Endocrine Drugs, Hormones and

Related Compounds
Overview
Endocrine System

- composed of hormone-releasing organs such

as the:
hypothalamus thymus
pituitary gland pancreas
thyroid gland gonads
parathyroid -ovaries
adrenal glands -testes
pineal gland
Endocrine System
Endocrine System
-is controlled by the hypothalamus and
the pituitary gland

-along with the Nervous System, it

coordinates and directs body function

-maintains homeostasis by releasing

chemicals called hormones
Endocrine vs Nervous
- the nervous system communicates
locally by electrical impulses and
neurotransmitters directed through
neurons to other neurons or to specific
target organs such as muscle or glands

- nerve impulses generally act within

milliseconds
Nervous System
Endocrine vs Nervous
- the endocrine system releases
hormones into the blood stream
- the hormones are then carried by the
blood stream into target cells
throughout the body
- hormones have broader range of
response times (they act from seconds
to days or longer)
Endocrine vs Nervous
NOTE: there is close interrelationship
between the endocrine and nervous
systems
Endocrine System
Processes controlled by the endocrine
System:
1. growth & development
2. reproduction
3. body defenses
4. water, electrolyte and
nutrient balance
5. regulation of cellular metabolism
and energy balance
Hormones
Hormones
- Greek word, “to arouse”

- chemical substances secreted by the

cells into the extracellular fluids that
stimulate or regulate the metabolic
activity of other cells in the body.

- Gen. MOA: binding of the hormone to

the target cell or organ elicits response.
Endocrine Drugs
Endocrine Drugs
- Hormones are pharmacologically
classified as drugs
- can be natural (from animals), semi-
synthetic or synthetic compounds
- Indications:
a. replacement therapy
b. treatment for certain disorders
c. diagnostic purposes
Endocrine Drugs
I. Hypothalamic & Pituitary Hormones
II. Steroid Hormones
A. Gonadal Hormones
1. Estrogens
2. Progestins
3. Androgens
B. Hormones of the Adrenal Cortex
1. Adrenocorticosteroids
2. Adrenal Androgens
III. Thyroid Hormones and Drugs for Thyroid
Disorders
IV. Anti-diabetic Agents
Hypothalamic & Pituitary
Hormones
Hypothalamus
- master endocrine organ
- secretes releasing/inhibiting hormones
Pituitary Gland
- weighs 600 mg and rests in the sella
turcica under a layer of dura mater in
the brain
-composed of 2 lobes:
a. anterior lobe
b. posterior lobe
 Hypothalamic & Pituitary Hormones
Hypothalamic Hormone Pituitary Target Organ Target Organ
Hormone Hormone
1. G rowth H orm one – G rowth H or m one (G H ) Liver S om atom edins
Releasing H o rm o n e aka: Som atotropin
(GHRH)
aka: Serm orelin
2. Growth H o r m o ne – Inhibits Growth H o r m on e
Inhibiting H o r m o n e (GHIH)
aka: Som atostatin
3. Corticotropin – Releasing Adrenocorticotropic Adrenal Cortex Glucocorticoids
H o r m o n e (CRH) H o r m o n e (ACTH) Mineralocorticoids
aka: Corticotropin Adrenal Androgens
4. Thyrotropin – Releasing Thyroid – Stimulating Thyroid Gland T 3 (Triiodothyronine)
H o r m o n e (TRH) H o r m o n e (TSH) T 4 (Thyroxine)
aka: Thyrotropin
5. Gonadotropin – Releasing
H o r m o n e (GnRH) or Gonadotropins Ovaries (Fem ales) Estrogen (by FSH)
Luteinizing H o r m on e – a. Follicle Stimulating Testes (Males) Progesterone (by L H
Releasing H o r m on e H o r m o n e (FSH) in fem ales)
(LH R H ) b. Luteinizing H o r m on e Testosterone (by L H
(LH ) in m ales)
6. Prolactin – Releasing Prolactin Breasts
H o r m o n e (PRH)

7. Prolactin – Inhibiting Inhibits Prolactin

H o r m o n e (PIH)

