Classifications: alpha-adrenergic antagonist; ergot alkaloid; Therapeutic: antimigraine
Pregnancy Category: X
2 mg sublingual tablets
Natural amino acid alkaloid of ergot. Alpha-adrenergic blocking agent with direct stimulating action on cranial and peripheral
vascular smooth muscles and depressant effect on central vasomotor centers. Ergotamine activity can damage vascular endothelium
with subsequent occlusion, thrombosis, and gangrene.
In vascular headache, exerts vasoconstrictive action on previously dilated cerebral vessels, reduces amplitude of arterial
pulsations, and antagonizes effects of serotonin.
As single agent or in combination with caffeine to prevent or abort migraine, cluster headache (histamine cephalalgia), and
other vascular headaches. Not recommended for migraine prophylaxis because of the possibility of adverse effects.
Hypersensitivity to ergotamine; sepsis, obliterative vascular disease, thromboembolic disease, prolonged use of excessive
dosage, liver and kidney disease, severe pruritus, diabetes mellitus; marked arteriosclerosis, history of MI, peripheral vascular
disease; coronary artery disease, angina; basilar/hemiplegic migraine; hepatic disease; biliary tract disease; cholestasis;
hypertension; infectious states, anemia, malnutrition; pregnancy (category X), use in children.
Lactation, older adult patients.
Route & Dosage
Adult: SL 12 mg followed by 12 mg q30min until headache abates or until max of 6 mg/24 h or 10 mg/wk
- Instruct patient to allow sublingual (SL) tablet to dissolve under tongue and not to drink, eat, or smoke while tablet is
in place. Do not crush SL tablets.
Adverse Effects (≥1%)Body as a Whole:
Paresthesias; pain (spasms) of facial muscles, tongue, limbs, and lumbar
region with difficulty in walking; muscle pains,
numbness, coldness and cyanosis of digits (Raynaud's phenomenon). CNS:
Delirium; convulsive seizures; confusion; depression; drowsiness. GI: Nausea; vomiting; diarrhea
; abdominal pain; unquenchable thirst; partial necrosis of tongue, disagreeable aftertaste. CV:
Rapid, weak, or irregular pulse; intermittent claudication, complete absence of medium- and large-vessel pulsations in extremities;
precordial distress and pain; angina pectoris, transient bradycardia or tachycardia; elevated or lowered BP. Skin:
Itching and cold skin; gangrene of nose, digits, ears. Urogenital:
Kidney failure. Other: Symptoms
With high doses of beta-adrenergic blockers
, possibility of additive vasoconstrictor effects; erythromycin, troleandomycin
may cause severe peripheral vasospasm. Eletriptan, naratriptan, rizatriptan, sumatriptan, or zolmitriptan
may increase risk of coronary ischemia, separate drugs by 24 h; azole antifungals (ketoconazole, itraconazole, fluconazole, clotrimazole), nefazodone, fluoxetine, fluvoxamine, amprenavir, delavirdine, efavirenz, indinavir, nelfinavir, ritonavir, and saquinavir,
may inhibit ergot metabolism
and increase toxicity
; sibutramine, dexfenfluramine, nefazodone, fluvoxamine
may increase risk of serotonin syndrome
. Food: Grapefruit juice
may increase toxicity
Variable absorption orally. Peak:
0.53 h. Distribution:
Crosses bloodbrain barrier. Metabolism:
Extensive first-pass metabolism
in liver. Elimination:
96% eliminated in feces; excreted in breast milk. Half-Life:
2.7 h initial phase, 21 h terminal phase.
Assessment & Drug Effects
- Monitor adverse GI effects. Nausea and vomiting are adverse reactions that occur in about 10% of patients after they take
ergotamine. Patient may need an antiemetic. Consult with physician.
- Monitor patients with PVD carefully for development of peripheral ischemia.
- Monitor long-term effectiveness. Patients receiving high ergotamine doses for prolonged periods may experience increased frequency
of headaches, fatigue, and depression. Discontinuation of the drug in these patients results in severe withdrawal headache
that may last a few days.
- Overdose symptoms: Nausea, vomiting, weakness, and pain in legs, numbness and tingling in fingers and toes, tachycardia or
bradycardia, hypertension or hypotension, and localized edema.
Patient & Family Education
- Begin drug therapy as soon after onset of migraine attack as possible, preferably during migraine prodrome (scintillating
scotomas, visual field defects, nausea, paresthesias usually on side opposite to that of the migraine).
- Notify physician if migraine attacks occur more frequently or are not relieved.
- Lie down in a quiet, dark room for 23 h after drug administration.
- Report claudication, muscle pain or weakness of extremities, cold or numb digits, irregular heartbeat, nausea, or vomiting.
Carefully protect extremities from exposure to cold temperatures; provide warmth, but not heat, to ischemic areas.
- Do NOT increase dosage without consulting physician; overdosage is the chief cause of adverse effects from the drug.