OBJECTIVETo investigate the antimicrobial activity of Pariet, Tekpron, Nexium, respectively, against Helicobacter pylori (H. pylori) in vitro.

METHODSAntimicrobial effects of these medicines were evaluated through detection of MICs for 3 H. pylori strains isolated from different countries.

RESULTSThe 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.

CONCLUSIONSThe 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.

2-Pyridinylmethylsulfinylbenzimidazoles ; Benzimidazoles ; pharmacology ; Enzyme Inhibitors ; pharmacology ; Esomeprazole ; analogs & derivatives ; pharmacology ; Helicobacter pylori ; drug effects ; Lansoprazole ; Microbial Sensitivity Tests ; Proton Pump Inhibitors ; Rabeprazole

This work aimed to set up a high performance liquid chromatography (HPLC) method to determine the concentration of lansoprazole in human plasma and study the pharmacokinetic characters of lansoprazole in Chinese healthy volunteers after intravenous (IV) infusion. In accordance with double 3 x 3 Latin square design with self-crossover design, 12 volunteers were randomly divided into six groups, with half males and half females. The volunteers were administered with single dose of 15, 30, 60 mg of lansoprazole by IV infusion at a constant speed respectively, to study the clinical pharmacokinetics of lansoprazole. The linear range of lansoprazole in human plasma was 0.020-4.970 microg/ml (r = 0.9999); The intra-day and inter-day RSD were less than 10%. After receiving single doses of 15, 30 and 60 mg of lansoprazole, t(1/2) were (1.663 +/- 0.405) h, (1.541 +/- 0.339)h and (1.747 +/- 0.156) h; Cmax were (1.065 +/- 0.094) microg/ml, (2.104 +/- 0.312) microg/ml and (3.786 +/- 0.356) microg/ml; AUC(0-infinity) were (2.376 +/- 0. 432) microg x h/ ml, (4.722 +/- 0.753) microg x h/ml and (10.495 +/- 2.129) microg x h/ml respectively. The improved HPLC method is simple, rapid and reproducible. It could be used for determination of the concentration of lansoprazole in human plasma. The pharmacokinetics of lansoprazole for injection was found to fit the linear dynamics in vivo within the dose range of 15 to 60 mg. In addition, the results suggested that gender had no statistic significant effect on the pharmacokinetic process of lansoprazole after IV infusion of single dose.
2-Pyridinylmethylsulfinylbenzimidazoles ; administration & dosage ; blood ; pharmacokinetics ; Chromatography, High Pressure Liquid ; methods ; Female ; Humans ; Infusions, Intravenous ; Lansoprazole ; Male ; Proton Pump Inhibitors

BACKGROUND/AIMS: The aim of this study was to evaluate the efficacy and cost efficiency of omeprazole 10 mg and rabeprazole 10 mg once daily for 24 weeks in the maintenance therapy. METHODS: This was a randomized, open-label study enrolling 279 patients with erosive esophagitis A or B (Los Angeles classification) and typical gastroesophageal reflux disease symptoms. Patients who showed complete endoscopic and symptomatic healing after 8 weeks of proton pump inhibitor treatment were randomly allocated to maintenance treatment with omeprazole 10 mg once daily or rabeprazole 10 mg once daily for 42 weeks. The primary efficacy endpoint was the proportion of patients with symptomatic remission at 42 weeks. RESULTS: At the end of 42 weeks of maintenance therapy, 96.4% of omeprazole and 95.1% of rabeprazole treated patients remained symptom free (P > 0.05). Two drugs were also comparable with regard to the severity and frequency of reflux symptoms during the maintenance phase (P > 0.05). By the cost-minimization analysis, the mean total costs per patient for remaining symptom-free for 6 months were 241,775 won for omeprazole and 287,115 won for rabeprazole, respectively. CONCLUSIONS: Omeprazole 10 mg appeared to have similar efficacy in maintaining symptomatic remission as rabeprazole 10 mg, but was superior to rabeprazole 10 mg in terms of cost efficiency in the maintenance therapy of gastroesophageal reflux disease symptoms.
2-Pyridinylmethylsulfinylbenzimidazoles ; Cost-Benefit Analysis ; Esophagitis ; Gastroesophageal Reflux ; Humans ; Omeprazole ; Proton Pumps

