Hormones and related Drugs.pptx Pharmacolgy

Thyroid Hormone
The thyroid gland secretes three hormones, named thyroxine (T4)
triiodothyronine (T3) and calcitonin.
T3 & T4 are produced by thyroid follicle cell have similar biological
activity and the term 'thyroid hormone” restricted to these only.
Calcitonin produced by interfollicular 'C' cells and regulates calcium
metabolism.
usually produces more T4 hormone than T3, but T4 is converted to
T3 when it reaches cells and tissues in your body.
Thyroxine (T4) has 4 iodine molecules attached to its molecular
structure. When T4 gets into the cells of the body, it loses one
molecule and becomes T3.
Thyroid function tests that check both TSH and T4 levels are the
most accurate ways to diagnose thyroid conditions
Hypothyoridism and hyperthyroidism

Biosynthesis of thyroid hormone
Dietary iodine Inorganic iodide
lodide + Tyrosine Monoiodotyrosine (MDT)
MDT + lodide Diiodotyrosine (DIT)
coupling reaction bind with MDT & DIT T3 & T4
Hypothyroidism
Hypothyroidism is present when the thyroid gland is producing
little or no thyroid hormones.
This slows the body down
People of any age can develop hypothyroidism However,
women aged 60 and over are most prone to this

Symptoms:
- Weight gain - Muscle weakness:
- Sensitivity to cold - Puffy face
- Menstrual problems - Hair loss
- Tiredness - Depression
- Decreases heart rate - Dry skin etc.
Causes of hypothyroidism
lodine deficiency in diet (most common cause)
Autoimmune thyroiditis
Previous treatment with radioactive iodine
Injury to hypothalamus or anterior pituitary gland
Certain medications
Previous thyroid surgery etc.

Thyroxine
It is available in its salt form thyroxine sodium is a
synthetic thyroid hormone that is chemically identical to
thyroxine (T4), which is naturally secreted by the
follicular cells of the thyroid gland.
Mechanism of action
Thyroxin (T4) enters the cell
T4 converted to T3 (active metabolite)
T3 combines with thyroid hormone receptor that
regulates varied metabolic function.

Indication
Hypothyroidism
Cretinism,
Myxedema coma
Side-effect;
Tachycardia
Sweating
Hyperpyrexia, Headache
Heat intolerance
Weight loss
Thyrotoxicosis
CV collapse
Insomnia
Alopecia
Allergic reaction
Contraindication
hypersensitivity,
angina,
pituitary disease,
adrenal failure,
cardiac failure
Dose:
Adult: 50-100 mcg(µg) once
daily
Child: 5 µg/kg

Hyperthyroidism
Hyperthyroidism occurs when the thyroid gland over secretes
thyroid
Thus increasing the metabolic rate of the body and speeding up the
Radioactive iodine is the most common treatment given
Symptoms:
- weight loss - Enlarged thyroid gland
- Heat intolerance - Clubbing
- Heart palpitations - Eye problems
- Muscle weakness - Menstrual cycle changes
- Increase bowel movement -diarrhoea
Drugs Used in Hyperthyroidism
Propyltiouracil
Methimazole
Carbimazole

Propylthiouracil (PTU)
PTU or 6-n-propylthiouracil is a thiouracil-derived drug
It decrease the amount of thyroid hormone produced by thyroid
gland.
It has risk of serious liver injury, including liver failure and death
So no longer recommended in non pregnant adults and in children
as the front line antithyroid medication.
Mechanism of action
 It acts by inhibiting the enzyme thyroid peroxidase, which usually
converts iodide to an iodine molecule and incorporates the iodine
molecule into amino acid tyrosine.
Hence, DIT or MIT does not get produced, which are the main
constituents in the production of T4 and T3
Peripherally, it acts by inhibiting the conversion of T4 to T3

Indication
Graves' disease.
used to decrease symptoms of hyperthyroidism in preparation for
surgical removal of the thyroid gland or before radioactive iodine
therapy in patients.
Side-effect:
Acute liver injury, acute liver failure and death.
Hypothyroidism
Hypersensitivity
Potential teratogenicity
GI: nausea, stomach pain, vomiting
Contraindication
hepatitis, abnormal liver function tests
Pregnancy, blood disorde

Dose:
Adults: Initial dose is 300 to 900 mg TDS. The maintenance usually
100 to 150 mg daily.
Children (6 years of age and older): Initial dose is 50 mg TDS
Carbimazole
Carbimazole is a pro-drug as after absorption as it is converted to
the active form as Methimazole.
Mechanism of action
It acts as an inhibitor of thyroid peroxidase enzyme from coupling
and iodinating the tyrosine residues on thyroglobulin, hence
reducing the production of the thyroid hormones T3 and T4.
Indication:
It is used in the treatment of hyperthyroidism and thyrotoxicosis.
It is also used in the treatment of Grave's disease.

