Androgens & Antiandrogens. The testis has two major functions: 1. Spermatogenesis occurring within the seminiferous tubules 2. Production of androgenic.

Slides:



Advertisements
Similar presentations
GnRH, LH, FSH.
Advertisements

Number of Nuclear Positions and Steroid Classification
Male Reproductive Function Anatomy Hormonal Control Pathophysiology.
Hormonal Control of Reproduction in the Male. Dr. M. Alzaharna (2014) Spermatogenesis Spermatogenesis goes on continuously from puberty to senescence.
Male and Female Reproductive System Review MARIEL ARVIZU, MD DOCTOR OF SCIENCE CANDIDATE NUTRITION DEPARTMENT HARVARD SCHOOL OF PUBLIC HEALTH.
Pharmacology in Nursing Men’s Health Drugs
Mosby items and derived items © 2011, 2007, 2004 by Mosby, Inc., an affiliate of Elsevier Inc. CHAPTER 35 Men’s Health Drugs.
Gonad Hormones : Male Prof.Dr.Gülden Burçak
Female Sex Hormones (Estrogens and Progestins)
The Reproductive System
IB Chemistry Opt B Human Biochemistry B6 Hormones.
Gonadal Hormones & Inhibitors
Androgens agonists and antagonists. What are androgens ? Steroid derived from cholesterol found in males and females Androgens produced by testes: 1.Testesterone.
ESTROGENS AND ANDROGENS
Drugs affecting reproductive system
Chapter 37 Sex Hormones. Copyright 2007 Thomson Delmar Learning, a division of Thomson Learning Inc. All rights reserved Sex Hormones Endocrine.
By Lennart Nilsson, 1965.
Reproductive Hormonal Pharmacology Douglas Danforth, Ph.D. The Ohio State University.
SEX HORMONE THERAPY Anti-progestogens Mifiproston RU 486 : 19 nor testosterone derivative with different side chains. It has strong affinity for progestogen.
SEX HORMONES ผศ. พญ. มาลียา มโนรถ. Sex Hormones F 21 carbon : progestin F 19 carbon : androgen F 18 carbon : estrogen.
Human Endocrine Physiology February 27, 2014.
Adrenal Androgens Dr. Eman El Eter.
Estrogens & Antiestrogens. Menstrual cycle... Changes and hormonal events Menstrual cycle... Changes and hormonal events Natural estrogens: Natural estrogens:
1 Male Reproductive System. 2 Basic Anatomy Testes (gonads) Encased within scrotum and stored outside body Scrotum expands and contracts to heat and cool.
Androgens & Antiandrogens Munir Gharaibeh, MD, PhD, MHPE Faculty of Medicine The Jordan University April 2014.
1 Practice Questions Diuretics. Pharmacology Practice Questions 1 - An 80-yr old woman with a history of acute MI & CHF presents to the ER Dept with a.
Drugs affecting reproductive system Basic & Clinical Pharmacology.
Male Reproductive Physiology GUYTON & HALL, Chapter 80
Androgenic Steroids Overall Organization of the Topic
Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Chapter 65 Androgens.
414 PHG Substance of abuse.  By the end of this lectures the student should be able to:  Discuss the source and sythesis of anabolic hormones  Explain.
Adrenal Androgens.
Steroid Hormones.
Male sex hormones Androgens Types: 1.Natural androgens: – Androsterone and testosterone 2.Synthetic androgens: – Testosterone propionate. – Anabolic.
HORMONES OF THE GONADS. The gonads are bifunctional organs that produce germ cells and the sex hormones. The ovaries produce ova and the steroid hormones.
Male Reproduction Felix E. Grissom, Ph.D Numa P.G. Adams
Estrogens and Androgens
Oral Contraceptives Estrogen and Progestin. 2 Hormonal contraceptives Hormonal contraceptives contain either a combination of an estrogen and a progestin.
The Gonadal Hormones & Inhibitors By S. Bohlooli, PhD School of Medicine, Ardabil University of Medical Sciences.
Steroids Sex (Gonadal) Hormones Agonist & Antagonists 8 أ.م.د. وحدة اليوزبكي Head of Department of Pharmacology- College of Medicine- University of Mosul-
Androgens Also called androgenic hormone or testoid
Gonads:- According to both sexes, the gonads are two: Ovaries (female) secrete: –P–Progesterone –O–Oestrogen: It is the end product that can control secretion.
Testosterone Dr. Hazrat Bilal Malakandi DPT (IPMR KMU), MSPT* (KMU)
Anticancer drugs: chemotherapy. Hormonal treatment  Hormone-receptor positive (hormone dependent) forms of breast, prostate and ovarian cancer are subject.
Male sex hormones By Akrum Hamdy. Male sex hormones Androgens Synthesis& secretion Regulation Pharmacological actions Pharmacokinetics Preparations Therapeutic.
Hormones of Testes - Testosterone Lecture NO: 2nd MBBS
GnRH, LH, FSH.
DRUGS USED IN MALE INFERTILITY.
HORMONES OF THE GONADS.
Drugs for Men’s Health and Reproductive Disorders
DRUGS USED IN MALE INFERTILITY.
The gonadal hormones and inhibitors
DRUGS USED IN MALE INFERTILITY.
Male hypogonadism.
GnRH, LH, FSH.
Estrogens & Antiestrogens
Testicular Physiology
Chapter 65 Androgens 1.
Text Only in Females’ slide Only in Males’ slides Important Numbers
Androgenic Steroids Overall Organization of the Topic
Principles of Pharmacology The Pathophysiologic Basis of Drug Therapy
Androgenic Steroids Overall Organization of the Topic
Male Reproductive System
Hormonal Control of Reproduction in the Male
Drugs affecting reproductive system
Reproductive pharmacology
Androgenes and Antiandrogenes
Anjanette Acosta Physiology 3
Androgenes and Antiandrogenes
The Pharmacology of Androgens
Presentation transcript:

