What is the use of Alfuzosin (alpha-1 adrenergic receptor blocker)?

From the Guidelines

Alfuzosin is an alpha-1 adrenergic receptor blocker primarily used to treat benign prostatic hyperplasia (BPH) symptoms in men, with a standard dosage of 10 mg once daily, taken after the same meal each day, as recommended by the AUA guideline on management of BPH 1. The use of alfuzosin is based on the hypothesis that clinical BPH is partly caused by alpha1-adrenergic-mediated contraction of prostatic smooth muscle, resulting in bladder outlet obstruction, and alfuzosin inhibits this process, thus relieving the bladder outlet obstruction 1. Key benefits of alfuzosin include:

• Relaxing the smooth muscles in the prostate and bladder neck, which improves urine flow and reduces symptoms like frequent urination, urgency, weak stream, and nighttime urination
• Less impact on blood pressure compared to other alpha blockers, and does not typically require dose titration
• Improvement in urinary symptoms typically begins within a few days, though full benefits may take 2-4 weeks to develop However, potential side effects and considerations include:
• Dizziness, headache, and postural hypotension, especially when starting treatment
• Patients should avoid suddenly standing up to minimize dizziness risk
• Should not be used in patients with severe liver impairment or alongside other alpha blockers
• Patients taking medications for erectile dysfunction should exercise caution due to potential additive blood pressure-lowering effects It is also important to note that combination therapy with a 5 alpha-reductase inhibitor may be considered for patients with LUTS associated with demonstrable prostatic enlargement, as it has been found to be more effective in relieving and preventing the progression of symptoms than alpha-blocker monotherapy in long-term studies 1.

From the FDA Drug Label

Alfuzosin is a selective antagonist of post-synaptic alpha1-adrenoreceptors, which are located in the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra. The symptoms associated with benign prostatic hyperplasia (BPH) such as urinary frequency, nocturia, weak stream, hesitancy and incomplete emptying are related to two components, anatomical (static) and functional (dynamic). Blockade of these adrenoreceptors can cause smooth muscle in the bladder neck and prostate to relax, resulting in an improvement in urine flow and a reduction in symptoms of BPH

The use of Alfuzosin, an alpha-1 adrenergic receptor blocker, is to improve symptoms of Benign Prostatic Hyperplasia (BPH), such as:

• Urinary frequency
• Nocturia
• Weak stream
• Hesitancy
• Incomplete emptying by relaxing the smooth muscle in the bladder neck and prostate, resulting in an improvement in urine flow and a reduction in symptoms of BPH 2

From the Research

Use of Alfuzosin

• Alfuzosin is a functionally uroselective alpha 1-adrenergic antagonist indicated for the management of moderate to severe benign prostatic hyperplasia (BPH) 3, 4, 5.
• It can improve urinary voiding symptoms and increase urinary flow rates while causing few cardiovascular adverse effects 3, 4.
• Alfuzosin has been shown to improve patients' perception of quality of life, allowing patients to increase their physical activities and improve their ability to handle day-to-day activities 3.

Administration and Dosage

• The usual dose of alfuzosin for patients with BPH is 2.5 mg twice or thrice daily of the immediate-release (IR) formulation or 5 mg of extended-release (ER) alfuzosin twice daily or 10 mg of ER alfuzosin once daily 3.
• No dosage titration is needed for ER alfuzosin, and its onset of peak action is within days of the start of treatment 3, 4, 6.
• The once-daily formulation of alfuzosin 10mg is well tolerated and causes fewer vasodilatory adverse events than immediate-release alfuzosin 2.5mg three times daily 4, 6.

Efficacy and Safety

• Alfuzosin has been shown to be effective in improving lower urinary tract symptoms and relieving bladder outlet obstruction in patients with BPH 4, 5, 7.
• The benefits of alfuzosin have been confirmed in general practice, with a 51% reduction in mean total symptom score and a 56% decrease in mean irritative symptoms 5.
• Alfuzosin has a good safety profile, with a low risk of first-dose effect and postural symptoms related to orthostatic hypotension 5, 7.
• Central nervous system effects are also limited due to poor penetration of the blood-brain barrier 5.