A.8- androgens, anti androgens Flashcards
function of testosterone
- male reproductive development
- maintains fertility, libido
- cause male hair baldness
- anabolic effects–> ↑ muscle mass and strength, ↑ RBC’s production
synthetic analogues of testosterone
Nandrolone, Oxandrolone
Testosterone undecanoate
how is Nandrolone given?
parenteral
how is testosterone given?
transdermal, buccal, subcutaneous implant
indications of androgens (Testosterone, Nandrolone)
hypogonadism in boys hormone replacement therapy in men weight gain in patients with 'wasting syndrome' anemias- stimulate RBC production illicit use in athletes
SE of testosterone
females- virilization (hirsutism, enlarged clitoris, deepened voice), menstrual irregularity
males- feminization and gynecomastia (due to feedback inhibition of the pituitary)
↑ libido and aggression
prostate pathology
both- cholestatic jaundice, ↑ of liver enzymes
contraindications for testosterone
pregnancy
prostate/ breast cancer
CHF
types of antiandrogens
receptor inhibitors
5𝝰 reductase inhibitors
GnRH analogs and antagonists
synthesis inhibitors
agents affecting sexual activity- non hormonal
PDE- 5 inhibitors (e.g- sildenafil, alprostadil)
drugs causing sexual disturbances
𝝰1 blockers- prolonged ejaculation
antidepressants
antipsychotics
mechanism of PDE-5 inhibitors
phosphodiesterase inhibition–> cGMP ↑–> vasodilation
how is sildenafil given?
oral
how is alprostadil given?
intracavernosal injection (into the corpus cavernosum of the penis)
indications for sildenafil (“viagra” )
erectile dysfunction
pulmonary hypertension
BPH
SE in sildenafil
severe hypotension when combined with nitrates
priapism (prolonged erection)
blue tinted vision
list receptor inhibitors (antiandrogens)
Bicalutamide
flutamide
spironolactone
cyproterone
what is bicalutamide?
competitive inhibitor of androgen receptors
how is bicalutamide given?
orally
indications for bicalutamide and flutamide
prostate cancer
precocious puberty
SE of bicalutamide
gynecomastia, hot flushes, impotence, hepatotoxicity
what is the mechanism of 5𝝰- reductase inhibitor
conversion of testosterone into dihydrotestosterone (DHT) in prostate, hair follicles
example of 5𝝰- reductase inhibitor
Finasteride
“Fine im bald..”
indictions of finasteride
BPH
prevent male baldness!
what is ketoconazole used for?
prostate cancer (if resistant to 1st line anti-androgens)
