Pharmocology-Autonomics1.2/serotonin

Question	Answer
how many receptor subtypes exist?	seven, receptors interrelated and many have may functions
actions of 5HT?	GI motility, contraction of sm muscle (bronchi, uterus), vascular constriction (direct) and dialation (endoth dep), platlet aggregation, stimulate nociceptive nerve endings, excite/inhibit CNS
pathologic roles of 5HT in periphery?	peristalsis, vomiting, platlet aggregation and hemostasis, inflammatory mediator, nociceptor sensitization, microvascular control
roles of 5HT in CNS?	appetite, sleep, mood hallucinations, stereotyped behavior, pain perception, vomiting
clinical conditions associated with 5HT?	GI disorders, migraine, carcinoid syndrome, mood disorders, anxiety
mechanisms for altering amount of seretonin?	1.altered tryptophan in diet, tyryptophan hydroxylase inhibitor 2.deplete 5HT storage sites(amphetamines and reserpine) 3.inhibit presynaptic reuptake (antidepressants, SSRIs) 4.MAO inhibition
what are the seretonin receptor agonists?	LSD, mCPP, buspirone, sumatriptan, ergotamine (PA/antagonist), metoclopramide, cisapride
what is LSD?	nonselective, ergot derivative that alters human behavoir at low doses (hallucinations, psychosis)and sleep
what is mCPP?	nonselective, active metabolite of trazodone (antidepressant), anxiety is a symptom, elevates cortisol, GH, and prolactin secretion
what is bispirone?	partial agonist, anxiolytic (can't perscribe if IHD)
what is sumatriptan used for?	used for migriane tx
what is metoclopramide and cisapride?	GI prokinetic agent
what are seretonin receptor antagonists?	ketanserin, Ergot alkaloids, clozapine, risperidone(respiradol), cyproheptadine(periactin), ondansetron, graisetron, tropisetron
what are ergot alkaloids?	nonselective antagonists, also affecting DA and histamine receptors. They include ergotamine, ergometrine, methysergide
ergotamine: 5HT receptor? alpha receptor? DA receptor? uterine contraction? use? side effects?	5HT PA/ANT, alpha PA, DA inactive, some uterine contraction, use: migraine, side effects: emesis and vasoconstriction
Ergometrine: 5HT receptor? alpha receptor? DA receptor? uterine contraction? use? side effects?	5HT PA/ANT, alpha weak ANT/PA, DA weak, uterine contration, use: prevent pp hem, no side effects
methysergide: 5HT receptor? alpha receptor? DA receptor? uterine contraction? use? side effects?	5HT PA/ANT, no alpha DA or uterine contration, use: migraine (proph), side effects: emesis
what is clozapine (clozaril)?	"atypical" antipsychotic with reduced extrapyramidal side effects. high DA receptor affinity
what is risperidal?	5HT antagonist and D2 antagonist effects
what is periactin used for?	used to treat sexual side effects of SSRI's and postgastrectomy dumping syndrome, migraine prophylaxis, carcinoid syndrome. commonly used as an antihistamine. Side effects: anticholinergic, weight gain
what are ondansetron, granisetron, and tropisetron used for?	anti-emetic drugs block receptors
how are 5HT modulators used to tx emesis?	vagal afferents sending info from gut to vomiting center of brain, receptors in the chemoreceptor trigger zone
what agents used to tx emesis?	5HT3 antagonists: ondansetron, granisetron
how are 5HT modulators used to tx migraine?	receptors in BV of carotid circulation, trigeminal nerve that innervate circulation. stimulation cause direct/indirect vasoconstriction via inhibit release of 5HT and vasoactive peptides from trigeminal N.
what agents used to tx acute migraine?	5HT1 agonists: sumatriptan, xolitriptam, rizatriptan, naratriptan (acute migraine w/ or w/o aura and cluster HA, not prophylaxis, not for CV disease b/c vasospasm)
what agents used for migraine prophylaxis?	methysergide (blocks in periphery, weak vasoconstrictor, stimulate in CNS)
what are agents used to tx psychosis?	5HT2 antagonists: olanzapine, quetipine, clozapine, respiridone (schitzophrenia, acute psychosis, aggression in alzheimers)
what agents used to tx anxiety?	partial agonists: bispirone to decrease seritonergic effects in the brain
traditional antidepressants for depression?	nonselective, increase NE and serotonin by inhibiting reuptake or reducing metabolism
name some SSRI's:	reuptake inhibitor: fluoxetine, sertraline, paroxetine
what are SSRI's used for?	major depression, OCD, premenstrual syndrome, anorexia nervosa, PTSD
how do you treat obesity?	5HT2 receptors. sibutramine inhibits reuptake of serotonin, NE, and DA. increase in 5HT increases feelings of satiation, and increase in NE increases metabolic rate. Does NOT stimulate NE release, as with amphetamines

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