Ergotamine tartrate (sublingual tablet): Difference between revisions
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|authorTag={{AP}} | |authorTag={{AP}} | ||
|genericName=Ergotamine tartrate | |genericName=Ergotamine tartrate | ||
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|drugClass=alpha adrenergic blocking agent | |drugClass=alpha adrenergic blocking agent | ||
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|adverseReactions=[[Pruritus]], [[Nausea and vomiting]], [[Muscle weakness]], [[Paresthesia]] and [[Visual disturbance]] | |adverseReactions=[[Pruritus]], [[Nausea and vomiting]], [[Muscle weakness]], [[Paresthesia]] and [[Visual disturbance]] | ||
|blackBoxWarningTitle=<span style="color:#FF0000;">WARNING</span> | |blackBoxWarningTitle=<span style="color:#FF0000;">WARNING</span> | ||
|blackBoxWarningBody=<i><span style="color:#FF0000;"> | |blackBoxWarningBody=<i><span style="color:#FF0000;"></span></i> 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. | ||
|fdaLIADAdult=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. | |||
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Ergotamine in adult patients. | |offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Ergotamine in adult patients. | ||
|offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Ergotamine in adult patients. | |offLabelAdultNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Ergotamine in adult patients. | ||
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Ergotamine in pediatric patients. | |offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of Ergotamine in pediatric patients. | ||
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> of Ergotamine in pediatric patients. | |offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non–Guideline-Supported Use</i> 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. | |||
|alcohol=Alcohol-Ergotamine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication. | |alcohol=Alcohol-Ergotamine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication. | ||
}} | }} | ||
Revision as of 17:49, 29 December 2014
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
{{#ask: Page Name::Ergotamine tartrate (sublingual tablet) |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}
Package and Label Display Panel
{{#ask: Label Page::Ergotamine tartrate (sublingual tablet) |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}
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
 | |
| Clinical data | |
|---|---|
| Routes of administration | Oral |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Metabolism | hepatic |
| Excretion | renal |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value). |
| 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
FDA Package Insert
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-HT1B receptor, and by inhibiting trigeminal neurotransmission by 5-HT1D receptors. Ergotamine also has effects on the dopamine and noradrenaline receptors. It is its action on the D2 dopamine and 5-HT1A receptors that can cause some side effects. [1]
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.[2]
Illegal uses
Ergotamine is also a precursor of LSD, lysergic acid diethylamide.
See also
References
- ↑ Tfelt-Hansen P, Saxena PR, Dahlof C, Pascual J, Lainez M, Henry P, Diener H, Schoenen J, Ferrari MD, Goadsby PJ (2000). "Ergotamine in the acute treatment of migraine: a review and European consensus". Brain. 123: 9–18. PMID 10611116.
- ↑ Schardl CL, Panaccione DG, Tudzynski P (2006). "Ergot alkaloids--biology and molecular biology". Alkaloids Chem. Biol. 63: 45–86. PMID 17133714.
- ↑ "MEDIHALER ERGOTAMINE (ERGOTAMINE TARTRATE) AEROSOL, METERED [3M RIKER]".
- ↑ "ERGOMAR (ERGOTAMINE TARTRATE) TABLET, ORALLY DISINTEGRATING [ROSEDALE THERAPEUTICS]".
Template:Antimigraine preparations
- Pages with script errors
- CS1 maint: Multiple names: authors list
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- ECHA InfoCard ID from Wikidata
- Chemical articles with unknown parameter in Infobox drug
- Articles without EBI source
- Chemical pages without ChemSpiderID
- Chemical pages without DrugBank identifier
- Articles without KEGG source
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- Antimigraine drugs
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