Efficacy of esomeprazole in treating acid-related diseases in Japanese populations

Sugimoto, Mitsushige; Furuta, Takahisa

doi:10.2147/ceg.s23926

Cited by 24 publications

(17 citation statements)

References 71 publications

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“…As newer generations PPIs, esomeprazole suggested less influence by CYP2C19 genotype than other proton pump inhibitors, but the fraction through CYP2C19 metabolism was about 70% [21]. The PK studies showed that the AUC of esomeprazole in CYP2C19 PM phenotypes was 3-fold higher than in individuals with NM phenotypes [22]. In the current study, the proportion of PM phenotypes in HPAG was 23.08% and no patient in LPAG.…”

Section: Discussionmentioning

confidence: 60%

Effects of Plasma Albumin on the Pharmacokinetics of Esomeprazole in ICU Patients

Tian

Wang

et al. 2018

BioMed Research International

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Objectives To evaluate the effects of plasma albumin on pharmacokinetics of esomeprazole in ICU patients. Methods This study was performed in 32 consecutive intensive care unit (ICU) patients. They were divided into two groups according to the plasma albumin levels. Nineteen patients with low plasma albumin levels (<30 g/L; male/female, 12/7) were assigned to low plasma albumin group (LPAG). Thirteen patients with plasma albumin levels >30 g/L (male/female, 9/4) were assigned to high plasma albumin group (HPAG). All patients were received intravenous (IV) of 40 mg esomeprazole in 5 min. Blood samples were collected via basilic vein at different time points and concentrations of esomeprazole were determined by UPLC-MS/MS. Results MRT(0-∞), t1/2, V, CL, and Cmax between two groups were significantly difference (P<0.05). Compared with HPAG, MRT(0-∞), t1/2, and V of esomeprazole in LPAG were increased by 1.42-fold, 1.49-fold, and 1.24-fold, respectively; the maximum drug concentration of esomeprazole in LPAG was decreased to 82.5%. AUC(0-∞) of LPAG was 1.23 times than that of group B. CL in LPAG was 80% of HPAG. There was no statistical difference between the two groups of AUC(0-∞) and CL. Conclusions Some pharmacokinetic parameters of esomeprazole may be changed in ICU patients with low plasma albumin.

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Section: Discussionmentioning

confidence: 60%

Effects of Plasma Albumin on the Pharmacokinetics of Esomeprazole in ICU Patients

Tian

Wang

et al. 2018

BioMed Research International

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“…One important characteristic that could potentially affect patient outcome is CYP2C19 genotype. Although we did not determine the genotypes of the patients, as the CYP2C19 genotype reportedly does not change the pharmacokinetics of either vonoprazan or esomeprazole dramatically, the CYP2C19 genotype is unlikely to influence the present results. Some clinical characteristics, such as H. pylori infection, ulcer size >1200 mm 2 , and ulcer location, can prolong ulcer healing .…”

Section: Discussionmentioning

confidence: 81%

Effect of vonoprazan on the treatment of artificial gastric ulcers after endoscopic submucosal dissection: Prospective randomized controlled trial

Tsuchiya

Kato²,

Tanida³

et al. 2017

Digestive Endoscopy

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Background and Aim: Proton pump inhibitors are effective for the treatment of gastric ulcers after endoscopic submucosal dissection (ESD). However, the most excellent therapy is controversial. Vonoprazan, an active potassium-competitive acid blocker, has a strong gastric acid secretion inhibitory effect, but its efficacy for the treatment of post-ESD gastric ulcers is unclear. Herein, we aimed to determine the healing effect of vonoprazan on post-ESD gastric ulcers. Methods:We carried out a prospective randomized controlled trial examining 92 patients who had undergone ESD for the treatment of gastric neoplasms between April 2015 and June 2016 at Machida Municipal Hospital. Patients were treated with 20 mg/day vonoprazan (V group) or 20 mg/day esomeprazole (E group) for 8 weeks. We evaluated the 8-week cure rate for artificial ulcers and any complications after ESD.Results: A total of 80 patients (median age, 73.5 years; 71.3% male) were analyzed. Cure rate for the V group was significantly higher than that for the E group (94.9% [37/39] vs 78.0% [32/41], respectively; P = 0.049). In a multivariate analysis, only vonoprazan was correlated with ulcer healing (odds ratio = 6.33; 95% CI = 1.21-33.20; P = 0.029). Delayed bleeding was experienced only in the E group (7.3% [3/41]), but no significant difference compared with the V group was observed (P = 0.241). Conclusion:Vonoprazan was significantly superior to esomeprazole for the healing of post-ESD gastric ulcers and should be considered as a treatment of first choice.

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“…After the advent of omeprazole in 1989, PPIs have been recognized to be more effective clinically than histamine-2 receptor antagonists (H2RAs), 1 and a number of PPIs have been developed. 2 Esomeprazole, the S-isomer of omeprazole, also known as NEXIUM ® . Esomeprazole was developed to provide further improvement on efficacy for acid-related diseases with higher systemic bioavailability due to the less first-pass metabolism and lower plasma clearance.…”

Section: What Is K Nown and Objec Tivementioning

confidence: 99%

Population pharmacokinetic analysis of esomeprazole in Japanese subjects with various CYP2C19 phenotypes

et al. 2020

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What is known and objective Esomeprazole, the S‐isomer of omeprazole, is a proton pump inhibitor which has been approved by over 125 countries, also known as NEXIUM®. Esomeprazole was developed to provide further improvement on efficacy for acid‐related diseases with higher systemic bioavailability due to the less first‐pass metabolism and lower plasma clearance. Esomeprazole is primarily metabolized by CYP2C19. Approximately <1% of Caucasians and 5%‐10% of Asians have absent CYP2C19 enzyme activity. Although the influence of various CYP2C19 phenotypes on esomeprazole pharmacokinetics has been studied, this is the first report in the Japanese population where 27 low CYP2C19 metabolizers were included. Methods In this study, a population PK model describing the PK of esomeprazole was developed to understand the difference of CYP2C19 phenotypes on clearance in the Japanese population. The model quantitatively assessed the influence of CYP2C19 phenotype on esomeprazole PK in healthy Japanese male subjects after receiving repeated oral dosing. The inhibition mechanism of esomeprazole on CYP2C19 activity was also included in the model. Results and discussion CYP2C19 phenotype and dose were found as statistically significant covariates on esomeprazole clearance. The apparent clearance at 10‐mg dose was 17.32, 9.77 and 7.37 (L/h) for homozygous extensive metabolizer, heterozygous extensive metabolizer and poor metabolizer subjects, respectively. And the apparent clearance decreased as dose increased. What is new and conclusion The established population PK model well described the esomeprazole PK and model‐predicted esomeprazole PK was in good agreement with external clinical data, suggesting the robustness and applicability of the current model for predicting esomeprazole PK.

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Efficacy of esomeprazole in treating acid-related diseases in Japanese populations

Cited by 24 publications

References 71 publications

Effects of Plasma Albumin on the Pharmacokinetics of Esomeprazole in ICU Patients

Effects of Plasma Albumin on the Pharmacokinetics of Esomeprazole in ICU Patients

Effect of vonoprazan on the treatment of artificial gastric ulcers after endoscopic submucosal dissection: Prospective randomized controlled trial

Population pharmacokinetic analysis of esomeprazole in Japanese subjects with various CYP2C19 phenotypes

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