Reproductive

pharmacology
SYLLABUS
Gonadal hormones and antagonists (p. 703 & 705)
Anabolic steroids (p. 705): Preparation, basis for use, misuse
Hormonal contraception (p. 710):
Types, mechanism of action, pharmacological action, uses, choice of preparation, adverse effects,
contraindication
Oxytocics (p. 714) and Tocolytics (p. 716):
Mechanism of action, uses, adverse effects
Medication during pregnancy and lactation (p. 721):
Examples of safe drugs
Drugs causing teratogenicity and its categories (p. 722)
Types of damage to fetus and its prevention
Sexually transmitted diseases (p. 719):
Preparation of choice
VII
Antiviral agents (p. 717):

Introduction

General principles- classification, mechanism of action, indications, adverse effects, contraindications

Therapeutic uses and drug interactions

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 Pharmacology

VII

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PHARMACOLOGY
GONADAL HORMONES AND iv. Testosterone propionate + testosterone phenyl
ANTAGONISTS propionate +testosterone isocaproate- i.m.
Male Gonadal Hormones/ Androgens Uses:
i. Testicular failure
Past Questions:
- Primary (in children)
1. Write the pharmacological basis for the use of:
- Secondary (in later life)
a. Anabolic steroid in renal failure (3) [01 June]
ii. Hypopituitarism
b. Use of Danazol (3) [02 June]
iii. AIDS related muscle washing
c. Anabolic steroids(3) [11 July]
iv. Hereditary angioneurotic edema
d. Use of anabolic steroids in renal failure
v. Ageing
(3) [04 June]
Contraindications:
2. Short notes:
i. Carcinoma of prostate
a. Anabolic steroids (3) [06 June]
ii. Carcinoma of male breast
b. Danazol (3) [10 Jan, 04 June, 03 Dec, 03 June]
iii. Liver and kidney disease
c. Anabolic steroids (3) [10 Jan, 03
iv. Pregnancy
June,01 Dec]
v. Congestive cardiac failure, epilepsy and
Classification:
migraine –used with caution.
1. Natural:
Adverse effects:
a. Testicular androgens: (Potent)
i. Testosterone
VIIhair, voice change and
i. Virilization, excess body
menstrual irregularities in women
ii. Dihydrotestosterone ii. Acne in both sexes
b. Adrenal androgens: (least patent) iii. Oligozoospermia(due to feedback inhibition of
i Dehydroepiandrosterone(DHEA) FSH)
ii. Androstenedione iv. Precocious puberty and short stature due to
c. Metabolite of testosterone: (lesser potent) early closure of epiphyses if given to children
i. Androsterone v. High doses causes edema
2. Synthetic: (given orally) vi. Cholestatic jaundice especially with
a. Methyl testosterone 17- alkyl substituted methyltestosterone & fluoxymesterone and
b. Fluoxymesterone derivatives of testosterone anabolic steroids.
c. Testosterone undecanoate vii. Hepatic carcinoma
d. Mesterolone viii. Gynaecomastia
Preparations of Androgens: ix. Lowering of HDL and rise in LDL levels.
i. Testosterone (free)-i.m. Impeded androgens/antiandrogens:
ii. Testosterone propionate- i.m. Classification:
iii. Testosterone propionate + testosterone i. GnRH agonists- Leuprolide, Nafarelin,
enanthate- i.m. Buserelin, Doserelin
ii. GnRH antagonists- Cetrorelix, Ganirelix
iii. Androgen synthesis inhibitor – Ketoconazole
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 Pharmacology

iv. 5-reductase inhibitor- Finasteride, muscle relaxation of the prostate by blocking 1

Dutasteride receptor present there thus improving urinary
v. Androgen receptor blocker- symptoms.
Non- steroidal –Flutamide, Bicalutamide Androgen receptor blocker:
Steroidal- Cyproterone acetate, Spironolactone - Flutamide and Bicalutamide are two non-
vi. Others- Danazol steroidal drugs competitively blocking action of
GnRH agonist & antagonist androgens, both testosterone and
 Refer Paper VI dihydrotestosterone on accessory sex organs
and pituitary gland.
5-reductase inhibitor:
Finasteride: - They are deprived of any other hormonal
activity.
Mechanism of action:
- They are effectively used in the treatment of
- It inhibits selectively the isoenzyme type II 5-
reductase that converts testosterone to prostatic cancer with metastasis.
dihydrotestosterone(DHT). - They block the action of androgens and its
- 5-reductase type II isoenzyme is metabolite (DHT, which is the one of the
predominantly found in male urogenital tract. causative factors for prostatic cancer)
Indication: competitively.
- Benign prostatic hyperplasia (BPH) - If combined with GnRH agonist, result is better
- Male pattern baldness (MPB) because GnRH agonist will block the action of
- Hirsutism. the residual androgens by suppressing LH and
ADRs: then testosterone secretion from the pituitary
- Impotence and testis respectively.
VII volume
- Decreased ejaculatory ADRs:
- Gynaecomastia - Gynaecomastia
- Errectile dysfunction - Gastrointestinal side effects
- Testicular pain - Hepatotoxicity – more with Flutamide than
- Decreased libido Bicalutamide. Thus, Flutamide is of limited use.
Note:
Rationale of combining Finasteride with 1-blocker Danazol: [10,04,03,02]
(Prazosin) in BPH:
- It is orally active ethisterone derivative having
- DHT (Dihydrotestosterone ) leads to hyperplasia of weak androgenic, anabolic and progestational
the substance of the prostate leading to the BPH. activities.
The enlarged prostate provides mechanical
obstruction to the prostatic urethra leading to the Mechanism of action:
urinary symptoms. In addition, the smooth muscle - The most prominent action is suppression of
of the prostate gets contracted mediated by 1 gonadotropin secretion from pituitary in both
adrenergic receptor leading to more obstructive men and women leading to inhibition of
urinary symptoms. testicular /ovarian function.
- Thus, use of Finasteride decreases the - In addition, it exerts androgenic action by
concentration of DHT in male congenital tract by
binding to its receptor, but the action is very
inhibition of type II isoenzyme 5 -reductase and
weak. Thus it is also called impeded/
thus relief of mechanical obstruction. In addition,
use of Prazosin concurrently causes smooth attenuated androgen.

