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44 Cards in this Set

  • Front
  • Back
what is the role of DHT?
testosterone is a prohormone for DHT
effects of DHT
what are general effects of structure on function of testoterones?
what is primary testicula failure and how is it treated?
what is secondary testicular failure and how is treated?
lab testing for testostone, FSH, LH etc
controversy of steroids in athletes
male menopause treatment and controversy?
side effects of testosterones
treatement for over production of androgen
effect of long acting GnRH analogs/
5alpha recutase inhibitor
effective in benign prostate hyperplasia

other stuff?
male contraceptives
1. Describe the sources of anabolic/androgenic hormones.
a. In males the androgens are synthesized in the testes and adrenal cortex.
b. In females the androgens are synthesized in the ovaries and adrenal cortex.
How are anabolic steroids synthesized?
c. For synthesis of androgens from cholesterol, functioning 17-hydroxylase and 3-hydroxysteroid dehydrogenase are needed (also cholesterol desmolase and 17,20-desmolase). Adrostenedione is synthesized in the adrenal cortex (zona reticularis) and converted to testosterone in the testis.
what regulates secreation of androgens?
d. Gonadotropin releasing hormone is secreted by the hypothalamus and causes release of leutenizing hormone and follicle stimulating hormone from the pituitary. LH and FSH work on the testis to stimulate testosterone production and spermatogenesis. Testosterone gives negative feedback to the hypothalamus and pituitary to suppress GnRH and LH/FSH secretion, respectively.
2. Define the roles of LH and FSH on gonadal function. Define the importance of androgens for sexual differentiation and puberty.
a. Prior to puberty testosterone levels are low. At puberty, LH secretion increases and stimulates testosterone production in the testes (Leydig cells produce testosterone). Testosterone is required for spermatogenesis.
b. Follicle stimulating hormone binds to Sertoli cell receptors in the testes and stimulates spermatogenesis. Once this occurs, spermatogenesis can be maintained by adequate levels of testosterone.
c. In addition to the increase in testosterone that occurs at puberty, there are surges of testosterone during certain periods of gestation and infancy. The first surges of testosterone are important for development of primary sex characteristics (reproductive organs). The second surge during puberty induces the development of secondary sex characteristics (masculinization).
androgens have what two effects?
a. Androgens have anabolic and androgenic effects. The androgen effects include the production of masculine characteristics. The anabolic effects include overall body growth, including increased protein synthesis and decreased protein breakdown.
what is relation of testosterone to DHT?
b. In most tissues, testosterone serves as a prohormone. Many tissues contain 5-reductase, which catalyzes the conversion of testosterone to dihydrotestosterone (DHT). The cytosolic androgen receptor exhibits a higher affinity for DHT than testosterone, and the DHT-receptor complex is more readily transported to the nucleus than the T-receptor complex

c. In the hypothalamus and pituitary, testosterone is the active steroid and is responsible for feedback inhibition.
what are the causes of primary hypogonadisM
b. Primary causes include genetic/chromosomal causes (i.e. Klinefelters syndrome) and direct damage to Leydig cells or seminiferous tubules.
what is the level of testerone and gonadotrpin in primary hypodandism?
gonadotropin - high

what is used to treat primary hypogonadism?
enanthate or cypionate
what are enanthate and cypionate?
long acting testoserone esters
c. Secondary testicular failure is due to ?
lack of gonadotropins. This again may be a genetic abnormality (i.e. Prader-Willi syndrome) or may be due to hypopituitarism or decreased hypothalamus release of GnRH.
in secondary hypogonadism what will testerone and gonadotropin levels be?

