Non-steroidal agent.

MECH: Antiestrogenic effect on mammary epithelium (competitive antagonist on estrogen receptors). Pro-estrogenic on uterine endometrium and bone.

USE: Treatment of estrogen receptor (ER) positive advanced breast tumors. Estrogen has stronger affinity for receptor so must use higher concentration of Tamoxifen over estrogen.

AE: Incr. risk endometrial cancer with long use.

Non-steroidal agent.

MECH: Has two isomers, cis- is a weak estrogen agonist while trans- is a potent antagonist. Blocks estrogen binding in hypothalamus inhibiting estradiol's negative feedback on gonadotropins. This increases FSH and LH release forcing ovulation.

USE: To stimulate ovulation in infertile patients with ovulation disorders so they can get pregnant.

AE: Hot flashes, stomach pain, headache, vomiting, multiple pregnancy.

MECH: Actions include 1) Stimulation of endometrium secretory gland growth to facilitate implantation of fertilized egg; 2) High levels trigger negative feedback in hypothalamus ---> stops release of gonadotropin thus suppressing ovulation.

USE: 1) Contraception - used with estrogens or in progestin-only formulations. 2) Hormone replacement therapy on post-men women. Suppresses the growth of endometrial cancers mitigating the pro-endometrial cancer effects of estrogen therapy.

Micronized Progesterone increases the half-life thus decreasing first pass metabolism.

Transvaginal progesterone is a vaginal gel which minimizes systemic side-effects.

AE: Fatigue and drowsiness.

Orally administered.

MECH: Actions include 1) Stimulation of endometrium secretory gland growth to facilitate implantation of fertilized egg; 2) High levels trigger negative feedback in hypothalamus ---> stops release of gonadotropin thus suppressing ovulation.

USE: 1) Contraception - used with estrogens or in progestin-only formulations. 2) Hormone replacement therapy on post-men women. Suppresses the growth of endometrial cancers mitigating the pro-endometrial cancer effects of estrogen therapy.

AE: Edema, abd. bloating, anxiety, irritability, depression, muscular pain, hirsutism, acne. Also increases risk of thrombosis and PE.

CONTRA: Pts with thromboembolic disorders, liver disease, vaginal bleeding, pregnancy.

Orally administered.

MECH: Actions include 1) Stimulation of endometrium secretory gland growth to facilitate implantation of fertilized egg; 2) High levels trigger negative feedback in hypothalamus ---> stops release of gonadotropin thus suppressing ovulation.

USE: 1) Contraception - used with estrogens or in progestin-only formulations. 2) Hormone replacement therapy on post-men women. Suppresses the growth of endometrial cancers mitigating the pro-endometrial cancer effects of estrogen therapy.

AE: Edema, abd. bloating, anxiety, irritability, depression, muscular pain, hirsutism, acne. Also increases risk of thrombosis and PE.

CONTRA: Pts with thromboembolic disorders, liver disease, vaginal bleeding, pregnancy.

Orally administered.

MECH: Actions include 1) Stimulation of endometrium secretory gland growth to facilitate implantation of fertilized egg; 2) High levels trigger negative feedback in hypothalamus ---> stops release of gonadotropin thus suppressing ovulation.

USE: 1) Contraception - used with estrogens or in progestin-only formulations. 2) Hormone replacement therapy on post-men women. Suppresses the growth of endometrial cancers mitigating the pro-endometrial cancer effects of estrogen therapy.

AE: Edema, abd. bloating, anxiety, irritability, depression, muscular pain, hirsutism, acne. Also increases risk of thrombosis and PE.

CONTRA: Pts with thromboembolic disorders, liver disease, vaginal bleeding, pregnancy.

Orally administered.

MECH: Actions include 1) Stimulation of endometrium secretory gland growth to facilitate implantation of fertilized egg; 2) High levels trigger negative feedback in hypothalamus ---> stops release of gonadotropin thus suppressing ovulation.

USE: 1) Contraception - used with estrogens or in progestin-only formulations. 2) Hormone replacement therapy on post-men women. Suppresses the growth of endometrial cancers mitigating the pro-endometrial cancer effects of estrogen therapy.

AE: Edema, abd. bloating, anxiety, irritability, depression, muscular pain, hirsutism, acne. Also increases risk of thrombosis and PE.

CONTRA: Pts with thromboembolic disorders, liver disease, vaginal bleeding, pregnancy.

USE: Contraception--this is The Pill.

MECH: Estrogen - Constant estrogen suppresses FSH secretion inhibiting follicle maturation. Also prevents LH surge. Progestin - Primarily suppresses LH preventing ovulation. Thickens cervical mucus making it impenetrable to sperms. Develops endometrial atrophy making it resistant to implantation.

USE: Contraception--less effective than combo. For use when estrogen is contraindicated as in pts. with family hx of endometrial cancer.

AE: More likely to produce irregular cycle than combo treatment.

USE: Morning after contraception. Must be taken within 72 hours of sex.

MECH: Large dose hormones. Mechanism not completely known may interfere with implantation or delay ovulation.

Synthetic steroid similar to progesterone.

MECH: Competitively inhibits progestin binding causing breakdown of uterine lining detaching embryo or fetus.

USE: Medical abortion of early pregnancy (< 50 days).

CAUTION: Only physicians can administer. May require prompt surgery if abortion is incomplete.

MECH: Phosphodiesterase 5 (PDE5) inhibitor. PDE5 inhibits breakdown of cGMP in the following pathway:

Sexual arousal--->NO release from corpus cavernosum synapse neurons---->Accumulation of GTP---->Guanylyl cyclase makes cGMP--->cGMP decreases intracellular Ca via PKG---->Promotes sm. muscle relaxation--->ERECTION!

AE: Headache, dizziness, flushing and vision changes, upsot stomach, stuffy or runny nose, UTI, diarrhea. PDE5 expressed in corpus cavernosum and retina.

CAUTION: Some men lose vision due to non-arteritic ischemic optic neuropathy (NAION)--sudden decreased blood flow to optic nerve. ALSO, cause sudden hypotension when taken with nitrates and alpha-blockers. USE ONLY ONCE PER DAY!