8. O xytocin Stored in the Posterior

Pituitary Gland
9. Vasopressin Stored in the Posterior
Pituitary Gland
Growth Hormone
Growth Hormone (GH)
- aka: Somatotropin, Asellacrin
- a large polypeptide: about 191 amino
acids (MW: 21,500)
- released by the anterior pituitary in
response to GHRH (Sermorelin)
produced by the hypothalamus
- produced synthetically by recombinant
DNA technology
Growth Hormone (GH)
- animal source is ineffective in humans
- induces the release of somatomedins in
the liver
- promotion of cell proliferation and bone
growth at open epiphyses
- boosts cartilage synthesis
Growth Hormone (GH)
Indications:
- for long term treatment in growth
hormone deficiency in children
(Dwarfism)
- for non-GH deficient short children (can
grow up to 2 cm per year)
Dwarfism
Somatrem
- a therapeutically equivalent drug of GH
- contains an extra terminal methionyl
group
Growth Hormone Inhibiting
Hormone
Growth Hormone Inhibiting
Hormone (GHIH)
- aka: Somatostatin
- inhibits Growth Hormone
- Indications:
Pituitary Gigantism (pre-pubertal)
Acromegaly (post-pubertal)
Pituitary Gigantism
Acromegaly
macrognathia (large jaw)
wide-spaced teeth
macroglossia
thickened lips
broad nose
enlarged joints
cardiomegaly
organomegaly
Octreotide
- synthetic octapeptide analog of
somatostatin
- 45x more potent than GHIH
Adrenocorticotropic Hormone
Adrenocorticotropic Hormone (ACTH)

- aka: Corticotropin, Acthar

- single-chain polypeptide containing 39
amino acids
- precursor: pro-opiomelanocortin
- released by the anterior pituitary in
response to CRH produced by the
hypothalamus
Adrenocorticotropic Hormone (ACTH)

- stimulates the adrenal cortex to produce

adrenocorticosteroids & androgens
- is used primarily for the diagnosis and
differentiation of primary & secondary
adrenal insufficiency
- Primary: Addison’s Disease associated
with adrenal atrophy
- Secondary: caused by inadequate
secretion of ACTH by the pituitary
Addison’s Disease
• hyposecretion of adrenocorticosteroids

• characterized by:
– anorexia
– dehydration
– weakness and lethargy
– hyperpigmentation (bronze-colored skin)
Cushing’s Syndrome
• hypersecretion of adrenocorticosteroids

• characterized by:
– moon face
– buffalo hump
– pendulous abdomen
– hypertension
Cushing's Syndrome
Cosyntropin
- synthetic human ACTH
- more preferred since animal ACTH can
cause allergic reactions
Thyrotropin Stimulating
Hormone
Thyrotropin Stimulating Hormone (TSH)

- aka: Thyrotropin
- released by the anterior pituitary in
response to TRH (aka: Protirelin)
produced by the hypothalamus
- stimulates the thyroid to produce T3 and
T4
- T3: triiodothyronine (most active)
- T4: thyroxine
(converted to T3 in the body)
Thyrotropin Stimulating Hormone (TSH)

- the thyroid hormones T3 and T4 are

essential for the normal growth and
maturation of the body
- Conditions:
hypothyroidism
hyperthyroidism
Hypothyroidism
- inability of the thyroid gland to supply
sufficient thyroid hormone to the body
- manifestations:
Cretinism (infant-state)
Myxedema (adult-state)
Cretinism
- infant-state hypothyroidism
- characterized by physical and mental
retardation
Myxedema
- adult-state hypothyroidism
- characterized by:
• bradycardia
• weakness and lethargy
• dry skin and hair
• coldness
• goiter
Hyperthyroidism
- overabundance of thyroid hormone in
the body
- thyrotoxicosis
- Forms:
Graves’ Disease - most common
Plummer’s Disease - less common
- with cardiac abnormalities
Graves' Disease
Gonadotropins
Gonadotropins
- include:
Follicle-Stimulating Hormone (FSH)
Luteinizing Hormone (LH)
- released by the anterior pituitary gland
in response to GnRH / LHRH
- stimulates the gonads (ovaries & testes)
to produce sex hormones
- Females: FSH  estrogen
LH  progesterone
- Males: LH  testosterone
Gonadotropins
NOTE: Pituitary gonadotropins (FSH, LH)
are not available for therapeutic use,
however, there are non-pituitary
gonadotropins that have FSH-like or
LH-like activity and are the ones used
therapeutically
Non-Pituitary Gonadotropins
1. Menotropins
2. Urofollitropin
3. Human Chorionic Gonadotropin
Non-Pituitary Gonadotropins
- Indications:
women: to induce ovulation &
pregnancy
men: to induce spermatogenesis

