esomeprazole, Nexium
Esomeprazole MUPS 40 mg tablets and esomeprazole MUPS 40 mg tablets encapsulated in hard gelatine are bioequivalent.

Talpes S, Knoerzer D, Huber R, Pfaffenberger B.

ALTANA Pharma AG, Konstanz, Germany.

OBJECTIVE: To investigate the bioequivalence of esomeprazole MUPS 40 mg tablets administered with and without a hard gelatine capsule. MATERIAL AND METHODS: Bioequivalence of the esomeprazole MUPS 40 mg tablet administered without (Reference) and with a hard gelatine capsule (Test) was evaluated using a randomized, two-period crossover study. In each study period 49 healthy male Caucasian subjects received a single oral dose of 40 mg esomeprazole. Blood samples were collected at specified time intervals, and serum was separated and analyzed for esomeprazole concentrations using a validated HPLC-MS method. The primary parameters were AUC (extent of absorption) and Cmax (rate of absorption). The time-to-peak plasma concentration, tmax, and the elimination half-life, t1/2, were determined as secondary characteristics. Point estimates and 90%-confidence intervals were obtained for the ratio of the population medians of Test and Reference, using a multiplicative model and a parametric analysis except in the case of tmax, where an additive model and a non-parametric analysis was used. Bioequivalence of Test and Reference was concluded if the 90%-confidence intervals were entirely within the predefined equivalence ranges. RESULTS: The AUC(0-infinity) and Cmax-ratios (Test/Reference) were 1.00 and 1.01, respectively. The 90%-confidence intervals for AUC(0-infinity) (0.94-1.06) and Cmax (0.93-1.09) of these ratios were within the predefined equivalence range of 0.80-1.25 and 0.75-1.33, respectively. The ratios and 90%-confidence intervals of the secondary characteristics t1/2 and tmax were also within the respective predefined equivalence ranges. Both esomeprazole formulations were well tolerated and safe. CONCLUSION: The encapsulation of esomeprazole MUPS 40 mg tablets does not influence the extent and rate of absorption assessed by using AUC(0-infinity) and Cmax. Thus, bioequivalence could be demonstrated.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15704615&dopt=Abstract esomeprozole Nexium



esomeprazole, Nexium
Efficacy of esomeprazole 40 mg vs. lansoprazole 30 mg for healing moderate to severe erosive oesophagitis.

Fennerty MB, Johanson JF, Hwang C, Sostek M.

Oregon Health & Science University, Portland, OR 97239-3098, USA. fannerty ohsu.edu

BACKGROUND: Secondary analyses from previous studies indicated that esomeprazole was more effective than lansoprazole and omeprazole in healing moderate or severe (Los Angeles grades C or D) erosive oesophagitis (EE). AIM: To compare prospectively healing rates with esomeprazole vs. lansoprazole in patients with moderate to severe EE. METHODS: In this multicentre, randomized, double-blind, parallel-group trial, adult patients with endoscopically confirmed moderate or severe EE received esomeprazole 40 mg (n = 498) or lansoprazole 30 mg (n = 501) once daily for up to 8 weeks. The primary end point was EE healing through week 8. Secondary assessments included investigator-assessed resolution of symptoms and safety and tolerability. RESULTS: Time to healing was significantly different (P = 0.007), favouring esomeprazole. Estimated healing rates at week 8 were 82.4% with esomeprazole 40 mg and 77.5% with lansoprazole 30 mg. Heartburn resolved at week 4 in 72% and 64% of patients who received esomeprazole and lansoprazole, respectively (P = 0.005). Control of other GERD symptoms was similar between treatments. Both treatments were well tolerated. CONCLUSIONS: With 8 weeks' treatment, esomeprazole 40 mg once daily heals moderate to severe EE faster and in more patients, and resolves heartburn in more patients after 4 weeks of treatment, than lansoprazole 30 mg once daily.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15709997&dopt=Abstract esomeprozole Nexium



esomeprazole, Nexium
[Gastroesophageal reflux disease refractory to esomeprazole.]

[Article in Spanish]

Velasco M, Ortiz V, Ponce J.

Servicio de Medicina Digestiva. Hospital Universitari La Fe. Valencia. Espana.

