-
Fundamental & Clinical Pharmacology Aug 2019Renal ischemia/reperfusion injury (IRI), which occurs in many pathological conditions, is associated with high rate of morbidity and mortality. Activation of...
Renal ischemia/reperfusion injury (IRI), which occurs in many pathological conditions, is associated with high rate of morbidity and mortality. Activation of inflammatory responses and oxidative stress contribute to induce organ damage following IRI. Pantoprazole, a proton pump inhibitor, which is mostly prescribed for gastroesophageal reflux disease (GERD) has been shown to exert anti-inflammation effects. In order to evaluate the effects of pantoprazole on renal ischemia/reperfusion injury, four different doses of pantoprazole (4.5, 9, 18, and 36 mg/kg) were administered 30 min before the induction of IRI in male Wistar rats. Serum concentration of creatinine and blood urea nitrogen (BUN) were measured to assess renal function. Histopathological changes, malondialdehyde (MDA) level and toll-like receptor 4 (TLR-4) expression in renal tissue were determined and compared to control group. The results revealed that pretreatment with 18 and 36 mg/kg of pantoprazole leads to the significant decline in serum creatinine and BUN levels and the severity of necrosis grade in comparison with control group (P < 0.05). Pantoprazole also reduced the MDA level and TLR-4 expression in renal tissue. In summary, pantoprazole attenuates renal injury following ischemia/reperfusion. This effect is mediated partially through inhibition of oxidative stress and TLR-4 signaling pathway.
Topics: Animals; Blood Urea Nitrogen; Blotting, Western; Creatinine; Dose-Response Relationship, Drug; Kidney Diseases; Male; Malondialdehyde; Pantoprazole; Rats; Rats, Wistar; Reperfusion Injury; Toll-Like Receptor 4
PubMed: 30720886
DOI: 10.1111/fcp.12451 -
Drug Development Research Jun 2024Hepatocellular carcinoma (HCC) is one of the deadliest cancers. The prevention and therapy for this deadly disease remain a global medical challenge. In this study, we...
Hepatocellular carcinoma (HCC) is one of the deadliest cancers. The prevention and therapy for this deadly disease remain a global medical challenge. In this study, we investigated the effect of pantoprazole (PPZ) on the carcinogenesis and growth of HCC. Both diethylnitrosamine (DEN) plus CCl4-induced and DEN plus high fat diet (HFD)-induced HCC models in mice were established. Cytokines and cell proliferation-associated gene in the liver tissues of mice and HCC cells were analyzed. Cellular glycolysis and Na/H exchange activity were measured. The preventive administration of pantoprazole (PPZ) at a clinically relevant low dose markedly suppressed HCC carcinogenesis in both DEN plus CCl4-induced and HFD-induced murine HCC models, whereas the therapeutic administration of PPZ at the dose suppressed the growth of HCC. In the liver tissues of PPZ-treated mice, inflammatory cytokines, IL1, CXCL1, CXCL5, CXCL9, CXCL10, CCL2, CCL5, CCL6, CCL7, CCL20, and CCL22, were reduced. The administration of CXCL1, CXCL5, CCL2, or CCL20 all reversed PPZ-suppressed DEN plus CCL4-induced HCC carcinogenesis in mice. PPZ inhibited the expressions of CCNA2, CCNB2, CCNE2, CDC25C, CDCA5, CDK1, CDK2, TOP2A, TTK, AURKA, and BIRC5 in HCC cells. Further results showed that PPZ reduced the production of these inflammatory cytokines and the expression of these cell proliferation-associated genes through the inhibition of glycolysis and Na/H exchange. In conclusion, PPZ suppresses the carcinogenesis and growth of HCC, which is related to inhibiting the production of inflammatory cytokines and the expression of cell proliferation-associated genes in the liver through the inhibition of glycolysis and Na/H exchange.
Topics: Animals; Carcinoma, Hepatocellular; Glycolysis; Liver Neoplasms; Mice; Pantoprazole; Male; Cell Proliferation; Humans; Mice, Inbred C57BL; Carcinogenesis; Diethylnitrosamine; Cytokines; Cell Line, Tumor; Diet, High-Fat
PubMed: 38764200
DOI: 10.1002/ddr.22198 -
Scientific Reports Jun 2022In this work, new optical evidences concerning the changes induced of the UV light on pantoprazole sodium (PS), in solid state and as aqueous solution, are reported by...
In this work, new optical evidences concerning the changes induced of the UV light on pantoprazole sodium (PS), in solid state and as aqueous solution, are reported by UV-VIS spectroscopy, photoluminescence (PL), Raman scattering and FTIR spectroscopy. New evidences concerning the products of the PS photodegradation pathways are reported by the correlated studies of thermogravimetry and mass spectrometry. The influence of the excipients and alkaline medium on the PS photodegradation is also studied. New aspects regarding the chemical mechanism of the PS photodegradation in the presence of the water vapor and oxygen form air and the alkaline medium are shown. Our results confirm that the PS photodegradation induced of the water vapors and oxygen from air leads to the generation of 5-difluoromethoxy-3H-benzimidazole-2-thione sodium, 5-difluoromethoxy-3H-benzimidazole sodium, 2-thiol methyl-3, 4-dimethoxypyridine and 2-hydroxymethyl-3, 4-dimethoxypyridine, while in the alkaline medium, compounds of the type of the 2-oxymethyl-3,4-dimethoxypyridine sodium salts are resulted.
