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H2 Receptor Blockers These drugs have completely changed the management of acid peptic disorders. General effects of these drugs are a marked reduction in stomach acid production in response to meals and other stimuli is observed. Usually ulcers heal with adequate doses and there is no disturbance of the bowel activity. Any of the four drugs given below produce healing in 4 to 8 weeks when adequate doses are taken to suppress acid by 70% (in 24 hours). The doses used, and the preparations available are shown in the table: Adverse Effects (Mostly with cimetidine): The drugs especially cimetidine may cause headache, bowel upset, dry mouth, dizziness or skin rash. Confusion, dilirium, fits and heart rhythm changes occur when used intravenously. Enlargement of male breast, loss of sex desire, impotence and temporary disease in sperm counts may occur with use of cimetidine. White cell count (polymorphs) falls on longer use of cimetidine. H2 blockers or proton pump inhibitors produce healing of ulcers easily in almost 80% to 100% cases. But as soon as they are stopped recurrence occurs. Therefore, continuous use in low doses or longer time (duration is uncertain, may be 1 to 2 years) for acid suppression is needed. To cure the ulcer, one needs to identify the presence of H Pylori and use 1 to 2 week eradication regimes, and acid suppression may be done in H pylori negative cases only. Drug Interaction (Mostly with cimetidine) Toxicity of theophylline, phenytoin, anti-diabetic drugs, nifedipine, quinidine, propranolol, warfarin is increased because cimetidine decreases their metabolic inactivation by liver. Antacids reduse absorption of H2 blockers and thus they should be taken after a gap of 2 to 3 hours. Because of these interactions cimetidine is not a popular drug. Anti-Cholinergic Drugs Pirenzepine and telezepine are two drugs which reduce volume of stomach juice without much adverse effects caused by other anticholinergic drugs. These have limited role in the management of peptic ulcer because they decrease the activity of stomach. The acid stays in the stomach for a longer time and may cause damage to ulcerated surface. Systemic side effects such as dry mouth, constipation and urinary retention may occur in the elderly. Inhibitors of Acid Pump: Omeprazole (Lomac, Lokit, Omezac, Omez, Omezol, Protoloc) It is the single largest selling drug in the world. This inhibits the so-called proton pump situated in the secretory cells of the stomach. Thus, the final phase of acid secretion is inhibited by this drug. It is more potent and longer acting than histamine blockers. A dose of 20 to 40mg acts for more than 24 hours and produces complete inhibition of acid secretion. The ulcer heals within 2 to 4 weeks, that is, twice as fast as with ranitidine. The healing rate is almost 100%. Its profound and long-lasting effect may make it a drug of choice in peptic ulcers and reflux esophagitis. It inhibits H pylori organism also and therefore it is used along with other antibiotics for eradication of H pylori. It is also available in combination with domperidone for the treatment of reflux esophagitis (heart burn). Dosage: A 20 to 40 mg per day dose is given before breakfast. Adverse Effects: It causes infrequent adverse effects like nausea, diarrhoea, pain in the abdomen, dizziness, headache and skin rash. These are generally mild and do not requir reduction in dosages. It reduces disposal of diazepam, phenytoin and warfarin from the body and therefore at times dose adjustments of these drugs need to be done.
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