how is secondary hypogonadism treated?
ii. Treatment should include treating the underlying cause of the hypogonadism if possible. Gonadotropins have been used, and adrogens are not added until the time of normal puberty. You want to slowly increase to mimic the normal surge of testosterone
i. Symptoms of high androgen levels (exogenous or endogenous) include:
1. Virilizing effects in adolescent males and females – acne, hirsuitism, male pattern baldness, coarsening of the voice
2. Inhibition of spermatogenesis
3. Feminizing effects because testosterone is converted to an estrogen by aromatase enzymes in peripheral tissues.
4. Hepatic abnormalities – cholestatic hepatitis, hepatic adenocarcinoma
5. Changes in lipoprotein profiles (decrease HDL, increase LDL)
6. Increase in aggressive behavior (roid rage) can cause psychotic symptoms
ii. Some situations in which suppression of androgens would be favorable include
1. Male pattern baldness
2. Virilizing syndromes in women (i.e. hirsutism)
3. Acne
4. Hyperplasia and carcinoma of the prostate
5. Male contraception
iii. Hypergonadism can be treated by
androgen suppression, inhibitors of androgen synthesis, 5-reductase inhibitors, and androgen receptor antagonists.
c. The effects of androgens on increasing muscle mass is controversial. ?
i. They are effective when used to counter muscle wasting due to various causes, such as muscle wasting due to anti-inflammatory steroid use. They induce a positive nitrogen balance in hypogonadal individuals.
ii. Use by athletes with normal gonadal function has not been proven to reliably increase muscle mass. There is often an increase in muscle mass seen in these individuals, but this may be due to increased aggressiveness leading to a greater training limit, rather than the steroids actually causing more muscle to form.
iii. Increased muscle mass is seen in well-trained athletes who use these, but not in a normal male.
iv. There may be a more beneficial effect in females
v. Double-blind studies have yielded both positive and negative results regarding use of androgens to increase muscle mass.
5. Describe the rationale for the clinical uses of anabolic/androgenic hormones in: anemia
b. Androgens stimulate RBC development, both directly and indirectly. They stimulate the synthesis of erythropoietin by the kidney (indirectly increasing RBC production) and also directly stimulate elements in the bone marrow causing stem cell differentiation. Because of these effects, androgens are useful in treating various anemias.
6. Compare the routes of administration, absorption, and relative duration of action of synthetic androgens and testosterone.
a. Testosterone is a poor drug. It exhibits a high first pass effect when given orally. When injected, it is rapidly absorbed and metabolized. It also has mixed anabolic and androgenic effects that cannot be separated out.
b. Synthetic manipulation of testosterone seeks to solve these problems.
i. Type B manipulation: 17 substitution (methyltestosterone)
ii. Type C manipulation: ring alteration (mesterolone)
iii. Type B and Type C manipulation allows drugs to be orally active. These drugs are not metabolized to testosterone proper. They can cause liver toxicity and liver cancer.
iv. Type A manipulation: 17 esterification (enanthate or cypionate)
1. This modification causes absorption of the drugs to be greatly delayed. They are injected weekly or monthly and are metabolized to testosterone proper.
v. Most preparations involve combinations of type AC or type BC changes.
what are the type B and C manipulations of testostoner?

mesterolone-type C
what is use/problems of Type B and C?
iii. Type B and Type C manipulation allows drugs to be orally active. These drugs are not metabolized to testosterone proper. They can cause liver toxicity and liver cancer.
what are the type A manipulations of testosterone?
enanthate or cypionate
what is use of type A manipulations
1. This modification causes absorption of the drugs to be greatly delayed. They are injected weekly or monthly and are metabolized to testosterone proper.
how are most preparations of synthetic androgens done?
v. Most preparations involve combinations of type AC or type BC changes.
7. Describe the adverse effects of androgens/anabolic steroids when used in males and females
a. Side effects of high androgen levels:
i. Virilizing effects: acne, hirsutism, male pattern baldness, coarsening of the voice.
ii. Inhibition of spermatogenesis
iii. Feminizing side effects
iv. Hepatic abnormalities, including hepatocellular carcinoma
v. Changes in lipoprotein profiles (decrease HDL and increase LDL)
vi. Increase in aggressive behavior
. Correlate the hepatotoxicity of certain androgens/anabolic steroids with their chemical structure.
b. High, prolonged doses of drugs that have a 17 substitution or a ring alteration can cause liver toxicity and hepatocellular carcinoma. (types B and C)
what are the drugs used for androgen suppression
GnRH long acting- constant GnRH is inhibitory instead of stimulating

ketoconazole-blocks androgens synthesis at super high levels(higher than used in corticosteroid blocking) only mildly effective will lead to adrenal hyperplasia to overcome

finasteride- 5alphareductase inhibitor

cyproterone acetate/flutamide-androgen receptor blockers

androgen receptor blockers/5alphareductase inhibitors are both used in prostate cancer.
what is gossypol?
destroys seminefarious tubules inhibits speratogenesis also decreases sperm motility
levels in semineforous tubule disease?
high FSH
normal LH
low T
levels in leydig cell failure?
normal FSH
High LH
low T