- Adverse effects:
ovarian enlargement
multiple births
gynecomastia in men
Menotropin
- aka:
Human Menopausal Gonadotropin
(hMG)
Pergonal®
- obtained from the urine of post-
menopausal women
- partially broken down into FSH and LH
in the body
Urofollitropin
- Metrodin®
- obtained from the urine of post-
menopausal women
- high in FSH-like activity
Human Chorionic Gonadotropin
- aka: hCG, Follutein®
- a placental hormone
- LH agonist effect
-obtained from the urine of pregnant
women
Hormones of the Posterior
Pituitary Gland
Hormones of the Posterior
Pituitary Gland
1. Oxytocin
2. Vasopressin
Oxytocin
- stimulates uterine contraction and plays an
important role in the induction of labor
- also promotes breast milk ejection
- Indications:
to induce contraction during labor
to control postpartum bleeding
- Contraindications:
abnormal fetal presentation
fetal distress
premature births
Oxytocin
Vasopressin
- aka: Antidiuretic Hormone (ADH)
- has both antidiuretic and vasopressor
activity
-acts by binding to its receptor in the
kidneys promoting the reabsorption of
water in the collecting tubules
-Indications:
Diabetes Insipidus
Postoperative Abdominal Distention
Diabetes Insipidus (DI)
- a disorder due to the deficiency or lack
of response to Antidiuretic Hormone
(ADH)
- 2 Types:
a. Central DI - deficiency in ADH
b. Nephrogenic DI - sufficient ADH
but body does not respond
to the hormone
Desmopressin
- modified analog of vasopressin
- more preferred for DI and nocturnal
enuresis because it is largely free of
pressor effects and is longer-acting
Steroid Hormones
Steroid Hormones
- contain the steroid nucleus, CPPP
cyclopentanoperhydrophenanthrene
Steroid Hormones
• Carbon 3 & Carbon 17
• -OH (sterol)
• =O (sterone)
Gonadal / Sex Hormones
Steroid Hormones
A. Gonadal / Sex Hormones
1. Estrogens
2. Progestins
3. Androgens
B. Hormones of the Adrenal Cortex
1. Adrenocoticosteroids
a. Glucocorticoids
b. Mineralocorticoids
2. Adrenal Androgens
Gonadal / Sex Hormones
Estrogens
Estrogens
- basic nucleus: estrane

Estradiol
Estrogens
- Effects:
1.normal female maturation and
development
2. inhibit bone resorption
3. increase HDL, decrease LDL
4. decrease platelet adhesiveness
Estrogens
- Indications:
contraception
postmenopausal hormone therapy
primary hypogonadism
osteoporosis
Natural Steroidal Estrogens
Estradiol - most potent estrogen
produced by women
Estrone, Estriol - have about one tenth
the potency of estradiol
* Premarin - a preparation of conjugated
estrogens (sulfate esters of estrone &
equilin)
- obtained from pregnant mare’s urine
Premarin
Synthetic Steroidal Estrogens
Ethinyl estradiol
Mestranol
Quinestrol
Synthetic Nonsteroidal Estrogens
Diethylstilbestrol - possible cause of a
rare, clear cell cervical or vaginal
adenocarcinoma among daughters of
women who took the drug during early
pregnancy
Estrogen Antagonists /
Antiestrogens

