5-HT and migrane COPY Flashcards
ondansetron, granisetron, dolasetron
5-HT3 receptor antagonist
- Ondansetron, granisetron, dolasetron
- 5-HT3 receptor antagonists
- Treatment of nausea and vomiting in cancer chemo
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)
divalproex
anticonvulsant - used in preventive threapy for migrane
weight gain, tremor, hari loss, hemotological and liver problems, teratogenicity
dexfenfluramine
5-HT2c agonist
Appetite suppression
Withdrawn due to toxicity
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
propranolol
B blocker - used in preventive therapy for migranes
metoprolol
B blocker - used in preventive therapy for migranes
cabergoline
non selective 5-HT agonist
lysergic acid diethylamine
LSD - non selective 5-HT agonist
no clinical use
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)
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
cisapride
5-HT4 agonist
Used for treatment of GERD and motility dissorders
bronmocriptine
non selective 5-HT agonist
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
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)
methysergide
non selective 5-HT agonist
serotonin antaboinsts
AE: drowsiness, leg cramp, hair loss, retrorbital fibrosis