Testosterone & Antitestoterones(7)

MALE SEX HORMONES: BY DR.UMA KADAM M.B.B.S. MD ASSOCIATE PROFESSOR PHARMACOLOGY SKNMC DR.UMA K.

Male sex hormones ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],DR.UMA K.

Androgens: ,[object Object],[object Object],[object Object],[object Object],DR.UMA K.

DR.UMA K. Estriol Estrone Cholesterol Pregnenolone Progesterone 17- α - Hydroxy pregnenolone 17- Hydroxy progesterone Dehydro-epi androsterone Andro-stenedione TESTOSTERONE ESTRADIOL Aromatase Aromatase Corticosteroids Corticosteroids DHT 5  -reductase

DR.UMA K. Testes Leydig Cells Sertoli Cells Negative feedback Estradiol Inhibin Negative feedback FSH Negative feedback Testosterone LH LH & FSH HYPOTHALAMUS ENDOCRINE FACTORS Pituitary GnRH Regulation of secretion

[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],Regulation of secretion: DR.UMA K.

Mechanism of action of steroid hormones ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],DR.UMA K.

DR.UMA K. MECHANISM OF ACTION: T DHT DHT- R T- R R R T- R Nucleus 90% 10% 5-  -reductase Cytoplasm

DR.UMA K. ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

Actions of Testosterone & DHT : ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],DR.UMA K. ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

Pharmacokinetics: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],DR.UMA K.

DR.UMA K. Testosterone Preparations Dose Testosterone aqueous suspension 50-100mg / 2 weeks ,[object Object],[object Object],[object Object],[object Object],[object Object],25-50 mg / 3 times a week 40-60mg / 1 or 2 week 100 – 200mg / 2 weeks 250 mg / 2 weeks ,[object Object],[object Object],[object Object],[object Object],Transdermal patches 2 patches /day (back, abdomen, thigh) Implants wall of abdomen/thigh

Clinical uses of testosterone: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],DR.UMA K.

DR.UMA K. Adverse effects of testosterone: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

Anabolic steroids….. DR.UMA K.

DR.UMA K. Anabolic Steroids Drug Anabolic Androgenic ratio Preparation & Dose Methandienone 3:1 5 – 15 mg/day, p.o. Nandrolone phenylpropionate 3:1 10 – 50 mg/wk, i.m. Nandrolone decanoate 3:1 25 – 50 mg/3 wk, i.m. Stanozolol 3:1 2 - 6 mg/day, p.o. Ethyloestrenol 3:1 8 - 16 mg/day, p.o. Oxandrolone 3:1 5 – 10 mg/day, p.o. Fluoxymesterone 3:1 5 – 10 mg/day, p.o.

Uses of anabolic steroids ,[object Object],[object Object],[object Object],[object Object],[object Object],DR.UMA K.

Anti-androgens DR.UMA K. ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

Danazol DR.UMA K. ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],Side effects: Dose related Amenorrhea (High doses) Androgenic side effects

DR.UMA K. Cyproterone acetate: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

Flutamide: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],DR.UMA K.

DR.UMA K. Finasteride ,[object Object],[object Object],[object Object],[object Object],[object Object],5  reductase inhibitors Side effects: Loss of libido & impotence in 5 % pts . Also used for prevention of hair loss ,[object Object],[object Object],[object Object],[object Object]

DR.UMA K. Parasympathetic Sympathetic Acetylcholine Noradrenaline Hypothalamus ANS Muscarinic Receptors vasoconstriction Penile flaccidity Penile erection

DR.UMA K. Penile Erection Vasodilatation Muscarinic Receptors  Ca ++ ↑ NO GTP cGMP cAMP ATP ↑ VP AC GC 5’ GMP PDE V SILDENAFIL

Sildenafil: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],DR.UMA K.

Testosterone & Antitestoterones(7)

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