Ergotamine tartrate (sublingual tablet)

Ergotamine tartrate (sublingual tablet)
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alberto Plate [2]

Disclaimer

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Black Box Warning

WARNING See full prescribing information for complete Boxed Warning. Serious and/or life-threatening peripheral ischemia has been associated with the coadministration of ergotamine tartrate with potent CYP 3A4 inhibitors including protease inhibitors and macrolide antibiotics. Because CYP 3A4 inhibition elevates the serum levels of ergotamine tartrate, the risk for vasospasm leading to cerebral ischemia and/or ischemia of the extremities is increased. Hence, concomitant use of these medications is contraindicated.

Overview

Ergotamine tartrate (sublingual tablet) is an alpha adrenergic blocking agent that is FDA approved for the prophylaxis of vascular migraine. There is a Black Box Warning for this drug as shown here. Common adverse reactions include Pruritus, Nausea and vomiting, Muscle weakness, Paresthesia and Visual disturbance.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

For best results, dosage should start at the first sign of an attack. Early Administration Gives Maximum Effectiveness. 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 24hour period. Total weekly dosage should not exceed five tablets (10 mg) in any one week. Ergomar® Sublingual Tablets should not be used for chronic daily administration.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Ergotamine in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Ergotamine in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding Ergotamine tartrate (sublingual tablet) FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Ergotamine in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Ergotamine in pediatric patients.

Contraindications

Coadministration of ergotamine with potent CYP 3A4 inhibitors (ritonavir, nelfinavir, indinavir, erythromycin, clarithromycin and troleandomycin) has been associated with acute ergot toxicity (ergotism) characterized by vasospasm and ischemia of the extremities (See PRECAUTIONS: DRUG INTERACTIONS), with some cases resulting in amputation. There have been rare reports of cerebral ischemia in patients on protease inhibitor therapy when ergotamine was coadministered, at least one resulting in death. Because of the increased risk for ergotism and other serious vasospastic adverse events, ergotamine use is contraindicated with these drugs and other potent inhibitors of CYP 3A4 (e.g., ketoconazole, itraconazole) (See WARNINGS: CYP 3A4 INHIBITORS).

Ergomar® Sublingual Tablets may cause fetal harm when administered to pregnant women. Ergomar® Sublingual Tablets are contraindicated in women who are or may become pregnant. If this drug is used during pregnancy or if the patient becomes pregnant while taking this product, the patient should be apprised of the potential hazard to the fetus. Peripheral vascular disease, coronary heart disease, hypertension, impaired hepatic or renal function and sepsis.

Hypersensitivity to any of the components.

Warnings

WARNING See full prescribing information for complete Boxed Warning. Serious and/or life-threatening peripheral ischemia has been associated with the coadministration of ergotamine tartrate with potent CYP 3A4 inhibitors including protease inhibitors and macrolide antibiotics. Because CYP 3A4 inhibition elevates the serum levels of ergotamine tartrate, the risk for vasospasm leading to cerebral ischemia and/or ischemia of the extremities is increased. Hence, concomitant use of these medications is contraindicated.

There is limited information regarding Ergotamine tartrate (sublingual tablet) Warnings' in the drug label.

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Ergotamine tartrate (sublingual tablet) Clinical Trials Experience in the drug label.

Postmarketing Experience

There is limited information regarding Ergotamine tartrate (sublingual tablet) Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Ergotamine tartrate (sublingual tablet) Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There is no FDA guidance on usage of Ergotamine tartrate (sublingual tablet) in women who are pregnant.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Ergotamine tartrate (sublingual tablet) in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Ergotamine tartrate (sublingual tablet) during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Ergotamine tartrate (sublingual tablet) in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Ergotamine tartrate (sublingual tablet) in pediatric settings.

Geriatic Use

There is no FDA guidance on the use of Ergotamine tartrate (sublingual tablet) in geriatric settings.

Gender

There is no FDA guidance on the use of Ergotamine tartrate (sublingual tablet) with respect to specific gender populations.

Race

There is no FDA guidance on the use of Ergotamine tartrate (sublingual tablet) with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Ergotamine tartrate (sublingual tablet) in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Ergotamine tartrate (sublingual tablet) in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Ergotamine tartrate (sublingual tablet) in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Ergotamine tartrate (sublingual tablet) in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Ergotamine tartrate (sublingual tablet) Administration in the drug label.

Monitoring

There is limited information regarding Ergotamine tartrate (sublingual tablet) Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Ergotamine tartrate (sublingual tablet) and IV administrations.

