Cohen: Headaches + Pharm Flashcards
Sumatriptan
“Imetrex” - Seratonin 5-HT Agonist
MOA: activates 5-HT receptor on presynaptic trigeminal nn. endings inhibiting release of vasodilating peptides;; stimulates vasoconstriction
– duration of use is often shorter than h/a
- given oral, nasal, subcu a couple hours after start of migraine
USE: ** first line ** tx of migraine attacks that are severe
ADR’s: mild - tingling, warmth, dizziness, mm. eakness, fatigue, flushing, nausea, sweating, neck pain
CI: CAD and cerebral vascular disease!
relative CI: angina, ischemic heart disease, HTN - d/t slight vasoconstriction
DDI: DO NOT USE w/in 24 hours of ergotamine which have severe vasoconstriction
Dihdroergotamine (DHE)
Ergot Alkaloids
MOA: constriction of peripheral and cranial blood vessels - may also affect peptide release and act as agonist at 5HT1 (act on agonists and antagonists on MANY different receptors, thus have more SE’s)
USE:
- migraines
- DHE used specifically for intracatible severe pain
Caution: vasoconstriction is long-lasting and cumulative when doses are repeated!
ADR’s: GI problems, prolonged vasospasm, gangrene, bowel infarction, severe vasoconstriction, weakness, fatigue, pareshtesias
CI: obstructive vascular diseases, collagen diseases, uncontrolled HTN, hepatic/renal dysfunction
Ergotamine
Ergot Alkaloids
MOA: constriction of peripheral and cranial blood vessels - works on multiple receptors other than 5HT1… may also affect peptide release and act as agonist at 5HT1 (act on agonists and antagonists on MANY different receptors, thus have more SE’s)
USE:
- migraines
Caution: vasoconstriction is long-lasting and cumulative when doses are repeated! can raise BP
ADR’s: GI problems, prolonged vasospasm, gangrene, bowel infarction, severe vasoconstriction, weakness, fatigue, pareshtesias
CI: obstructive vascular diseases, collagen diseases, uncontrolled HTN, hepatic/renal dysfunction
“analgesics”
- aspirin, acetaminophen, caffeine (excedrin)
- ibuprofen (advil)
analgesics: MOA: prevent neurogenic mediated inflamation in the trigeminovascular system through inhibition of PG synthesis
USE:
- common headaches - reasonable first choice for mid/moderate migraine attacks
ADR’s: ** GI problems **
- dyspepsia, nausea, vomiting, diarrhea
- somnolence, dizziness
CI: ulcer disease, renal dysfunction, hypersensitivity to aspirin
metoclopramide
= reglan - antiemetic
MOA: block D2 like dopamine receptors in the chemoreceptor trigger zone and solitary tract nucleus
USE: adjuncts for nausea/vomiting that accompany migraine h/a
- single dose given 15-30 mins prior to abortive therapy
ADRs: drowsinness, dizziness
propanolol
beta antagonist - migraine prophylaxis
MOA: may raise migraine threshold by modulating adrenergic/ serotenoergic NT in cortical and subcortical pathways
USE: most widely used drugs for migraine prophylaxis
ADRs: drowsiness, fatigue, sleep disturbances
CI: CHF, PVD, asthma, depression, DM
verapamil
CCB - migraine prophylaxis
MOA: inhibits Ca2+ entry from select voltage sensitive areas of vascular smooth mm. produces relaxation of vascular smooth mm. and vasodilation
use: migraine prophylaxis - off label use
amitriptyline
antidepressant - migraine prophylaxis
MOA: bneficial effects may result from down regulation of central 5HT2 receptors, increased levels of synaptic NE and enhanced opioid receptor actions
ADRs: sedating d/t being antidepressant, weight gain
topiramate
anticonvulsant - migraine prophylaxis
MOA: enhance GABA mediated inhibition, modulate excitatory NT glutamate, inhibit sodium and calcium ion channel activity
** particularly useful in pts. w/ migraines and comorbid seizures, anxiety disorders, or bipolar disorders **
ADRs: paresthesia, fatigue, anorexia, diarrhea, w/l, taste perversion
common vs. classic migraine?
classic = has aura which may involve nausea, scotomas, speech problems - aura followed by severe throbbing unilateral h/a
common = lacks aura phase
migraines:
- involve trigeminal nn. – nerves release peptides and promote vasodilation
migraine criteria **
> = 5 attacks lasting 4–72 hours
> = 2 of the following
Unilateral , Pulsating, Moderate or severe intensity , Aggravation by routine physical activity
> = 1 of the following
- Nausea and/or vomiting
- Photophobia and phonophobia (sensitive to light or sound)
No evidence on history or examination of disease that might cause headaches
when to do migraine prophylaxis?
for patients with 3+ migraines per month
Great! Amitriptyline, propanalol, topiramate
Fair: verapamil
- are only ones approved by FDA
tx of cluster h/a?
sumatriptan injection, high dose O2, nasal lidocaine
preventative: verapamil, lithium, prednisone
other options: deep brain stimulation or occipital nn. stimulator
tx of trigeminal neuralgia?
carbamazepine, may require radiological or surgical ablation as well
primary vs. secondary h/a?
Primary Headaches: No obvious pathological cause, but a well-known syndrome of headaches, such as migraine, tension-type, cluster, etc.
- migraine, tension, cluster h/a
Secondary Headache, or Headaches: A pathological cause can be found, such as tumor, hemorrhage, infection, etc.
–> warning signs: single h/a, sudden onset, onset after age 50, recent onset <6 mos, systemic disease (malignancy, AIDs), change in h/a pattern, abnormal neuro exam
