Pharmacokinetics and metabolism of the proton pump inhibitor
pantoprazole in man

Radhofer-Welte, S

doi:10.1358/dot.1999.35.10.561695

Cited by 24 publications

(20 citation statements)

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“…In short, pantoprazole is rapidly absorbed and achieves a maximum plasma concentration (C max ) 2–3 hours after a single dose (Table 2). 46 The drug is subject to low first-pass hepatic metabolism, reflected in a bioavailability of 77% 47,48. This is not affected by the ingestion of food 47.…”

Section: Pharmacokineticsmentioning

confidence: 99%

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Pantoprazole for the Treatment of Peptic Ulcer Bleeding and Prevention of Rebleeding

Rensburg

Cheer²

2012

Clin Med Insights Gastroenterol

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Adding proton pump inhibitors (PPIs) to endoscopic therapy has become the mainstay of treatment for peptic ulcer bleeding, with current consensus guidelines recommending high-dose intravenous (IV) PPI therapy (IV bolus followed by continuous therapy). However, whether or not high-dose PPI therapy is more effective than low-dose PPI therapy is still debated. Furthermore, maintaining pH ≥ 4 appears to prevent mucosal bleeding in patients with acute stress ulcers; thus, stress ulcer prophylaxis with acid-suppressing therapy has been increasingly recommended in intensive care units (ICUs). This review evaluates the evidence for the efficacy of IV pantoprazole, a PPI, in preventing ulcer rebleeding after endoscopic hemostasis, and in controlling gastric pH and protecting against upper gastrointestinal (GI) bleeding in high-risk ICU patients. The review concludes that IV pantoprazole provides an effective option in the treatment of upper GI bleeding, the prevention of rebleeding, and for the prophylaxis of acute bleeding stress ulcers.

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Section: Pharmacokineticsmentioning

confidence: 99%

“…46 The drug is subject to low first-pass hepatic metabolism, reflected in a bioavailability of 77% 47,48. This is not affected by the ingestion of food 47. The pharmacokinetics of pantoprazole are linear after both oral and IV administration, with area under the curve (AUC) and C max increasing in proportion to IV doses up to 240 mg 49…”

Section: Pharmacokineticsmentioning

confidence: 99%

Pantoprazole for the Treatment of Peptic Ulcer Bleeding and Prevention of Rebleeding

Rensburg

Cheer²

2012

Clin Med Insights Gastroenterol

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“…It is generally accepted that PPIs have various extents to which their hepatic metabolism depends on a given CYP isoenzyme 22. For instance, since pantoprazole has lower affinity for CYP2C19 compared to omeprazole and esomeprazole,23 pantoprazole is expected to have more favorable drug-drug interactions during the secondary biotransformation 24…”

Section: Discussionmentioning

confidence: 99%

Pantoprazole Does Not Reduce the Antiplatelet Effect of Clopidogrel: A Randomized Controlled Trial in Korea

et al. 2017

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Background/AimsConcerns that proton pump inhibitors (PPIs) diminish the efficacy of clopidogrel could hamper the appropriate prescription of PPIs. We evaluated the influence of pantoprazole on the antiplatelet effect of clopidogrel compared with ranitidine, which is regarded as safe, after stratification of the population according to the presence of a cytochrome (CYP) 2C19 polymorphism in Korea.MethodsForty patients who underwent dual antiplatelet therapy were randomized to receive pantoprazole (n=20) or ranitidine (n=20). Platelet aggregation was evaluated by impedance aggregometry at baseline (D0) and 8 days after acid-lowering treatments (D9). CYP2C19 was genotyped by polymerase chain reaction restriction fragment length polymorphism.ResultsAfter co-treatment, the percentage of clopidogrel low-response was 11.1% (2/18) in the pantoprazole group and 10.5% (2/19) in the ranitidine group (p=0.954). The impedance values with adenosine diphosphate stimulus after acid-lowering treatments did not significantly differ between the two groups. In a multiple regression analysis, only ST-elevation myocardial infarction was marginally associated with a reduced antiplatelet effect (odds ratio, 12.07; 95% confidence interval, 0.84 to 173.78). However, pantoprazole use did not affect the antiplatelet effect after correction for the CYP2C19 polymorphism.ConclusionsThis study showed that pantoprazole does not increase platelet aggregation in patients receiving dual antiplatelet therapy (ClinicalTrials.gov number: NCT02733640).

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“…Thus, the true incidence of drug interactions is difficult to appreciate. 40,42 Most likely, the reported incidence will be affected by numerous factors, and will inversely correlate with the number of years the drug has been on the market and physicians' experience with the drug. Drug interactions can lead to unpredictable changes in the blood plasma level of the affected concomitant medication.…”

Section: Concomitant Medication and Drug Interactionmentioning

confidence: 99%

“…Metabolic drug interactions: effect of proton pump inhibitors (PPIs) on concomitant drugs[39][40][41][42] …”

mentioning

confidence: 99%

Heartburn in primary care: problems below the surface

2004

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Heartburn is a common physiological event often associated with an underlying occurrence of gastroesophageal reflux disease (GERD). Studies show that GERD is a highly prevalent and chronic condition that significantly impacts on the patient's quality of life (QoL) and, in the long term, increases the risk for developing esophageal adenocarcinoma, more commonly referred to as Barrett's esophagus. Data indicate that symptom severity is a poor predictor of either the presence of erosive mucosal lesions or the development of complications. Given that lifestyle modifications are often insufficient for long-term treatment of GERD, drugs that inhibit gastric acid production--such as the proton pump inhibitors (PPIs)--are now the most effective strategy. Although generally well tolerated, the potential of PPIs for interactions with other drugs needs to be considered. This review discusses the symptoms and risk factors associated with GERD, possible links to Helicobacter pylori infection, and effective treatment strategies within a primary care setting.

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Pharmacokinetics and metabolism of the proton pump inhibitor pantoprazole in man

Cited by 24 publications

References 0 publications

Pantoprazole for the Treatment of Peptic Ulcer Bleeding and Prevention of Rebleeding

Pantoprazole for the Treatment of Peptic Ulcer Bleeding and Prevention of Rebleeding

Pantoprazole Does Not Reduce the Antiplatelet Effect of Clopidogrel: A Randomized Controlled Trial in Korea

Heartburn in primary care: problems below the surface

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