Lafutidine is a second-generation, potent, and long-acting histamine H2-receptor antagonist (H2RA) used primarily for the treatment of gastroesophageal reflux disease (GERD) and peptic ulcer disease. It is distinguished from other H2RAs by its unique mucosal protective properties, including capsaicin-sensitive afferent neuron stimulation and increased gastric mucosal blood flow, which promote ulcer healing and mucosal defense. It is effective in both acid suppression and mucosal protection.
Adult: 10mg once daily, usually after the evening meal or at bedtime. For active ulcers/GERD, treatment duration is typically 4-8 weeks.
Note: Swallow the tablet whole with a glass of water. Can be taken with or without food, but taking it after the evening meal is often recommended for optimal control of nocturnal acid breakthrough. Do not crush or chew.
Lafutidine exerts a dual mechanism of action: 1) Competitive and reversible inhibition of histamine at the H2 receptors of gastric parietal cells, leading to a significant reduction in basal and stimulated gastric acid secretion. 2) A unique gastroprotective effect mediated by stimulating capsaicin-sensitive sensory neurons in the gastric mucosa. This releases calcitonin gene-related peptide (CGRP) and nitric oxide (NO), leading to increased gastric mucosal blood flow, mucus secretion, and bicarbonate production, thereby enhancing mucosal defense and promoting healing.
Pregnancy: Category B2 (Australian Category). Animal studies have not shown teratogenicity, but no adequate and well-controlled studies in pregnant women. Use only if potential benefit justifies potential risk to the fetus.
Driving: May cause dizziness or visual disturbances. Patients should not drive or operate machinery if they experience these effects.
| Ketoconazole, Itraconazole | Reduced absorption of these drugs due to increased gastric pH. Separate administration by at least 2 hours. | Moderate |
| Atazanavir, Rilpivirine (HIV Protease/NNRTI Inhibitors) | Significantly reduced plasma concentration, leading to loss of virologic response. Contraindicated. | Major |
| Warfarin | Potential for altered INR; monitor coagulation parameters closely. | Moderate |
| Midazolam (oral) | Increased bioavailability and effect of midazolam due to CYP3A4 inhibition by Lafutidine. Monitor for excessive sedation. | Moderate |
| Sucralfate | May decrease absorption of Lafutidine. Administer Lafutidine at least 2 hours before sucralfate. | Minor |
| Antacids | No significant interaction, but may be taken separately if desired. | Minor |