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Flashcards in Migraine Meds Deck (27):

Which serotonin receptors vasodilate?

• Serotonin 2 (5 HT-2) . Low levels


Which serotonin receptors mediate vasoconstriction?

• Serotonin 1 (5 HT-1) . High levels


Propranolol/ Inderal


Class: Non-selective Beta blocker
• Indication: Hypertension, angina, AMI,
panic attacks and migraine headache • MOA: Blocks adrenergic stimulation which serves to decrease heart rate and myocardial oxygen demand and also decreases renin release.
• Char: P.O., 10 to 100 mg per day. Non- selective beta blockade with potential for bronchoconstriction via antagonism of Beta 2 receptors in bronchi.


Propranolol/ Inderal SE

• Side effects: Bronchoconstriction, hypotension, bradycardia, fatigue, impotence. Abrupt discontinuation may cause rebound hypertension and tachycardia with subsequent increase in myocardial oxygen demand. Abrupt discontinuation increases the risk of arrythmias, stroke, angina and M.I.


Amitriptyline/ Elavil


• Class: Tricyclic antidepressant (TCA)
• Indication: migraine/ tension headache,
chronic pain, bipolar disorder and
• MOA: CNS modulation of both serotonin
and norepinephrine.
• Char: PO and IM. Usually taken at
bedtime to minimize side effects of drowsiness and dizziness.


Amitriptyline/ Elavil SE

• Side effects: Dizziness and marked drowsiness. Anticholinergic effects such as dry mouth, constipation, urinary hesitancy and blurred vision. Do not use with monoamine oxidase (MAO) inhibitors. The full benefits of Amitriptyline may take days to several weeks to be observed whereas side effects are usually noted within first several days.


Topiramate/ Topamax


• Class: Anticonvulsant
• Indication: Anticonvulsant approved for
use in treating epilepsy and prophylaxis of migraine headaches. Off-label use for bipolar disorder.
• MOA: Block voltage-dependent sodium channels in the CNS, augmenting the activity of the neurotransmitter gamma- amino butyrate (GABA) at some subtypes of the GABA-A receptor. MOA as a migraine medication is not fully known.
Char: PO tablets. Also available in capsules which are designed to be opened to deliver in a sprinkle form for pediatric patients.

**also for weight loss/seizures


Topiramate/ Topamax SE

• Side effects; Fatigue, dizziness, vision changes, acute angle glaucoma, nausea and constipation.


Migraine prophylaxis

• Beta blockers:
Propanolol/ Inderal
Metopralol/ Lopressor

• Calcium channel blockers
Verapamil/ Isoptin

• Tricyclic antidepressants
Amitriptyline/ Elavil
Nortyptylene/ Aventyl

• Ergotamines
Methysergide/ Sansert
Dihydroergotamine/ Migranal

• Anti-seizure medications
Gabapentin/ Neurontin Valproic acid/ Depakote Topiramate/ Topamax


Methysergide/ Sansert


• Class: Ergot derivative – serotonin 2 receptor antagonist.
• Indication: Prophylaxis of migraine and cluster headache
• MOA: MOA not fully known, yet it appears to be a Serotonin 2 receptor antagonist which results in vasoconstrictor effect.
Char: PO. Should never be used beyond ~6 months without a drug free interval. Dosage must be tapered to avoid rebound. Do not use within 24 hrs of a triptan because of increased risk of vasoconstrictive spasm.



pathological syndromes affecting humans or animals that have ingested plant material containing ergot alkaloid, such as ergot- contaminated grains.

The common name for ergotism is "St. Anthony's Fire",
symptoms: severe burning sensations in the limbs, sometimes leading to gangrene and loss of limbs due to severely restricted blood circulation.

These are caused by effects of ergot alkaloids on the vascular system due to vasoconstriction of blood vessels,


Methysergide/ Sansert

• Side effects: Multiple potential side effects make methysergide a less attractive choice then newer treatment options.
These side effects include but are not limited to hypertension, thrombophlebitis, nausea and vomiting. Pulmonary fibrosis and retroperitoneal fibrosis are severe and potentially life threatening occurrences.

Side effects: Heart valve thickening has also been reported.

Contraindicated in pregnancy (Category X) and in patients with peripheral vascular disease.

• Methysergide is usually reserved for cases refractive to other medications and treatment modalities.


