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Alimentary Pharmacology & Therapeutics Apr 1998Omeprazole 20 mg once daily (o.d.) and lansoprazole 30 mg o.d. have similar acid-inhibitory effects in healthy Helicobacter pylori-positive subjects. However, little is... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
BACKGROUND
Omeprazole 20 mg once daily (o.d.) and lansoprazole 30 mg o.d. have similar acid-inhibitory effects in healthy Helicobacter pylori-positive subjects. However, little is known about the acid-inhibitory effects of the o.d. and twice daily (b.d.) doses in H. pylori-negative subjects.
AIM
To compare the decrease in gastric acidity of omeprazole 20 mg (o.d. and b.d.) with lansoprazole 30 mg (o.d. and b.d.) in healthy H. pylori-negative subjects on day 6-7 of dosing.
METHODS
A randomized, investigator-blind, crossover study design was used. Intragastric pH was measured continuously with glass electrodes positioned in the gastric corpus. Sixteen H. pylori-negative subjects, whose intragastric acidity fell below pH 4 for 70% of a 24-h baseline period. were entered in the study.
RESULTS
Both dosing regimens of omeprazole and lansoprazole significantly increased median gastric pH and percentages of time above pH 4 during the entire 24-h period, night- and daytime, compared to baseline. There were no significant differences in median gastric pH values or time above pH thresholds 3, 4 and 5 between the o.d. dosing regimens. During the night the percentage of time spent above pH 3 and 4 was significantly higher with omeprazole 20 mg b.d. than with lansoprazole 30 mg b.d.
CONCLUSIONS
This comparative study demonstrates that daily doses of omeprazole 20 mg and lansoprazole 30 mg are equally effective in raising intragastric pH in H. pylori-negative subjects on day 6 of dosing. During the night, omeprazole 20 mg b.d. provides superior gastric acid suppression compared to lansoprazole 30 mg b.d.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Administration, Oral; Adult; Anti-Ulcer Agents; Cross-Over Studies; Double-Blind Method; Gastric Acid; Helicobacter pylori; Humans; Lansoprazole; Omeprazole
PubMed: 9690721
DOI: 10.1046/j.1365-2036.1998.00304.x -
Drug Design, Development and Therapy 2021Bioequivalence tests are fundamental step in assessing the equivalence in bioavailability between a test and reference product. In practice, two separate linear mixed... (Comparative Study)
Comparative Study
BACKGROUND AND OBJECTIVE
Bioequivalence tests are fundamental step in assessing the equivalence in bioavailability between a test and reference product. In practice, two separate linear mixed models (LMMs) with random subject effects, which have an area under the concentration-time curve (AUC) and the peak concentration (C) as the responses, have become the gold standard for evaluating bioequivalence. Recently, Lee et al developed a multivariate hierarchical generalized linear model (HGLM) for several responses that modeled correlations among multivariate responses via correlated random effects. The objective of this study was to apply this multivariate analysis to the bioequivalence test in practice and to compare the performance of multivariate HGLM and separate LMMs.
METHODS
Three pharmacokinetic datasets, fixed-dose combination (naproxen and esomeprazole), tramadol and fimasartan data were analyzed. We compared the 90% confidence interval (CI) for the geometric mean ratio (GMR) of a test product to a reference product using the multivariate HGLM and two conventional separate LMMs.
RESULTS
We found that the 90% CIs for the GMRs of both AUC and C from the multivariate HGLM were narrower than those from the separate LMMs: (0.843, 1.152) vs (0.825, 1.177) for C of esomeprazole in fixed-dose combination data; (0.805, 0.931) vs (0.797, 0.941) for C in tramadol data; (0.801, 1.501) vs (0.762, 1.578) for C and (1.163, 1.332) vs (1.009, 1.341) for AUC in fimasartan data, consistent with the random subject effects from two separate LMMs being highly correlated in the three datasets (correlation coefficient r = 0.883; r = 0.966; r = 0.832).
CONCLUSION
This multivariate HGLM had good performance in the bioequivalence test with multiple endpoints. This method would provide a more reasonable option to reduce the 90% CI by adding correlation parameters and thus an advantage especially in evaluating the bioequivalence of highly variable drugs with broad 90% CIs.