Proton pump inhibitor (PPI) is a prodrug which is activated by acid. Activated PPI binds covalently to the gastric H+, K+-ATPase via disulfide bond. Cys813 is the primary site responsible for the inhibition of acid pump enzyme, where PPIs bind. Omeprazole was the first PPI introduced in market, followed by pantoprazole, lansoprazole and rabeprazole. Though these PPIs share the core structures benzimidazole and pyridine, their pharmacokinetics and pharmacodynamics are a little different. Several factors must be considered in understanding the pharmacodynamics of PPIs, including: accumulation of PPI in the parietal cell, the proportion of the pump enzyme located at the canaliculus, de novo synthesis of new pump enzyme, metabolism of PPI, amounts of covalent binding of PPI in the parietal cell, and the stability of PPI binding. PPIs have about 1hour of elimination half-life. Area under the plasmic concentration curve and the intragastric pH profile are very good indicators for evaluating PPI efficacy. Though CYP2C19 and CYP3A4 polymorphism are major components of PPI metabolism, the pharmacokinetics and pharmacodynamics of racemic mixture of PPIs depend on the CYP2C19 genotype status. S-omeprazole is relatively insensitive to CYP2C19, so better control of the intragastric pH is achieved. Similarly, R-lansoprazole was developed in order to increase the drug activity. Delayed-release formulation resulted in a longer duration of effective concentration of R-lansoprazole in blood, in addition to metabolic advantage. Thus, dexlansoprazole showed best control of the intragastric pH among the present PPIs. Overall, PPIs made significant progress in the management of acid-related diseases and improved health-related quality of life.
2-Pyridinylmethylsulfinylbenzimidazoles ; Benzimidazoles ; Gastric Acid ; Genotype ; Half-Life ; Hydrogen-Ion Concentration ; Imidazoles ; Nitro Compounds ; Omeprazole ; Proton Pump Inhibitors ; Proton Pumps ; Protons ; Pyridines ; Quality of Life

BACKGROUND/AIMS: Reflux esophagitis is a recurring condition for which many patients require maintenance therapy. This comparative, randomized multicenter study was designed to evaluate the effect of long-term maintenance treatment comparing proton pump inhibitor, rabeprazole and H2 receptor antagonist, ranitidine. METHODS: Eighty four patients with healed reflux esophagitis confirmed by endoscopy were randomly allocated to receive maintenance treatment with either rabeprazole 10 mg once daily or ranitidine 300 mg once daily for 32 weeks. Patients were seen every 8 weeks or at symptomatic relapse. RESULTS: Of 84 initially treated patients, 73 entered the maintenance study. The percentage of asymptomatic patients after 90-day and 210-day treatment were 97% and 81.5%, for rabeprazole and 74.3% and 62.3%, for ranitidine, respectively. After 32 weeks, the relapse rates of esophagitis were 21.3% in the rabeprazole group and 62.9% in the ranitidine group (RR: 0.405, 95% CI: 0.215-0.766). CONCLUSIONS: Maintenance treatment with rabeprazole (10 mg once daily) is superior to ranitidine (300 mg once daily) in keeping the patients with reflux esophagitis in remission over a 32 week period.
2-Pyridinylmethylsulfinylbenzimidazoles ; Adult ; Anti-Ulcer Agents/*therapeutic use ; Benzimidazoles/*therapeutic use ; Esophagitis, Peptic/*drug therapy ; Female ; Humans ; Male ; Middle Aged ; Omeprazole/*analogs & derivatives/therapeutic use ; Ranitidine/*therapeutic use

