GASTROESOPHAGEAL REFLUX The desired actions of H2 antagonists include the following: AND ULCER These drugs are used in the following conditions: ● Short-term treatment of active duodenal ulcer or benign gastric ulcer. DISEASE ● Selectively block H2 receptors located on the parietal cells. DISEASE ● Prevents the release of gastrin, a hormone that causes local release of ● Treatment of pathological hypersecretory conditions such as Zollinger–Ellison syndrome histamine (due to stimulation of histamine receptors), ultimately blocking ● Prophylaxis of stress-induced ulcers and acute upper GI bleeding in critical the production of hydrochloric acid. patients HISTAMINE-2 ● Decreases pepsin production by the chief cells. ● Treatment of erosive gastroesophageal reflux Pharmacokinetics: ● Relief of symptoms of heartburn, acid indigestion, and sour stomach. ANTAGONISTS Cimetidine, ranitidine, and famotidine are available in oral and parenteral forms. Adverse Effects: Nizatidine is available only in oral form. Cimetidine was the first drug in this class to be developed. The adverse effects most commonly associated with H2 antagonists include the following: ● Gatrointestinal system (GI) effects of diarrhea or constipation. Contraindication and Cautions: ● Central Nervous System (CNS) effects of dizziness, headache, The contraindications and cautions when using H2 antagonists include: somnolence, confusion, or even hallucinations. ● Allergy. The H2 antagonists should not be used with known allergy to ● Cardiovascular System (CS) effects of cardiac arrhythmias and any drugs of this class to prevent hypersensitivity reactions. hypotension ● Pregnancy or lactation. Caution should be used during pregnancy or ● Reproductive System (RS) effects of Impotence. lactation because of the potential for adverse effects on the fetus or ● Misc: gynecomastia (more common with long-term use of cimetidine) nursing baby. ● Hepatic or renal dysfunction. Caution should be used in patients with hepatic or renal dysfunction, which could interfere with drug metabolism and excretion.
Antacids ● Prolonged or continual use. Care should also be taken if prolonged or
continual use of these drugs is necessary because they may be masking serious underlying conditions.