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

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

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: 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

BACKGROUND/AIMS: The aim of this study was to evaluate the eradication rate of a triple therapy regimen that included a proton pump inhibitor, amoxicillin, and tetracycline instead of clarithromycin in treatment-Naive patients and in patients who did not respond to standard triple therapy. METHODS: This study included 110 patients infected with Helicobacter pylori. Patients in groups A and B were treatment-Naive, and those in group C were not responsive to previous standard triple therapy. Patients in group A (n=40) received lansoprazole 30 mg b.i.d., amoxicillin 1,000 mg b.i.d., and clarithromycin 500 mg b.i.d. for 14 days. Patients in groups B (n=40) and C (n=30) received lansoprazole 30 mg b.i.d., amoxicillin 1,000 mg b.i.d., and tetracycline 500 mg q.i.d. for 14 days. RESULTS: In group A, eradication was achieved in 18 (45%) of the 40 patients included in the intention-to-treat (ITT) analysis and in 18 (47.4%) of the 38 patients included in the per-protocol (PP) analysis. In group B, eradication was achieved in 15 (37.5%) of the 40 patients included in the ITT analysis and in 15 (39.3%) of the 38 patients included in the PP analysis. In group C, eradication was achieved in 14 (46.6%) of the 30 patients included in the ITT analysis and in 14 (43.8%) of the 29 patients included in the PP analysis. There was no statistically significant difference among the 3 groups with regard to eradication rates (p>0.05). CONCLUSIONS: Despite the low rate of resistance to tetracycline, the combination of lansoprazole, amoxicillin, and tetracycline instead of clarithromycin is not a good option for the eradication of H. pylori.
2-Pyridinylmethylsulfinylbenzimidazoles ; Amoxicillin ; Clarithromycin ; Helicobacter ; Helicobacter pylori ; Humans ; Pilot Projects ; Proton Pumps ; Tetracycline

BACKGROUND/AIMS: Endoscopic mucosal resection (EMR) currently serves as the minimally invasive treatment of choice for early gastric cancer and premalignant lesions of the stomach. There have been few studies addressing whether a proton pump inhibitor or a histamine 2-receptor antagonist is the most effective treatment for iatrogenic ulcers after EMR. We compared the effectiveness of pantoprazole and famotidine in treating iatrogenic ulcers and preventing bleeding after EMR without endoscopic submucosal dissection. METHODS: Between March 2006 and April 2007, we retrospectively analyzed the effect of famotidine (40 mg/day) and pantoprazole (40 mg/day) on the healing of iatrogenic ulcers and control of bleeding after EMR. RESULTS: During the study period, 126 patients underwent EMR. Eighty-one received famotidine, and 45 received pantoprazole. The mean duration of drug therapy was 44 days in each group. The stages of ulcers at 1 to 3 months after EMR were mostly scar stage, and there was no specific difference between the groups. Delayed bleeding was seen after EMR in one patient (1.2%) from the famotidine group and in one patient (2.2%) from the pantoprazole group. There were no other major complications after EMR. CONCLUSIONS: Famotidine was no different than pantoprazole in its effectiveness toward preventing delayed bleeding and promoting healing of iatrogenic ulcers after EMR.
2-Pyridinylmethylsulfinylbenzimidazoles ; Cicatrix ; Famotidine ; Hemorrhage ; Histamine ; Humans ; Proton Pumps ; Retrospective Studies ; Stomach ; Stomach Neoplasms ; Ulcer

BACKGROUND/AIMS: Several rescue therapies have been recommended to eradicate Helicobacter pylori infection in patients with a failure of first-line eradication therapy, but they still fail in more than 20% of cases. The aim of this study was to evaluate the efficacy and safety of levofloxacin, metronidazole, and lansoprazole (LML) triple therapy relative to quadruple therapy as a second-line treatment. METHODS: In total, 113 patients who failed first-line triple therapy for H. pylori infection were randomly assigned to two groups: LML for 7 days and tetracycline, bismuth subcitrate, metronidazole and lansoprazole (quadruple) for 7 days. RESULTS: According to intention-to-treat analysis, the infection was eradicated in 38 of 56 patients (67.9%) in the LML group and 48 of 57 (84.2%) in the quadruple group (p=0.042). Per-protocol analysis showed successful eradication in 38 of 52 patients (73.1%) from the LML group and 48 of 52 (92.3%) from the quadruple group (p=0.010). There were no significant differences in the adverse effects in either treatment group. CONCLUSIONS: LML therapy is less effective than quadruple therapy as a second-line treatment for H. pylori infection. Therefore, quadruple therapy should be considered as the primary second-line strategy for patients experiencing a failure of first-line H. pylori therapy in Korea.
2-Pyridinylmethylsulfinylbenzimidazoles ; Bismuth ; Helicobacter ; Helicobacter pylori ; Humans ; Korea ; Metronidazole ; Ofloxacin ; Organometallic Compounds ; Tetracycline