ED Drugs Flashcards
(21 cards)
Alprostadil MOA
Synthetic PGE1; stimulates AC/cAMP/PKA pathway to decrease intracellular Ca2+ resulting in smooth muscle relaxation thus ERECTION
Alprostadil Tox
Local action-avoids systemic effects; MC=penile, urethral, or testicular pain; rarely CV AE’s
Alprostadil PK
Rapid onset (mins); Effects lasts up to several hours
Alprostadil Admin
Administrations: Urethral Suppository vs. Intra-cavernosal Injection
PDE-5 Inhibitors
Avanafil, Sildenafil Tadalafil, Vardenafil
Avanafil Tox
h/a; NAION, sudden hearing loss, unstable angina
Avanafil DME
3A4»2C; fecal/renal elim; .5-.75 hr onset, 5 hr half-life
Sildenafil Tox
h/a, indigestion, visual disturbances, epistaxis; NAION, sudden hearing loss
Sildenafil DME
3A4»2C; fecal/renal elim; >1 hr onset, 4 hr half-life
Tadalafil Tox
h/a, indigestion, nausea, backache, myalgia, flushing, RTIs, nasopharyngitis; NAION, sudden hearing loss, angina, MI, tachycardia
Tadalafil DME
3A4; fecal/renal elim; 2-4 hr onset, <35 hr half-life
Vardenafil Tox
h/a, flushing, rhinitis; NAION, sudden hearing loss, angina, MI
UNIQUE = heart stuff
Vardenafil DME
3A4 & 2C; fecal/renal elim; 1 hr onset & dec by high fat meal, 5 hr half-life
Vardenafil DDI
NITRATES;
DDI’s with >70 drugs that inc risk of QT prolongation/arrhythmias
Testosterone use in ED
May improve response of hypogonadal men to PDE-5 inhibitors
Yohimbine MOA
Inc relaxation of penile smooth muscle in 2 ways; 1. alpha-2 receptor inhibitor
2. antagonizes presynaptic inhibition of NANC nerves to inc release of NO
Yohimbine Tox
Crosses BBB easily: anxiety, antidiuresis, dizziness, flushing, h/a, HTN, inc motor activity, irritability, nervousness/restlessness, sinus tachycardia, tremor; Worsens renal fxn in failure/dysfxn=CI
Yohimbine PK
Rapid (variable) absorption; complete rapid metabolism; 30 min half-life
Yohimbine DDI
MAOI action at supra-clinical doses: tyramine & caffeine interactions possible
PDE-5 inhibitor also used for BPH
Tadalafil (35 hour half life)
Yohimbine CI
renal failure/dsyfxn
