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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 -
Journal of Veterinary Internal Medicine 2010Despite frequent clinical use, information about the pharmacokinetics and efficacy of pantoprazole in camelids is not available.
BACKGROUND
Despite frequent clinical use, information about the pharmacokinetics and efficacy of pantoprazole in camelids is not available.
OBJECTIVES
To examine the pharmacokinetics of both IV and SC pantoprazole and to determine whether pantoprazole administration would increase 3rd compartment pH in alpacas.
ANIMALS
Six healthy adult alpacas.
METHODS
Alpacas were fitted with a 3rd compartment cannula for measuring gastric pH. After recovery, alpacas received 1 mg/kg pantoprazole IV, q24h for 3 days or 2 mg/kg SC q24h for 3 days. Alpacas received both IV and SC pantoprazole, with a minimum of 3 weeks between treatments. Third compartment pH was recorded and plasma samples were taken for pharmacokinetic analysis.
RESULTS
Pantoprazole induced a slow but sustained increase in 3rd compartment pH when given by both the IV and SC routes. Third compartment pH was significantly increased as compared with baseline values (1.81+/-0.7; mean+/-SD) at 24 (2.47+/-0.8), 48 (3.53+/-1.0) and 72 hours (4.03+/-1.3) after daily IV administration of pantoprazole. Third compartment pH increased from 1.73+/-0.6 at baseline to 3.05+/-1.1, 4.02+/-1.4, and 3.61+/-1.6 at 24, 48, and 72 hours after SC administration, respectively. Pharmacokinetic analysis demonstrated that pantoprazole had a short elimination half-life (0.47+0.06 h) and a high clearance rate (12.2+/-2.9 mL/kg/min) after both IV and SC administration.
CONCLUSIONS AND CLINICAL RELEVANCE
Based on the results of this study, pantoprazole represents a safe and effective drug for increasing 3rd compartment pH in camelids. Either IV or SC administration is likely to be an effective treatment for gastric ulcers.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Animals; Anti-Ulcer Agents; Camelids, New World; Hydrogen-Ion Concentration; Pantoprazole; Stomach Ulcer
PubMed: 20384953
DOI: 10.1111/j.1939-1676.2010.0508.x -
Praxis 2019
Topics: Gastroesophageal Reflux; Humans; Pantoprazole; Proton Pump Inhibitors
PubMed: 31822229
DOI: 10.1024/1661-8157/a003342 -
Clinical Drug Investigation 2007Gastro-oesophageal reflux disease (GORD) is associated with a broad array of symptoms that may be typical or atypical of the disease and that may be accompanied by... (Comparative Study)
Comparative Study Review
Gastro-oesophageal reflux disease (GORD) is associated with a broad array of symptoms that may be typical or atypical of the disease and that may be accompanied by erosive oesophagitis. Symptom scales that have historically been employed to assess response to treatment in GORD clinical trials do not typically account for the heterogeneous, episodic nature of GORD and the poor correlation between patients' and physicians' assessment of symptoms. The ReQuest questionnaire permits self-assessment of changes on a broad range of GORD-related symptoms on a daily basis and in combination with the Los Angeles (LA)-classification (ReQuest/LA-classification) to assess complete remission of GORD. Pantoprazole and esomeprazole are two of the newer proton pump inhibitors and are the first to be systematically reviewed using the ReQuest(trade mark) questionnaire. Results from recent head-to-head trials have shown pantoprazole and esomeprazole to be highly and equally effective treatments for (i) rapid and sustained relief of ReQuest-assessed GORD-related symptoms in patients with non-erosive GORD or endoscopically confirmed erosive GORD, and (ii) achieving a combined outcome comprising endoscopically confirmed healing and ReQuest-assessed symptom relief in patients with erosive GORD. There is some preliminary evidence to suggest that pantoprazole may be the better choice of treatment in terms of its potential to maintain control of symptoms in patients for whom night-time symptoms are a concern and if taken as on-demand rather than continuous maintenance therapy.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Anti-Ulcer Agents; Databases, Factual; Esomeprazole; Gastroesophageal Reflux; Humans; Pantoprazole; Proton Pump Inhibitors; Psychometrics; Reproducibility of Results; Severity of Illness Index; Surveys and Questionnaires; Treatment Outcome
