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Withdrawn due to toxicity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