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This document discusses H2 receptor antagonists, which are drugs used to treat ulcers. It describes how excess acid secretion in the stomach can damage the mucus membrane and cause ulcers. H2 receptor antagonists work by blocking histamine from binding to H2 receptors on parietal cells, which inhibits gastric acid production. The document traces the development of H2 receptor antagonists from early compounds like burimamide and metiamide to more widely used drugs like cimetidine, ranitidine, and famotidine. It also introduces proton pump inhibitors, which directly inhibit the H+/K+ ATPase pump to block acid secretion. Common uses of H2 antagonists and proton pump inhibitors are described for treating
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This document discusses histamine receptors and their antagonists. It begins with an introduction to histamine and its physiological effects. It then describes the three main histamine receptor subtypes (H1, H2, H3) and their locations in the body. The document focuses on H1 and H2 receptor antagonists, classifying and providing examples of different types of antihistamines. It discusses the mechanisms of action and structure-activity relationships of H1 receptor antagonists like mepyramine and H2 receptor antagonists like ranitidine and cimetidine. References are provided at the end.
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H2 antagonists are drugs that block the release of histamine by binding to H2 receptors in the stomach. This inhibits acid secretion and is used to treat peptic ulcers and gastric disorders like heartburn. Examples include cimetidine, ranitidine, and famotidine. They work by competitively blocking H2 receptors in parietal cells of the stomach, which suppresses both basal and stimulated acid secretion in a dose-dependent manner.
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The H2 receptor antagonists are reversible competitive blockers of histamine at the H2 receptors, particularly those in the gastric parietal cells, where they inhibit acid secretion. They are highly selective, do not affect the H1 receptors, and are not anticholinergic agents.
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This document discusses various drugs used to treat gastric acid-related disorders. It describes antacids that neutralize acid in the stomach, including aluminum and magnesium compounds, calcium carbonate, and sodium bicarbonate. It also discusses H2 receptor antagonists, proton pump inhibitors, and other drugs that reduce acid secretion. The document provides details on the mechanisms of action, pharmacokinetics, therapeutic uses and potential side effects of these different drug classes.
Gastrointestinal drugs
This document discusses various drugs used to treat gastrointestinal conditions related to acid production and regulation in the stomach. It begins by describing the anatomy and cells of the gastric gland responsible for acid and enzyme secretion. It then discusses acid-related diseases like ulcers and reflux and describes various classes of acid-controlling drugs including antacids, H2 receptor antagonists, and proton pump inhibitors. For each drug class, it provides details on mechanisms of action, indications, side effects, drug interactions and nursing implications.
L8 DRUGS EFFECTING GIT.pptx
This document summarizes drugs used to treat gastrointestinal disorders including peptic ulcers, gastroesophageal reflux disease, chemotherapy-induced nausea and vomiting, and diarrhea or constipation. It describes classes of drugs like H2 receptor antagonists, proton pump inhibitors, antacids, cytoprotective agents, antiemetics, antimotility agents, and laxatives. It provides details on specific drugs, their mechanisms of action, indications, and side effects for treating various GI conditions.
نموذج شرائح .pptx
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This document discusses drugs used to treat gastrointestinal tract conditions. It begins by introducing peptic ulcers and gastroesophageal reflux disease. It then discusses the aggressive and protective factors involved in these conditions. The document outlines how drugs like antacids, H2 blockers, and proton pump inhibitors work to neutralize or decrease stomach acid production. It provides details on the mechanisms, indications, side effects and nursing considerations for various classes of gastrointestinal drugs including antacids, H2 blockers, proton pump inhibitors, sucralfate, and misoprostol.
Drugs Acting on the GI Tract Peptic Ulcer
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Group 5_ Year 3 Pharmacology 2023.pptx
This document discusses acid secretion disorder drugs and anti-emetic drugs. It begins by explaining the physiology of gastric acid secretion, which is regulated by gastrin, histamine, and acetylcholine. It then discusses acid secretion disorders like GERD, gastritis, and ulcers. The main drugs used for acid secretion disorders are outlined, including antacids, H2 receptor antagonists like ranitidine, and proton pump inhibitors like omeprazole. It provides details on their mechanisms of action, pharmacokinetics, uses and side effects. The document also briefly discusses anti-emetic drugs and the physiology of vomiting before concluding.