PubMed: 17803341
DOI: 10.2165/00044011-200727100-00001 -
Medical Oncology (Northwood, London,... Aug 2021Cisplatin is used to treat solid malignancies including head and neck cancer. However, nephrotoxicity limits its use. In this study, we looked for a possible protective... (Randomized Controlled Trial)
Randomized Controlled Trial
Cisplatin is used to treat solid malignancies including head and neck cancer. However, nephrotoxicity limits its use. In this study, we looked for a possible protective effect of pantoprazole against cisplatin-induced nephrotoxicity. We used novel biomarkers for early detection of nephrotoxicity. Sixty chemotherapy naïve head and neck cancer patients completed the study. Following complete history taking and thorough clinical examination, patients were randomly divided into three groups: 20 patients in each. Group I (control group) received cisplatin without pantoprazole, groups II and III received pantoprazole 80 mg and 40 mg, respectively, concurrently with cisplatin. Blood and urine samples were collected at baseline, and 48 h after the first and third cycles of cisplatin administration. Assessment of serum creatinine and soluble FasL (sFasL), as well as urinary neutrophil gelatinase-associated lipocalin (NGAL) and kidney injury molecule-1 (KIM-1) was performed. Nephrotoxicity was detected in 6 patients in group I, none in group II and 3 patients in group III. Serum creatinine significantly increased at the end of treatment in group I compared to groups II and III. Group I also had significantly higher urinary KIM-1 and NGAL and serum sFasL compared to groups II and III after the first and third cycles. On the contrary, there was no significant difference between groups II and III. Pantoprazole prevented the increase in acute kidney injury biomarkers in cisplatin-treated patients. Therefore, it is a promising agent in reducing cisplatin-induced nephrotoxicity.Trial registration Clinical Trials.gov identifier: NCT04217512, registered in January 2020 " retrospectively registered".
Topics: Acute Kidney Injury; Antineoplastic Combined Chemotherapy Protocols; Cisplatin; Docetaxel; Female; Fluorouracil; Follow-Up Studies; Head and Neck Neoplasms; Humans; Male; Middle Aged; Pantoprazole; Prognosis; Proton Pump Inhibitors; Retrospective Studies
PubMed: 34357466
DOI: 10.1007/s12032-021-01558-y -
Clinical Therapeutics Aug 2001Patients with impaired hepatic function usually require gastric acid-suppressant therapy but are at increased risk for drug interactions and may require dosage...
BACKGROUND
Patients with impaired hepatic function usually require gastric acid-suppressant therapy but are at increased risk for drug interactions and may require dosage adjustments. The proton pump inhibitor pantoprazole is rapidly absorbed and eliminated, primarily by cytochrome P450 (CYP) 2C19 isozymes.
OBJECTIVE
This study sought to determine whether dosage adjustment of pantoprazole is required in patients with moderate or severe hepatic impairment by comparing the pharmacokinetic profile of pantoprazole in such patients with that in healthy slow metabolizers of pantoprazole, in whom no dosage adjustment is required.
METHODS
Patients with moderate (Child-Pugh class B) and severe (Child-Pugh class C) hepatic impairment received oral pantoprazole 40 mg once daily on days 1 through 4 and then on alternate days (days 6 and 8). Serial blood samples were collected on days 4 and 8 for analyses of plasma pantoprazole concentrations. Pharmacokinetic data were compared between the 2 groups with hepatic impairment and against historical data from 17 healthy subjects who were genetically slow CYP2C19 metabolizers of pantoprazole.
