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PubMed2001

Pharmacokinetic differences between lansoprazole enantiomers and contribution of cytochrome P450 isoforms to enantioselective metabolism of lansoprazole in dogs.

The purpose of this study was to evaluate the pharmacokinetics of lansoprazole enantiomers and contribution of cytochrome P450 enzymes to enantioselective metabolism in dogs. The mean Cmax and area under the curve (AUC) values of (+)-lansoprazole were 4-5 times greater than those of (-)-lansoprazole following oral administration of 30-mg racemic lansoprazole to dogs. The CLtot/F values of (+)-lansoprazole were significantly smaller than those of (-)-lansoprazole (p<0.05). The mean unbound fraction of (-)-lansoprazole was significantly greater than that of the (+)-lansoprazole. The amount of (+)-lansoprazole remaining was significantly greater than that of the (-)-lansoprazole after incubation of racemic lansoprazole in dog liver microsomes. When the effects of ticlopidine or ketoconazole on the metabolism of lansoprazole were studied using dog liver microsomes, ticlopidine significantly inhibited the formation of 5-hydroxylansoprazole, but not another metabolite, lansoprazole sulfone; however ketoconazole significantly inhibited formation of both metabolites. When the amount of (+)- and (-)-enantiomers remaining was measured in the presence and absence of ticlopidine, the amount of (+)-lansoprazole was significantly greater than that of the (-)-lansoprazole. On the other hand, there was no significant difference between the amount of (+)- and (-)-enantiomers remaining in combination with ketoconazole. These results suggest that the enantioselective pharmacokinetics of lansoprazole enantiomers are probably ascribable to their enantioselective protein binding and/or metabolism, and among the cytochrome P450 enzymes, CYP3A contributed to the enantioselective metabolism of lansoprazole.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1996

Efficacy and safety of lansoprazole in the treatment of erosive reflux esophagitis. The Lansoprazole Group.

OBJECTIVES: This study was designed to compare lansoprazole 30 mg, lansoprazole 15 mg, omeprazole 20 mg, and placebo in the treatment of erosive reflux esophagitis. METHODS: In a double-blind, multicenter study, 1284 patients with endoscopically diagnosed erosive reflux esophagitis were randomized to received lansoprazole 30 mg (n = 422), lansoprazole 15 mg (n = 218), omeprazole 20 mg (n = 431), or placebo (n = 213) once daily for 8 wk. At 2, 4, 6, and 8 wk, healing was evaluated endoscopically. Patients kept daily diaries of symptoms. RESULTS: Healing rates at 2, 4, 6, and 8 wk were 65.3%, 83.3%, 89.4%, and 90.0%, respectively, for lansoprazole 30 mg; 56.3%, 74.6%, 80.3%, and 78.8% for lansoprazole 15 mg; 60.9%, 82.0%, 89.7%, and 90.7% for omeprazole 20 mg; and 23.9%, 32.8%, 36.6%, and 40.0% for placebo (all active treatments higher than placebo, p < 0.001). Healing rates with lansoprazole 30 mg were significantly higher than with lansoprazole 15 mg at all time points (p < 0.05). Healing rates with omeprazole 20 mg were significantly higher than with lansoprazole 15 mg at 4, 6, and 8 wk and were similar to those with lansoprazole 30 mg. Based on patient diaries, lansoprazole 30 mg produced better symptomatic relief than lansoprazole 15 mg or omeprazole 20 mg, primarily early in the treatment course. CONCLUSIONS: Both lansoprazole 30 mg and omeprazole 20 mg were more effective than lansoprazole 15 mg in esophageal mucosal healing. Compared with omeprazole 20 mg, lansoprazole 30 mg was as safe, was similarly effective with respect to esophageal healing, and provided superior symptomatic relief, primarily early in treatment. Lansoprazole 30 mg provided greater symptomatic relief than lansoprazole 15 mg.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1994

Double-blind comparison of lansoprazole, ranitidine, and placebo in the treatment of acute duodenal ulcer. Lansoprazole Study Group.

