药代动力学与实验治疗学杂志

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Pharmacokinetics of Olanzapine: A Comprehensive Review

Dam Arkin

Olanzapine is a widely prescribed antipsychotic medication used in the management of various psychiatric disorders, including schizophrenia and bipolar disorder. Understanding the pharmacokinetics of olanzapine is crucial for optimizing dosing strategies, predicting drug interactions, and ensuring therapeutic efficacy and safety.This review aims to provide a comprehensive overview of the pharmacokinetic profile of olanzapine, including its absorption, distribution, metabolism, and elimination. Olanzapine is primarily administered orally and is rapidly and extensively absorbed from the gastrointestinal tract. Its bioavailability is high, reaching approximately 60-65% due to first-pass metabolism. Food intake does not significantly affect its absorption. Once absorbed, olanzapine exhibits a large volume of distribution, indicating extensive tissue distribution. It binds extensively to plasma proteins, mainly albumin, which may influence its pharmacokinetic interactions with other highly protein-bound drugs. Olanzapine is metabolized primarily in the liver by the cytochrome P450 enzyme system, mainly CYP1A2, resulting in the formation of multiple metabolites. These metabolites, including N-desmethyl-olanzapine and 2-hydroxy-olanzapine, exhibit pharmacological activity but are generally less potent than the parent compound.