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Journal of Medical Case Reports Mar 2022Omeprazole belongs to the pharmacological classifications of proton pump inhibitors and is a widely used medicine. All proton pump inhibitors have a common mechanism of...
BACKGROUND
Omeprazole belongs to the pharmacological classifications of proton pump inhibitors and is a widely used medicine. All proton pump inhibitors have a common mechanism of action and are prodrugs that require activation in an acidic environment. Omeprazole is extensively metabolized in the liver by cytochrome 2C19 and cytochrome 3A4, which are responsible for drug interactions. Omeprazole-induced galactorrhea is a rare adverse event of drug metabolism and is often underreported.
CASE PRESENTATION
This is a case of a 26-year-old unmarried Asian (Bhutanese) female who underwent kidney transplant and was administered standard antirejection medication (tacrolimus, prednisolone, and leflunomide) along with an antihypertensive agent. She came to the emergency department with complaints of nausea, vomiting, abdominal pain, chronic gastritis, anemia, hypertension, and loss of appetite. The tacrolimus trough level was in the subtherapeutic range at admission. The tacrolimus dose was adjusted, and oral omeprazole was administered. After 3 days, she experienced milk production from her left breast, which according to the patient was her second incidence after omeprazole ingestion.
CONCLUSION
Causality assessment using Naranjo's algorithm and recovering from galactorrhea after stopping omeprazole and omeprazole rechallenge with the reappearance of galactorrhea confirmed omeprazole as the causative agent. Tacrolimus interferes with omeprazole metabolism and increases tacrolimus levels in the blood. Caution needs to be taken when omeprazole is administered with other drugs that interfere with metabolizing enzymes.
Topics: Adult; Bhutan; Female; Galactorrhea; Humans; Kidney Transplantation; Omeprazole; Pregnancy; Tacrolimus
PubMed: 35339194
DOI: 10.1186/s13256-022-03337-3 -
Journal of Veterinary Pharmacology and... Apr 2017Omeprazole is used concurrently with clopidogrel to reduce gastrointestinal adverse effects. In humans, the concurrent use of these two drugs can reduce the antiplatelet... (Clinical Trial)
Clinical Trial
Omeprazole is used concurrently with clopidogrel to reduce gastrointestinal adverse effects. In humans, the concurrent use of these two drugs can reduce the antiplatelet efficacy of clopidogrel. Our objective was to determine the effects of omeprazole and clopidogrel on platelet function in healthy dogs. A crossover study utilized turbidimetric aggregometry (ADP and collagen) and the PFA-100 with the collagen/ADP cartridge to evaluate platelet function in eight healthy dogs during the administration of clopidogrel (1 mg/kg/24 h p.o.), omeprazole (1 mg/kg/24 h p.o.), and a combination of clopidogrel and omeprazole. Drug metabolite concentrations were also measured. Compared to pretreatment, on Days 3 and 5, with ADP as the agonist, there was a significant decrease in maximum amplitude on aggregometry for both clopidogrel and clopidogrel/omeprazole groups. The following revealed no significant differences between clopidogrel and clopidogrel/omeprazole groups when compared on Days 3 and 5: maximum amplitude on aggregometry with ADP or collagen agonists, and PFA-100 closure times. When compared to the clopidogrel group, clopidogrel metabolite concentrations in the clopidogrel/omeprazole group were significantly higher on Days 3 and 5. The concurrent administration of omeprazole and clopidogrel in healthy dogs was associated with an increase in the plasma concentration of an inactive metabolite of clopidogrel, but does not significantly alter the antiplatelet effects of clopidogrel.
Topics: Animals; Blood Platelets; Clopidogrel; Cross-Over Studies; Dogs; Drug Therapy, Combination; Female; Male; Omeprazole; Platelet Aggregation Inhibitors; Platelet Function Tests; Proton Pump Inhibitors; Ticlopidine
PubMed: 27452307
DOI: 10.1111/jvp.12340 -
Journal of Primary Care & Community... 2023The aims of this study were to analyze proton pump inhibitor (PPI) users in Germany, defining and classifying them in terms of treatment appropriateness, and to analyze...