Clomiphene - fertility drug; it induces

ovulation by negative feedback
mechanism

Tamoxifen & Toremifene - palliative

treatment of advanced breast cancer in
postmenopausal women
Estrogen Related Drugs
Aromatase Inhibitors
Selective Estrogen Receptor Modulators
Aromatase Inhibitors
- are potent and selective non-steroidal
inhibitors of aromatase, an enzyme
reponsible for the conversion of
androgens to estrogens
- used to treat advanced breast cancer
- Anastrozole, Letrozole
SERMs
- Selective Estrogen Receptor Modulators
- reduce bone resorption and decrease
bone turnover
- used for the prevention of osteoporosis
- Raloxifene
Progestins
Progestins
- basic nucleus: pregnane
Progestins
- Effects:
1. endometrial changes
2.alveolobular development of
secretory apparatus in breasts
3. hepatic glycogenesis &ketogenesis
4. increase lipoprotein lipase
activity and fat deposition
Progestins
- Indications:
contraception
for menstrual disorders
-dysfunctional uterine bleeding
-dysmenorrhea
endometriosis
 Natural Progestin
Progesterone
-endogenous progestin produced in
response to luteinizing hormone (LH)
- also synthesized by the adrenal cortex
-in females, it promotes the development
of a secretory endometrium that can
accommodate implantation of a newly
forming embryo
Synthetic Progestins
- more stable to first-pass metabolism,
allowing for lower doses when
administered orally
- medroxyprogesterone
hydroxyprogesterone
megestrol
norethindrone
norgestrel
Progestin Antagonist /
Antiprogestin

Mifepristone
- aka: RU 486
-progestin antagonist with partial
agonist activity
-can cause abortion of the fetus due to
the interference with progesterone and
the decline in hCG
Oral & Implantable
Contraceptives
Major Classes
1. Combination Pills
2. Progestin Only Contraceptives
3. Postcoital Contraceptives
Combination Pills
- contain both estrogen and progestin
- provided as 21 day or 28 day-packs
- most common type of oral contraceptives
- estrogen: suppresses ovulation
ethinyl estradiol - most common
mestranol
Combination Pills
- progestin: prevents implantation in the
endometrium and makes the cervical
mucus impenetrable to the sperm
norethynodrel
norethindrone
norgestrel
Progestin Only Contraceptives
- less effective than combination pills
- dosage forms/ delivery systems:
a. “mini-pill” - low dose progestins
350 g norethindrone or
75 g norgestrel
b.progestin implants - subdermal implant
of 216 mg of norgestrel (Norplant®)
effective for 5 years
Progestin Only Contraceptives
c. intramuscular - given every 3 months
150 mg of medroxyprogesterone
acetate (Depo-Provera®)
Progestin Only Contraceptives

d. intrauterine device (IUD) - for yearly

insertion; Progestasert®
Postcoital Contraceptives
- called, “morning-after pills”
- high dose estrogen administered within
72 hours after coitus and continued 2x
for 5 days
- ethinyl estradiol
diethylstilbestrol
conjugated estrogens
estrone
Androgens
Androgens
- basic nucleus: androstane

Testosterone
Androgens

- group of steroids that have anabolic

and/or masculinizing effects in both
males and females
Endogenous Androgen
Testosterone
- primary natural endogenous androgen
- synthesized by Leydig cells in the testes
of males and in smaller amounts by the
cells in the ovary of females, and in the
adrenal gland
-produced in response to LH
Synthetic Androgens
Methyltestosterone
Danazol
Stanozolol
Nandrolone
Therapeutic Uses
1. Androgenic Effects
- in hypogonadism in males
2. Anabolic Effects
-in senile osteoporosis, severe burns,
speedy recovery from surgery or from
chronic debilitating diseases
3. Endometriosis (Danazol)
Unapproved Use
Used to increase lean body mass, muscle
strength and aggressiveness in athletes
and body builders (Nandrolone &
Stanozolol)
Antiandrogens
- inhibit the action of androgens by
interfering with androgen synthesis or
by blocking their receptors
a. Finasteride - used in Benign Prostatic
Hypertrophy (BPH)
Antiandrogens
b. Flutamide - for prostatic carcinoma

c. Cyproterone acetate - for hirsutism in

females
Hormones of the Adrenal
Cortex
Hormones of the Adrenal Cortex
1. Adrenocorticosteroids
a. Mineralocorticoids
b. Glucocorticoids
2. Adrenal Androgens
Adrenal Cortex
3 Zones:
1. Zona glomerulosa
- produces mineralocorticoids
2. Zona fasciculata
- produces glucocorticoids
3. Zona reticularis
- produces adrenal androgens
Adrenal Cortex

