ERGOTAMINE TARTRATE
(er-got'a-meen)
Ergomar, Ergostat
Classifications: autonomic nervous system agent; alpha-adrenergic antagonist (sympatholytic); ergot alkaloid
Pregnancy Category: X

Availability

2 mg sublingual tablets

Actions

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 by unknown mechanism, with subsequent occlusion, thrombosis, and gangrene.

Therapeutic Effects

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, marked arteriosclerosis, history of MI, coronary artery disease, 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/24h or 10 mg/wk

Administration

Sublingual

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). Nervous System: Delirium; convulsive seizures; confusion; depression; drowsiness; Digestive: Nausea; vomiting; diarrhea; abdominal pain; unquenchable thirst; partial necrosis of tongue, disagreeable aftertaste. Cardiovascular: 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

Patient & Family Education


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