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Structure, moa,uses of any 2 PPIs. MOA - PPIs are taken orally and absorbed into the bloodstream. ¯ The PPIs are transported to the stomach, where they are activated by gastric acid. ¯ The activated PPIs bind covalently to the H+/K+ ATPase proton pump on the surface of parietal cells. ¯ This binding prevents the proton pump from functioning, preventing the secretion of acid into the stomach. ¯ The PPI-bound proton pump complex is eventually degraded, but the PPI remains attached. ¯ This means that the proton pump cannot be repaired or replaced , and acid secretion remains inhibited until new proton pumps are synthesized. Omeprazole Peptic Ulcer GERD Zollinger-Ellison syndrome NSAID induced Acidity Pantoprazole Erosive esophagitis (caused by GERD) Prevention of Stomach ulcer NSAID induced Acidity Lansoprazole Peptic Ulcer GERD Zollinger-Ellison syn
Describe structure, moa, uses of H1 and H2 antagonist (any2) . (5mark) H2 antagonist MOA - (a) Gastrin stimulates the release of histamine from Enterochromaffin like Cell. (b) Then Histamine binds with H2 Receptor of Gastric Parietal cell (c) Binding of Histamine to H2 receptor increases the intracellular cyclic AMP and activates Protein Kinase A (d) PKA stimulates the release of Gastric acid by the H + /K + ATPase pump (proton pump). (e) Competitively and reversibly blocking the H2 receptor we can supress the release of Gastric Acid secretion induced by Histamine. Drugs Structure Uses Cimetidine Heartburn GERD Stomach and Duodenal ulcer Ranitidine Zollinger-Ellison Syndrome Gastroesophageal Reflex Disease Peptic Ulcer Famotidine Zollinger-Ellison Syndrome GERD Heartburn
General structural features of 1st gen. H1 antagonist. Structure moa, uses of chlorpheniramine maleate, promethazine hydrochloride , doxylamine succinate . General Structure of H1 Antagonists Aryl group: The diaryl substitution is essential for significant H1-receptor affinity. The optimal antihistaminic activity depends upon the co-planarity of two aryl substitutions . Nature of ‘X’: The X-connecting moiety of H1-antihistamines may be a simple carbon chain or saturated carbon-oxygen moiety, which serves as a spacer group for the required pharmacophore . Alkyl chain (The carbon chain): The carbon chain consists of two or three atoms in H1-antihistamines . Terminal Nitrogen : This is a basic, terminal amine functional group . Contains small alkyl substituting. Promethazine USES - Allergic reaction, Motion sickness Insomnia, Cough, Nausea chlorpheniramine maleate USES- symptoms of allergic reactions; over-the-counter products f
Outline the synthesis of promethazine. Structure, moa, uses of 1st gen. (Any 2) and 2nd gen. H1 antagonist (any 2) (10 mark) Synthesis of Promethazine H1 Antagonist (1st gen) (a) Chlorpheniramine Malate Uses- symptoms of allergic reactions; over-the-counter products for cold; depression, nausea and vomiting, motion sickness, and vertigo. (b) Diphenhydramine Uses: Allergic reaction, Motion sickness; Insomnia, Cough, Nausea H1 Antagonists (2nd Gen) (a) Cetirizine USES: Allergic Rhinitis; Chronic hives (b) Loratadine Uses : Allergic Rhinitis; Chronic hives Mechanism of Action