Vol.:(0123456789) Drugs & Therapy Perspectives https://doi.org/10.1007/s40267-019-00611-1 REVIEW ARTICLE Tamsulosin in urology: beyond benign prostatic hyperplasia G. G. Laxman Prabhu 1  · Hiren Prajapati 2  · Alok Chaturvedi 2  · Nilanj Dave 2  · Amit B. Jain 2 © Springer Nature Switzerland AG 2019 Abstract Tamsulosin, a third-generation uroselective α 1A adrenergic receptor blocker (antagonist), has been approved for the treatment of signs and symptoms of benign prostatic hyperplasia for more than two decades. Apart from this approved use, more recent evidence has been published regarding the of-label use of tamsulosin in various other urological conditions. However, further research is needed regarding the use of tamsulosin in these indications. This review highlights the possible therapeutic uses of tamsulosin for the management of various urological conditions. Introduction Tamsulosin is third-generation uroselective α 1A adrenergic receptor blocker (antagonist) [1]. Initially marketed in Japan as an immediate-release formulation, a modifed delayed- release formulation of tamsulosin was later developed, which provides a more consistent release of tamsulosin over the dosing interval [2]. This modifed-release formula- tion was approved by the US Food and Drug Administration (FDA) in 1997 for the treatment of benign prostatic hyper- plasia (BPH) [3], the prevalence of which increases with age (i.e. from 25% in men aged 40–49 years up to 80% in men aged 70–79 years) [4]. Many studies have been published on the efcacy and safety of tamsulosin for the treatment of BPH. Apart from its approved indication, tamsulosin has also been used of-label in many other urological conditions (Fig. 1). This review highlights the potential uses of tamsu- losin beyond BPH. Pharmacology of tamsulosin Mechanism of action Tamsulosin is a subtype-selective α 1A and α 1D adrenoceptor blocker. The former receptors predominate (≈  70%) in the prostate gland, prostatic capsule, prostatic urethra and blad- der. Relaxation of the prostate and bladder smooth muscle is associated with improved maximal urine fow and alleviation of lower urinary tract symptoms (LUTS) in patients with BPH [5]. The starting dosage of oral tamsulosin for BPH management is 0.4 mg once daily with food; this dosage can be increased to 0.8 mg once daily in patients who fail to respond to the 0.4 mg dose after 2–4 weeks of administra- tion [3]. Pharmacokinetics The pharmacokinetics of tamsulosin hydrochloride have been studied in both adult healthy volunteers and patients with BPH after single and/or multiple doses ranging from 0.1 to 1 mg (Table 1) [3]. Therapeutic uses of tamsulosin In addition to the approved indication of BPH, tamsulosin has been used of-label in several urological conditions. * G. G. Laxman Prabhu gglaxman@gmail.com * Hiren Prajapati hiren_prajapati@intaspharma.com Alok Chaturvedi alok_chaturvedi@intaspharma.com Nilanj Dave nilanj_dave@intaspharma.com Amit B. Jain amitb_jain@intaspharma.com 1 Department of Urology, KMC Hospital, Mangalore, Karnataka, India 2 Department of Medical Afairs, Intas Pharmaceuticals Limited, Ahmedabad, Gujarat, India