title: Actions of cimetidine and ranitidine at some cholinergic sites: implications in toxicology and anesthesia.
abstract: Cimetidine and ranitidine are specific and potent H2-receptor antagonists widely used in the effective therapy of peptic ulcer disease. The drugs also possess other pharmacological properties unrelated to H2-receptor antagonism. More recently large experimental doses of cimetidine or ranitidine were found to have anticholinesterase, ganglion blocking and neuromuscular blocking activities. Actions of the drugs at such cholinergic sites may account for some of their clinically documented adverse effects. The toxicological implications of these findings including the potential for drug interactions to occur, especially during some anesthetic procedures, are discussed.
mesh_terms: D000758:Anesthesia; D000818:Animals; D000959:Antihypertensive Agents / Q000009:adverse effects; D001919:Bradycardia / Q000139:chemically induced; D002800:Cholinesterase Inhibitors / Q000494:pharmacology; D002927:Cimetidine / Q000009:adverse effects* / Q000494:pharmacology / Q000627:therapeutic use; D003221:Confusion / Q000139:chemically induced; D003577:Cytochrome P-450 Enzyme System / Q000494:pharmacology; D003967:Diarrhea / Q000139:chemically induced; D004347:Drug Interactions; D007172:Erectile Dysfunction / Q000139:chemically induced; D005730:Ganglionic Blockers / Q000494:pharmacology; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D008297:Male; D006899:Mixed Function Oxygenases / Q000037:antagonists & inhibitors; D009466:Neuromuscular Blocking Agents / Q000494:pharmacology; D010437:Peptic Ulcer / Q000188:drug therapy; D011899:Ranitidine / Q000009:adverse effects* / Q000494:pharmacology / Q000627:therapeutic use; D011950:Receptors, Cholinergic / Q000187:drug effects* / Q000502:physiology; D011970:Receptors, Histamine H2 / Q000187:drug effects; D015043:Zollinger-Ellison Syndrome / Q000188:drug therapy
chemical_list: D000959:Antihypertensive Agents; D002800:Cholinesterase Inhibitors; D005730:Ganglionic Blockers; D009466:Neuromuscular Blocking Agents; D011950:Receptors, Cholinergic; D011970:Receptors, Histamine H2; D002927:Cimetidine; D011899:Ranitidine; D003577:Cytochrome P-450 Enzyme System; D006899:Mixed Function Oxygenases