alfuzosin (Uroxatral)
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Introduction
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
- bioavailability 50% with food; lower without
- metabolized by cyt P450 3A4
elimination via liver
Adverse effects
- prolongation of QT interval (no reports of torsades)
- abnomal ejaculation is least likely among alpha-1 blockers used for BPH
- see tamsulosin
- drug adverse effects of alpha-1 adrenergic receptor antagonists
- drug adverse effects of antihypertensive agents
Drug interactions
- drugs that inhibit cyt P450 3A4 (ketoconazole, ritonavir) can increase alfuzosin levels
- phosphodiesterase-5 inhibitors (Viagra, Levitra, Cialis ...)[2]
- drug interaction(s) of phosphodiesterase-5-inhibitors with alpha-1-adrenergic receptor antagonists
- drug interaction(s) of loop diuretics with alpha-1 adrenergic receptor antagonist
- drug interaction(s) of NSAIDs & antihypertensives
Mechanism of action
- alpha-1 adrenergic receptor antagonist
- reduces total peripheral resistance through both arterial & venous dilation
- increases urine flow in BPH by relaxing smooth muscle tone in the bladder neck of the prostate
- relaxes internal urethral sphincter
- enhances glycolysis[4]
- may improve glucose tolerance with long-term therapy
- may lower risk of Parkinson's disease (RR=0.88)[4]
More general terms
Additional terms
References
- ↑ Prescriber's Letter 10(9):53 2003
- ↑ 2.0 2.1 2.2 Setter M. In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 29-Oct 2, 2004
- ↑ 3.0 3.1 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: https://www.ncbi.nlm.nih.gov/pubmed/18423747
- ↑ 4.0 4.1 4.2 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: https://www.ncbi.nlm.nih.gov/pubmed/33523098 PMCID: PMC7851758 Free PMC article https://jamanetwork.com/journals/jamaneurology/fullarticle/2775976