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31 Cards in this Set
- Front
- Back
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What locations does testesterone negatively feedback?
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The hypothalamus and the pituitary
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How is dihydrotestosterone formed and what are its functions?
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It is converted from testosterone by 5 alpha reductase; it is necessary for development of the male genitalia and is the active steroid in most tissues (except hypothalamus and pituitary)
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What is the action of testosterone at the hypthalamus and pituitary?
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It acts as negative feedback on GnRH and LH/FSH
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What is the function of testosterone in the CNS?
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facilitation of libido and sexual function as well as aggressive behavior
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What is the effect of testosterone on the hematopoietic system?
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direct stimulation of stem cells in the marrow
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What are the three main types of synthetic testosterone?
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Type A - testosterone esters (cypionate and enanthate)
Type B - Methyltestosterone Type C - Mesterolone |
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Which types of synthetic testosterone are orally active?
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Methyltestosterone (type B) and Mesterolone (type C) are orally active
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Which type of synthetic testosterone is NOT orally active?
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Testosterone esters such as enanthate and cypionate (type A)
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Why is testosterone not a good drug?
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1) high first pass effect
2) rapidly absorbed and metabolized 3) mixed anabolic and androgenic effect |
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Which synthetic testosterone is given as an injection?
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Type A (enanthate or cypionate)
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Which synthetic testosterone derivatives are metabolized to testosterone and which are not?
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Type B and C are NOT metabolized to testosterone but type A is.
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Which synthetic testosterone derivatives have a high risk of liver cancer?
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Type B and C
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What effect will a 17 alpha substitution have on testosterone and in what class will this be?
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A 17 alpha substitution will cause the drug to be orally active; it will be in the type B class (methyltestosterone)
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What effect will ring alterations have on testosterone and in what class would this drug be?
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A ring alteration will make the molecule orally active; it will be a type C drug (mesterolone)
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What effect will a 17beta esterification have on testosterone and in what class will this drug be?
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It will delay the absorption of the drug (must be given as injection); it will be a type A drug (testosterone ester such as cypionate and enanthate)
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What are the major uses of anabolic/androgenic steroids?
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1) Hypogonadism/primary testicular failure
2) Stimulation of erythropoiesis 3) hereditary angioneurotic edema 4) delayed growth in children 5) To counter muscle wasting |
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What is the drug of choice for primary testicular failure, and what are some examples of this failure?
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Long-acting testosterone esters such as enanthate or cypionate; Klinfelter's direct damage to Leydig cells
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In patients with secondary testicular failure, when are patients given androgens?
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At puberty
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How do androgens stimulate erythropoiesis?
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Both indirectly through stimulation of EPO in the kidney and directly by recruitment of stem cells
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Are androgens used in the treatment of aplastic anemia?
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No, they are contraindicated in aplastic anemia and cause hepatocellular carcinoma; CS-factors should be used instead
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What is the drug of choice in the treatment of hereditary angioneurotic edema?
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Danazol (type BC); it increases the synthesis of the inhibitor of C1
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Describe the pattern of growth stimulation mediated by synthetic androgens
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They cause a short term growth spurt with eventual epiphyseal calcification, which limits the growth
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How do anabolics help athletes gain muscle mass?
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The androgren effect allows them to push past their training limit
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What is the major concern in the abuse of anabolic/androgenic steroids?
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Liver Cancer
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Describe the most common side effects of high androgen levels
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1) Virilizing effects (adolescent males and females) - acne, male pattern baldness, hirsutism, coarsening of voice
2) inhibition of spermatogenesis - decreased LH and FSH 3) Feminizing effect - testosterone converted into estrogen, gynecomastia 4) changes in lipoprotein profiles (decreased HDL increased LDL) 5) Aggressive behavior |
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What are some scenarios where androgens would want to be suppressed?
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1) male pattern baldness
2) acne 3) virilizing syndromes in women 4) prostatic hyperplasia 5) male contraception |
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What drugs are long acting GnRH analogs and how do they work?
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Leuprolide acetate and Goserelin suppress testosterone production by acting as a continuous level of GnRH, which inhibits LH/FSH rather than stimulates their release
(Pulsatile GnRH required for LH/FSH release) |
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What is the mechanism of ketoconazole?
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It inhibits androgen synthesis by blocking the P450s; requires high doses and causes gynecomastia
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What drug is a 5alpha reductase inhibitor and for what is it used?
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Finasteride is a 5AR inhibitor used in benign prostatic hyperplasia and blocks hirsutism in women
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What drugs are androgen receptor antagonists and for what are they used?
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Cyproterone acetate and flutamide are used in women with excess androgen production and in advanced prostate carcinoma
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What is gossypol and what are its effects?
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It is a drug that destroys the seminiferous epithelium and does not effect endocrine function; it is reversible
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