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- It suppresses gonadal function directly as well i. Catabolic states – In cases of acute illness,
as by inhibiting steroidogenic enzymes. severe trauma & major surgery
Uses: ii. Bone marrow stimulation (as they help in
i. Endometriosis erythropoiesis) in case of hypoplastic &
ii. Menorrhagia hemolytic anemia and leukemia

iii. Fibrocytic disease of breast iii. Growth stimulation in boys

iv. Hereditary angioneurotic edema iv. Induction of male puberty

v. Idiopathic thrombocytopenic purpura v. Kidney failure (as they reduce urea production
which is to be filtered out from kidney)
vi. Symptomatic fibroid
vi. To enhance physical ability in athletes.
vii. Precocious puberty
vii. Osteoporosis.
ADRs:
- Hypoestrogenic - decreased size of breast, FEMALE GONADAL HORMONES
decreased libido, atrophic vaginitis, hot flushes,
Past Questions:
amenorrhea
1. Enumerate the drugs used in anovulation related
- Androgenic - Acne, weight gain & edema,
female sub-fertility. Write down about the
hirsutism, deepening of voice
mechanism of action and adverse effect of
- Metabolic - Elevation of LDL, total cholesterol,
clomiphene citrate. [2+2+1=5] [13 July]
reduction of HDL
2. Pharmacological basis and use of: (3)
Anabolic steroids/Anabolic androgenic
a. Mifepristone is used to terminate
steroids (AAS): [11,10,04,03,02,01]
early pregnancy.
- They are the synthetic androgens with higher
(3) [11July, 07 June, 04 June, 02
anabolic and lower androgenic activity i.e.
Dec(2)] VII
anabolic to androgenic ratio is greater than 1.
b. Clomiphene citrate is used in
Drugs are:
disorder of ovulation in patients wishing to be
 Nandrolone pregnant.
 Oxymetholone (2) [02 Dec]
 Stanazolol c.Using clomiphene for sterility
 Methandienone [10 July, 04 June, 02June]
- Anabolic activity is observed by the following d. Estrogen in hormone replacement
physiological action: therapy (HRT) [04Dec]
a. Rapid bone growth, both in length and girth e. Tamoxifen in cancer breast (4)
b. Muscle building [09 Jan]
c. Positive nitrogen balance 3. Write short Note on: (3)
d. Retention of water and minerals (Na, K, Ca, a. Adverse effects of oestrogens [03 Dec]
P, S) - increase body weight b. Contraindication of oestrogen [05 Dec]
e. Improving appetite. c. Clomiphene citrate [05 June]
ADRs: d. Tamoxifen [01 Dec]
- Both anabolic and androgenic effects are Estrogens:
mediated through the same receptors, thus
Classification:
adverse effects are similar to testosterone.
1. Natural:
Uses:
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 Pharmacology

- β-Estradiol–most potent  To reduce vasomotor symptoms (like hot

- Estrone flushes) and genital atrophy
- Estriol  To prevent osteoporosis
β-estradiol is synthesized in Graafian follicle  To prevent cardiovascular risks
and corpus luteum of ovary and in placenta. ii. Premature ovarian failure
2. Synthetic: iii. Gonadal dysgenesis.
- Steroidal - Ethinyl estradiol, Mestranol, Risk of HRT:
Tibolone
- When used estrogen alone
- Non steroidal–Diethylstilbestrol (stilbestrol),
a. Endometrial cancer
Hexestrol, Dienestrol.
b. Gall bladder disease.
Preparations:
1. Estradiol benzoate/ cypionate /enathate/ - Combined estrogen & progestin
valarate – i.m. a. Breast cancer
2. Conjugated estrogens- oral b. Venous thromboembolic disease
3. Dienestrol – topical (vagina) c. Dementia, Alzheimer’s disease
4. Fosfestrol tetra sodium- iv/ oral ADRs- similar to estrogen
5. Mestranol –oral 2. Pharmacotherpy:
Uses: - Oral contraception
Broadly used in two therapies: - Senile vaginitis
1. Replacement therapy
- Vulvovaginitis
2. Pharmaco-therapy
- Acne
1. Replacement therapy: [05]
VII - Hirsutism
- It is known as hormone replacement
therapy (HRT). - Turner’s syndrome
- Estrogen is used in dose lower than that of - Delayed puberty in girls
dose of contraception. - Dysfunctional uterine bleeding
- Progestin may be added mainly to reduce - Carcinoma of prostate in males
the risks of endometrial carcinoma and Adverse effects:
dysfunctional uterine bleeding (DUB).
- Females:
HRT can be used either cyclically (3 weeks
Minor
treatment and 1 week gap) or continuously
with added progestin on later days of each  Nausea, vomiting
month.  Breast tenderness
- In case of hysterectomy done patients, no  Breakthrough bleeding (bleeding between
need to add progestin as no risk of menstrual cycles)
carcinoma of endometrium is retained.
 Weight gain
- It should be used at smallest effective dose
and for the shortest duration. Major:

Indications:  Increased risk of endometrial carcinoma

i. Menopausal women - to overcome short  Thromboembolism
and long term complications of estrogen  Worsening of migraine & endometriosis.
deficiency which are as follows:
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- Growing females: Early epiphyseal fusion & Newer compounds

short status  Desogestrel
- Males: Decrease libido, gynaecomastia &  Norgestimate
feminization.  Gestodene
Contraindication of estrogen: [05, 04] Uses:
i. Males - loss of libido, gynaecomastia, feminization 1. Diagnostic
ii. Children - early fusion of epiphyses leading to - Progesterone challenge test for
short status amenorrhea.
iii. Pregnancy - especially in 1 st trimester- increase 2. Therapeutic
of vaginal and cervical carcinoma - Contraception
iv. Post-menopausal women - increased risk of - Hormone replacement therapy
endometrial carcinoma - Dysfunctional uterine bleeding
v. Thromboembolic disorders
- Endometriosis
vi. Oestrogen dependent tumors (Breast)
- Premenstrual syndrome
vii. Acute liver disease
- Threatened abortion
viii. Severe hypertension
- Endometrial carcinoma
ix. Migraine
- Dysmenorrhoea
x. Endometriosis
ADRs:
xi. Diabetes mellitus
xii. Undiagnosed vaginal bleeding - Breast engorgement and mastalgia
xiii. Mentally ill - Acne, oligomenorrhoea, loss of libido & virilism
due to androgenic progestin
xiv. Obese person
- Irregular bleeding or amenorrhoea due to
xv. Gall bladder disease VII
prolonged use
Progestins: [03,01]
- Increased risk of breast cancer
Classification:
- Blood sugar may rise
1. Natural: (from ovaries and placenta)
- Weight gain due to salt & water retention
- Progesterone
- Masculinization of female fetus and other
- 17- hydroxy- progesterone
congenital abnormalities if used in pregnancy
2. Synthetic:
- Depression & mood changes
a. Progesterone derivatives:
- Leg cramps
 Medroxy progesterone acetate
- Decreased plasma HDL level with 19-
 Megestrol acetate
nortestosterone derivatives.
 Dydrogesterone
Antiestrogens:
 Hydroxy progesterone caproate
Classification:
 Nomegestrol acetate.
1. Pure estrogen receptor antagonist:
b. 19- Nortestosterone derivativeses:
Clomiphene citrate
Older compounds
2. Selective estrogen receptor modulators
 Norethindrone
(SERMs):
 Lynestrenol
a. Tamoxifen citrate
 Allylestrenol
b. Raloxifene
 Levonorgestrel
c. Ormeloxifene
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 Pharmacology