Contraindicated
hyperthyroidism due to nodular goiter
Adverse effects:
Blurred vision or double vision
continuous back-and-forth eye movements
Fever
Loss of taste
Sore throat
Mild leucopenia
Malaise
Mouth ulcer/Nausea
Alopecia
Dose:
Adult: 20-60 mg daily as single or divided dose
Child (4 to 12 year): 15 mg daily

Anti-diabetic drugs
Diabetes Mellitus (DM)
DM is a chronic condition that is characterized by raised of blood
glucose levels (Hyperglycemia).
The term diabetes mellitus describes a metabolic disorder of
multiple causes characterized by chronic hyperglycaemia with
disturbances of carbohydrate, fat and protein metabolism resulting
from defects in insulin secretion, insulin action, or both.
It is a metabolic disorder characterized by hyperglycaemia,
glycosuria, hyperlipidaemia, negative nitrogen balance and
sometimes ketonaemia.
The effects of DM include long-term damage, dysfunction and
failure of various organs.
It may present with characteristic symptoms such as thirst, polyuria,
blurring of vision, hunger, fatigue and weight loss.

Types
1) Type 1 diabetes (B-cell destruction)
2) Type 2 diabetes (Progressive insulin secretary defect)
Type I
It is a Insulin-dependent diabetes mellitus (IDDM) or juvenile onset
diabetes mellitus.
There is B-cell destruction in pancreatic islets;
 majority of cases are autoimmune (type 1A) antibodies that
destroy beta cells are detectable in blood but some are idiopathic
(type 1B) in where no B-cell antibody is found.
 In all type 1 cases circulating insulin levels are low or very low, and
patients are more prone to ketosis.
This type is less common and has a low degree of genetic
predisposition.

Type II
It is a Non-insulin-dependent DM (NIDDM) or maturity onset
diabetes mellitus.
There is no loss or moderate reduction in B-cell mass; insulin in
circulation is low, normal or even high, no anti B-cell antibody is
demonstrable;
It is caused by progressive insulin secretary defect
has a high degree of genetic predisposition;
 generally has a late onset (past middle age).
over 90% cases of diabetes are type 2 DM.
Other types:
Gestational diabetes mellitus (GDM)
GDM is a type of diabetes that is first seen in a pregnant woman
who did not have diabetes before she was pregnant.
insulin or only diet modification is used for treatment and
whether or not the condition persists after pregnancy

In this case generally blood sugar returns to its usual level soon
after delivery. But have a higher risk of getting type 2 diabetes
Pre-diabetes
It is a condition in which blood glucose levels are higher than
normal but not high enough to be classified as full-blown diabetes.
It is a wakeup call on the path to diabetes.
 Lifestyle changes can help many people with pre-diabetes delay or
prevent it from becoming diabetes.
Weight control, regular exercise and nutrition with low-fat protein,
vegetables, limits calories and sugar, fiber-rich foods may be useful
to control measures for pre-diabetes.

Symptoms of diabetes:
Blurred vision
Thirst
Fatigue
Painful and frequent urination
Sores that do not heal.
Weight loss
Hunger
Nausea and vomiting
Vaginal infection in female
Hand or feet numbness
Sexual problems

Hormones and related Drugs.pptx Pharmacolgy

Insulin
It is peptide hormone that regulates the level of sugar (glucose) in
the blood and that is produced by the beta cells of the islets of
Langerhans in the pancreas.
Insulin is derived from a 74-amino-acid prohormone molecule
called proinsulin which is relatively inactive,
 Insulin is secreted when the level of blood glucose rises—as after a
meal.
When the level of blood glucose falls, secretion of insulin stops, and
the liver releases glucose into the blood.
Insulin is a two polypeptide chains having 51 aminoacids and
molecular weight of 808.
'A' chain has 21 and 'B' chain has 30 amino acids connected to each
other by disulfide linkages.

Role of insulin
It plays an important role in carbohydrate, protein and fat
metabolism. It causes rapid uptake, storage, and use of glucose by
almost all tissues of the body but especially by the muscles, adipose
tissue and liver.
Modify the activity of enzyme & the results reactions in the body.
Building muscle following sickness or injury via the transportation of
amino acids to the muscle tissue, which is required to repair muscular
damage and increase size and strength.
 It helps to regulate the uptake of amino acids, DNA replication, and
the synthesis of proteins.
Managing breakdown of protein and lipids due to changes in fat cells.
Uptake of amino acids and potassium into the cells that cannot take
place in the absence of insulin.
Managing the excretion of sodium and fluid volume in the urine.
Enhancing the memory and learning capabilities of the brain.

Insulin Onset time Time duration Example
Rapid-acting insulin 15 minutes 2 to 4 hours Insulin aspart (Novolog)
Insulin lispro (Humalog)
Insulin glulisine (Apidra)
Regular insulin 30 minutes 3 to 6 hours Insulin regular (Novolin R)
Intermediate-
acting insulin
1 to 2 hours 12 hours NPH (Novolin N)
Long-acting insulin 2 to 4 hours 24 hours Insulin detemir (Levemir)
Insulin glargine (Lantus,
Basaglar)
Ultra-long-acting
insulin
6 hours 36 to 42 hours Insulin degludec (Tresiba)
Insulin glargine U300 (Toujeo)
Inhaled insulin 12-15
minutes
3 hours Inhaled insulin (Afrezza

Mechanism of action
It acts as an agonist of insulin receptor. After binding of alpha unit
of insulin to receptor (where as beta unit auto phosphorylated), it
stimulates tyrosine kinase which in turn activates downstream
signaling molecule including Phosphoinositide-3 kinase (Pl3 kinase)
and protein kinase B (PKB or AKT) thus regulates metabolism and
catabolism of glucose.
Indication:
All type 1 DM patients.
High risk type 2 DM patients.
All pregnant diabetics which are not controlled with diet.
All acutely or chronically ill persons with DM.
All patients preparing for or just having surgery.
Any person who desires strict control.

