A Study to Evaluate the Symptomatic Efficacy and Safety of LafaxidTM (Lafutidine 10mg) in Patients with Acid Peptic Disorders in India.

Aims: To evaluate the symptomatic efficacy and safety of Lafaxid™ (lafutidine 10 mg) in Indian patients with Acid Peptic disorder (APD). Study Design: An observational, prospective, uncontrolled, open-label multi-centric study. Place and Duration of Study: Patients were recruited from 12 cities across India by 61 investigators, between October 2010 and December 2011. Methodology: We included 1500 patients (973 men, 527 women; age range 15-85 years) with Acid Peptic disorder. Lafutidine (10 mg tablets) was prescribed by the physicians as once daily dose (OD) for 28 days. The efficacy was analysed based on the change in the symptom baseline score on the 100 point Visual Analogue Scale (VAS) for individual symptoms, and the safety was determined based on adverse events reported during the study with the prescribed usage of lafutidine on day 14 and day 28 after start of the treatment. Results: Lafutidine monotherapy was given to 1378 patients. A very high reduction in the mean VAS score was observed from baseline for individual symptoms, viz. nausea, vomiting, belching, heart burn, epigastric pain, acid regurgitation, abdominal bloating & loss of appetite at the end of the study. The global mean VAS score (a sum of individual symptom VAS score) of these patients decreased from 120.34 ± 67.58 to 14.18 ± 26.97 at the end of the study (P < .001). There were 124 APD patients, previously treated but uncontrolled, with acid inhibitors like PPIs, H2RAs etc., also showed a significant reduction (157.42 ± 83.88 to 26.47 ± 46.34) in the VAS score on day 28 (P<.001). During the entire study, adverse events of mild and moderate nature were observed in 0.4% (6 patients) of the total patient population. Conclusion: The present study demonstrates that therapy with Lafaxid™ is symptomatically effective and well tolerated in patients with APDs.

Quantitative determination of Cimetidine in both bulk and formulations using neutralization titrations.

Cimetidine is the selective H2 receptor antagonist and inhibits the secretion of hydrochloric acid in the stomach. In the present study, simple titrimetric method was developed. Respective quantities of Cimetidine were taken in aqueous methanol and acetic acid titrated against 0.1N hydrochloric acid and 0.1N perchloric acid using methyl orange and crystal violet as indicators for neutralization and non-aqueous titrations. All the titrations are carried out by running simultaneous blank determinations. The final titer values are subtracted from blank to get actual amount of acid consumed was determined. These methods were found to be sensitive and inexpensive, do not require any sample processing steps and can be utilized for estimation of cimetidine in bulk and formulations.

Rebamipide May Be Comparable to H2 Receptor Antagonist in Healing Iatrogenic Gastric Ulcers Created by Endoscopic Mucosal Resection: A Prospective Randomized Pilot Study

Endoscopic mucosal resection (EMR) results in the formation of iatrogenic gastric ulcers and the optimal treatments for such ulcers are still unclear. We aimed to evaluate the efficacy of rebamipide in the management of EMR-induced ulcers by comparing it with an H2 receptor antagonist. After EMR, patients were randomly assigned into either rebamipide or famotidine groups. All patients received a one-week lansoprazole 30 mg q.d. therapy followed by three-week famotidine (20 mg b.i.d.) or rebamipide (100 mg t.i.d.) therapy. Four weeks after the treatments, ulcer sizes, stages, bleeding rates, and ulcer-related symptoms were compared using endoscopy and a questionnaire. A total of 63 patients were enrolled in this study. Finally, 51 patients were analyzed, 26 in rebamipide and 25 in famotidine group. Baseline characteristics were not significantly different between the two groups. Four weeks after EMR, the two groups were comparable in terms of ulcer reduction ratio (P=0.297), and ulcer stage (P=1.000). Moreover, no difference was observed with regard to ulcer-related symptoms, drug compliance, adverse drug event rates, and bleeding rates. Our data suggest that rebamipide is not inferior to famotidine in healing iatrogenic gastric ulcers, and could be a therapeutic option in the treatment of such ulcers.

Anaphylaxis Induced by Intravenous Ranitidine Injection: 2 Case Reports / 대한구급학회지

Histamine type 2 (H2) receptor antagonists are widely used for stress ulcer prophylaxis in critical and postoperative care. Though ranitidine is one of the most commonly used H2 receptor antagonists, with a low incidence of adverse reactions, a few anaphylactic reactions associated with ranitidine have been reported. This report describes 2 additional cases of anaphylaxis induced by ranitidine used for stress ulcer prophylaxis.