3. Aromatase inhibitors: - They behave as estrogenic agonist in one organ

a. Letrozole whereas possess anti-estrogenic action at the
other organs. They are orally active. For e.g.:
b. Anastrazole
- Tamoxifene citrate has agonistic action on
Clomiphene citrate: [10, 05, 04,02]
uterus, bones and pituitary whereas antagonist
- It is non-steroidal drug given orally. action on breast and blood vessels.
Mechanism of action:
- Similarly, Raloxifene possesses anti-estrogenic
- Clomiphene binds to both α & β receptors of action on uterus and breast whereas
estrogen and acts as pure estrogen antagonist estrogenic action on bone.
in all human tissues, even in pituitary.
Tamoxifene citrate: [13,09]
- In pituitary gland, it blocks the estrogen
- Mechanism of action
receptors and thus blocks negative feedback of
estrogen in pituitary causing release of more - It acts as estrogen antagonist on:
gonadotropins. Thus, it leads to increase in  Blood vessels - Inhibitions of hot flushes
amount of plasma LH and FSH at each  Breast carcinoma cell – Inhibition of breast
secretory pulse and ultimately on response to cancer cells
gonadotropins, ovary enlarges and ovulates.
 Pituitary – Inhibition of negative feedback
- Thus, infertility primarily due to anovulation is
of estrogen on pituitary, so more release of
treated.
gonadotropins
Uses:
- It acts as estrogen agonist on:
i. Anovulatory infertility – chief use
 Endometrium - Risk of endometrial
ii. To aid in-vitro fertilization
carcinoma
iii. Oligo-zoospermia in males by increasing
gonadotropins & promoting spermatogenesis.  Bone – Improvement in bone mass
Contraindication: VII  Lipid profile- Decrease LDL
- Patients who are hypogonadotropic and hypo Uses:
estrogenic i. Carcinoma of breast – standard treatment:
- Presence of cystic ovaries - Used in both pre & post-menopausal
ADRs: woman
- Visual disturbances - Used in post mastectomy (due to breast
- Headache cancer) adjuvant therapy
- Hot flushes - Palliative treatment in advanced breast
- Breast tenderness carcinoma
- Abdominal discomfort - Male breast cancer
- Rashes - Prophylaxis of breast cancer in high risk
- Loss of hair females
- Multiple pregnancies ii. Hormone replacement therapy
- Increased of risk of ovarian tumor. iii. Alternative to Clomiphene in treatment of
Selective estrogen receptor modulator infertility for both male and female
(SERMs): iv. Benign breast disease
- They are non-steroidal compounds which have Adverse drug reactions:
both estrogenic and anti-estrogenic action
- Venous thromboembolism
mediated through α & β receptors of estrogen
in various organs of the body. - Increased risk of endometrial carcinoma

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- Menstrual irregularities a. As it is progesterone antagonist, it

- Vaginal bleeding antagonizes the action of progesterone
mediated through its receptors  & .
b. Blocks progesterone support to
Raloxifene:
endometrium.
- It differs from Tamoxifen in having antagonistic
c. Prostaglandin release from endometrium is
action on estrogenic receptors even in uterus
not inhibited resulting in uterine contraction.
thus reducing risk of endometrial carcinoma.
d. Sensitizes myometrium to PGs and induces
- It is principally used for treatment of
menstruation.
osteoporosis in postmenopausal women and
has advantages over use of estrogen in HRT e. In case of implantation, blocks decidualization.
Aromatase inhibitors: f. Softening of cervix
- Mechanism of action: They are non-steroidal g. Secondary luteolysis
orally active drugs which inhibit the enzyme h. At high doses, its anti-glucocorticoid action
aromatase used in final step for synthesis of is manifested not at usual doses due to
estrogen. Thus, aromatase inhibitors produce feedback inhibition of decreased
estrogen deprievation in body. They inhibit glucocorticoid; more ACTH produced and
aromatase enzyme all over the body including then glucocorticoids produced more.
breast cancer cells.  Uses:
- They do not cause antagonism of estrogen in a. Termination of pregnancy or therapeutic
the periphery abortion: [11,07,04,02]
Uses: - Pregnancy can be terminated till 7 weeks of
1. Early breast cancer gestation by using a single oral dose of
Mifepristone.
2. Advanced breast cancer VII
3. Alternative to Clomiphene in anovulatory - Effects are more improved by concurrent
infertility as it causes hypoestrogenic state in use of single oral dose of Misoprostol as
the body and due to negative feedback, Mifepristone sensitizes myometrium to
prostaglandins and prostaglandins too
gonadotropins are released which cause
cause uterine contraction.
ovulation.
- Mifepristone blocks the progestational
Adverse drug reactions:
activity during the implantation and early
i. Hot flushes (due to less estrogen) pregnancy to terminate pregnancy by:
ii. Gastrointestinal upset 1. Inhibiting the decidualization of the
iii. Thinning of hair endometrium of the uterus which helps
iv. Joint pain in the nutrition of embryo.
Antiprogestins: 2. Inhibiting progesterone directly causing
uterine contraction and conceptus
- Mifepristone: [11,07,04,02]
dislodgement
 It is a steroidal synthetic drug acting as 3. Sensitizing myometrium to prostaglandin
competitive antagonist of progesterone causing release of prostaglandin from
receptor along with anti-glucocorticoid and endometrium and leading to uterine
anti-androgenic action. contractility and dislodgement of
 Mechanism of action: conceptus.
- Both of the actions make the endometrium
unsupportive to implantation. As a result,
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 Pharmacology

implantation fails to occur leading to e. Progesterone combined with

pregnancy termination. In addition, it also oestrogen in oral contraceptive [10 Jan]
causes fall in hCG levels and secondary f. Progestins for contraception [10 July, 05
luteolysis (decrease in progesterone level). Dec]
g. Injectable contraceptives [08
b. Cervical ripening Jan]
c. Induction of labour: Mifepristone causes h. Combining the different drug in oral
pills [02 June]
uterine contraction by inhibiting
progesterone anti-motility action on uterus 3. Mention: (3 + 2= 5) [02 June]
and sensitizing uterus to prostaglandin and a. The important adverse effects of
oral contraceptive
thence more uterine contraction mediated
by prostaglandin. Classification:
d. Emergency contraceptives (post coital Female:
contraceptives) 1. Oral contraceptives:
e. Once a month contraceptive as it causes A. Steroidal:
menstruation irrespective of conception. i. Combined pills (estrogens + progestins):
f. Cushing’s syndrome
 ADRs: Nausea, vomiting, headache, uterine ii. Mini pills (progestin only pills)
cramps and diarrhea. Long term use causes a. Norethindrone
endometrial hyperplasia. b. Norgestrel
 Contraindication: iii. Post coital/morning after (emergency
a. Age >35years contraceptives) pills:
b. Heavy smoker a. Levonorgestrel
c.
VII
Adrenal insufficiency b. Levonorgestrel+ ethinyl estradiol
d. Corticosteroid therapy B. Non – steriodal: Centchroman
HORMONAL CONTRACEPTIVES 2. Injectables
Past Questions: i. Depot Medroxy progesterone acetate
(DMPA)
1. Short notes:
ii. Norethindrone enanthate (NET-EN)
a. Injectable contraceptives[07June]
iii. Oestradiol valerate + 17 hydroxy
b. Combination pills [04 Dec]
progesterone caproate(combined)
c. Oral contraceptive [08 July, 05 June, 01
Dec] 3. Newer agents
d. Adverse effects of oral contraceptive [03 i. Subcutaneous implants- Levonorgestrel
Dec] ii. Intrauterine inserts (progestaserts)-
2. Pharmacological basis and use of: Levonorgestrel
a. Emergency contraceptives [11 iii. hCG vaccine.
July]
Male:
b. Estrogen and progestin in oral
i. Gossypol
contraceptive pills [09 Jan]
c.Progesterone for delaying menstruation [01 ii. Androgens
June] iii. Antiandrogens
d. Progesterone with oestrogen in oral iv. GnRH analogues
contraceptive [07 July, 08 Jan] v. Estrogen and progestins
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vi. Cytotoxic drugs. regression of the glands making