RESULTS
Twenty-two patients participated in the study, 13 in the Child-Pugh class B group and 9 in the Child-Pugh class C group. No clinically significant differences in pantoprazole pharmacokinetics were noted between the patients with hepatic impairment and the healthy slow metabolizers of pantoprazole on days 4 and 8. Pantoprazole was well tolerated. Four Child-Pugh class B patients and 3 Child-Pugh class C patients reported > or = 1 adverse event. Adverse events were generally mild or moderate, and were similar to those reported in healthy subjects. Two patients discontinued the study because of severe events related to their underlying disease.
CONCLUSIONS
The pharmacokinetics and tolerability of pantoprazole were similar in patients with moderate hepatic impairment, patients with severe hepatic impairment, and healthy slow metabolizers of pantoprazole, in whom no dosage adjustment is required. Thus, no dosage adjustment of pantoprazole is required in patients with hepatic impairment, regardless of its severity. However, caution should be exercised when giving pantoprazole to patients with severe hepatic impairment.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Adolescent; Adult; Aged; Benzimidazoles; Dose-Response Relationship, Drug; Enzyme Inhibitors; Female; Humans; Liver Diseases; Male; Middle Aged; Omeprazole; Pantoprazole; Sulfoxides
PubMed: 11558857
DOI: 10.1016/s0149-2918(01)80100-4 -
European Journal of Pharmacology Aug 1992The action of the H+/K(+)-ATPase inhibitors pantoprazole and omeprazole was compared in different in vitro test systems. In gastric membrane vesicles under conditions... (Comparative Study)
Comparative Study
The action of the H+/K(+)-ATPase inhibitors pantoprazole and omeprazole was compared in different in vitro test systems. In gastric membrane vesicles under conditions shown to result in acidification of the vesicle interior, pantoprazole and omeprazole inhibited H+/K(+)-ATPase activity with IC50 values of 6.8 and 2.4 microM, respectively. When intravesicular acidification was reduced by inclusion of imidazole (5 mM), a membrane permeable weak base, the inhibitory action of omeprazole was partially lost (IC50 30 microM) and that of pantoprazole almost completely lost. After incubation for 40 min with pumping membrane vesicles, a half-maximal reduction in intravesicular H+ concentration occurred at pantoprazole and omeprazole concentrations of 1.1 and 0.6 microM, respectively. Again, when the intravesicular H+ concentration was reduced by inclusion of imidazole (2.5 mM), pantoprazole (20 and 60 microM) did not reduce the remaining intravesicular proton concentration, whereas omeprazole (10 and 30 microM) did. Both drugs inhibited, with similar potency, papain activity at pH 3.0 and inactivated the enzyme in a similar time-dependent manner; at pH 5.0 omeprazole (IC50 17 microM) was more potent than pantoprazole (IC50 37 microM) and enzyme inhibition was faster than with pantoprazole. These results indicate that pantoprazole is a potent inhibitor of H+/K(+)-ATPase under highly acidic conditions and that it is more stable than omeprazole at a slightly acidic pH such as pH 5.0.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Animals; Benzimidazoles; Glutathione; Hydrogen-Ion Concentration; In Vitro Techniques; Omeprazole; Pantoprazole; Papain; Proton Pump Inhibitors; Sulfoxides; Swine
PubMed: 1330598
DOI: 10.1016/0014-2999(92)90178-7 -
Chemosphere Jan 2022A new electrochemical sensor based on LiFeMnO/C-CN (LFMO/CCN)/1-ethyl-3-methylimidazolium chloride modified carbon paste electrode (CPE) has been constructed to measure...
A new electrochemical sensor based on LiFeMnO/C-CN (LFMO/CCN)/1-ethyl-3-methylimidazolium chloride modified carbon paste electrode (CPE) has been constructed to measure pantoprazole sodium (PNZS). The electrochemical impedance spectroscopy (EIS) method was employed to evaluate the electrode charge-transfer resistances. Moreover, the differential pulse voltammetry method was used to detect PNZS in phosphate buffer solution (PBS) at pH 7.0. The detection limit of 80.0 × 10 M and 10.9 × 10 M was obtained under optimal conditions in the linear concentration range of PNZS 0.09-100 μM and 100-900 μM. Chronoampermetry technique was utilized to determine the diffusion coefficient (D) of PNZS on the modified electrode surface. The CCN/LFMO/IL/CPE was successfully used to determine PNZS in various drug formulations such as tablets and vials. Finally, simultaneous determination of PNZS and acetaminophen was accomplished with no interference based on the proposed sensor.