OBJECTIVES: To study in a double-blind controlled manner the effects of lansoprazole 15 mg or 30 mg daily compared with ranitidine 300 mg once daily and placebo in the relieving of symptoms and healing of acute duodenal ulceration. METHODS: Two hundred eighty patients with duodenal ulcer entered in to the study from 30 centers. They were randomized in a double-blind manner into four groups with 80 patients entered into each active treatment group and 40 patients into the placebo group. Endoscopy was performed at 2- and 4-wk intervals to assess healing. Symptom relief was recorded, serum gastrin levels were measured, and gastric mucosal biopsies were obtained to evaluate for the presence of acute and chronic inflammation, the presence of neoplasia, and the extent of gastric endocrine growth at the time of endoscopy. RESULTS: After 4 wk of treatment using per protocol analysis, 19 of 40 (47.5%) patients receiving placebo had healed compared with 55 of 78 (70.5%) receiving ranitidine (p < 0.05 vs. placebo), 61 of 76 (80.3%) receiving lansoprazole 30 mg (p < 0.05 vs. placebo), and 72 of 78 (92.3%) receiving lansoprazole 15 mg (p < 0.05 vs. placebo and ranitidine). In patients with evaluable data, lansoprazole 30 mg and ranitidine produced greater relief of night-time symptoms and lansoprazole 15 mg produced greater relief of both day- and night-time symptoms than did placebo after 4 wk of treatment. Ranitidine increased fasting serum gastrin levels (22%; p < 0.05 vs. placebo), whereas both lansoprazole regimens produced more marked rises in serum gastrin (54% and 60%; p < 0.05 vs. placebo and ranitidine). Lansoprazole 15 mg and 30 mg also increased the density of antral G-cells (105.8% and 128.80%; p < 0.05 vs. baseline) and greater curvature Grimelius-positive cells (20.33% and 28.8%; p < 0.05 vs. baseline); there were no increases in the density of antral EC- or D-cells, and there was no alteration of gastric endocrine growth as judged by the Solcia classification. Both ranitidine and lansoprazole were associated with decreased antral Helicobacter pylori density accompanied, in the lansoprazole groups, by decreased antral inflammation scores. All antisecretory regimens were associated with increased inflammatory scores in the greater curvature. CONCLUSIONS: In acute duodenal ulceration, treatment with lansoprazole 15 and 30 mg produced 4-wk healing rates and symptom relief superior to those produced by placebo and the 15-mg dose similar to those produced by placebo. The 15-mg dose of lansoprazole was also superior to ranitidine in healing duodenal ulcer after 4 wk of therapy.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1999

Double-blind comparison of lansoprazole 15 mg, lansoprazole 30 mg and placebo as maintenance therapy in patients with healed duodenal ulcers resistant to H2-receptor antagonists.

BACKGROUND: Maintenance antisecretory therapy is often used to prevent duodenal ulcer recurrence and control symptoms. This study compared the efficacy and safety of lansoprazole 15 mg and 30 mg daily with placebo in preventing ulcer recurrence in patients with a recent history of duodenal ulcer disease. METHODS: Fifty-six patients were treated with either lansoprazole 15 mg, 30 mg or placebo o.m. RESULTS: Within 1 month of study initiation, 27% (four out of 15) of placebo-treated patients experienced ulcer recurrence as compared to 13% (two out of 15) and 6% (one out of 18) of lansoprazole 15 mg and 30 mg treated patients, respectively. Median time to first ulcer recurrence was > 12 months in lansoprazole patients. At Month 12, significantly (P < 0.001) more lansoprazole 15 mg patients (70%) and lansoprazole 30 mg patients (85%) remained healed. Eighty-two per cent of lansoprazole 15 mg and 76% of lansoprazole 30 mg patients remained asymptomatic during the entire study period. All placebo patients became symptomatic, experienced ulcer recurrence, or withdrew from the study by month six. The incidence of adverse events was comparable among the three treatment groups. CONCLUSIONS: Lansoprazole safely and effectively reduces duodenal ulcer recurrence and ulcer-related symptoms.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed2004

Double-blind, randomized controlled study to assess the effects of lansoprazole 30 mg and lansoprazole 15 mg on 24-h oesophageal and intragastric pH in Chinese subjects with gastro-oesophageal reflux disease.

