Alfuzosin
Pronunciation
(al FYOO zoe sin)
U.S. Brand Names
Uroxatral™
Synonyms
Alfuzosin Hydrochloride
Generic Available
No
Canadian Brand Names
Xatral
Use
Treatment of the functional symptoms of benign prostatic hyperplasia (BPH)
Pregnancy Risk Factor
B
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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