Combined oral contraceptives (COC): endometrium non-receptive to embryo.
[07,08,10,09,05] c. Alteration of character of cervical mucus by
- They are the most effective reversible method of progesterone so as to prevent sperm
contraception. Commonly used components are: penetration making cervical mucus thick,
 Estrogen- Ethinyl estradiol viscid and scanty.
 Progestin–Norgestrel, Levonorgestrel, d. Interference with tubal motility and alters
Desogestrel tubal transport of ovum.
- Rationale of combination of two hormones is: - Benefits of COCs:
 Reduction of amount of estrogen and i. Contraception:
progestin without compromising efficacy - Protection against unwanted pregnancy
but reducing adverse effects of each
- Convenient to use
component
- Not intercourse related
 Both the components synergise to inhibit
- Reversibility of fertility.
ovulation.
ii. Non contraceptive benefits:
 Progestin promotes prompt bleeding at end
of cycle and also reduces risk of a. Improvement of menstrual
development of endometrial carcinoma due abnormalities:
to estrogen. - Regulation of menstrual cycle
- Method of administration are: - Reduction of dysmenorrhea
 One tablet is taken orally each day for 21 - Reduction of menorrhagia
days from 5th of menstruation. Next course - Reduction of premenstrual syndrome
is started after a gap of 7 days for - Protection VII
against iron deficiency
maintenance of 28 days cycle. anemia
b. Protection against health disorders
 If one tablet is missed, next day two tablets
- Pelvic inflammatory disease
are taken, if 2 tablets are missed then it is
stopped and other methods (barrier) of - Ectopic pregnancy
contraception are used and next course - Endometriosis
started on 5th day of bleeding. - Fibroid uterus
- Mechanism of action - Hirsutism and acne
- Functional ovarian cysts
a. Inhibition of ovulation:
- Benign breast disease
- Both the hormones synergistically act on the
- Post menopausal osteoporosis
hypothalamo-pituitary axis.
- Rheumatoid arthritis
- The release of GnRH from the hypothalamus
c. Prevention of malignancies:
is prevented through a negative feedback
- Endometrial carcinoma
mechanism. Thus, there is no peak release
of FSH & LH and then follicle growth is - Ovarian carcinoma
nether initiated and if even initiated no - Epithelial ovarian cancer
ovulation occurs. - Contraindications:
b. Producing static endometrial hypoplasia: Relative contraindication:
There is stromal edema, decidual reaction a. Age> 40 years

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 Pharmacology

b. Smoker <35 years Absolute contraindication

b. History of jaundice a. Circulatory disease
c. Mild hypertension b. Arterial or venous disease
d. Gall bladder disease c. Severe hypertension
e. Diabetes d. History of stroke
f. Sickle cell anemia e. Heart disease: Vascular, ischemic
g. Headache f. Diabetes with vascular complication
h. Cancer of cervix g. Migraine with focal neurologic symptoms.
i. Unexplained vaginal bleeding h. Diseases of the liver: Active liver disease,
j. Hyperlipidemia liver adenoma, carcinoma.
k. Benign liver tumors g. Others
l. Breast feeding (post-partum 6 weeks – 6
- Pregnancy, breast feeding (post partum
months)
6 weeks), major surgery of prolonged
m. Heavy smoker
immobilization, oestrogen-dependent
n. Post breast cancer.
neoplasms ( Eg:Breast cancer)
- Adverse drug reactions
Minor Minor
- Nausea & vomiting - Depression
- Headache (estrogen) - Hypertension (estrogen)
- Leg cramps (progestin) - Vascular complications (estrogen)
- Mastalgia (estrogen+progestin) a. Venous thromboembolism
VII
- Weight gain (progestin) b. Arterial thrombus
- Chloasma (estrogen) - Cholestatic jaundice
- Acne (progestin) - Genital carcinoma:
- Menstrual abnormalities : a. ed risk of endometrial carcinoma
a. Brea through bleeding(BTB) b. ed risk of cervical carcinoma
b. Amenorrhoea (estrogen+progestin)
c. Menorrhagia (estrogen)
d. Hypomenorrhoea (progestin)
- Loss of libido (progestin) due to dry vagina
- Leucorrhoea
a. Estrogen–due to excessive cervical mucus
secretion
b. Estrogen + progestin - increased incidence of
candidial infection
- Precipitation of diabetes.
Preparations of COCs: - Levonorgetrel 0.25mg + Ethinyl estradiol
1. Monophasic 50mcg
- Norgestrel 0.3mg + Ethinyl estradiol 30mcg - Desogestrel 0.15mg + Ethinyl estradiol 30
mcg
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2. Phased regimens (biphasic or triphasic) - No adverse effects in patients with

- Ethinyl estradiol (35-35-35mcg) + hypertension, fibroid, diabetes, epilepsy,
Norethindrone (0.5-0.75-1.0mg) smoking and history of thromboembolism.
- Ethinyl estradiol (30-40-30mcg) + - Reduces risks of endometrial cancer and PID.
Levonorgestrel(50-75-125mg)
Disadvantages:
Phased regimens:
- They permit reduction in total steroid doses - Acne, mastalgia, headache, break through
than that of monophasic regimens without bleeding & amenorrhoea
compromising efficacy. - Simple cysts of ovary may be seen.
- They are biphasic or triphasic.
- Dose of estrogen is kept constant (or varied Contra-indications:
slightly) while amount of progestin is low in 1 st - Pregnancy, recent breast cancer,
phase and progressively higher in 2 nd & 3rd thromboembolic disease, arterial disease.
phases.
Emergency pills/postcoital pills: [11,09]
- They are particularly recommended for women
They includes following preparations;
over 35 years of age or presence of any other
a. Levonorgestrel (0.75mg)
risk factors.
b. Levonorgestrel (0.25mg) + ethinyl estradiol
Progestin only pills (POP) /minipills: [10,05]
(50mcg) - Yuzpe method
- They are the contraceptives used orally which
c. Mifepristone (600mg)
are devoid of estrogen compound. It contain
only very low dose of a progestin in any one to Indication:
the following form. - Unprotected intercourse
 Norethindrone 0.35mg - Condom rupture VII
 Norgesrel 75mg - Missed pill
st
- It has to be taken daily from 1 day of the cycle - Delay in taking ‘POP’ more than 3 hours.
without any gap and at same time of the day.
- Sexual assault/rape
Delay in intake for more than 3 hours should
Mechanism of action:
take 2 tablets and extra precaution is taken for
2 days - Ovulation is either prevented or delayed when
Mechanism of action: the drug is taken in beginning of the cycle.
- It works mainly by making cervical mucus thick - Fertilization is interfered.
and viscous, thereby preventing sperm - Implantation is prevented (except for
penetration. levororgestrel only regime) as endometrium is
- Endometrium also becomes atrophic so rendered unfavorable.
blastocyst implantation is hampered. - Interferes with function of corpus luteum or
Advantages: may cause leuteolysis.
- Side effects of estrogen are totally eliminated. Ways of taking emergency pills:
- No adverse effects on lactation so can be given - Levonorgestrel(0.75mg)  Two doses taken at
in lactating mother thus called lactation pills. 12 hours interval with 1st dose within 72 hours
of intercourse.
- No on and off regime, so easy to use.

