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INHIBITORS (UROLOGIC)
BY DR. LEONARDO A. TORRES, FPSECP, FPSP, FPSA, RBA-ABI
FORMER CHAIR , REVIEWER AND FACULTY
UPH-DJGTMU, PLM, AUP, CEU
GONADAL HORMONES - INHIBITORS
ANDROGENS
DIHYDROTESTOSTERONE - POTENT
DIHYDROEPIANDROSTERONE (DHEA) – ADRENAL
ANDROGENIC / ANABOLIC
TESTOSTERONE IM/TOP. P, E, U, C 1 : 1
METHYLTESTOSTERONE PO/SL 1 : 1
FLUOXYMESTERONE PO 1:2
OXYMETHOLONE 1:3
OXANDROLONE 1 : 3 - 1:13
NANDROLONE 1 : 2.5 -1: 4
REVIEW OF PHYSIO. - ANDROGENS
• SERTOLI CELLS: Mullerian duct inhibitory factors:
• ( INHIBIN AND ACTIVIN ) – FSH-r
• TESTOSTERONE: ADULT MEN = 8 MG. OD
• PLASMA LEVELS IN MALE = 0.6 mcg./dL.
• Plasma level in women = 0.03 mcg./dL.
• DHEA / S : ( - ) ATHEROSCLEROSIS / SLE
• GROWTH-PROMOTING EFFECTS: SEXUAL, LEAN
• BODY MASS, HAIR GROWTH, SEBUM, EPO,
• ( - ) HDL ( + ) LDL
• MOA: INTRACELLULAR PROTEIN S. DNA-RNA
CLINICAL USES OF ANDROGEN
• HRT – HYPOGONADISM CAUTION: HPN, Polycythemia
• GYNE.: Breast engorgement, Endometriosis, Post-
• menopausal, Breast tumors
• Protein-Anabolic agents: Trauma, Surgery, Debilitating d.
• Anemia: Refractory replaced by EPO-recombinant
• Osteoporosis: replaced by Bisphosphonates
• Growth Stimulators: delayed puberty X acc. Epi. Closure
• Anabolic steroid in Sports: X (Strength, Performance,Aggre)
• Aging: ( + ) lean body mass, Ht, ( - ) bone resorption
• ADR/S: Hirsutism, Acne, Na Retention, Hepatic d., BPH,
• Gynecomastia, Azoospermia, Erythrocytosis, HepatoCA.!
GONADAL HORMONES-INHIBITORS
ANTI-ANDROGENS
KETOCONAZOLE - STEROID-INHIBITOR (ANTI-GLUCOCORTICOID)
FINASTERIDE - 5-A-REDUCTASE-INHIBITOR- Hypospadias in male fetus- Terato.
DUTASTERIDE - “ LONG t ½ + TAMSULOSIN ( COMBINED)- BPH
CYPROTERONE Ac. - RECEPTOR-INHIBITOR (OCP) – NOT RELIABLE
ABIRATERONE – NEW ANTI-17-HYDROXYLASE - RPrCA
FLUTAMIDE - COMPE.ANDROGEN ANTAGONIST
BICALUTAMIDE + GnRH ( - ) TUMOR FLARE
NILUTAMIDE - SURGICAL CASTRATION
SPIRONOLACTONE - ANTI-ALDOSTERONE / (-) 17-A-HYDROXYLASE
MALE CONTRACEPTION
GOSSYPOL - Hypokalemia ( MAJOR ADR )
GnRH-ANTAGONIST + TESTOSTERONE
IM TESTOS. ENANTHATE + L-NORGESTREL PO OD = AZOOSPERMIA