5-HT and migrane Flashcards
buspirone
5-HT1 partial agonist
Non-benzodiazepine anxiolytic
dexfenfluramine
5-HT2c agonist
Appetite suppression
Withdrawn due to toxicity
cisapride
5-HT4 agonist
Used for treatment of GERD and motility dissorders
almotriptan
selective 5-HT1d and 5-HT1b receptor agonist
oral
- 5-HT1b/1d agonists (sumatriptan)
- Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP)
- Constrict cerebral and meningeal vessels in treatment of actue migrane headaches
- Efficacy agasint migrane similar to other classes of drugs
- Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
eletriptan
selective 5-HT1d and 5-HT1b receptor agonist
oral
- 5-HT1b/1d agonists (sumatriptan)
- Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP)
- Constrict cerebral and meningeal vessels in treatment of actue migrane headaches
- Efficacy agasint migrane similar to other classes of drugs
- Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
frovatriptan
selective 5-HT1d and 5-HT1b receptor agonist
oral
- 5-HT1b/1d agonists (sumatriptan)
- Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP)
- Constrict cerebral and meningeal vessels in treatment of actue migrane headaches
- Efficacy agasint migrane similar to other classes of drugs
- Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
naratriptan
selective 5-HT1d and 5-HT1b receptor agonist
oral
- 5-HT1b/1d agonists (sumatriptan)
- Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP)
- Constrict cerebral and meningeal vessels in treatment of actue migrane headaches
- Efficacy agasint migrane similar to other classes of drugs
- Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
rizatriptan
selective 5-HT1d and 5-HT1b receptor agonist
oral
- 5-HT1b/1d agonists (sumatriptan)
- Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP)
- Constrict cerebral and meningeal vessels in treatment of actue migrane headaches
- Efficacy agasint migrane similar to other classes of drugs
- Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
sumatriptan
selective 5-HT1d and 5-HT1b receptor agonist
oral
- 5-HT1b/1d agonists (sumatriptan)
- Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP)
- Constrict cerebral and meningeal vessels in treatment of actue migrane headaches
- Efficacy agasint migrane similar to other classes of drugs
- Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
zolmitriptan
selective 5-HT1d and 5-HT1b receptor agonist
oral
- 5-HT1b/1d agonists (sumatriptan)
- Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP)
- Constrict cerebral and meningeal vessels in treatment of actue migrane headaches
- Efficacy agasint migrane similar to other classes of drugs
- Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
phenoxybenzamine
5-HT2 antagoinst
- Long acting 5-HT2 antagonists (+ alpha adrenergic receptors)
*
cyproheptadine
5-HT2 antagonist
- Cyprohepatidine
- 5-HT2 antagonist and H1 receptor antagonist
- Useful for the SM effects of carcinoid tumors
- Serotonin syndorme treatment
alosetron
5-HT3 receptor antagonist
treatment of IBS drug
ondansetron, granisetron, dolasetron
5-HT3 receptor antagonist
- Ondansetron, granisetron, dolasetron
- 5-HT3 receptor antagonists
- Treatment of nausea and vomiting in cancer chemo
dihydroergotamine
non selective 5-HT agonist
ergot derivative
taking with caffene may help absorption
Mechanism - vasoconstriction due to stimulation of alpha and 5-HT receptors
Disadvantages
Complex pharmacology/kinetics
Potent and sustained vasoconstrictor effects
Increased risk of vascular effects - contraindicated in patients with CAD
ergonovine
non selective 5-HT agonist
ergot derivative
taking with caffene may help absorption
Mechanism - vasoconstriction due to stimulation of alpha and 5-HT receptors
Disadvantages
Complex pharmacology/kinetics
Potent and sustained vasoconstrictor effects
Increased risk of vascular effects - contraindicated in patients with CAD
