Reproductive Drugs

Question 1

Major ovarian estrogen, esters given by IM injections, in contraceptives

Answer 1

Estradiol, estradiol cypionate, ethinyl estradiol

Question 2

Effects of estrogens

Answer 2

For female reproductive development (vagina, uterus, uterine tube), for appearance of secondary sex characteristics and growth spurt in puberty, for metabolism (decreases bone resorption, enhances coagulability and increase triglyceride levels by increasing HDL and decreasing LDL cholesterol)

Question 3

Usage of estrogens

Answer 3

Hypogonadim, in hormonal replacement therapy for women with estrogen deficiency resulting in premature ovarian failure, menopause or surgical removal of ovaries, to ameliorate hot flushes and atrophic changes in the UI tract, for bone loss and osteoporosis, in hormonal contraceptives

Question 4

Toxicity of estrogens

Answer 4

In hypogonadal girls: premature closure of epiphyses in long bones (short stature)
In HRT: risk of endometrial cancer (prevented if we use progestins with it)
In postmenopausal women: risk of breast cancer, and myocardial events
In general, we have also nausea, breast tenderness, migraine headaches, DVT, gallbladder diseases, hypertriglyceridemia, hypertension

Question 5

Diethylstilbestrol DES

Answer 5

Nonsteroidal estrogenic compound associated with infertility, ectopic pregnancy, vaginal adenocarcinoma if women that took it while being pregnant with a girl for spontaneous abortions

Question 6

Progesterone or synthetic medroxyprogesterone effects and usage

Answer 6

Induce changes in the endometrium and maintains pregnancy, affect carbs metabolism and stimulate fat deposition
Used in contraceptives, in HRT with estrogen to decrease risk of endometrial cancer, promoting and maintaining pregnancy

Question 7

Toxicity of progestins

Answer 7

Increase bp, decrease HDL, reversible decrease in bone density, changes libido, headache, depression, mood swings, salt retention, acne, hirsutism, increase apetite and weight gain

Question 8

Combination oral contraceptives methods of administration

Answer 8

-monophasic for 21-24 days
-triphasic: 3 successive 7-day periods to mimic the cycle
-four-phasic: in 4 phases we take estradiol valerate and dienogest
Monophasic and triphasic are followed by 4-7 days of placebo seen with withdrawal bleeding

Question 9

Progestins used in combination oral contraceptives

Answer 9

Norethindone, norethidone acetate, levonorgestrel, desogestrel…

Question 10

Usage of combination oral contraceptives

Answer 10

Hypogonadism, acne, hirsutism, dysmenorrhea, menorrhagia, endometriosis, decreases risk of ovarian and endometrial cancer, less benign breast disease, ectopic pregnancy, iron deficiency anemia

Question 11

Adverse effects of combination oral contraceptives

Answer 11

DVT,PE,MI in smokers (not taken if >35y), breast caner risk, continuous bleeding (if used for a long period)

Question 12

Postcoital contraceptives or emergency contraceptives

Answer 12

-oral preparations of levonorgestrel alone, estrogen alone or mixed for up to 72 hours after intercourse
-ulipristal (agonist/ antagonist of progesterone) up to 5 days after intercourse (efficacy >=85%)
-levonorgestrel pill that delays ovulation up to 72 hours after intercourse (same efficacy)
- most efficient are IUD:
Hormonal: up to 3-5 years avoided in pelvic inflammatory disease and a case with previous ectopic pregnancies
Copper: inducing inflammatory reaction that is toxic to the ova, sperm and impairs implantation. Up to 5 days and its efficacy is 99%.

Question 13

Tamoxifen/ taromfiene

Answer 13

Antagonist: breast cancer->hot flushes
Agonist: endometrial hyperplasia (endometrial cancer risk), osteoporosis in postemnopausal women->DVT risk

Question 14

Raloxifene

Answer 14

Partial agonist: prevent and treat osteoporosis->DVT risk
Antagonist: breast cancer->hot flushes

Question 15

Clomiphene

Answer 15

SERM non steroidal esteogenic compound that induces ovulation by blocking estrogen receptors in the anterior pituitary->vasomotor changes, multiple births, ovarian hyperstimulation syndrome, ascites, thromboembolism

Question 16

Patient resistant to tamoxifene for treatment of breast caner we use:

Answer 16

Pure estrogen receptor antagonist fluvestrant

Question 17

Aromatase inhibitors for breast cancer treatment

Answer 17

Anastrozole, letrozole… are nonsteroidal competitive inhibitors
Exemestane is an irreversible aromatase inhibitor

Question 18

Danazol

Answer 18

Inhibiting cytochrome P450 enzymes involved in gonadal steroid synthesis
It is a weak partial agonist of progestin, androgen, glucocorticoid receptors
Used for endometriosis and fibrocystic diseases of the breast

Question 19

For treatment of precocious puberty in children, short term (<6months) treatment of endometriosis and uterine fibroids in women

Answer 19

Leuprolide a GnRH agonist

Question 20

Antagonists of GnRH for ovarian hyperstimulation

Answer 20

Cetrorelix, ganitrelix

Question 21

For complete abortion

Answer 21

Mifepristine (RU486 orally active steroid antagonist of progesterone and glucocorticoids) and misoprostol
Side effects: n&v, diarrhea, vaginal cramping, bleeding and intrauterine infections

Question 22

Active testosterone that has little effect orally so is injected or given by transdermal patch

Answer 22

Dihydrotestosterone DHT

Question 23

Testosterone effects and usage

Answer 23

Normal male features development and major changes during puberty. After puberty, it maintains secondary sex characteristics, increases muscle size and mass, increases RBCs production, decrease urea nitrogen secretion, maintain bone density, affects fertility, libido and causes balldness
Used for hypogonadism, wasting syndrome (AIDs and anemi) and athletic performance

Question 24

Toxicity of testosterone

Answer 24

-Virilization if females (bigger clittoris, hirsutism, deepened voice), menstrual irregularity, verilization of girl from a mother with testosterone toxicity
- in men: feminization (gynecomastia, testicular shrinkage, infertility) happens because of - feedback to pituitary so conversion of exogenous androgens to estrogens
-cholestatuc jaundice, elevation of liver enzymes, hepatocellular carcinoma, premature closure of epiphysis in children, edema, aggression

Question 25

Flutamide and spironolactone

Answer 25

Receptor inhibitors
Flutamide nonsteroidal competitive antagonist of androgen receptors used for prostate carcinoma
Spironolactone (potassium sparing diuretic) used for hirsutism treatment

Question 26

Finasteride or dutasteride having a longer half life

Answer 26

Inhibits 5alpha reductase (no DHT for prostate or hair follicles) used for benign prostatic hyperplasia and low doses to prevent hair loss in men