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Japanese Journal of Pharmacology Apr 1989The antiulcer effects of OPC-12759, a novel antiulcer agent were compared with those of cetraxate in various experimental ulcer models and on gastric secretion in rats....
The antiulcer effects of OPC-12759, a novel antiulcer agent were compared with those of cetraxate in various experimental ulcer models and on gastric secretion in rats. OPC-12759 (0.3-30 mg/kg, b.i.d., p.o.) significantly accelerated the healing rate of acetic acid-induced gastric ulcer in a dose-dependent manner, while cetraxate did not. When administered orally at 0.3-30 mg/kg, b.i.d., for 7 days, pretreatment with OPC-12759 (0.3-30 mg/kg, b.i.d., p.o.) prevented the formation of acute gastric ulcers, induced by: restraint water immersion stress, aspirin, indomethacin, histamine, serotonin, platelet activating factor (PAF) and DDC. Cetraxate showed antiulcer activity against a part of the OPC-12759-positive gastric ulcer models. Given intraperitoneally at the single dosing range of 10-100 mg/kg, OPC-12759 inhibited the formation of these acute gastric ulcer models. OPC-12759 administered orally at 0.3-30 mg/kg, b.i.d., for 7 days did not inhibit basal gastric secretion in pylorus ligated rats. The results indicated that OPC-12759 possesses wide spectrum antiulcer activity as compared with cetraxate.
Topics: Alanine; Animals; Anti-Ulcer Agents; Gastric Mucosa; Male; Perfusion; Quinolones; Rats; Rats, Inbred Strains; Stomach Ulcer; Stress, Psychological
PubMed: 2542684
DOI: 10.1254/jjp.49.441 -
Chemical & Pharmaceutical Bulletin 2011A new series of novel (2S)-2-({2-[1,4-dihydro-3,5-bis(methoxycarbonyl)-2,6-dimethyl-4-(2-nitrophenyl)pyridin-1-yl]-2-oxoethyl}amino)-3-(4-hydroxyphenyl) propanoic acid...
A new series of novel (2S)-2-({2-[1,4-dihydro-3,5-bis(methoxycarbonyl)-2,6-dimethyl-4-(2-nitrophenyl)pyridin-1-yl]-2-oxoethyl}amino)-3-(4-hydroxyphenyl) propanoic acid (3a) and its analogues 3b-j has been synthesized. These compounds were evaluated for their in vitro antioxidant activity, anti-inflammatory activity and antiulcer activity. Compounds 3b and f exhibited significant antioxidant action comparable with that of standard. Efficacy against inflammation and ulceration was also found to be significant. The chemical structures of these compounds were confirmed on the basis of spectral data.
Topics: Amino Acids; Animals; Anti-Inflammatory Agents; Anti-Ulcer Agents; Antioxidants; Butyrates; Nifedipine; Pyridines; Structure-Activity Relationship
PubMed: 21881260
DOI: 10.1248/cpb.59.1153 -
Biomedicine & Pharmacotherapy =... Jun 2021This study investigated the gastroprotective effects and possible mechanism of Kangfuxin (KFX), an ethanol extract of Periplaneta americana L. (Dictyoptera; Blattidae),...
