenal gland. It
produces hormones that support vital organ functions and bodily
processes. Many conditions can affect the adrenal cortex. Some
cause the overproduction of hormones, while others limit hormone
production.
 Adrenocortical Agents

Adrenocortical agents are drugs used as short-term treatment to suppress immune

system in patients with inflammatory disorders. They are also used for replacement
therapy to maintain hormone levels when adrenal glands are not functioning
adequately.

The 3 types of Corticosteroids;

1. Androgen
2. Glucocorticoids
3. Mineralocorticoids
DRUG CLASSIFICATION
• ANDROGEN

• GLUCOCORTICOIDS

• MINERALOCORTICOIDS
 GLUCOCORTICOIDS

Glucocorticoids are powerful medicines that fight inflammation

and work with your immune system to treat wide range of
health problems.

Your body actually makes its own glucocorticoids. These

hormones have many jobs, such as controlling how your
cells use sugar and fat and curbing inflammation.
Sometimes, though, they aren’t enough. That’s when the
man-made versions can help.
 PREDNISONE
DRUG
Prednisone is a synthetic
corticosteroid that has CLASSIFICATION
• ADRENOCORTICAL
anti-inflammatory
properties. It works to
AGENTS
suppress the body's THERAPEUTIC
immune system by CLASS
reducing the activity of • CORTICOSTEROIDS
inflammatory
substances in the
body.
 MECHANISM OF ACTION
Actions Enters target cells and binds to
intracellular corticosteroid receptors, initiating
many complex reactions responsible for its anti-
inflammatory and immunosuppressive effects.
 INDICATIONS/THERAPEUTIC USES

• Indications: Replacement therapy in adrenal cortical insufficiency,

short-term management of various inflammatory and allergic
disorders, hypercalcemia associated with cancer. hematological
disorders, ulcerative colitis, acute exacerbations of multiple
sclerosis, palliation in some leukemias, trichinosis with systemic
involvement.
Side Effects Adverse Effects

WEIGHT GAIN CHRONIC INSOMNIA

INDIGESTION CUSHING SYNDROME
INSOMNIA LETHARGY
 CONTRAINDICATIONS
Prednisone has a tendency to raise the level of
glucose, or sugar, in the blood, which can
cause increased body fat or diabetes in some
people. It is important to avoid "simple
carbohydrates and concentrated sweets, such
as cakes, pies, cookies, jams, honey, chips,
breads, candy and other highly processed
foods.
 MINERALOCORTICIODS

Mineralocorticoids are a class of corticosteroids,

which in turn are a class of steroid hormones.
Mineralocorticoids are produced in the adrenal cortex
and influence salt and water balances.
 FLUDROCORTISONE
Fludrocortisone is a synthetic DRUG
corticosteroid medication CLASSIFICATION
primarily used to treat • ADRENOCORTICAL
conditions like adrenal
insufficiency by helping
AGENTS
regulate salt and water THERAPEUTIC
balance in the body.
CLASS
A synthetic adrenal steroid • CORTICOSTEROIDS
with high
mineralocorticoid activity
that is a commonly used
drug to treat adrenocortical
insufficiency.
 MECHANISM OF ACTION
Fludrocortisone's primary mechanism of action
involves its binding to mineralocorticoid receptors,
promoting the retention of sodium and excretion of
potassium in the kidneys. This leads to increased water
retention and helps regulate electrolyte balance in the
body.
 INDICATIONS/THERAPEUTIC USES

Fludrocortisone is mainly indicated for the treatment of

conditions associated with adrenal insufficiency, such as
Addison's disease. It helps to replace deficient levels of
mineralocorticoids and glucocorticoids in the body, contributing
to electrolyte balance and overall hormonal regulation.
 Side Effects Adverse Effects
FRONTAL AND OCCIPITAL
FLUID RETENSION,HIGH HEADACHES,
BLOOD PRESSURE, LOW ARTHRALGIA,
LEVEL OF POTASSIUM WEAKNESS, INCREASED
BLOOD VOLUME,EDEMA,
HYPERTENSION, HEART
(Other potential side effects can involve FAILURE, RASH,
changes in mood or behavior,
gastrointestinal issues, and increased ANAPHYLAXIS.
susceptibility to infections.)
 CONTRAINDICATIONS

Potassium-depleting diuretics, Acute

glomerulonephritis, Hypercortisolism,
Viral or bacterial skin diseases
uncontrolled by antibiotics
 4
THYROID AND PARATHYROID
AGENTS
Drugs used to treat thyroid disease
 THYROID GLAND

• Thyroid is a small, butterfly-shaped gland located at the

front of your neck under your skin.