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 Pharmacology

- Yuzpe method  Two tablets are taken within - Non contraceptive benefits are reduction of
72 hours of intercourse and after 12 hours, two risk of iron-deficiency anemia, endometriosis
more tablets are repeated. and salpingitis.
- Mifepristone 600mg is taken single dose within Centchroman:
72 hours of intercourse. - Non steroidal anti-estrogenic compound used
ADRs: as once-a-week contraceptive pill.
- In ‘Yuzpe’ method, nausea & vomiting. So, - It acts by preventing implantation of fertilised
ovum
prophylactically, 1 hour before the
administration of pills, antiemetic Advantages:
(metoclopramide) is taken. - No usual side effects of hormonal
contraception
- No any adverse effects in other regimes.
- Menstrual cycle not disturbed.
Injectable contraceptives: [08]
OXYTOCICS & TOCOLYTICS
Preparations:
Past Questions:
a. Depot medroxy progesterone acetate (DMPA)
150mg at 3 month intervals given i.m. Oxytocics:
b. Norethindrone (Norethisterone) enanthate 1. Compare and contrast the effect of ergometrine
(NET-EN) 200 mg at 2 months interval given and oxytocin of uterus (6, 3) [03 Dec, 01
i.m. June]
c. Medroxy progesterone acetate (MPA) + 2. Name the drug of choice in the following
estradiol cypionate i.m. inj. every month.
condition giving reason: (32=6) [04 Dec]
Mechanism of action:
a. Postpartum Haemorrhage (PPH)
i. Inhibits ovulation by suppressing the mid cycle
LH peak. b. Dysfunctional uterine bleeding (DUB)
VII
ii. Cervical mucus becomes thick and viscid, 3. The danger of misused oxytoxin (3) [02 June]
thereby preventing sperm penetration. 4. Short notes: (3)
iii. Endometrium is atrophic preventing blastocyst a. Oxytocin [08 July, 04 June]
implantation. b. Contraindications of oxytocin [06 June]
Disadvantages on use:
c. Ergometrine [10 July, 05 June]
i. Breast cancer risk is slightly increased in
d. Indications of ergometrine [05 Dec]
women <35years.
ii. Menstrual irregularities, excessive bleeding or 5. Pharmacologicalbasis and use of: (3)
amenorrhea are very common. a. Oxytocin is used for induction of labour
iii. Return of fertility after discontinuation is [10 Jan, 08 Jan, 05 Dec, 05 June, 04 Dec, 04 June,
usually delayed for several months (4- 01 Dec]
8months). b. Oxytocin in therapy [08 Jan, 05 June]
iv. Loss of bone mineral density & hot flushes (due
c. Ergometrine in post-partum haemorrhage
to low estrogen caused by Gn suppression by
negative feedback of progestin) [07 June]
v. Over weight Tocolytics: (3)
vi. Headache 1. Pharmacological basis and use of:
Advantages: a. Use of Tocolytics [02 June]
- Similar to ‘POP’ and b. Tocolytics in therapy [08 Jan, 01 Dec]
Oxytocics
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 Reproductive

 These are the drugs which increase uterine  Low concentration allows normal relaxation
motility, especially at term. in between contractions, thus fetal
Classification: oxygenation does not suffer.
1. Posterior pituitary hormone  Lower segment is spared i.e., not
contracted thus fetal descent is not
– Oxytocin, Desamino oxytocin
compromised.
2. Amine Ergot alkaloids
 Also uterine contraction are consistently
– Ergometrine, Methylergometrine
increased so therapy won’t fail.
3. Prostaglandins
- Labour is mainly induced in
– Misoprostol, PGE2, PGF2  Post maturity
4. Miscellaneous
 Prematurely in case of toxemia of
– Ethacridine, Quinine. pregnancy, ruptured membranes or diabetic
Oxytocin: [10, 08, 05, 04, 02, 01] mother
Mechanism of action:
In Uterus: ii. Uterine inertia:
- Oxytocin combines with specific G-protein - When uterine contractions are feeble and
coupled oxytocin receptors which mediate the labour is not progressing satisfactorily -
response mainly by depolarization of muscle oxytocin is infused to augment contraction
fibres and influx of Ca2+ ions as well as through because of above mentioned reasons.
phospho-inositide hydrolysis and IP3 mediated iii. Breast engorgement:
intracellular release of Ca2+ ions, and causes - This may occur due to inefficient milk ejection
uterine contraction. reflex; oxytocin effectively contracts
- Also, oxytocin increases PG synthesis and myoepithelial cells of alveoli of lactiferous
release by the endometrium which may ducts to eject milk. VII
contribute to contractile response. iv. Post-partum hemorrhage:
In breast: - Especially in women in whom ergometrine is
contraindicated, oxytocin immediately injected
- Oxytocin contracts myoepithelial cells of
will check post-partum hemorrhage by helping
mammary alveoli and forces milk into bigger
in uterine contraction as contraction of uterine
milk sinusoids & thus ejects milk as a result of
muscles compresses blood vessels and arrests
suckling reflex from infant. hemorrhage.
Uses: B. Diagnostic:
A. Therapeutic: - Oxytocin challenge test
i. Induction of labour: - Contraction stress test.
Dangers: [07]
[10, 08, 05, 04, 02, 01]
A. Maternal:
- Slow i.v. infusion of oxytocin can be given for i. Uterine hyperstimulation: Excessive duration of
induction of labour because: uterine contraction or increased frequency of
 It has short half-life and its slow i.v. infusion contraction causing reduced placental blood
can control intensity of action and action flow.
can be quickly terminated. ii. Uterine rupture
 Oxytocin increases force and frequency of iii. Water intoxication due to its antidiuretic action
uterine contractions iv. Hypotension

