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This Concept Map, created with IHMC CmapTools, has information related to: Autacoids, Anti-Migraines, Autacoid Drugs Histamine Acute poisoning-CNS actions DANGEROUS Children: CNS excitation ->convulsions->coma, hallucinations, resp depression, death -like atropine poisoning –fixed dilated pupils, flushing, fever Adults:Excitation preceded by drowsiness, coma Thus, depression-excitation-depression Treatment Generally supportive Physostigmine to counter CNS anti-chol actions, Autacoid Drugs Histamine H1 receptor antagonists-1st gen- PO, IV DIPHENHYDRAMINE(Benadryl) -pre-surgical sedation -anti-cholinergic-dry mouth, etc. -physostigmine can counter CHLORPHENIRAMINE-PO, IV -less sedation-use for allergies phenothiazines, piperazines -dist'd to CNS->sedation -can be exploited for sedation -also prevents N/V, cough motion sickness, vertigo ADRs-excitement in KIDS -histamine release in HIGH concen ALL H1 ANTAGONISTS -alkylamine group like histamine -COMPETITIVE antag Pharmacokinetics-met'd by CYP-3A4 -erythromycin, ketocon->torsades, Autacoid Drugs Ergot Alkaloids ERGOTAMINE Oxytocic effects- -uterus at term is sensitive -control post-partum hemorrh, Autacoid Drugs Eicosanoids Derived from Arachidonic Acid All short-lived, locally-acting, Autacoid Drugs Ergot Alkaloids ERGOTAMINE ADRs GI - smooth muscle ->Cramps, N/V/D CTZ stimulation->Emesis Arteriospastic effects -paresthesias, cold limbs, claudication -angina Muscle weakness Hypersensitivity – localized edema/itching toxic effects acute arterial occlusion->gangrene (cannot be reversed) CNS – confusion, hallucinations, Autacoid Drugs Eicosanoids PGE1 ALPROSTADIL (PGE1) -infants w/ congen HD -keeps ductus arteriosus patent -ED-injection/cream for erection MISOPROSTAL (PGE1 analogue) -anti-ulcer -abortifacient, Autacoid Drugs Serotonin 5-HT agonists BUSPIRONE-5-HT1A agonist -for anxiety, depression SUMATRIPTAN-abort migraines tegaserod, cisapride-5-HT4 agonist ->GI motility -for IBS w/ constipation -cispride off mkt-prolong QT int -was also for GERD, Autacoid Drugs Eicosanoids PGE2 - oxytocic DINOPROSTONE-induce labor -cervical ripening -evaculate uterine contents CARBOPROST (synthetic) -abortifacient -control postpartum bleeding latanoprost-glaucoma eye drops -inc'd aq humor outflow, Autacoid Drugs Endothelin-1 BOSENTAN -ET_A, ET_B antagonist ->treat PAH (decreases pulm resistance), Autacoid Drugs Histamine H2 receptor antagonists -competitive CIMETADINE-OTC -peptic ulcer dz -Zollinger-Ellison Syn, Autacoid Drugs Ergot Alkaloids ERGOTAMINE Poorly absorbed-high molec wt Met'd in liver Admin: oral, intranasal, subling, Autacoid Drugs Serotonin Physiology: In periph: ->plt aggregation ->stim GI motility ->vasoconstriction CNS: inhibitory ->mood, appetite, sleep, emotions, pain processing mostly G-receptor-coupled -BUT 5-HT3 is ligand-gated 90% body 5-HT in enterochroms, Autacoid Drugs Endothelin-1 Physiological opposite of NO -via ET_A, ET_B receptors ->constriction -esp in pulm aa HTN ->cardiac dysfcn on reperfusion, Autacoid Drugs Ergot Alkaloids ERGOTAMINE 5-HT1D/1B effects ->vasoconstriction -decrease dilation per pulse in migraine -for orthostatic HTN -induce coronary aa spasm -control post-partum bleeding ADR: abortion -partial agonist, Autacoid Drugs Histamine H1 receptors-PLC->IP3, DAG-coupled ALLERGY and inflammation Tissue growth, wound healing, keloid and scar formation Urticaria Cough reflex, vasodilation, inc perm Bronchoconstriction, GI contraction H2 receptors-G protein->A. cyclase ->cAMP Allergy and inflammation Gastric acid, other gland secretion Increase HR, contractility (little) H3 receptors-presynaptic G protein Activate presynaptic receptors-> ↓ Hist, other NT release Nerve Endings ->pain (dermis), pruritus (epi), Autacoid Drugs Serotonin 5-HT_3 antagonists ONDANSETRON- -antiemetic effects, Autacoid Drugs Histamine Physiology:-in mast cells -released by: Chemicals causing dmg (bile salts, detergents, venoms) Sunburn, ionizing radiation Organic Bases (I.V.)-morphine, curare, some ABX Polypeps: C3a, C5a, somatostatin, substance P, dextran, venoms ->exocytosis Allergens (IgE-coupled), Autacoid Drugs Serotonin SSRIs -antidepressants -other CNS d/os, Autacoid Drugs Eicosanoids PGI2-Prostacyclin -made by endothelia EPOPROSTANOL-IV -Tx pulm aa HTN (dilate vessels), Autacoid Drugs Histamine Uses: Common cold, emesis, hypnosis Parkinsonism Petit mal seizures Local anesthesia