• It’s a part of your endocrine system and controls many of

your body’s important functions by producing and
releasing (secreting) certain hormones like Thyroxine
(T4), Triiodothyronine (T3), Reverse triiodothyronine
(RT3) and Calcitonin.
In response to low levels of thyroid hormone in the blood,
the hypothalamus releases thyrotropin-releasing
hormone (TRH) to the anterior pituitary. The pituitary
then releases thyroid-stimulating hormone (TSH) to
the thyroid gland, which releases thyroid hormone (T3
and T4) into the bloodstream. When thyroid hormone
levels increase in the blood, the pituitary decreases
production and release of TSH. This negative feedback
process is regulated by the hypothalamus, ensuring the
thyroid hormone levels stay within normal limits.
 THYROID GLAND

• Thyroid agents are used to replace thyroid hormone

when the function is low or to suppress thyroid
function when it is too high.

• They include thyroid hormones and antithyroid drugs,

which are further classified as Thioamides and Iodine
solutions.
DRUG CLASSIFICATION

• THYROID HORMONES

• ANTITHYROID AGENTS
 THYROID HORMONE
● There are several hormone replacement products
available for treating hypothyroidism.

● These products replace low levels of natural thyroid

hormone and suppress the overproduction of TSH
by the pituitary. They can contain both natural and
synthetic thyroid hormone.
 LEVOTHYROXINE
Levothyroxine, a DRUG
synthetic salt of •CLASSIFICATION
THYROID
T4, is the most HORMONE
commonly used THERAPEUTIC
replacement CLASS
hormone due to • HORMONE
its predictable
bioavailability
and reliability.
 MECHANISM OF ACTION
Triiodothyronine (T3) and L-thyroxine (T4) diffuse
into the cell nucleus and bind to thyroid receptor
proteins attached to DNA. This hormone nuclear
receptor complex activates gene transcription and
synthesis of messenger RNA and cytoplasmic proteins.
 INDICATIONS/THERAPEUTIC USES

• Thyroid replacement hormones increase the metabolic rate of body

tissues, leading to increased oxygen consumption, respiration, heart
rate, growth, and metabolism of fats, carbohydrates, and proteins.

• They are used for replacement therapy in hypothyroidism, treatment

of myxedema coma, suppression of TSH in goiters treatment and
prevention, and management of thyroid cancer.

• They are also used in conjunction with antithyroid drugs for treating
thyroid toxicity, preventing goiters formation during thyroid
overstimulation, and treating thyroid overstimulation during
pregnancy.
 Side Effects Adverse Effects
Increased appetite
Tremors
Weight loss Headache
Heat sensitivity Palpitation
Excessive sweating Tachycardia
Headache Nausea
Vomiting
Hyperactivity Skin Allergy
Nervousness Diarrhea
Anxiety
 CONTRAINDICATIONS
• Acute myocardial infarction.
• Uncorrected adrenal insufficiency.
• Acute myocarditis, pancarditis.
• Active cardiac arrhythmias.
• Thyrotoxicosis.
• Hyperthyroidism
 ANTITHYROID AGENTS
• Drugs used to block the production of thyroid
hormone and to treat hyperthyroidism include
the Thioamides and Iodide solutions.
• These groups of drugs are not chemically
related, they both block the formation of
thyroid hormones within the thyroid gland.
Thioamides
• The most common anti thyroid drugs which act by inhibiting the enzyme
thyroid peroxidase, thus reducing the synthesis of TH in the thyroid.
Propylthiouracil
Propylthiouracil is a
DRUG
• CLASSIFICATION
medication used to treat
hyperthyroidism. This THIOAMIDES
includes hyperthyroidism
due to Graves’ disease and
toxic multinodular goiter. THERAPEUTIC CLASS
In a thyrotoxic crisis it is • ANTITHYROID AGENTS
generally more effective
than methimazole.
 MECHANISM OF ACTION
These drugs are well absorbed from the GI tract and are then
concentrated in the thyroid gland. The onset and duration of
PTU varies with each patient. Methimazole has an onset of
action of 30 to 40 minutes and peaks in about 60 minutes.
Some excretion can be detected in the urine. Methimazole
crosses the placenta and is found in a high ratio in breast
milk. PTU has a low potential for crossing the placenta and
for entering breast milk.
 INDICATIONS/THERAPEUTIC USES
• Thioamides lower thyroid hormone levels by
preventing the formation of thyroid hormone
in the thyroid cells, which lowers the serum
levels of thyroid hormone.
• They also partially inhibit the conversion of
T4, to T3, at the cellular level. These drugs
are indicated for the treatment of
hyperthyroidism.
 SIDE EFFECTS ADVERSE EFFECTS

Abnormal loss of hair Neuritis

Dizziness Vertigo
Heartburn Drowsiness
Hives Skin rash
Loss of taste Skin pigmentation
Pain in the chest, upper Nausea
stomach, or throat. Vomiting
 CONTRAINDICATIONS

