Stereoselective Pharmacodynamics and Pharmacokinetics of Proton Pump Inhibitors
Abstract
Proton pump inhibitors (PPIs) are a group of gastric acid suppressing drugs, that are strong and long-lasting inhibitors of the proton pump (referred to as acid pump antagonists). They work by irreversibly blocking the H+/K+ ATPase. PPIs are used to treat peptic ulcer disease, gastroesophageal reflux disease, nonsteroidal anti-inflammatory drug-induced gastrointestinal lesions, and Zollinger-Ellison syndrome. The structure of PPIs are similar, they all have a similar core with a sulphur atom chiral center combined with different substituent groups. In relation to the sulphur atom chiral center, the pharmacodynamics, pharmacokinetics are diverse between the racemates and their stereoisomers, which are mainly observed in the following aspects. In regards to pharmacodynamics, the main features of the similarities and differences involve the duration of drug action and the ability to control nocturnal gastric acid secretion. In regards to pharmacokinetic and metabolic pathways, the similarities and differences are measured by the pharmacokinetic and metabolic parameters. These parameters including time to maximal plasma concentration (Tmax), maximal plasma concentration (Cmax), area under the plasma concentration curve (AUC), bioavailability (F) and elimination half-life (t1/2). Compare to the racemates, the stereoisomer (the R-one or the S-one) exhibited less individual differences and better efficiency in acid secretion control. Nowadays, the main reason for PPI development is…
Read the paper
Related studies
- Advantages and Disadvantages of Long-term Proton Pump Inhibitor Use
- Ivth brazilian consensus conference on helicobacter pylori infection
- A pSMAD/CDX2 complex is essential for the intestinalization of epithelial metaplasia
- S2k-Leitlinie Gastroösophageale Refluxkrankheit und eosinophile Ösophagitis der Deutschen Gesellschaft für Gastroenterologie, Verdauungs- und Stoffwechselkrankheiten (DGVS) – März 2023 – AWMF-Registernummer: 021–013
- Step-by-step management of refractory gastresophageal reflux disease
- Insights into Effects/Risks of Chronic Hypergastrinemia and Lifelong PPI Treatment in Man Based on Studies of Patients with Zollinger–Ellison Syndrome
Go deeper in Evidence Hub
Evidence Hub adds a study data sheet (design, sample size, evidence level, key numbers), an AI summary and a chat grounded in the paper's text.