Zona glomerulosa

Zona fasciculata

Zona reticularis

Kidney
Mineralocorticoids
- possess sodium-retaining and
potassium-secreting effects
- essential for fluid and electrolyte
balance

- endogenous: aldosterone
desoxycorticosterone

- synthetic: fludrocortisone
Glucocorticoids
- Endogenous: Cortisol
Cortisone
Corticosterone
Hydrocortisone
- essential for the metabolism of
carbohydrates, fats and proteins
- they enhance response of the vascular
and bronchial smooth muscles to
catecholamines
Glucocorticoids
Other Preparations:
Prednisone Betamethasone
Methylprednisolone Dexamethasone
Triamcinolone
- anti-inflammatory, anti-allergy and
immunosuppressant effects
- inhibit cell growth and division
- catabolic effects on protein and bones
Glucocorticoids
Therapeutic Uses:
Allergy
Inflammation of joints and bones
Skin diseases
Organ transplant immunosuppression
Pulmonary Diseases: Bronchial Asthma
COPD
Glucocorticoids
Adverse effects:
Cushing’s syndrome
Adrenal suppression
osteoporosis
PUD
impaired wound healing
increased susceptibility to infection
hyperglycemia/DM
cataract
Addison’s Disease
• hyposecretion of adrenocorticosteroids

• characterized by:
– anorexia
– dehydration
– weakness and lethargy
– hyperpigmentation (bronze-colored skin)
Cushing’s Syndrome
• hypersecretion of adrenocorticosteroids

• characterized by:
– moon face
– buffalo hump
– pendulous abdomen
– hypertension
Cushing's Syndrome
 Thyroid Hormones and
Drugs for Thyroid Disorders
Thyroid Gland
Thyroid Hormone Synthesis
1. Iodide uptake
2. Peroxidation of iodide to iodine
3. Organification of iodine
4. Coupling reaction: DIT + DIT  T4
MIT + DIT  T3
5. Proteolysis
6. Peripheral conversion of T4 to T3
Thyroid Hormones
- the thyroid hormones T3 and T4 are
essential for the normal growth and
maturation of the body
T4
- thyroxine
- converted to T3 by the action of the
enzyme deiodinase
- 99.98% protein bound to thyroxine-
binding globulin
- 0.02% is in free form
- half-life: 7 days
 T3
- triiodothyronine
- most active form
- 3-4x more potent than T4
- responsible for most of the effects of the
thyroid hormones
- has 10-fold greater affinity for the receptors
- 99.8 % protein bound
- 0.2% is in free form
- half-life: 1.5 days
Hypothyroidism
- inability of the thyroid gland to supply
sufficient thyroid hormone to the body
- manifestations:
Cretinism (infant-state)
Myxedema (adult-state)
Cretinism
- infant-state hypothyroidism
- characterized by physical and mental
retardation
Myxedema
- adult-state hypothyroidism
- characterized by:
• bradycardia
• weakness and lethargy
• dry skin and hair
• coldness
• goiter
Thyroid Hormone Preparations
Preparation T4:T3 ratio
Thyroid, USP
Beef 4:1
Pork 2-3:1
Thyroglobulin 2:1
Levothyroxine Pure T4
Levothyronine Pure T3
Liotrix 4:1
Hyperthyroidism
- overabundance of thyroid hormone in
the body
- thyrotoxicosis
- Forms:
Graves’ Disease - most common
Plummer’s Disease - less common
- with cardiac abnormalities
Graves' Disease
Antithyroid Drugs
1. Thioamides
2. Inorganic Anions/Anionic Inhibitors
3. Iodides
4. Radiocontrast dyes
5. Beta-blocker
6. Dexamethasone
7. Radioactive Iodine
Thioamides
- MOA: inhibit iodine organification and
coupling
- examples:
Propylthiouracil (PTU)
Methimazole
Carbimazole
- S/E:
pruritic maculopapular rash
agranulocytosis
Inorganic Anions
- aka: Anionic Inhibitors
- MOA: interfere with the uptake of iodine
and cause the discharge of intra-
thyroidal iodine
- examples:
Potassium perchlorate
Potassium thiocyanate
- S/E:
aplastic anemia, nephrotic syndrome
Iodides
- MOA: inhibit organification and hormone
release
- they decrease the size and vascularity
of goiter
- examples:
KISS - Potassium iodide saturated
solution
Lugol’s solution - strong iodine
solution
Radiocontrast Dyes
- MOA: inhibit peripheral conversion of T4
to T3; also inhibit proteolysis
- examples:
Ipodate
Iopanoic acid
Beta-blocker
- MOA: symptomatic relief of the
sympathetic manifestations of
hyperthyroidism; may also inhibit
peripheral conversion of T4 to T3
- Propranolol
Dexamethasone
- MOA: inhibits peripheral conversion of
T4 to T3
Radioactive iodine
- 131I
- MOA: destruction of thyroid cells by
emission of high-energy beta radiation
- can offer cure
- Contraindicated to pregnant women
or women who will become pregnant
Anti-diabetic Agents
Pancreas
- is a mixed gland
- Exocrine portion
-releases pancrealipase &
chymotrypsin
- Endocrine portion
-1million islets of Langerhan
-have at least 4 hormone-producing
cells
Endocrine Pancreas
Cell Type % islet Hormone
A (alpha) 20 glucagon
proglucagon
B (beta) 75 insulin
pro-insulin
D (delta) 3-5 somatostatin
F (PP cell) <2 pancreatic
polypeptide (PP)
Diabetes Mellitus (DM)
- diabetes = Greek “siphon”
mel = honey
- “something sweet is passing through or
siphoning from the body”
- a metabolic disorder in which glucose
levels in the blood are too high and
begins to spill in the urine because the
kidney tubule cells cannot reabsorb it
fast enough
Types of DM
Type 1
Type 2
Gestational DM
Secondary DM
Type 1
- insulin-dependent DM (IDDM)
- juvenile-onset DM
- ketosis-prone diabetes
- most common in children
- insulin secretion is destroyed
- dependent upon exogenous insulin to
sustain life
Type 2
- non-insulin-dependent DM (NIDDM)
- adult-onset DM
- not insulin dependent
- endogenous insulin levels may appear
normal or increased but beta-cell
dysfunction is manifested by a relative
insulin insufficiency
Gestational DM
- defined as any degree of glucose
intolerance that has its onset during
pregnancy
Secondary DM
- broad term used to classify patients who
have unusual causes of DM due to
certain diseases of the pancreas,
endocrinopathies or drugs
3 Cardinal Signs of DM
1.Polyuria - excessive urination to flush
out the glucose and ketones