Hypersensitivity,
Indiosyncratic Reaction to Thioamides
IODINE SOLUTION
-Iodide solution treats overactive thyroid and protects your thyroid
glands from the effects of radioactive iodine

STRONG IODINE SOLUTION

Used to treat overactive DRUG CLASSIFICATION

thyroid, iodine
• THIOAMIDES
deficiency, and to protect
the thyroid gland from
the effects of radiation THERAPEUTIC DRUG
from radioactive forms of
iodine. • ANTITHYROID AGENTS
 MECHANISM OF ACTION
Iodine rapidly penetrates into
microorganisms and oxidizes key proteins,
nucleotides, and fatty acids, eventually
leading to cell death
 INDICATIONS/THERAPEUTIC USES

• Used to treat overactive thyroid, iodine

deficiency, and to protect the thyroid gland
from the effects of radiation from radioactive
forms of iodine.
• Adjunct therapy for hyperthyroidism
 SIDE EFFECTS ADVERSE EFFECTS

Burning of mouth or throat Rash

Confusion Hypothyroidism
Headache (severe) Allergic reaction
Increased watering of mouth Swelling of the salivary
Irregular heartbeat
Metallic taste
gland
Numbness
 CONTRAINDICATIONS
Iododerma
Laryngeal edema
Swelling of salivary glands or increased
salivation upon previous exposure to
iodides
Allergy to Antithyroid Drugs
 5
AGENTS TO CONTROL BLOOD
GLUCOSE LEVELS
Antidiabetic and Glucose-Elevating Agents
 SULFONYUREAS
AND OTHER GLUCOSE-
INSULIN ANTIDIABETIC ELEVATING
AGENTS AGENTS

Only parenteral Other antidiabetic Raises the blood level

antidiabetic agent agents may be used in of glucose when
available for patients who will still severe hypoglycemia
exogenous have a functioning occurs (less than 40
replacement. pancreas. mg/dL).
 INSULIN
Insulin circulates through the body and reacts with specific insulin receptor
sites to stimulate the transport of glucose into the cells to be used for energy,
a process called facilitated diffusion.

Indication/Therapeutic Uses: Mechanism of Action:

Used to treat type 1 diabetes and type 2 Insulin acts by directly binding to its
diabetes of more severe cases. receptors on the plasma membranes
of the cells.
Stimulates the synthesis of glycogen
from glucose, of fats from lipids, and of
proteins from amino acids.
 INSULIN
Side Effects: Adverse Effects:
Convulsions (seizures)
Unconsciousness Hypoglycemia
Low blood sugar (mild) Ketoacidosis
Weight gain Electrolyte disturbances like hypokalemia
Depressed skin at the place of injection Pain at the injection site
swelling of face, fingers, feet, or ankles Lipodystrophy at the injection site
Thickening of the skin at the place of injection

Contraindications:
No absolute contraindications.
Care should be taken during pregnancy and lactation.
 SULFONYLUREAS
Bind to potassium channels on pancreatic beta cells.
They may improve insulin binding to insulin receptors and increase the
number of insulin receptors.
Effective only in patients who have functioning beta cells.
Further classified as first-generation or second-generation sulfonylureas.

First-gen sulfonylureas Second-gen sulfonylureas

Include glimepiride (Amaryl). glipizide
Include chlorpropamide (Diabinese),
(Glucotrol), and glyburide (DiaBeta and
tolazamide (Tolinase), and tolbutamide
others).
(Orinase).
Have several advantages over the first-
The use of these drugs has been steadily
generation drugs, including the following:
declining as more effective drugs have
 Excreted in urine and bile.
become available.
 Does not interact with as many
Associated with an increased risk of
protein-bound drugs as the first-gens.
cardiovascular disease and death.
 Have a longer duration of action.
 SULFONYLUREAS
Indication/Therapeutic Uses:
Stimulate insulin release from the
beta cells in the pancreas.
Improve insulin binding to
insulin receptors
May actually increase the number
of insulin receptors.
Adjunct to diet and exercise to
lower blood glucose levels in
type 2 diabetes mellitus.
Mechanism of Action:
Rapidly absorbed from the GI tract
and undergo hepatic metabolism
Their primary mechanism of action
is to close ATP-sensitive K-
channels in the beta-cell plasma
membrane, and so initiate a chain
of events which results in insulin
release.
 SULFONYLUREAS
Adverse Effects:
Side Effects: Hypoglycemia
Nausea and vomiting
Low blood sugar (mild) Epigastric discomfort
Skin reactions (erythema Heartburn
multiforme, exfoliative dermatitis) Anorexia
Photosensitivity Allergic skin reactions
Increased risk of cardiovascular mortality
(1st -gen agents)