BACKGROUND/AIMS: Although intravenous proton pump inhibitor (PPI) has been used for the prevention of post endoscopic submucosal dissection (ESD) bleeding, the route of administration has not been confirmed. The aim of the present study was to compare the efficacy of intravenous and oral PPI administration for the prevention of delayed post ESD bleeding. METHODS: Total 166 consecutive patients were randomly assigned to 30 mg lansoprazol twice a day (PO group) and 120 mg pantoprazole intravenous injection (IV group) for 48 hours. Finally, 65 patients in PO group and 87 patients in IV group were analyzed. After ESD, all patients underwent follow up endoscopy after 24 hours and were observed the symptoms of bleeding up to 60 days after ESD. RESULTS: Age, sex and use of anticoagulants were not different between groups. At follow up endoscopy after 24 hours, oozing and exposed vessel was noted in 4.6% of PO group and 8.0% of IV group and there was no significant difference. Delayed bleeding occurred in 4 of 65 patients (6.2%) in the PO group and 8 of 87 patients (9.2%) in the IV group (p>0.999). By multivariate analysis, oozing or exposed vessels at follow up endoscopy were risk factors for delayed bleeding (OR=17.5, p=0.022). CONCLUSIONS: There was no significant difference in the delayed bleeding, length of hospital stay according to the administration route. Bleeding stigmata at follow up endoscopy was risk factor of delayed bleeding. Oral PPI administration can cost-effectively replace IV PPI for prevention of post ESD bleeding.
2-Pyridinylmethylsulfinylbenzimidazoles/therapeutic use ; *Administration, Oral ; Aged ; Anticoagulants/therapeutic use ; Endoscopic Mucosal Resection/*adverse effects ; Female ; Gastroscopy ; Humans ; *Injections, Intravenous ; Lansoprazole/therapeutic use ; Male ; Middle Aged ; Odds Ratio ; Postoperative Hemorrhage/etiology/*prevention & control ; Prospective Studies ; Proton Pump Inhibitors/*therapeutic use ; Risk Factors ; Stomach Neoplasms/surgery

Anaphylaxis to proton pump inhibitors (PPIs) has rarely been reported. Different patterns of cross-reactivity between PPIs have also been demonstrated using skin tests. Here, we report a case of anaphylaxis to lansoprazole with tolerance to other commercially available PPIs, which was proved by skin tests and oral provocation tests (OPTs). A 47-year-old female patient visited our Emergency Department with a sudden onset of whole body urticaria, facial swelling, dyspnea, and loss of consciousness that developed 1 hour after ingestion of 30 mg of lansoprazole for her episodic epigastric soreness. The skin prick test (SPT) and the intradermal test (IDT) with lansoprazole, esomeprazole, rabeprazole, and pantoprazole were performed. Lansoprazole showed positive reactions in both the SPT (3 mg/mL) and the IDT (0.003 mg/mL). Rabeprazole (3 mg/mL) showed a positive reaction only in IDT. The SPT and the IDT with esomeprazole and pantoprazole were all negative. The OPT with 30 mg of lansoprazole was positive (showing generalized rash and facial swelling 30 minuites after ingestion), while OPTs with esomeprazole, pantoprazole, and rabeprazole were all negative. Other PPIs could be safe alternatives in cases of anaphylaxis to 1 PPI. Skin tests seem to be helpful to define cross-reactivity between PPIs.
Anaphylaxis* ; Dyspnea ; Eating ; Emergency Service, Hospital ; Esomeprazole ; Exanthema ; Female ; Humans ; Intradermal Tests ; Lansoprazole* ; Middle Aged ; Proton Pump Inhibitors* ; Rabeprazole ; Skin ; Skin Tests ; Unconsciousness ; Urticaria