Topics: Area Under Curve; Biological Availability; Biphenyl Compounds; Datasets as Topic; Drug Combinations; Esomeprazole; Humans; Linear Models; Male; Models, Statistical; Multivariate Analysis; Naproxen; Pyrimidines; Randomized Controlled Trials as Topic; Tetrazoles; Therapeutic Equivalency; Tramadol
PubMed: 34465979
DOI: 10.2147/DDDT.S318576 -
Gut Jan 1988Single intravenous doses of 10, 20, 40, and 80 mg and repeated once daily intravenous doses of 10 and 20 mg omeprazole induced a powerful and long lasting inhibition of...
Single intravenous doses of 10, 20, 40, and 80 mg and repeated once daily intravenous doses of 10 and 20 mg omeprazole induced a powerful and long lasting inhibition of pentagastrin stimulated gastric acid secretion (PAO) in healthy male volunteers. Single intravenous doses of 10, 20, 40, and 80 mg omeprazole inhibited PAO by 30% (p less than 0.01), 45% (p less than 0.01), 61% (p less than 0.01), and 80% (p less than 0.01), respectively when measured 1.5 h after dose, and by 20% (NS), 27% (NS), 36% (p less than 0.01) and 59% (p less than 0.01), respectively when measured 24 h after dose. Six days after repeated once daily intravenous doses of 10 and 20 mg omeprazole, PAO was inhibited by 63% (p less than 0.01) and 82% (p less than 0.01), respectively when measured 1.5 h after dose, and by 32% (p less than 0.01) and 43% (p less than 0.01), respectively when measured 24 h after dose. The inhibition of PAO by 10 mg administered intravenously as a single bolus injection was comparable with the inhibition by 20 mg as a single oral dose. Repeated once daily administration of 10 mg intravenously and 20 mg orally also resulted in comparable reductions in PAO. The reduction in PAO after repeated once daily oral administration of 20 mg was comparable with the effect of a single intravenous dose of 40 mg. Terminal half lives were short, but significantly (p less than 0.05) prolonged after a single intravenous injection of 80 mg. Repeated once daily intravenous administration of 10 and 20 mg did not result in prolongation of terminal half lives. It is concluded that intravenous administration of omeprazole causes a potent and long acting inhibition of pentagastrin stimulated gastric acid secretion in man. Its potency is augmented after repeated once daily administration.
Topics: Adult; Gastric Acid; Half-Life; Humans; Injections, Intravenous; Male; Omeprazole; Pentagastrin; Time Factors
PubMed: 3343017
DOI: 10.1136/gut.29.1.75 -
Alimentary Pharmacology & Therapeutics Oct 2015
Topics: Esomeprazole; Humans; Male; Proton Pump Inhibitors; Pyrroles; Rabeprazole; Sulfonamides
PubMed: 26374257
DOI: 10.1111/apt.13384 -
Molecules (Basel, Switzerland) Apr 2022Objective: The present study aimed to develop and optimize esomeprazole loaded proniosomes (EZL-PNs) to improve bioavailability and therapeutic efficacy. Method: EZL-PNs...
Objective: The present study aimed to develop and optimize esomeprazole loaded proniosomes (EZL-PNs) to improve bioavailability and therapeutic efficacy. Method: EZL-PNs formulation was developed by slurry method and optimized by 33 box-Bhekhen statistical design software. Span 60 (surfactant), cholesterol, EZL concentration were taken as independent variables and their effects were evaluated on vesicle size (nm), entrapment efficiency (%, EE) and drug release (%, DR). Furthermore, optimized EZL-PNs (EZL-PNs-opt) formulation was evaluated for ex vivo permeation, pharmacokinetic and ulcer protection activity. Result: The EZL-PNs-opt formulation showed 616 ± 13.21 nm of vesicle size, and 81.21 ± 2.35% of EE. EZL-PNs-opt exhibited negative zeta potential and spherical confirmed scanning electron microscopy. EZL-PNs-opt showed sustained release of EZL (95.07 ± 2.10% in 12 h) than pure EZL dispersion. The ex-vivo gut permeation result exhibited a significantly (p < 0.05) enhanced flux than pure EZL. The in vivo results revealed 4.02-fold enhancement in bioavailability and 61.65% protection in ulcer than pure EZL dispersion (43.82%). Conclusion: Our findings revealed that EZL-PNs formulation could be an alternative delivery system of EZL to enhance oral bioavailability and antiulcer activity.
