Headache Deck 2 Flashcards
Drugs for Headaches
Serotonin Agonist Drugs (The Triptans) Ergot Alkaloids Aspirin-like Drugs Miscellaneous Drugs: Medications for prophylaxis Antiepileptic drugs Tricyclic antidepressants Calcium channel blockers Beta-blocker
Sumatriptan [Imitrex]
Mechanism of action
Binds to receptors on intracranial blood vessels and causes vasoconstriction
Diminishes perivascular inflammation
Sumatriptan [Imitrex] - therapeutic use
Aborting an ongoing migraine attack to relieve headache and associated symptoms
Prompt treatment of migraine attacks - important to successful acute therapy.
Sumatriptan [Imitrex] - administration
Oral or intranasal administration (dependent on the preparation).
Sumatriptan - ADR
Adverse effects
Chest symptoms
Transient “heavy arms” or “chest pressure” experienced by 50% of users
Coronary vasospasm
Rare angina as a result of vasospasm
Teratogenesis
Others - vertigo, malaise, fatigue, and tingling sensations
Sumatriptan has a
Very bad taste when taken in intranasal form
Drug interactions - ergot alkaloids, sumatriptan, and other triptans (all cause
Drug interactions - ergot alkaloids, sumatriptan, and other triptans (all cause vasoconstriction)
All triptans should be limited to
All triptans should be limited to no more than 10 days of use per month to avoid medication overuse headache.
Triptans should be avoided in patients with
Triptans should be avoided in patients with hemiplegic migraine, basilar migraine, ischemic stroke, ischemic heart disease, Prinzmetal’s angina, uncontrolled hypertension, and pregnancy
Triptans with NSAIDs - effective than using
Triptans with NSAIDs - effective than using
Eletriptan is primarily metabolized by cytochrome P-450 enzyme CYP3A4.
Should not be used within
at least 72 hours of treatment with other drugs that are potent CYP3A4 inhibitors such as ketoconazole, itraconazole, nefazodone, troleandomycin, clarithromycin, ritonavir, and nelfinavir.
Serotonin syndrome in patients who
who use triptans in combination with a selective serotonin reuptake inhibitor (SSRI) or a selective serotonin-norepinephrine reuptake inhibitor (SNRI) - low to non-existent - discuss risk and benefits and s/s of serotonin syndrome.
Intravenous (IV) metoclopramide, and IV or intramuscular (IM) chlorpromazine and prochlorperazine can be used as
Intravenous (IV) metoclopramide, and IV or intramuscular (IM) chlorpromazine and prochlorperazine can be used as
These medications act as antiemetics mainly because they are
dopamine receptor antagonists.
In contrast to IV or IM preparations, oral antiemetics should not be
considered as monotherapy in acute migraine
Antiemetics are commonly used as
adjunctive therapy to treat migraine
Opioid analgesics - when to use
Severe migraine – not responded to first-line medication.
Potential for abuse
Butorphanol nasal spray [Stadol NS]
Ergot MOA
MOA: complex action, precise mechanism is unknown
partial agonist and/or antagonist activity against tryptaminergic, dopaminergic and alpha-adrenergic receptors depending upon their site
Highly active uterine stimulant
Causes constriction of peripheral and cranial blood vessels and produces depression of central vasomotor centers
Ergot are
Second-line drug use
Ergot SE
well-tolerated – n/v in about 10%, weakness in legs, myalgia, numbness and tingling in the fingers and toes, angina-like pain, tachycardia or bradycardia
Ergotism
Ergot catuion
Caution in patients with CVD; pregnancy category X.
Diphydroergotamine (DHE) - MOA
Alpha-adrenergic blocker
Weaker arterial vasoconstrictor and more potent venoconstrictor than ergotamine tartrate
Potent 5-HT 1b/1d receptor agonist.
Fewer side effects than ergotamine
Does not cause the development of physical dependence or rebound headaches
Diphydroergotamine (DHE) CI
HTN or ischemic heart disease, in combination with MAO inhibitors, and older adults, use of CYP3A4 inhibitors
Preventative Medications
Beta blockers
Antiepileptic Drugs
Tricyclic antidepressants
Calcium Channel Blockers
Beta Blockers - are
First-line drugs for migraine prevention
Beta Blockers - propranolol
Propranolol - two divided doses starting at 40 mg daily; dose range 40 to 160 mg daily
Beta Blockers do not use as
Do not use as initial therapy in patients over 60 and in smokers.
Beta Blockers limiuted use in
Used cautiously as well in patients with asthma, diabetes mellitus, or depression, and in those with cardiac conduction disturbances or sinus node dysfunction
Beta Blockers used cautiously as
Used cautiously as well in patients with asthma, diabetes mellitus, or depression, and in those with cardiac conduction disturbances or sinus node dysfunction
Calcium-Channel Blockers - Are
Widely used
Calcium-Channel Blockers data support
Data support efficacy is limited
Calcium-Channel Blockers example
Verapamil - three divided doses starting at 120 mg daily, dose range 120 to 240 mg daily
Sodium valproate and topiramate – effective for
for migraine prevention; insufficient evidence to determine the effectiveness of gabapentin
Divalproex [Depakote ER]
MOA, SE, Warning, Interactions
MOA: unknown, likely increases GABA
SE: nausea, fatigue, weight gain, tremor, bone loss, reversible hair loss.
Black box warning – fatal pancreatitis and hepatitis. Pregnancy category x
Drug interactions: other anticonvulsants, ASA, antacids, psychotropics, H2 blockers, BZDs, warfarin
Topiramate [Topamax]
MOA, SE, Warning, Interactions
MOA: blocks sodium channels, enhances GABA in brain, reduces activity of calcium channels, blocks glutamate activity
SE are common: metabolic acidosis, moderate weight loss, paresthesias, fatigue, cognitive disinfection
Drug interactions: phenytoin and valproic acid, ethinyl estradiol, Digoxin, other CNS depressants.
Pregnancy category c, not to be used in lactation, pediatrics 2 to 16 approved for use
Amitriptyline [Elavil]
Prevent
migraine and tension-headaches
Amitriptyline - MOA
MOA: increases the synaptic concentration of serotonin and/or norepinephrine in the central nervous system by inhibition of their reuptake by the presynaptic neuronal membrane pump.
Amitriptyline SE
SE: hypotension and anticholinergic effects (drug mouth, constipation, urinary retention, blurred vision, tachycardia)
Amitriptyline excessive dose causes
dysrhythmias.
Additional Therapies
ACE inhibitors/ARBs Botulinum toxin Butterbur Coenzyme Q10 Feverfew Magnesium Melatonin Riboflavin Acupunture