Ergonovine is the most selective for the uterus
If oxytocin fails, is utilized to limit post partum hemorrhage
ergotamine mixtures, ergotamine tartrate
non selective 5-HT agonist
- Taking with caffeine may help absorption
- Mechanism - vasoconstriction due to stimulation of alpha and 5-HT receptors
- Disadvantages
- Complex pharmacology/kinetics
- Potent and sustained vasoconstrictor effects
- Increased risk of vascular effects - contraindicated in patients with CAD
methylergonovine
non selective 5-HT agonist
- Taking with caffeine may help absorption
- Mechanism - vasoconstriction due to stimulation of alpha and 5-HT receptors
- Disadvantages
- Complex pharmacology/kinetics
- Potent and sustained vasoconstrictor effects
- Increased risk of vascular effects - contraindicated in patients with CAD
methysergide
non selective 5-HT agonist
serotonin antaboinsts
AE: drowsiness, leg cramp, hair loss, retrorbital fibrosis
lysergic acid diethylamine
LSD - non selective 5-HT agonist
no clinical use
ergotamine
non selective 5-HT agonist
Ergotamine: potent vasoconstrictor
ergocryptine
non selective 5-HT agonist
bronmocriptine
non selective 5-HT agonist
cabergoline
non selective 5-HT agonist
propranolol
B blocker - used in preventive therapy for migranes
metoprolol
B blocker - used in preventive therapy for migranes
amitriptyline
antidepressant - used in preventive threapy for migrane
drowsyness
divalproex
anticonvulsant - used in preventive threapy for migrane
weight gain, tremor, hari loss, hemotological and liver problems, teratogenicity
topiramate
anticonvusant - used in preventive threapy for migrane
weight gain, tremor, hari loss, hemotological and liver problems, teratogenicity
flunarizine
CCB - used in preventive threapy for migrane
tiredness, weight gain, depression ,parkinsonism
verapamil
CCB - used in preventive threapy for migrane
constipation, leg swelling, arterioventricular conduction disturbances
methysergide
serotonin antagonist - used in preventive threapy for migrane (withdrawn)
fluoxetine
prozac - SSRI - used in preventive threapy for migrane
anxiety, insomnia
metoclopramide
antiemetic - used in migrane acute attacks
Adjunctive therapy to combat nausea and vomiting due to migraine or ergot alkaloid treatment
Centrally acting dopamine receptor antagonists
chlorpromazine
antiemetic - used in migrane acute attacks
Adjunctive therapy to combat nausea and vomiting due to migraine or ergot alkaloid treatment
Centrally acting dopamine receptor antagonists
prochlorperazine
antiemetic - used in migrane acute attacks
Adjunctive therapy to combat nausea and vomiting due to migraine or ergot alkaloid treatment
Centrally acting dopamine receptor antagonists
NSAIDs
- used in migrane acute attacks
not selective for migranes - can have other probelms
- Non specific pain therapy
- Aspirin
- Naproxen, ibuprofen (NSAIDs)
- Acetaminophen
- Geneally poorly effects - can also get sensitized to the pain
meperidine
opiates
- used in migrane acute attacks
not selective for migranes - can have other probelms
- Meperidine, butophanol, oxycodone, hydromorphone
- AE
- Rebound headaches, dizziness, nausea, vomiting, impaired cognitive function, constipation
butorphanol
opiate
- used in migrane acute attacks
not selective for migranes - can have other probelms
- Meperidine, butophanol, oxycodone, hydromorphone
- AE
- Rebound headaches, dizziness, nausea, vomiting, impaired cognitive function, constipation
oxycodone
opiates
- used in migrane acute attacks
not selective for migranes - can have other probelms
- Meperidine, butophanol, oxycodone, hydromorphone
- AE
- Rebound headaches, dizziness, nausea, vomiting, impaired cognitive function, constipation
hydromorphone
opiate
- used in migrane acute attacks
not selective for migranes - can have other probelms
- Meperidine, butophanol, oxycodone, hydromorphone
- AE
- Rebound headaches, dizziness, nausea, vomiting, impaired cognitive function, constipation