The aims of this study were to analyze proton pump inhibitor (PPI) users in Germany, defining and classifying them in terms of treatment appropriateness, and to analyze the PPI prescription practices of healthcare providers. The updated DGVS (Deutsche Gesellschaft für Gastroenterologie, Verdauungs-und Stoffwechselkrankheiten) gastroesophageal reflux disease (GERD) treatment guideline (published March 2023) for mild heartburn symptoms recommends carrying out a probatory treatment of mild symptoms via other medication such as antacids, alginates, and H2 blockers before escalating to PPI treatments, if the patient profile allows. This retrospective cross-sectional study was based on data from the IQVIA™ Disease Analyzer database (DA) and included adult patients (18 years or older) in 1006 general and 39 gastroenterological practices in Germany who received at least 1 PPI prescription or alginate between September 2019 and September 2021 (hereinafter referred to as the index period). Analyses included indications associated with PPI prescription, co-diagnoses, co-therapies of PPI patients, duration of PPI therapy, dosages of PPI prescriptions, and proportions of practices prescribing PPIs and alginates. A total of 472 146 patients taking PPIs and 9101 patients taking alginates were available for analysis. Very few patients (4.5%) of the total cohort were treated in complete adherence to treatment guidelines. Conditions such as gastritis and duodenitis (47.2%) and reflux diseases (38.4%) were more frequently associated with PPI prescriptions. The average PPI treatment period lasted 141 days, and 36.6% of patients were treated for >6 months. High doses were prescribed relatively often (ie, 42.8% of esomeprazole prescriptions were 40 mg, 59.1% of lansoprazole prescriptions 30 mg, 28.6% of omeprazole prescriptions 40 mg). With each practice prescribing PPIs to at least 10% of their patients; 72% of general practitioners (GPs) and 8% of GENTS (Gastroenterologists) prescribed alginates. This study highlights that discrepancies exist between clinical guidelines and real-life prescribing practices of PPIs in Germany. Particular attention should be given to the incidence of patients being prescribed high-dose or long-duration PPI with mild indications. These findings are particularly apt considering the publication (March 2023) of new guidelines on the "management of gastroesophageal reflux disease and eosinophilic esophagitis," by the DGVS.
Topics: Adult; Humans; Proton Pump Inhibitors; Retrospective Studies; Cross-Sectional Studies; Omeprazole; Lansoprazole; Gastroesophageal Reflux
PubMed: 38142444
DOI: 10.1177/21501319231221002 -
The FEBS Journal Jul 2021Under physiological conditions, cells produce low basal levels of reactive oxygen species (ROS); however, in pathologic conditions ROS production increases dramatically,...
Under physiological conditions, cells produce low basal levels of reactive oxygen species (ROS); however, in pathologic conditions ROS production increases dramatically, generating high concentrations of toxic unsaturated aldehydes. Aldehyde dehydrogenases (ALDHs) are responsible for detoxification of these aldehydes protecting the cell. Due to the physiological relevance of these enzymes, it is important to design strategies to modulate their activity. It was previously reported that omeprazole activation of ALDH1A1 protected Escherichia coli cells overexpressing this enzyme, from oxidative stress generated by H O . In this work, omeprazole cell protection potential was evaluated in eukaryotic cells. AS-30D cell or hepatocyte suspensions were subjected to a treatment with omeprazole and exposure to light (that is required to activate omeprazole in the active site of ALDH) and then exposed to H O . Cells showed viability similar to control cells, total activity of ALDH was preserved, while cell levels of lipid aldehydes and oxidative stress markers were maintained low. Cell protection by omeprazole was avoided by inhibition of ALDHs with disulfiram, revealing the key role of these enzymes in the protection. Additionally, omeprazole also preserved ALDH2 (mitochondrial isoform) activity, diminishing lipid aldehyde levels and oxidative stress in this organelle, protecting mitochondrial respiration and transmembrane potential formation capacity, from the stress generated by H O . These results highlight the important role of ALDHs as part of the antioxidant system of the cell, since if the activity of these enzymes decreases under stress conditions, the viability of the cell is compromised.
Topics: Aldehyde Dehydrogenase 1 Family; Animals; Cell Survival; Cells, Cultured; Enzyme Activation; Female; Humans; Hydrogen Peroxide; Light; Lipid Peroxidation; Omeprazole; Oxidants; Oxidative Stress; Rats, Wistar; Reactive Oxygen Species; Rats
PubMed: 33400378
DOI: 10.1111/febs.15698 -
Alternative Therapies in Health and... Mar 2023Helicobacter pylori (Hp) is one of the most prevalent pathogenic microorganisms in the world, which is related to gastric ulcer.
