esomeprazole, Nexium
Cost-minimization analysis of treatment of gastroesophageal reflux disease. Implications of varying holding time on conclusions.

Kivioja A, Linnosmaa I, Vehvilainen A, Vohlonen I.

Department of Social Pharmacy, Center for Pharmaceutical Policy and Economics, University of Kuopio, P.O. Box 1627, FIN-70211, Kuopio, Finland. akseli.kivioja uku.fi

Gastroesophageal reflux disease (GERD), is a common disorder. The most effective medical treatment for GERD is a proton pump inhibitor (PPI). The aim of this study was to specify the most inexpensive PPI therapy for GERD, and to examine the implications of varying outcome measure, holding time, on the conclusions about the cost-effectiveness of the treatments. Proton pump inhibitors that have holding time of intragastric pH>4 for at least 11h in 24h period (esomeprazole, lansoprazole, omeprazole and rabeprazole), were included. In this cost-minimization analysis (CMA), data on holding times were gathered from scientific publications listed in MEDLINE, prices of proton pump inhibitors from the Finnish database of drug prices and the treatment dosages were taken from the official guide of drug therapies in Finland. A decision tree was applied and the probabilities utilized were acquired from three expert physicians. The cost-minimization analysis was performed in three settings. At first, drugs that had a holding time (pH>4) of 11h or more were included. Secondly, drugs that had a holding time of 12h or more were included, and thirdly, a holding time of 13h or more was required. In the first analysis, the least expensive PPI treatment was lansoprazole (average cost of 138.89 per patient). In the second analysis, least expensive treatment was rabeprazole (193.81 per patient), and in the third, rabeprazole again (193.81 per patient). Esomeprazole and omeprazole were not among two of the least expensive alternatives in any of the settings. Which proton pump therapy turns out to be the least expensive for GERD, depends on the length of the holding time desired. Varying the holding time of the drug had a profound effect on the conclusions about the cost-effectiveness of the alternative treatments.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=14757488&dopt=Abstract esomeprozole Nexium



esomeprazole, Nexium
Stability of esomeprazole capsule contents after in vitro suspension in common soft foods and beverages.

Johnson DA, Roach AC, Carlsson AS, Karlsson AA, Behr DE.

Division of Gastroenterology, Eastern Virginia School of Medicine, Norfolk, Virginia 23505, USA. dajevms aol.com

STUDY OBJECTIVE: To determine the in vitro stability of esomeprazole pellets from an opened capsule after suspension in various common soft foods and beverages. DESIGN: In vitro study. SETTING: Pharmaceutical company research laboratory. MEASUREMENTS AND MAIN RESULTS: Pellets from opened esomeprazole 20-mg capsules were suspended in 100 ml of tap water, milk (1.5% fat), orange juice, apple juice, yogurt, or cultured milk for 30 minutes, then added to 500 ml of hydrochloric acid to simulate gastric acid exposure. After a 2-hour incubation, the mixture was filtered through a sieve, and the collected pellets were dissolved in an alkaline solution. Esomeprazole concentrations were measured using reverse-phase liquid chromatography The stability of the esomeprazole pellets exceeded 98% in all beverages and soft foods except milk. CONCLUSION: Administration of the pellets from an opened esomeprazole capsule shortly after suspending them in tap water, yogurt, cultured milk, orange juice, or apple juice may be a practical alternative for patients who cannot swallow an intact capsule. Bioavailability studies comparing esomeprazole administered as an intact capsule to that of the pellets from an opened capsule suspended in these beverages or soft foods are recommended to confirm these findings.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12820815&dopt=Abstract esomeprozole Nexium



esomeprazole, Nexium
[In-vitro activity of rabeprazole, lansoprazole, and esomeprazole against Helicobacter pylori]

[Article in Chinese]

He LH, Yin Y, You YH, Yan XM, Zhang JZ.

Department of Diagnosis, Institute for Communicable Disease Control and Prevention, Chinese Center for Disease Control and Preventive, Beijing 102206, China.

