Pharmacokinetic profile of immediate‐release omeprazole in patients with gastro‐oesophageal reflux associated with gastroparesis

Wo, John M.; Eversmann, Jennifer; Mann, Surinder K

doi:10.1111/j.1365-2036.2009.04203.x

Cited by 5 publications

(4 citation statements)

References 12 publications

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“…Omeprazole mean (SD) plasma concentrations at 1.5 hours after the fourth and fifth doses were similar to the previously published omeprazole 40 mg once-daily PK data. 33 Pharmacodynamics Mean PT-time profiles of rivaroxaban were similar between both treatments; PT was increased after rivaroxaban administration for both treatments, with the maximum increase in PT observed approximately 4 hours after rivaroxaban administration. For both treatments, PT subsequently decreased gradually and values returned to near baseline by the end of the 72-hour sampling period (Fig.…”

Section: Pharmacokineticsmentioning

confidence: 94%

Effect of Multiple Doses of Omeprazole on the Pharmacokinetics, Pharmacodynamics, and Safety of a Single Dose of Rivaroxaban

Moore

Plotnikov

Thyssen

et al. 2011

Journal of Cardiovascular Pharmacology

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Many patients with acute coronary syndrome receive chronic dual antiplatelet therapy (acetylsalicylic acid and clopidogrel) for secondary event prophylaxis, and new oral anticoagulants are being investigated as adjunctive therapy in this indication. Gastrointestinal side effects such as bleeding are commonly associated with antiplatelet use; accordingly, many patients receive proton pump inhibitors (PPIs) to mitigate this. PPIs can reduce the antiplatelet activity of clopidogrel through cytochrome P450 2C19 inhibition, and pantoprazole reduces the bioavailability of dabigatran, a direct thrombin inhibitor that acts via cytochrome P450 2C19-independent mechanisms. These observations support the investigation of potential pharmacokinetic and pharmacodynamic interactions between PPIs and anticoagulants. We evaluated the influence of administering once-daily omeprazole 40 mg for 5 days on the pharmacokinetics and pharmacodynamics of a single 20-mg dose of the oral direct factor Xa inhibitor, rivaroxaban, in a randomized, open-label, 2-way, crossover, drug-drug interaction study in healthy subjects. No clinically meaningful interactions were observed; geometric mean ratios were 101%, 101%, and 93.5% for rivaroxaban area under the plasma concentration-time curve from time 0 to the time of the last quantifiable concentration (AUClast), or until infinity (AUC∞), and maximum plasma concentration (Cmax), respectively. Prothrombin time increased similarly in both treatment groups, with maximal values observed approximately 4 hours post rivaroxaban administration. A single 20-mg rivaroxaban dose appears well tolerated when administered alone or after 5 days of once-daily omeprazole 40 mg administration.

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Section: Pharmacokineticsmentioning

confidence: 94%

Effect of Multiple Doses of Omeprazole on the Pharmacokinetics, Pharmacodynamics, and Safety of a Single Dose of Rivaroxaban

Moore

Plotnikov

Thyssen

et al. 2011

Journal of Cardiovascular Pharmacology

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“…The study in patients with GERD reported that the mean T max was 32 min for IR-O and 97 min for DR-O. The C max was 21 % higher for IR-O than DR-O, but the AUC was similar [ 24 ] . These results were similar to the fi ndings in our study.…”

mentioning

confidence: 95%

Pharmacokinetics of a New Immediate-release Compound Omeprazole Capsule and its Comparison with the Enteric-coated Formulation under Fasting and Fed Conditions

