Reproductive

Pharm
Drug Mechanism Use ADR
Continuous: induce hypogonadism, prostate
Leuprolide, Bus-, Nafar-, GnRH agonists - intermittent stimulates FSH / Headache, nausea, hypoestrogenic state (hot flashes, vaginal
cancer, uterine fibroids, endometriosis, PCOS,
Goserelin LH release, continuous suppresses FSH / LH dryness, bone density loss) - limit use to 6 mo.
precocious puberty - Intermittent: infertility
GnRH receptor antagonist --> inhibits FSH / LH -- Supress LH surge in IVF cycle, endometriosis, GI, weight gain, fluid retention, cramps, headache, female
Cetro-, Ganirelix
> lower estrogen menorrhagia, gynecomastia virilization
HPG

Urofolli-, Folli-, Menotropin FSH injection --> inc. follicular development

Multifollicular development and induction of Headache, cramps, edema, ovarian hyperstim. syndrome,
ovulation thromboembism, multiple births
hCG injection Mimics LH surge --> stimulate ovulation
Androgenic, anti-estrogenic, anti-progestogenic -
Endometriosis, fibrocystic breast disease - Weight gain, acne, hair growth, hepatic effects, intracranial
Danazol -> decreased FSH / LH --> regression of normal /
replaced by GnRH agonists hypertension, thromboembolism
ectopic endometrium
GI, breast tenderness, migraine, thromboembolism, CAD,
Stimulates endometrial growth, reduces LDL / Replacement in patients without breast cancer
Estrogens contraindicated in heavy smokers, endometrial hyperplasia /
raises HDL, etc. history, osteoporosis, atrophy of UG tissue
cancer - DES --> clear cell vaginal adenocarcinoma in offspring
Hypothalamic estrogen receptor antagonist --> Abdominal / breast pain, hot flashes, multiple births, ovarian
Clomiphene Infertility
inc. GnRH --> inc. FSH / LH --> ovulation enlargement / cancer risk, visual disturbances
SERM: estrogen agonist in endometrium / bone, Estrogen-sensitive breast cancer, Hot flashes, thrombosis, endometrial cancer, endometriosis,
Tomoxifen antagonist in breast / vagina. Also upregulates progesterone resistant endometrial / ovarian hair/nail thinning, vaginal discharge, DDI w/ CYP inhibitors
Estrogen

TGF-B cancer, melanoma, osteoporosis (SSRIs)

Estrogen sensitive breast cancer, osteoporosis,
SERM - estrogen agonist in bone, antagonist in Hot flashes, joint / muscle pain, weight gain, vaginal
Raloxifene safe for patients with history of endometrial
breast / endometrium discharge, thromboembolism, CV disease
cancer - only for post-menopausal women
Competitive estrogen receptor antagonist -->
Fulvestrant Estrogen sensitive breast cancer Hot flashes, injection site rxns, elevated LFTs
down regulation of receptor
Le-, anastrozole = competitive Aromatase inhibitors --> dec. estrogen / Breast cancer in post-menopausal females
Ischemic heart disease (anastrozole), DDI w/ estrogen
Exemestane = non-comp estradiol only
Inhibits FSH / LH secretion --> prevent follicle Contraception, reduced endometrial / ovarian Breast cancer in women receiving HRT w/ high TGs,
Oral contraceptives (P+E) development / ovulation, make environment cancer risk, off-label: PCOS, endometriosis, depression, HTN, hypercoag., fluid retention, weight gain, DDI
unfavorable for sperm / embryo implantation acne / hirsutism, menorrhagia / dysmenorrhea w/ anticonvulsants, rifampin
Contraceptives

