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Amiodarone is also safe to use in individuals with cardiomyopathy and atrial fibrillation, to maintain normal sinus rhythm. Amiodarone prolongation of the action potential is uniform over a wide range of heart rates, so this drug does not have reverse use-dependent action. Amiodarone was the first agent described in this class. [4]
"Indiana University Department of Medicine Clinical Pharmacology Drug Interactions Flockhart Table ™". "INHIBITORS, INDUCERS AND SUBSTRATES OF CYTOCHROME P450 ISOZYMES". "The Life Raft Group: Long List of Inhibitors and Inducers of CYP3A4 and CYP2D6". "DRUGBANK Online: Cytochrome P-450 Enzyme Inhibitors".
Amiodarone is an antiarrhythmic medication used to treat and prevent a number of types of cardiac dysrhythmias. [4] This includes ventricular tachycardia, ventricular fibrillation, and wide complex tachycardia, atrial fibrillation, and paroxysmal supraventricular tachycardia. [4]
Budiodarone (ATI-2042) is an antiarrhythmic agent and chemical analog of amiodarone that is currently being studied in clinical trials.Amiodarone is considered the most effective antiarrhythmic drug available, [1] [2] [3] but its adverse side effects, including hepatic, pulmonary and thyroid toxicity as well as multiple drug interactions, [4] are discouraging its use.
Effects on P450 isozyme activity are a major source of adverse drug interactions, since changes in P450 enzyme activity may affect the metabolism and clearance of various drugs. For example, if one drug inhibits the P450-mediated metabolism of another drug, the second drug may accumulate within the body to toxic levels.
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Following is a table of selected substrates, inducers and inhibitors of CYP1A2. Inhibitors of CYP1A2 can be classified by their potency , such as: Strong inhibitor being one that causes at least a 5-fold increase in the plasma AUC values of sensitive substrates metabolized through CYP1A2, or more than 80% decrease in clearance thereof.
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