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    Androgen Pharmacology

    Uploaded by

    Sri Nurliana Basry
    This document summarizes key information about androgen pharmacology. It discusses how testosterone primarily circulates bound to sex hormone binding globulin or albumin in the blood. About 4% of testosterone is converted to DHT in tissues like the prostate and fat. Testosterone levels peak during fetal development, at birth, and during puberty to stimulate development of male reproductive organs and secondary sex characteristics. Androgens like testosterone and DHT decline with age starting in the 20s. Various topical gels and patches can be used to deliver testosterone transdermally. Antiandrogens like flutamide and nilutamide work by blocking the androgen receptor to suppress testosterone activity.

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    Androgen Pharmacology

    Uploaded by

    Sri Nurliana Basry
    51 views10 pages
    This document summarizes key information about androgen pharmacology. It discusses how testosterone primarily circulates bound to sex hormone binding globulin or albumin in the blood. About 4% of testosterone is converted to DHT in tissues like the prostate and fat. Testosterone levels peak during fetal development, at birth, and during puberty to stimulate development of male reproductive organs and secondary sex characteristics. Androgens like testosterone and DHT decline with age starting in the 20s. Various topical gels and patches can be used to deliver testosterone transdermally. Antiandrogens like flutamide and nilutamide work by blocking the androgen receptor to suppress testosterone activity.

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    This document summarizes key information about androgen pharmacology. It discusses how testosterone primarily circulates bound to sex hormone binding globulin or albumin in the blood. About 4% of testosterone is converted to DHT in tissues like the prostate and fat. Testosterone levels peak during fetal development, at birth, and during puberty to stimulate development of male reproductive organs and secondary sex characteristics. Androgens like testosterone and DHT decline with age starting in the 20s. Various topical gels and patches can be used to deliver testosterone transdermally. Antiandrogens like flutamide and nilutamide work by blocking the androgen receptor to suppress testosterone activity.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    51 views10 pages

    Androgen Pharmacology

    Uploaded by

    Sri Nurliana Basry
    This document summarizes key information about androgen pharmacology. It discusses how testosterone primarily circulates bound to sex hormone binding globulin or albumin in the blood. About 4% of testosterone is converted to DHT in tissues like the prostate and fat. Testosterone levels peak during fetal development, at birth, and during puberty to stimulate development of male reproductive organs and secondary sex characteristics. Androgens like testosterone and DHT decline with age starting in the 20s. Various topical gels and patches can be used to deliver testosterone transdermally. Antiandrogens like flutamide and nilutamide work by blocking the androgen receptor to suppress testosterone activity.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    of 10

    Androgen Pharmacology

    Monday, September 29, 2008


    8:51 AM

    KNOW THE ONES IN BLUE

    PHA 551 Endocrine Page 1

    Primarily circulating in the bound to the hormone "SEX HORMONE BINDING GLOBULIN" (SHBG) <high affinity, low capacity>
    Also binds to albumin, transcortin, and alpha-1 acid glycoprotien (all to lesser extent) <low affinity, high capacity>

    DHT

    About 4% is converted to DHT - very potent - much happens in the prostate


    Conversion of testosterone (by aromatase) happens a lot in the fat

    This makes up the majority of the estrogens found in the male circulation

    Some conversion of testosterone to estrogen in the brain

    Epitestosterone is an unnatural inactive metabolite - know someone is taking extra testosterone if you
    find this in their circulation

    PHA 551 Endocrine Page 2

    Heat shock proteins =


    chaperone proteins

    3 peaks of testosterone levels


    Fetal
    Neonatal
    Puberty

    Where male reproductive track


    develops from

    Testosterone leads to development of internal genitalia


    Conversion of testosterone to DHT stimulates development of external genitalia

    Usually complete by the tome the infant is one month of age

    Stimulating testicular growth


    Increased testicular SIZE
    Stimulates Sertoli cells - seminiferous tubule development
    Once developed, spermatogenesis begins

    PHA 551 Endocrine Page 3

    Causes further enlargement of genitalia - by the time they're 20 yoa there is an 8 fold increase

    Serum testosterone levels ~ 500-700 ng/dL

    Testosterone and DHT levels begin to decline


    See male pattern baldness due to decrease in testosterone THIS STATEMENT

    IS INCORRECT

    By age 80, testosterone levels decrease to < 40% of early adulthood levels
    Increased ratio of SHBG to testosterone
    Leads to decreased free testosterone levels

    PHA 551 Endocrine Page 4

    Many are esthers - following injection, get slow hydrolysis of the ester groups - gives prolonged
    release of testosterone

    PHA 551 Endocrine Page 5

    Testoderm - applied to scrotal skin (very thin there - don't need any type of chemical adjuvant to help get it in
    the skin
    Testoderm TTS and Androderm - can be applied to non-scrotal skin - thicker skin - has chemical adjuvants to
    help deliver the testosterone
    Topical testosterone gels - (T-gels) - Androgel and Testim -

    PHA 551 Endocrine Page 6

    Block testosterone from binding - no activity at receptor

    NILUTAMIDE

    Extensive hepatic metabolism


    Hydroxyflutamide - active metabolite
    There is Also an active metabolite of nilutamide - long half life as well (2.5-5 DAYS)

    PHA 551 Endocrine Page 7

    Increase in FSH and LH - initially - then it settles down to "major effect"

    Sustained supression of GnRH - levels eventually leads to testosterone levels that were equivalent
    to being castrated!
    Also see regression of secondary sex organs - prostate, etc.

    PHA 551 Endocrine Page 8

    These active metabolites contribute to the length of activity of these drugs

    PHA 551 Endocrine Page 9

    PHA 551 Endocrine Page 10

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