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Each sublingual tablet of ERGOMAR contains 2 mg ergotamine tartrate, USP.
Inactive Ingredients: Corn starch, D & C Yellow No. 10, FD & C Blue No. 1, lactose monohydrate NF, magnesium stearate, peppermint oil, saccharin sodium.
Pharmacological Category: Vasoconstrictor, uterine stimulant, alpha adrenoreceptor antagonist.
Therapeutic Class: Anti-migraine.
Chemical Name: Ergotaman-3',6', 18-trione, 12'-hydroxy-2'-methyl-5'-(phenyl-methyl)-,(5'(alpha))-,[R-(R*,R*)]-2, 3-dihydroxybutanedioate(2:1)(tartrate).
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The pharmacological properties of ergotamine are extremely complex; some of its actions are unrelated to each other, and even mutually antagonistic. The drug has partial agonist and/or antagonist activity against tryptaminergic, dopaminergic and alpha adrenergic receptors depending upon their site, and it is a highly active uterine stimulant. It causes constriction of peripheral and cranial blood vessels and produces depression of central vasomotor centers. The pain of a migraine attack is believed to be due to greatly increased amplitude of pulsations in the cranial arteries, especially the meningeal branches of the external carotid artery. Ergotamine reduces extracranial blood flow, causes a decline in the amplitude of pulsation in the cranial arteries, and decreases hyperperfusion of the territory of the basilar artery. It does not reduce cerebral hemispheric blood flow. Long term usage has established the fact that ergotamine tartrate is effective in controlling up to 70% of acute migraine attacks, so that it is now considered specific for the treatment of this headache syndrome. Ergotamine produces constriction of both arteries and veins. In doses used in the treatment of vascular headaches, ergotamine usually produces only small increases in blood pressure but it does increase peripheral resistance and decrease blood flow in various organs. Small doses of the drug increase the force and frequency of uterine contraction; larger doses increase the resting tone of the uterus also. The gravid uterus is particularly sensitive to these effects of ergotamine. Although specific teratogenic effects attributable to ergotamine have not been found, the fetus suffers if ergotamine is given to the mother. Retarded fetal growth and an increase in intrauterine death and resorption have been seen in animals. These are thought to result from ergotamine induced increases in uterine motility and vasoconstriction in the placental vascular bed.
The bioavailability of sublingually administered ergotamine has not been determined.
Ergotamine is metabolized by the liver by largely undefined pathways, and 90% of the metabolites are excreted in the bile. The unmetabolized drug is erratically secreted in the saliva, and only traces of unmetabolized drug appear in the urine and feces. Ergotamine is secreted into breast milk. The elimination half-life of ergotamine from plasma is about 2 hours, but the drug may be stored in some tissues, which would account for its long lasting therapeutic and toxic actions.
ERGOMAR is indicated as therapy to abort or prevent vascular headache, e.g., migraine, migraine variants, or so called "histaminic cephalalgia."
ERGOMAR is contraindicated in peripheral vascular disease (thromboangitis obliterans, luetic arteritis, severe arteriosclerosis, thrombophlebitis, Raynaud' disease), coronary heart disease, hypertension, impaired hepatic or renal function, severe pruritis, and sepsis. It is also contraindicated in patients who are hypersensitive to any of its components. ERGOMAR may cause fetal harm when administered to a pregnant woman by virtue of its powerful uterine stimulant actions. ERGOMAR is contraindicated in women who are, or may become, pregnant.
General: Although signs and symptoms of ergotism rarely develop even after long term intermittent use of ergotamine, care should be exercised to remain within the limits of recommended dosage.
Drug Interactions: The effects of ERGOMAR may be potentiated by triacetyloleandomycin which inhibits the metabolism of ergotamine. The pressor effects of ERGOMAR and other vasoconstrictor drugs can combine to cause dangerous hypertension.
Carcinogenesis: No studies have been performed to investigate ERGOMAR for carcinogenic effects.
Pregnancy: Pregnancy Category X--See CONTRAINDICATIONS section.
Nursing Mothers: Ergotamine is secreted into human milk. It can reach the breast-fed infant by this route and exert pharmacologic effects in it. Caution should be exercised when ERGOMAR is administered to a nursing woman. Excessive dosing or prolonged administration of ergotamine may inhibit lactation.
Nausea and vomiting occur in up to 10% of patients after ingestion of therapeutic doses of ergotamine. Weakness of the legs and pain in limb muscles are also frequent complaints. Numbness and tingling of the fingers and toes, precordial pain, transient changes in heart rate and localized edema and itching may also occur, particularly in patients who are sensitive to the drug.
Patients who take ergotamine for extended periods of time may become dependent upon it and require progressively increasing doses for relief of vascular headaches, and for prevention of dysphoric effects which follow withdrawal of the drug.
Overdosage with ergotamine causes nausea, vomiting, weakness of the legs, pain in limb muscles, numbness and tingling of the fingers and toes, precordial pain, tachycardia or bradycardia, hypertension or hypotension and localized edema and itching together with signs and symptoms of ischemia due to vasoconstriction of peripheral arteries and arterioles. The feet and hands become cold, pale and numb. Muscle pain occurs while walking and later at rest also. Gangrene may ensue. Confusion, depression, drowsiness and convulsions are occasional signs of ergotamine toxicity. Overdosage is particularly likely to occur in patients with sepsis or impaired renal or hepatic function. Patients with peripheral vascular disease are specially at risk of developing peripheral ischemia following treatment with ergotamine. Some cases of ergotamine poisoning have been reported in patients who have taken less than 5 mg of the drug. Usually, however, toxicity is seen in doses of ergotamine tartrate in excess of about 15 mg in 24 hours or 40 mg in a few days.
Treatment of ergotamine overdosage consists of the withdrawal of the drug followed by symptomatic measures including attempts to maintain an adequate circulation in the affected parts. Anticoagulant drugs, low molecular weight dextran and potent vasodilator drugs may all be beneficial. Intravenous infusion of sodium nitroprusside has also been reported to be successful. Vasodilators must be used with special care in the presence of hypotension.
Nausea and vomiting may be relieved by atropine or antiemetic compounds of the phenothiazine group. Ergotamine is dialyzable.
All efforts should be made to initiate therapy as soon as possible after the first symptoms of the attack are noted, since success is proportional to rapidity of treatment, and lower dosages will be effective. At the first sign of an attack or to relieve symptoms after onset of an attack one 2 mg tablet is placed under the tongue. Another tablet should be taken at half-hour intervals thereafter, if necessary, but dosage must not exceed three tablets in any 24 hour period. Dosage should be limited to not more than five tablets (10mg) in any one week.
20 tablets (green) each containing 2 mg ergotamine tartrate, supplied in foil strips in a plastic child resistant container. Each tablet is debossed with the following product identification code: LB 2. Protect from light and heat. Keep out of the reach of children.
NDC 59417-120-20 Containers of 20.
CAUTION:
Rx only
Manufactured for:
Radford, VA 24143, USA
By: Mikart, Inc.
Atlanta, GA 30318 USA
©Lotus Biochemical Corporation
All Rights Reserved
Rev. 7/00