Irregular bleeding, acne, hirsutism, fluid retention, dec. HDL /

FAOS: Medroxyprogesterone, Progestins: Stimulates endometrial secretions / Contraception, stimulate appetite - Norplant:
inc. LDL, depression, change in libido, breast discomfort, HTN,
Norethindrone spiral artery development, supresses ovulation implanted drug strip (5 yr release)
thromboembolism
Progestin only contraceptive: thickens cervical Contraception, decreases endometrial cancer Irregular bleeding, acne, follicular cysts, breast cancer risk,
Lerchenfeldt: Norethinidrone
mucus --> prevent sperm entry risk, MUST take regularly DDI w/ anticonvulsants, rifampin
?? - Alters sperm transport, inhibits ovulation, Contraception after unprotected sex or GI, need to take within 72 hrs of intercourse, less effective
Levonorgestrel
prevents implantation contraceptive failure (morning after pill) than standard contraceptives
Maternal pulmonary edema, tremor, arrythmia, hypokalemia,
Terbutaline, Ritodrine,
B2-adrenergic agonists --> relaxes uterus Prevent premature labor contraindicated for hyperthyroid, cardiac disease, use as
Salmeterol
inpatient for 72 hrs max
Rare: maternal death from HTN episodes, arrhythmias, uterine
Gq --> release of Ca2+ --> muscle contraction in Induce labor, abortion, milk letdown,
Partuition

Oxytocin, Ergometrine rupture, water intoxification (antidiuretic); fetal death, DDI w/

uterus and mammary glands - also inc. PG synth controlling postpartum uterine hemorrhage
QT-prolonging drugs
Dino = PGE2, Miso = PGE1 --> relaxes smooth Abnormal uterine contractions, GI, postpartum DIC,
Dinoprostone, Misoprostol Promote cervical ripening
muscle --> cervical dilation contraindicated in prior C-section / maj. uterine surgery
Competitive progesterone receptor antagonist -- Alternative to surgical termination of Diarrhea, pain, heavy bleeding, GI, anorexia, abdominal pain,
Mifepristone
> contraction of myometrium pregnancy bacterial infections
Thromboembolism (higher in women), breast pain, headache,
Follitropin alfa / beta FSH injection --> spermatogenesis Infertility
cramps, acne vulgaris, 18 mo. Max
Stimulates testosterone production and Hypo-hypogonadism, prepubertal Gynecomastia, precocious puberty, edema, headache,
hCG injection
spermatogenesis cryptorchidism, infertility thromboembolism
Gradual decrease of LH / FSH --> infertility, salt / water
Converted to DHT --> modifies gene Testicular failure, delayed puberty, anemia,
Methyl-, testosterone retention, edema, hepatotoxicity, contraindicated for breast /
transcription - also decreases LH release anabolic use
prostate cancer
Not approved in US - hirsutism, prostate Breast swelling, decreased libido, erection problems,
Cyproterone Competitive androgen receptor antagonist
Male

cancer, BPH, hypersexuality, priapism galactorrhea

1st Gen: Flutamide,
bicalutamide, nilutamide. Competitive testosterone receptor antagonist
2nd Gen: enzalutamide
Finasteride
Tadal-, Varden-, Sildenafil
Bromocriptine, Cabergoline
Other
Hot flashes, GI, impotence / dec. libido / dec. ejaculate,
Prostate cancer, hirsutism
gynecomastia, hepatitis
Gynecomastia, lip swelling, testicular pain, GI, dec. libido,
Inhibit 5a-reductase --> no conversion of Sexual dysfunction, BPH, male-pattern
decreases PSA, inc. risk of high grade prostate cancer,
testosterone to DHT --> dec. prostate size baldness
pregnant women shouldn't make contact
Inhibit PDE5 (cGMP phosphodiesterase) --> Headache, flushing, dyspepsia, alteration in blue-green color
Erectile dysfunction
vasodilation --> erection vision, DDI with nitrates, a-blockers, CYP inhibitors
Hypotension, nausea, confusion, headache, psychosis,
Dopamine agonists --> inhibit PRL secretion Hyperprolactinemia, Parkinson's in high doses
hallucinations

Trastuzumab Monoclonal antibody against ERBB2 (HER2) Metastatic breast cancer w/ ERBB2 Cardiotoxicity
Ketoconazole, Abiraterone, Inhibit steroid synth, displace estradiol / DHT
PCOS, hirsutism Liver toxicity (rare but fatal), gynecomastia, pruritis, GI
Spironolactone from SHBG, inc. estradiol:testosterone ratio