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endogenous made from tryptophan neurotransmitter widely found in nature |
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Platelets uptake 5-HT and store it in secretory granules. Platelet aggregation triggers 5-HT release and vasoconstriction |
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Carcinoid tumor and serotonin |
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psychotic behaviors may result from tumors of the enterochromaffin cells that excrete high amounts of 5-HT into circulation |
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Five members expressed by neurons in the CNS G protein coupled receptors Inhibit adenylate cyclase regulate ion channels inhibit neuronal 5-HT release |
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G protein coupled Activate PL-c Increase intracellular calcium brain, gut, and platelets |
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Methysergide ketanserin cyproheptadine |
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ligand gated ion channels Cause cell depolarization brain, GI tract, spurs emetic response |
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GProtein coupled activate adenylate cyclase CNS and GI tract mediate secretion and peristalsis |
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e.g. Sumatriptan used for acute treatment of migraine, not prophylaxis contra in patients with CV, brain dz Raise serotonin levels SQ dosing to avoid nausea/vomit |
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serotonin excess that is fatal SSRI + 'triptans cognitive + autonomic dysfunctions |
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e.g. methysergide used prophylactically for migraines but not a first line tx long term therapy not good; metabolite is psychidelic, inflammatory fibrosis |
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e.g. ondansetron treat nausea, but not motion sickness Side effects: constipation |
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e.g. metoclopramide, mosapride prokinetic, upper GI emptying treats GERD and IBS relieves GI dysmotility syndromes anti-dopaminergic effect |
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