Assessment of potential pharmacokinetic interactions of ezetimibe/simvastatin and extended-release niacin tablets in healthy subjects.
Background: Efforts to lower plasma lipid levels sometimes require multiple agents with different mechanisms of action to achieve results specified by national treatment guidelines. Methods: This was an open-label, randomized, three-period, multiple-dose crossover study that assessed the potential f...
| Published in: | European Journal of Clinical Pharmacology Vol. 67; no. 5; pp. 483 - 493 |
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| Main Authors: | , , , , , , , |
| Format: | clinical trial research tables/charts Journal Article |
| Published: |
Springer Nature
May2011
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| Online Access: | View this record in EBSCOhost |
| fields | @attributes: recordID: 1 pdfLink: plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=104876944&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 104876944 longDbName: CINAHL Complete uiTag: AN controlInfo: bkinfo: dissinfo: jinfo: jid: 00316970 NP9 jtl: European Journal of Clinical Pharmacology issn: 00316970 maglogo: N pubinfo: dt: May2011 vid: 67 iid: 5 pid: 237 pub: Springer Nature place: New York, New York artinfo: ui: 104876944 59983369 10.1007/s00228-010-0955-6 NLM21120461 104876944 ppf: 483 ppct: 10 formats: fmt: @attributes: type: P tig: atl: Assessment of potential pharmacokinetic interactions of ezetimibe/simvastatin and extended-release niacin tablets in healthy subjects. aug: au: Kosoglou, Teddy Zhu, Yali Statkevich, Paul Triantafyllou, Ilias Taggart, William Xuan, Fengjuan Kim, Kenneth Cutler, David affil: Merck & Co., Inc., Whitehouse Station USA sug: subj: Drug Interactions Ezetimibe Simvastatin Pharmacokinetics Niacin Pharmacokinetics Niacin Administration and Dosage Ezetimibe Simvastatin Administration and Dosage Hyperlipidemia Drug Therapy Funding Source Human Clinical Trials Crossover Design Delayed-Action Preparations Descriptive Statistics Drug Therapy, Combination Male Female Biological Availability Confidence Intervals Analysis of Variance Adult Middle Age Ezetimibe Simvastatin Blood Niacin Blood Adult: 19-44 years Middle Aged: 45-64 years Male Female ab: Background: Efforts to lower plasma lipid levels sometimes require multiple agents with different mechanisms of action to achieve results specified by national treatment guidelines. Methods: This was an open-label, randomized, three-period, multiple-dose crossover study that assessed the potential for pharmacokinetic interaction between extended-release niacin and ezetimibe/simvastatin and their major metabolites. Eighteen adults received three randomized treatments: (A) extended-release (ER) niacin 1000 mg/day for 2 days, followed by 2000 mg/day for 5 days; (B) ezetimibe/simvastatin 10 mg/20 mg/day; (C) coadministration of Treatments A and B. Treatments were given once a day after a low fat breakfast for a total of 7 days, with a 7-day inter-dose period. Results: There were small (mean ≤35%) increases in drug exposure for all analytes after coadministration of ER niacin and ezetimibe/simvastatin 10 mg/20 mg. The least-square mean between treatment C (maximum plasma concentration) ratios (×100) were 97, 98, and 109% for ezetimibe, simvastatin and niacin, respectively. The corresponding ratios for total ezetimibe, simvastatin acid, and nicotinuric acid were 99, 118, and 110%. The AUC (area under the plasma concentration-time curve from time zero to 24 h after dosing) ratios for ezetimibe, simvastatin, and niacin were 109, 120, and 122%, respectively, and the corresponding ratios for total ezetimibe, simvastatin acid, and nicotinuric acid were 126, 135 and 119%. Conclusion: There is a small pharmacokinetic drug interaction between ER niacin and ezetimibe/simvastatin and although this is not considered to be clinically significant, the concomitant use of these drugs should be appropriately monitored, especially during the niacin titration period. pubtype: Academic Journal doctype: clinical trial research tables/charts Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
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