2013, Number 1
Rodríguez-Wong U, Ocharán-Hernández ME, Toscano-Garibay J, Garrido-Acosta O, Anguiano-Robledo L, Cruz-Rico J, Ruiz-Pérez NJ, Sánchez-Navarrete J, Pérez-Cruz E, Montes-Vera MR
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ABSTRACTDiltiazem is a calcium antagonist that inhibits both slow calcium channel activity in vascular smooth muscle and cardiac muscle, as well as the release of calcium stored in the sarcoplasmic reticulum. Although the liver is recognized as the major site responsible for the metabolism of this drug, there is little information regarding the role of other organs in the biotransformation of diltiazem and its metabolites. The presence of cytochrome P-450 and other biotransforming enzymes in many other organs suggests that extrahepatic tissues contribute to the biotransformation of endogenous and exogenous substrates. In vitro studies have demonstrated that the cytochrome P-450 metabolism necessary for diltiazem and metabolites are present not only in the liver but also in organs such as intestine, kidney and lungs.