Lansoprazole

Abstract

Lansoprazole is an effective acid pump inhibitor acting at the final enzymatic step of the acid secretory pathway of the parietal cell, decreasing gastric acid secretion regardless of the primary stimulus. Results of short term (less than 8 weeks) clinical trials have shown lansoprazole to be significantly superior to placebo and ranitidine in the treatment of duodenal ulcer, both in the rate of healing and in overall healing at 4 weeks. Lansoprazole appears to heal duodenal ulcer more quickly than famotidine, and demonstrates slightly greater efficacy at 4 weeks, although both drugs appear to have equivalent efficacy overall. Gastric ulcers and reflux oesophagitis are also healed by lansoprazole 30 mg/day for 4 to 8 weeks, with healing rates after 8 weeks of approximately 85 to 95% for both indications. Lansoprazole appears to be superior to ranitidine and comparable to omeprazole in treating reflux oesophagitis. Furthermore, lansoprazole has relieved reflux symptoms more quickly than either ranitidine or omeprazole. Preliminary data also indicate that lansoprazole may be effective in the treatment of peptic ulcer disease and reflux oesophagitis refractory to H2-receptor antagonists, and in patients with Zollinger-Ellison syndrome. While direct comparisons with omeprazole are limited, results suggest that lansoprazole, used for short term treatment, is at least as effective as omeprazole in the treatment of peptic ulcer and reflux oesphagitis. Lansoprazole has been well tolerated in short term clinical trials, with an incidence of adverse effects comparable with that of other agents in its therapeutic class. Trials assessing long term tolerability data are ongoing and will be required as part of the assessment of the safety profile, if lansoprazole is to be used prophylactically to prevent ulcer recurrence. Thus, by virtue of its ability to heal ulcers and rapidly relieve associated symptomatology, lansoprazole represents a useful alternative for the treatment of acid related disorders.

Intramolecular Nonbonded S...N Interaction in Rabeprazole

“…4. The generation of 8e, 8f, 9, and cystine definitely suggest that sodium rabeprazole (1) also inhibits the gastric (H ϩ -K ϩ )-ATPase in the action mechanism reported previously, [18][19][20] and the same intramoleculer nonbonded S · · · N interactions will also exist in the other inhibitors of the gastric (H ϩ -K ϩ )-ATPase such as lansoprazole 24) and omeprazole. 25) In conclusion, the intramoleculer nonbonded S · · · N interactions in the crystal structures of rabeplazole derivatives 7a-d and the intermolecular nonbonded S · · · N interaction between ethylmethylsulfoxide S and N of the pyridine moiety in a solution were recognized.…”

Determination of lansoprazole and two of its metabolites by liquid–liquid extraction and automated column-switching high-performance liquid chromatography: application to measuring CYP2C19 activity

“…Lansoprazole is effective in the treatment of various peptic diseases, including gastric and duodenal ulcer and reflux esophagitis, Zollinger-Ellison syndrome [2]. A combination of clarithromycin and amoxycillin with lansoprazole has proven to be highly effective in the eradication of H. pylori [3].…”

A New Synthetic Process of Lansoprazole

“…The aqueous layer was extracted with dichloromethane and the organic layer was washed with brine and dried over Na2SO4. Evaporation of the solvent afforded 250 mg of pure 7 (97%): 1 …”