Alfuzosin Hydrochloride

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

Introduction

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

Uses for Alfuzosin Hydrochloride

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 Hydrochloride Dosage and Administration

Administration

Oral Administration

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

Do not chew or crush tablets.¹

Dosage

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

Adults

BPH

Oral

10 mg daily.¹

Cautions for Alfuzosin Hydrochloride

Contraindications

• 
  

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

  
  


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

  
  


• 
  

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

  
  

Warnings/Precautions

Warnings

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

Pregnancy

Category B.¹

Not indicated for use in women.¹

Lactation

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 Hydrochloride

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

Drug	Interaction	Comment
α1-Adrenergic blocking agents	Possible pharmacokinetic and pharmacologic interactions1	Concomitant use not recommended1
Atenolol	Increased plasma atenolol and alfuzosin concentrations; reductions in blood pressure and heart rate1
Cimetidine	Increased plasma alfuzosin concentrations1
Digoxin	Pharmacokinetic interaction unlikely1
Diltizem	Increased plasma alfuzosin concentrations1
Hydrochlorothiazide	Pharmacokinetic interaction unlikely1
Hypotensive agents	Potential for hypotension1
Itraconazole	Increased plasma alfuzosin concentrations1	Concomitant use contraindicated1
Ketoconazole	Increased plasma alfuzosin concentrations1	Concomitant use contraindicated1
Ritonavir	Increased plasma alfuzosin concentrations1	Concomitant use contraindicated1
Warfarin	Pharmacologic interaction unlikely1

Alfuzosin Hydrochloride Pharmacokinetics

Absorption

Bioavailability

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

Food

Food increases extent of absorption by 50%.¹

Distribution

Plasma Protein Binding

82–90%.¹

Elimination

Metabolism

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

Half-life

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

Stability

Storage

Oral

Tablets

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

ActionsActions

• 
  

  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.)

  
  

Preparations

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

Alfuzosin Hydrochloride

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets, extended-release	10 mg	Uroxatral (with povidone)	Sanofi-Synthelabo

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Uroxatral 10MG 24-hr Tablets (SANOFI-AVENTIS U.S.): 30/$142.99 or 90/$395.97

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions April 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

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. [PubMed 11893233]

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. [PubMed 12887479]

4. Lee M. Alfuzosin hydrochloride for the treatment of benign prostatic hyperplasia. Am J Health Syst Pharm. 2003; 60:1426-39. [IDIS 500185] [PubMed 12892027]

5. Chapple C. Medical treatment for benign prostatic hyperplasia. BMJ. 1992; 304:1198-9. [IDIS 296671] [PubMed 1381250]

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. [PubMed 1695785]

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. [PubMed 11744466]

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. [PubMed 10720857]

10. Anon. Alfuzosin (Uroxatral)--another alpha₁-blocker for benign prostatic hyperplasia. Med Lett Drugs Ther. 2004; 46:1-2. [PubMed 14691408]

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. [PubMed 7508331]

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. [PubMed 9352699]

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.

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