Alfuzosin Hydrochloride

Name: Alfuzosin Hydrochloride

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

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

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.)

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