| Flap 1 |
Flap 2 |
| 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 |