This study investigated the gastroprotective effects and possible mechanism of Kangfuxin (KFX), an ethanol extract of Periplaneta americana L. (Dictyoptera; Blattidae), on improving healing quality and preventing recurrence of gastric ulcer. The effects of KFX were investigated in patients treated with endoscopic submucosal dissection (ESD), gastric ulcer animal model, and rat gastric mucosal cells and fibroblasts. Moreover, the relationship between KFX and p38/NF-κB pathway were explored both in vivo and in vitro. In patients, KFX exhibited protective effects against gastric ulcers and resulted in a decrease in the CD3 expression. In vivo animal experiments confirmed that KFX accelerated ulcer healing by promoting neovascularization (increased CD34 expression), suppressing inflammation (decreased interleukin-1β (IL-1β), myeloperoxidase (MPO), tumor necrosis factor α (TNF-α), intercellular adhesion molecule-1 (ICAM-1), and IL-8 expression), and enhancing growth factor expression, including the epidermal growth factor receptor (EGFR) and hepatocyte growth factor (HGF). In vitro experiments demonstrated that treatment with 10% KFX rat serum decreased IL-1β, IL-1Ra, SIL-1RAP, TNF-α, and ICAM-1 expression in rat gastric mucosal cells or fibroblasts and increased IL-1R expression compared to that in the group treatment with 10% normal rat serum. Furthermore, KFX inhibited the activation of p38/NF-κB pathway both in vivo and in vitro. In conclusion, KFX treatment could effectively improve healing quality and prevent gastric ulcer recurrence, which might be attributed to neovascularization, suppressed inflammation, and enhanced growth factor expression. The p38/NF-κB pathway may be one of important mechanism to mediate the effects of KFX.
Topics: Animals; Anti-Ulcer Agents; Cells, Cultured; Female; Gastric Mucosa; Humans; Male; Materia Medica; Rats; Recurrence; Stomach Ulcer; Treatment Outcome; Wound Healing
PubMed: 33761454
DOI: 10.1016/j.biopha.2021.111513 -
Lansoprazole fast disintegrating tablet: a new formulation for an established proton pump inhibitor.Digestion 2003Lansoprazole is a proton pump inhibitor (PPI) which is an effective and well-tolerated treatment option in the management of acid-related disorders. Lansoprazole fast... (Review)
Review
Lansoprazole is a proton pump inhibitor (PPI) which is an effective and well-tolerated treatment option in the management of acid-related disorders. Lansoprazole fast disintegrating tablet (LFDT)--a new, patient-friendly and more convenient formulation of lansoprazole which can be taken with or without water--is the first PPI to be made available as an orally disintegrating tablet. It represents an innovative drug delivery system, comprising enteric-coated microgranules of lansoprazole compressed with an inactive, rapidly dispersing matrix to form a tablet. When the tablet is placed on the tongue and sucked gently it disintegrates rapidly in the mouth, releasing the enteric-coated microgranules which are swallowed with the patient's saliva without water. Alternatively, the tablet can be swallowed with a drink of water. Studies have shown that the bioavailability of LFDT is comparable to lansoprazole capsules, at both 15 and 30 mg doses; the indications and recommended dosages for LFDT are therefore identical to lansoprazole capsules. The new formulation may be of particular benefit to those with active life-styles who do not always have water available, patients who have difficulty in swallowing, and elderly patients.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Administration, Oral; Anti-Ulcer Agents; Biological Availability; Chemistry, Pharmaceutical; Clinical Trials as Topic; Humans; Lansoprazole; Omeprazole; Peptic Ulcer; Proton Pump Inhibitors; Tablets
PubMed: 12743433
DOI: 10.1159/000070393 -
BMC Pediatrics Jul 2016The aim of this study was to determine the effect of gestational age on pharmacokinetics of ranitidine in newborns with gastroesophageal reflux. (Clinical Trial)
Clinical Trial
BACKGROUND
The aim of this study was to determine the effect of gestational age on pharmacokinetics of ranitidine in newborns with gastroesophageal reflux.
METHODS
A prospective, descriptive and pharmacokinetic study was carried out in 30 pre-term and 20 full-term babies. 3 mg/kg of ranitidine was administered intravenously to all the babies and at 0.25, 0.5, 1, 2, 4, and 8 h following the administration, samples of blood were drawn to assess ranitidine levels using high performance liquid chromatographic technique.
RESULTS
Pharmacokinetics of ranitidine had a bi-exponential behavior with a half-life elimination of (t1/2el) 2.79 h, area under curve (AUC) of 1688 ng/mL, volume of distribution (Vd) of 1.44 L/kg, and clearance (Cl) of 5.9 L/kg/h. The median plasmatic concentration in pre-terms was 1113 ng/mL and 280 ng/mL in full-terms. Vd, t1/2 and Cl presented high values in preterm although the correlation of Cl with glomerular filtration in term newborns was better.