Adverse effects:
Insulin resistance
Hypokalaemia
Lipoatrophy
Blurred vision
 Hypoglycaemia
Contraindication and precautions:
Contraindicated in hypoglycaemia.
Precaution with hypertension.
Dose:
Adult: As soluble insulin, dose as per blood glucose level;
initial loading dose of 20 units, followed by 6 units per hour until
blood glucose drops to 10 mmol/L.
Child: 0.4-0.8 unit/kg/day

Oral Hypoglycemic Drugs
Anti-diabetic medications treat diabetes mellitus by lowering
glucose levels in the blood are administered orally and are thus
also called oral hypoglycemic agents or oral antihyperglycemic
agents.
Classification
1. Sulfonyl urea:
First generation: Tolbutamide, chlorpropamide
Second generation: Glibenclamide, glipizide, gliclazide.
Third generation: Glimepiride
2. Biguanides:
Metformin - Phenformin
3. d-Phenyl alanine analogues (Meglitinide):
Repaglinide
Nateglinide

4. Thiazolidinediones:
Rosiglitazone
Pioglitazone.
5. a-Glucosidase inhibitors:
Acarbose
Miglitol
6. Incretin enhancers:
Sitagliptin
Vildagliptin
Saxagliptin
Linagliptin

Glimepiride
Glimepiride is a medium- to long-acting sulfonylurea antidiabetic
drug.
It is sometimes classified as either the first 3rd generation
sulfonylurea or as 2nd generation.
Mechanism of action
It acts partially by blocking potassium channels among B-cells of
pancreatic Islets of Langerhans.
By blocking potassium channels, the cell depolarizes which results in
the opening of voltage-gated calcium channels.
The resulting calcium influx encourages insulin release from B-cells.
Indication:
Used in type-2 DM

Side-effect
low blood sugar (hypoglycemia).
Symptoms may include:
trembling or shaking
nervousness or anxiety
fast heart rate or palpitations
intense hunger
fatigue or tiredness
unexplained weight gain
blurred or impaired vision
numbness in lips or tongue
weakness or fatigue
lack of coordination
Hypersensitivity
Dizziness weakness
Contraindication
Contraindicated with
hypersensitivity and diabetic
ketoacidosis.
Dose:
 Adult: 1 to 2 mg daily, max. 8 mg.
 Child: Not recommended.

Metformin
It is used with a proper diet and exercise program and possibly
with other medications to control high blood sugar.
It works by helping to restore your body's proper response to the
insulin you naturally produce
It also decreases the amount of sugar that your liver makes and
that your stomach/intestines absorb.
Mechanism
It acts by reduction of hepatic glucose production through
activation of the enzyme AMP-activated protein kinase (AMPK).
It also works by delaying absorption of glucose from the GIT,
increasing insulin sensitivity and glucose uptake into the cells and
tissues (tissue glycolysis),
increasing glucose to lactate conversion by enterocytes,

Side-effect
low blood sugar;
stomach problems (diarrhea,
nausea, pain, gas, heartburn)
Lactic acidosis. Symptoms can
include:
tiredness
weakness
unusual muscle pain
trouble breathing
unusual sleepiness
Lowers Vit B12
Hypersensitivity
Contraindication
severe renal or hepatic
impairment.
severe infection or shock and
with hypersensitivity reaction.
Dose:
Adult: 500 mg BID/TDS or 850
mg OD/BID; max 2000 mg.
Child: 10 yrs-500 to 850 mg OD.

Sitagliptin
It is an oral antihyperglycemic of the dipeptidyl peptidase-4 (DPP-4)
inhibitor class.
It is used either alone or in combination with other oral
antihyperglycemic agents
Mechanism of action
 It selectively inhibits the DPP-4 inhibitor that activate incretin
hormones and increases the hormone concentration and for
prolonged action leading to reduced of hepatic glucose production
with increase in insulin synthesis.
Indication:
type-2 DM.

Adverse effects:
Hypoglycaemia
Angioedema
URTI
GI disorder: Nausea, Diarrhoea, Vomiting
Exfoliative dermatitis
Nasopharyngitis
Contraindication
diabetic ketoacidosis,
 type-1 DM,
hypersensitivity reactions.
Dose:
Adult: 100 mg PO, once daily. Child: Not available

Linagliptin
It is a DPP-4 inhibitor used to manage hyperglycemia in patients
with type 2 diabetes mellitus.
MOA/indication/ contraindication
 same as sitagliptin
Note: Individuals who have poor liver or kidney function may be
good candidates for this medication.
This drug is not known to cause weight gain and does not cause low
blood sugar when taken by itself.
Side effect:
abdominal pain,
diarrhea,
common cold.
Dose:
5mg PO/day

Pioglitazone
It is one of the thiazolidinedione class with hypoglycemic action to
treat diabetes.
 It has been found to be associated with bladder tumors and has
been withdrawn in some countries.
Mechanism of action
Pioglitazone selectively stimulates the nuclear receptor peroxisome
proliferator activated receptor gamma (PPAR-y).
 It modulates the transcription of the genes involved in the control
of glucose and lipid metabolism in the muscle, adipose tissue and
the liver.
 As a result, it reduces insulin resistance in the liver and peripheral
tissues, decreases gluconeogenesis in the liver and reduces quantity
of glucose and glycated hemoglobin in the bloodstream.
Indication:
Used in the treatment of type-2 DM

