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Ergotamine Tartrate

Pronunciation: er-GOT-a-meen TAR-trate
Class: Ergotamine derivative

Trade Names

Ergomar
- Tablets, sublingual 2 mg

Pharmacology

Reduces extracranial blood flow, causes decline in amplitude of pulsation in the cranial arteries, and decreases hyperperfusion of the territory of the basilar artery; produces constriction of both arteries and veins.

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Pharmacokinetics

Absorption

Poorly absorbed following GI and SL administration.

Metabolism

Metabolized by the liver.

Elimination

Half-life is approximately 2 h; 90% of metabolites are excreted in the bile. Unmetabolized ergotamine is erratically excreted in the saliva, and trace amounts are excreted in the feces and urine.

Indications and Usage

Abort or prevent vascular headache (eg, migraine).

Contraindications

Peripheral vascular disease; coronary heart disease; hypertension; hepatic or renal function impairment; sepsis; hypersensitivity to any component of the product; pregnancy; potent CYP3A4 inhibitors (eg, erythromycin, ritonavir).

Dosage and Administration

SL 2 mg under tongue at first sign of attack or to relieve symptoms after onset of an attack; another tablet should be taken at 30-min intervals thereafter, if necessary (max, 6 mg per 24 h and 10 mg in any 1 wk). Ergotamine tartrate should not be used for chronic daily administration.

General Advice

For SL administration only. Do not crush, chew, or swallow tablet.

Storage/Stability

Store at controlled room temperature (59° to 86°F). Protect from light and heat.

Drug Interactions

Beta adrenergic blockers (eg, propranolol)

Unopposed ergot action may occur, increasing the risk of peripheral ischemia and possible peripheral gangrene.

Caffeine

Retroperitoneal and/or pleuropulmonary fibrosis as well as fibrotic thickening of the aortic, mitral, tricuspid, and/or pulmonary valves have been reported in patients receiving ergotamine and caffeine currently.

Clotrimazole, fluoxetine, fluvoxamine, grapefruit juice, metronidazole, nefazodone, NNRT inhibitors (eg, delavirdine, efavirenz), zileuton

May inhibit ergotamine metabolism (CYP3A4), increasing the risk of ergot toxicity (eg, ischemia of the extremities, peripheral vasospasm).

Nicotine, vasoconstrictors

Risk of ischemia and peripheral vasospasm may be increased.

Potent CYP3A4 inhibitors (eg, azole antifungal agents [eg, itraconazole, posaconazole], macrolide antibiotics [eg, erythromycin], protease inhibitors [eg, ritonavir])

The risk of ergot toxicity (eg, ischemia of the extremities, peripheral vasospasm) may be increased. These agents are contraindicated in patients receiving ergotamine.

Selective 5-hydroxytriptamine 1 receptor agonists (eg, eletriptan, sumatriptan)

Coadministration of these agents within 24 h of ergotamine administration is contraindicated.

Sibutramine

Risk of serotonin syndrome may be increased; coadministration with ergotamine is not recommended.

Sympathomimetics

May cause extreme elevations in BP.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Absence of pulse, cold extremities, cyanosis, ECG changes, gangrene, hypertension, ischemia, precordial distress and pain, transient bradycardia or tachycardia.

CNS

Numbness, parasthesias, vertigo, weakness.

GI

Nausea, vomiting.

Hypersensitivity

Localized edema and itching.

Musculoskeletal

Muscle pain.

Miscellaneous

Fibrotic complications.

Precautions

Warnings

Serious and/or life-threatening peripheral ischemia has been associated with the coadministration of ergotamine tartrate with potent CYP3A4 inhibitors, including macrolide antibiotics and protease inhibitors. Because CYP3A4 inhibitors elevate ergotamine plasma concentrations, the risk for vasospasm resulting in cerebral ischemia and/or ischemia of the extremities is increased. Coadministration of these agents is contraindicated.


Pregnancy

Category X .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Dependency

Psychological dependency has been reported. To avoid ergotism, patients should not exceed the recommended dosages with long-term use.

Ergotism

Signs and symptoms are rare; however, remain within limits of recommended dosage.

Overdosage

Symptoms

Coma; drowsiness; hypertension; hypotension; numbness, tingling, pain, and cyanosis of the extremities associated with diminished or absent peripheral pulses; reversible bilateral papillitis with ring scotomata; seizures; shock; stupor; vomiting.

Patient Information

  • Explain that drug is to be used only during migraine and does not prevent or reduce the number of attacks. Emphasize that drug is used only to treat actual migraine attack.
  • Instruct patient in proper use of SL tablet. Caution patient not to chew, crush, or swallow tablet.
  • Advise patient that drug is to be taken as soon as symptoms of migraine appear, and that the dose may be repeated every 30 min if needed, but that no more than 3 tablets should be used in any 24-h period or 5 tablets used in any 1-wk period.
  • Caution patient not to exceed the dosing guidelines because of the risk of toxic effects developing.
  • Advise patient to stop taking the drug and notify health care provider if any of the following occur: changes in heart rate; chest pain, tightness, or pressure; itching; muscle pain in arms or legs; numbness, tingling, coldness, or paleness in the fingers or toes; sudden worsening of headache; swelling; weakness in the legs.
  • Instruct patient that if they have migraine prophylactic medications prescribed to take daily as directed.
  • Advise patient that if not currently taking a migraine prophylactic drug to discuss the use of such drugs with health care provider.
  • Advise women of childbearing potential to avoid becoming pregnant while taking this medicine and to notify health care provider immediately if they do become pregnant.

Copyright © 2009 Wolters Kluwer Health.

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