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Alfuzosin: Drug information

Alfuzosin: Drug information
(For additional information see "Alfuzosin: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Uroxatral
Brand Names: Canada
  • APO-Alvuzosin;
  • Auro-Alfuzosin;
  • SANDOZ Alfuzosin;
  • Xatral
Pharmacologic Category
  • Alpha 1 Blocker
Dosing: Adult
Benign prostatic hyperplasia

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

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.

Dosing: Kidney Impairment: Adult

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: Adult

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.

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

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

Generic Equivalent Available: US

Yes

Dosage Forms: Canada

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

Administration: Adult

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.

Use: Labeled Indications

Benign prostatic hyperplasia: Treatment of signs and symptoms of benign prostatic hyperplasia.

Use: Off-Label: Adult

Ureteral stones, expulsion

Adverse Reactions

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

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

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).

Other warning/precautions:

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

Metabolism/Transport Effects

Substrate of CYP3A4 (major); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

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 Interactions

Food increases the extent of absorption. Management: Administer immediately following a meal at the same time each day.

Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies.

Breastfeeding Considerations

It is not known if alfuzosin is present in breast milk.

Dietary Considerations

Take immediately following a meal.

Monitoring Parameters

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).

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 BPH symptoms.

Pharmacokinetics

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)

Pharmacokinetics: Additional Considerations

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.

Pricing: US

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

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Brand Names: International
  • Afluprost (RU);
  • Alcinin (GR);
  • Alfabax (PL);
  • Alfasin XR (BD);
  • Alfirum (UA);
  • Alfron XL (KR);
  • Alfsin XL (KR);
  • Alfu (IE);
  • Alfu-Kal XL (IL);
  • Alfumax (BD);
  • Alfunar (DE);
  • Alfural (HK);
  • Alfurion (PL);
  • Alfurix XL (KR);
  • Alfusin (IN);
  • Alfutor ER (ZW);
  • Alfuwin (ZA);
  • Alfuzo XL (TW);
  • Alfuzon XL (KR);
  • Alfuzostad (CZ);
  • Alsiful S.R. (VN);
  • Apo-Alfuzosin (SG);
  • Azosin SR (TW);
  • Benestan (ES, PT);
  • Benestan OD (PT);
  • Benprostex (EG);
  • Besavar (GB);
  • Bundisarin (DK, NL);
  • Dalfaz (AR, ES, PL, RU);
  • Efzu (IN);
  • Flotral (LB, PE, VN);
  • Fozal (PH);
  • Fuzocim (AE, CH, LB);
  • Lafunomyl (SE);
  • Lafuzo (TW);
  • Lura XL (KR);
  • Mittoval (IT);
  • Nuo Shu An (CN);
  • Ofoxal (MT);
  • Ofuxal (GR);
  • Profuzosin (PH);
  • Prostazosin (DK);
  • Prosterol (EG);
  • Ranfuzosin (SG);
  • Rantral (ZA);
  • Rilif (GR);
  • Unibenestan (ES);
  • Urion (FR);
  • Uritab XL (BH, ET);
  • Uriten (BD);
  • Uroxatral (CL);
  • Uroxatral OD (AR, PY, UY);
  • Uroxatral uno (DE);
  • Vasran (GB);
  • WeiPing (CN);
  • Xatger (IE);
  • Xatosin XL (KR);
  • Xatral (AE, AT, BD, BE, BF, BJ, CH, CI, CN, DK, ET, FI, FR, GB, GH, GM, GN, GR, HK, IE, IL, IT, KE, KW, LR, MA, ML, MR, MU, MW, NE, NG, NL, PH, SA, SC, SD, SE, SG, SL, SN, TN, TR, TZ, UG, VN, ZA, ZM, ZW);
  • Xatral LP (BG, FR);
  • Xatral OD (BR, CO, CR, CU, DO, EC, GT, HN, MX, NI, PA, PE, PH, PY, SE, SV, VE);
  • Xatral Retard (LU);
  • Xatral SR (AE, AU, BH, CY, EE, EG, IL, LT, LV, MT, PK, RO, SA, SK, TR);
  • Xatral XL (AE, BH, EG, IL, JO, KR, KW, LB, MT, QA, TH, TR, TW);
  • XAtral XL (SA);
  • Xatral XL PR (CY);
  • Zapros XL (KR)


For country code abbreviations (show table)
  1. Agrawal M, Gupta M, Gupta A, Agrawal A, Sarkari A, Lavania P. Prospective randomized trial comparing efficacy of alfuzosin and tamsulosin in management of lower ureteral stones. Urology. 2009;73(4):706-709. doi:10.1016/j.urology.2008.11.013 [PubMed 19193417]
  2. Ahmed AF, Al-Sayed AY. Tamsulosin versus alfuzosin in the treatment of patients with distal ureteral stones: prospective, randomized, comparative study. Korean J Urol. 2010;51(3):193-197. doi:10.4111/kju.2010.51.3.193 [PubMed 20414396]
  3. Assimos D, Krambeck A, Miller NL, et al. Surgical management of stones: American Urological Association/Endourological Society guideline, part I. J Urol. 2016b;196(4):1153-1160. doi:10.1016/j.juro.2016.05.090 [PubMed 27238616]
  4. Assimos D, Krambeck A, Miller NL, et al. Surgical management of stones: American Urological Association/Endourological Society guideline, part II. J Urol. 2016a;196(4):1161-1169. doi:10.1016/j.juro.2016.05.091 [PubMed 27238615]
  5. Campschroer T, Zhu X, Vernooij RW, Lock MT. Alpha-blockers as medical expulsive therapy for ureteral stones. Cochrane Database Syst Rev. 2018;4(4):CD008509. doi:10.1002/14651858.CD008509.pub3 [PubMed 29620795]
  6. Gurbuz MC, Polat H, Canat L, Kilic M, Caskurlu T. Efficacy of three different alpha 1-adrenergic blockers and hyoscine N-butylbromide for distal ureteral stones. Int Braz J Urol. 2011;37(2):195-200; discussion 201-2. doi:10.1590/s1677-55382011000200006 [PubMed 21557836]
  7. Hollingsworth JM, Canales BK, Rogers MA, et al. Alpha blockers for treatment of ureteric stones: systematic review and meta-analysis. BMJ. 2016;355:i6112. doi:10.1136/bmj.i6112 [PubMed 27908918]
  8. Lerner LB, McVary KT, Barry MJ, et al. Management of lower urinary tract symptoms attributed to benign prostatic hyperplasia: AUA guideline part I, initial work-up and medical management. J Urol. 2021;206(4):806-817. doi:10.1097/JU.0000000000002183 [PubMed 34384237]
  9. Oestreich MC, Vernooij RW, Sathianathen NJ, et al. Alpha-blockers after shock wave lithotripsy for renal or ureteral stones in adults. Cochrane Database Syst Rev. 2020;11(11):CD013393. doi:10.1002/14651858.CD013393.pub2 [PubMed 33179245]
  10. Settas G, Fitt AW. Intraoperative floppy iris syndrome in a patient taking alfuzosin for benign prostatic hypertrophy. Eye (Lond). 2006;20(12):1431-1432. doi:10.1038/sj.eye.6702291 [PubMed 16498436]
  11. Uroxatral (alfuzosin) [prescribing information]. St. Michael, Barbados: Concordia Pharmaceuticals Inc; May 2020.
  12. Xatral (alfuzosin) [product monograph]. Laval, Quebec, Canada: Sanofi-aventis Canada Inc; January 2019.
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