migraine treatment (pharm exam 4) ================================= drug class/ indications moa toxicity/ side effects ----
Migraine Treatment (pharm exam 4)
=================================
DRUG
class/ indications
MOA
Toxicity/ side effects
----------------------
Special Considerations
A. Acute Migraine
1.Metaclopramide
(Reglan)
anti-emetic
Stim. muscarinic receptors (increases peristalis) / D2 rec. antagonist
extrapyramidal motor defects (Parkinson-like) -reversible
-avoid in children,
- may cause drowsiness, fatigue, restlessness, and insomnia
2. NSAIDS/ Acetaminophen
Analgesics
blocks neurogenic plasma protein extravasation and central processing
of trigeminal nociceptive input
GI effects (ulcers), overuse can induce med-related headaches
(rebound)
3. Ergotamin/ DHE - Dihydroergotamine
Complex – agonism, partial, and antagonism of 5HT, Adren, and DA rec.
N/V, “ergotism” – muscle cramps, paresthesias, angina, localized
edema, and peripheral ischemia b/c of vasoconstriction
-w/ Caffiene to INC. absorption (WIGRAINE) and metoclopramide b/c of
N/V
-Dependence (use less than 2x /wk. )
-rebound headaches
-Not for preg. women (ototoxic), CAD, PVD, or HTN
4. Triptans
triptan
5 HT receptor agonists
SE’s – burning sensation at injection site, tightness in chest, flush,
dizziness, tingling
-success 50-70% in 2 hrs.
-faster onset than DHE
-CORONARY VASOSPASM
-don’t use w/ergot or mao inh. or SSRI’s
a. Sumatriptan
prototype triptan
suppository, nasal, or sub Q
does not enter cns
b. zolmitriptan
triptan
enters cns, may work when sumatriptan doesn’t
c. Naratriptan
triptan
fewer side effects
enters cns, less effective
B. Preventative Therapy
1. Beta Blockers
Propanolol, Metoprolol
Beta -blockers
unclear but not related to CNS penetration or cardiac selectivity
-Contraindictions- Asthma, AV block, and diabetes
- fatigue, orthostatic hypotension, impotence
-efficacy up to 65%
-not for acute therapy
2. Valproic Acid
neuroleptic
?????
3. Methysergide
5HT rec. antagonist
Acts as 5HT antagonist in perifphery but as agonist in CNS
-may lead to fibrosis and should not be used more than 6 months (drug
holidays)
-reserved for pts. w/ cluster headaches or who don’t respond to
prohylactics
4. Aspirin and NSAIDs
reduce frequency by 20-40%
-long-term = GI problems
a. naproxen
NSAID
better established and nearly equal to serotonin antagonists
useful in prohpylaxis of menstrual migraine
5. Flunarizine
Ca antagonist
not approved in all countries (US)
effective but high risk of side effects
6. Verapamil
Ca antagonist
marginally effective
OTHERS
1.
DA antagonists (lisuride)
2.
TCAs (amytriptyline)
3.
Fever few (herbal)
poor efficacy and poorly controlled studeies