ALFUZOSIN HYDROCHLORIDE
Clinical safety rating
cautionComprehensive clinical and safety monograph for ALFUZOSIN HYDROCHLORIDE (ALFUZOSIN HYDROCHLORIDE).
Selective antagonist of postsynaptic alpha-1 adrenergic receptors in the prostate, bladder base, and prostatic urethra, leading to smooth muscle relaxation and improved urine flow.
| Metabolism | Extensively metabolized in the liver, primarily via CYP3A4, to inactive metabolites. |
| Excretion | Primarily hepatic metabolism (CYP3A4); 11% renal excretion as unchanged drug; 69% fecal elimination (biliary), 24% urinary (total). |
| Half-life | Terminal elimination half-life: 5-7 hours in patients with benign prostatic hyperplasia; 7-10 hours in elderly; prolonged in hepatic impairment. |
| Protein binding | 82-90% bound to human serum albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Approximately 2.5-3.2 L/kg; indicates extensive extravascular distribution. |
| Bioavailability | Oral immediate-release: 64% (first-pass metabolism); extended-release: 49% relative to immediate-release. |
| Onset of Action | Oral: 1-2 hours for symptomatic improvement in urinary flow; maximum effect at 6-8 hours. |
| Duration of Action | 24 hours for once-daily extended-release formulation; clinical improvement sustained with regular dosing. |
| Molecular Weight | 425.9 |
10 mg orally once daily immediately after the same meal each day. Extended-release tablet.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | For CrCl 30-49 mL/min: 10 mg once daily; for CrCl <30 mL/min: contraindicated. |
| Liver impairment | Child-Pugh A: 10 mg once daily; Child-Pugh B or C: contraindicated. |
| Pediatric use | Not established; safety and efficacy in children <18 years have not been studied. |
| Geriatric use | No specific dose adjustment recommended; monitor for orthostatic hypotension and dizziness. |
| 1st trimester | Limited human data; animal studies show no teratogenicity. Use only if clearly needed. |
| 2nd trimester | Limited human data; no known fetal risk. Caution advised. |
| 3rd trimester | Risk of hypotension and syncope in mother; may cause fetal hypoxia. Avoid near term. |
Clinical note
Comprehensive clinical and safety monograph for ALFUZOSIN HYDROCHLORIDE (ALFUZOSIN HYDROCHLORIDE).
| Placental transfer | Unknown; molecular weight suggests possible placental transfer, but no data available. |
| Breastfeeding | Excretion into breast milk is unknown. Due to potential for adverse effects in infants (hypotension), caution is advised. Consider alternative agents or discontinue breastfeeding. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | Alfuzosin hydrochloride is classified as FDA Pregnancy Category B. Animal studies have not shown teratogenic effects, but there are no adequate and well-controlled studies in pregnant women. First trimester: no evidence of fetal harm from animal data. Second and third trimesters: potential risk of maternal hypotension affecting uteroplacental perfusion; limited human data available. |
| Fetal Monitoring | Monitor maternal blood pressure and heart rate for hypotension and reflex tachycardia. Assess fetal heart rate if maternal hypotension occurs. In late pregnancy, monitor for signs of preterm labor or decreased fetal movements due to potential uterine relaxation effects, though not well established. |
| Fertility Effects | In animal studies, no impairment of fertility was observed. Human data are lacking; however, alpha-blockers may rarely cause ejaculatory dysfunction, which could impact male fertility. No known effect on female fertility. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to alfuzosin or any componentModerate to severe hepatic impairment (Child-Pugh class B or C)Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir)
| Precautions | Risk of hypotension, especially orthostatic hypotension, particularly with dose initiation or increase, May cause syncope, especially in patients with predisposing factors (e.g., hypovolemia, concurrent antihypertensives), Use with caution in patients with hepatic impairment, Intraoperative floppy iris syndrome (IFIS) during cataract surgery in patients on or previously treated with alpha-1 blockers, Should not be used in combination with other alpha-1 blockers |
| Food/Dietary | Take with food to reduce the risk of hypotension. Avoid grapefruit juice as it may increase alfuzosin levels. High-fat meals may alter absorption; consistency in meal timing is advised. |
| Clinical Pearls | Alfuzosin is a selective alpha-1 adrenergic antagonist used for benign prostatic hyperplasia (BPH). It has fewer cardiovascular side effects than other alpha-blockers due to its higher affinity for alpha-1a receptors in the prostate. Do not use in patients with moderate to severe hepatic impairment. Avoid use with strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir). Use with caution in patients with prolonged QT interval or on QT-prolonging drugs. Administer after the same meal each day to reduce first-dose syncope. |
| Patient Advice | Take this medication immediately after a meal at the same time each day. · Avoid situations that may cause dizziness or fainting, especially after the first dose or when increasing dose. · Do not crush, chew, or open the tablet; swallow whole. · Do not drive or operate heavy machinery until you know how the medication affects you. · Inform your doctor if you experience severe dizziness, fainting, or irregular heartbeat. · Avoid alcohol, which can increase dizziness and blood pressure-lowering effects. · Do not take with other alpha-blockers or medications for erectile dysfunction without consulting your doctor. |
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