Generic Name: Ergotamine Tartrate
Class: Non-selective alpha-Adrenergic Blocking Agents
VA Class: CN105
CAS Number: 379-79-3
Possible serious and/or life-threatening cerebral and/or peripheral ischemia when used concomitantly with potent CYP3A4 inhibitors (see Interactions); concomitant use contraindicated.138 139 140
Introduction
Naturally occurring ergot alkaloid.b 140
Uses for Ergomar
Vascular Headaches
Prevention or abortion of vascular headaches (e.g., migraine, cluster headaches), when used alone or in fixed combination with caffeine.138 139 140 Should not be used for chronic daily management of vascular headaches.138 139 140
Generally not preferred for terminating acute cluster headaches; onset of action is slower than that of other therapies (e.g., sumatriptan, oxygen).134 136 141 142
Has been used for short-term (e.g., up to 3 weeks) prophylaxis of episodic cluster headaches to suppress a series of attacks and reduce duration of cluster period.134 136 137 141 142 Prophylactic administration at bedtime may be particularly useful in selected patients with nocturnal cluster attacks.134 135 136 139 140 141
Ineffective in the treatment of muscle contraction headaches.b
Ergomar Dosage and Administration
General
- Vascular Headaches
Administer as soon as possible after onset of first symptoms of vascular headache.138 139 140
After administering the initial dose, patient should lie down and relax in a quiet, darkened room.b
Do not administer within 24 hours of a selective serotonin agonist (e.g., sumatriptan).115 116 144 145 (See Specific Drugs under Interactions.)
Administration
Administer orally or rectally (as fixed-combination preparation containing ergotamine and caffeine).139 140
Administer sublingually (as single-entity preparation).138
Sublingual Administration
Place tablets under the tongue and allow to dissolve.138
Rectal Administration
If suppositories become softened, chill them in ice-cold water to solidify before removing the foil wrapper.139
Dosage
Available as ergotamine tartrate; dosage expressed in terms of the salt.138 139 140
Adults
Vascular Headaches
Oral
Fixed-combination ergotamine and caffeine (e.g., Cafergot) tablets: 2 mg of ergotamine tartrate (2 tablets) initially, followed by 1 mg at 30-minute intervals until attack has abated (maximum 6 mg per attack).140
For short-term prophylaxis of cluster headaches, 3–4 mg daily (in divided doses) has been administered for up to 3 weeks.135 142 May be administered 30–60 minutes prior to an expected attack in patients with consistent attack patterns.135 142 In selected patients with nocturnal attacks, 1–2 mg may be given at bedtime on a short-term basis.134 137 140 142 Monitor carefully to avoid excessive weekly dosages;142 give due consideration to recommended maximum weekly dosage (see Prescribing Limits under Dosage and Administration).140
Sublingual
Ergotamine tartrate (Ergomar) tablets: 2 mg (1 tablet) initially, followed by 2 mg at 30-minute intervals until attack has abated (maximum 6 mg per 24-hour period).138
For short-term prophylaxis of cluster headaches, 3–4 mg daily (in divided doses) has been administered for up to 3 weeks.135 142 May be administered 30–60 minutes prior to an expected attack in patients with consistent attack patterns.135 142 Monitor carefully to avoid excessive weekly dosages;142 give due consideration to recommended maximum weekly dosage (see Prescribing Limits under Dosage and Administration).140
Rectal
Fixed-combination ergotamine and caffeine (e.g., Migergot) suppositories: 2 mg of ergotamine tartrate (1 suppository) initially.139 If necessary, may give a second 2-mg dose after 1 hour.139
In selected patients with cluster headaches at night, 1–2 mg may be given at bedtime on a short-term basis.137 139 142 Give due consideration to recommended maximum weekly dosage (see Prescribing Limits under Dosage and Administration).139 142
Prescribing Limits
Adults
Vascular Headaches
Oral
Maximum 6 mg (6 Cafergot tablets) per attack or 10 mg (10 Cafergot tablets) per week.140
Sublingual
Maximum 6 mg (3 Ergomar tablets) per 24-hour period or 10 mg (5 Ergomar tablets) per week.138
Rectal
Maximum 4 mg (2 Migergot suppositories) per attack or 10 mg (5 Migergot suppositories) per week.139
Cautions for Ergomar
Contraindications
Known or suspected pregnancy.138 139 140
Concomitant therapy with potent CYP3A4 inhibitors.124 125 126 127 138 139 140 (See Interactions.)
