Pharmcology of Migraine Headache Flashcards
Effective medications for the management of many acute migraine attacks
Simple Analgesics and NSAIDs
An option when migraine-associated nausea and vomiting are severe
Suppository preparations of simple analgesics and NSAIDs
Analgesics that have demonstrated the most consistent evidence of efficacy include
Acetominophen and acetominophen/aspirin/caffeine (excedrin migraine)
NSAIDS that have demonstrated the most consistent evidence of efficacy include
Aspirin, Ibuprofen, Naproxen, and Diclofenac
Appear to prevent neurogenically-mediated inflammation in the trigeminovascular system by inhibiting cyclooxygenase (COX)-mediated prostaglandin synthesis
Analgesics and NSAIDs
Should be avoided or used cautiously in patients with previous ulcer disease, renal disease, or hypersensitivity to aspirin
Analgesics and NSAIDs
Migraine-specific medications, and their introduction represented a major advance in migraine pharmacotherapy
Seratonin receptor agonists (triptans)
They are appropriate first-line therapy for patients with mild-to-severe migraine, and are used for rescue therapy when non-specific medications (e.g., analgesics and NSAIDS) are ineffective
Triptans
The different triptans differ primarily with regard to pharmacokinetics and pharmacodynamics. Slower onset of action and reduced efficacy are seen with
Frovatriptan and Naratriptan
That said, frovatriptan and naratriptan also have the longest half-lives and therefore less
Headache recurrence
Selective agonists at serotonin 5-HT1B and 5-HT1D receptors
Triptans
Relief of migraine is the result of three key actions:
1) Normalization of dilated intracranial arteries through enhanced vasoconstriction.
2) Inhibition of vasoactive peptide release from perivascular trigeminal neurons.
3) Inhibition of transmission through second-order neurons ascending to the thalamus
Triptans
What are some of the mild adverse effects of Triptans?
Paresthesias, dizziness, fatigue, and flushing
Up to 25% of patients receiving triptans report tightness, pressure, heaviness, or pain in the
Chest, neck, or throat
The triptans are partial agonists at 5-HT coronary artery receptors, and are therefore contraindicated in patients with a history of
Ischemic heart disease, uncontrolled hypertension, and cerebrovascular disease
The triptans should not be given to patients receiving
SSRIs or SNRIs
Can be considered for the treatment of moderate-to severe migraine attacks
-Their use, however, is limited by issues of efficacy and side effects
Ergotamine tartrate and dihydroergotamine
Ergotamine is available in oral, sublingual, and rectal preparations, with dihydroergotamine being available for
Intranasal and parenteral administration
Non-selective agonists at serotonin 5-HT1 receptors.
-Cause constriction of intracranial blood vessels and inhibit the development of neurogenic inflammation in the trigeminovascular system
Ergot Alkaloids and Derivatives (Ergotamine tartrate and dihydroergotamine)
Central inhibition of the trigeminovascular pathway has also been reported with
Ergot Alkaloids and Derivatives (Ergotamine tartrate and dihydroergotamine)
Among the most common adverse effects to Ergotamine tartrate and dihydroergotamine
Nausea and vomiting
Contraindicated in patients with renal or hepatic failure; coronary, cerebral, or peripheral vascular disease; uncontrolled hypertension, and sepsis
Ergotamine tartrate and dihydroergotamine
Ergotamine tartrate and dihydroergotamine are also contraindicated in women who are
Pregnant or nursing
Among the most widely used drugs for migraine prophylaxis
B-Adrenergic antagonists (B-blockers)
B-Blockers with established efficacy in migraine prophylaxis include:
Metoprolol, Propanolol, and Timolol
Although not first-line treatment for hypertension or anxiety, may be useful along with other therapy in patients with comorbid hypertension or angina
B-blockers
Adverse effects can include drowsiness, fatigue, sleep disturbances, vivid dreams, memory disturbance, depression, impotence, bradycardia, and hypotension
B-blockers
B-blockers should be used with caution in patients with
CHF or peripheral vascular disease
Antidepressants with established efficacy in migraine prophylaxis include the:
- ) Tricyclic Antidepressant
- ) SNRI
- ) Amitriptyline
2. ) Venlafaxine
May be particularly useful in patients with comorbid depression or insomnia
Antidepressants
Thought to be related to downregulation of central 5-HT2 receptors, increased levels of synaptic norepinephrine, and enhanced endogenous opioid receptor actions
Antidepressants
Anticholinergic side effects are common with
-Limit the use of this agent in patients with benign prostatic hyperplasia and glaucoma
Amitriptyline
Most common adverse effects with venlafaxine are
Nausea, vomitting, and drowsiness
Have emerged as important therapeutic options for migraine prophylaxis, with valproate (Depakene®), divalproex (Depakote®), and topiramate (Topamax®) having established efficacy
Anticonvulsants
May be particularly useful in patients with comorbid seizure disorder or bipolar illness
Anticonvulsants
The most extensively studied medication for migraine prophylaxis
Topiramate (anticonvulsant)
The benefits of topiramate are observed as early as two weeks after initiation of therapy, with significant reductions in migraine frequency within the
Month
Thought to function via enhancement of GABA mediated inhibition, modulation of glutamate, and inhibition of Na+ and Ca2+ channel activity
Anticonvulsants
Nausea and vomiting are the most common side effects of
-These effects are self-limited and are less common with titration of doses
Valproate and Divalproate
The most serious side effect of valproate therapy is
Hepatotoxicity
Contraindicated in pregnant women (potential for teratogenicity) and patients with a history of pancreatitis or chronic liver disease
Valproate
Paresthesia is the most common adverse effect of
Topiramate
Should be used with caution or avoided in patients with a history of kidney stones or cognitive impairment
Topiramate
Useful for the prevention of migraine headaches that occur in a predictable pattern, such as menstrual migraine
NSAIDs and triptans