CONCLUSIONS
Plasma levels of ranitidine depend on the gestational age of the newborns. However, the possible relationship between after-birth age and pharmacokinetics of the neonates as their internal organs get matured without minding their gestational background.
Topics: Anti-Ulcer Agents; Area Under Curve; Chromatography, High Pressure Liquid; Female; Gastroesophageal Reflux; Gestational Age; Half-Life; Humans; Infant, Newborn; Infant, Premature; Infant, Premature, Diseases; Injections, Intravenous; Male; Prospective Studies; Ranitidine
PubMed: 27412521
DOI: 10.1186/s12887-016-0630-x -
Fitoterapia Oct 2020Jatropha elliptica (Pohl) Oken (Euphorbiaceae) roots are used in folk medicine to treat gastric ulcers. The purpose of this work was to evaluate the gastroprotective...
Jatropha elliptica (Pohl) Oken (Euphorbiaceae) roots are used in folk medicine to treat gastric ulcers. The purpose of this work was to evaluate the gastroprotective activity of ethanol extract (JER) and hexane fraction (ERH) of J. elliptica roots in mice, as well as to analyze the acute toxicity of the extract and identify the potential active compounds. No signs of toxicity were observed in JER. In both acidified ethanol and indometacin-induced gastric ulcer models, all doses tested of JER and ERH significantly reduced gastric lesions. Dereplication of JER was performed by HPLC-DAD-ESI-MS/MS and resulted in the annotation of compounds fraxetin, propacin, jatrophone and jatropholones A and B. GC-MS analysis of ERH revealed the diterpenes jatrophone, jatropholone A and jatropholone B as the major components. The chemical study of this fraction has led to the isolation of these compounds, in addition to the sequiterpene cyperenoic acid and the diterpene 2β-hydroxyjatrophone, both reported for the first time in J. elliptica. The isolated compounds were tested against L929 cells and only cyperenoic acid and the mixture of jatropholones A and B did not show toxicity, being then selected as good candidates for bioassays using acidified ethanol-induced gastric ulcer model. Cyperenoic acid significantly decreased gastric lesions and preserved gastric mucus layer. The mixture of jatropholones A and B caused a smaller reduction of gastric lesions, without preservation of the gastric mucus layer. The study showed that J. elliptica roots present gastroprotective activity in mice, without causing acute toxic effects. The activity is related, at least in part, to the occurrence of terpenes, mainly the sesquiterpene cyperenoic acid.
Topics: Animals; Anti-Ulcer Agents; Brazil; Cell Line, Tumor; Diterpenes; Female; Jatropha; Male; Medicine, Traditional; Mice; Molecular Structure; Phytochemicals; Plant Extracts; Plant Roots; Sesquiterpenes; Stomach Ulcer; Toxicity Tests, Acute
PubMed: 32827695
DOI: 10.1016/j.fitote.2020.104707 -
Alimentary Pharmacology & Therapeutics Oct 1999Rabeprazole is a new, highly potent proton pump inhibitor (PPI) being introduced for the treatment of disorders of gastric acid hypersecretion. Rabeprazole joins other... (Review)
Review
Rabeprazole is a new, highly potent proton pump inhibitor (PPI) being introduced for the treatment of disorders of gastric acid hypersecretion. Rabeprazole joins other drugs in this class, such as omeprazole, pantoprazole, and lansoprazole, which share a common mechanism of action. Each of these drugs is a substituted benzimidazole, which inhibits activity of the H+, K+ -ATPase located on the apical surface of parietal cells, thereby preventing the secretion of gastric acid. As a result of structural and functional similarities, the PPIs share many pharmacokinetic features. They have comparable rates of absorption, maximum plasma concentrations, and total drug absorptions resulting in similar bioavailability after single-dose administration. With multiple dosing, rabeprazole differs from omeprazole in that its pharmacokinetic profile does not change significantly