Reproductive Pharmacology (Male And Male Hormones)

Front 1

Danazol

Back 1

Synthetic androgen that acts as partial agonist at androgen receptors.

Used to treat endometriosis and hereditary angioedema.

Tox: weight gain, edema, acne, hirsutism, masculinization, lowered HDL levels, hepatotoxicity.

Front 2

Testosterone, methytestosterone

Back 2

Agonist at androgen receptors.

Used to treat hypogonadism and promote development of secondary sex characteristics
-Stimulates anabolism to promote recovery after burn or injury.

Tox: causes masculinization in females

-Decreases intratesticular testosterone in males by inhibiting release of LH (via negative feedback), which leads to gonadal atrophy.

-Premature closure of epiphyseal plates.

-Increased LDL, decreased HDL

Front 3

Antiandrogens

Back 3

Antiandrogens act on reaction: testosterone converted to DHT (more potent), with 5-alpha-reductase as the enzyme.

Front 4

-Finasteride

Back 4

Finasteride is a 5-alpha-reductase inhibitor – decreases conversion of testosterone to DHT.

-Useful in BPH
-Also promotes hair growth – used to treat male-pattern baldness.

"To prevent male-pattern hair loss, give a drug that will encourage female breast growth."

Front 5

-Flutamide

Back 5

Flutamide is a non-steroidal competitive inhibitor of androgens at the testosterone receptor.

-Used in prostate carcinoma

Front 6

-Ketoconazole

Back 6

Ketoconazole inhibits steroid synthesis, by inhibiting 17,20-desmolase

Front 7

-Spironolocatone

Back 7

Spironolactone inhibits steroid binding, 17-alpha-hydroxylase, and 17,20-desmolase.

-Ketoconazole and spironolactone are used in the treatment of polycystic ovarian syndrome to prevent hirsutism.
-Both have side effects of gynecomastia and amenorrhea.

Front 8

Leuprolide

Back 8

Leuprolide is a GnRH analog with agonist properties when used in pulsatile fashion (emulating physiologic GnRH secretion post-puberty).
-Vs. antagonist properties when used in continuous fashion (down regulates GnRH receptor in pituitary, causing decreased FSH/LH).

"Leuprolide can be used in lieu of GnRH)"

Use: infertility (pulsatile), prostate cancer (continuous – use with flutamide).
-Uterine fibroids (continuous), precocious puberty (continuous)

Tox: Antiandrogen, nausea vomiting

Front 9

Tamsulosin

Back 9

Tamsulosin is an alpha1-antagonist used to treat BPH by inhibiting smooth muscle contraction.

-Selective for alpha1A,D receptors (found on prostate), as opposed to vascular alpha1B receptors.

Front 10

Sildenafil, Vardenafil

"Fill the penis"

Back 10

Sildenafil and Vardenafil inhibit phosphodiesterase 5, causing increased cGMP, smooth muscle relaxation in the corpus cavernous, increased blood flow, and penile erection.

Used to treat erectile dysfunction.

Tox: "Hot and sweaty," then headache, heartburn, hypotension.

-Headache, flushing, dyspepsia, impaired blud-green color vision.
-Risk of life-threatening hypotension in patients taking nitrates.