Men’s Health Pharmacology Flashcards
(47 cards)
Fxns of Testosterone
development of 2nd male traits, hair growth (pubic/puberty), anabolic effects of muscle
AEs of test
acne, hair loss/baldness, excessive prostate growth, promotion of prostate cancer
Metabolites of test
test—- estradiol by aromatase; binds to ER
test— DHT by 5alpha reductase binds to AR
test- itself can bind to AR
Impact of estradiol
increase bone density + libido
Impact of DHT
external genitalia (maturation during puberty, adulthood prostate diseases) , hair follicle growth during puberty
Impact of test direct binding to AR
internal genitalia
Skeletal muscle: increase mass+ strength
RBC production
Bone growth
General trends to test levels throughout life
Gestation: a lot of fluctuations
Childhood: drop suddenly (little to no)
Puberty: sharp increase to induce 2nd male traits
Adulthood: slow decline that starts at age 30-50
** test levels important in each stage; disruption — big impacts)
—- low T in teens: may impair puberty
—low levels in adults: impact muscle mass + sex drive
What hormone is released by hypothalamus + what does it work on
GnRH — and works on anterior pituitary
What does the anterior pituitary release + what do they do
Release FSH and LH in response to GnRH
- FSH: stimulates sperm production in serotoli cells
- LH: stimulates interstitial cells to make T
—- increase in T levels works as negative feedback on AP to decrease FSH and LH release
T or F: androgen receptors are nuclear receptors
T- found in cytoplasm of cells; binds to androgens, dimerize + go into nucleus + bind to AREs to recruit transcription machinery —- increase production of shit
AR: one gene but has different isoforms
T or F: most often test binds directly to AR by itself but can bind as DHT form sometimes
F- more often binds as DHT form (main androgen)
T or F: Test is highly protein bound in blood
T- 60% bound by albumin; 40% SHBG
What is BPH
cell division in the prostate that increases the size of the prostate eventually causing impaired urine flow from the bladder through the urethra
— reducing bladder emptying + increase urination urgency
T or F: activation of the SNS or PNS systems can worsen BPH
T-
NE binds to alpha 1AR results in SM contraction, urethral compression + further impairing bladder emptying
What is the key driver of prostate cell division + enlargement
DHT
— primarily impacts stromal cell group once in DHT form (75% growth) + also impacts epithelial cells (25%)
** aka causes increase in mainly stromal cells
How does blocking 5alpha reductase help with BPH
blocks the conversion of test to DHT—- decrease DHT binding to + increasing growth of stromal/prostate
How can we provide symptom relief in BPH
Block adrenergic or cholinergic R (blocks the SNS and PNS systems)
- doesn’t help with prostate size
Main Adrenergic target
Alpha 1 (SNS)
Main cholinergic target
M3 (PNS)
T or F: Alpha 1 + M3 receptors are also found in the periphery so we want to try to use selective options
T alpha 1 selective —- uroselective
Impact of nonselective MR antagonists
anti-ACH effects - dry mouth, decrease urination
Impact of nonselective alpha receptor antagonists OR alpha-1 antagonists
orthostatic hypotension + tachy
- dizzy, drowsiness, fatigue
What is mirabegron + its main target
Beta 3 receptor agonist
- helps relax detrusor muscle
How does Desmopressin work
Vasopressin V2 receptor agonist
- increase water excretion + used for nocturnal enuresis
