[PHARM] Male Hormones part 2

• GnRH analogs (goserelin, nafarelin, buserelin, leuprolide acetate) produce effective gonadal __________ when blood levels are continuous rather than pulsatile

• stimulation

• suppression

Steroid Synthesis Inhibitors

• Inhibitor of adrenal & gonadal steroid synthesis w/o affecting ovarian aromatase but reduces human placental aromatase activity

• Displaces estradiol and dihydrotestosterone from sex hormone binding protein in vitro and increases the estradiol:testosterone ratio

• Ketoconazole

• Abriterone

• Finasteride

• Dutasteride

Steroid Synthesis Inhibitors

Adverse Effects:

• Reversible Gynecomastia due to increase in estradiol: testosterone ratio

• Not useful in women with increased androgen levels because of associated toxicity with prolonged use of the required dose

• Ketoconazole

• Abriterone

• Finasteride

• Dutasteride

Streoid Precursors to Androgens Inhibitors

• 17α-hydroxylase inhibitor

• For metastatic prostate CA

• Ketoconazole

• Abriterone

• Finasteride

• Dutasteride

Streoid Precursors to Androgens Inhibitors

• 5α-reductase inhibitor

• For reduction of prostate size in men with BPH

• For hirsutism in women

• For early male pattern baldness in men

• Ketoconazole

• Abriterone

• Finasteride

• Dutasteride

Steroid Precursors to Androgens Inhibitors

• Orally active enzyme inhibitor that decreases dihydrotestosterone levels

• Effect starts within 8 hours and lasts after 24 hrs

• Excreted in feces

• Not approved for use in women or children

• Ketoconazole

• Abriterone

• Finasteride

• Dutasteride

Steroid Precursors to Androgens Inhibitors

• For treatment of BPH

• Orally active steroid derivative with a slow onset of action and much longer half-life

• Not approved for use in women or children

• Ketoconazole

• Abriterone

• Finasteride

• Dutasteride

Receptor Inhibitors

• For management of prostatic carcinoma who have not had prior endocrine therapy

• May be useful in managing excessive androgen synthesis in women

• Flutamide

• Bicalutamide, Nilutamide, & Enzalutamide

• Cyproterone & Cyproterone acetate

• Spironolactone

Receptor Inhibitors

• Although not a steroid, it behaves like a competitive antagonist at the androgen receptor

• Often causes mild gynecomastia & mild reversible hepatic toxicity

• Flutamide

• Bicalutamide, Nilutamide, & Enzalutamide

• Cyproterone & Cyproterone acetate

• Spironolactone

Receptor Inhibitors

• Management of metastatic carcinoma of the prostate

• Potent orally active antiandrogens that can be administered as a single daily dose

• Flutamide

• Bicalutamide, Nilutamide, & Enzalutamide

• Cyproterone & Cyproterone acetate

• Spironolactone