Adverse effects:
Oedema, bladder tumors
Pharyngitis
Headache
Anaemia
Sinusitis
URTI
Contraindication
hypersensitivity.
Precaution with anaemia, jaundice, hepatic dysfunction, CHF
Dose:
Adult: 15-30 mg once daily.
Child: Not recommended

Voglibose
It is an alpha-glucosidase inhibitor indicated in the management of
blood glucose in patients with type II diabetes
It lowers post-meal blood sugar levels. Therefore, it should be taken
before meals
Mechanism of Action
It acts from a reversible inhibition of membrane bound intestines α-
glycosidase hydrolize enzymes which hydrolize oligosaccharides and
disaccharides to glucose and other monosaccharides in the brush
border of the small intestine.
Thus, delays the absorption as well as digestion of dietary
polysaccharides by reversibly inhibiting carbohydrate digestive
enzymes
Indication:
Type-II DM( specifically for lowering post-prandial blood glucose)

Side effects
Flatulence, Abdominal pain, Diarrhea, Bloating (common)
CNS: Nausea ,vomiting, dizziness
Abnormal liver function (rare)
Metabolic hypoglycaemic episodes are not uncommon in
patients who are on voglibose therapy
Contraindications:
Hypersensitivity
Diabetic ketoacidosis.
Inflammatory bowel disease, colonic ulceration
Dose:
0.1-0.3 mg * TID

Repaglinide
It is an antidiabetic drug that belongs to meglitinide category
MOA
Increases insulin secretion by blocking ATP-dependent potassium
channels on beta islet cells, which facilitates calcium entry through
calcium channels; increased intracellular calcium stimulates insulin
release from pancreatic beta cells
Indication:
Type 2 Diabetes Mellitus
Side-effect
hypoglycemia followed by weight gain
hunger, tiredness, muscle weakness,
blurred vision,
heart palpitations
cold temperature,
confusion, loss of consciousness.
upper respiratory infections

Contraindications
Hypersensitivity
Diabetic ketoacidosis
Type I diabetes mellitus
Dose:
0.5-2 mg for 2-4 time/day according to glucose level

Glibenclamide:
Dose: 2.5-5 mg OD
Glipizide:
Dose2.5-5mg OD

Glucagon
It is a natural hormone which regulate blood glucose (sugar) levels
and increases blood sugar level
It is secreted by alfa-islets cell of pancreas
It prevents blood sugar from dropping too low.
The alpha cells in pancreas make glucagon and release it in response
to a drop in blood sugar, prolonged fasting, exercise and protein-rich
meals.
Function
Prompting the liver to increase glucose production
Causing the liver to decrease glucose consumption
Initiating the release of glucose from glycogen, (glycogenolysi)
Promoting the production of glucose from amino
acids(gluconeogenesis)
Initiating the release of glucose into the bloodstream

Mechanism of action
Glucagon binds to high affinity hepatic glucagon receptors.
Binding of glucagon leads to activation of Adenylate cyclase
 Adenylate cyclase converts ATP to cAMP (second messenger).
CAMP activates cAMP dependent protein kinase
This results in phosphorylation dependent activation or inhibition of
key enzymes of carbohydrate and lipid metabolism
Therapeutic Uses
Hypoglycemia-
Cardiogenic shock- Glucagon used to stimulate the heart in B
adrenergic blocker treated patients.
Glucagon is used to relax the intestinal tract to facilitate
radiographic examination of GIT.

Side-effect
increased hunger and thirst
increased urination
blurred vision
Nausea, vomiting
fast heartbeat
difficulty breathing
loss of consciousness, nervousness
Contraindication:
Hypersensitivity
Dose-
0.5-1.0 mg i.v. or i.m.

Corticosteroids
The adrenal cortex secretes steroidal hormones which have
glucocorticoid, mineralocorticoid and weakly androgenic activities.
The term 'corticosteroid' or 'corticoid' includes natural gluco- and
mineralo-corticoids and their synthetic analogues.
Action of Corticosteroids
The corticosteroids have widespread actions.
 They maintain fluid-electrolyte, cardiovascular and energy substrate
homeostasis and functional status of skeletal muscles and nervous
system.
They prepare the body to withstand effects of all kinds of noxious
stimuli and stress.
Corticosteroids have some direct and some permissive actions.
Actions of corticosteroids are divided into:
Glucocorticoid: Effects on carbohydrate, protein and fat metabolism
and other activities that are linked to these.
Mineralocorticoid: Effects on Na+, K+ and fluid balance.

