Clinical pharmacology of antisecretory drugs. Focus on H2-histamine receptor blockers

Abstract

The purpose of the review is to illuminate the physiology of hydrochloric acid secretion and the clinical pharmacology of H2-histamine receptor blockers, also known as H2-histamine receptor antagonists, H2-histamine blockers, and H2-blockers.The main provisions. Antagonists of H2-histamine receptors (cimetidine, ranitidine, famotidine, nizatidine, lafutidin) selectively block the histamine receptors of parietal cells, preventing the activation of acid secretion by histamine secreted by enterochromaffin-like cells of the stomach. When using the means of this pharmacological group, both the total amount of gastric juice and its acidity decrease. H2-histamine blockers are rapidly absorbed after oral administration and for a long time inhibit the basal and stimulated acidity of the gastric mucosa. This class of drugs is approved by the FDA for short-term use in the treatment of uncomplicated gastroesophageal reflux disease, peptic ulcer or duodenal ulcer, hypersecretion of the stomach and mild infrequent heartburn. Off-label H2-histamine receptor blockers can also be used to prevent stress ulcers, esophagitis, gastritis, and gastrointestinal bleeding. Sometimes H2-histamine blockers are included in the Helicobacter pylori eradication regimen. Due to their safety, H2-histamine blockers are sold over the counter. However, they are gradually replaced by even more effective drugs - inhibitors of H+,K+-ATPase (PPI).Conclusion. H2-histamine receptor antagonists inhibit basal, nocturnal and stimulated secretion. Despite the presence of powerful antisecretory drugs in the doctor’s arsenal, such as proton pump inhibitors, H2-histamine blockers have not lost their importance in clinical practice. The knowledge of the clinical pharmacology of H2-histamine receptor blockers allows a competent approach to the choice of a treatment strategy and monitoring the safety and effectiveness of treatment of patients with acid-dependent diseases.