BACKGROUND
Helicobacter pylori (Hp) is one of the most prevalent pathogenic microorganisms in the world, which is related to gastric ulcer.
OBJECTIVE
To observe the effect of lansoprazole and omeprazole combined with antibiotics on gastric juice pH and inflammatory factors in elderly patients with Hp positive gastric ulcer.
DESIGN
This study was a prospective observation study.
SETTING
This study was performed in Department of Gastroenterology, First Affiliated Hospital of Soochow University.
PARTICIPANTS
One hundred and ten elder patients with Hp positive gastric ulcer admitted to our hospital from January 2019 to May 2020.
INTERVENTION
The control group was treated with omeprazole combined with antibiotics, and the observation group was treated with lansoprazole combined with antibiotics.
PRIMARY OUTCOME MEASURES
The level of gastric juice pH, interleukin-1 (IL-1), interleukin-8 (IL-8), tumor necrosis factor-α (TNF-α) and heat shock protein-70 (HSP-70).
METHODS
The changes of gastric juice pH value, IL-1, IL-8, TNF-α and HSP-70 levels before and after treatment were detected in the two groups. The total effective rate, Hp eradication rate, mature type of regenerated mucosal tissue surrounding ulcer and adverse reaction rate were statistically analyzed.
RESULTS
The total effective rate and Hp eradication rate in the observation group were higher than those in the control group, while the adverse reaction rate in the observation group was lower than that in the control group (P < .05). After treatment, the pH value of gastric juice and HSP-70 in the observation group were higher than those in the control group, while the IL-1, IL-8 and TNF-α were lower than those in the control group (P < .05). The mature type of regenerated mucosal tissue structure around ulcer in the observation group was better than that in the control group (P < .05).
CONCLUSION
The overall effect of lansoprazole combined with antibiotics in the treatment of Hp positive gastric ulcer in the elderly is better than that of omeprazole combined with antibiotics.
Topics: Humans; Aged; Omeprazole; Lansoprazole; Stomach Ulcer; Interleukin-8; Anti-Ulcer Agents; Tumor Necrosis Factor-alpha; Ulcer; Prospective Studies; Helicobacter Infections; Anti-Bacterial Agents; Gastric Juice; Anti-Infective Agents; Interleukin-1; Hydrogen-Ion Concentration; Helicobacter pylori; Drug Therapy, Combination
PubMed: 36525356
DOI: No ID Found -
Drug-drug interaction of microdose and regular-dose omeprazole with a CYP2C19 inhibitor and inducer.Drug Design, Development and Therapy 2017A microdose drug-drug interaction (DDI) study may be a valuable tool for anticipating drug interaction at therapeutic doses. This study aimed to compare the magnitude of... (Clinical Trial)
Clinical Trial
PURPOSE
A microdose drug-drug interaction (DDI) study may be a valuable tool for anticipating drug interaction at therapeutic doses. This study aimed to compare the magnitude of DDIs at microdoses and regular doses to explore the applicability of a microdose DDI study.
PATIENTS AND METHODS
Six healthy male volunteer subjects were enrolled into each DDI study of omeprazole (victim) and known perpetrators: fluconazole (inhibitor) and rifampin (inducer). For both studies, the microdose (100 μg, cold compound) and the regular dose (20 mg) of omeprazole were given at days 0 and 1, respectively. On days 2-9, the inhibitor or inducer was given daily, and the microdose and regular dose of omeprazole were repeated at days 8 and 9, respectively. Full omeprazole pharmacokinetic samplings were performed at days 0, 1, 8, and 9 of both studies for noncompartmental analysis.
RESULTS
The magnitude of the DDI, the geometric mean ratios (with perpetrator/omeprazole only) of maximum concentration (C) and area under the curve to the last measurement (AUC) of the microdose and the regular dose were compared. The geometric mean ratios in the inhibition study were: 2.17 (micro) and 2.68 (regular) for C, and 4.07 (micro), 4.33 (regular) for AUC. For the induction study, they were 0.26 (micro) and 0.21 (regular) for C, and 0.16 (micro) and 0.15 (regular) for AUC. There were no significant statistical differences in the magnitudes of DDIs between microdose and regular-dose conditions, regardless of induction or inhibition.