BACKGROUND: Previous studies have suggested that the acid secretory capacity of the Chinese population is lower than that of the Western population. AIM: To compare the effect of lansoprazole 30 mg and 15 mg once daily on the 24-h oesophageal and intragastric pH profiles in Chinese patients with gastro-oesophageal reflux disease. METHODS: Forty-four patients (male to female ratio, 27 : 17; mean age, 53 years; 55% with oesophagitis) with gastro-oesophageal reflux disease were randomized to receive lansoprazole 30 mg or 15 mg once daily for 4 weeks. Measurement of the 24-h oesophageal and intragastric pH, gastro-oesophageal reflux disease symptoms and quality of life was performed at baseline and during the last week of each dosing period. RESULTS: Lansoprazole 30 mg maintained an intragastric pH > 4 for 10.5 h vs. 9.6 h for lansoprazole 15 mg (P = 0.44). The percentage total time at oesophageal pH < 4 was similar for lansoprazole 30 mg and 15 mg (2.0% vs. 2.3%, P = 0.30). The proportion of patients with complete cure of heartburn and acid regurgitation and the quality of life assessment were similar for lansoprazole 30 mg and 15 mg. Both dosages of lansoprazole were well tolerated and the compliance was 100% in both groups. CONCLUSION: Lansoprazole dosages of 30 mg and 15 mg once daily provide a satisfactory decrease for oesophageal acid exposure and are equally effective for the treatment of gastro-oesophageal reflux disease in the Chinese population.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1999

Standard-dose lansoprazole is more effective than high-dose ranitidine in achieving endoscopic healing and symptom relief in patients with moderately severe reflux oesophagitis. The Dutch Lansoprazole Study Group.

BACKGROUND: In the treatment of reflux oesophagitis, H2-receptor antagonists are still widely used in spite of the apparent higher efficacy of proton pump inhibitors. In an attempt to compensate for the lower efficacy, H2-receptor antagonists are now increasingly being used at a higher dose. OBJECTIVE: To assess whether or not standard-dose lansoprazole (30 mg o.d.) is more effective than high-dose ranitidine (300 mg b.d.) in moderately severe reflux oesophagitis (grades II-III). METHODS: Lansoprazole or ranitidine was given to 133 patients for 4-8 weeks in a double-blind, randomized, parallel group, multicentre trial. RESULTS: The percentage of patients with endoscopically-verified healing was significantly higher on lansoprazole than on ranitidine both after 4 weeks (79% vs. 42%) and 8 weeks (91% vs. 66%), though smoking had a negative impact on oesophagitis healing with lansoprazole. Heartburn, retrosternal pain and belching improved significantly better with lansoprazole than with ranitidine, as did the patient-rated overall symptom severity. Relief of heartburn appeared somewhat faster with ranitidine, but was more pronounced with lansoprazole. The number of patients with adverse events was similar in both treatment groups. CONCLUSION: Standard-dose lansoprazole is better than high-dose ranitidine in moderately severe reflux oesophagitis.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1995

Lansoprazole versus ranitidine for the treatment of reflux oesophagitis. UK Lansoprazole Clinical Research Group.

BACKGROUND: Lansoprazole is a H+.K(+)-ATPase (proton pump) inhibitor with an anti-secretory action and is therefore potentially useful in the treatment of gastro-oesophageal reflux. METHODS: This study was conducted to determine the efficacy and short-term safety of lansoprazole at doses of 30 mg or 60 mg once daily, compared with ranitidine 150 mg twice daily, in the treatment of patients with reflux oesophagitis. This was a double-blind, stratified, randomized, comparative, parallel group study conducted in five centres in the UK. A total of 229 patients (155 men) aged 18-79 years with endoscopically-confirmed oesophagitis were randomized to receive lansoprazole 30 mg p.o. daily, lansoprazole 60 mg p.o. daily, or ranitidine 150 mg p.o. b.d. Efficacy was assessed by endoscopic examination at 4 weeks and 8 weeks, together with symptom relief and antacid usage. RESULTS: Lansoprazole 30 mg and 60 mg were superior at 4 and 8 weeks (P < 0.01) to ranitidine in healing reflux oesophagitis: respective healing rates being 84%, 72% and 39% after 4 weeks and 92%, 91% and 53% after 8 weeks. Relief of heartburn with lansoprazole 30 mg and 60 mg was superior to that achieved with ranitidine at both week 4 (P < 0.01) and week 8 (P < 0.02). Sixty-four patients experienced a total of 85 adverse events, one-third of which were considered drug-related. The incidence and severity were similar in the three groups. CONCLUSION: Lansoprazole 30 mg and 60 mg once daily are more effective than ranitidine 150 mg twice daily in the short-term treatment of reflux oesophagitis.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1995