Topics: Administration, Cutaneous; Biological Availability; Drug Carriers; Drug Liberation; Esomeprazole; Humans; Particle Size; Ulcer
PubMed: 35566099
DOI: 10.3390/molecules27092748 -
Alimentary Pharmacology & Therapeutics Dec 2000Comparative studies of omeprazole and lansoprazole are scarce and even scarcer are comparisons of higher doses. Most of the comparative studies have assessed the effect... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
Omeprazole 40 mg once a day is equally effective as lansoprazole 30 mg twice a day in symptom control of patients with gastro-oesophageal reflux disease (GERD) who are resistant to conventional-dose lansoprazole therapy-a prospective, randomized, multi-centre study.
BACKGROUND
Comparative studies of omeprazole and lansoprazole are scarce and even scarcer are comparisons of higher doses. Most of the comparative studies have assessed the effect of the two proton pump inhibitors (PPIs) on gastric acid secretion or gastric pH. Few studies have compared clinical end-points such as oesophageal healing and symptom control.
AIM
To determine the clinical efficacy of omeprazole 40 mg daily as compared to lansoprazole 30 mg twice a day in symptom control of patients with severe symptomatic GERD.
METHODS
Ninety-six patients who failed a standard dose of lansoprazole (30 mg once daily), were enrolled in a prospective fashion from three VA medical centres and were randomized to receive 6 weeks of either omeprazole 40 mg daily or lansoprazole 30 mg twice daily. Patients reported daily on symptom severity and frequency, antacid consumption and side-effects.
RESULTS
Forty-six patients received omeprazole and 44 lansoprazole. Although not statistically significant, there was a consistent trend of better symptom control in the omeprazole group for daytime and night-time heartburn and acid regurgitation. There was no statistical difference between the two groups in mean antacid consumption overall and at the end of each of the 6 weeks of the study. In addition, there was no significant difference in the overall frequency of side-effects between the two groups nor for each individual side-effect.
CONCLUSION
Omeprazole 40 mg once daily is equally effective and tolerated as lansoprazole 30 mg twice daily in symptom control of patients with GERD.
Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Adult; Aged; Aged, 80 and over; Drug Administration Schedule; Enzyme Inhibitors; Female; Gastroesophageal Reflux; Humans; Lansoprazole; Male; Middle Aged; Omeprazole; Prospective Studies
PubMed: 11121907
DOI: 10.1046/j.1365-2036.2000.00882.x -
Anales de Pediatria (Barcelona, Spain :... Mar 2013Critical patients usually have hemodynamic disturbances which may become worse by the administration of some drugs. Omeprazole is a drug used in the prophylaxis of the... (Comparative Study)
Comparative Study Observational Study Randomized Controlled Trial
INTRODUCTION
Critical patients usually have hemodynamic disturbances which may become worse by the administration of some drugs. Omeprazole is a drug used in the prophylaxis of the gastrointestinal bleeding in these patients, but its cardiovascular effects are unknown. The objective was to study the hemodynamic changes produced by intravenous omeprazole in critically ill children and to find out if there are differences between two different doses of omeprazole.
MATERIAL AND METHODS
A randomized prospective observational study was performed on 37 critically ill children aged from 1 month to 14 years of age who required prophylaxis for gastrointestinal bleeding. Of these, 19 received intravenous omeprazole 0.5mg/kg every 12 hours, and 18 received intravenous omeprazole 1mg/kg every 12 hours. Intravenous omeprazole was administered in 20 minutes by continuous infusion pump. Heart rate, systolic, diastolic and mean arterial blood pressure, central venous pressure and ECG were recorded at baseline, and at 15, 30, 60 and 120 minutes of the infusion.
RESULTS
There were no significant changes in the electrocardiogram, heart rate, blood pressure and central venous pressure. No patients required inotropic therapy modification. There were no differences between the two doses of omeprazole.
CONCLUSIONS
Intravenous omeprazole administration of 0.5mg/kg and 1mg/kg is a hemodynamically safe drug in critically ill children.
Topics: Adolescent; Child; Child, Preschool; Critical Illness; Female; Hemodynamics; Humans; Infant; Infusions, Intravenous; Male; Omeprazole; Prospective Studies; Proton Pump Inhibitors
PubMed: 22818224
DOI: 10.1016/j.anpedi.2012.06.002 -
Journal of Veterinary Internal Medicine Mar 2019Although the demand for esomeprazole is increasing in veterinary medicine, the pharmacokinetics (PK) and pharmacodynamics of esomeprazole have been described in only a...
BACKGROUND
Although the demand for esomeprazole is increasing in veterinary medicine, the pharmacokinetics (PK) and pharmacodynamics of esomeprazole have been described in only a few studies.
OBJECTIVE
To determine the PK of 0.5 and 1 mg/kg esomeprazole administered IV q12h and to investigate its effects on intragastric pH in healthy dogs.
