Please enable JavaScript.
Coggle requires JavaScript to display documents.
Androgens, ADRs:, Uses:, Testosterone preparations, Actions of both…
Androgens
Most important androgens are testosterone and dihydrotestosterone(DHT).
Less potent androgens include androstenidione and DHEA(dehydroepiandrostenidione).
Testosterone is converted to DHT by 5-alpha reductase and to estradiol by aromatase.
ADRs:
17-alkyl substituted compounds(methyltestosterone and fluoxymestane) are morely to cause cholestatic jaundice and peliosis hepatis.
Increased chances of acne, erythrocytosis, gynaecomastia and azoospermia.
Androgens are contraindicated in pregnant females, infants, carcinoma of the male breast and prostate and patients with cardiac and renal diseases.
Long term oral therapy is associated with liver adenomas and carcinomas.
Polycythemia and hypertension due to erythropoietic action may be a problem.
Masculinising actions(hirsutism, amenorrhea, clitoral enlargement and deepening of voice in females).
Increased risk of atherosclerosis due to decrease in HDL and increase in LDL cholesterol.
Use of androgens during pregnancy may result in masculinization of the female fetus and under-masculinization of the male fetus.
Sodium retention and edema can occur rarely, so caution is advised in patients with heart and kidney disease.
Uses:
These can also be used to reduce breast engorgement during postpartum period.
Sometimes these are used for chemotherapy of breast tumors in premenopausal women.
These are frequently abused by athletes due to their anabolic properties.
Long acting derivatives like testosterone enanthate IM
are indicated for hypogonadal men to compensate for the decreased endogenous secretion.
It can also be administered by transdermal route.
These agents have been used to stimulate growth in boys with delayed puberty.
Androgens have been used in the treatment of osteoporosis.
Testosterone preparations
Testosterone Esters
Effective for weeks to months.
Wide fluctuations in serum concentrations
Testosterone enanthate, testosterone
cypionate, Testosterone undecanoate
Administered as Deep IM injections
Testosterone undecanoate for oral
administration
Testosterone Transdermal Patch
Treatment of male hypogonadism
Testosterone Transdermal Patch
One FDA-approved product
Transdermal Testosterone Gels
Several FDA-approved products
Treatment of male hypogonadism
17α-Alkylated Androgens
Oxandrolone, Methyltestosterone, Danazol
• Treatment of angioedema
• Treatment of hemolytic anemia
• Angioedema prophylaxis
• Endometriosis
• Fibrocystic breast diseas
• Oral administration
• Risk of hepatoxicity
Actions of both testosterone and DHT:
Increase in mass and strength of skeletal muscle and bone.
Epiphysial fusion.
Most of the actions of androgens are mediated by DHT.
whereas testosterone is itself active at few sites.
danazol:
It is a compound with weak androgenic, progestational and glucocorticoid activities.
It decreases the secretion of gonadotropins from the pituitary by causing feedback inhibition.
Its major use is in the treatment of endometriosis.
Other uses include fibrocystic disease of breast, haemophilia, Christmas disease, ITP and angioneurotic edema.
Weight gain, edema, acne, increased hair growth, hot flushes and changes in libido are the major adverse effects of this drug.
It can also produce mild to moderate hepatocellular damage.
Actions of DHT:
Development and maturation of external genitalia(scrotum, penis, urethra etc) in males.
Male behaviour and changes of puberty.
Growth and hypertrophy of prostate in the elderly.
Growth of hair follicles(pubic, axillary and beard) during puberty.
Loss of scalp hair in adults.
Activation of sebaceous glands.
Actions of testosterone:
F- feed back inhibition of LH
I – internal genitalia development
S – spermatogenesis
H - hematopoiesis
Pharmacokinetics:
Testosterone is inactive orally due to high first pass metabolism.
17-alkylated derivatives like methyltestosterone and fluoxymestrane are effective orally.