Benign prostatic hyperplasia (monotherapy or combination therapy):
Note: In patients with moderate to severe predominant storage lower urinary tract symptoms, use in combination with beta-3 agonist or anticholinergic agent. In patients with a significantly enlarged prostate (prostate volume >30 mL, prostate-specific antigen >1.5 ng/dL, or palpable prostate enlargement on digital rectal exam), use in combination with 5-alpha reductase inhibitor (AUA [Lerner 2021]).
Oral: 10 mg once daily
Ureteral stone(s) expulsion (off-label use): Note: Consider for use in patients with ureteral stones >5 and ≤10 mm (Campschroer 2018; Hollingsworth 2016). Although most evidence exists for distal ureteral stones, given the low side effect profile of alpha-blockers, may consider use in patients with stones in any location of ureter (AUA/ES [Assimos 2016b]). Additionally, may consider for use after shock wave lithotripsy to help pass stone fragments (AUA/ES [Assimos 2016a]; Oestreich 2020).
Oral: 10 mg once daily until stone passage or for up to 4 weeks (Agrawal 2009; Ahmed 2010; Campschroer 2018; Gurbuz 2011).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling; use with caution in severe renal impairment (CrCl <30 mL/minute).
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.
Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet Extended Release 24 Hour, Oral, as hydrochloride:
Uroxatral: 10 mg [contains hydrogenated castor oil]
Generic: 10 mg
Yes
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet Extended Release 24 Hour, Oral, as hydrochloride:
Xatral: 10 mg
Generic: 10 mg
Oral: Administer immediately following a meal at the same time each day. Swallow tablet whole; do not crush or chew.
Bariatric surgery: Tablet, extended release: Some institutions may have specific protocols that conflict with these recommendations; refer to institutional protocols as appropriate. No IR formulation available; prazosin is the drug within class most similar in structure with an IR formulation available if needing to switch.
Benign prostatic hyperplasia: Treatment of signs and symptoms of benign prostatic hyperplasia.
Ureteral stones, expulsion
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Adverse reactions reported in adults.
1% to 10%:
Gastrointestinal: Abdominal pain (1% to 2%), constipation (1% to 2%), dyspepsia (1% to 2%), nausea (1% to 2%)
Genitourinary: Impotence (1% to 2%)
Nervous system: Dizziness (6%), fatigue (3%), headache (3%), pain (1% to 2%)
Respiratory: Bronchitis (1% to 2%), pharyngitis (1% to 2%), sinusitis (1% to 2%), upper respiratory tract infection (3%)
<1%: Cardiovascular: Hypotension, orthostatic hypotension, syncope
Postmarketing:
Cardiovascular: Atrial fibrillation, chest pain, edema, flushing, tachycardia
Dermatologic: Pruritus, skin rash, toxic epidermal necrolysis, urticaria
Gastrointestinal: Diarrhea, vomiting
Genitourinary: Priapism
Hematologic: Thrombocytopenia
Hepatic: Hepatic injury (including cholestatic and hepatocellular), jaundice
Hypersensitivity: Angioedema
Ophthalmic: Intraoperative floppy iris syndrome (with cataract surgery) (Settas 2006)
Respiratory: Rhinitis
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
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).
Other warning/precautions:
• Limitation of use: Not intended for use as an antihypertensive drug.
Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alpha-/Beta-Agonists: Alpha1-Blockers may diminish the vasoconstricting effect of Alpha-/Beta-Agonists. Similarly, Alpha-/Beta-Agonists may antagonize Alpha1-Blocker vasodilation. Risk C: Monitor therapy
Alpha1-Agonists: Alpha1-Blockers may diminish the vasoconstricting effect of Alpha1-Agonists. Similarly, Alpha1-Agonists may antagonize Alpha1-Blocker vasodilation. Risk C: Monitor therapy
Alpha1-Blockers: May enhance the antihypertensive effect of other Alpha1-Blockers. Risk X: Avoid combination
Beta-Blockers: May enhance the orthostatic hypotensive effect of Alpha1-Blockers. The risk associated with ophthalmic products is probably less than systemic products. Risk C: Monitor therapy
Blood Pressure Lowering Agents: Alfuzosin may enhance the hypotensive effect of Blood Pressure Lowering Agents. Risk C: Monitor therapy
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Alfuzosin. Risk C: Monitor therapy
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Alfuzosin. Risk X: Avoid combination
Dapoxetine: May enhance the orthostatic hypotensive effect of Alpha1-Blockers. Risk C: Monitor therapy
Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Fosamprenavir: May increase the serum concentration of Alfuzosin. Risk X: Avoid combination
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Haloperidol: QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of Haloperidol. Risk C: Monitor therapy
Nitroglycerin: Alfuzosin may enhance the hypotensive effect of Nitroglycerin. Risk C: Monitor therapy
Phosphodiesterase 5 Inhibitors: Alpha1-Blockers (Uroselective) may enhance the hypotensive effect of Phosphodiesterase 5 Inhibitors. Risk C: Monitor therapy
QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Caution) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Risk C: Monitor therapy
Rilmenidine: Alpha1-Blockers may enhance the hypotensive effect of Rilmenidine. Risk C: Monitor therapy
Food increases the extent of absorption. Management: Administer immediately following a meal at the same time each day.
Adverse events have not been observed in animal reproduction studies.
It is not known if alfuzosin is present in breast milk.
Take immediately following a meal.
International Prostate Symptom Score (IPSS) (baseline and 4 to 12 weeks after treatment initiation); urinalysis (baseline); BP; prostate-specific antigen; objective and subjective signs of relief of benign prostatic hyperplasia and lower urinary tract symptoms (AUA [Lerner 2021]; manufacturer’s labeling).
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
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%; 11% as unchanged drug)
Altered kidney function: Mean Cmax and AUC values were increased ~50% in patients with mild, moderate, or severe renal impairment.
Hepatic function impairment: In patients with moderate or severe hepatic impairment, clearance is decreased and plasma concentrations are increased 3- to 4-fold.
Older adult: Plasma concentrations in patients ≥75 years were ~35% greater than in those <65 years.
Tablet, 24-hour (Alfuzosin HCl ER Oral)
10 mg (per each): $4.21 - $4.22
Tablet, 24-hour (Uroxatral Oral)
10 mg (per each): $30.72
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