CONCLUSION
Our results may be used as partial evidence that microdose DDI studies may replace regular-dose studies, or at least be used for DDI-screening purposes.
Topics: Adult; Cross-Over Studies; Cytochrome P-450 CYP2C19; Cytochrome P-450 CYP2C19 Inhibitors; Dose-Response Relationship, Drug; Drug Interactions; Fluconazole; Healthy Volunteers; Humans; Male; Middle Aged; Omeprazole; Rifampin; Young Adult
PubMed: 28408803
DOI: 10.2147/DDDT.S131797 -
Journal of Veterinary Internal Medicine 2023Rebound gastric hyperacidity (RGH) secondary to hypergastrinemia has been suggested to contribute to the rapid recurrence of equine squamous gastric disease (ESGD) in...
Evaluation of the effects of medium-term (57-day) omeprazole administration and of omeprazole discontinuation on serum gastrin and serum chromogranin A concentrations in the horse.
BACKGROUND
Rebound gastric hyperacidity (RGH) secondary to hypergastrinemia has been suggested to contribute to the rapid recurrence of equine squamous gastric disease (ESGD) in horses after discontinuation of omeprazole.
HYPOTHESIS/OBJECTIVES
To evaluate changes in serum gastrin and chromogranin A (CgA) concentrations in response to medium-term (57-day) omeprazole treatment and after omeprazole discontinuation.
ANIMALS
Fourteen mature Thoroughbred racehorses in simulated race training.
METHODS
Horses received 2.28 g of oral omeprazole PO q24h for 57 days within a 61-day period, excluding a withholding period applied mid-protocol during which treatment was stopped as part of a concurrent study. Serum samples were collected on day 0 before omeprazole treatment, on day 1 of each week of the treatment period, and for an additional 5 weeks after discontinuation of treatment. Serum gastrin and CgA concentrations were analyzed using radioimmunoassay (RIA) and ELISA, respectively.
RESULTS
Median serum gastrin concentrations increased 2.5-fold from baseline to day 7 (P < .001) but did not increase further during the omeprazole treatment period. Median serum gastrin concentrations returned to baseline within 2 to 4 days after administration of the last dose of omeprazole. No effect of treatment or discontinuation was seen in serum CgA concentrations.
CONCLUSIONS AND CLINICAL IMPORTANCE
Serum gastrin concentrations increased in response to omeprazole treatment but returned to baseline within 2 to 4 days after the last dose of omeprazole. No effect of treatment or discontinuation was seen in serum CgA concentrations. Our results do not support the use of tapering protocols in horses.
Topics: Horses; Animals; Omeprazole; Chromogranin A; Anti-Ulcer Agents; Gastrins; Stomach
PubMed: 37390114
DOI: 10.1111/jvim.16795 -
European Journal of Gastroenterology &... Jan 2023Nonsteroidal anti-inflammatory drugs and proton pump inhibitors are known to affect the diagnostics of gastrointestinal disorders. The aim of this study was to... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND AND AIM
Nonsteroidal anti-inflammatory drugs and proton pump inhibitors are known to affect the diagnostics of gastrointestinal disorders. The aim of this study was to investigate to what extent omeprazole, diclofenac or co-administration of these affects faecal calprotectin levels and the normalisation interval after cessation.
METHODS
Participants received 20 mg omeprazole daily for 2 weeks in the first sequence, 50 mg oral diclofenac three times daily for 2 weeks in the second and co-administration of these for 2 weeks in the third, with washout periods in between. The first two sequences were randomised to a different order. Faecal calprotectin was measured on days 0, 4, 7, 14, 21, 28 and 35 and thereafter at 7-day intervals until normalisation in each sequence.
RESULTS
Thirty-two healthy volunteers were included. During drug intake, 39% on diclofenac (median 70.8 µg/g; range 50.2-1080 µg/g), 53% on omeprazole (median 85.3 µg/g; range 51.1-249 µg/g) and 69% on omeprazole + diclofenac (median 101.5 µg/g; range 51.5-532 µg/g) had faecal calprotectin levels above normal. In the diclofenac sequence, faecal calprotectin returned to normal in all participants within 2 weeks of cessation and in the omeprazole and co-administration sequences, within 3 weeks of cessation. No statistical significant difference was found with respect to drug order.
