Pharmacology Mnemonics - Flash Cards

Name: Methysergide (Sansert)

Class: Anti-Migraine (Serotonin Agonist)

Mechanism: Partial agony at 5-HT₂ vascular receptors & partial agonist at a-adrenergic receptors (can act as a blocker) ® vasoconstriction (cerebral vasc. most sensitive), uterine smooth muscle contraction, n/v, diarrhea.

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Toxicity/S.E.s: Weight gain, peripheral edema, fibrosis (retroperitoneal, pleuropericardial, subendocardial). Concurrent use of ergot alkaloids, b adrenergic blockers, erythromycin, or dopamine ® ­ risk of arterial spasm & occlusion. Occasional central stim. & hallucinations.

Utility: Migraine prevention. Reserved for recurrent, refractory, severe migraine, as fibrosis is assoc. w/prolonged use.

Special Features: Relatively ineffective in treatment of impending/active migraines. Useful as a prophylactic.

Name: Dihydroergotamine

Class: Anti-Migraine (Serotonin Agonist)

Mechanism: Partial agony at 5-HT₂ vascular receptors & partial agonist at a-adrenergic receptors (can act as a blocker) ® vasoconstriction (cerebral vasc. most sensitive), uterine smooth muscle contraction, n/v, diarrhea.

Absorption: IV. Investigational use intranasally & orally.

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Toxicity/S.E.s: Most common = GI (n/v, diarrhea). Most dangerous = vasospasm from overuse/overdose (intense & prolonged, but can be blocked w/a blockers). Drowsiness.

Utility: Treat migraines.

Special Features: Lower direct smooth muscle, vasospasm, and serotonin effects and more selective a receptor blockade than ergotamine.

Name: Ergotamine

Class: Anti-Migraine (Serotonin Agonist)

Mechanism: Partial agony at 5-HT₂ vascular receptors & partial agonist at a-adrenergic receptors (can act as a blocker) ® vasoconstriction (cerebral vasc. most sensitive), uterine smooth muscle contraction, n/v, diarrhea.

Absorption: IV, IM, oral, sublingual, rectal, & inhaler.

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Toxicity/S.E.s: Most common = GI (n/v, diarrhea). Most dangerous = vasospasm from overuse/overdose (intense & prolonged, but can be blocked w/a blockers). Drowsiness.

Utility: Treat migraines.

Special Features: Most effective when given during prodrome period. Often combined w/caffeine to facilitate absorption.

Name: Sumatriptan (Imitrex)

Class: Anti-Migraine (Serotonin Agonist)

Mechanism: Stim 5-HT_1D receptors ® cranial vasoconstriction ® ­ resistance in carotid arteriovenous anastomoses and shunts w/minor effects on systemic and coronary artery vasculature.

Absorption: Subcut. (96% bioavailability) ® peak plasma conc. in 5-20 min. Response in 10-30 min; 10-13 hour duration. Oral (14% bioavailability) ® clinical response in 30-60 min.

Dist.:

Metabolism.: 80% Metabolism.

Excretion, t½: 2 hr.

Toxicity/S.E.s: Pain, swelling, redness at injection site. Feeling of heaviness, tightness in chest (injection). Neuro symptoms (tingling, warm/burning sensation). Rare vasospasm in patients w/coronary artery disease (® angina, MI). 34-46% headaches recur in 24-48 hr.

Utility: Partial/complete relief of migraine headache in 80% w/in 2 hr (subcut). Relieves n/v, photophobia, phonophobia.

Special Features: Oral effective, w/few side effects at lowest doses. Expensive.