Skip to Content

Alfuzosin

Pronunciation

Pronunciation

(al FYOO zoe sin)

Index Terms

  • Alfuzosin HCl
  • Alfuzosin Hydrochloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet Extended Release 24 Hour, Oral, as hydrochloride:

Uroxatral: 10 mg

Uroxatral: 10 mg [contains hydrogenated castor oil]

Generic: 10 mg

Brand Names: U.S.

  • Uroxatral

Pharmacologic Category

  • Alpha1 Blocker

Pharmacology

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 BPH symptoms.

Absorption

Decreased 50% under fasting conditions

Distribution

Vd: 3.2 L/kg

Metabolism

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

Excretion

Feces (69%); urine (24%; 11% as unchanged drug)

Time to Peak

Plasma: 8 hours following a meal

Half-Life Elimination

10 hours

Protein Binding

82% to 90%

Special Populations: Renal Function Impairment

Mean Cmax and AUC values were increased ~50% in patients with mild, moderate, or severe renal impairment.

Special Populations: Hepatic Function Impairment

In patients with moderate or severe hepatic impairment, clearance is decreased and plasma concentrations are increased 3- to 4-fold.

Special Populations: Elderly

Plasma concentrations in patients ≥75 years were ~35% greater than in those <65 years.

Use: Labeled Indications

Benign prostatic hyperplasia: Treatment of signs and symptoms of benign prostatic hyperplasia (BPH)

Use: Unlabeled

Facilitation of expulsion of ureteral stones

Contraindications

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

Canadian labeling: Additional contraindications (not in US labeling): Concurrent use with other alpha1-blockers

Dosing: Adult

Benign prostatic hyperplasia (BPH): Oral: 10 mg once daily

Ureteral stones, expulsion (off-label use): Oral: 10 mg once daily, discontinue after successful expulsion (average time to expulsion 1-2 weeks) (Agrawal, 2009; Ahmed, 2010; Gurbuz, 2011). Note: Patients with stones >10 mm were excluded from studies.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling; use with caution in severe renal impairment (CrCl <30 mL/minute).

Dosing: Hepatic Impairment

Mild hepatic impairment (Child-Pugh class A): There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied); use with caution.

Moderate or severe hepatic impairment (Child-Pugh class B or C): Use is contraindicated.

Administration

Administer immediately following a meal at the same time each day. Swallow tablet whole; do not crush or chew.

Dietary Considerations

Take immediately following a meal.

Storage

Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light and moisture.

Drug Interactions

Alpha-/Beta-Agonists: Alpha1-Blockers may diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Similarly, Alpha-/Beta-Agonists may antagonize Alpha1-Blocker vasodilation. Monitor therapy

Alpha1-Agonists: Alpha1-Blockers may diminish the vasoconstricting effect of Alpha1-Agonists. Similarly, Alpha1-Agonists may antagonize Alpha1-Blocker vasodilation. Monitor therapy

Alpha1-Blockers: May enhance the antihypertensive effect of other Alpha1-Blockers. Avoid combination

Aprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Beta-Blockers: May enhance the orthostatic hypotensive effect of Alpha1-Blockers. The risk associated with ophthalmic products is probably less than systemic products. Exceptions: Levobunolol; Metipranolol. Monitor therapy

Blood Pressure Lowering Agents: Alfuzosin may enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Bosentan: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates. Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Alfuzosin. Avoid combination

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates. Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification

Dapoxetine: May enhance the orthostatic hypotensive effect of Alpha1-Blockers. Monitor therapy

Dasatinib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates. Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. Consider therapy modification

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Highest Risk QTc-Prolonging Agents: QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying) may enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents. Management: Avoid such combinations when possible. Use should be accompanied by close monitoring for evidence of QT prolongation or other alterations of cardiac rhythm. Consider therapy modification

Idelalisib: May increase the serum concentration of CYP3A4 Substrates. Avoid combination

Ivacaftor: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Luliconazole: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Mitotane: May decrease the serum concentration of CYP3A4 Substrates. Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Consider therapy modification

Moderate Risk QTc-Prolonging Agents: QTc-Prolonging Agents (Indeterminate Risk and Risk Modifying) may enhance the QTc-prolonging effect of Moderate Risk QTc-Prolonging Agents. Monitor therapy

Netupitant: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Nitroglycerin: Alfuzosin may enhance the hypotensive effect of Nitroglycerin. Monitor therapy

Palbociclib: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Alpha1-Blockers. Management: Ensure patient is stable on one agent prior to initiating the other, and always initiate combination using the lowest possible dose of the drug being added. When tadalafil is used for treatment of BPH, concurrent alpha 1-blockers are not recommended. Consider therapy modification

Protease Inhibitors: May increase the serum concentration of Alfuzosin. Avoid combination

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

Simeprevir: May increase the serum concentration of CYP3A4 Substrates. Monitor therapy

St John's Wort: May decrease the serum concentration of CYP3A4 Substrates. Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

Stiripentol: May increase the serum concentration of CYP3A4 Substrates. Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

Telaprevir: May increase the serum concentration of Alfuzosin. Avoid combination

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates. Monitor therapy

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% (Limited to important or life-threatening): Angioedema, atrial fibrillation, chest pain, edema, hepatic injury (including cholestatic), hypotension, intraoperative floppy iris syndrome (with cataract surgery), priapism, pruritus, thrombocytopenia, toxic epidermal necrolysis

Warnings/Precautions

Concerns related to adverse effects:

• Angina: Discontinue if symptoms of angina occur or worsen.

• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).

• Floppy iris syndrome: Intraoperative floppy iris syndrome has been observed in cataract surgery patients who were on or were previously treated with alpha1-blockers; there appears to be no benefit in discontinuing alpha1-blocker therapy prior to surgery. May require modifications to surgical technique.

• Orthostatic hypotension/syncope: May cause orthostatic hypotension and syncope within a few hours following administration; anticipate a similar effect if therapy is interrupted for a few days, if dosage is rapidly increased, or if another antihypertensive drug, PDE-5 inhibitors, or nitrates is introduced. Use with caution in patients with symptomatic orthostatic hypotension.

• Priapism: Priapism has been associated with use (rarely); seek immediate medical assistance for erections lasting longer than 4 hours.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with histories of tachyarrhythmia or with certain cardiovascular conditions, such as myocardial ischemia.

• Hepatic impairment: Use with caution in patients with mild hepatic impairment; contraindicated in moderate-to-severe impairment.

• Prostate cancer: Rule out prostatic carcinoma before beginning therapy (many symptoms of BPH and prostate cancer are similar).

• QT prolongation: Alfuzosin has been shown to prolong the QT interval alone (minimal) and with other drugs with comparable effects on the QT interval (additive). Use with caution in patients with known QT prolongation (congenital or acquired).

• Renal impairment: Use with caution in patients with severe renal impairment (CrCl <30 mL/minute).

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Other warning/precautions:

• Limitation of use: Not intended for use as an antihypertensive drug.

Monitoring Parameters

Urine flow, blood pressure, PSA

Pregnancy Risk Factor

B

Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience headache or loss of strength and energy. Have patient report immediately to prescriber severe dizziness, passing out, angina, or priapism (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

Hide