PURPOSE: Human factor is one of the major causes of medication errors. The purpose of this study was to identify nurses' perception and experience of medication errors, examine the relationship of Dominance, Influence, Steadiness, Conscientiousness (DISC) behavior patterns and medication errors by nurses. METHODS: A descriptive survey design with a convenience sampling was used. Data collection was done using self-report questionnaires answered by 308 nurses from one university hospital and two general hospitals. RESULTS: The most frequent DISC behavioral style of nurses was influence style (41.9%), followed by steadiness style (23.7%), conscientiousness style (20.4%), and dominance style (14.0%). Differences in the perception and experience level of medication errors by nurses' behavioral pattern were not statistically significant. However, nurses with conscientiousness style had the lowest scores for in experience of medication errors and the highest scores for perception of medication errors. CONCLUSION: The results of this study show that identification of the behavior pattern of nurses and application of this education program can prevent medication errors by nurses in hospitals.
2-Pyridinylmethylsulfinylbenzimidazoles ; Dacarbazine ; Data Collection ; Fibrinogen ; Humans ; Medication Errors ; Surveys and Questionnaires

BACKGROUND/AIMS: Ecabet sodium is known for its bactericidal effect against H. pylori. It was reported that a supplement of ecabet sodium to conventional triple therapy showed good results in Asia. The Aim of this study was to ascertain the efficacy of additional ecabet sodium on conventional triple therapy for eradication of H. pylori. METHODS: We reviewed the cases of 111 patients (Group A) with H. pylori infection who received ecabet sodium with triple therapy (20 mg of rabeprazole, 1 g of amoxicillin, 500 mg of clarithromycin and 1 g of ecabet sodium, twice daily for 7 days). Another 186 patients (Group B) received PPI-based triple therapy (same as the above, except without the ecabet sodium). Eradication was evaluated 4 weeks later after completion of treatment by 13C-UBT. RESULTS: Eradication rates were 74.8% (83/111) in group A and 70.4% (131/186) in group B by intention-to-treat analysis (p=0.420), and 75.2% (82/109) in group A and 70.7% (128/181) in group B by per protocol analysis (p=0.405). CONCLUSIONS: The addition of ecabet sodium to conventional triple therapy did not increase the eradication rate of H. pylori in this study. These findings imply that ecabet sodium as an additional agent cannot overcome antibiotic resistance, which is the most important cause of failure of triple therapy.
2-Pyridinylmethylsulfinylbenzimidazoles ; Amoxicillin ; Asia ; Clarithromycin ; Diterpenes, Abietane ; Drug Resistance, Microbial ; Helicobacter ; Helicobacter pylori ; Humans ; Korea ; Sodium

BACKGROUND/AIMS: This study assessed the efficacy of a rifaximin plus levofloxacin-based rescue regimen in patients that had failed both triple and quadruple standard regimens for the eradication of Helicobacter pylori. METHODS: We treated patients for H. pylori between August 2009 and April 2011. The triple regimen consisted of combined treatment with amoxicillin, clarithromycin, and pantoprazole for 1 week. For failed cases, a quadruple regimen of tetracycline, metronidazole, bismuth dicitrate, and lansoprazole for 1 week was administered. The rescue regimen for persistently refractory cases was rifaximin 200 mg t.i.d., levofloxacin 500 mg q.d., and lansoprazole 15 mg b.i.d. for 1 week. RESULTS: In total, 482 patients were enrolled in this study. The eradication rates associated with the first and second regimens were 58% and 60%, respectively. Forty-seven out of 58 patients who failed with the second-line regimen received rifaximin plus levofloxacin-based third-line therapy. The eradication rate for the third regimen was 65%. The cumulative eradication rates were 58%, 85%, and 96% for each regimen, respectively. CONCLUSIONS: A rifaximin plus levofloxacin-based regimen could be an alternative rescue therapy in patients with resistance to both triple and quadruple regimens for the eradication of H. pylori.
2-Pyridinylmethylsulfinylbenzimidazoles ; Amoxicillin ; Bismuth ; Clarithromycin ; Helicobacter ; Helicobacter pylori ; Humans ; Metronidazole ; Ofloxacin ; Rifamycins ; Tetracycline