CONCLUSION
Short-term intake of omeprazole, diclofenac or co-administration appears to increase faecal calprotectin levels. In patients with increased faecal calprotectin on omeprazole alone or in combination with diclofenac, a repeated faecal calprotectin test is recommended at least 3 weeks after cessation. On diclofenac alone, it is sufficient to repeat the faecal calprotectin test 2 weeks after cessation.
Topics: Humans; Leukocyte L1 Antigen Complex; Omeprazole; Diclofenac; Feces; Proton Pump Inhibitors
PubMed: 36468569
DOI: 10.1097/MEG.0000000000002473 -
British Journal of Hospital Medicine... Oct 2021Gastrointestinal bleeding significantly increases morbidity and mortality rates postoperatively in patients undergoing cardiac surgery. The prophylactic prescribing of...
AIMS/BACKGROUND
Gastrointestinal bleeding significantly increases morbidity and mortality rates postoperatively in patients undergoing cardiac surgery. The prophylactic prescribing of proton pump inhibitors post-cardiac surgery is currently a class IIa recommendation of the European Association of Cardio-Thoracic Surgery.
METHOD
A retrospective review of patients who underwent cardiac surgery between July and December 2019 in the authors' hospital was carried out, using discharge summaries. New treatment charts were introduced with a pre-printed proton pump inhibitor included in the 'regular medication' section of the treatment chart and two reaudits were performed using the same methodology.
RESULTS
Before the intervention, 47% were prescribed omeprazole postoperatively, compared to 74% (<0.001) and 66% (=0.008) in the first and second reaudits respectively. Gastrointestinal bleeding was more common pre-intervention (4% vs 1% respectively; =0.10).
CONCLUSIONS
This intervention resulted in a statistically significant improvement in the prescription of postoperative omeprazole and a decrease in gastrointestinal bleeds. However, other risk factors such as diabetes mellitus, arteriosclerosis and procedure urgency may have contributed to the absence of statistical significance in the latter.
Topics: Cardiac Surgical Procedures; Gastrointestinal Hemorrhage; Humans; Omeprazole; Proton Pump Inhibitors; Retrospective Studies; Thoracic Surgery
PubMed: 34726935
DOI: 10.12968/hmed.2021.0339 -
International Journal of Molecular... Aug 2022(1) Background: Oxaliplatin is used as first-line chemotherapy not only for colorectal cancer but also for gastric and pancreatic cancers. However, it induces peripheral...
(1) Background: Oxaliplatin is used as first-line chemotherapy not only for colorectal cancer but also for gastric and pancreatic cancers. However, it induces peripheral neuropathy with high frequency as an adverse event, and there is no effective preventive or therapeutic method. (2) Methods: The effects of omeprazole, a proton pump inhibitor (PPI), on oxaliplatin-induced peripheral neuropathy (OIPN) was investigated using an in vivo model and a real-world database. (3) Results: In a rat model, oxaliplatin (4 mg/kg, i.p., twice a week for 4 weeks) caused mechanical hypersensitivity accompanied by sciatic nerve axonal degeneration and myelin sheath disorder. Repeated injection of omeprazole (5−20 mg/kg, i.p., five times per week for 4 weeks) ameliorated these behavioral and pathological abnormalities. Moreover, omeprazole did not affect the tumor growth inhibition of oxaliplatin in tumor bearing mice. Furthermore, clinical database analysis of the Food and Drug Administration Adverse Event Reporting System (FAERS) suggests that the group using omeprazole has a lower reporting rate of peripheral neuropathy of oxaliplatin-treated patients than the group not using (3.06% vs. 6.48%, p < 0.001, reporting odds ratio 0.44, 95% confidence interval 0.32−0.61). (4) Conclusions: These results show the preventing effect of omeprazole on OIPN.
Topics: Animals; Antineoplastic Agents; Mice; Neoplasms; Omeprazole; Oxaliplatin; Peripheral Nervous System Diseases; Rats; Rodentia
PubMed: 36012136
DOI: 10.3390/ijms23168859