Prodromal phase medications

• Triptans
Sumatriptan /Imitrex
Zolmitriptan /Zomig
Eletriptan /Relpax
Naratriptan / Amerge
Rizatriptan /Maxalt
Almotriptan /Axert


Sumatriptan/ Imitrex


• Class: Serotonin agonist
• Indication: Migraine and cluster headache
• MOA: Serotonin agonist at 5-HT 1D and
1B receptors, found in small, peripheral nerves that innervate the intracranial vasculature.
• Char: PO/SQ/Nasal spray. Effectively aborts or markedly reduces the severity of migraines in majority of migraine patients. Onset of action between 10 and 60 minutes. Maximum of 2 doses in 24 hours!!!
Sumatriptan is structurally similar to serotonin (5HT), and is a 5-HT (types 5-HT1D and 5-HT1B agonist. The specific receptor subtypes it activates are present on the cranial arteries and veins. Acting as an agonist at these receptors, Sumatriptan reduces the vascular inflammation associated with migraine.


Sumatriptan/ Imitrex SE

• Side effects: Dizziness, tingling, facial flushing, weakness, chest tightness or pain, arrythmias and hypertension. Use with caution in patients with high blood pressure and in patients with angina.
• Category C in that no adequate and well controlled studies have been done in humans but should be used cautiously, if at all, during pregnancy.

others in this cat:Zomig, Amerge, Maxalt


Serotonin syndrome

an uncommon potential side effect of all of the triptans.

Symptoms of serotonin syndrome may include:
agitation, tremor, ataxia, fever, chills and diarrhea.

• Frequent use of triptans (daily basis) can result in rebound headaches. Maximum dose generally 2 to 3 doses in a 24 hour period and no more then 12 to 18 doses per month!!!.


Pain phase medications

• Aspirin*
• NSAIDs i.e. Ibuprofen
• Acetaminophen/ Tylenol*
• Tylenol with codeine
• Hydrocodone/ Vicodin
• Butorphanol/ Stadol

***caffeine added-vasoconstriction


Ibuprofen/ Motrin, Advil

• Class: NSAID
• Indication: Inflammation, pain, fever
• MOA: Reversible inhibition of COX-1 and COX-2 enzymes. Anti-inflammatory and analgesic effect largely due to blockade of prostaglandin synthesis at target tissues.
• Char: PO, PR. No increased risk for Reye’s syndrome has been noted.


Opiate/ Narcotic analgesics

• Codeine – T#3, T#4
• Hydrocodone – Vicodin
• Morphine sulfate - MS Contin
• Meperidine - Demerol
• Hydromorphone - Dilaudid
• Fentanyl - Duragesic
• Oxycodone - Oxycontin, Percodan, Percocet
• Butorphanol/ Stadol



• Class: Opioid analgesic
• Indication: Pain relief, antitussive
• MOA: Opioid agonist, much weaker analgesic then morphine.
• Char: PO, IV, IM, SQ, - Lower abuse potential. Effective antitussive – codeine is able to suppress cough at doses which are lower then a typical analgesic dose.
• Side effects: Sedation, constipation.


Butorphanol/ Stadol

• Class: Opiod analgesic
• Indication: Migraine headache that is refractory to triptans and to other agents as well as less potent analgesics. Butorphanol may also used in other acute pain conditions.
• MOA: Mixed agonist-antagonist of opiod receptors.
Char: Nasal spray, IM. Usually dosed as 1 spray in 1 nostril every 3 to 5 hours as needed for control of severe pain. Marked dependency potential exists.

also cluster headaches


Butorphanol/ Stadol SE

• Side effects: Nasal irritation, drowsiness, dysphoria, nausea and vomiting. Because of the mixed agonist-antagonist properties of Butorphanol, withdrawal symptoms can be precipitated in patients with underlying addiction to opiates.

highly addictive


Anti-emetic antihistamines include:

Diphenhydramine (Benadryl),
Prochlorperazine (Compazine),
Promethazine (Phenergan)
Hydroxyzine (Vistaril),
• All of these drugs may be given PO/ PR/
and IV.


Prochlorperazine/ Compazine

• Class: Typical neuroleptic
• Indication: Anti-emetic particularly when
associated with migraine headaches, vertigo,
• MOA: Primarily H1-histamine receptor
antagonist. Also a D2 dopaminergic receptor antagonist and an alpha-adrenergic receptor antagonist.
• Char: PO, PR, IM and IV. Often causes drowsiness.


Prochlorperazine/ Compazine SE

• Side effects: Drowsiness, dry mouth, constipation and urinary retention. Lowers seizure threshold. Extrapyramidal side effects generally seen only when Prochlorperazine is given at high doses over long periods of time.


Ondansetron/ Zofran

• Category: Antiemetic
• MOA: Blockade of serotonin (5HT3) receptor
sites results in signifigant anti-nausea effect.
• Indication: Severe nausea
• Char: PO, IV. Effective agent for severe
• Side effects: Dizziness, headache. Generally
well tolerated.


Additional treatment options

• Riboflavin (vitamin B2) 400 mg/ day
• Magnesium 600 mg to 2000 mg/ day
• Biofeedback
• Acupuncture
• Botulinum toxin (Botox) injection has shown promise as a therapeutic agent.