over the course of therapy. All the PPIs are metabolized rapidly, resulting in short half-lives. However, their duration of activity is much longer, due to the way in which they bind to H+, K+ -ATPase. All are metabolized by hepatic cytochrome P450 enzymes, although only omeprazole has demonstrated significant interactions with other drugs metabolized by this pathway. Rabeprazole, which has a low potential for interacting with drugs metabolized by cytochrome P450, does interfere with the absorption of digoxin and ketoconazole because of its antisecretory effects. The pharmacokinetics of rabeprazole are altered slightly in elderly subjects and in patients with renal and moderate hepatic disease. However, the pharmacokinetic findings suggest that no dosage adjustment is required in these special populations.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Anti-Ulcer Agents; Benzimidazoles; Enzyme Inhibitors; Humans; Omeprazole; Rabeprazole
PubMed: 10555604
DOI: 10.1046/j.1365-2036.1999.00034.x -
Molecules (Basel, Switzerland) May 2014Essential oils have attracted considerable worldwide attention over the last few decades. These natural products have wide-ranging pharmacological activities and... (Review)
Review
Essential oils have attracted considerable worldwide attention over the last few decades. These natural products have wide-ranging pharmacological activities and biotechnological applications. Faced with the need to find new anti-ulcer agents and the great effort on the development of drugs for the treatment of ulcers, in this review, the anti-ulcer activities of 21 bioactive compounds found in essential oils are discussed.
Topics: Anti-Ulcer Agents; Humans; Oils, Volatile; Ulcer
PubMed: 24802985
DOI: 10.3390/molecules19055717 -
Basic & Clinical Pharmacology &... Mar 2004Proton pump inhibitors are used at different dosages for the treatment of acid-related gastrointestinal disorders, such as gastro-oesophaeal reflux and peptic ulcer... (Review)
Review
Proton pump inhibitors are used at different dosages for the treatment of acid-related gastrointestinal disorders, such as gastro-oesophaeal reflux and peptic ulcer disease. Comparisons of four different proton pump inhibitors: lansoprazole, omeprazole, pantoprazole, and rabeprazole show that they all have similar potency and efficacy. Rabeprazole, however, displays a slightly more rapid onset of acid inhibition than the others; the clinical advantage of this seems limited. The S-isomer of omeprazole, esomeprazole, exhibits a somewhat higher potency than the other proton pump inhibitors. Reports supporting a clinical advantage of this property are not convincing. To conclude, all inhibitors seem comparable as regards inhibition of gastric acid secretion.
Topics: Anti-Ulcer Agents; Esophagitis, Peptic; Gastric Acid; Humans; Peptic Ulcer; Proton Pump Inhibitors
PubMed: 15049339
DOI: 10.1111/j.1742-7843.2004.pto940302.x -
Canadian Family Physician Medecin de... Jul 2006A 36-year-old pregnant patient has symptoms of peptic disease. Treatment with diet and lifestyle modifications and also antacids has given her little relief. If she were... (Review)
Review
QUESTION
A 36-year-old pregnant patient has symptoms of peptic disease. Treatment with diet and lifestyle modifications and also antacids has given her little relief. If she were not pregnant, I would prescribe a proton pump inhibitor (PPI) for her. She is now 4 weeks pregnant, and I need to determine whether PPIs are safe during pregnancy.
ANSWER
Data currently available suggest that omeprazole is not teratogenic in humans. While information on other PPIs is limited, a systematic review of the evidence suggests that they are also not teratogenic.
Topics: Anti-Ulcer Agents; Breast Feeding; Drug-Related Side Effects and Adverse Reactions; Female; Gastroesophageal Reflux; Humans; Pregnancy; Pregnancy Complications; Proton Pump Inhibitors
PubMed: 16893146
DOI: No ID Found