Pharm - Male Flashcards
Short acting selective alpha 1 blockers
Prazosin, Alfuzosin
Long acting selective alpha 1 blockers
Terazosin, Doxazosin
alpha 1 alpha pertially selective blockers
Tamsulosin, Silodosin
PDE-5 Inhibitors (for BPH)
Tadalafil
5 alpha reductase inhibitors
Finasteride, Dutasteride
Type of alpha receptor in prostate
alpha-1a
Type of alpha receptor in the bladder detrusor muscle
alpha-1d
Prazosin PKPD
demethylation; conjugation; fecal elimination (2-4hr half life)
Alfuzosin PKPD
3A4; fecal/renal elimination; (10hr half life)
Terazosin PKPD
Hepatic-fecal/renal elimination; 12hr half life
Doxazosin PKPD
3A4>2D6; fecal elimination; 5-22hrs
Tamsulosin PKPD
3A4/2D6; renal/fecal elimination; 5-15hrs half life; bioavailability decreased by food
Silodosin PKPD
3A4; glucuronide conjugaiton; fecal/urine elimination; 13hr half life
Prazosin Dosing requirements
needs dosing every 12hrs with dose titration; making it a less attractive drug to use due to that and short half life.
Alpha 1 blocker SE
GI (xerostemia), CNS (dizziness, somnolence), retrograde ejaculation, floppy iris syndrome
Tadalafil MOA
PDE5 inhibtor which causes smooth muscle relaxation
Tadalafil PKPD
3A4; fecal elimination
Tadalafil AE
non-arteritic ischemic optic neuropathy; retinal artery occlusion; hearing loss
Tadalafil contraindications
concurrent organic nitrates - profound hypotension exacerbated by alcohol consumption
Finasteride: Dutasteride
F - type 2 5 alpha reductase enzyme; D - type 1&2; competitive long binding time, slow reversal; extensive 3A4 metabolism; pregnancy category X
Finasteride: Dutasteride AE
well tolerated; ejaculatory dysfunction, decreased libido, gynecomastia; decreases PSA levels (can be issue if using to monitor prostate cancer)
Beta sitosterols
herbal therapy used OTC for BPH - shows improved urinary symptoms and flow but no reduction in prostate size
Saw Palmetto
herbal therapy used OTC for BPH; no proven benefit.
Alprostadil MOA
mimics PGE1 which activated adenylate cyclase to increase intracellular cAMP