Classification
1. Glucocorticoids:
a. Short acting: Hydrocortisone.
b. Intermediate acting: Prednisolone, methylprednisolone,
triamcinolone, deflazacort.
c. Long acting: Dexamethasone, betamethsone.
2. Mineralocorticoids:
Desoxycorticosterone acetate, Aldosterone, Fludrocortisone
Betamethasone
Betamethasone is a corticosteroid with anti-inflammatory and
immunosuppressive action
its derivatives betamethasone sodium, betamethasone phosphate,
betamethasone acetate etc

Mechanism of action
It activates lipocortins, which inhibit phospholipase A2 and block
the synthesis of leukotrienes from arachidonic acid, thus
interrupting the inflammatory cascade.
 It controls the rate of protein synthesis, depresses the migration of
polymorphonuclear leukocytes and fibroblasts, reverses capillary
permeability and lysosomal stabilization at the cellular level to
prevent or control inflammation
Indication:
 Used for its anti-inflammatory or immunosuppressive properties
inflammation due to corticosteroid responsive dermatoses.
Combine with clotrimazole are used together to treat cutaneous
tinea infections

Side-effect:
Decreased resistance to infection
Decreased carbohydrate and glucose tolerance( hyperglycemia)
CNS: Depression, emotional instability, euphoria, insomnia, mood
swings
GI disturbance
Itchiness, burning or stinging, thinning of the skin, lightened color of
treated skin
Contraindicated
hypersensitivity, renal and hepatic problems.
Dose:
Adult: 0.5-5mg/day PO after food;
for skin disorder-0.1% over affected area.
Child: <12 yrs-0.0175 to 0-125 mg/kg/day.

Dexamethasone
Dexamethasone and its derivatives, dexamethasone sodium,
dexamethasone phosphate and dexamethasone acetate are
synthetic long acting glucocorticoids.
Mechanism of action
It acts as glucocorticoid receptor agonist.
Its anti-inflammatory activity is due to the inhibition of
phospholipase A2 inhibitory proteins (Lipoproteins).
Indication:
It is used for it's anti-inflammatory or immunosuppressive
properties.
It cross BBB so used alone to manage cerebral edema.
Dexamethasone with tobramycin, it is used to treatments of
corticosteroid responsive inflammatory ocular conditions.
It is also used as prophylaxis of nausea and vomiting.

Side-effect:
Decreased resistance to infection
CNS: Depression, mood changes, nervousness
blurred vision
fast, slow, pounding, or irregular heartbeat or pulse
troubled breathing at rest
Wt gain
Contraindication
Hypersensitivity
Dose:
 Adult: 0.75 to 9 mg/day with or without food.
 Child: 0.02 to 0.3 mg/kg/day in divided dose.

Hydrocortisone
Hydrocortisone is the most important human glucocorticoid.
It is essential for life and regulates or supports a variety of important
cardiovascular, metabolic, immunologic and homeostatic functions.
Mechanism of action
It acts as an agonist of Glucocorticoid receptor and Annexin A1
(Lipocortin-I).
It also acts by inhibiting genes that code for TNF-alfa, IL-1, IL-2, IL-3, IL-
4, IL-5, IL-6 & IL-8.
Indication:
For inflammatory and pruritic
endocrine (hormonal) disorders (adrenal insufficiency, Addisons
disease).
immune and allergic disorders. Such as arthritis, lupus, severe asthma,
ulcerative colitis and Crohn's disease.

Adverse effects:
Muscle wasting
Joint damage
Osteoporosis
Hirsutism (hair growth)
Hyperglycaemia
Glycosuria
Obesity
Hypopigmentation
Local irritation
GI disturbance
Acne
Bleeding etc.
Contraindication:
tubercular or syphilitic lesion
bacterial, viral or fungal
infection.
Dose:
Adult: 20-30 mg daily in 2-3
divided doses,
0.1-2.5% cream/ointment lotion
to apply affected area.
Child: 400-800 µg/kg/day in 2-3
divided doses.

Prednisolone
It is a synthetic, anti-inflammatory glucocorticoid that derives from
cortisone
Mechanism of action:
It decreases inflammation via suppression of the migration of
polymorphonuclear leukocytes and reversing increased capillary
permeability.
It also suppresses the immune system by reducing the activity and
the volume of the immune system.
Indication:
anti-inflammatory or immunosuppressive agent
asthma allergic reactions
arthritis inflammatory bowel disease
treat a broad range of diseases, including dermatologic, ophthalmic,
respiratory, hematologic, neoplastic, GI, antineoplastic agent

Side-effect
fluid retention including swelling of the face and swelling
of the abdomen
weight gain
decrease in the amount of urine
high blood pressure
irregular periods
muscle cramps
thin skin that bruises easily, and acne
osteoporosis (thinning of the bones)
 Problems sleeping (insomnia), Feeling restless, Mild mood
changes
shortness of breath

Contraindication:
Systemic fungal infection
Hypersensitivity
Osteoporosis
Hypertension
Dose:
Adults- 5 to 60 milligrams (mg) per day.
Children-0.14 to 2 mg per kilogram (kg) per day

Gonadal Hormone and their Antagonists
Gonadal steroids is also known as sex steroids that are steroid
hormones that interact with vertebrate androgen or estrogen
receptors.
Natural sex steroids are made by the gonads (ovaries or testes)
There are also many synthetic sex steroids are available. Some of are:
Synthetic androgens are often referred to as anabolic steroids.
Synthetic estrogens and progestins are used in methods of hormonal
contraception.
Ethinylestradiol is a semi-synthetic estrogen.

