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Pharmacology
Migraine
29
Medical
Graduate
10/09/2009

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Term
Migraine pathogenesis
Definition
abnormal activation of trigemminal sensory nerve; assoc w. large release of inflam mediators
Term
What serotonergic receptor is involved in tx of migraine?
Definition
5HT1B/D
Term
Mechanism of action: serotonergic agonist in migraines
Definition
1. reduce release of inflamm peptides by nerve endings (by activating 5HT1B/D which are present on nerve endings of cranial sensorry afferents) -> reducing activation of nociceptive fibers
2. reduce vessel wall stretch and prodxn of inflamm substances (constriction of meningeal vessels and reduces extravasation)
Term
Mechanism of action: NSAIDs in migraine
Definition
work centrally and may reduce sensitizing effects of PGs on trigemminal nerve endings
Term
Drugs with the suffix "-triptan" are used to tx what?
Definition
migraines (structurally related to serotonin)
Term
Sumatriptan is what kind of drug?
Definition
serotonergic agonist of 5HT1B/1D/1F receptors
Term
Mechanism of action: sumatriptan
Definition
1. activates inhib presyn R's on CN V sensory n.-> reduced release of inflamm mediators & reduc their excitability
2. activates 5HT1 in CN V nucleus -> reduced synaptic transmission inter CN V nonciceptives and 2nd order neurons
3. 5HT1 act. in central pain pathways
4. 5HT1 act. in cerebral conductance vessels
Term
side effect: sumatriptan
Definition
coronary circulation may be adversely affected; avoid in CAD or printzmetal angina
Term
route of admin: sumatriptan
Definition
oral, sc or IN for faster action
Term
elimination: sumatriptan
Definition
80% hepatic, 20% renal
Term
what types of drugs are triptans incompatible with?
Definition
SSRIs and MAOIs
Term
Mechanism of action: ergotamine (what receptors are involved?)
Definition
partial agonist activity at serotonergic, dopaminergic and adrenergic receptors
Term
Side effects: ergotamines
Definition
DA receptor agonist -> emesis
5HT2/alpha1 Rs -> peripheral vasoconstriction (gangrene, thrombosis) and uterine contractions
Term
Dependence: Ergotamines
Definition
yes
Term
Route of adminis: ergotamines
Definition
sublingually or suppository as it has very low and erratic oral bioavailability
Term
Which migraine med is administered as a nasal spray?
Definition
dihydroergotamine
Term
What kinds of ppl should not take erogtamines?
Definition
pregnant, peripher vasc dz, HT, ischemic HD, renal or hepatic dz
Term
Mechanism of action in tx of migraines: Metclopramide
Definition
tx prominent sx of migraines: emesis by acting as a prokinetic
Term
role of butalbital in tx of migraines
Definition
a barbituate that can be used in mixture as a sedative with an ANALGESIC (aspirin) and CAFFEINE
Term
draw back of using butalbital in tx migraines
Definition
barbituate dependence
Term
Combination analgesics are generally made of what 3 types of meds?
Definition
a SEDATIVE + ANALGESIC + Vasoconscritor
Term
How can propanolol & timolo be used in migraine tx?
Definition
as prophylaxis (mechanism of protective effect is not known)
Term
How can amitryptyline and nortryptyline be used in migraine tx?
Definition
prophylaxis (unknown mechanism)
Term
what kind of drug is valproate? what's it's role in migraine tx?
Definition
anticonvulsant; prophylaxis
Term
what kind of drug is topiramate? what's it's role in migraine tx?
Definition
anticonvulsant, prophylaxis
Term
what kind of drug is gabapentin? what's it's role in migraine tx?
Definition
anticonvulsant; prophylaxis
Term
what kind of drug is methysergide? what's it's role in migraine tx?
Definition
semisynthetic ergot derivative; 3rd line drug in tx. of migraines
Term
mechanism of action in migraine: methysergide
Definition
although it's a 5HT R antagonist; it's activity in migraine may be due to a metabolite that has agonist activity at serotonergic/a1 receptors
Term
why is methysergide a 3rd ling drug in tx of migraine?
Definition
serious inflamm fibrosis of the lung, heart, or peritoneal cavity can occur
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