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alfuzosin (Uroxatral)

Tradename: Uroxatral (FDA approved 2003) Indications: - benign prostatic hypertrophy - may hasten passage of ureteral stones [3] Contraindications: - concurrent administration of phosphodiesterase-5 inhibitors [2] Dosage: 10 mg, titration NOT needed Pharmacokinetics: 1) bioavailability 50% with food; lower without 2) metabolized by cyt P450 3A4 Drug interactions: 1) drugs that inhibit cyt P450 3A4 (ketoconazole, ritonavir) can increase alfuzosin levels 2) phosphodiesterase-5 inhibitors (Viagra, Levitra, Cialis ...) [2] Adverse effects: 1) prolongation of QT interval (no reports of torsades) 2) abnomal ejaculation is least likely among alpha-1 blockers used for BPH 3) see tamsulosin Mechanism of action: 1) alpha-1 adrenergic receptor antagonist 2) reduces total peripheral resistance through both arterial & venous dilation 3) increases urine flow in BPH by relaxing smooth muscle tone in the bladder neck of the prostate 5) relaxes internal urethral sphincter 7) enhances glycolysis [4] - may improve glucose tolerance with long-term therapy 8) may lower risk of Parkinson's disease (RR=0.88) [4]

Interactions

drug interactions drug adverse effects (more general classes)

Related

benign prostatic hyperplasia (BPH)

General

alpha-1 adrenergic receptor antagonist; prostate-selective alpha blocker

Properties

MISC-INFO: elimination route LIVER

Database Correlations

PUBCHEM correlations

References

  1. Prescriber's Letter 10(9):53 2003
  2. Setter M. In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 29-Oct 2, 2004
  3. Pedro RN et al Alfuzosin stone expulsion therapy for distal ureteral calculi: a double-blind, placebo controlled study. J Urol. 2008 Jun;179(6):2244-7; discussion 2247. PMID: 18423747
  4. Simmering JE, Welsh MJ, Liu L et al Association of Glycolysis-Enhancing alpha-1 Blockers With Risk of Developing Parkinson Disease. JAMA Neurol. 2021;78(4):407-413. Feb 1. PMID: 33523098 PMCID: PMC7851758 Free PMC article https://jamanetwork.com/journals/jamaneurology/fullarticle/2775976