Contraindications:
Known allergy to any sulfonylureas
Type 1 diabetics
Pregnancy
 GLUCOSE-ELEVATING AGENTS
Used in the following events:
 Hypoglycemia  Certain cancers
 Pancreatic disorders  Disorders of the anterior pituitary
 Kidney disease  Unbalanced treatment of diabetes mellitus
Two agents used in these conditions:
 Diazoxide (Proglycenn)  Glucagon (GlucaGen)

Indication/Therapeutic Uses:
Increase the blood glucose level by Mechanism of Action:
decreasing insulin release and accelerating Glucagon causes the liver to convert
stored glycogen into glucose, which
the breakdown of glycogen in the liver to
is released into the bloodstream.
release glucose.
Treatment of hypoglycemic reactions
Management of severe hypertension
(Diazoxide)
GLUCOSE-ELEVATING AGENTS
Adverse Effects: Contraindications:
Diazoxide:
Hypotension Diazoxide:
Glucagon: Headache Known allergies to
Glucose:
Nausea and Cerebral ischemia sulfonamides or
None
vomiting Weakness thiazides
Heart failure Pregnancy
Arrythmias
 SULFONYLUREAS AND OTHER
ANTIDIABETIC AGENTS
Other antidiabetic agents may be used in patients who still have a
functioning pancreas. These agents include the sulfonylureas and other
agents that do not fit into a specific classification (see The sulfonylureas
were the first oral agents introduced to treat type 2 diabetes.
 SULFONYLUREAS
The sulfonylureas bind to potassium channels on pancreatic beta cells.
They may improve insulin binding to insulin receptors and increase the
number of insulin receptors. They are also known to increase the effect
of antidiuretic hormone on renal cells. They are effective only in patients
who have
 FIRST-GENERATION SULFONYLUREAS
The first-generation sulfonylureas include chlorpropamide (Diabinese),
tolazamide (Tolinase), and tolbutamide (Orinase). However, the use of these
drugs has been steadily declining as more effective drugs have become
available. Some patients may still be treated with these drugs.
Chlorpropamide has been the most frequently used of the group because it
has the most predictable effects and has been proven to be very to be very
reliable. Tolbutamide is preferred for patients with renal dysfunction, who may
not be able to excrete chlorpropamide, because it is more easily cleared from
the body. Tolazamide, which is used even less frequently, is usually tried after
the first two drugs have been shown to be ineffective. It is not as predictably
effective in many patients, but it can be very effective in some patients who do
not respond to chlorpropamide. Tolbutamide and tolazamide are sometimes
used in combination with insulin to reduce the insulin dose and decrease the
risk of hypoglycemia in certain type 2 diabetics who have begun to use insulin
to control their blood glucose level.
The first-generation sulfonylureas were associated with an increased risk of
cardiovascular disease and death in a somewhat controversial study.

SECOND-GENERATION SULFONYLUREAS
The second-generation drugs include glimepiride (Amaryl). glipizide (Glucotrol), and
glyburide (DiaBeta and others for usual indications for each drug. Second- generation
sulfonylureas have several advantages over the first- generation drugs, including the
following:
• They are excreted in urine and bile, making them safer for patients with renal
dysfunction.
• They do not interact with as many protein-bound drugs as the first-generation drugs.
• They have a longer duration of action, making it possible to take them only once or
twice a day, thus increasing compliance.
Glimepiride is a much less expensive drug than most of the other sulfonylureas, which
has advantages for some people.
 OTHER ANTIDIABETIC AGENTS
Several other antidiabetic agents are available. Although these drugs are
structurally unrelated to the sulfonylureas, they frequently are effective when
used in combination with sulfonylureas or insulin.
• Acarbose and miglitol are inhibitors of alpha-glucosidase (an enzyme that
breaks down glucose for absorption); they delay the absorption of glucose.
They have only a mild effect on glucose levels and have been associated
with severe hepatic toxicity.
• Metformin decreases the production and increases the uptake of glucose. It
is effective in lowering blood glucose levels and does not cause
hypoglycemia as the sulfonylureas do.
• The thiazolidinediones are drugs that decrease insulin resistance; they are
used in combination with sulfonylureas, insulin, or metformin to treat
patients with insulin resistance.
• The newest of the antidiabetic agents include pramlintide and exenatide,
which were released in 2005, and sitagliptin, which was made available in
2007.
• Pramlintide works to modulate gastric emptying after a meal, causes a
feeling of fullness or satiety, and prevents the postmeal rise in glucagon
that usually elevates glucose levels.
• Exenatide is an incretin that mimics the effects of GLP-1: enhancement of
glucose-dependent insulin secretion by the beta cells in the pancreas,
depression of elevated glucagon secretion, and slowed gastric emptying to
help moderate and lower blood glucose levels.
• Sitagliptin is a DDP-4 inhibitor. It slows the breakdown of GLP-1 in the
body, prolonging the effects of increased insulin secretion, decreased
glucagon secretion, and slowed GI emptying.
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