ERGOTAMINE TARTRATE

ERGOTAMINE TARTRATE
(er-got'a-meen)
Ergomar, Ergostat
Classifications: alpha-adrenergic antagonist; ergot alkaloid;
Therapeutic: antimigraine

Pregnancy Category: X

Availability

2 mg sublingual tablets

Action

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.

Therapeutic Effect

In vascular headache, exerts vasoconstrictive action on previously dilated cerebral vessels, reduces amplitude of arterial pulsations, and antagonizes effects of serotonin.

Uses

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.

Contraindications

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.

Cautious Use

Lactation, older adult patients.

Route & Dosage

Vascular Headaches
Adult: SL 1–2 mg followed by 1–2 mg q30min until headache abates or until max of 6 mg/24 h or 10 mg/wk

Administration

Sublingual
  • 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, weakness, 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 of ergotism.

Interactions

Drug: With high doses of beta-adrenergic blockers, sympathomimetics, 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.

Pharmacokinetics

Absorption: Variable absorption orally. Peak: 0.5–3 h. Distribution: Crosses blood–brain 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.

Nursing Implications

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 2–3 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.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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