Pharmacology: Repro Flashcards
Leuprolide
GnRH analog
- Agonist if pulsatile
- Antagonist if continuous: downregulates GnRH receptor in the pituitary and decr FSH/LH
Testosterone/methyltestosterone
Agonist at androgen receptors
- Female masculinization
- Decr LH in males from incr neg fedback, resulting in gondal atrophy
- Premature closure of epiphyseal plates
- Incr LDL, decr HDL
Finasteride
5alpha-reductase inhibitor: decr conversion of T to DHT
Tx: BPH, male-pattern baldness
Flutamide
Competitive inhibitor of androgens at the testosterone receptor, nonsteroidal
Tx: Prostate cancer
Ketoconazole
Inhibits steroid synthesis via desmolase
- SEs: Gynecomastia, amenorrhea
Spirnolactone
Aldosterone receptor antagonist, androgen receptor antagonist, inhibits steroid synthesis
- Tx: hyperandrogenism (hirsutism, androgenic alopecia, acne, seborrhea); PCOS; male pattern baldness; hyperaldo (Conn’s syndrome/primary hyperaldo)
- SEs: Gynecomastia, amenorrhea
Ethinyl estradiol
Synthetic estrogen
- Tx: Hypogonadism or ovarian failure, menstrual abnormalities, HRT, men with androgen-dependent prostate cancer
- SEs: incr risk of endometrial cancer, thrombosis
- *Contraindications: ER+ breast cancer, history of DVTs
DES
Synthetic estrogen
Increased risk of clear cell adenocarcinoma of the vagina in females exposed to DES in utero
Mestranol
Synthetic estrogen
- Tx: Hypogonadism or ovarian failure, menstrual abnormalities, HRT, men with androgen-dependent prostate cancer
- SEs: incr risk of endometrial cancer, thrombosis
- *Contraindications: ER+ breast cancer, history of DVTs
Clomiphene
SERM
- Partial agonist at estrogen receptors in hypothalamus
- Prevents normal feedback inhibition, incr release of LH and FSH from pituitary –> stimulates ovulation
Tx: Infertility, PCOS
SEs: Hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances
Tamoxifen
SERM
- Antagonist on breast tissue
- Agonist at uterus/endometrium and bone
Raloxifene
SERM
- Agonist on bone, decr resorption
HRT
For menopausal sx, osteoporosis
Give PG to decrease risk of endometrial cancer
Possible incr CV risk
Anastrozole
Aromatase inhibitor
- Blocks synthesis of estrogen
- For postmenopausal women with ER+ breast cancer
Exemestane
Aromatase inhibitor
- Blocks synthesis of estrogen
- For postmenopausal women with ER+ breast cancer
Progestins
Bind progestin receptor
- Reduces growth and increases vascularization of endometrium
Tx: OCPs, endometrial cancer, AUB
Mifepristone (RU-486)
Competitive inhibitor of PG at PG receptors
- Medical abortion, give with misoprostol (PGE1 analog)
COCs
ES and PG inhibit LH/FSH –> no LH/FSH –> no ES surge –> no LH surge –> no ovulation
PG also thicken cervical mucus, inhibit endometrial proliferation
Ritodrine
Beta-2 agonist, relaxes uterus
- Reduces PUCs
Also a fast-acting bronchodilator
Terbutaline
Beta-2 agonist, relaxes uterus
- Reduces PUCs
Also a fast-acting bronchodilator
Tamsulosin
alpha1-antagonist, selective for alpha1A,D receptors on the prostate (vs. vascular alpha1B receptors)
- Inhibits smooth muscle contraction–relaxes bladder neck and smooth muscle fibers on the prostate
Prazosin
Non-selective alpha1-blocker
Terazosin
Non-selective alpha1-blocker
Doxazosin
Non-selective alpha1-blocker
Sildenafil
Increases cGMP by inhibit cGMP phosphodiesterase
- Relaxes smooth muscle in corpus cavernosum, increases BF and erection
Vardenafil
Increases cGMP by inhibit cGMP phosphodiesterase
- Relaxes smooth muscle in corpus cavernosum, increases BF and erection
Danazol
Synthetic androgen (testosterone), acts as partial agonist at androgen receptors
- inhibits ovarian steroidogenesis resulting in decreased secretion of estradiol and may increase androgens
- pituitary hormones largely unaffected (possible incr LH)
Tx: endometriosis, hereditary angioedema
SEs: weight gain, edema, acne, hirsutism, masculinization, contra in pregnancy as could masculinize a female fetus