2.Polydipsia - excessive thirst resulting

from water loss

3.Polyphagia - excessive hunger due to

inability to use sugars and the loss of
fats and proteins from the body
Insulin
- is the storage and anabolic hormone of
the body
- produced by the Beta-cells of the
pancreas
- principal hormone required for proper
glucose use in normal metabolic
processes
- previously extracted from beef/pork
pancreas
- now is produced via recombinant DNA
Insulin - Effects
1.It facilitates transport of glucose across
cell membrane
2.In the liver, it promotes glycogenesis
and gluconeogenesis
3.In the muscles, it increases amino acid
transport, protein synthesis and
glycogenesis
4.In adipose tissues, it increases
triglyceride storage
Insulin - Indications
• Diabetes Mellitus Type 1
• Diabetes Mellitus Type 2 that cannot be
controlled by diet, exercise and oral
hypoglycemic agents (OHAs)
• Ketoacidosis
• Diabetic coma
Insulin Preparations
Pharmakokinetic Species Type Activity in hours
Type Peak Duration
Ultra rapid-acting Human
Insulin Lispro (Modified) 0.25 – 0.50 3 –4

Rapid acting
Insulin injection, USP Human, Pork 0.50 – 3 5 –7
(Regular, Crystalline)
Intermediate acting
NPH Insulin Human, Pork 8 – 12 18 – 24
(Isophane)
Lente Insulin Human, Pork 8 – 12 18 – 24
(Insulin zinc susp)
Long acting
Ultralente Insulin Human 8 – 16 18 – 28
(Insulin zinc susp
extended)
Ultra long acting
Insulin glargine Human No peak > 24
(Modified)
Oral Hypoglycemic Drugs
• Insulin secretagogues
• Biguanides
• Alpha-glucosidase inhibitors
• Thiazolidinedione derivatives
Insulin Secretagogues
• Sulfonylureas
• Meglitinides
Sulfonylureas
MOA:
- stimulate pancreatic release of insulin
- inhibit pancreatic release of glucagons
- increase insulin receptor binding
- decrease hepatic extraction of insulin
Sulfonylureas
Ist Generation
Chlorpropamide Acetohexamide
Tolbutamide Tolazamide

