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Pharm Androgens
KYCOM Block 11
41
Pharmacology
Graduate
10/22/2013

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Cards

Term
3 functions of FSH, which are the main ones
Definition
main: spermatogenesis in seminiferous tubules
regulate testicular growth
steroidogenesis
Term
what are the 4 functions of LH, which is the main one
Definition
main: regulate testosterone release from leydig cells
regulate resticular growth
steroidogenesis
spermatogenesis
Term
how is the release of testosterone regulated
Definition
it feeds back to hypothalamus and pituitary
Term
what is the process of testosterone production
Definition
cholesterol > progesterone > andostenedione or androstendione . testosterone
Term
what enzyme produces testosterone
Definition
12B-hydrosteroid dehydrogenase
Term
how is testosterone transported in the body
Definition
sex hormone binding globulin (can enter cell too may have role in action)

some on albumin

1-2% unbound
Term
what enzyme turns testosterone into DHT, where is it located
Definition
steroid 2a-reductase in non-genital skin and liver

steroid 5a-reductase in urogenital tract
Term
what is the difference between testosterone and DHT
Definition
DHT has a higher binding affinity
Term
what are the 6 general functions of testosterone
Definition
embryo: virilize urigenital tract of male

growth of testes, scrotum, penis

thicken and make skin more oily

increase height and muscle

axillary hair

larynd development
Term
what are the testosterone drugs (5)
Definition
testosterone aq
testosterone cypionate
fluxymesterone
testosterone gel (androgel)
danzol
Term
what are the anti-androgens (5)
Definition
spironolactone
flutamide
ketoconazole
cimetidine
finasteride
Term
what is used to treat impotence (3)
Definition
sildenafil
vardenaful
tadalafil
Term
MOA spironolactone (3)
Definition
stop androgen binding to receptor

stop synthesis of androgens

decrease p450enz 12a-hydroxylase C12-20 lyase complex which decreases testosterone
Term
MOA flutamide
Definition
non-steroid competitive inhibitor of DHT
Term
MOA ketoconazole
Definition
H2 receptor antagonist that competes for receptor
Term
finasteride MOA
Definition
5a-reductase competitive inhibitor of conversion enzyme of DHT to testosterone
Term
MOA impotence treatment
Definition
normally NO activates gyanulyl cyclase which causes smooth m. relaxation of corpus callosum letting blood in then phosphodiesterase (PDE) closes it off

drug inhibits PDE
Term
11 uses of all testosterone drugs
Definition
androgenic: hypogonadism, failure of hypo-pit-axis

anabolic: osteroperosis, burns, surgery recovery

counteract cortical hormone effects

growth: skeletal muscle growth in pre-pubescent boys and dwarfism

unapproved: increase lean body mass, muscle strength, agression
Term
clinical use of fluoxymesterone
Definition
more focused on anabolic effects of androgens (little androgenic effects)

osteoperosis, burns, surgurical recovery
Term
clinical use of danzol (3)
Definition
not very androgenic

endometrosis, fibrocystic breast disease, hereditary angioedema
Term
clinical use of spironolactone (2)
Definition
women: hirsutism
men: causes impotence
Term
clinical use of flutamide (1)
Definition
prostate cancer (with GnRH blocker or an estrogen)
Term
clinical use of ketoconazole (1)
Definition
prostate cancer (high dose)
Term
clinical use of cimetidine
Definition
women: histutism
Term
clinical use of finasteride (3)
Definition
prostatic hyperplasia

male pattern baldness (low dose)
Term
side effects flutamide (2)
Definition
hepatitis, anemia
Term
side effects ketoconazole
Definition
hepatotoxic
Term
side effect cimetidine
Definition
males with zollinger ellison get cynecomastia
Term
side effect finasteride
Definition
impotence
Term
side effects impotence treatment (6)
Definition
no effect in absence of stimulation

headache
flushing
dyspenia
change in color vision
decreased BP
Term
what is a major contraindication to impotence drugs
Definition
nitrates
Term
what is the longest lasting impotence drug, how long
Definition
36h
tadaladil
Term
side effects of all testosterone drugs in females only (8)
Definition
masculinization
acne
facial hair
deeper voices
male pattern baldness
muscle development
menstural irregularities
virilization of fetus
Term
side effects of all testosterone drugs in males only (5)
Definition
priapism
impotence
decreased spermatogenesis
gynecomastia
Term
side effects of all testosterone drugs in any sex or age (6)
Definition
increased LDL
decreased HDL
coronary artery disease
fluid retention
edema
PANCREATITIS
Term
side effects of all testosterone drugs in kids only (4)
Definition
abnormal sexual maturity
premature closure of epiphysis
hepatic abnormalities
psychosis
Term
side effect of testosterone gel
Definition
absorbed to skin, transfered to others on hands
Term
side effects of danzol
Definition
interacts with progesterone and androgen receptors and supresses pituitary-ovarian axis decreasing FSH and LH
Term
how are the 5 testosterone drugs administered
Definition
testosterone aq- IM
testosterone cypionate- IM
fluxymesterone- oral
testosterone gel- topical
danzol- oral
Term
where is testosterone gel metabolized and excreted
Definition
metabolized in liver
excreted in urine
Term
which testosterone has the shortest and longest half life, how long
Definition
testosterone aq: short 10-100 min
testosterone cypopnate: long 8d
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