ANIMALS
Six adult Beagles.
METHODS
Open-label, randomized, and crossover design. The dogs received 0.5 or 1 mg/kg esomeprazole IV q12h for 48 hours. Plasma concentrations of esomeprazole were measured by high-performance liquid chromatography-tandem mass spectrometry. Intragastric pH was determined using the Bravo pH monitoring system and recorded as mean percentage time (MPT) for which pH was ≥3 and ≥4 for 24 hours in each group.
RESULTS
The peak plasma concentration and area under the curve from the time of dosing to the last measurable concentration in the 1 mg/kg group were higher than those in the 0.5 mg/kg group. However, when the dosage normalized, intergroup differences were not significant. The MPTs for which intragastric pH was ≥3 and ≥4 for 48 hours were 88% ± 7% and 81% ± 9% for the 0.5 mg/kg group and 90% ± 9% and 85% ± 11% for the 1 mg/kg group, respectively, with no significant intergroup differences.
CONCLUSIONS AND CLINICAL IMPORTANCE
The pharmacokinetic parameters and acid suppressant effect for 0.5 and 1 mg/kg esomeprazole were not significantly different. Furthermore, the efficacy of esomeprazole 0.5 mg/kg IV q12h was sufficient to increase intragastric pH in Beagles.
Topics: Animals; Anti-Ulcer Agents; Area Under Curve; Chromatography, High Pressure Liquid; Cross-Over Studies; Dogs; Dose-Response Relationship, Drug; Esomeprazole; Gastric Acid; Gastric Acidity Determination; Hydrogen-Ion Concentration; Injections, Intravenous; Random Allocation
PubMed: 30548689
DOI: 10.1111/jvim.15383 -
Alimentary Pharmacology & Therapeutics Feb 2003Gastric acid suppression is the most effective medical therapy to control acidic gastro-oesophageal reflux: individuals in whom therapy fails usually have inadequate... (Comparative Study)
Comparative Study Review
Gastric acid suppression is the most effective medical therapy to control acidic gastro-oesophageal reflux: individuals in whom therapy fails usually have inadequate acid suppression. Twenty-four-hour intragastric pH-metry measures the percentage of time that gastric pH is above 4 or 3, the critical thresholds for tissue damage and symptom generation in the distal oesophagus. Effective medical therapy must control gastric acidity throughout the daytime, including the postprandial period. It is therefore useful to report the percentage of patients in whom gastric acidity is controlled above pH 4 for at least 16 out of 24 h. Esomeprazole was compared with standard-dose proton pump inhibitors in healthy volunteers and patients with gastro-oesophageal reflux disease. Esomeprazole, 40 mg daily, was significantly more effective at controlling gastric acidity above pH 4 for more than 16 h than lansoprazole, 30 mg daily (38% of individuals vs. 5%, respectively). Esomeprazole, 40 mg daily, also suppressed gastric acidity more effectively and in more individuals than pantoprazole, 40 mg daily, and rabeprazole, 20 mg daily. Esomeprazole, 20 mg daily, was significantly more effective at controlling gastric acidity than lansoprazole, 15 mg daily. The improved acid control with esomeprazole compared with other proton pump inhibitors is likely to result in superior healing rates and improved symptom relief, with fewer therapy-resistant patients.
Topics: Anti-Ulcer Agents; Esomeprazole; Gastric Acid; Gastroesophageal Reflux; Humans; Hydrogen-Ion Concentration; Proton Pump Inhibitors
PubMed: 12614300
DOI: 10.1046/j.1365-2036.17.s1.3.x -
Tijdschrift Voor Psychiatrie 2018A 12-year-old girl with no psychiatric history developed psychotic symptoms, including formal thought disorder and delusional ideas after omeprazole was initiated. Given...
A 12-year-old girl with no psychiatric history developed psychotic symptoms, including formal thought disorder and delusional ideas after omeprazole was initiated. Given the co-occurrence of omeprazole initiation and the start of these symptoms, omeprazole was discontinued and replaced by ranitidine which led to immediate symptom reduction followed by complete remission. Although the proton pump inhibitor (ppi) omeprazole is considered safe and is commonly prescribed, it can cause rare major psychiatric side-effects. Despite conducting a literature search to uncover a possible causal mechanism to explain these side-effects, no conclusive explanatio was found.
Topics: Child; Female; Humans; Mental Disorders; Omeprazole; Proton Pump Inhibitors
PubMed: 30536296
DOI: No ID Found