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 Pharmacology

v. Soft tissue injury due to overt contraction of - Due to the following reasons oxytocin is preferred
uterus. over the ergometrine for induction of labour:
B. Fetal: Oxytocin Ergometirne
- Fetal distress
- Uterus is contracted - Uterus is contracted
- Fetal hypoxia for shorter duration for longer duration
- Fetal death of time due to its due to its longer half
Amine- ergot alkaloids: [10,05,04] shorter half-life. life.
Mechanism of action: - There occurs normal - No normal relaxation
- They increase force, frequency and duration of relaxation between between
uterine contraction. contractions. contractions.
 They act directly on the myometrium
stimulating uterine contraction which comes
- Lower segment is - Whole of uterus is
so frequently one after another with increasing
intensity that uterus passes into a state of not contracted contracted.
spasm without any relaxation in between. - Force and frequency - Force and frequency
Uses: of contraction is of contraction is
i. Post-partum hemorrhage: [04, 07] less. more.
- Ergometrine produces sustained tonic Tocolytics [10,08,05,02,01]
uterine contraction causing compression of  These are drugs which decrease uterine motility.
perforating uterine arteries and then arrest Classification:
of hemorrhage. i. Adrenergic agonists:
- It also contracts lower uterine segment,  Ritodrine
thus bleeding from that segment is too
 Terbutaline
controlled. VII
 Isoxsuprine
ii. After Caesarean section/instrumental delivery
to prevent uterine atony ii. Calcium channel blockers
iii. To ensure normal involution of uterus in post-  Nifedipine
partum period  Niscadipine
Contraindications: [05]  Verapamil
i. Patients with vascular disease, hypertension iii. Prostaglandin synthesis inhibitor
and toxemia  Indomethacin.
ii. Presence of sepsis – as it may cause gangrene iv. Magnesium sulphate
iii. Liver and kidney diseases v. Nitric oxide (NO) donors: GTN
rd
iv. Before 3 stage of labour and during vi. Oxytocin antagonists
pregnancy vii. Progesterone
ADRs: Mechanism of action of Tocolytics:
- Nausea & vomiting - Relaxation of uterine muscle by:
- Rise in BP i. Decreasing intracellular Ca2+ concentration
- Decreased milk secretion as inhibit prolactin  CCBs & MgSO4
secretion.
 2-agonists
Effect of oxytocin and ergometrine on ii. Reducing effect of Ca2+ on muscle: MgSO4
uterus: [03, 01]
iii. Indirectly by inhibiting:

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 Synthesis of prostaglandins- Indomethacin glucocorticoid therapy for fetal lung

 Receptor action of oxytocin- Atosiban maturation.
Indications: ii. Dysmenorrhoea.
i. Preterm labour: iii. Threatened abortion:
- To postpone labour in order to improve - Tocolytics relaxes uterine muscles and
perinatal outcome. cause uterine hypotony to arrest
- Suppression of labour may be needed to threatened abortion.
allow fetus to mature, to initiate
Adverse effects:
Group Adverse effects
Calcium channel - Hypotension, headache, tachycardia, flushing and nausea in mother
blockers
Mgso4 Maternal:
Flushing, perspiration, headache, muscular weakening, cardiac arrhythmia
Neonatal:
Respiratory depression, hypotonia& lethargy.
Indomethacin Maternal:
Heart burn, asthma, thrombocytopenia & renal injury.
Neonates:
Constriction of ductus arteriosus
Pulmonary hypertension
β2 –agonists Maternal: VII
Headache, palpitation, pulmonary edema, hypertension, hypoglycemia,
hypokalemia
Fetal:
Hypoglycemia, tachycardia & IUFD.
Oxytocin antagonists - Nausea, vomiting & rarely chest pain
ANTI-VIRAL DRUGS b. Pyrimidine analogues:
- Idoxuridine
Past Question:
- Influridine
1. Short notes:
- Cidofovir
a. Anti-retroviral drugs [10 July]
2. Anti –Retroviral drugs:
b. Adverse effects of zidovudine [05 Dec]
a. Nucleoside reverse transcriptase Inhibitors
Classification: [10] (NRTIs)
1. Anti-herpes viral (DNA polymerase inhibitor) drugs: - Zidovudine
a. Purine analogues: - Lamivudine
- Acyclovir - Stavudine
- Valacyclovir - Abacavir
- Ganciclovir - Didanosine
- Famiciclovir b. Non-Nucleoside reserve transcriptase
- Penciclovir inhibitors (NNRTIs)

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 Pharmacology

- Nevirapine  Varicella Zoster & Epstein Barr virus

- Efavirenz  Cytomegalo virus- not affected.
c. Protease inhibitors (PIs) Uses:
- Ritonavir - Effective in both normal as well as
- Indinavir immunocompromised person.
i. Genital herpes simplex- caused by type II
- Saquinavir
HSV
- Lapinavir
ii. Mucocutaneous Herpes simplex –caused by
3. Anti- influenza drugs: type I HSV
- Amantadine iii. Herpes simplex encephalitis (type I virus)
- Rimantadine iv. Herpes simplex Keratoconjunctivitis
4. Non selective antiviral drugs: v. Herpes zoster
- Ribavirin vi. Chicken pox
- Interferon-α Adverse drug reactions:
Acyclovir - Topical: Stinging and burning sensation after
 It is deoxiguanosine analogue. each application
- Oral: Headache, nausea, malaise, CNS effects.
Mechanism of action: - Intravenous – Rashes, sweating, emesis and
fall in BP
Acyclovir
- Reversible neurological manifestations
Herpes virus specific Thymidine kinase
(tremors, lethargy, disorientation
Acyclovir monophosphate hallucinations, convulsions & coma)
VII
Cellular kinases (of host cell) - Dose dependent decrease in G.F.R. is most
important toxicity.
Acyclovir
Inhibits competitively herpes virus DNA polymerase Anti- Retroviral drugs [05]
triphosphate
 They are drugs effective against retro-virus (HIV).
They are useful in prolonging and improving the
Gets incorporated into viral DNA and stops lengthening of DNA strand. quality of life and postponing complaints of AIDS
The terminated DNA inhibits DNA polymerase irreversibly. or AIDS related complex (ARC) but do not cure
infection.
NRTIs:
Replication of virus checked - They are either purine or pyrimidine
nucleoside analogue which after intracellular
Decreased viral load phosphorylation in host cell are converted to
triphosphate compounds and inhibits viral
reverse transcriptase i.e., RNA dependent DNA
polymerase causing interruption of viral
Spectrum: replication and thus decreasing viral load and
- It is only active against Herpes group of virus in finally improving condition of patients.
descending order of Zidovudine: [05]
 Herpes simplex type I - It is thymidine nucleoside analogue.
 Herpes simplex type II Mechanism of action:
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 Reproductive