Topics: Carbon; Electrochemical Techniques; Electrodes; Nanocomposites; Pantoprazole
PubMed: 34560499
DOI: 10.1016/j.chemosphere.2021.132311 -
Cellular and Molecular Neurobiology Jan 2021Recent studies have shown that proton pump inhibitors have positive effects on the nervous system. However, its effect on epileptic seizure and neuronal damage are still...
The Effects of Proton Pump Inhibitors (Pantoprazole) on Pentylenetetrazole-Induced Epileptic Seizures in Rats and Neurotoxicity in the SH-SY5Y Human Neuroblastoma Cell Line.
Recent studies have shown that proton pump inhibitors have positive effects on the nervous system. However, its effect on epileptic seizure and neuronal damage are still unclear. In this study, it was aimed to investigate the effect of pantoprazole on pentylenetetrazole-induced epileptic seizures in rats and neurotoxicity in the SH-SY5Y cell line. Animals were divided into three groups: control, saline (1 mL/kg serum physiologic), and pantoprazole (10 mg/kg). Pentylenetetrazole (45 mg/kg) was given to induce a seizure and a passive avoidance test trial was carried out to evaluate memory function. 8-hydroxy-2'-deoxyguanosine (8-OHdG), caspase-3, and brain-derived neurotrophic factor (BDNF) levels were measured in the brain by commercial kits. SH-SY5Y cells were treated with saline or pantoprazole for one hour, and then pentylenetetrazole (30 µm) was added to the medium to induce neurotoxicity. After 24 h, cell viability, total antioxidant, total oxidant status, and apoptosis were measured in SH-SY5Y cells. It was found that pantoprazole treatment postponed epileptic seizure onset, protected memory, reduced 8-OHdG, caspase-3, and also increased BDNF in the brain. In addition, it blocked pentylenetetrazole toxicity, apoptosis, increased antioxidant, and decreased oxidant status in SH-SY5Y cells. Pantoprazole significantly improved seizure, oxidative stress, and apoptosis. Thus, pantoprazole could be used as a supportive therapeutic agent in epilepsy.
Topics: 8-Hydroxy-2'-Deoxyguanosine; Animals; Antioxidants; Apoptosis; Brain; Brain-Derived Neurotrophic Factor; Caspase 3; Cell Line, Tumor; Cell Survival; Humans; Male; Neuroblastoma; Neurotoxins; Oxidants; Oxidative Stress; Pantoprazole; Pentylenetetrazole; Proton Pump Inhibitors; Rats, Wistar; Seizures; Rats
PubMed: 32862257
DOI: 10.1007/s10571-020-00956-6 -
Journal of Anesthesia Aug 2011The most frequent causes of anaphylaxis during anesthesia are neuromuscular blocking agents, antibiotics, and latex. Proton pump inhibitors (PPI) are widely used during...
The most frequent causes of anaphylaxis during anesthesia are neuromuscular blocking agents, antibiotics, and latex. Proton pump inhibitors (PPI) are widely used during major surgery for the prevention of stress ulcers, but cases of perioperative anaphylactic reactions to these have rarely been reported. We present a 50-year-old male patient who experienced an episode of anaphylaxis with hypoxemia, hypotension, tachycardia, and generalized erythema after intravenous injection of pantoprazole 40 mg and methylprednisolone 1 g during general anesthesia. After resuscitation, the patient recovered without any sequelae. Six months after the surgery, a skin test was positive to pantoprazole.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Anaphylaxis; Anesthesia, General; Drug Hypersensitivity; Humans; Male; Middle Aged; Pantoprazole; Proton Pump Inhibitors
PubMed: 21626263
DOI: 10.1007/s00540-011-1148-x