Alfuzosin

Pronunciation

(al FYOO zoe sin)

U.S. Brand Names

Uroxatral™

Synonyms

Alfuzosin Hydrochloride

Generic Available

Canadian Brand Names

Xatral

Use

Treatment of the functional symptoms of benign prostatic hyperplasia (BPH)

Pregnancy Risk Factor

Pregnancy Implications

Teratogenic effects were not observed in animal studies; however, alfuzosin is not indicated for use in women.

Lactation

Not indicated for use in women

Contraindications

Hypersensitivity to alfuzosin or any component of the formulation; moderate or severe hepatic insufficiency (Child-Pugh class B and C); potent CYP3A4 inhibitors (eg, itraconazole, ketoconazole, ritonavir)

Warnings/Precautions

Not intended for use as an antihypertensive drug. May cause orthostasis, syncope, or dizziness. Patients should avoid situations where injury may occur as a result of syncope. Discontinue if symptoms of angina occur or worsen. Use caution with history of QT prolongation or use with medications which may prolong the QT interval. Rule out prostatic carcinoma before beginning therapy. Use caution with renal or mild hepatic impairment.

Adverse Reactions

1% to 10%:

Central nervous system: Dizziness (6%), fatigue (3%), headache (3%), pain (1% to 2%)

Gastrointestinal: Abdominal pain (1% to 2%), constipation (1% to 2%), dyspepsia (1% to 2%), nausea (1% to 2%)

Genitourinary: Impotence (1% to 2%)

Respiratory: Upper respiratory tract infection (3%), bronchitis (1% to 2%), pharyngitis (1% to 2%), sinusitis (1% to 2%)

<1%: Hypotension, postural hypotension, syncope

Postmarketing and/or case reports: Chest pain, priapism, rash, tachycardia

Overdosage/Toxicology

Hypotension would be expected in case of overdose. Treatment is supportive.

Drug Interactions

Substrate of CYP3A4 (major)

CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of alfuzosin. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.

CYP3A4 inhibitors: May increase the levels/effects of alfuzosin. Example inhibitors include azole antifungals, ciprofloxacin, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, and verapamil. Concurrent use of itraconazole, ketoconazole, or ritonavir is contraindicated.

Ethanol/Nutrition/Herb Interactions

Food: Food increases the extent of absorption.

Stability

Store at controlled room temperature of 15°C to 30°C (59°F to 86°F); protect from light and moisture

Mechanism of Action

An antagonist of alpha1 adrenoreceptors in the lower urinary tract. Smooth muscle tone is mediated by the sympathetic nervous stimulation of alpha1 adrenoreceptors, which are abundant in the prostate, prostatic capsule, prostatic urethra, and bladder neck. Blockade of these adrenoreceptors can cause smooth muscles in the bladder neck and prostate to relax, resulting in an improvement in urine flow rate and a reduction in symptoms of BPH.

Pharmacodynamics/Kinetics

Absorption: Decreased 50% under fasting conditions

Distribution: Vd: 3.2 L/kg

Protein binding: 82% to 90%

Metabolism: Hepatic, primarily via CYP3A4; metabolism includes oxidation, O-demethylation and N-dealkylation; forms metabolites (inactive)

Bioavailability: 49% following a meal

Half-life elimination: 10 hours

Time to peak, plasma: 8 hours following a meal

Excretion: Feces (69%); urine (24%)

Dosage

Oral: Adults: 10 mg once daily

Dosage adjustment in renal impairment: Bioavailability and maximum serum concentrations are increased by ~50% with mild, moderate, or severe renal impairment

Note: Safety has not been evaluated in patients with creatinine clearances <30 mL/minute.

Dosage adjustment in hepatic impairment:

Mild hepatic impairment: Use has not been studied

Moderate or severe hepatic impairment (Child-Pugh class B and C): Clearance is decreased ¹ /3 to ¹ /4 and serum concentration is increased three- to fourfold; use is contraindicated

Administration

Tablet should be swallowed whole; do not crush or chew. Administer once daily (with a meal); should be taken at the same time each day.

Monitoring Parameters

Urine flow; blood pressure

Dietary Considerations

Take following a meal at the same time each day.

Patient Education

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy without consulting prescriber. Take exactly as directed, with a meal at the same time each day. Swallow tablet whole; do not crush or chew. May cause drowsiness, dizziness, impaired judgment (use caution when driving or engaging in tasks that require alertness until response to drug is known); or postural hypotension (use caution when rising from sitting or lying position or when climbing stairs). Report unusual chest pain, respiratory difficulty, or any persistent adverse reactions.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause dizziness

Mental Health: Effects on Psychiatric Treatment

Alfuzosin may cause orthostasis. Concomitant use with psychotropics may produce additive effects on blood pressure. Use caution with thioridazine and ziprasidone; may prolong QT interval. Use caution with nefazodone; may increase levels of alfuzosin resulting in toxicity.

Dosage Forms

Tablet, extended release, as hydrochloride: 10 mg

International Brand Names

Alfetim® (ES, HU); Alfuzol® (AR); Benestan® (ES, PT); Dalfaz® (AR, PL, RU); Mittoval® (IT); Urion® (AT, DE, FR, NL); Uroxatral® (CL, DE); Xatral® (AT, BE, BR, CH, CO, CR, CZ, DK, DO, EC, FI, FR, GB, GT, HN, IE, IL, IT, LU, NL, NO, PA, RO, SE, SG, SV, TH, TR, YU, ZA); Xatral OD® (SE); Xatral SR® (IL); Xatral Uno® (CH, CZ); Xatral XL® (IL)

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