Zidovudine proteins and enzymes of virus. This protease

acts at a late step in HIV replication. This
enzyme is inhibited by protease inhibitors.
Incorporation into growing viral DNA & terminates chain elongation
Zidovudine triphosphate - As protease inhibitor act at a late step of
viral cycle, they are effective in both newly
and chronically infected cells.
- Zidovudine thus prevents infection of new cells
Single stranded viral RNAReverse transcriptase Double stranded viral DNA Indication:
by HIV but has no effect on virus directed DNA - They are used in combination with either
that has already integrated to host  2 NRTIs
chromosome.
 Or 1NRTI + 1NNRTI for controlling HIV
Adverse drug reactions: infection
- Anemia & neutropenia ADRs:
- Nausea, anorexia, abdominal pain, headache, - Gastro-intestinal intolerance
insomnia & myalgia - Asthenia
- Myopathy, lactic acidosis, hepatomegaly, - Headache
convulsion & encephalopathy - Dizziness
Uses: - Limb and facial tingling
Only against retrovirus: - Numbness & rashes
- In HIV infection  Immune status is improved - Lipodystrophy & dyslipidemia
and opportunistic infections become less - DM is exacerbated.
common.
HAART (Highly active anti retro viral
- Makes sense of well-being & patients gain
therapy):
weight.
- Anti-retroviral therapy (ART) is treatment of
- Reduces neurological manifestations of AIDS VII
people infected with HIV using anti-retroviral
and new Kaposi lesions do not appear.
drugs. The standard treatment consisting of a
- Mortality is reduced.
combination of at least 3 drugs or more is
NNRTIs: called HAART that suppress HIV replication.
- They are nucleoside unrelated compounds
- The goal of therapy is to maximally and
which directly inhibit HIV reverse
durably inhibit viral replication so that the
transcriptase without need for intracellular
patient can attain and maintain effective
phosphorylation.
immune response towards potential
Indications:
microbial pathogens.
- In HIV infections in combination with NRTIs.
- Three drugs are used in order to reduce the
ADRs:
likelihood of the virus developing resistance.
- Rashes (commonest)
- The principles of regimens of the HAART are:
- Headache
 3 drugs in regimen should belong to at
- Neuropsychiatric symptoms - dizziness,
least 2 different classes.
insomnia  Efavirenz
 3 NRTI regimen is used only when a NNRTI
- Hepatotoxic Nevirapine
or PI cannot be used such as in patients
Retroviral protease inhibitors (PIs):
receiving Rifampicin.
Mechanism of action:
 Treatment is practically life-long.
- An aspartic protease enzyme encoded by HIV
is involved in the production of structural

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 Pharmacology

 3 class regimen (NRTI+NNRTI+PI) is  Zidovudine + lamivudine + Lapinavir

reserved for advanced cases who have SEXUALLY TRANSMITTED
failed other all regimens.
DISEASES
 No contraindication to pregnant women
Past Questions:
Preferred Regimen of HAART
1. Mention the drug therapy of Trichomoniasis.
- 2NRTI +NNRTI:
(3) [04 Dec]
 Zidovudine + Lamivudine + Efavirenz
2. Short notes:
- 2NRTI + PI:
a. Treatment of primary syphilis (3) [10 July]
Treatment
Disease/causative organism 1st choice Alternatives
1. Gonorrhoea
- Non-penicillinase - Amoxicillin 3g oral/ Ampicillin - Cefixime 400mg once
producing(penicillin 3.5g oral +Probenecid 1 oral/doxycyline 100mg
sensitive) gsingle dose BD7days and or
Erythromycin 500mg BID 5
days oral
- Penicillinase - Ceftriaxone 250mg i.m./ - Ciprofloxacin 250-500mg oral
producing(Penicillin cefuroxime 250mg i.m. once/ ofloxacin 200-400mg
resistant) Or oral once
- Azithromycin 1.0 gm oral
VII single dose
2. Syphilis [10]
- Early(Primary, secondary - Benzathine pencillin 2.4MU - Doxycycline 100mg BD oral
and latent,1 year) i.m.weekly4weeks 15days/ceftriaxme 1gm i.m.
- Procaine penicillin G 1.2 MU 7days
i.m.20days - Or Erythromycin 500mg QID
oral 15days
- Late(>1year) - Benzathine penicillin 2.4 - Doxycycline or Erythromycin
million units (MU) in 1-3weekly for 30 days or ceftriaxone 1g.
inj. Or procaine penicillin g 1.2 i.m. /i.v.15days
MU i.m.10days

3. Chlamydia trachomatis
- Nonspecificurethritis - Azithromycin 1g oral single - Erythromycin 500mg QID
dose OR oral7days
Doxycycline 100mg BD oral 
7days
- Lymphogranuloma - Azithromycin 1.0mg oral - Erythromycin 500mg QID oral

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 Reproductive

venereum (LGV) weekly  3 weeks or  3weeks

doxycycline 100mg BD oral 
3weeks
4. Granuloma - Doxycycline 100mg BD oral  - Erythromycin 500mg QID oral
inguinale/Donovanosis 3weeks  3weeks
OR
- Azithromycin 500mg OD oral 
7days
5. Chancroid - Ceftriaxone 0.25mg i.m. single - Ciprofloxacin 500mg BD oral
dose  3 days or
- Azithromycin 1g oral single - Doxycycline 100mg BD oral 
dose 7days
- Erythromycin 0.5mg QID oral X
7days
6. Genital Herpes simplex
- 1st episode - Acyclovir 200mg 5 times a
day/400mg TDS oral  10days
or
- Valaciclovir 0.5-1.0g BD oral 
10 days
- Acyclovir 5% ointment locally 6
VII
times a day  10days-in mild
cases
- Recurrent episode - The above drugs given for 3-5
days(topical is not effective)
- Suppressive treatment - Acyclovir 400mg BD oral  6-
12months or
- Valaciclovir 500mg OD oral  6-
12 months
7. Trichomonas vaginitis - Metronidazole 2g single dose - Clotrimazole 100mg
[04] or 400mg TDS for 7days intravaginal every night 6-12
tinidazole 2g single dose or days.
6oomg OD 7days (treat the
male partner also if recurrent)

MEDICATION DURING  It refers to capacity of a drug to cause fetal

PREGNANCY & LACTATION abnormalities when administered to the pregnant
mother.
Teratogenicity

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 Pharmacology

 The placenta does not strictly constitute a barrier iii. Growth and development-(56 days onwards)-
and any drug can cross it to a greater or lesser developmental and functional abnormalities
extent. can occur e.g.-Hypoplasia of organs, especially
 The embryo is one of the most dynamic biological lungs & kidneys, premature closure of ductus
systems and in contrast to adults, drug effects are arteriosus.
often irreversible. Type of malformation depends
on drugs as well as the stage of exposure.
 Teratogenic drugs can affect the fetus at 3 stages:
i. Fertilization & implantation  (conception to
17days) failure of pregnancy which often
goes unnoticed.
ii. Organogenesis (18-55days of gestation)
most vulnerable period, deformities are
produced.