Therapeutic Effect of Low-Dose Omeprazole vs. Standard-Dose Ranitidine in Mild to Moderate Reflux Esophagitis / 대한소화기학회지

BACKGROUND/AIMS: Proton pump inhibitors (PPI) and H2-receptor antagonists (H2RA) are commonly prescribed for the treatment of mild to moderate reflux esophagitis (MMRE). There remains great controversy in their usefulness as the first choice and the appropriateness. We prospectively compared the efficacy and safety of the 8-week low-dose PPI vs. standard-dose H2RA in MMRE. METHODS: One hundred patients with MMRE were randomized to receive either low-dose of omeprazole (L-OMP: 10 mg, q.d.) or standard-dose of ranitidine (S-H2RA: 150 mg, b.i.d.) for 8 weeks. The H. pylori status using rapid urease test, histological examination and culture, reflux esophagitis (RE) grading, gastrointestinal symptoms using 4-point scale, adverse event and the standard laboratory examination were assessed at baseline and 8-week end point of therapy. RESULTS: Improvement rate of RE [intention to treat (n=82)/per protocol (n=72)] were shown in 69.1%/63.9% for L-OMP and 65.0%/63.9% for S-H2RA group (p=0.697, p=1.000). Complete healing rates of RE were 54.7%/50.0% for L-OMP and 42.5%/41.7% for S-H2RA. No significant difference in healing rate, the rapidity of symptom resolution, adverse events, and laboratory monitoring was found between the two groups. CONCLUSIONS: The low-dose omeprazole therapy produced similar healing rates and safety in the treatment of MMRE. In addition, L-OMP is advantageous in its once-a-day dosing and might be an alternative to S-H2RA, especially in Korean patients with MMRE.

H2 Receptor Antagonists and Gastric Cancer in the Elderly: A Nested Case-Control Study / 예방의학회지

OBJECTIVE: To test if the intake of H2 receptor antagonists (H2-RAs) increases the risk of gastric cancer in the elderly. METHODS: The source population for this study was drawn from the responders to a questionnaire survey administered to the Korea Elderly Pharmacoepidemiological Cohort (KEPEC), who were beneficiaries of the Korean Medical Insurance Corporation, were at least 65 years old, and residing in Busan in 1993. The information on H2-RAs exposure was obtained from a drug prescription database compiled between Jan. 1993 and Dec. 1994. The cases consisted of 76 gastric cancer patients, as confirmed from the KMIC claims data, the National Cancer Registry and the Busan Cancer Registry. The follow-up period was from Jan. 1993 to Dec. 1998. Cancer free controls were randomly selected by 1:4 individual matching, which took in to consideration the year of birth and gender. Information on confounders was collected by a mail questionnaire survey. The odds ratios, and their 95% confidence intervals, were calculated using a conditional logistic regression model. RESULTS: After adjusting for a history of gastric ulcer symptoms, medication history, and body mass index, the adjusted OR (aOR) was 4.6 (95% CI=1.72-12.49). The odds ratio of long term use (more than 7 days) was 2.3 (95% CI=1.07-4.82). The odds ratio of short term use was 4.6 (95% CI=1.26-16.50). The odds ratio of parenteral use was 4.4 (95% CI=1.16-17.05) and combination use between the oral and parenteral routes (aOR, 16.8; 95% CI=1.21-233.24) had the high risk of gastric cancer. The aOR of cimetidine was 1.7 (95% CI=1.04-2.95). The aOR of ranitidine was 2.0 (95% CI=1.21-3.40). The aOR of famotidine was 1.7 (95% CI=0.98-2.80). CONCLUSION: The intake of H2-RAs might increase the risk of gastric cancer through achlorhydria in the elderly.

The Effects of Ranitidine (300mg) and Omeprazole (10, 20mg) on Gastroesophageal Reflux and Intragastric pH in Healthy Subjects / 대한소화관운동학회지

BACKGROUND/AIMS: This study was done to compare the effects of Omeprazole (OMD) 10 or 20 mg with Ranitidine(RAN) 300 mg on intragastric acidity and gastroesophageal reflux in healthy subjects. METHODS: Ten healthy male volunteers were studied after administrations of 5 days dosing with either RAN 300 mg, OMD 10 mg or 20 mg, once each morning. On the 5(th) day, intragastric pH and lower esophageal pH were measured by a dual channel antimony pH catheter for 10 hours. RESULTS: Gastroesophageal reflux was reduced after administrations of RAN 300 mg, OMD 10 mg or 20 mg (p 0.05). The gastric holding time of pH > 4 was significantly prolonged over fasting and postprandial periods after RAN 300 mg, OMD 10 mg or 20 mg administrations (p 0.05). OMD administrations (10 mg or 20 mg) exhibited a more potent effect on gastric acid suppression during the postprandial period than RAN 300 mg (p < 0.05). CONCLUSIONS: OMD 10 mg was as potent as RAN 300 mg on inhibition of gastric acid, but less potent than OMD 20 mg. There was no difference among the three drugs in regard to gastroesophageal reflux in healthy subjects.

INFLUENCE OF H_2-RECEPTOR ANTAGONIST ON GASTRIC MUCOUS MEMBRANE AND GASTRIC JUICE IN SEVERE BURNED RATS / 第二军医大学学报

In this study, 119 adult wistar rats were used, and divided into four groups (control group, burn group, burn-cimetidine treatment group and burn-ranitidine reatment grup). 20% TBSA full thickness burn was produced by immersion of the clipped back of the rat in 100℃ boiling water for 15s. The rats of the control group were immersed in 37℃ water for 15 s. In the treatment groups, the animals were treated with cimetidine (0.1 mg/g) or ranitidine (0.05 mg/g) intraperitoneally every 12 h, respectively. All animals were given fluid therapy according to the TBSA and body weight. In the animals treated with cimetidine or ranitidine, the H+ concentration of gastric juice was greatly decreased as compared with that of the burn group (P