Cardiovascular Safety of the Oral Controlled Absorption System (OCAS) Formulation of Tamsulosin Compared to the Modified Release (MR) Formulation

Aims: Tamsulosin, a superselective subtype alpha 1a and 1d blocker, is used for the treatment of male Lower Urinary Tract Symptoms (LUTS) commonly caused by Benign Prostatic Hyperplasia (BPH). This prospective study evaluated the efficacy and safety of a new formulation, Tamsulosin OCAS® (Oral Controlled Absorption System), for LUTS associated with BPH in Thai patients. Materials and Methods: Fifty one patients over 40 years old with complaints of LUTS associated with BPH were recruited. Patients received an 8 week course of once daily 0.4 mg tamsulosin OCAS®, and were followed up at 2 (visit 3), 4 (visit 4) and 8 (visit 5) weeks post-treatment. At each visit, patients were assessed using the International Prostate Symptom Score (IPSS), Nocturia Quality of Life (N-QoL) Questionnaire, QoL Assessment Index (IPSS-QoL), and International Index of Erectile Function (IIEF). The primary outcome was efficacy of Tamsulosin. The secondary outcomes included change in the mean number of nocturia episodes, hours of undisturbed sleep (HUS) and uroflowmetry measurements. Results: Total IPSS significantly decreased at week 8 from baseline (from 19.52 to 6.08; p < 0.001). Similarly, the voiding and storage subscores of IPSS also continued to improve significantly starting from the second and third visits, respectively (p < 0.001 versus baseline). The IPSS-QoL and N-QoL scores significantly improved at visit 3 through end of study. In addition, we observed significant nocturia and HUS improvement in their last clinic visit. Uroflowmetry parameters, Q max and Q ave , improved significantly at 3 rd clinic visit . Three patients experienced mild dizziness. Conclusion: Tamsulosin OCAS® treatment led to significant improvements in LUTS, HUS and QoL in Thai patients with bladder outlet obstruction from BPH with few side effects.

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“…The randomized crossover study concluded that Tamsulosin OCAS® had a lower incidence of positive stress test than conventional Tamsulosin (15).…”

Section: Discussionmentioning

confidence: 99%

The efficacy and safety of oral Tamsulosin controlled absorption system (OCAS) for the treatment of lower urinary tract symptoms due to bladder outlet obstruction associated with benign prostatic hyperplasia: an open-label preliminary study

Lojanapiwat

Permpongkosol

2011

Int. braz j urol.

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“…In both studies blood samples for PK were withdrawn before and at 1,2,3,4,5,6,7,8,10,12,14,24,30,36 and 48 h after tamsulosin HCl administration. Paroxetine sparse sampling was performed before and at 3, 5 and 8 h after tamsulosin HCl administration.…”

Section: Methodsmentioning

confidence: 99%

Effects of strong CYP2D6 and 3A4 inhibitors, paroxetine and ketoconazole, on the pharmacokinetics and cardiovascular safety of tamsulosin

Troost

Tatami

Tsuda

et al. 2011

Brit J Clinical Pharma

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WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT• Tamsulosin metabolism involves both CYP2D6 and 3A4. However, data on potential drug-drug interactions between tamsulosin and inhibitors of CYP2D6 and 3A4 are limited and information on potential pharmacodynamic consequences of such pharmacokinetic interactions is missing. WHAT THIS STUDY ADDS• This study provides information on the drug-drug interactions of tamsulosin with strong CYP2D6 and strong CYP3A4 inhibitors after single dose administration in healthy subjects. AIMTo determine the effect of the strong CYP2D6 inhibitor paroxetine and strong CYP3A4 inhibitor ketoconazole on the pharmacokinetics and safety (orthostatic challenge) of tamsulosin. METHODSTwo open-label, randomized, two-way crossover studies were conducted in healthy male volunteers (extensive CYP2D6 metabolizers). RESULTSCo-administration of multiple oral doses of 20 mg paroxetine once daily with a single oral dose of the 0.4 mg tamsulosin HCl capsule increased the adjusted geometric mean (gMean) values of Cmax and AUC(0,•) of tamsulosin by factors of 1.34 (90% CI 1.21, 1.49) and 1.64 (90% CI 1.44, 1.85), respectively, and increased the terminal half-life (t1/2) of tamsulosin HCl from 11.4 h to 15.3 h. Co-administration of multiple oral doses of 400 mg ketoconazole once dailywith a single oral dose of the 0.4 mg tamsulosin increased the gMean values of Cmax and AUC(0,•) of tamsulosin by a factor of 2.20 (90% CI 1.96, 2.45) and 2.80 (90% CI 2.56, 3.07), respectively. The terminal half-life was slightly increased from 10.5 h to 11.8 h. These pharmacokinetic changes were not accompanied by clinically significant alterations of haemodynamic responses during orthostatic stress testing. CONCLUSIONThe exposure to tamsulosin is increased upon co-administration of strong CYP2D6 inhibitors and even more so of strong 3A4 inhibitors, but neither PK alteration was accompanied by clinically significant haemodynamic changes during orthostatic stress testing.

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“…Safety studies showed that tamsulosin OCAS has a better cardiovascular safety profile than conventional formulations currently available, also in situations that stress the cardiovascular system, and in older patients [12–14]. Probably, this is because tamsulosin OCAS has a lower C max and its PKs do not depend on food intake.…”

Section: Discussionmentioning

confidence: 99%

Introduction and summary

Kerrebroeck

2006

BJU International

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Cardiovascular Safety of the Oral Controlled Absorption System (OCAS) Formulation of Tamsulosin Compared to the Modified Release (MR) Formulation

Cited by 28 publications

References 14 publications

The efficacy and safety of oral Tamsulosin controlled absorption system (OCAS) for the treatment of lower urinary tract symptoms due to bladder outlet obstruction associated with benign prostatic hyperplasia: an open-label preliminary study

The efficacy and safety of oral Tamsulosin controlled absorption system (OCAS) for the treatment of lower urinary tract symptoms due to bladder outlet obstruction associated with benign prostatic hyperplasia: an open-label preliminary study

Effects of strong CYP2D6 and 3A4 inhibitors, paroxetine and ketoconazole, on the pharmacokinetics and cardiovascular safety of tamsulosin

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