Monograph
G04CA02 - Tamsulosin |
Propably not porphyrinogenic |
PNP |
Rationale
Tamsulosin is not suspected to be an inducer or a mechanism-based inhibitor of CYP enzymes, and is not observed to alter the metabolism of other CYP metabolized drugs.
Chemical description
Alpha1-adrenoceptor antagonist, sulphamoyl phenethylamine derivative
Therapeutic characteristics
Tamsulosin is indicated for lower urinary tract symptoms associated with benign prostate hyperplasia. It is administered orally.
Hepatic exposure
The maximal plasma concentration of tamsulosin is about 16 ng/ml, which is equivalent to 40 nM (Franco-Salinas 2010).
Metabolism and pharmacokinetics
Tamsulosin is metabolized by CYP3A4 and CYP2D6 (Kamimura 1998).
Tamsulosin has not been found to be an inhibitor of CYP1A2 (Miyazawa 2002), CYP2C9 (Rolan 2003), or CYP2D6 and CYP3A4 (Modi 2008).
In the literature tamsulosin is not reported to be an inducer or inhibitor of any of the quantitatively major CYP enzymes and the absence of such characteristics is also in accordance with review-papers (FDA, Hisaka 2010, Isoherranen 2009 and Pelkonen 2008). No drug-drug interaction with tamsulosin as a perpetrator has been reported in the literature.
IPNet drug reports
Uneventful use reported in 7 patients with acute porphyria.
References
| # |
Citation details |
PMID |
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| * | Scientific articles |
| 1. |
Franco-Salinas G1, de la Rosette JJ, et al. Pharmacokinetics and pharmacodynamics of tamsulosin in its modified-release and oral controlled absorption system formulations.
Clin Pharmacokinet. 2010 Mar;49(3):177-88. |
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| 2. |
Hisaka, A., Y. Ohno, et al. (2010). "Prediction of pharmacokinetic drug-drug interaction caused by changes in cytochrome P450 activity using in vivo information." Pharmacol Ther 125(2): 230-248.
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| 3. |
Isoherranen, N., H. Hachad, et al. (2009). "Qualitative analysis of the role of metabolites in inhibitory drug-drug interactions: literature evaluation based on the metabolism and transport drug interaction database." Chem Res Toxicol 22(2): 294-298.
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| 4. |
Pelkonen, O., M. Turpeinen, et al. (2008). "Inhibition and induction of human cytochrome P450 enzymes: current status." Arch Toxicol 82(10): 667-715.
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| 5. |
Identification of cytochrome P450 isozymes involved in metabolism of the alpha1-adrenoceptor blocker tamsulosin in human liver microsomes.
Kamimura H, Oishi S, et al. Xenobiotica. 1998 Oct;28(10):909-22. |
9849639 |
| 6. |
Effects of the concomitant administration of tamsulosin (0.8 mg/day) on the pharmacokinetic and safety profile of theophylline (5 mg/kg): a placebo-controlled evaluation.
Miyazawa Y, Starkey LP, et al. J Int Med Res. 2002 Jan-Feb;30(1):34-43. |
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| 7. |
Effect of dapoxetine on the pharmacokinetics and hemodynamic effects of tamsulosin in men on a stable dose of tamsulosin.
Modi NB, Kell S, et al. J Clin Pharmacol. 2008 Dec;48(12):1438-50. |
18832488 |
| 8. |
A placebo-controlled pharmacodynamic and pharmacokinetic interaction study between tamsulosin and acenocoumarol.
Rolan P, Terpstra IJ, et al. Br J Clin Pharmacol. 2003 Mar;55(3):314-6. |
12630984 |
| * | Government bodies |
| 9. |
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| * | Drug interaction databases |
| 10. |
U.S.FoodandDrugAdministration (FDA). (27.10.2014). "Drug Developement and Drug Interactions: Table of Substrates, Inhibitors and Inducers." Retrieved 09.03.2015, from
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