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24 Cards in this Set

  • Front
  • Back
How's DHT formed
from Testosterone via 5alpha-reductase

Type I: non-genital
II: urogenital incl. prostate
How's E2 formed?
from T via CYP19 (aromatase)
Oral androgens
modified at 17 alpha position, relative weak


NOT that good.
Injectable androgens
modified at 17 beta position to prolong absorption
Testosterone enanthate
transdermalmost often used androgens.

HOWEVER, must alos give LH, FSH to induce spermatogenesis
21-hydroxylase, results in increase ACTH, which causes increase DHEA.

Tx goal is to supress DHEA by supression of ACTH with hydrocortisone with Neg inhibition on Pituitary gland.
Patches with androgen
Testoderm, androderm
Herediatary Angioedema and androgen???
imparied C1 esterase inhibitor, so overactive complement cascade > blood vessel permeability

Tx: DANAZOL AND STANOZOLOL. These, NOT THRU ANDROGEN ACTION, but via IRRITATION of liver cause hepatic synthesis of esterase inhibitor.
Other uses of androgens?
Anemia in males, AIDS related muscle wasting, Andropause (age related decrease in T).
Flutamide and Bicalutamide: Antiandrogens
Androgen receptor antagonist. This however, causes increase in LH secretion and increase in Testosterone, so must used with GnRH in combo to trt metastatic cancer.

Bicalutamide is LEAST TOXIC.
Cyproterone Acetate: anti-androgen
Weak antagonist at androgen receptor. Used for hirsutism in women.
Finasteride and Dutasteride
Block Type II 5 alpha reductase to prevent T to DHT coversion. For Tx of BPH and male patterened baldness (propecia).

Dutasteride blocks both Type I and Type II 5 alpha reductase.

May be used in combo with alpha blockers for BPH.
male psudohermaphroditism
Type II 5 alpha reductase deficiency, no DHT, so female phenotype
Androgen Insensitivity Syndrome
Testicular feminization, Androgen binding site mutation, so female external phenotype. Aromatase in mammary gland cause breast devp't.
Kennedy's Dz
And-R mutation, andr resistance.
17alpha ethinyl estradiol, Equilin
17alpha modified

Equilin is from equine, conjugated with SO4 to avoid first pass metabolism in liver.
E2 tx reduces what?
reduces bone absorption (increase bone mass), lipoprotein profile, vasodilation, atherosclerosis are all reduced.
E2 increases what?
Ethinyl estradiol/norethindrone acetate
E2-Prog com HRT., studeny halted due to Increase risk of Heart attack, Stroke, blood clots, breast cancer.
What to use for osteoporosis if ERT is not so good?
use alendronate instead.
partial antagonist and agonist actions on ERs.

Antag at breast, Agonist at endometrium and bone. Protects from osteoporosis but increased risk of THROMBOSIS.
Tamoxifen: trans vs. cis
Trans is anti-estrogenic, cis is estrogenic

Trans isomer marketed for breast cancer
partial agonist at bone and antagonist at breast and endometrium

protects bones, No endometrial prolif unlike tamoxifen
Aromatase inhibitor, for tx of breast cancer. Produces hot flashes, but no increase in risk of uterine cancer or thrombosis.