Indications
Management of symptomatic benign prostatic hyperplasia
(BPH).
Action
Selectively blocks alpha1-adrenergic receptors in the
lower urinary tract to relax smooth muscle in the bladder
neck and prostate. Therapeutic Effects: Increased
urine flow and decreased symptoms of BPH.
Pharmacokinetics
Absorption: 49% absorbed following oral administration;
food enhances absorption.
Distribution: Unknown.
Metabolism and Excretion: Mostly metabolized
by the liver (CYP3A4 enzyme system); 11% excreted
unchanged in urine.
Half-life: 10 hr.
TIME/ACTION PROFILE
ROUTE ONSET PEAK DURATION
PO-ER within hr 8 hr 24 hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity; Moderate to
severe hepatic impairment; Potent inhibitors of the
CYP3A4 enzyme system; Concurrent use of other alphaadrenergic
blocking agents; Severe renal impairment;
Pedi: Children.
Use Cautiously in: Congenital or acquired QTc
prolongation or concurrent use of other drugs known
to prolong QTc; Mild hepatic impairment; Symptomatic
hypotension; Concurrent use of antihypertensive agents,
phosphodiesterase type 5 inhibitors, or nitrates (qrisk
of postural hypotension); Previous hypotensive episode
with other medications; Geri: Consider age-related
changes in body mass and cardiac, renal, and hepatic
function when prescribing.
Adverse Reactions/Side Effects
CNS: dizziness, fatigue, headache. EENT: intraoperative
floppy iris syndrome. Derm: TOXIC EPIDERMAL NECROLYSIS Resp: bronchitis, sinusitis, pharyngitis. CV:
postural hypotension. GI: abdominal pain, constipation,
dyspepsia, nausea. GU: erectile dysfunction, priapism.
Hemat: thrombocytopenia.
Interactions
Drug-Drug: Ketoconazole, itraconazole, and ritonavirpmetabolism
and significantlyqlevels and effects
(concurrent use contraindicated). Levels areqby
cimetidine, atenolol, and diltiazem. Mayqlevels
and effects of atenolol and diltiazem (monitor BP
and heart rate).qrisk of hypotension with antihypertensives,
nitrates, phosphodiesterase type
5 inhibitors (including sildenafil, tadalafil, and
vardenafil) and acute ingestion of alcohol.
Route/Dosage
PO (Adults): 10 mg once daily.
Availability (generic available)
Extended-release tablets: 10 mg.
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