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Pharmacokinetics

Absorption

Bioavailability

Absorption is variable following oral administration.

Undergoes first-pass metabolism following oral administration.

Distribution

Extent

Crosses the blood-brain barrier and is distributed into milk.

Elimination

Metabolism

Extensively metabolized in the liver, mainly by CYP3A4.

Elimination Route

Metabolites are excreted mainly (90%) in bile; only traces of unchanged drug are excreted in urine and feces.

Eliminated by dialysis.

Half-life

Biphasic; terminal half-life is approximately 21 hours.

Stability

Storage

Oral

Tablets

Tight, light-resistant container at 15–30°C.

Sublingual

Tablets

20–25°C (may be exposed to 15–30°C). Protect from light and heat.

Rectal

Suppositories

<25°C. Protect from moisture.

Actions

• Complex pharmacologic effects, including α-adrenergic blocking activity, direct stimulation of peripheral and cranial vascular smooth muscle, and serotonin antagonist activity.
• Mechanism by which ergotamine aborts vascular headaches is probably direct vasoconstriction of dilated carotid artery bed.
• Has greater vasoconstrictor activity than other ergot alkaloids but less α-adrenergic blocking activity than dihydroergotamine; weaker antagonist of serotonin than is methysergide.

Advice to Patients

• Risk of ergotism; importance of informing clinicians if intermittent claudication; muscle pain; or numbness, coldness, and pallor of the digits occur.
• Importance of informing clinicians if persistent paresthesia, chest/muscle/abdominal pain, speeding or slowing of heart rate, swelling, or itching occurs.
• Importance of taking ergotamine exactly as prescribed.
• Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.
• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.
• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

On February 26, 2007, FDA warned 20 firms that manufacture or distribute unapproved drug preparations containing ergotamine tartrate of the agency’s intention to take enforcement action (e.g., seizure, injunction, other judicial proceeding) against all firms attempting to manufacture or distribute such preparations after April 25, 2007, or August 25, 2007, respectively, without an approved new drug application (NDA). Unapproved preparations manufactured or distributed before these dates may still be found on pharmacy shelves for a short period of time. Manufacturers' labelings for most of these unapproved preparations omit critical drug interaction warnings, and the preparations have not undergone FDA review of safety, efficacy, quality, and labeling. There currently are approved ergotamine-containing preparations on the US market.

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit drugstore.com.

AHFS Drug Information. © Copyright, 1959-2008, Selected Revisions December 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.