Reproductive Drugs Flashcards
GnRH agonist
Name
Uses (3)
Adverse rxns (4)
- Luprolide
- Uses
- Single dose used for evaluation of precocious / delayed puberty w/ “LHRH test”
- Pulsed GnRH used to stimulate FSH release for ovulation. Ex: Kallman Syndrome.
- Long-acting agonists / antagonists used for suppressing central precocious puberty, treating endometriosis, fibroids, androgen deprivation for prostate cancer, or shutting down endogenous ovarian function for exogenous ovulation induction for fertility.
- Adverse rxns – precipitate sxs of hypogonadism in both genders: hot flashes, bone loss, low libido, infertility / amenorrhea. All are reversible except bone loss.
Exogenous gonadotropin uses (3)
Recombinant FSH injections stimulate ovarian follicle development.
hCG has longer halflife than LH and is used to simulate LH surge to trigger ovulation. hCG also enhances sperm / testosterone production in males
2 DA agonists
Use
Mechanism
Adverse Rxns
- Cabergoline, Bromocriptine
- Use – hyperprolactinemia / prolactinoma
- Mechanism – DA inhibits prolactin production
- Adverse rxns – nausea, hypotension / dizziness
Physiologic effects of estrogen (7)
Female secondary sex characteristics, closes epiphyses, proliferates endometrium, maintains bone mass, stimulates hepatic production of sex hormone binding globulin / thyroid hormone binding globulin / and blood clotting factors.
Exogenous estrogen
Uses (4)
Adverse Rxns (4)
- Uses
- Postmenopausal hormone therapy utilizes oral / topical estradiol or conjugated equine estrogens (CEE) which contain sulfated esters of estrone. Reduces sxs of estrogen deficiency (hot flashes, urogenital atrophy)
- Premature ovarian failure – stimulate secondary sex characteristics in girls w/ prepubertal ovarian failure (Turner) or during reproductive years.
- Contraception
- Prevention / treatment of osteoporosis
- Adverse rxns – nausea / vomiting, breast tenderness, endometrial hyperplasia / risk of endometrial carcinoma if unopposed by progestin, thrombosis (exacerbated by smoking).
Tamoxifen Type of drug Use Mechanism Positive effect Negative effects (4)
- SERM (selective estrogen receptor modifier)
- Use – treats estrogen-receptor-positive breast cancer.
- Mechanism – estrogen antagonist at breast tissue, agonist at endometrium and bone
- Positive effects – reduced bone loss
- Negative effects – risk of endometrial hyperplasia / carcinoma, thrombosis, hot flashes, multiple births
Clomiphene citrate (Clomid) Type of drug Use Mechanism Adverse rxns (4)
- SERM (selective estrogen receptor modifier)
- Use – ovulation induction
- Mechanism – inhibits estrogen binding in hypothalamus and anterior pituitary → increased GnRH / gonadotropins → follicle stimulation / ovulation.
- Has some very slight agonist action (hence being a SERM), but all clinical uses are strictly as an antagonist.
- Adverse rxns – multiple births, hot flashes, thin endometrium, thick mucous (may inhibit sperm production)
Raloxifene Type of drug Use Mechanism Positive effects Negative effects
- SERM (selective estrogen receptor modifier)
- Use – prevention / treatment of postmenopausal osteoporosis
- Mechanism – estrogen antagonist in breast, agonist in bone, no effect on endometrium.
- Positive effects – decreases risk of ER+ breast cancer
- Negative effects – thrombosis, hot flashes
2 types of aromatase inhibitors & names
Use
Mechanism
Adverse rxns
- 2 types
- Type 1 (Exemestane): irreversible, steroidal-structure
- Type 2 (Anastrozole, Letrozole): reversible, nonsteroidal
- Use – ER+ BC, ovulation induction (off-label, reversible AI’s only)
- Mechanism – aromatase converts androgens → estrogen, so inhibition decreases estrogen levels.
- Side effects – hot flashes and bone loss
Physiologic effects of progestins (4)
Inhibits proliferation of endometrium, prepares endometrium for embryo implantation, supports maternal / fetal needs during pregnancy, with drawal triggers menses
Medroxyprogesterone acetate used for?
Used w/ estrogens for HRT in postmenopausal women.
Drospirenone effects
Progestin used in OCPs and postmenopausal HRT
Has antimineralocorticoid and antiandrogen activity.
Exogenous progestin
Uses (4)
Adverse rxns (3)
- Uses
- HRT to counteract estrogen to prevent endometrial hyperplasia. ALL women w/ a uterus on estrogen therapy need progesterone as well.
- Contraception
- Support of pregnancies w/ no CL present until placenta takes over. Natural progesterone is preferred to avoid androgenic effects
- IVF
- Adverse effects – weight gain, edema, menstrual disorders
Postmenopausal hormone therapy
Pros (2)
Cons (4)
What should be taken concomitantly?
- Pros: improves bone density and decreases colon cancer
- Cons: increases risk of DVT, stroke, breast cancer, and coronary heart disease.
- Take aspirin to avoid clotting
Progestin antagonist Name Uses (2) Mechanism (2) Adverse rxns (2)
- Mifepristone (RU486)
- Use – termination of pregnancy, treating Cushing’s syndrome
- Mechanism – Competitive agonist of progesterone → breakdown of decidualized endometrium by blocking PR’s → detachment of implanted blastocyst and decrease in hCG, further decreasing progesterone production from CL
- Also blocks glucocorticoid binding to the glucocorticoid receptor
- Adverse rxns – vaginal bleeding, adrenal insufficiency