A comparison of three doses of lansoprazole (15, 30 and 60 mg) and placebo in the treatment of duodenal ulcer. The Lansoprazole Study Group.

BACKGROUND: Lansoprazole is a new proton pump inhibitor for the treatment of peptic ulcer disease. METHODS: A double-blind, multicentre study was undertaken in 296 patients with endoscopically proven duodenal ulcer to compare the efficacy and safety of lansoprazole 15, 30 or 60 mg with placebo. Ulcer healing was documented by endoscopy at 2 and 4 weeks; patients whose ulcers healed after 4 weeks were followed for up to 6 months post-treatment. RESULTS: Four-week healing rates of 89.4%, 91.7% and 89.9% were obtained with lansoprazole 15, 30 and 60 mg, respectively, compared with 46.1% on placebo (P < 0.001). All three doses of lansoprazole produced rapid symptom relief, although patients taking 60 mg lansoprazole required fewer antacids than did those taking 15 mg. At 6 months, the percentages of patients healed were 45.3%, 40.0% and 38.4% in the lansoprazole 15, 30 and 60 mg dosage groups, respectively, and 25.3% for the placebo group. No significant adverse events were documented during the period of this trial. CONCLUSION: Lansoprazole is an effective and safe treatment for duodenal ulcer and the 15 mg dose is as effective as 30 or 60 mg.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1999

Simplified lansoprazole suspension--a liquid formulation of lansoprazole--effectively suppresses intragastric acidity when administered through a gastrostomy.

OBJECTIVE: Lansoprazole suppresses intragastric acidity when given as nonencapsulated intact granules. Because the administration of granules via small-bore tubes may still be problematic, we studied the effect of a liquid formulation of lansoprazole obtained by suspending the contents of a standard 30-mg capsule in 10 cc of 8.4% NaHCO3. METHODS: Six men with an established gastrostomy had a baseline 24-h intragastric pH study. Through the gastrostomy, they then received 7 days of once-daily dosing with 30 mg lansoprazole as intact granules in orange juice. After a 7-day washout period, they then received 7 days of once-daily dosing with the liquid formulation. Intragastric pH monitoring was repeated after each dosing period. RESULTS: Baseline mean intragastric pH was 1.8 +/- 0.5 (SD). This increased to 4.5 +/- 0.5 with lansoprazole granules in orange juice, and to 5.1 +/- 1.1 after the liquid formulation. At baseline, intragastric pH was >3, 4, and 5 for 19.5%, 12.7%, and 8.1%, respectively, of the 24-h recording period. Corresponding values after lansoprazole granules in orange juice were 77.5%, 67%, and 49.6% (p < 0.01 for each comparison with baseline). After the liquid formulation, the corresponding values were 84%, 77.9%, and 65.9% respectively (p < 0.01 for each comparison with baseline; p > 0.05 for each comparison with lansoprazole granules in orange juice). CONCLUSIONS: A liquid formulation of lansoprazole suppressed intragastric acidity when given through a gastrostomy. The degree of suppression was comparable to that obtained with intact nonencapsulated granules in orange juice.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1996

Lansoprazole prevents recurrence of erosive reflux esophagitis previously resistant to H2-RA therapy. The Lansoprazole Maintenance Study Group.