Androgens & Antiandrogens

The testis has two major functions: 1. Spermatogenesis occurring within the seminiferous tubules 2. Production of androgenic hormones

Naturally occurring androgenic hormones are: 1. Testosterone, the principal androgenic hormone produced by the Leydig cells of testis. 2. Dehydroepiandrosterone (DHEA) (Adrenal cortex produces DHEA) 3. Androstenedione The testes produce other hormones like 1) Small quantities of Estradiol 2) Inhibin and 3) Activin

Testosterone synthesis Testosterone synthesis From cholesterol DE Deh DE Deh Cholesterol Pregnenolone Progesterone Hyd Hyd Testosterone Androstenedione Hydroxyprog. 5α-reductase 5α-reductase 5α-dihydrotestosterone 5α-dihydrotestosterone

Androgens and anabolic steroids Testosterone is the natural androgen GnRH GnRH - ↓ - ↓ LH; FSH LH; FSH - ↓ - ↓ Testosterone; spermatogenesis Testosterone; spermatogenesis

Transport & MOA of androgens: Transport & MOA of androgens: SHBG SHBG 5α-reductase 5α-reductase Testosterone 5α-dihydrotestosterone (sex organs) Testosterone 5α-dihydrotestosterone (sex organs) (skeletal muscles) (skeletal muscles) cytosloic; nuclear receptors increase transcription of a specific protein androgen effects cytosloic; nuclear receptors increase transcription of a specific protein androgen effects DHT is 10 times more potent than testosterone and mediates effects of testosterone on skin and sexual apparatus (prostate; DHT is 10 times more potent than testosterone and mediates effects of testosterone on skin and sexual apparatus (prostate; seminal vesicle, epididymis…)

Testosterone physiological & pharmacological effects: Testosterone physiological & pharmacological effects: - Virilizing=masculinizing effect 1° & 2° sexual characteristics 1° & 2° sexual characteristics - ↑ Spermatogenesis - ↑ Erythropoiesis - Anabolic or growth promoting effect (bone; skeletal muscles)

Testosterone metabolism: Testosterone metabolism: Androsterone Androsterone Hepatic → 17-ketosteroids Etiocholanolone Etiocholanolone Clinical uses: Clinical uses: - Testosterone deficiency Hypogonadism; impotency; ↓ libido; aging; infertility… Hypogonadism; impotency; ↓ libido; aging; infertility… - Anemia; leukemia; lymphoma - Endometriosis (Danazol is particularly used)

Cont. Testosterone clinical uses, - Antiestrogenic effect Breast cancer Breast cancer - Anabolic effect Osteoporosis Osteoporosis ** Use by athletes is an abuse

Testosterone preparations: Testosterone preparations: 1° use for androgen replacement: - Testosterone I.M; S.C - Testosterone propionate I.M, S.L - Testosterone cypionate I.M; depo I.M - Methyltestosterone O; S.L - Fluoxymestrone O 1° use for breast cancer: Testolactone (progesterone derivative and aromatase inhibitor) O

Cont. testosterone preparations, 1° use for anabolism (osteoporosis): Androgen:anabolic ratio=1:2 or 1:3 ( Androgen:anabolic ratio=1:2 or 1:3 (promote + ve anabolism and muscular growth but little effect on sex) - Ethylestrenol O - Stanozolol O - Oxandrolone O - Nandrolone decanoate I.M - - Methandienone O

Testosterone side effects: Testosterone side effects: - Virilization (masculinization) Hirsutism; acne; menstrual disorders in ♀’s - Precocious puberty & hirsutism in children - Salt & water retention - Jaundice; gall bladder stones (methyltestosterone) - Enlargement of prostate - ? Liver cancer

Antiandrogens Antiandrogens - Estrogens: Diethylstilbesterol; mestranol... - Progestins: Cyproterone acetate - GnRH superagonists (Leuprolide acetate); GnRH antagonists (Ganirelix) Pro-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly Pro-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly - Flutamide; B - Flutamide; Bicalutamide and Nilutamide - 5α- reductase inhibitors: Finasteride - Ketoconazole - Spironolactone - Gossypol

Antiandrogens clinical uses: Antiandrogens clinical uses: - Ca prostate - Benign hyperplasia of the prostate (Finasteride) - Severe acne and hirsutism in ♀’s (Spironolactone; Cyproterone acetate) - Precocious puberty - ♂ antifertility agents (♂ contraceptive) (Gossypol) - ♂ baldness (Cyoctol - ♂ baldness (Cyoctol=topical antiandrogen; Finasteride) Antiandrogens side effects: Antiandrogens side effects: ↓ libido; impotency; ↓ spermatogenesis; ↓ ejaculate