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Class: Selective alpha-1-Adrenergic Blocking Agents
VA Class: HS900
Chemical Name: N-[3-[(4-Amino-6,7-dimethoxy-2-quinazolinyl)methylamino]propyl]tetrahydro-2-furancarboxamide monohydrochloride
Molecular Formula: C19H27N5O4•HCl
CAS Number: 81403-68-1
Brands: Uroxatral

Medically reviewed by Last updated on March 23, 2020.


α1-Adrenergic blocker; quinazoline derivative;1 2 structurally and pharmacologically related to prazosin.1 2 3

Uses for Alfuzosin

Benign Prostatic Hyperplasia (BPH)

Reduction of urinary obstruction and relief of associated manifestations (e.g., hesitancy, interrupted or weak stream, sensation of incomplete bladder emptying or straining, urgency, nocturia) in patients with symptomatic BPH.1 2 3

Although drug therapy usually is not as effective as surgical therapy, it may provide adequate symptomatic relief with fewer and less serious adverse effects compared with surgery.14

May consider combined therapy with an α1-adrenergic blocker and 5α-reductase inhibitor for men with bothersome moderate to severe BPH and demonstrable prostatic enlargement.14 Has been more effective than therapy with either drug alone in preventing long-term BPH symptom progression.14 Men at risk for BPH progression are most likely to benefit from combination therapy.14

Other Uses

Manufacturer states that alfuzosin should not be used for the treatment of hypertension.1

Alfuzosin Dosage and Administration


Oral Administration

Administer orally once daily immediately after the same meal each day.1

Do not chew or crush tablets.1


Available as alfuzosin hydrochloride; dosage is expressed in terms of the salt.1



10 mg daily.1

Cautions for Alfuzosin


  • Moderate or severe hepatic impairment (Child-Pugh class B or C).1

  • Concomitant use with potent inhibitors of CYP3A4 (e.g., itraconazole, ketoconazole, ritonavir).1

  • Known hypersensitivity to alfuzosin or any ingredient in the formulation.1



Postural Hypotension

Potential for postural hypotension, dizziness, or syncope.1

Administer with caution in patients with symptomatic hypotension or those who have had a hypotensive response to other drugs.1

General Precautions

Prostate Cancer

Exclude possibility of prostate cancer prior to initiation of therapy.1

Intraoperative Floppy Iris Syndrome

Intraoperative floppy iris syndrome (IFIS) observed during phacoemulsification cataract surgery in some patients currently receiving or previously treated with α1-adrenergic blocking agents.1

If patient has received α1-adrenergic blockers, ophthalmologist should be prepared to modify the surgical technique (e.g., through use of iris hooks, iris dilator rings, or viscoelastic substances) to minimize complications of IFIS.1 There does not appear to be a benefit from discontinuing α1-blocker therapy prior to cataract surgery.1

Coronary Insufficiency

If new or worsening symptoms of angina pectoris occur, discontinue therapy.1

Congenital or Acquired QT-Interval Prolongation

Modest QT-interval prolongation possible.1

Consider potential for QT-interval prolongation in patients with known history of QT-interval prolongation and/or in those receiving concomitant therapy with drugs known to prolong QT interval.1

Specific Populations


Category B.1

Not indicated for use in women.1


Not indicated for use in women.1

Pediatric Use

Not indicated for use in children.1

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults.1

Hepatic Impairment

Use not recommended in patients with moderate to severe hepatic impairment.1 Not studied in patients with mild hepatic impairment.1

Renal Impairment

Use with caution in patients with severe renal impairment.1

Common Adverse Effects

Dizziness, headache, fatigue, upper respiratory tract infection.1

Interactions for Alfuzosin

Extensively metabolized by CYP3A4.1

Drugs Affecting Hepatic Microsomal Enzymes

Pharmacokinetic interaction with potent inhibitors of CYP3A4 (increased plasma alfuzosin concentrations).1 Concomitant use contraindicated.1

Specific Drugs




α1-Adrenergic blocking agents

Possible pharmacokinetic and pharmacologic interactions1

Concomitant use not recommended1


Increased plasma atenolol and alfuzosin concentrations; reductions in blood pressure and heart rate1


Increased plasma alfuzosin concentrations1


Pharmacokinetic interaction unlikely1


Increased plasma alfuzosin concentrations1


Pharmacokinetic interaction unlikely1

Hypotensive agents

Potential for hypotension1


Increased plasma alfuzosin concentrations1

Concomitant use contraindicated1


Increased plasma alfuzosin concentrations1

Concomitant use contraindicated1


Increased plasma alfuzosin concentrations1

Concomitant use contraindicated1


Pharmacologic interaction unlikely1

Alfuzosin Pharmacokinetics



Absolute bioavailability of 49% following oral administration under fed conditions.1 Peak plasma concentration attained in about 8 hours.1


