Alfuzosine

Pharmacologic Category

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.

* See Dosage and Administration in AHFS Essentials for additional information.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal 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.

Calculations

Use: Labeled Indications

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

* See Uses in AHFS Essentials for additional information.

Use: Off-Label: Adult

Facilitation of expulsion of ureteral stonesLevel of Evidence [B]

Data from two randomized unblinded active-controlled studies and one randomized placebo-controlled study in patients with symptomatic, uncomplicated distal ureteral stones ≤1 cm size supports the use of alfuzosin in the facilitation of ureteral stone expulsion Ref. Additional trials may be necessary to further define the role of alfuzosin in the management of distal ureteral stones.

Level of Evidence Definitions

Level of Evidence Scale

Class and Related Monographs

Alpha-1 Adrenergic Blockers

Comparative Efficacy

ALFUZOSIN

Clinical Practice Guidelines

Benign Prostatic Hyperplasia:

CUA, “Guideline on Male Lower Urinary Tract Symptoms/Benign Prostatic Hyperplasia (MLUTS/BPH),” 2018

Ureteral Calculi:

EAU/AUA Nephrolithiasis Guideline Panel, "Management of Ureteral Calculi," 2007

Administration: 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.

Dietary Considerations

Take immediately following a meal.

Storage/Stability

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

Medication Patient Education with HCAHPS Considerations

What is this drug used for?

• In men, it is used to treat the signs of an enlarged prostate.

• It may be given to you for other reasons. Talk with the doctor.

Frequently reported side effects of this drug

• Headache

• Loss of strength and energy

Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:

• Severe dizziness

• Passing out

• Chest pain

• Erection that lasts more than 4 hours

• Signs of a significant reaction like 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. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

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).

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.

* See Cautions in AHFS Essentials for additional information.

Geriatric Considerations

Alfuzosin is a functionally uroselective alpha-blocker, therefore, having minimal effects on the cardiovascular system. Alfuzosin appears to be well tolerated in elderly. In one study, orthostatic changes were minimal and not influenced by age.

Pregnancy Risk Factor

Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies.

Breast-Feeding Considerations

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

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%, postmarketing, and/or case reports: Angina pectoris (pre-existing CAD), angioedema, atrial fibrillation, chest pain, diarrhea, edema, flushing, hepatic injury (including cholestatic), hypotension, intraoperative floppy iris syndrome (with cataract surgery), jaundice, orthostatic hypotension, priapism, pruritus, rhinitis, skin rash, syncope, systolic hypotension, tachycardia, thrombocytopenia, toxic epidermal necrolysis, urticaria, vomiting

* See Cautions in AHFS Essentials for additional information.

Allergy and Idiosyncratic Reactions

Alpha-Blocker, Non-Quinazoline Allergy

Toxicology

Alpha Adrenergic Blockers

Metabolism/Transport Effects

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

Drug Interactions Open Interactions

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

Aprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: 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. Risk C: Monitor therapy

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

Bosentan: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

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

CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

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

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). 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). Risk D: Consider therapy modification

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

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Duvelisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). 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. Risk D: Consider therapy modification

Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Erdafitinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Fosnetupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

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

Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination

Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Larotrectinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

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

Netupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

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

Palbociclib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Phosphodiesterase 5 Inhibitors: Alpha1-Blockers (Uroselective) may enhance the hypotensive effect of Phosphodiesterase 5 Inhibitors. Risk C: Monitor therapy

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

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

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Simeprevir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy

Stiripentol: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). 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. Risk D: Consider therapy modification

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Risk C: Monitor therapy

Food Interactions

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

Genes of Interest

Cytochrome P450 3A4

Monitoring Parameters

Urine flow, blood pressure, PSA

Advanced Practitioners Physical Assessment/Monitoring

Obtain thorough medication list to make sure patient is not taking similar medications. Doses may need to be adjusted with history of QT prolongation, CAD, hypotension, or if taking HIV medications. Patients are at risk for dizziness and fainting. Monitor their fluid volume status if taking diuretics or with episodes of excessive vomiting, diarrhea, or sweating. Instruct patients that medications need to taken whole, not broken or crushed, to avoid orthostatic hypotension.

Nursing Physical Assessment/Monitoring

Assess blood pressure and monitor for hypotension, dizziness, somnolence, and impotence at beginning of therapy and on a regular basis.

