Class: Antiadrenergic agent, peripherally acting
- Tablets, extended release 10 mg
Mechanism of Action
Selective blockade for alpha 1 -adrenergic receptors in the lower urinary tract, which cause smooth muscle in the bladder neck and prostate to relax, resulting in improved urine flow and a reduction in symptoms of benign prostatic hyperplasia (BPH).
Bioavailability is about 49%. Time to reach C max is about 8 h. The C max and AUC are about 13.6 ng/mL and 194 ng•h/mL, respectively.
Following IV administration, the Vd is about 3.2 L/kg. Protein binding is 82% to 90%.
Extensive hepatic metabolism with only 11% excreted unchanged in the urine. The major isozyme responsible for metabolism is CYP3A4.
After 7 days, 69% is recovered in the feces and 24% in the urine.Renal function impairment
The mean C max and AUC values were increased about 50% in patients with mild, moderate, or severe renal function impairment.Hepatic function impairment
In patients with moderate or severe hepatic function impairment, plasma concentrations of alfuzosin were increased 3- to 4-fold.
Indications and Usage
Treatment of signs and symptoms of benign prostatic hyperplasia.
Patients with moderate or severe hepatic function impairment; coadministration with potent CYP3A4 inhibitors (eg, itraconazole, ketoconazole, ritonavir); hypersensitivity to any component of the product.
Dosage and AdministrationAdults
PO 10 mg/day, immediately after the same meal each day. Do not cut, chew, or crush tablet. Instruct patient to swallow tablet whole.
Store at controlled room temperature (59° to 86°F). Protect from light and moisture.
Plasma levels may be elevated by alfuzosin, increasing the pharmacologic and adverse reactionsCimetidine
Alfuzosin levels may be elevated, increasing the pharmacologic and adverse reactionsModerate CYP3A4 inhibitors (eg, diltiazem)
Alfuzosin plasma levels may be elevated, increasing the pharmacologic and adverse reactionsPotent CYP3A4 inhibitors (eg, itraconazole, ketoconazole, ritonavir)
Because plasma concentrations of alfuzosin may be increased more than 2-fold, coadministration of these agents is contraindicated.
Laboratory Test Interactions
None well documented.
Orthostatic hypotension (7%); tachycardia (postmarketing).
Dizziness (6%); headache, fatigue (3%).
Sinusitis, pharyngitis (1% to 2%).
Abdominal pain, constipation, dyspepsia, nausea (1% to 2%).
Impotence (1% to 2%); priapism (postmarketing).
Upper respiratory tract infection (3%); bronchitis (1% to 2%).
Pain (1% to 2%); chest pain (postmarketing).
Monitor patient for orthostatic hypotension. Notify health care provider if symptomatic orthostatic hypotension or new onset or worsening of angina pectoris is noted.Urinary symptoms
Assess changes in urinary symptoms such as frequency, hesitancy, weak stream, volume, dribbling, and nocturia.
Category B .
Use not indicated.
Safety and efficacy not established.
Use with caution.
Do not administer to patients with moderate or severe hepatic function impairment
Do not use in combination with other alpha-blockers.
Discontinue if symptoms of angina pectoris appear or worsen.
Postural hypotension with or without symptoms may occur within a few h following administration of alfuzosin.
Rule out presence of carcinoma of the prostate before starting alfuzosin.
Use with caution and monitor patients with a known history of QT prolongation or patients taking medication known to prolong the QT interval.
- Advise patient to take prescribed dose every day immediately after the same meal each day.
- Advise patient not to cut, crush, or chew tablet and to swallow the tablet whole with a full glass of water.
- Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
- Caution patient that drug may cause dizziness or fainting and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
- Advise patient to contact health care provider if urinary symptoms do not improve or worsen while taking this medication.
- Instruct patient to report the following symptoms to health care provider: dizziness, fainting, chest pain, prolonged or painful erection, or bothersome side effects.