Food increases extent of absorption by 50%.1


Plasma Protein Binding




Extensively metabolized in the liver via oxidation, O-demethylation, and/or N-dealkylation to form pharmacologically inactive metabolites.1

CYP3A4 is the principal hepatic isoenzyme involved in the drug’s metabolism.1

Elimination Route

Excreted in feces (69%) and urine (24%) as unchanged drug and metabolites.1


10 hours.1

Special Populations

In patient with moderate to severe hepatic impairment, plasma alfuzosin concentrations are 3- to 4-fold higher than in healthy individuals; pharmacokinetics not studied in patients with mild hepatic impairment.1

In patient with mild to severe renal impairment, AUC is 50% higher than in healthy individuals.1





25°C (may be exposed to 15–30°C).1 Protect from moisture and light.1


  • Blocks α1-adrenergic receptors in the lower urinary tract to cause relaxation of smooth muscle in the bladder neck and prostate and improve symptoms of BPH (e.g., urine flow).1

Advice to Patients

  • Risk of feeling faint or dizzy, particularly following initiation of therapy; avoid situations where injury could result if syncope occurs.1

  • Importance of exercising caution when driving or operating machinery.1

  • Importance of taking alfuzosin exactly as prescribed.1 Importance of taking alfuzosin with the same meal each day and of not chewing or crushing the tablets.1

  • Importance of advising male patients being considered for cataract surgery that they should inform their ophthalmologist of current or prior α1-blocker (e.g., alfuzosin) therapy.1

  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as concomitant illnesses.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Alfuzosin Hydrochloride


Dosage Forms


Brand Names



Tablets, extended-release

10 mg

Uroxatral (with povidone)


AHFS DI Essentials™. © Copyright 2021, Selected Revisions April 1, 2010. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.


1. Sanofi-Aventis US LLC. Uroxatral (alfuzosin hydrochloride) extended-release tablets prescribing information. New York, NY; 2006 Apr.

2. McKeage K, Plosker GL. Alfuzosin: a review of the therapeutic use of the prolonged-release formulation given once daily in the management of benign prostatic hyperplasia. Drugs. 2002; 62:633-53.

3. Roehrborn CG, Van Kerrebroeck P, Nordling J. Safety and efficacy of alfuzosin 10 mg once-daily in the treatment of lower urinary tract symptoms and clinical benign prostatic hyperplasia: a pooled analysis of three double-blind, placebo-controlled studies. BJU Int. 2003; 92:257-61.

4. Lee M. Alfuzosin hydrochloride for the treatment of benign prostatic hyperplasia. Am J Health Syst Pharm. 2003; 60:1426-39.

5. Chapple C. Medical treatment for benign prostatic hyperplasia. BMJ. 1992; 304:1198-9.

6. Lepor H. Role of long-acting selective alpha-1 blockers in the treatment of benign prostatic hyperplasia. Urol Clin North Am. 1990; 17:651-9.

7. Kirby RS. Alpha-adrenoceptor inhibitors in the treatment of benign prostatic hyperplasia. Am J Med. 1989; 87(Suppl 2A):26-30S.

8. Roehrborn CG for the ALFUS Study Group. Efficacy and safety of once-daily alfuzosin in the treatment of lower urinary tract symptoms and clinical benign prostatic hyperplasia: a randomized, placebo-controlled trial. Urology. 2001; 58:953-9.

9. van Kerrebroeck P, Jardin A, Laval KU et al., for the ALFORTI Study Group. Efficacy and safety of a new prolonged release formulation of alfuzosin 10 mg once daily versus alfuzosin 2.5 mg thrice daily and placebo in patients with symptomatic benign prostatic hyperplasia. Eur Urol. 2000; 37:306-13.

10. Anon. Alfuzosin (Uroxatral)--another alpha1-blocker for benign prostatic hyperplasia. Med Lett Drugs Ther. 2004; 46:1-2.

11. Buzelin JM, Hebert M, Blondin P et al. Alpha-blocking treatment with alfusozin in symptomatic benign prostatic hyperplasia; comparative study with prazosin. Br J Urol. 1993; 72:922-7.

12. Buzelin JM, Fonteyne E, Kontturi M et al. Comparison of tamsulosin with alfuzosin n the treatment of patients with lower urinary tract symptoms suggestive of bladder outlet obstruction (symptomatic benign prostatic hyperplasia). Br J Urol. 1997; 80:597-605.

13. Sanofi-Aventis, New York, NY: Personal communication.

14. American Urological Association. Guideline on the management of benign prostatic hyperplasia (BPH)(2003/updated 2006). Available from website. Accessed 2006 Aug 10.