NDLI: The effect of ticagrelor on the metabolism of midazolam in healthy volunteers.

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The effect of ticagrelor on the metabolism of midazolam in healthy volunteers.

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The effect of ticagrelor on the metabolism of midazolam in healthy volunteers.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Teng, Renli Butler, Kathleen
Description	Country affiliation: United States Author Affiliation: Teng R ( AstraZeneca LP, Wilmington, DE, USA. renli.teng@astrazeneca.com)
Abstract	BACKGROUND: In vitro studies have demonstrated that ticagrelor, an oral antiplatelet agent, is a substrate, activator, and inhibitor of cytochrome P450 (CYP) 3A. Thus, potential CYP3A-mediated drug-drug interactions may occur. OBJECTIVES: The goal of this article was to report study results on the effect of ticagrelor on the pharmacokinetics of oral midazolam (oral midazolam study) and oral versus intravenous (IV) midazolam (oral/IV midazolam study). Secondary objectives included assessing the effect of midazolam on ticagrelor pharmacokinetic parameters, and the safety and tolerability of ticagrelor/midazolam coadministration. METHODS: Two randomized crossover studies were conducted in healthy volunteers (n = 28 in each) with ticagrelor and midazolam. In the first study, volunteers received oral ticagrelor (400 mg daily) or placebo for 6 days, then oral midazolam (7.5 mg). The second study regimen was a single dose of ticagrelor 270 mg, then ticagrelor 180 mg BID for 6 days with a single oral (7.5 mg) or IV (2.5 mg) dose of midazolam. RESULTS: After oral midazolam administration, ticagrelor significantly reduced the AUC(0-∞) of midazolam (30%-32%) and 4-hydroxymidazolam (42%-47%) but not 1-hydroxymidazolam. After administration of IV midazolam, ticagrelor reduced the AUC(0-∞) of midazolam (12%) and 4-hydroxymidazolam (23%) but not 1-hydroxymidazolam. CONCLUSIONS: These results indicate that ticagrelor can weakly activate the metabolism of midazolam to its major 1'-hydroxy metabolite, and at the same time, seems to weakly inhibit midazolam 4'-hydroxylation. Furthermore, ticagrelor affects both hepatic and intestinal CYP3A activity.
File Format	HTM / HTML
ISSN	01492918
Issue Number	7
Volume Number	35
e-ISSN	1879114X
Journal	Clinical Therapeutics
Language	English
Publisher	Elsevier
Publisher Date	2013-07-01
Publisher Place	United States
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Discipline Pharmacology Adenosine Analogs & Derivatives Cytochrome P-450 Cyp3a Metabolism Midazolam Pharmacokinetics Administration & Dosage Adverse Effects Administration, Oral Adolescent Adult Area Under Curve Cross-over Studies Double-blind Method Drug Administration Schedule Drug Interactions Drug Therapy, Combination Female Healthy Volunteers Humans Injections, Intravenous Male Middle Aged Young Adult Clinical Trial Journal Article Randomized Controlled Trial Research Support, Non-u.s. Gov't
Content Type	Text
Resource Type	Article
Subject	Pharmacology Pharmacology (medical)

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