OBJECTIVE: To investigate the antimicrobial activity of Pariet, Tekpron, Nexium, respectively, against Helicobacter pylori (H. pylori) in vitro. METHODS: Antimicrobial effects of these medicines were evaluated through detection of MICs for 3 H. pylori strains isolated from different countries. RESULTS: The MIC(99) contents were 2.25 mg/L, 42.5 mg/L and 360 mg/L, respectively, for the three medicines. The strains under testing exhibited the same susceptibility to each medicine. Nexium did not inhibit the bacteria under the concentration of 3.6 - 36 mg/L with more and bigger H. pylori colonies seen when compared with controls. CONCLUSIONS: The growth inhibitory activity appeared to be different among the three PPI medicines under investigation, with Rabeprazole the most potential agent of the three. Data suggested that the action of growth inhibition in vitro was resting on the characteristic of the given PPI as well as the supplements of the medicine.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12848906&dopt=Abstract esomeprozole Nexium



esomeprazole, Nexium
Facing chirality in the 21st century: Approaching the challenges in the pharmaceutical industry.

Federsel HJ.

Process R&D, AstraZeneca R&D, Sodertalje, Sweden. hans-jurgen.federsel astrazeneca.com

How is process R&D organized and operated in today's pharmaceutical industry at the dawn of the 21st century? A way to respond to the challenges with regard to reduced time to market is to build on early involvement and a front-loading approach. This means that activities are initiated during the lead optimization phase starting up to 2 years ahead of candidate drug nomination and a model built on this concept covering the stages through to commercial launch is advocated as the appropriate way forward. However, given the high attrition rate in a pharma R&D pipeline focused risk management needs to be applied and options judiciously evaluated. From a molecular perspective, the chemical targets in many instances present a formidable complexity both with regard to the overall structure but increasingly also when it comes to their stereochemical features. Thus, a novel triazolo pyrimidine compound with six stereogenic centers requiring 28 transformations for its assembly is examined to underscore this, but also the difficulties in designing a feasible route for the relatively simple (S)-azetidinecarboxylic acid are highlighted. Furthermore, the successful development of a unique and highly efficient catalytic asymmetric sulfide oxidation to the corresponding (S)-sulfoxide esomeprazole is discussed, together with the remarkable effect that normal sea sand has on the stereoselectivity of a steroid trans-acetalization. Copyright 2003 Wiley-Liss, Inc.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12884384&dopt=Abstract esomeprozole Nexium



esomeprazole, Nexium
Quality of life in relation to symptoms in patients with gastro-oesophageal reflux disease-- an analysis based on the ProGERD initiative.

Kulig M, Leodolter A, Vieth M, Schulte E, Jaspersen D, Labenz J, Lind T, Meyer-Sabellek W, Malfertheiner P, Stolte M, Willich SN.

Institute of Social Medicine, Epidemiology, and Health Economics, Charite University Medical Center, Berlin, Germany. michael.kulig charite.de

AIMS: To determine the impact of gastro-oesophageal reflux disease (GERD) on the quality of life, to assess changes in the quality of life during treatment with esomeprazole and to define factors that can predict these changes. METHODS: Patients with GERD (n=6215) were included in a prospective cohort study (ProGERD). All patients underwent endoscopy and received esomeprazole. At baseline and after 2 weeks of treatment, symptoms and quality of life were assessed. Factors that influenced changes in the quality of life were determined by multiple regression analyses. RESULTS: At baseline, the quality of life in GERD patients was lower than that in the general population, and was similar to that in patients after acute coronary events. No differences in symptoms or quality of life were observed between the subgroups of patients with non-erosive GERD, erosive GERD and Barrett's oesophagus. After treatment with esomeprazole, the symptoms and quality of life were improved in all subscales within 2 weeks (P<0.001). The mean score of the disease-specific quality of life instrument (Quality of Life in Reflux and Dyspepsia Patients) increased from 4.6 to 6.2 points, representing a highly relevant clinical improvement. The generic quality of life (SF-36) reached levels similar to those in the general population, but, again, no difference was found between the three different subgroups of GERD patients. The main factors associated with an improvement in the quality of life after treatment were symptom relief, severe erosive reflux disease, absence of extra-oesophageal disorders, avoidance of non-steroidal anti-inflammatory drug intake and positive Helicobacter pylori status. CONCLUSIONS: GERD causes a significant impairment in the quality of life that can be attenuated or normalized within a time period as short as 2 weeks by treatment with esomeprazole. These findings were similar across the whole GERD patient spectrum.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=14535869&dopt=Abstract esomeprozole Nexium