Topics: Benzimidazoles; Mass Spectrometry; Oxygen; Pantoprazole; Photolysis; Sodium; Spectroscopy, Fourier Transform Infrared
PubMed: 35680962
DOI: 10.1038/s41598-022-13648-6 -
Clinical Pharmacology in Drug... May 2021This study aimed to evaluate the bioequivalence of 2 pantoprazole sodium enteric-coated tablet formulations, a generic formulation and a branded formulation, and to... (Comparative Study)
Comparative Study Randomized Controlled Trial
This study aimed to evaluate the bioequivalence of 2 pantoprazole sodium enteric-coated tablet formulations, a generic formulation and a branded formulation, and to investigate their pharmacokinetic and safety profiles. The study was designed as a single-center, randomized, open-label, single-dose, dual-period, and 2-sequence crossover trial, and was divided into fasting and postprandial human bioequivalence trials. In the first trial, 36 subjects were fasted overnight before they were given generic or branded tablets (during 2 separate administration periods). Separately, 42 subjects were provided a high-fat meal 1 hour before the drugs were administered. Blood specimens of each subject were obtained up to 24 hours after drug administration. No significant differences were observed between the pharmacokinetic profiles of the generic and branded pantoprazole sodium enteric-coated tablets. Bioequivalence was evaluated using 90% confidence intervals for the ratio of test/reference log area under the concentration-time curve over 24 hours, log area under the concentration-time curve to infinity (AUC ), and log peak concentration (C ). The 90% confidence intervals of the least squares geometric mean ratio of C , area under the concentration-time curve from time zero to the last measurable concentration (AUC ), and AUC of 36 subjects in the fasting trial and of 40 of 41 subjects in the postprandial trial (C [41], AUC [41], and AUC [40]) were in accordance with the bioequivalence criteria. No severe adverse effects were detected. The generic and branded pantoprazole sodium enteric-coated tablets were considered bioequivalent with similar safety profiles.
Topics: Adult; Area Under Curve; Cross-Over Studies; Drugs, Generic; Fasting; Female; Food-Drug Interactions; Humans; Male; Pantoprazole; Proton Pump Inhibitors; Tablets, Enteric-Coated; Therapeutic Equivalency; Young Adult
PubMed: 33128847
DOI: 10.1002/cpdd.888 -
The Journal of the Association of... Jun 2015
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Adult; Anaphylaxis; Humans; Male; Pantoprazole; Proton Pump Inhibitors
PubMed: 26710417
DOI: No ID Found -
Alimentary Pharmacology & Therapeutics Jan 2014
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Esomeprazole; Female; Gastroesophageal Reflux; Humans; Male; Pantoprazole; Proton Pump Inhibitors
PubMed: 24330240
DOI: 10.1111/apt.12577 -
Journal of Pediatric Gastroenterology... Oct 2010
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Gastroesophageal Reflux; Humans; Infant; Infant, Newborn; Pantoprazole; Proton Pump Inhibitors; Randomized Controlled Trials as Topic; Reproducibility of Results; Treatment Outcome
PubMed: 20871256
DOI: 10.1097/MPG.0b013e3181f79600 -
Scandinavian Journal of Gastroenterology Jul 2003
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Adult; Anaphylaxis; Benzimidazoles; Enzyme Inhibitors; Female; Gastroesophageal Reflux; Humans; Male; Omeprazole; Pantoprazole; Sulfoxides
PubMed: 12889570
DOI: 10.1080/00365520310002797 -
Critical Care Medicine Jul 2017
Topics: Critical Illness; Humans; Pantoprazole; Peptic Ulcer; Pilot Projects; Ulcer
PubMed: 28622218
DOI: 10.1097/CCM.0000000000002489 -
Revista de Gastroenterologia de Mexico... 2020Levo-pantoprazole, the S-enantiomer of pantoprazole, is a proton pump inhibitor that has been shown in animal studies to be faster and stronger than its racemic... (Comparative Study)
Comparative Study Randomized Controlled Trial
Intragastric pH effect of 20mg of levo-pantoprazole versus 40mg of racemic pantoprazole the first seven days of treatment in patients with gastroesophageal reflux disease.
INTRODUCTION/AIM
Levo-pantoprazole, the S-enantiomer of pantoprazole, is a proton pump inhibitor that has been shown in animal studies to be faster and stronger than its racemic formulation. There are no studies on humans and therefore our aim was to evaluate the effects of levo-pantoprazole versus racemic pantoprazole on intragastric pH.
MATERIALS AND METHODS
A randomized controlled study was conducted on patients with erosive gastroesophageal reflux disease that were given 20mg of levo-pantoprazole (n = 15) versus 40mg of racemic pantoprazole (n = 15) for 7 days. Baseline and end-of-treatment symptom evaluation and intragastric pH measurement were carried out.
RESULTS
There were no differences between the groups in the baseline evaluations. From 40 to 115min after the first dose of levo-pantoprazole, the mean intragastric pH was higher, compared with that of racemic pantoprazole (p < 0.05). After one week, levo-pantoprazole and racemic pantoprazole significantly reduced intragastric acid production and its esophageal exposure (p < 0.05). Even though there was no statistically significant difference, a larger number of patients that received levo-pantoprazole stated that their heartburn improved within the first 3 days.
CONCLUSIONS
The S-enantiomer of pantoprazole (levo-pantoprazole) had a faster and stronger effect with respect to acid suppression, compared with its racemic formulation. Although the effect on symptoms was faster with levo-pantoprazole, occurring within the first days of treatment, it was equivalent to that of the racemate at one week of treatment.
Topics: Adult; Female; Gastroesophageal Reflux; Humans; Hydrogen-Ion Concentration; Male; Middle Aged; Pantoprazole; Proton Pump Inhibitors; Time Factors; Treatment Outcome
PubMed: 31104856
DOI: 10.1016/j.rgmx.2019.02.006