OBJECTIVE: This randomized, double-blind study was designed to determine whether the proton pump inhibitor lansoprazole could prevent relapse among patients with healed erosive reflux esophagitis that had been resistant to healing with at least 3 months of H2-receptor antagonist therapy. RESULTS: By the end of the year, 13% of placebo patients remained healed compared with 67% of lansoprazole 15 mg and 55% of lansoprazole 30 mg patients (p < 0.001 for time to first relapse). All placebo patients were symptomatic by the end of the study whereas only one-third of the lansoprazole patients was symptomatic at the end of the 12-month study period. The two lansoprazole doses were comparably effective in maintaining healing and in symptom control and were well tolerated. Fasting serum gastrin values increased significantly to about 1.5-2 times the baseline values over the first 2 months of lansoprazole treatment; no further increase was noted. CONCLUSION: Erosive relapse can be prevented in most patients for up to 1 yr with lansoprazole 15 mg or 30 mg once daily.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1998

Double-blind comparison of lansoprazole 15 mg, lansoprazole 30 mg, and placebo in the maintenance of healed gastric ulcer.

Our purpose was to compare the safety and efficacy of lansoprazole 15 mg and 30 mg with placebo in preventing recurrence in 49 patients with a history of gastric ulcer. Within one month, 40% of patients receiving placebo experienced ulcer recurrence compared to 0% and 7% of patients receiving lansoprazole 15 mg and 30 mg, respectively. All placebo patients became symptomatic, experienced ulcer recurrence or withdrew from the study by month 9. As compared to placebo, a significantly (P < 0.001) higher percentage of patients treated with lansoprazole 15 mg (83%) and lansoprazole 30 mg (93%) with healed gastric ulcer disease remained healed at month 12. Of patients asymptomatic at baseline, 100% and 59% of those treated with lansoprazole 15 mg and 30 mg, respectively, remained asymptomatic at month 12. The incidence of adverse events was comparable among the treatment groups. Lansoprazole safely and effectively reduces ulcer recurrence in patients with a history of gastric ulcer disease.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed2000

Omeprazole 40 mg once a day is equally effective as lansoprazole 30 mg twice a day in symptom control of patients with gastro-oesophageal reflux disease (GERD) who are resistant to conventional-dose lansoprazole therapy-a prospective, randomized, multi-centre study.

BACKGROUND: Comparative studies of omeprazole and lansoprazole are scarce and even scarcer are comparisons of higher doses. Most of the comparative studies have assessed the effect of the two proton pump inhibitors (PPIs) on gastric acid secretion or gastric pH. Few studies have compared clinical end-points such as oesophageal healing and symptom control. AIM: To determine the clinical efficacy of omeprazole 40 mg daily as compared to lansoprazole 30 mg twice a day in symptom control of patients with severe symptomatic GERD. METHODS: Ninety-six patients who failed a standard dose of lansoprazole (30 mg once daily), were enrolled in a prospective fashion from three VA medical centres and were randomized to receive 6 weeks of either omeprazole 40 mg daily or lansoprazole 30 mg twice daily. Patients reported daily on symptom severity and frequency, antacid consumption and side-effects. RESULTS: Forty-six patients received omeprazole and 44 lansoprazole. Although not statistically significant, there was a consistent trend of better symptom control in the omeprazole group for daytime and night-time heartburn and acid regurgitation. There was no statistical difference between the two groups in mean antacid consumption overall and at the end of each of the 6 weeks of the study. In addition, there was no significant difference in the overall frequency of side-effects between the two groups nor for each individual side-effect. CONCLUSION: Omeprazole 40 mg once daily is equally effective and tolerated as lansoprazole 30 mg twice daily in symptom control of patients with GERD.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1998

Dual therapy using a double dose of lansoprazole with amoxicillin versus triple therapy using a double dose of lansoprazole, amoxicillin, and clarithromycin to eradicate Helicobacter pylori infection: results of a prospective randomized open study.

