Repro Flashcards
Leuprolide
MOA
GnRH analog
Pulsatile - agonist
Continuous - antagonist
Leuprolide
Clinical use
Infertility (pulsatile)
Prostate cancer, uterine fibroids (continuous)
Precocious puberty (continuous)
Estrogens (Ethinyl estradiol, DES, mestranol)
Clinical use
Binds estrogen receptors.
For hypogonadism, ovarial failure, menses abnormalities, HRT.
Estrogens
Toxicity
Inc. risk Endometrial cancer.
Bleeding in postmenopause.
CI in ER-positive breast cancer, hx of DVT.
Clomiphene
[MOA, clinical use]
SERM – Estrogen receptor antagonist at hypothalamus.
Prevents feedback inhibition – inc. LH/FSH – ovulation.
For infertility (anovulation).
Tamoxifen
[MOA, clinical use, toxicity]
SERM: Antagonist at breast; agonist at bone, uterus.
Treat and prevent recurrence of ER/PR-positive breast cancer.
Tox: inc. risk of thromboembolism, endometrial cancer.
Raloxifene
[MOA, clinical use]
SERM: Antagonist at breast, uterus; agonist at bone.
Treat osteoporosis.
Inc. risk of thromboembolism.
Hormone replacement therapy.
For what?
Estrogen? Progesterone?
For menopausal sx, osteoporosis.
Unopposed estrogen inc. risk of endometrial cancer – add progesterone (estrogen + progesterone).
Progestins
[MOA, clinical use]
Bind progesterone receptors. Used in OCPs.
Dec. growth and inc. endometrial vascularization.
For endometrial cancer, abnormal uterine bleeding.
Oral contraception
MOA
Estrogen + progestin.
Inhibit LH/FSH – no estrogen surge – no LH surge – no ovulation.
> Progestins: thick cervical mucus, limits sperm access to uterus; inhibit endometrial proliferation, so harder to implant.
Oral contraception
Contraindications
Smokers > 35 y.o
Hx of thromboembolism, stoke
Hx. of estrogen-dependent tumor
Terbutaline, Ritodrine
Clinical use
B2-agonists
Relax the uterus.
To dec. contraction frequency in labor.
Testosterone
Clinical use
Androgen receptor agonist.
For hypogonadism; to develop secondary sex chars.
Testosterone
Toxicity
Masculinization in females.
Gonadal atrophy in males (inhibits LH release) – dec. intratesticular testosterone.
Premature closure of epiphyseal plates.
Finasteride
[MOA, use]
Antiandrogen; 5a-reductase inhibitor (testosterone –> DHT).
For BPH, male-pattern baldness.
Flutamide
[MOA, use]
Antiandrogen; Nonsteroidal competitive androgen receptor inhibitor.
For prostate CA.
Ketoconazole
[MOA, use, SE]
Antiandrogen.
Inhibits 17,20-desmolase (cholesterol – androgen) – Inhibits steroid synthesis.
For polycystic ovarian syndrome – reduce androgenic sx.
SE: gynecomastia, amenorrhea
Spironolactone
[MOA, use, SE]
Antiandrogen.
Inhibits steroid binding, 17a-hydroxylase, 17,20-desmolase.
For polycystic ovarian syndrome.
SE: gynecomastia, amenorrhea
Tamsulosin
[MOA, use]
a1-antagonist (alpha1A,D receptors in prostate).
Inhibit smooth muscle contraction, for BPH.
Treat BPH
Sildenafil, Vardenafil, Tadalafil
[MOA, clinical use]
Inhibit PDE-5 – inc. cGMP – smooth muscle relaxation in corpus cavernosum, inc. blood flow – penile erection.
For erectile dysfunction.
Sildenafil, Vardenafil, Tadalafil
Toxicity
Life-threatening Hypotension in pts taking nitrates.
Headache, heartburn
Anastrozole/Exemestane
[MOA, use]
Aromatase inhibitors.
Used in postmenopausal women w/ ER-positive breast cancer.
*Source of estrogen after menopause becomes peripheral conversion of androgens.
Danazol
[MOA, use]
> Partial agonist at androgen receptors – induces a state of pseudomenopause by suppressing ovarian fxn and inhibits FSH/LH secretion, causing endometrial atrophy.
For endometriosis, hereditary angioedema.
Mifepristone (RU-486)
[MOA, use]
Competitive inhibitor of pregestins at progesterone receptor.
Termination of pregnancy.
*Administer w/ misoprostol (PGE1)
