Drugs for GU Disorders - Konorev Flashcards
Cause of epithelial tissue hyperplasia
androgens
Cause of stromal tissue hyperplasia
estrogens
aromatase
converts androgens to estrogens
Tx: dynamic prostatic pathogenic factors
selective alpha-1 andrenergic antagonists
Tx: static prostatic pathogenic factors
5alpha-reductase inhibitors
second generation alpha-1 andrenergic antagonists
- terazosin
- doxazosin
- alfuzosin
third generation alpha-1 andrenergic antagonists
- tamulosin
- silodosin
5alpha-reductase inhibitors
- finasteride
- dutasteride
benefits of using alpha-1 and antagonisis over 5alpha-reductase inhibitors
- faster acting
- effective reduction of LUTS
- ass’d w/ less sexual dysfxn
alfuzosin
- second generation alpha-1 and antagonist
- more uroselective (d/t PK not selectivity)
- doesn’t need titration
AE: doxazosin
- may cause orthostatic hypotension
- first does syncope
- dizziness
AE: terazosin
- may cause orthostatic hypotension
- first does syncope
- dizziness
tamsulosin
- alpha-1A selective (prostatic sm), some 1B activation (vasculature)
- used in BPH pts who have significant orthostatic hypotension
silodosin
- highly alpha-1A selective
- no orthostatic hypotension
- severe ejaculatory dysfxn
AE: alpha-1 antagonists
- syncope, dizziness, hypotension (2nd gen)
- ejaculatory dysfxn (3rd gen)
- nasal congestion
- flu-like s/s
DI: alpha-1 antagonists + PDE5 inhibitor
marked systemic hypotension
DI: alpha-1 antagonists + cimetidine, diltiazem
decreased alpha-1 antagonists metabolism
DI: alpha-1 antagonists + carbamazepine, phenytoin
increased metabolism
MOA: finasteride
- selective type II reductase inhibitor
- inhibits DHT synthesis from T
MOA: Dutasteride
- non-selective ( type I and II) reductase inhibitor
- inhibits DHT synthesis from T
Type I enzyme reductase locations
skin, hair follicles, liver
Type II enzyme reductase locations
prostate, genital tissue, scalp
-responsible for epithelial tissue enlargement in prostate
MOA: 5alpha-reductase inhibitors
- reduce DHT formation
- prevent AR activation
- shrink prostate
negative aspects of 5alpha-reductase inhibitors
- need 6-12 m to develop effect
- more pronounced sexual dysfunction
- “second-line” agent