Overdosage

There is limited information regarding Ergotamine tartrate (sublingual tablet) overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

Pharmacology

There is limited information regarding Ergotamine tartrate (sublingual tablet) Pharmacology in the drug label.

Mechanism of Action

There is limited information regarding Ergotamine tartrate (sublingual tablet) Mechanism of Action in the drug label.

Structure

There is limited information regarding Ergotamine tartrate (sublingual tablet) Structure in the drug label.

Pharmacodynamics

There is limited information regarding Ergotamine tartrate (sublingual tablet) Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Ergotamine tartrate (sublingual tablet) Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Ergotamine tartrate (sublingual tablet) Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Ergotamine tartrate (sublingual tablet) Clinical Studies in the drug label.

How Supplied

There is limited information regarding Ergotamine tartrate (sublingual tablet) How Supplied in the drug label.

Storage

There is limited information regarding Ergotamine tartrate (sublingual tablet) Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Ergotamine tartrate (sublingual tablet) Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Ergotamine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Ergotamine tartrate (sublingual tablet) Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Ergotamine tartrate (sublingual tablet) Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

Ergotamine
ERGOMAR (ergotamine tartrate) tablet® FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information
Labels and Packages
Medihaler ergotamine (ergotamine tartrate) aerosol, metered® FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information
Labels and Packages
Clinical Trials on Medihaler ergotamine (ergotamine tartrate) aerosol, metered
ClinicalTrials.gov

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [3]; Associate Editor(s)-in-Chief: Pratik Bahekar, MBBS [4]

For patient information about Ergotamine, click here.

Synonyms / Brand Names: CAFERGOT^®, ERGOMAR(ergotamine tartrate)tablet^®, Medihaler ergotamine (ergotamine tartrate)^®

Overview

Ergotamine tartrate (sublingual tablet)

Clinical data
Routes of administration	Oral
ATC code	N02CA02 (WHO)
Legal status
Legal status	AU: S4 (Prescription only) UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Metabolism	hepatic
Excretion	renal
Identifiers
IUPAC name Ergotaman-3',6',18-trione, 12'-hydroxy-2'-methyl-5'-(phenylmethyl)-, (5'-alpha)- (9CI)
CAS Number	113-15-5
PubChem CID	9787
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C33H35N5O5
Molar mass	581.66 g/mol

Ergotamine is an ergopeptine and part of the ergot family of alkaloids; it is structurally and biochemically closely related to ergoline. It possesses structural similarity to several neurotransmitters, and has biological activity as a vasoconstrictor. It is used medicinally for migraine prevention (sometimes in combination with caffeine), and to induce childbirth and prevent post-partum haemorrhage.

Category

Anti Migraine Drugs

ERGOMAR (ergotamine tartrate) tablet

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

Medihaler ergotamine (ergotamine tartrate) aerosol, metered

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

Mechanism of action

The mechanism of action of ergotamine is complex. The molecule shares similarity with neurotransmitters such as serotonin, dopamine, and adrenaline and can thus bind to several cell receptors acting both as agonist and antagonist in signal transduction within cellular tissues. The anti-migraine effect is due to constriction of the intercranial extracerebral blood vessels through the 5-HT_1B receptor, and by inhibiting trigeminal neurotransmission by 5-HT_1D receptors. Ergotamine also has effects on the dopamine and noradrenaline receptors. It is its action on the D2 dopamine and 5-HT_1A receptors that can cause some side effects.

Biosynthesis

Ergotamine is a secondary metabolite (natural product) and the principal alkaloid produced by the ergot fungus, Claviceps purpurea, and related fungi in the family Clavicipitaceae. Its biosynthesis in these fungi requires the amino acid, L-tryptophan, and dimethylallyl diphosphate. These precursor compounds are the substrates for the enzyme, dimethylally-tryptophan (DMAT) synthase, catalyzing the first step in ergot alkaloid biosynthesis, i.e., the prenylation of L-tryptophan. Further reactions, involving methyltransferase and oxygenase enzymes, yield the ergoline, lysergic acid. Lysergic acid (LA) is the substrate of lysergyl peptide synthetase, a nonribosomal peptide synthetase, which covalently links LA to the amino acids, L-alanine, L-proline, and L-phenylalanine. Enzyme-catalyzed or spontaneous cyclizations, oxygenations/oxidations, and isomerizations at selected residues precede, and give rise to, formation of ergotamine.

Illegal uses

Ergotamine is also a precursor of LSD, lysergic acid diethylamide.

See also

• Cafergot, a preventative migraine treatment with ergotamine.

References

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