Alfuzosin is a post-synaptic α1-adrenergic receptor antagonist commonly used to improve lower urinary tract symptoms associated with benign prostatic hyperplasia (BPH).1,2 It displays high-affinity with non-selectivity for the three known human α1 adrenoceptors (pKi = 8.0, 8.0, and 8.5 for α1A, α1B, and α1D, respectively).3Consistent with a role for α1 adrenoceptors in mediating contraction of smooth muscle, alfuzosin was first described as having anti-hypertensive effects with peripheral vasodilator properties.1 In patients with BPH, alfuzosin increases mean urinary flow rate and decreases residual volume.2 Alfuzosin produces minimal vasodilatory and sexual function side effects.4,5,6
1
Sinclair, A.J., Davies, I.B., and Warrington, S.J. Alfuzosin and the venous reflex response: Studies in normal subjects. Br J Clin Pharmacol 27 19-22 (1989).
2
Jardin, A., Bensadoun, H., Delauche-Cavallier, M.C., et al. Alfuzosin for treatment of benign prostatic hypertrophy. Lancet 337 1457-1461 (1991).
3
Kenny, B.A., Miller, A.M., Williamson, I.J.R., et al. Evaluation of the pharmacological selectivity profile of α1 adrenoceptor antagonists at prostatic α1 adrenoceptors: Binding, functional and in vivo studies. Br J Pharmacol 118 871-878 (1996).
4
Roehrborn, C.G., and Rosen, R.C. Medical therapy options for aging men with benign prostatic hyperplasia: Focus on alfuzosin 10 mg once daily. Clin Interv Aging 3(3) 511-524 (2008).
5
Nickel, J.C., Sander, S., and Moon, T.D. A meta-analysis of the vascular-related safety profile and efficacy of α-adrenergic blockers for symptoms related to benign prostatic hyperplasia. Int J Clin Pract 62(10) 1547-1559 (2008).
6
Michel, M.C. The forefront for novel therapeutic agents based on the pathophysiology of lower urinary tract dysfunction: α-blockers in the treatment of male voiding dysfunction - how do they work and why do they differ in tolerability? J Pharmacol Sci 112 151-157 (2010).