Page 702 - First Aid for the USMLE Step 1 2020, Thirtieth edition [MedicalBooksVN.com]_Neat

658 SectioN iii RepRoductive ` REPRODUCTIVE—PHARmACOlOgy

Danazol

mECHANISm Synthetic androgen that acts as partial agonist at androgen receptors.
ClINICAl USE Endometriosis, hereditary angioedema.
ADVERSE EFFECTS Weight gain, edema, acne, hirsutism, masculinization,  HDL levels, hepatotoxicity, idiopathic
intracranial hypertension.

Testosterone, methyltestosterone
mECHANISm Agonists at androgen receptors.
ClINICAl USE Treat hypogonadism and promote development of 2° sex characteristics; stimulate anabolism to
promote recovery after burn or injury.

ADVERSE EFFECTS Masculinization in females;  intratesticular testosterone in males by inhibiting release of LH (via
negative feedback) Ž gonadal atrophy. Premature closure of epiphyseal plates.  LDL,  HDL.

Antiandrogens
Finasteride 5α-reductase inhibitor ( conversion of Testosterone 5α-reductase DHT (more potent).
testosterone to DHT). Used for BPH and
male-pattern baldness. Adverse effects:
gynecomastia and sexual dysfunction.
Flutamide, Nonsteroidal competitive inhibitors at androgen
bicalutamide, receptors. Used for prostate carcinoma.
apalutamide,
enzalutamide
Ketoconazole Inhibits steroid synthesis (inhibits 17,20
desmolase/17α-hydroxylase). Used in PCOS to reduce androgenic symptoms.
Spironolactone Inhibits steroid binding, 17,20 desmolase/17α- Both can cause gynecomastia and amenorrhea.
hydroxylase.

Tamsulosin α -antagonist used to treat BPH by inhibiting smooth muscle contraction. Selective for α
1 1A/D
receptors (found on prostate) vs vascular α receptors.
1B

Minoxidil

mECHANISm Direct arteriolar vasodilator.
ClINICAl USE Androgenetic alopecia (pattern baldness), severe refractory hypertension.

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