Drugs online research references
Pharmacol Res. 2002 Jul;46(1):75-84.
Protective effect of omeprazole against acute gastric mucosal lesions induced by compound 48/80, a mast cell degranulator, in rats.
Kobayashi T, Ohta Y, Inui K, Yoshino J, Nakazawa S.
Department of Internal Medicine, Second Teaching Hospital, School of Medicine, Fujita Health University, Nagoya, Aichi 454-0012, Japan.
Omeprazole, a proton pump inhibitor is known to function not only as a proton pump inhibitor but also as an anti-inflammatory agent, an antioxidant or a stimulator of gastric mucus secretion. We have shown that the pathogenesis of acute gastric mucosal lesions induced by compound 48/80, a mast cell degranulator, in rats involves neutrophil infiltration, lipid peroxidation, and mucin depletion, but not acid secretion, in the gastric mucosal tissue. Therefore, we examined whether omeprazole protects against acute gastric mucosal lesions induced by compound 48/80 in rats. Rats were injected with omeprazole (10 or 50 mgkg(-1), i.p.) at 0.5h before injection of compound 48/80 (0.75 mgkg(-1), i.p.). Omeprazole prevented gastric mucosal lesion development at 0.5 and 3h after compound 48/80 injection. Omeprazole attenuated decreased nonprotein sulfhydryl content and increased myeloperoxidase and xanthine oxidase (XO) activities and lipid peroxide (LPO) content in the gastric mucosa at 0.5h after compound 48/80 injection and increased myeloperoxidase and XO activities and LPO content, but not decreased hexosamine and adherent mucus contents, in the gastric mucosa at 3h. These results indicate that omeprazole protects against compound 48/80-induced acute gastric mucosal lesions in rats possibly through its anti-inflammatory and antioxidant actions.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12208124&dopt=Abstract
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clinic.ub.es
OBJECTIVE: To examine the pharmacokinetics of omeprazole during intravenous infusion in patients with varying degrees of liver dysfunction (Child-Pugh categories A to C). DESIGN: Nonblinded single-period study. PATIENTS: Thirteen patients, five males and eight females with a mean age of 59 years and proven hepatic cirrhosis, classified according to Child-Pugh criteria as A (n = 5), B (n = 4) or C (n = 4). METHODS: Each patient received an 80mg bolus of omeprazole over 30 minutes followed by a continuous infusion of 8 mg/h for 47.5 hours. Blood samples were taken frequently throughout the infusion and during the subsequent 24-hour washout period for determination of omeprazole and its metabolites. Laboratory screening was also performed at the start of the study, after 72 hours and at the 14 day follow-up visit. RESULTS: Data were evaluable for 12 patients. For omeprazole, the mean total area under the plasma concentration-time curve (AUC) was 286.5 micromol x h/L, peak plasma concentration was 14.9 micromol/L and terminal elimination half-life was 4.1 hours; these values were higher than those observed historically in control patient populations. Concentrations of the metabolite omeprazole sulphone were also increased, but there was a decrease in concentrations of hydroxy-omeprazole. Deviations from normal values increased with increasing disease severity for all parameters. For example, in patients with liver dysfunction of Child-Pugh categories A, B and C, AUC(48 )was 240.8, 280.4 and 323.3 micromol x h/L compared with 151.3 micromol x h/L in the historical control population. Despite its altered pharmacokinetics, omeprazole was not associated with any serious or untoward effects. CONCLUSION: Exposure to omeprazole following intravenous administration was higher in patients with liver dysfunction than in the normal population. However, even in patients with severely impaired liver function, the omeprazole plasma concentration did not change by more than 100% and the drug was well tolerated.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12222996&dopt=Abstract
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po.rd.taisho.co.jp
The effects of oral administration of clarithromycin (CLR), amoxicillin (AMX), and lansoprazole (LPZ) on gastric emptying in rats were investigated by a glass powder method and a phenol red method. By both test methods, no significant effects on gastric emptying were observed when CLR, AMX, or LPZ was administered alone or when the three drugs were administered concomitantly. The levels of gastrointestinal absorption of [(14)C]CLR and [(14)C]AMX were measured. Four hours after injection of [(14)C]CLR or [(14)C]AMX into the stomach and duodenum loops of rats, 86.63 and 1.27% of the original amount of [(14)C]CLR administered were recovered in the contents of the stomach and duodenum loops, respectively, and 80.01 and 55.88% of the original amount of [(14)C]AMX administered were recovered in the contents of the stomach and duodenum loops, respectively.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12234874&dopt=Abstract
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