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- 1. UNIT-1 H2 ANTAGONIST LECTURE BY DR. JASMINE CHAUDHARY ASSOCIATE PROFESSOR
- 2. INTRODUCTION Also known as antiulcer and antisecretory. Approximately 2 L of acid is secreted by parietal cells in stomach in form of hydrochloric acid. This acid is helpful in killing bacteria and also aid in digestion by solubilizing food. Substances that stimulate acid secretion are Acetylcholine, Histamine, gastrin etc. and substance that regulate or inhibit acid secretion is somatostatin.
- 3. Excessive HCl secretion leads to damage of mucus membrane leading to ulcer. Ulcer is also caused by micro-organism Helicobacter pyroli and by frequent uses of NSAIDs. Therefore inhibition of gastric secretion is one of the therapeutic target for treatment of ulcer disease.
- 4. Strategies for treatment of ulcers 1. Antacids (Aluminium and magnesium hydroxide gel). 2. Targeting muscarinic receptor with muscarinic antagonist like dicyclomine. 3. H2 receptor antagonist (Cimetidine, ranitidine) 4. Antimicrobial therapy in combination with antisecretory drugs for H. pyroli infections 5. Mucosal protective agents: Sucraflate 6. Proton pump inhibitors: Omeprazole
- 5. H2 RECEPTOR ANTAGONISTS Block histamine to bind to H2 receptor and thus antagonise its action. The prototype of this class was Guanyl histamine which was partial agonist. Modifications in its structure leads to discovery of first selective H2 antagonist Burimamide but it was having very poor oral absorption. To improve oral absorption methyl group was introduced on imidazole ring and sulphur is introduced in side chain leading to discovery of Metiamide but it causes kidney damage
- 6. H2 RECEPTOR ANTAGONISTS To reduce this side effect, thione group was replaced by cyanoimino group giving Cimetidine. Cimetidine was the first potent H2 antagonist devoid of this side effect (kidney damage). Later it was investigated that whether imidazole ring is essential for activity or not so derivatives with other heterocyclic ring were synthesized and it was observed that imidazole ring is not essential for activity. Two new potent compounds (Ranitidine and Famotidine) having more activity than cimetidine were discovered.
- 7. Ranitidine consists of furan ring instead of imidazole ring and is five time more potent than cimetidine. Famotidine consists of thiazole ring and is 20 times more potent than cimetidine.
- 8. Burimamide (Poor oral absorption) Metiamide (Kidney damage) Cimetidine Ranitidine Famotidine
- 9. H2 antagonists are highly polar and don’t cross BBB therefore, don’t cause sedation as side effect. The first brain penetrating H2 blocker is Zolantidine.
- 10. MODE OF ACTION
- 11. MODE OF ACTION On parietal cells, 3 receptors are found to mediate HCl secretion. Cholinergic agonist/ Acetyl choline binds to muscarinic receptor Gastrin binds to gastrin receptor Histamine binds to histamine receptor In parietal cells, carbonic acid is produced from CO2 and water which gets hydrolysed to H+ ions and HCO3- ions with help of enzyme carbonic anhydrase (CA)
- 12. H+ ions are exchanged with K+ ions through H+/K+ ATPase pump. HCO3- ions are exchanged with Cl- ions (from Cl- channels) Both H+ ions and Cl- ions combines to form HCl. H2 antagonist block histamine to bind to receptor therefore inhibiting release of gastric acid.
- 13. Uses In treatment of peptic ulcer. In Heart burn Dyspepsia In Zollinger Ellison syndrome (pathological hypersecretory state due to tumors in small intestine resulting in excessive production of acid. Side Effects Hypotension Headache Tiredness Diarrhea/ Constipation
- 14. PROTON PUMP INHIBITORS Drugs which directly inhibitin H+/K+ ATPase pump and thus inhibit HCl release are called proton pump inhibitors. Examples include Omeprazole, Pantoprazole, Rabeprazole, Lansoprazole
- 16. USES To treat symptoms of gastroesophageal reflux disease (GERD) and other conditions caused by excess stomach acid. It is also used to promote healing of erosive esophagitis (damage to esophagus caused by stomach acid). Omeprazole may also be given together with antibiotics to treat gastric ulcer caused by infection with Helicobacter pylori (H. pylori). In heart burns also. Side effects include headache, dizziness, nausea, gas, bloating.