Reproductive Drugs Flashcards
(26 cards)
Major ovarian estrogen, esters given by IM injections, in contraceptives
Estradiol, estradiol cypionate, ethinyl estradiol
Effects of estrogens
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)
Usage of estrogens
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
Toxicity of estrogens
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
Diethylstilbestrol DES
Nonsteroidal estrogenic compound associated with infertility, ectopic pregnancy, vaginal adenocarcinoma if women that took it while being pregnant with a girl for spontaneous abortions
Progesterone or synthetic medroxyprogesterone effects and usage
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
Toxicity of progestins
Increase bp, decrease HDL, reversible decrease in bone density, changes libido, headache, depression, mood swings, salt retention, acne, hirsutism, increase apetite and weight gain
Combination oral contraceptives methods of administration
-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
Progestins used in combination oral contraceptives
Norethindone, norethidone acetate, levonorgestrel, desogestrel…
Usage of combination oral contraceptives
Hypogonadism, acne, hirsutism, dysmenorrhea, menorrhagia, endometriosis, decreases risk of ovarian and endometrial cancer, less benign breast disease, ectopic pregnancy, iron deficiency anemia
Adverse effects of combination oral contraceptives
DVT,PE,MI in smokers (not taken if >35y), breast caner risk, continuous bleeding (if used for a long period)
Postcoital contraceptives or emergency contraceptives
-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%.
Tamoxifen/ taromfiene
Antagonist: breast cancer->hot flushes
Agonist: endometrial hyperplasia (endometrial cancer risk), osteoporosis in postemnopausal women->DVT risk
Raloxifene
Partial agonist: prevent and treat osteoporosis->DVT risk
Antagonist: breast cancer->hot flushes
Clomiphene
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
Patient resistant to tamoxifene for treatment of breast caner we use:
Pure estrogen receptor antagonist fluvestrant
Aromatase inhibitors for breast cancer treatment
Anastrozole, letrozole… are nonsteroidal competitive inhibitors
Exemestane is an irreversible aromatase inhibitor
Danazol
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
For treatment of precocious puberty in children, short term (<6months) treatment of endometriosis and uterine fibroids in women
Leuprolide a GnRH agonist
Antagonists of GnRH for ovarian hyperstimulation
Cetrorelix, ganitrelix
For complete abortion
Mifepristine (RU486 orally active steroid antagonist of progesterone and glucocorticoids) and misoprostol
Side effects: n&v, diarrhea, vaginal cramping, bleeding and intrauterine infections
Active testosterone that has little effect orally so is injected or given by transdermal patch
Dihydrotestosterone DHT
Testosterone effects and usage
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
Toxicity of testosterone
-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