2nd Generation
Glibenclamide Glipizide
Gliclazide Glimepiride
Sulfonylureas
Side-effects:
hypoglycemia
blood dyscrasias
disulfiram-like reactions with 1st Gen
and glipizide
weight gain
Meglitinides
- MOA: increase pancreatic insulin
secretion
- short duration of action: 1 to 3 hours
- examples: Repaglinide
Nateglinide
- S/E:
hypoglycemia
weight gain
Biguanides
- unknown MOA
- reduce blood glucose level even in the
absence of beta cell function
- proven as a useful initial therapy among
DM Type 2 patients, especially among
obese patients
- not associated with hypoglycemia
- ex. Metformin (most proven)
Phenformin ( no longer available)
- S/E: lactic acidosis, megaloblastic
anemia
Alpha-glucosidase inhibitors
- MOA: competitive inhibition of intestinal
alpha-glucosidase enzyme, preventing
digestion of dextrins and disaccharides
into absorbable monosaccharides
- examples: Acarbose
Voglibose
Miglitol
- S/E: flatulence, potential hepatotoxicity
of acarbose
Thiazolidinedione derivatives
- MOA: insulin sensitizers - increase
skeletal muscle sensitivity to insulin;
they also decrease hepatic
gluconeogenesis
- examples: Rosiglitazone
Pioglitazone
- S/E: Hepatic failure (reason for the
withdrawal of Troglitazone), edema and
mild anemia
Let’s see how much
you can recall… :)
Question 1:
Which of the following is generally true of
hormones?
A. Exocrine glands produce them.
B.They travel throughout the body in the
blood.
C.They affect only non-hormone
producing organs.
D.All steroid hormones produce very
similar physiologic effects in the body.
B
Question 2:
All of the following substances are
endogenous tropic hormones secreted
by the pituitary gland EXCEPT:
A. Somatotropin
B. hCG
C. FSH
D. TSH
E. Corticotropin

B
Question 3:
Which of the following is secreted by the
posterior pituitary gland?
A. Luteinizing Hormone
B. ACTH
C. Oxytocin
D. Thyrotropin
E. Growth Hormone

C
Question 4:
ACTH or Adrenocorticotropic Hormone is
released by the anterior pituitary gland
in response to which hypothalamic
hormone?
A. GnRH
B. TRH
C. GHIH
D. CRH
E. PRH
D
Question 5:
All of the following are steroidal hormones
except:
A. testosterone
B. levothyroxine
C. cortisone
D. dexamethasone
E. estradiol

B
Question 6:
Which of the following insulins can be
administered IV?
A. Lente insulin
B. Isophane insulin
C. Protamine Zinc Insulin
D. Ultralente insulin
E. Regular insulin

E
Question 7:
It is a fertility drug. It induces ovulation by
negative feedback mechanism.
A. Tamoxifen
B. Ethinyl estradiol
C. Clomiphene
D. Finasteride
E. Prednisone

C
Question 8:
Which of the following is not properly
paired with its indication?
A. testosterone - hypergonadism
B. finasteride - BPH
C. cyproterone - hirsutism
D. PTU - hyperthyroidism
E. Tamoxifen - estrogen-dependent
breast cancer
A
Question 9:
Which of the following drugs can be used
for rheumatoid disorders?
A. diethylstilbestrol
B. triiodothyronine
C. methimazole
D. betamethasone
E. metformin

D
Question 10:
Which of the following is a sulfonylurea?
A. metformin
B. repaglinide
C. acarbose
D. rosiglitazone
E. glibenclamide

E
“Success is to be measured not so much by the
position that one has reached in life, but by the
obstacles which he has overcome.”

- Booker T. Washington
Thank You for Listening!