Peripheral vascular disease, CHD, or hypertension.138 139 140
Impaired hepatic or renal function.138 139 140
Sepsis.138 139 140
Known hypersensitivity to ergot alkaloids or any ingredient in the formulation.138 139 140
Warnings/Precautions
Warnings
Fibrosis
Possible retroperitoneal and pleuropulmonary fibrosis.106 138 139 140
Possible fibrotic thickening of the aortic, mitral, tricuspid, and/or pulmonary valves with continuous, long-term administration;100 101 102 103 104 105 106 107 138 139 140 do not administer on a chronic daily basis.138 139 140
Examine patients regularly for development of fibrotic complications; perform appropriate tests (e.g., ECG, laboratory tests, radiographic examination) if signs or symptoms of these conditions occur.100 109 113 114
Fetal/Neonatal Morbidity and Mortality
May cause fetal harm; fetal growth retardation observed in animals.138 139 140
General Precautions
Ergotism
Potential for ergotism, manifested by intense arterial vasoconstriction, producing signs and symptoms of peripheral vascular ischemia; if left untreated, can progress to gangrene.138 139 140 Do not exceed recommended dosages.138 139 140
If signs and symptoms of impaired circulation occur, discontinue therapy and keep affected extremities warm.b
Misuse and Abuse
Solitary rectal or anal ulcer associated with abuse of ergotamine suppositories (e.g., use of higher than recommended dosages or continual use at the recommended dose for many years); usually resolves 4–8 weeks following discontinuance of the drug.139
Possible withdrawal symptoms (e.g., rebound headache) upon discontinuance of the drug following indiscriminate use over long periods of time.138 139 140
Use of Fixed Combinations
When used in fixed combination with caffeine, consider the cautions, precautions, and contraindications associated with caffeine.139 140
Specific Populations
Pregnancy
Category X.138 139 140 (See Fetal/Neonatal Morbidity and Mortality and also see Contraindications under Cautions.)
Oxytocic effects are maximal in 3rd trimester; contraindicated in labor and delivery.138 139 140
Lactation
Distributed into milk; may cause vomiting, diarrhea, weak pulse, seizures, and unstable BP in nursing infants.128 129 138 139 140 Discontinue nursing or the drug.138 139 140
Inhibits prolactin, but no reports of decreased lactation.138 139 140
Pediatric Use
Safety and efficacy not established in children.138 139 140
Hepatic Impairment
Use contraindicated.138 139 140
Renal Impairment
Use contraindicated.138 139 140
Common Adverse Effects
Nausea, vomiting, abdominal pain, numbness and tingling of the fingers and toes, muscle pain in the extremities, weakness in the legs.138 139 140 b
Interactions for Ergomar
Extensively metabolized, principally by CYP3A4.138 139 140 Inhibits CYP3A.138 139 140
Drugs Affecting Hepatic Microsomal Enzymes
Potent CYP3A4 inhibitors: Potential pharmacokinetic interaction (increased serum ergotamine concentrations); potentially fatal cerebral ischemia and/or ischemia of the extremities possible.123 124 125 126 127 138 139 140 Concomitant use with potent CYP3A4 inhibitors contraindicated.123 124 125 126 127 138 139 140
Less-potent CYP3A4 inhibitors: Similar effects not reported to date; however, consider possibility of serious toxicity during concomitant use.138 139 140
Specific Drugs
Drug | Interaction | Comment |
|---|---|---|
Antifungals, azole (e.g., itraconazole, ketoconazole) | Inhibition of ergotamine metabolism; increased risk of potentially fatal cerebral ischemia and/or ischemia of the extremities123 124 125 126 127 138 139 140 | Concomitant use contraindicated124 125 126 127 138 139 140 |
Caffeine | Increased plasma ergotamine concentrations143 b | |
HIV protease inhibitors (e.g., ritonavir, nelfinavir, indinavir) | Inhibition of ergotamine metabolism; increased risk of potentially fatal cerebral ischemia and/or ischemia of the extremities123 124 125 126 127 138 139 140 | Concomitant use contraindicated124 125 126 127 138 139 140 |