Androgen and its antagonist
Androgens are substances which cause development of
secondary sex characters in the castrated male.
1. Natural androgen:
Testosterone, Dihydrotestosterone
2. Synthetic androgen:
Methyltestosterone, Fluoxymesterone
3. Anti-androgen:
Finasteride, Danazol, Flutamide,

Testosterone
Testosterone is a steroid hormone from the androgen group and is
found in humans and other vertebrates.
testosterone is secreted primarily by the testicles of males and to a
lesser extent in the ovaries of females.
plays a key role in the development of male reproductive system
promoting secondary sexual characteristics such as increased of
muscle and bone mass, and the growth of body hair
 essential for health and well-being as well as the prevention of
osteoporosis
Synthetic testosterone is available in the form of pellet
(implantation), injection, transdermal tablets, buccal gels etc

MOA
It increases serum testosterone levels by which it binds to cytosol
receptor protein and further dihydrotestosterone (DHT) is
metabolized to 3-Alfa androstanedol and 3- Beta androstanediol.
Indication:
hypogonadism.
Increased Muscle Mass
It is also used in the treatment of Klinefelter's syndrome
(chromosomal condition that affects male physical and cognitive
development)

Side-effect:
Breast swelling
Headache, anxiety
Increased facial or body hair growth, male-pattern baldness
Increased or decreased interest in sex
bloating or swelling of the face, arms, hands, lower legs, or feet
discouragement
enlarged prostate
feeling sad or empty
loss of interest or pleasure
Contraindication
breast cancer, prostate cancer.

Dose:
for Increased Muscle Mass : 125 Mg Per Week Might Be Ideal
Hypogonadism : IM INJECTION:
Testosterone Undecanoate: 750 mg (3 mL) IM injection followed by
750 mg (3 mL) injected after 4 weeks, then 750 mg (3 mL) every 10
weeks thereafter
Testosterone Enanthate and Cypionate: 50 to 400 mg IM injection
every 2 to 4 weeks

Flutamide
It is a new nonsteroidal antiandrogen
But it has no other hormonal activity.
Mechanism of action
It blocks the action of both endogenous and exogenous testosterone
by binding to the androgen receptor.
 In addition it is a potent inhibitor of testosterone-stimulated prostatic
DNA synthesis.
it is capable of inhibiting prostatic nuclear uptake of androgen.
Indication
management and treatment of androgen- dependent tumors like
prostate cancer
hyperandrogenism like polycystic ovarian syndrome (PCOS).
Hirsutism in women
Juvenile nasophyaryngeal angiofibroma

Side effects
Impotence
Reduced sperm count
loss of sexual interest/ability,
Decreased libido
Gynecomastia
Hot flashes,
Nausea, vomiting, Diarrhea
Contraindication
Hypersensitivity
Pregnancy
Sever hepatic impairment
Dose:
Prostate cance: 250mg * TDS
Female hirustism: 250mg/day

Finasteride
Finasteride is anti-androgenic compound and in a class of medication
called 5-alpha reductase inhibitors.
Mechanism of action
It Inhibit enzyme 5-alpha reductase so blocks conversion of
testosterone to more active dihydrotestosterone thus show anti-
androgenic action (esp. in prostate gland and hair follicles)
Indication
Benign prostatic hyperplasia
 Male pattern baldness

Side-effect:
Impotence
loss of interest in sex
Erectile dysfunction
Decrease libido
trouble having an orgasm
abnormal ejaculation
swelling/ enlarge/ tenderness in breasts
swelling in your hands or feet,
feeling like might pass out
Contraindication:
Children pregnancy and lactation
Dose:
BPH: 5 mg OD for 6 month
Male pattern baldness: 1mg OD for 3 month

Progesteron
It is the most important progestin in humans,
"Progestin" is a general term for a substance that causes some or all
of the biological effects of progesterone.
It is a precursor to the estrogens, androgens, and adrenocortical
steroids.
It is synthesized in the ovary, testis & adrenal from circulating
cholesterol. Large amounts are also synthesized by the placenta
during pregnancy.
Mechanism of action
Upon binding the hormone, progesterone receptor undergoes
dimerization that attaches to progesterone response element (PRE) of
target genes and regulates transcription through co-activators.
Indication:
hormone replacement therapy and hormonal contraception.
 dysmenorrhea, endometriosis and bleeding disorders when
estrogens are contraindicated.

Side-effect:
pain and swelling at inj. site,
breast tenderness,
Enlarged breasts.
weight gain or loss,
increased body or facial hair,
unusual vaginal bleeding
/discharge
swelling of the ankles or feet,
Head ache
dark patches on the skin or face
stopped menstrual periods,
frequent or painful urination,
dark urine,
Contraindication:
Hypersensitivity
 history of blood clots or
bleeding problems,
Breast or genital cancer, liver
disease, kidney problem
Dose:
Progesterone: 10-100 mg IM OD
Hydroxyprogesterone caproate:
250-500 mg IM at 2-14 days
intervals.
Norethisterone: 5-10 mg OD-BD
Levonorgestrel: 0.1-0.5 mg/day

Estrogen
Estrogen is the primary female sex hormone and is responsible for
development and regulation of the female reproductive system and
secondary sex characteristics.
Synthetic estrogens are used as part of some oral contraceptives, in
estrogen replacement therapy for post menopausal women and in
hormone replacement therapy for trans women.
Mechanism of action
Estrogens act through binding to nuclear receptors in estrogen-
responsive tissues. It modulates pituitary secretion of the
gonadotropins, luteinizing hormone and follicle stimulating
hormone through a negative feedback mechanism.