OBJECTIVES: The eradication of Helicobacter pylori is recommended in duodenal ulcer disease. The aim of this randomized open trial was to evaluate and compare H. pylori eradication and safety after a dual therapy consisting of lansoprazole (30 mg b.i.d.) and amoxicillin (1 g b.i.d.) versus a triple therapy consisting of lansoprazole (30 mg b.i.d.), amoxicillin (1 g b.i.d.), and clarithromycin (500 mg b.i.d.) administered from day 1 to day 14. METHODS: All patients with an ulcer received lansoprazole (30 mg) from day 15 to day 28. H. pylori status was determined from antral biopsies using histology, culture, and polymerase chain reaction (PCR) upon inclusion and 1-3 months after the end of the treatment. RESULTS: Of the 50 patients included in the study, five did not adhere to the protocol. H. pylori eradication was obtained in 37.5% of the patients receiving lansoprazole-amoxicillin (n = 9/24) and in 95.2% of the patients receiving lansoprazole-amoxicillin-clarithromycin (n = 20/21, p < 0.0002). Minor side effects appeared in 8.3% of the cases during dual therapy (n = 2/24) and in 52% during triple therapy (n = 13/22, p < 0.001). These side effects consisted mainly of diarrhea and a metallic taste. CONCLUSION: Concomitant administration of double doses of lansoprazole with amoxicillin and clarithromycin is very efficacious against H. pylori infection compared with dual therapy.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1993

Treatment of reflux esophagitis resistant to H2-receptor antagonists with lansoprazole, a new H+/K(+)-ATPase inhibitor: a controlled, double-blind study. Lansoprazole Study Group.

This multicenter, randomized, double-blind, 8-wk study compared the new H+/K(+)-ATPase inhibitor, lansoprazole, 30 mg daily, to ranitidine 150 mg bid for treatment of erosive reflux esophagitis resistant to histamine-2 receptor antagonists (H2RA). Patients were evaluated after 2, 4, 6, and 8 wk of treatment by symptom assessment and endoscopy. Healing rates for lansoprazole were 71%, 80%, 88%, and 89% at 2, 4, 6, and 8 wk, respectively, compared to 21%, 33%, 45%, and 38% for ranitidine (p < 0.001 at all points). Lansoprazole was significantly more effective than ranitidine for relief of heartburn and reduction of antacid tablet use. Increases in serum gastrin concentrations between the baseline and the 8-wk visit were greater in lansoprazole-treated than in ranitidine-treated patients. Lansoprazole was safe and well tolerated. In patients with erosive reflux esophagitis resistant to standard doses of H2RA, lansoprazole 30 mg/day is more effective than continuation of an H2RA (ranitidine 150 mg bid) for healing of esophagitis and improvement of symptoms.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1997

Prevention of duodenal ulcer recurrence with 15 mg lansoprazole: a double-blind placebo-controlled study. The Lansoprazole Study Group.

Although eradication of Helicobacter pylori cures duodenal ulcer, some patients are not infected and others are treatment failures. This randomized, double-blind, placebo-controlled study assessed the value of treatment with low-dose lansoprazole in preventing duodenal ulcer recurrence. One hundred eighty-six patients with endoscopic documentation of healed duodenal ulcer received 15 mg/day lansoprazole or placebo for 12 months or until ulcer recurred. Endoscopy results, symptom assessment, and fasting serum gastrin levels were obtained at multiple time points. Densities of E, EC, and G cells were assessed by biopsy when the ulcer recurred or at the final visit. Time to ulcer recurrence was significantly longer (P < 0.001) in the lansoprazole group (median >12 months) compared to placebo (median <3 months), and patients taking lansoprazole were asymptomatic longer (P < 0.05). Maintenance therapy with lansoprazole 15 mg/day suppresses acid and controls recurrence of duodenal ulcer disease.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed1995

Growth inhibition of Ureaplasma urealyticum by the proton pump inhibitor lansoprazole: direct attribution to inhibition by lansoprazole of urease activity and urea-induced ATP synthesis in U. urealyticum.