et al. 2013

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The present study was conducted to describe the pharmacokinetic profile of immediate-release compound omeprazole capsule and compare it with the enteric-coated formulation under fasting and fed condition.This study was designed to phase I, open-label, randomized, 3-part clinical trial. 12 subjects in part one received single doses (20 mg and 40 mg) and repeated doses (20 mg). Different 30 subjects in part 2 (fasting condition) and part 3 (fed condition) received either compound omeprazole capsule (40 mg) or delayed-release omeprazole (40 mg) separated by 7 days.Compound omeprazole capsule showed dose non-proportionality in the range from 20 mg to 40 mg. The AUC0-t of 20 mg omeprazole is 78% higher after repeated doses. The C max was higher and T max was lower for compound omeprazole capsule than delayed-release omeprazole. 90% CIs for AUC0-t of the 2 periods (test/reference) under fasting and fed conditions were 106.3% (102.2%~109.2%) and 104.1% (93.4%~109.6%), respectively. Presence of food reduced the rate (C max) and extent (AUC0-t) of systemic exposure of the test and reference formulations from 1 462 to 777 ng · mL-1, 1 055 to 602 ng · mL-1, 2 597 to 1 852 ng · h · mL-1 and 2 454 to 1 873 ng · h · mL-1, respectively.Exposed dose of omeprazole in subjects with compound omeprazole capsule was time- and dose-dependent. Compared with delayed-release omeprazole, compound omeprazole capsule had rapid but similar degree of absorption of omeprazole.

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“…14 Given such characteristics of AD-206, it can be an alternative to conventional enteric-coated PPIs when rapid absorption or immediate management of symptoms for GERD is needed. 30,31 The systemic exposure of esomeprazole for AD-206 was similar to that of the conventional esomeprazole and satisfied the predetermined equivalent criteria after a multiple-dose for both doses. However, the systemic exposure of esomeprazole in AD-206 was lower than that of the conventional esomeprazole after a single-dose for both doses.…”

Section: Discussionmentioning

confidence: 91%

Section: Discussionmentioning

confidence: 99%

Comparative Pharmacokinetics/Pharmacodynamics of Fixed-Dose Combination of Esomeprazole and Calcium Carbonate (AD-206) to the Conventional Esomeprazole

Bae¹,

Kwon²,

Lee³

et al. 2021

DDDT

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Purpose: Proton pump inhibitors (PPIs) are used for the treatment of acid-related disorders. Demands for enhanced stability and faster onset led to the development of AD-206, a fixeddose combination of a PPI (esomeprazole) with an antacid salt (calcium carbonate). This study compared the pharmacokinetics (PKs) and pharmacodynamics (PDs) of AD-206 (Addpharma) with conventional esomeprazole (Nexium ® , AstraZeneca). Materials and Methods:A randomized, open-label, two-treatment, two-sequence crossover study was conducted with 2 different doses of esomeprazole at 20 and 40 mg with a fixed calcium carbonate dose of 600 mg in AD-206. Forty-four subjects were included in each dose group and randomly received either AD-206 or the conventional esomeprazole for 7 consecutive days in each period. After a single-and multiple-dose, blood samples for the PK analysis were analyzed, and 24-hour intragastric pH monitoring was conducted. Results:The systemic exposure of esomeprazole after a multiple-dose of AD-206 was similar to that of the conventional esomeprazole in both doses, but the time to reach the peak concentration was faster in AD-206. The percentage decrease from baseline in the integrated gastric acidity for a 24-hour interval after the dose was not significantly different between the AD-206 and the conventional esomeprazole after a single-and multiple-dose for both doses, and the time to reach pH 4 was faster for AD-206. Conclusion: AD-206 showed a similar systemic exposure and suppression of gastric acid secretion after a multiple-dose compared to the conventional esomeprazole.

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Pharmacokinetic profile of immediate‐release omeprazole in patients with gastro‐oesophageal reflux associated with gastroparesis

Abstract: SUMMARY BackgroundImmediate-release omeprazole has a more rapid absorption compared with delayed-release omeprazole in asymptomatic volunteers. However, effects of delayed gastric emptying on omeprazole absorption remain unknown.

Cited by 5 publications

References 12 publications

Effect of Multiple Doses of Omeprazole on the Pharmacokinetics, Pharmacodynamics, and Safety of a Single Dose of Rivaroxaban

Effect of Multiple Doses of Omeprazole on the Pharmacokinetics, Pharmacodynamics, and Safety of a Single Dose of Rivaroxaban

Pharmacokinetics of a New Immediate-release Compound Omeprazole Capsule and its Comparison with the Enteric-coated Formulation under Fasting and Fed Conditions

Comparative Pharmacokinetics/Pharmacodynamics of Fixed-Dose Combination of Esomeprazole and Calcium Carbonate (AD-206) to the Conventional Esomeprazole

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