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ANTIANDROGENS.pptx
- 1. ANTIANDROGENS IN DERMATOLOGY DR PARNEET SIGHU PG JR 1 MMC&H DVL
- 2. ANDROGENS Substances which cause development of secondary sex characters.
- 4. NATURAL ANDROGENS MALES FEMALES TESTOSTERONE DHT DEHYDROEPIANDROS TERONE ANDROSTENEDIONE ESTRADIOL
- 5. ANDROGEN RECEPTORS ANTIANDROGENS • SPIRONOLACTONE • CYPROTERONE ACETATE • FLUTAMIDE • CIMETIDINE ANDROGEN INHIBITORS • FINASTERIDE • DUTASTERIDE • LEUPORIDE • NAFARELIN • KETACONAZOLE 5-a REDUCTASE INHIBITORS GnRH ANALOGUE BOTH • OCP • PROGESTINS
- 6. CIRCULATING ANDROGENS 1. AGA 2. HIRSUTISM 3. HIDRADENITIS SUPPURATIVE 4. ACNE
- 9. 1. SPIRONOLACTONE • ALDOSTERONE ANTAGONIST • Weak ANTIANDROGEN. • Competitively inhibits DHT activity. ACTIVE METABOLITE - CANRENONE ABSORPTION - FOOD INCREASES METABOLISM - LIVER EXCRETION - URINE AND BILE HALF LIFE - 12 hours DOSING 50-200 mg daily 100 mg is well tolerated Start at 25 or 50 mg slowly titrated
- 10. INDICATIONS FDA APPROVED ---- NIL OFF LABEL USES : HIRSUTISM Decreases growth rate and diameter of facial hair. FPHL ACNE HIDRADDENITIS SUPPARITIVA ALWAYS ADDOCP TO DECREASE RISK OF MENORRHAGIAANDTERATOGENECITY • Unless female is not sexually active. • Permanent sterilization. FEMINIZING OF DEVELOPING MALE GENITALIAS.
- 11. ADVERSE EFFECTS HYPERKALEMIA • If already has renal insufficiency • HIGH K CONTANING FOOOD Bananas, orange, tomatoes • DRUGS NSAIDs ACEI , ARB HEPARIN DROSPERINONE BP MONITORING SERUM K Baseline, With any increase in dose SERUM K
- 12. 2. PROGESTINS Synthetic Progesterone 1. TESTOSTERONE DERIVATIVES All have androgenic effect except DIENOGEST 2. PROGESTERONE DERIVATIVES Have no androgenic effect except MPA 1.ESTRANES (First generation) 2. GONANES 3. PREGNANES • NORETHISTERONE • NORETHINDRONE • ETHYNOLDIOL ACETATE • DIENOGEST • LEVONORGESTEROL • NORGESTREL • DESOGESTREL • GESTODENE • NORGESTIMATE • MEDROXYPROGESTERONE ACETATE (MPA) • CYPROTERONE ACETATE • CHLORMADINONE ACETATE
- 13. A) CYPROTERONE ACETATE Most potent antiandrogen. competitive inhibition of DHT for AR binding. Also has progestational activity Gonadotropin suppression decreased TESTOSTERONE 2mg CPA + 0.035 mg EE INDICATIONS: • AGA • HIRSUTISM • VIRILIZING SYNDROME
- 14. ALDACTONE YASMIN HYPERKALEMIA DROSPERINONE (SPIRONOLACTONE DERIVATIVE) HYPERKALEMIA
- 15. 3. CIMETIDINE DOSE : 400mg QID Binds to AR
- 16. 4. FLUTAMIDE NON STEROID ANTIANDROGEN. INHIBITS ANDROGEN UPTAKE. FDA APPROVED USES PROSTATE CANCER OFF LABEL USES HIRSUTISM DOSE – 250 mg TDS
- 18. TESTOSTERONE DIHYDRO-TESTOSTERONE (DHT) HAIR LOSS 5 -a REDUCTASE I 5 -a REDUCTASE II FACE FINASTERIDE FDA APPROVED USE • AGA IN MEN DOSE- 1mg daily OFF LABEL USES • AGA IN FEMALES 1 mg daily 5 mg daily • ACNE 5mg daily For 1 year • HIRSUTISM 5-7.5 mg daily For 6 months • HIDRADENITIS SUPPURATIVA 1-5 mg daily DUTASTERIDE 3 times more potent FDA APPROVED USE • BPH DOSE- 0.5 mg daily Gelatin Capsule OFF LABEL USES • AGA IN MALES 0.5 mg daily for 2 weeks 0.5 mg daily for twice week • ACNE • HIRSUTISM • HIDRADENITIS SUPPURATIVA
- 19. Why do the same drugs have the opposite effects? It's because hair follicles in each area of the body have evolved to respond to differently to different types of hormones. In women, when hair loss on the scalp is related to hormonal issues (androgenic alopecia), it may also be treated by the same types of drugs.
- 20. TOPICAL FINASTERIDE More effective ,as it lowers only local DHT, so less side effects . FINASTERIDE(0.25%) + MINOXIDIL(3%)>MINOXIDIL ALONE SIDE EFFECTS • BREAST ISSUES – GYNACOMASTIA • PROSTATE CANCER AGE > 55 years • SEVERE MYOPATHY • SEXUAL AND PSYCHIATRIC DYSFUNCTION DECREASED LIBIDO ERECTILE DYSFUNCTION DECREASE IN EJACULATE VOLUME • TERATOGENECITY CATEGORY X DRUG ALWAYS COUNSEL PATIENT TO: • EXAMINE FOR BREAST TENDERNESS, LUMP, PAIN • NOT TO DONATE BLOOD FOR ATLEAST ONE MONTH
- 21. 3.KETACONAZOLE MOA – Inhibits CY3A4 enzyme ( required for Steroid synthesis) antiandrogenic effect DOSE – 400-800 mg daily INDICATIONS • HIRSUTISM • AGA FORMULATIONS • Shampoo • Cream • Foam
- 23. 5 alpha reductase inhibitor Provides Nutritional support to prostate - also improves urinary function DOSE- 160 mg BD daily Capsule form For 24 months STINGING NETTLE AGA Inhibit 5-a Reductase GREEN TEA ZINC AZELAIC ACID METHANOL EXTRACT POLYPHENOLIC COMPOUNDS DRAWBACK– STRICT MANUFACTURING STANDARDS REGARDING PURITY / CONSISTENCY OF DRUG CONCENTRATION
- 25. THANKS