Indication
Contraception,
menopause,
 hypogonadism,
 transgender women,
prostate cancer, breast cancer,
Infertility and Pregnancy support
Lactation suppression
Side:effect:
pain and swelling at inj. site,
breast tenderness,
Enlarged breasts.
weight gain
Hair loss
Hyperpigmentation
unusual vaginal bleeding
/discharge
Impotence
Risk of ovarian and endometrial
cancer

Contraindication
liver impairment,
Cardiovascular disease,
undiagnosed vaginal bleeding, breast cancer
pregnancy.
Dose:
0.3 to 0.625 mg/day orally; 25 mg IV/IM, twice daily.
Ethinyl estradiol 1 - 2mg / day
Estradiol cypionate 2-5 mg every 3-4 weeks
Estradiol valerate 2 - 20mg every other week
Estropipate1.25 - 2.5mg / day

Clomiphene citrate
It is a non-steroidal fertility medicine. It is a selective estrogen
receptor modulator (SERM) of the triphenylethylene group.
It has become the most widely prescribed drug for ovulation
induction.
It causes the pituitary gland to release hormones which are needed
to stimulate ovulation (the release of an egg from the ovary).
Mechanism of action
 The mechanism in stimulating ovulation is unknown but is believed
to be related to its antiestrogenic properties.
By clomiphene compets with estrogen for binding sites, the
gonadotropins, follicle-stimulating hormone (FSH) and luteinizing
hormone (LH), secretion is increased, which results in ovarian
follicle maturation

Indication:
ovulatory failure in female patients who wish to become pregnant.
increases Gonatotropic secretion which promotes spermatogenesis
and testosterone secretion
Side-effect:
Ovarian Enlargemen
Abdominal-Pelvic Discomfort/Distention
Nausea and Vomiting
Breast Discomfort
Blurred vision, photophobia,
Abnormal Uterine Bleeding
Menorrhagia
rapid weight gain
hot flash,

Contraindication:
hypersensitivity,
 liver dysfunction,
abnormal bleeding
pituitary tumors
pregnant women
Dose:
50 mg orally once a day for 5 days. Therapy should be initiated on
or near the 5th day of the menstrual cycle, but may be started at
any time in patients without recent uterine bleeding.

Tamoxifen
Tamoxifen is a medication that is used to prevent breast cancer in
women and men.
chemically related to clomiphene, tamoxifen citrate has complex
actions.
Mechanism of action
It acts as potent estrogen antagonist in breast carcinoma cells, blood
vessels and at some peripheral sites but as partial agonist in uterus,
bone, liver and pituitary gland.
Indication
used to treat some types of breast cancer in men and women.
 It lower a woman's chance of developing breast cancer if she has a
high risk (such as a family history of breast cancer).

Adverse effects:
vision changes, eye pain
Haemorrhage
weight loss,
 amenorrhoea
vaginal discharge,
hot flash,
skin changes
Dose:
20 to 40 mg orally. Dosages greater than 20 mg should be given in
divided doses for 5 years.

Uterine Stimulants
Oxytocin
Oxytocin is a hormone, neuropeptide secreted by the posterior
pituitary along with vasopressin (ADH).
Pituitary extract was first used in labour in 1909.
It plays a role in social bonding, sexual reproduction in both sexes and
during and after childbirth.
Oxytocin is released into the bloodstream as a hormone in response
to stretching of the cervix and uterus during labour and with
stimulation of the nipples from breast feeding.

Physiological role of oxytocin:
1. Labour:
 Oxytocin is released during labour and the uterus is highly sensitive
to it at this time. However, it does not appear to be essential for
initiating childbirth, though labour may be prolonged in its absence.
A facilitatory role is more probable.
2. Milk ejection reflex:
 It is mediated by oxytocin. The myoepithelial cells in breast are
more sensitive than myometrium to oxytocin. Milk ejection reflex is
absent in the hypophysectomized (surgical removal of pituitary
gland),
3. Neurotransmission:
Oxytocin appears to function as a peptide neurotransmitter in the
hypothalamus and brainstem to regulate autonomic neurones..

Mechanism of action
It acts as an agonist of oxytocin receptor and thereby increases
intracellular calcium level. The number of oxytocin receptors increases
markedly during later part of pregnancy.
Oxytocin increases Prostaglandin synthesis and release by the
endometrium which may contribute to the contractile response.
Oxytocin also contracts myoepithelium of mammary alveoli and forces
milk into the bigger milk sinusoids 'milk ejection reflex‘
Indication:
Induction of labour.
Uterine inertia (absence of effective uterine contractions during
labor).
Postpartum haemorrhage.
Breast enlargement.
Oxytocin challenge test (The contraction stress test) may be done
during pregnancy to measure the baby's heart rate during uterine
contractions

Side-effect:
Cardiovascular: Cardiac arrhythmia, hypertensive crisis, hypotension,
tachycardia,
Gastrointestinal: Nausea, vomiting
Genitourinary: Postpartum hemorrhage, uterine rupture, Uterine
hyperstimulation
Hematologic & oncologic: Pelvic hematoma
Hypersensitivity, Water intoxication
Contraindication:
hypersensitivity
Induction of labor in those cases where vaginal delivery is
contraindicated
cephalopelvic disproportion
Unfavorable fetal positions or presentations
multipaurous patients (producing more than one at a birth)

