Trade Names:Uroxatral- Tablets, ER 10 mgXatral (Canada)
Selective blockade for alpha-1-adrenergic receptors in the lower urinary tract, which causes 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%. T max is 8 h. The C max and AUC are about 13.6 ng/mL and 194 ng•h/mL, respectively. Steady-state is reached with the second dose. The extent of absorption is 50% lower under fasting conditions; should be taken immediately following a meal.
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. Elimination half-life is 10 h (oral).
The mean C max and AUC values were increased about 50% in patients with mild, moderate, or severe renal impairment.Hepatic Function Impairment
In patients with moderate or severe hepatic function impairment, plasma concentrations of alfuzosin were increased 3- to 4-fold.Elderly
The concentrations in patients 75 years of age and older were approximately 35% greater than in those younger than 65 years of age.
Treatment of signs and symptoms of BPH.
Patients with moderate or severe hepatic impairment; coadministration with potent CYP3A4 inhibitors (eg, itraconazole, ketoconazole, ritonavir); hypersensitivity to any component of the product.
PO 10 mg/day.
Store at 59° to 86°F. Protect from light and moisture.
Other alpha-blockers should not be coadministered.Amiodarone
Alfuzosin concentrations may be elevated, increasing the pharmacologic effects and risk of adverse reactions, including hypotension. Use with caution and monitor the patient's response.Antihypertensive medications, nitrates
Risk of hypotension and syncope may be increased. Use with caution.Beta-adrenergic blockers (eg, atenolol, propranolol)
Severity and duration of hypotension following the first dose of alfuzosin may be increased in patients receiving beta-adrenergic blockers. In addition, plasma levels of alfuzosin and atenolol may be elevated, increasing the pharmacologic effects and risk of adverse reactions, including hypotension. Use with caution.Cimetidine
Alfuzosin levels may be elevated, increasing the pharmacologic and adverse reactions.Clarithromycin, nefazodone
Alfuzosin concentrations may be elevated, increasing the pharmacologic effects and risk of adverse reactions, including hypotension. If possible, avoid coadministration with alfuzosin.Food
Alfuzosin absorption may be decreased under fasting conditions. Alfuzosin should be taken immediately after a meal.Moderate CYP3A4 inhibitors (eg, diltiazem)
Alfuzosin plasma levels may be elevated, increasing the pharmacologic effects and risk of adverse reactions, including hypotension. Use with caution.Phosphodiesterase type 5 inhibitors (eg, sildenafil, tadalafil, vardenafil)
The risk of hypotension may be increased. Doses of sildenafil greater then 25 mg should be avoided within 4 h of alfuzosin administration. Use with caution.Potent CYP3A4 inhibitors (eg, itraconazole, ketoconazole, ritonavir)
Because plasma concentrations of alfuzosin may be increased more than 2-fold, coadministration of these agents is contraindicated.
None well documented.
Orthostatic hypotension (7%); angina pectoris in patients with preexisting coronary artery disease, tachycardia (postmarketing).
Dizziness (6%); fatigue, headache (3%).
Pruritus, rash, urticaria (postmarketing).
Pharyngitis, sinusitis (1% to 2%); flushing, rhinitis (postmarketing).
Abdominal pain, constipation, dyspepsia, nausea (1% to 2%); diarrhea (postmarketing).
Impotence (1% to 2%); priapism (postmarketing).
Upper respiratory tract infection (3%); bronchitis (1% to 2%).
Pain (1% to 2%); angioedema, chest pain, edema, hepatocellular and cholestatic liver injury (including jaundice) (postmarketing).
Monitor patient for orthostatic hypotension. Assess changes in urinary symptoms such as dribbling, frequency, hesitancy, nocturia, volume, and weak stream.
Category B .
Use not indicated.
Not indicated for use in children.
Use with caution in patients with severe renal impairment.
Contraindicated in patients with moderate or severe hepatic impairment.
Discontinue if symptoms of angina pectoris appear or worsen.
Postural hypotension with or without symptoms may occur within a few hours following administration of alfuzosin.
Has been observed during cataract surgery in some patients on or previously treated with alpha-1 blockers.
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.
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