5-HT/Migraine

Question 1

• rapidly metabolized by MAO and stored, 90% found in enterochromaffin cells of GI treact
• stored in platelets and serotonergic nerve endings
• concentration in vesicles blocked by reserpine

Answer 1

serotonin (5-hydroxytryptamine)

Question 2

-5-HT3 receptors in GI tract and medulla produce the ______ reflex

Answer 2

vomiting

Question 3

5-HT2 stimulates platelet _______

Answer 3

activation

Question 4

• serotonin receptor on GI tract that stimulates smooth muscle
• increased tone, facilitation of peristalsis

Answer 4

5-HT2

Question 5

• serotonin receptor on GI tract that increases acetylcholine from nervous system
• prokinetic effect

Answer 5

5-HT4

Question 6

carcinoid syndrome in GI tract produces ______

Answer 6

diarrhea

Question 7

• 5HT1a partial agonist

- non benzodiazepine anxiolytic

Answer 7

buspirone

Question 8

• 5-HT2c agonist
• appetite suppression
• withdrawn due to toxicity

Answer 8

dexfenfluramine

Question 9

• inhibit release of vasodilating peptide CGRP
• constrict cerebral and meningeal vessels in treatment of acute migraine headaches
• adverse: tingling, warm sensations, muscle weakness, neck pain, chest discomfort

Answer 9

-triptans (5-HT1b/1d agonist)

Question 10

-5HT4 agonist used for treatment of GERD and motility disorders

Answer 10

cisapride

Question 11

-partial 5HT4 agonist, utilized for IBS with constipation

Answer 11

tegaserod

Question 12

• long acting 5-HT2 antagonist

- also alpha adrenergic antagonist

Answer 12

phenoxybenzamine

Question 13

• 5HT2 antagonist and H1 receptor antagonist
• useful for smooth muscle effects of carcinoid tumors
• serotonin syndrome treatment

Answer 13

cyprohepatidine

Question 14

• 5HT3 receptor antagonists

- treatment of nausea and vomiting in cancer chemo

Answer 14

-setrons

ondansetron, granisetron, dolasetron

Question 15

• HTN, hyperreflexia, tremor, clonus, hyperthermia, hyperactive bowel sounds, diarrhea, mydriasis, agitation, coma
• precipitating drugs: SSRIs, 2nd gen antidepressants, MAOIs, linezolid, tramadol, meperidine, fentanyl, ondansetron, sumatriptan, MDMA, LSD, St Johns Wort, ginseng

Answer 15

Serotonin syndrome

Question 16

• catecholamine and serotonin like

- admin with caffeine increases absorptin

Answer 16

ergot alkaloids

Question 17

• selectivity for dopamine receptors

- ergot alkaloids that suppress prolactin secretion, treat pituitary tumor

Answer 17

bromocriptine, cabergoline

Question 18

ergot alkaloid that’s a potent vasoconstrictor in vascular smooth muscle

Answer 18

ergotamine

Question 19

limited 5-HT effects, but preferred for treatment of migraine, an ergot alkaloid

Answer 19

dihydroergotamine

Question 20

• most selective ergot alkaloid for the uterus, stimulate smooth muscle
• if oxytocin fails, is utilized to limit postpartum hemorrhage

Answer 20

ergonovine

Question 21

• side effects: GI disturbances n/v/d due to increased GI motility resulting from activation of 5-HT receptors in CNS and GI
• prolonged vasospasm in arms and legs, may cause gangrene
• drowsiness and hallucinations occur infrequently

Answer 21

toxicity of ergot alkaloids

Question 22

• episodic attacks of headache lasting 4-72 hours
• two of following: unilateral pain, pain moderate to severe, throbbing, aggravation on movement
• one or more: nausea, vomiting, photophobia, phonophobia

Answer 22

migraine

Question 23

ergotamine, dihydroergotamine, triptans are _______ migraine drugs

Answer 23

specific

Question 24

• which beta blockers used in preventive therapy of migraine?
• adverse: tiredness, postural, contra in asthma

Answer 24

propanolol (b1, b2)

metoprolol (b1)

Question 25

antidepressant used in preventive migraine therapy? adverse - drowsiness

Answer 25

amitriptyline

Question 26

- anticonvulsants used in preventive therapy of migraine | - adverse: drowsiness, weight gain, tremor, hair loss, liver abnormality

Answer 26

valproate, topiramate

Question 27

calcium channel blockers used in preventive therapy of migraine? -adverse: tiredness, weight gain, depression, parkinsonism

Answer 27

flunarizine, verapamil

Question 28

- serotonin antagonist used in preventive therapy of migraine? - drowsiness, leg cramps, hair loss, retroorbital fibrosis

Answer 28

methysergide

Question 29

SSRI used in preventive therapy of migraine? | -adverse: anxiety, insomnia

Answer 29

fluoxetine

Question 30

NSAIDS are non specific therapy for treatment of ______ migraine attacks

Answer 30

acute

Question 31

analgesic overuse can _______ migraine, limit drug treatment to 2-3 days

Answer 31

transform

Question 32

- meperidine, butophanol, oxycodone, hydromorphone - relief for severe migraine, risk of dependence and tolerance - rebound headaches, dizziniess, n/v, cognitive function - risk of transforming migraine

Answer 32

opiate analgesics

Question 33

- metoclopramide - chlorpormazine - prochlorperazine

Answer 33

antiemetics, treat acute migraines

Question 34

- adjunctive therapy to combat n/v due to migraine and alkloid treatment - centrally acting dopaming receptor antagonists

Answer 34

antiemetics - metoclopramide, chlorpromazine, prochlorperazine

Question 35

- weak 5-HT3 receptor antagonist | - anti-emetic

Answer 35

metoclopramine

Question 36

- migraine specific therapy - vascoconstriction due to stimulation of alpha-adrenergic and 5-HT3 receptors - cerebral vasoconstriction has been attributed to partial agonist effects on neuronal 5-HT1d receptors

Answer 36

ergotamine, dihydroergotamine

Question 37

- effective, low cost - adverse: complex, variable absorption, potent and sustained vasoconstrictive effect --> increased risk of vascular effects

Answer 37

ergot derivatives

Question 38

- selective 5-HT1d and 1b receptor agonists - distinctive advantages: selective pharm, established efficacy - higher cost and restrictions in presence of CV disease - inhibit activation of trigeminal afferent nociceptors, cranial vasoconstriction

Answer 38

-triptans

Question 39

- mimic angina - contraindications - ischemic heart disease, HTN, cerebrovascular disease - tingling, sensation of warmth, dizzy, flushing, neck pain, stiffness

Answer 39

triptans