ALFUZOSIN

ALFUZOSIN
(al-fuz'o-sin)
UroXatral, Xatral 
Classifications: alpha-adrenergic antagonist;
Therapeutic: antagonist of alpha-1 receptors

Prototype: Prazosin
Pregnancy Category: B

Availability

10 mg extended-release tablet

Action

Alfuzosin is a short-acting, selective antagonist at alpha-1 receptors with a low incidence of hypotension and sexual dysfunction at therapeutic doses. Alpha-1 receptors cause contraction of smooth muscle in the prostate, prostatic capsule, prostatic urethra, bladder base, and bladder neck. Both alpha-1a (70%) and alpha-1b receptors exist in the prostate.

Therapeutic Effect

Blockade of alpha-1 receptors by alfuzosin causes smooth muscles in the bladder neck and prostate to relax, thereby reducing pressure on the urethra and improving urine flow rate. This results in a reduction in BPH symptoms.

Uses

Treatment of symptomatic benign prostatic hypertrophy (BPH).

Contraindications

Hypersensitivity to alfuzosin; severe hepatic insufficiency; concurrent treatment with potent CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, and ritonavir); angina; QT prolongation.

Cautious Use

Coronary artery disease, cardiac arrhythmias; hepatic disease; dizziness, light-headedness, orthostatic hypotension; pregnancy (category B).

Route & Dosage

Benign Prostatic Hypertrophy
Adult: PO 10 mg q.d.

Administration

Oral
  • Give immediately after same meal each day.
  • Ensure that extended-release tablet is not crushed or chewed. It must be swallowed whole.
  • Store at 15°–30° C (59°–86° F). Protect from light and moisture.

Adverse Effects (≥1%)

Body as a Whole: Fatigue, pain. CNS: Dizziness, headache. GI: Abdominal pain, dyspepsia, constipation, nausea. Respiratory: Upper respiratory infection, bronchitis, sinusitis, pharyngitis. Urogenital: Impotence, priapism.

Interactions

Drug: Increased risk of hypotension with other antihypertensive agents or sildenafil, vardenafil, and tadalafil; ketoconazole, itraconazole, protease inhibitors may increase alfuzosin levels and toxicity.

Pharmacokinetics

Absorption: 49% when taken with food. Peak: 8 h. Metabolism: In liver by CYP3A4. Elimination: 69% in feces, 24% in urine. Half-Life: 10 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor CV status and BP, especially if on concurrent treatment with antihypertensive drugs or inhibitors of CYP3A4. See INTERACTIONS.
  • Check postural vital signs to evaluate for orthostatic hypotension within a few hours following administration.
  • Withhold drug and report new or worsening angina to physician.
  • Lab tests: Baseline and periodic LFTs.

Patient & Family Education

  • Inform physician about all other prescription, nonprescription, or herbal drugs being taken.
  • Make position changes slowly to minimize dizziness.
  • Do not drive or engage in other hazardous activities until reaction to drug is known.
  • Moderate or eliminate grapefruit juice consumption while on this drug.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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© 2006-2017 medpill.info Last Updated On: 10/11/2017 (0.01)
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