PHARM_BPH Flashcards
name the short acting selective alpha-1 blocker
alfuzosin
name the two 5-alpha-reductase inhibitors
finasteride
dutasteride
which alpha-1 receptor predominates in smooth muscle of prostate & penile urethra?
alpha1-a
which alpha-1 receptor predominates in the bladder detrusor muscle?
alpha-1d
which alpha blocker is considered the superior alpha blocker because it has improvement in LUTS & has no AE on dizziness, asthenia, & ejaculatory dysfunction?
alfuzosin
what is the advantage of selective alpha-1a blockers?
dont have to titrate dose (diminsed effects on CV function)
what are the disadvantages of alpha-1a blockers?
abnormal retrograe ejaculation
block of dopamine & other regulatory CNS transmitters
what is floppy iris syndrome?
occasional AE during cataract surgery in pts taking any of the alpha-1 blockers
how does tadalafil work?
inhibits PDE5 which would normally degrade cGMP–>smooth-muscle relaxation
how is tadalafil metabolized?
CYP3A4 in liver
how is tadalafil eliminated?
fecal elimination
what are the AEs of tadalafil?
headache, Nausea, indigestion, nasopharyngitis, URIs
what are the must know contraindications for taking tadalafil?
organic nitrates
what happens if you take nitrates and tadalafil at the same time?
profound hypotension
exacerbated by alcohol consumption
what are the beta-sitosterols used for?
improved urinary symptoms of BPH but DO NOT significantly reduce size of prostate
does saw palmetto work for BPH?
NO
how does alprostadil work?
mimic of PGE1 which stimulates adenylate cyclase to increase cAMP–>PKA–>decrease intracellular Ca2+–>smooth muscle relaxation–>erection
how is alprostadil administered?
locally via urethral suppository or intra-cavernosal injection
how are all of the PDE inhibitors administered?
oral
which PDE5 inhibitor has a long half life and thus makes it useful for therapy in BPH?
tadalafil
how are all of the PDE5 inhibitors metabolized?
hepatic metabolism CYP3A4
what are some of the common AEs of PDE5 inhibitors?
headache
CV issues
sudden loss of hearing
loss of sight
replacing what hormone may improve response of hypogonadal men to PDE5 inhibitors such as sildenafil?
testosterone
which drug used to treat erectile dysfunction crosses the BBB easily potentially producing anxiety, antidiuresis, dizziness, flushing, headache and hypertension?
yohimbine