Lack of electrocardiographic effect of dexlansoprazole MR, a novel modified-release formulation of the proton pump inhibitor dexlansoprazole, in healthy participants.

The effect of the proton pump inhibitor dexlansoprazole, an enantiomer of lansoprazole, on QT intervals was assessed after oral administration of a modified-release formulation of dexlansoprazole (dexlansoprazole MR). In this randomized, positive-comparator, placebo-controlled, 4-period crossover study, 40 healthy participants received single doses of dexlansoprazole MR 90 mg, dexlansoprazole MR 300 mg, moxifloxacin 400 mg, and placebo separated by 5-day washout intervals. Twenty-four-hour electrocardiograms were obtained at baseline and during each dosing period.

Pharmacokinetics and pharmacodynamics of a known active PPI with a novel Dual Delayed Release technology, dexlansoprazole MR: a combined analysis of randomized controlled clinical trials.

Background: Dexlansoprazole MR is a novel Dual Delayed Release formulation of dexlansoprazole, an enantiomer of lansoprazole, designed to prolong the plasma concentration-time profile of dexlansoprazole and extend duration of acid suppression with once-daily (QD) dosing.

Objectives: To assess the pharmacokinetics and pharmacodynamics of dexlansoprazole at different doses of dexlansoprazole MR and delineate the exposure-response relationship following oral administration of dexlansoprazole MR.

Methods: Dexlansoprazole MR was evaluated in two prospective randomized studies in healthy subjects.

Drug interaction studies with dexlansoprazole modified release (TAK-390MR), a proton pump inhibitor with a dual delayed-release formulation: results of four randomized, double-blind, crossover, placebo-controlled, single-centre studies.

Background And Objective: Most proton pump inhibitors are extensively metabolized by cytochrome P450 (CYP) isoenzymes, as are many other drugs, giving rise to potential drug-drug interactions. Dexlansoprazole modified release (MR) [TAK-390MR] is a modified-release formulation of dexlansoprazole (TAK-390), an enantiomer of lansoprazole, which employs an innovative Dual Delayed Release technology designed to prolong the plasma dexlansoprazole concentration-time profile following once-daily oral administration. As with lansoprazole, dexlansoprazole is metabolized mainly by CYP3A and CYP2C19.

Greater immediate gastric acid suppression with lansoprazole 30 mg administered as a 2-minute intravenous bolus injection versus a 30-minute infusion.

Study Objective: To compare the pharmacokinetics, pharmacodynamics, and safety of lansoprazole administered as a 2-minute intravenous bolus injection versus a 30-minute continuous infusion.

Design: Phase I, open-label, randomized, crossover, single-center trial.

Setting: Clinical research facility.

Coadministration of lansoprazole and naproxen does not affect the pharmacokinetic profile of methotrexate in adult patients with rheumatoid arthritis.

Drugs prescribed for rheumatoid arthritis are often associated with gastrointestinal toxicity, and proton pump inhibitors may be coadministered for gastroprotection. In this open-label study, the effect of lansoprazole 30 mg qd and naproxen 500 mg bid on the pharmacokinetic profile of methotrexate was investigated. Twenty-seven adult rheumatoid arthritis patients on stable oral methotrexate doses (7.

Impact of stereoselectivity on the pharmacokinetics and pharmacodynamics of antiarrhythmic drugs.

Many antiarrhythmic drugs introduced into the market during the past three decades have a chiral centre in their structure and are marketed as racemates. Most of these agents, including disopyramide, encainide, flecainide, mexiletine, propafenone and tocainide, belong to class I antiarrhythmics, whereas verapamil is a class IV antiarrhythmic agent. Except for encainide and flecainide, there is substantial stereoselectivity in one or more of the pharmacological actions of chiral antiarrhythmics, with the activity of enantiomers differing by as much as 100-fold or more for some of these drugs.

Stereoselective pharmacokinetics and pharmacodynamics of anti-asthma agents.

Objective: To review the previously published studies on pharmacokinetics and pharmacodynamics of chiral drugs used in the treatment of asthma.

Data Sources: Primary and review articles were identified with a MEDLINE search (1980-May 2001) and through secondary sources.

Study Selection And Data Extraction: All English-language studies and reviews obtained from the MEDLINE search pertaining to stereoselective pharmacokinetics and pharmacodynamics of chiral anti-asthma drugs were assessed.