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

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

Anatomic Therapeutic Chemical (ATC) Classification

G04CA01

Generic Available (US)

Yes

Pricing: US

Tablet, 24-hour (Alfuzosin HCl ER Oral)

10 mg (per each): $3.54 - $4.22

Tablet, 24-hour (Uroxatral Oral)

10 mg (per each): $26.51

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.

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.

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%; 11% as unchanged drug)

Pharmacodynamics/Kinetics: Additional Considerations

Renal function impairment: 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.

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

Local Anesthetic/Vasoconstrictor Precautions

Alfuzosin is one of the drugs confirmed to prolong the QT interval and is accepted as having a risk of causing torsade de pointes. The risk of drug-induced torsade de pointes is extremely low when a single QT interval prolonging drug is prescribed. In terms of epinephrine, it is not known what effect vasoconstrictors in the local anesthetic regimen will have in patients with a known history of congenital prolonged QT interval or in patients taking any medication that prolongs the QT interval. Until more information is obtained, it is suggested that the clinician consult with the physician prior to the use of a vasoconstrictor in suspected patients, and that the vasoconstrictor (epinephrine, mepivacaine and levonordefrin [Carbocaine® 2% with Neo-Cobefrin®]) be used with caution.

Dental Health Professional Considerations

See Local Anesthetic/Vasoconstrictor Precautions

Effects on Dental Treatment

No significant effects or complications reported

Effects on Bleeding

No information available to require special precautions

Related Information

Oral Medications That Should Not Be Crushed or Altered

Index Terms

Alfuzosin HCl; Alfuzosin Hydrochloride

FDA Approval Date

June 12, 2003

References

Agrawal M, Gupta M, Gupta A, et al, “Prospective Randomized Trial Comparing Efficacy of Alfuzosin and Tamsulosin in Management of Lower Ureteral Stones,” Urology, 2009, 73(4):706-9.[PubMed 19193417]

Ahmed AF and 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):193-7.[PubMed 20414396]

Gurbuz MC, Polat H, Canat L, et al, “Efficacy of Three Different Alpha 1-Adrenergic Blockers and Hyoscine N-butylbromide for Distal Ureteral Stones,” Int Braz J Urol, 2011, 37(2):195-202.[PubMed 21557836]

Uroxatral (alfuzosin) [prescribing information]. St. Michael, Barbados: Concordia Pharmaceuticals Inc; August 2015.

Xatral (alfuzosin) [product monograph]. Laval, Quebec, Canada: Sanofi-aventis Canada Inc; January 2019.

Brand Names: International

Alfasin XR (BD); Alfirum (UA); Alfron XL (KR); Alfsin XL (KR); Alfu (IE); Alfu-Kal XL (IL); Alfumax (BD); Alfunar (DE); Alfurix XL (KR); Alfusin (IN); Alfutor ER (ZW); Alfuzo XL (TW); Alfuzon XL (KR); Alfuzostad (CZ); Alsiful S.R. (VN); Apo-Alfuzosin (SG); Azosin SR (TW); Benestan (PT); Benestan OD (PT); Benprostex (EG); Besavar (GB); Bundisarin (NL); Dalfaz (AR, ES, PL, RU); Danafusin (DK, SE); Flotral (LB, PE, VN); Fozal (PH); Fuzocim (AE, LB); Lafunomyl (FI, SE); Lafuzo (TW); Lura XL (KR); Mittoval (IT); Nuo Shu An (CN); Ofoxal (MT); Profuzosin (PH); Prosterol (EG); Ranfuzosin (SG); Tevax (IE); Unibenestan (ES); Urion (AT, FR); Uritab XL (ET); Uriten (BD); Uroxatral (CL); Uroxatral OD (AR, PY, UY); Uroxatral uno (CH, 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, IE, IL, IT, KE, KW, LR, MA, ML, MR, MU, MW, NE, NG, NL, PH, SA, SC, SD, SE, SL, SN, TN, TR, TZ, UG, VN, ZA, ZM, ZW); Xatral LP (BG, FR, HK, RO); 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, SG, SK, TR); Xatral XL (AE, BH, EG, IL, JO, KR, KW, LB, MT, QA, TH, TR, TW); XAtral XL (SA); Xatral XL PR (CY); Xatral XR 10 (SG); Zapros XL (KR)

Last Updated 3/18/20

Google Sites

Report abuse