Resistance to proton pump inhibitors (PPI) in gastroesophageal reflux disease (GERD), which has been described in patients treated with omeprazole, could explain some exceptional cases of treatment failure and the need for surgery. The objective test of resistance to PPI is obtained with 24-hour intragastric pH-metry performed during treatment. A gastric pH of less than 4 for more than 50% of recording time indicates resistance. We present a patient with non-erosive GERD and treatment failure to omeprazole and proven resistance to esomeprazole which, to our knowledge, has only been reported in patients with Barrett's esophagus.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15710084&dopt=Abstract esomeprozole Nexium



esomeprazole, Nexium
Effects of esomeprazole magnesium on nonsteroidal anti-inflammatory drug gastropathy.

Koch TR, Petro A, Darrabie M, Opara EC.

Division of Gastroenterology & Hepatology, Medical College of Wisconsin, Milwaukee, Wisconsin 53295, USA. TimKoch worldnet.att.net

It has been proposed that tissue damage induced by nonsteroidal anti-inflammatory drugs is related to increased tissue free radical production with antioxidant depletion. We have shown that esomeprazole increases gastric total antioxidant capacity in mice and, therefore, hypothesized that the protective effect of esomeprazole during treatment with a nonsteroidal anti-inflammatory drug is related to increased gastric antioxidant capacity and decreased tissue free radical production. A/J mice received one of four treatments by daily gavage: saline in vehicle (control), indomethacin, esomeprazole, or indomethacin and esomeprazole. After 10 days, all mice were sacrificed and validated assays were used to measure gastric total antioxidant capacity, lipid peroxide levels, and myeloperoxidase activity. Indomethacin-treated mice developed weight loss and melena. No mice receiving indomethacin and esomeprazole died, but the death rate while receiving indomethacin was 38% (chi2, P = 0.05). Gastric lipid peroxide levels increased in mice receiving indomethacin treatment compared to treatment with esomeprazole and indomethacin (P = 0.03). There was a strong trend (P = 0.08) toward increased gastric total antioxidant capacity in mice receiving esomeprazole and indomethacin compared to mice receiving indomethacin. Gastric myeloperoxidase activities were not different among the four groups. Esomeprazole significantly improved survival in mice that received indomethacin, reduced free radical production, as estimated by lipid peroxide levels, and appeared to increase gastric total antioxidant capacity. The mechanisms for the beneficial effects of esomeprazole in the treatment of gastropathy are more complex than previously thought.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15712643&dopt=Abstract esomeprozole Nexium



esomeprazole, Nexium
A comparative study of the early effects of tenatoprazole 40 mg and esomeprazole 40 mg on intragastric pH in healthy volunteers.

Galmiche JP, Sacher-Huvelin S, Bruley des Varannes S, Vavasseur F, Taccoen A, Fiorentini P, Homerin M.

CIC-INSERM-CHU de Nantes, France.

Summary Background : Tenatoprazole is a novel proton pump inhibitor with a seven-hour plasma half-life. Aim : To compare the effects of tenatoprazole 40 mg and esomeprazole 40 mg on intragastric acidity during the first 48 h in healthy volunteers. Methods : This randomized two-period crossover study included 24 Helicobacter Pylori-negative subjects; tenatoprazole 40 mg or esomeprazole 40 mg daily were given before breakfast for two consecutive days, with a 2-week wash-out between the administration periods. Intragastric pH was monitored for 48 h. Results : Over 48 h, tenatoprazole 40 mg exerted a more potent acid inhibition than esomeprazole 40 mg (median pH: 4.3 vs. 3.9, P < 0.08; per cent of time above pH 4: 57% vs. 49%, P < 0.03; proportion of subjects with at least half of the time above pH 4: 71% vs. 46%). These differences resulted from better night-time acid control with tenatoprazole 40 mg than esomeprazole 40 mg (first night median pH: 4.2 vs. 2.9, P < 0.0001; second night: 4.5 vs. 3.2, P < 0.0001). The duration of nocturnal acid breakthroughs was significantly reduced during both nights. In contrast, no significant difference was detected during the daytime periods between both regimens. Conclusion : Over the first 48 h, tenatoprazole 40 mg achieves a better overall and night-time control of gastric pH than esomeprazole 40 mg. The translation of better early control of acidity into clinical benefits deserves further studies.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15740541&dopt=Abstract esomeprozole Nexium