Dose:
adult dose for labor induction:
 Initial dose: 0.5 to 1 milliunits IV infusion per hour. At 30 to 60
minute intervals the dose should be gradually increased in
increments of 1 to 2 milliunits until the desired contraction pattern
has been established.
Usual adult dose for postpartum bleeding:
10 to 40 units IV infusion in 1000 mL at a rate sufficient to control
bleeding. 10 units IM after delivery of placenta

Female contraceptives
Female contraceptives are hormonal preparations used for reversible
suppression of fertility or control of birth.
 Hormonal contraceptives are of three types;
1. Oral contraceptives
2. Injectable contraceptives
3. Implanted contraceptives
Oral contraceptives
a) Estrogen
b) Progestin
c) Estrogen + progestin

Two types of preparations for oral administration;
1. Combined pill
 Estrogen + progestin combination
Commonly used contraceptive
Consist of 21 white tablets (levonorgestrel 0.15mg + ethinylestradiol
0.03mg) and 7 brown tablets containing 75mg ferrous fumarate
White tablets, start from 5th day of menstruation and continued for
21 days then followed by 7 brown tablets during menses
 'Nilokon white' and 'Sunaulo gulab' common brands in Nepal,
marketed by CRS company

2. Mini pill
 Progesterone only pill
Less effective than combined pill
Mechanism of action of pills
The main way the pill works is by stopping a woman's
ovaries from releasing an egg each month.
It also thickens the mucus at the entrance of the uterus
(womb), which prevents sperm from entering.
And it changes the lining of the uterus, making it less likely
the egg will implant.

Advantages
It is very effective if taken properly
It is safe for most women
Fertility returns as soon as they stop taking it
It can help regulate the menstrual cycle and reduce period
pain
It can improve acne, endometriosis symptoms, pre-
menstrual syndrome (PMS) and some symptoms of
menopause
It probably decreases the risk of endometrial and ovarian
cancers

Disadvantages
it is not suitable for every woman
it can cause side effects, especially when they first start
taking it, such as: tender breasts, nausea, bloating,
headache, weight gain, less interest in sex, brown patches
on the face, mood changes
There is an increased risk of very rare blood clots or stroke
it won't protect them from sexually transmitted infections
(STIs)

Injectable contraceptives
This consist synthetic version of the hormone progestogen, called
Depot medroxyprogesterone acetate,
The injection is also called Depo.
Depo prevent the body from producing its own hormone & releasing
egg from the ovaries. This is also how the contraceptive pill works
The injection thickens the fluid at the entrance to the uterus (womb),
which stops sperm from entering.
 It also thins the lining of the uterus, making it difficult for a fertilized
egg to attach and develop.
It is given as an IM into the buttock or the upper arm, and over the
next 12 weeks the DMPA is slowly released into the bloodstream.
To prevent pregnancy, an injection must be given every 12 weeks
The injection is usually given during the first 5 days of the menstrual
cycle, so it can start working straight away. If they have the injection
at some other time in their cycle, it can take up to 7 day to start work

Advantages
It is highly effective
It can be used by women who can't take estrogen.
Only need to have the injection once every 3 months
It is safe for use by most women, including those who are
breastfeeding
It usually stops menstrual bleeding, so is useful for women who have
heavy periods or period pain.
Depo-Provera may reduce the risk of ovarian cancer, endometrial
(uterine) cancer, endometriosis and pelvic infection.
It can be used if they're taking some medications that make the pill
or implant less effective.

Disadvantages:
It changes the pattern of the periods - they might become more
frequent or longer lasting, then stop completely.
If stop using it, it can take a while to get pregnant - it can take 18
months for fertility to return.
It can cause side effects such as weight gain, moodiness, decreased
sex drive, headaches and acne.
It might cause bone thinning if used for a long time.

Implanted contraceptives
A contraceptive implant is inserted under the skin on the inside of
the arm and offers a very effective and convenient long-term
contraception option.
The implant continuously releases small amounts of a hormone,
progestogen, that prevents pregnancy.
There need a prescription for the implant, and it needs to be
inserted and removed by a trained doctor or nurse.
The contraceptive implant is a type of LARC (long-acting reversible
contraceptive).
The hormone is released slowly over 3 years.
The hormone prevents eggs being released from the ovaries
(ovulation), and thickens the mucus at the entrance to the uterus
(womb) so sperm can't get through.

Advantages
It is very effective
it doesn't interfere with having sex
once it is taken out, fertility returns quickly
There is no need to take a pill or have injections
It is safe for use by most women, including those who are
breastfeeding
it lasts for 3 years, but can be removed earlier
it is not expensive
it might make the periods less painful and lighter, and
reduce pre- menstrual syndrome (PMS) and acne

Disadvantages
it might change the pattern of the vaginal bleeding,
especially in the first 3 months
it can cause slight bruising and pain when inserted or
removed
 It might move from its original position
if it's not inserted correctly it may not protect against
pregnancy.
It's important to have it inserted by a doctor or nurse who
is familiar with the technique
it can cause side effects such as tender breasts, mood
changes or headaches
it may leave a small scar

Post-coital contraceptive
Also known as emergency contraceptive pills
Single dose of mifepristone 600mg within 72 hours of intercourse or;
Levonorgestrel alone 0.75mg taken twice with 12 hour gap within 72
hours of intercourse

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