The proton pump inhibitors (PPIs) omeprazole and lansoprazole and the acid-activated analog of lansoprazole AG-2000, which potently inhibit the urease of Helicobacter pylori (K. Nagata, H. Satoh, T. Iwahi, T. Shimoyama, and T. Tamura, Antimicrob. Agents Chemother. 37:769-774, 1993), also inhibited the urease activities of cell-free extracts as well as intact cells of Ureaplasma urealyticum. The 50% inhibitory concentrations were between 1 and 25 microM. These compounds also inhibited the ATP synthesis induced by urea in ureaplasma cells. The 50% inhibitory concentrations for ATP synthesis were close to those for urease activity, but they were lower than those of urease inhibitors, such as acetohydroxamic acid, hydroxyurea, and thiourea. In addition, one of the metabolites of lansoprazole found in human urine, M-VI, also inhibited ureaplasmal urease activity and the ATP synthesis induced by urea at almost the same concentrations as those of lansoprazole. The inhibition of PPIs against ureaplasma urease was very similar to those against H. pylori urease, suggesting that the inhibitory mechanism against these ureases was due to the blockage of the SH residues on the cysteine of the enzyme. Omeprazole, lansoprazole, AG-2000, and M-VI inhibited the growth of U. urealyticum. Since ureaplasma urease is thought to be involved in the pathogenicity of this organism in the urogenital tract, PPIs and their analogs may be useful as chemotherapeutic agents against diseases caused by U. urealyticum.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed2002

Low-dose lansoprazole and clarithromycin plus metronidazole vs. full-dose lansoprazole and clarithromycin plus amoxicillin for eradication of Helicobacter pylori infection.

AIM: To compare, in a randomized controlled trial, the efficacy and tolerability of two 1-week triple therapies for Helicobacter pylori eradication. METHODS: One hundred and thirty-four consecutive patients with non-ulcer dyspepsia and H. pylori infection were randomized to receive lansoprazole 30 mg once daily, clarithromycin 250 mg twice daily, and metronidazole 500 mg twice daily (LCM group), or lansoprazole 30 mg twice daily, clarithromycin 500 mg twice daily, and amoxicillin 1000 mg twice daily (LCA group). H. pylori status was assessed by rapid urease test, histology and 13C-urea breath test before and after therapy. RESULTS: At 3 months, H. pylori eradication (intention- to-treat/per protocol analysis) was 92.4%/93.8% in the LCM group and 83.1%/85.7% in the LCA group (P=N.S.). Side-effects were more frequently reported in the LCA group (37.9%) than in the LCM group (19.7%) (P < 0.05). CONCLUSIONS: In this open, randomized controlled trial, eradication of H. pylori by low-dose lansoprazole and clarithromycin plus metronidazole was higher with significantly less side-effects than by full-dose lansoprazole and clarithromycin plus amoxicillin. This finding may be related to the stronger synergism of clarithromycin plus metronidazole, even at lower doses, than of clarithromycin plus amoxicillin. Considering the lower cost as well, LCM should be preferred to LCA in the eradication of H. pylori.

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed2000

Two weeks triple therapy with lansoprazole, amoxycillin and roxythromycin is better than dual therapy with lansoprazole and amoxycillin for H. pylori infection: a randomised, clinical trial.

AIMS: To compare the efficacy of 2 weeks of dual therapy of Lansoprazole and Amoxycilline with triple therapy of Lansoprazole, Amoxycilline and Roxythromycin for H. pylori eradication. SUBJECTS: Twenty-five suffering from dyspepsia and found H. pylori positive (CLO) during upper GI endoscopy. METHODS: Patients were divided into 2 groups, one group received Lansoprazole (30 mg) once a day, and amoxycilline (500 mg) three times a day (group I), while the second group received Lansoparazole and amoxycillin in similar dosage with the addition of Roxythromycin (150 mg) twice a day (group II). H. pylori status was confirmed on endoscopy using CLO test at entry to the protocol and then at 4 weeks. RESULTS: H. pylori eradication was 57% in group I and 86% in group II with healing of lesions in all cases. CONCLUSION: Better response with triple therapy (group II) indicates enhanced eradication of the pathogens with triple therapy while using roxythromycin (JPMA 50:157, 2000).

2-Pyridinylmethylsulfinylbenzimidazoles↗