Pharmacokinetic drug evaluation of opicapone for the treatment of Parkinson's disease.

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Svetel M, Tomic A, Kresojevic N, Kostic V

Pharmacokinetic drug evaluation of opicapone for the treatment of Parkinson's disease.

Expert Opin Drug Metab Toxicol. 2018 Mar;14(3):353-360. doi: 10.1080/17425255.2018.1430138. Epub 2018 Jan 24.

PubMed ID

29345156 [ View in PubMed

]

Abstract

INTRODUCTION: Opicapone (OPC) is a novel, potent, reversible, and purely peripheral third-generation COMT inhibitor, which provides an enhancement in levodopa (L-Dopa) availability. It represents adjunctive therapy for L-Dopa treated patients with PD and motor fluctuations. Areas covered: The purpose of this study was to evaluate pharmacokinetic of OPC for the treatment of PD. Expert commentary: Oral OPC exhibits linear, dose-dependent absorption. However, following concomitant ingestion of a high-fat, high-calorie meal, the maximum plasma concentration will be decreased. A once-daily bedtime administration of OPC 1 h after the last daily L-Dopa/AADCi, are considered to avoid any interaction during the L-Dopa absorption phase. There are no clinically relevant effects of age (in adults), renal impairment or race on the pharmacokinetics of OPC. OPC dose adjustment is not needed in patients with mild to moderate chronic hepatic impairment. Opicapone exhibits the lowest potential for cytotoxicity in comparison with other COMT inhibitors. It significantly decreases COMT activity, with half-life of COMT inhibition in human erythrocytes of 61.6 h and increases systemic exposure to L-Dopa. This provides an enhancement in L-Dopa availability that translates into clinical benefit for PD patients in terms of significant decrease of OFF periods and increase in ON-time without troublesome dyskinesia.

DrugBank Data that Cites this Article

Drugs

Opicapone

Drug Interactions

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drugs	Interaction
Integrate drug-drug interactions in your software
Isocarboxazid Opicapone	The risk or severity of adverse effects can be increased when Opicapone is combined with Isocarboxazid.
Nialamide Opicapone	The risk or severity of adverse effects can be increased when Opicapone is combined with Nialamide.
Phenelzine Opicapone	The risk or severity of adverse effects can be increased when Opicapone is combined with Phenelzine.
Tranylcypromine Opicapone	The risk or severity of adverse effects can be increased when Opicapone is combined with Tranylcypromine.

Food Interactions

Drug	Interaction
Opicapone	Take separate from meals. Take opicapone at least one hour before or after eating, as a moderate calorie meal decreases Cmax and overall plasma exposure to the drug, and delays Tmax.