Macrolide antibiotics (e.g., erythromycin, clarithromycin, troleandomycin) | Inhibition of ergotamine metabolism; increased risk of potentially fatal cerebral ischemia and/or ischemia of the extremities123 124 125 126 127 138 139 140 | Concomitant use contraindicated124 125 126 127 138 139 140 |
Methysergide (no longer commercially available in US) | Potential for excessive vasoconstriction143 | Decrease ergotamine dosage by about 50%; keep frequency of ergotamine administration at a minimumb |
Nicotine | Possible vasoconstriction and increased ischemic response138 139 140 | Concomitant use not recommended138 139 140 |
Propranolol | Potentiation of ergotamine’s vasoconstrictive action138 139 140 | Use with cautionb |
Serotonin (5-HT1) receptor agonists (e.g., sumatriptan) | Additive vasoconstrictor effects115 116 117 118 119 144 145 | Use within 24 hours contraindicated115 116 144 145 |
Sympathomimetic agents | Potential for extreme BP elevations138 139 140 | Concomitant use not recommended138 139 140 |
Ergomar Pharmacokinetics
Absorption
Bioavailability
Absorption is variable following oral administration.b
Undergoes first-pass metabolism following oral administration.b
Distribution
Extent
Crosses the blood-brain barrier and is distributed into milk.b
Elimination
Metabolism
Extensively metabolized in the liver, mainly by CYP3A4.b
Elimination Route
Metabolites are excreted mainly (90%) in bile;b only traces of unchanged drug are excreted in urine and feces.112
Eliminated by dialysis.b
Half-life
Biphasic; terminal half-life is approximately 21 hours.b
Stability
Storage
Oral
Tablets
Tight, light-resistant container at 15–30°C.140
Sublingual
Tablets
20–25°C (may be exposed to 15–30°C).138 Protect from light and heat.138
Rectal
Suppositories
2–8°C.139
ActionsActions
Complex pharmacologic effects, including α-adrenergic blocking activity, direct stimulation of peripheral and cranial vascular smooth muscle, and serotonin antagonist activity.138 139 140
Mechanism by which ergotamine aborts vascular headaches is probably direct vasoconstriction of dilated carotid artery bed.b
Has greater vasoconstrictor activity than other ergot alkaloids but less α-adrenergic blocking activity than dihydroergotamine;b 138 139 140 weaker antagonist of serotonin than is methysergide.b
Advice to Patients
Risk of ergotism; importance of informing clinicians if intermittent claudication; muscle pain; or numbness, coldness, and pallor of the digits occur.138 139 140
Importance of informing clinicians if persistent paresthesia, chest/muscle/abdominal pain, speeding or slowing of heart rate, swelling, or itching occurs.b 138 139 140
Importance of taking ergotamine exactly as prescribed.138 139 140
Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.138 139 140
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.138 139 140
Importance of informing patients of other important precautionary information.138 139 140 (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
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).130 131 132 Manufacturers’ labelings for most of these unapproved preparations omitted critical drug interaction warnings, and the preparations did not undergo FDA review of safety, efficacy, quality, and labeling.131 132 There currently are approved ergotamine-containing preparations on the US market.130 131 132
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Sublingual | Tablets | 2 mg | Ergomar | Rosedale |
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Oral | Tablets | 1 mg with Caffeine 100 mg* | Cafergot | Novartis |
Rectal | Suppositories | 2 mg with Caffeine 100 mg | Migergot | G&W |
Comparative Pricing
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
Cafergot 1-100MG Tablets (SANDOZ): 30/$49.99 or 90/$139.97
Migergot 2-100MG Suppositories (G & W LABS): 12/$95.99 or 36/$259.98
Disclaimer
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions December 2009. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
References
Only references cited for selected revisions after 1984 are available electronically.
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