The US-FDA has graded the documentation of risk for causing birth defects into five categories as follows:
Category Examples
A - Adequate studies in pregnant women have - Inj. Mag. Sulfate, thyroxine
No risk failed to demonstrate a risk to the foetus
B - Adequate human studies are lacking, but - Penicillin V, amoxicillin, cofactor,
No evidence of animal studies have failed to demonstrate a erythromycin, paracetamol,
risk in human
VII
risk to the foetus. OR lidocaine
- Adequate studies in pregnant women have
failed to demonstrate a risk to the foetus,
but animal studies have shown an adverse
effect on the foetus.
C - No adequate studies in pregnant women and - Morphine, codeine, atropine,
Risk cannot be animal studies are lacking or have shown an corticosteroids, adrenaline,
ruled out adverse effect on foetus, but potential thiopentone, bupivacaine
benefit may warrant use of the drug in
pregnant women despite potential risk.
D Benefit may - There is evidence of human foetal risk, but - Aspirin, phenytoin, carbamazepine,
outweigh the potential benefits from use of the drug valproate, lorazepam,
potential risk may be acceptable despite the potential risk. methotrexate
X - Studies in animals or humans have - Estrogens, isotretinoin,
Contraindicated demonstrated fetal abnormalities, and ergometrine, thalidomide
potential risk clearly outweighs possible
benefit.
Examples of Teratogenicity effects caused due to various drugs
Drugs Abnormality
- Thalidomide Phocomelia and other multiple defects

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 Reproductive

- Lithium Cardiovascular anomalies, fetal diabetes insipidus, fetal goiter

- ACE inhibitor Intrauterine growth retardation (IUGR), hypoplasia of organs, pulmonary & renal
hypoplasia, fetal loss
- Antithyroid Fetal goiter and hypothyroidism
drugs
- Indomethacin Premature ductus arteriosus closure
- Isotretinoin Heart and CNS defects, craniofacial defects
- Alcohol Fetal alcohol syndrome characterized by growth retardation, fetal anomalies typically confined
to face like thin upper lips, low set and unparallel ears, short length of nose, epicanthic fold,
flattened nasal bridge and CNS dysfunction like microcephaly & mental retardation.
- Warfarin Depressed nose, eye and hand defects, growth retardation
- Neural tube defects (spina bifida) and uterus and other defects

Anticonvulsant
s (valproate &
carbamazepine
)
- Phenytoin Left lip/palate, microcephaly and hypoplastic phalanges
- Tetracyclines Discolored and deformed teeth, retarded bone growth
- Anti-cancer Cleft palate, hydrocephalus, multiple defects and fetal death
drugs
- Androgens Virilization, limb, esophageal and cardiac effects
VII
- Progestin Virilization of female fetus
- Stilboestrol Vaginal carcinoma in teenage female offsprings
- Corticosteroids Intrauterine growth retardation, fetal adrenal suppression
- Narcotics Depression of CNS-apnea, bradycardia & hypothermia.
Prevention of teratogenic effects of drugs in - Domperidone - Promethazine,
pregnancy: dicyclomine
- Where possible using non drug therapy - Lansoprazole - Metoclopramide
- Prescribing drugs only when definitely needed - Morphine - Ranitdine
- Choosing the drug having the best safety - Fluroquinolones - Lactulose
record over time - Tetracycline - Paracetamol
- Avoiding newer drugs, unless safety is clearly - Chloramphenicol - Chlorpheniramine
established
- Streptomycin - Penicillins &
- Avoiding medication in the initial 10 weeks of
gestation as far as possible cephalosporins
- Using lowest effective dose - Tinidazole - Erythromycin
- Using drugs for shortest period necessary - Quinine - Isoniazid &Rifampicin
- Using drugs intermittently, if possible. - Albendazole - Chloroquine
Drugs related to pregnancy - Diethyl - Diloxanide furoate
Drugs Drugs safe to use during carbamazine
contraindicated pregnancy - Ketoconazole - Piperazine
during pregnancy - Amphotericin B - Zidovudine, Lamivudine

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 Pharmacology

- Ganciclovir - Nevirapine - Acetazolamide - Amiloride

- ACE inhibitors - Methyldopa, atenolol - Albendazole - Amiodarone
- Angiotensin - Nifedipine - Low dose aspirin - Androgens
receptor blockers - Bupivacaine - Anti-cancer drugs
(ARBs) - Cephalosporins - Chloramphenicol
- Metformin - Insulin - Cloxacillin - Chloroquine
- Suphonylureas - Low dose prednisolone - Sodium cromoglycate - Ciprofloxacin
- Radioactive iodine - Thyroxine - Diclofenac - Estrogens
- Trimipramine - Propylthiouracil - Digoxin - Fluconazole
- Warfarin - Haloperidol - Domperidone & - Indomethacin
- Ketotifen - Amytriptyline, cisapride
Imipramine Heparin. - Erythyromycin - Radioactive iodine
Drugs during breast feeding: - Ethambutol - Ketoconazole
- Some drugs are excreted in the milk and if they - Heparin - Lithium
are of pharmacologically significant quantity, - Ibuprofen - Metformin
then they may lead to toxic effects on infants. - Insulin - Methotrexate
Moreover, some of the drugs can affect - Methyldopa - Tetracycline
lactation only by antagonizing the action of the - Paracetamol - Iodine/iodides
hormones in lactation or simply by inhibiting - Piperacilin - Metronidazole
release of prolactin. Eg- bromocriptine - Piperazine
- Thus, drugs are to be cautiously administered - Piperazine
in lactating women. - Pyrazinamide
Drugs related to lactation - Warfarin & sod.
valproate
Drugs safe during Drugs contraindicated in
lactation lactation
VII

SPECIAL POINTS FOR MCQs

1. The main indication of HRT is vasomotor and other symptoms in perimenopausal period.
2. Oestrogen use has risk of endometrial carcinoma and progestins antagonize them.
3. Oestrogen use has risk of thromboembolic phenomenon.
4. Progestin use has risk of breast cancer.
5. Raloxifene is 1st line drug for treatment of osteoporosis in post-menopausal women.
6. Progestin only pills are called as lactation pill as they can be given during lactation.
7. Steroid hormones and their antagonist act on endometrium of uterus whereas oxytocics and
tocoloytics on the myometrium.
8. Yupze method is type of emergency pill containing both estrogen and progestin.
9. Prostaglandins promote myometrial contraction irrespective of the duration of gestation, whereas
oxytocin acts predominantly on the uterus at term or labour.
10. Valacyclovir is drug of choice in herpes zoster.

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11. Lamivudine is deoxycytidine analogue and inhibits both HIV reverse transcriptase as well as
hepatitis B virus DNA polymerase.
12. Frequency of spontaneous as well as drug induced malformations, especially neural tube defects,
may be reduced by folate therapy during pregnancy.
13. Fetal alcohol syndrome is characterized by triad of CNS defects, facial defects and growth
retardation.
14. The side effects of testosterone and its analogue are oligozoospermia (due to feedback inhibition)
and gynaecomastia.
15. Ketoconazole is androgen synthesis inhibitor.

VII

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