ergotamine/caffeine (Rx)

Brand and Other Names:Cafergot, Migergot
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

ergotamine/caffeine

oral tablet (Cafergot)

  • 1mg/100mg

rectal suppository (Migergot)

  • 2mg/100mg

Vascular Headache

Indicated as therapy to abort or prevent vascular headache (eg, migraine, migraine variants, “histaminic cephalalgia”)

Not for chronic daily use

Oral

  • 2 tablets (ergotamine 2 mg/caffeine 200 mg) PO at first sign of attack; may take 1 tablet (ergotamine 1 mg/caffeine 100 mg) q30min prn
  • Not to exceed 6 tablets/attack
  • Not to exceed 10 tablets/week

Rectal

  • Insert 1 suppository rectally at first sign of attack; may repeat once after 1 hr
  • Not to exceed 2 suppositories/attack
  • Not to exceed 5 suppositories/week

Short-term prevention

  • In carefully selected patients, with due consideration of maximum dosage recommendations, administration of the drug at bedtime may be an appropriate short-term preventive measure

Dosage Modifications

Renal or hepatic impairment

  • Contraindicated

Dosing Considerations

Not effective for other types of headaches; lacks analgesic properties

Safety and efficacy not established

Next:

Interactions

Interaction Checker

and ergotamine/caffeine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 
            Due to system maintenance, the drug interactions feature you are attempting to access is temporarily unavailable. Please try again later.
            Previous
            Next:

            Adverse Effects

            Frequency Not Defined

            Gastrointestinal: Nausea and vomiting; rectal or anal ulcer (from overuse of suppositories)

            Neurological: Paresthesia, numbness, weakness, and vertigo

            Allergic: Localized edema and itching

            Cardiovascular

            • Serious vasoconstrictive complications may occur including ischemia, cyanosis, absence of pulse, cold extremities, gangrene, precordial distress and pain, EKG changes, and muscle pains
            • Most commonly occurs with long-term therapy at relatively high doses; also reported with short-term or normal doses
            • Other cardiovascular adverse effects include transient tachycardia or bradycardia and hypertension
            Previous
            Next:

            Warnings

            Black Box Warnings

            Serious and/or life-threatening peripheral ischemia associated with coadministration of ergotamine and caffeine with potent CYP3A4 inhibitors including protease inhibitors and macrolide antibiotics

            Because CYP3A4 inhibition elevates ergotamine and caffeine serum levels, the risk for vasospasm leading to cerebral ischemia and/or ischemia of the extremities is increased

            Concomitant use of these medications is contraindicated

            Contraindications

            Potent CYP3A4 inhibitors owing to risk of acute ergot toxicity

            Pregnancy

            Peripheral vascular disease, coronary heart disease, hypertension, impaired hepatic or renal function, sepsis

            Hypersensitivity to any of the ingredients

            Cautions

            Ergotism

            • Although ergotism rarely develop even after long-term intermittent use of orally administered ergotamine, do not exceed dosage recommendations
            • Ergotism manifested by intense arterial vasoconstriction, producing signs and symptoms of peripheral vascular ischemia
            • Headache, intermittent claudication, muscle pains, numbness, or coldness and pallor of the digits may occur with chronic intoxication; if the condition is allowed to progress untreated, gangrene can result
            • While most cases result from frank overdosage, some cases involve hypersensitivity
            • There are few reports among patients taking doses within recommended limits or for brief periods
            • Withdrawal symptoms (eg, rebound headache) upon discontinuation are rare; typically reported with long, indiscriminate use

            Fibrotic complications

            • Retroperitoneal and/or pleuropulmonary fibrosis reported
            • Rare reports of fibrotic thickening of the aortic, mitral, tricuspid, and/or pulmonary valves with long-term, continuous use of ergotamine tartrate and caffeine
            • Do not use for chronic daily administration

            Drug interaction overview

            • Ergotamine is a CYP3A substrate and inhibitor
            • CYP3A inhibitors
              • Potent inhibitors: Contraindicated owing to risk for acute ergot toxicity (ergotism) characterized by vasospasm and ischemia of the extremities
              • Less potent inhibitors: Although not contraindicated, avoid if possible owing to risk for vasospasm
            Previous
            Next:

            Pregnancy & Lactation

            Pregnancy

            Contraindicated; ergotamine elicits oxytocic effects

            There are no studies on placental transfer or teratogenicity of the combination of ergotamine and caffeine

            Labor and delivery

            • Contraindicated in labor and delivery owing to ergotamine’s oxytocic effect, which is maximal in the third trimester

            Animal studies

            • Caffeine is known to cross the placenta and has been shown to be teratogenic in animals
            • Ergotamine crosses the placenta in small amounts, although it does not appear to be embryotoxic in this quantity; however, prolonged vasoconstriction of uterine vessels and/or increased myometrial tone leading to reduced myometrial and placental blood flow may have contributed to fetal growth retardation observed in animals

            Lactation

            Ergot drugs are known to inhibit prolactin, but there are no reports of decreased lactation with ergotamine/caffeine

            Ergotamine is excreted in breast milk and may cause symptoms of vomiting, diarrhea, weak pulse, and unstable blood pressure in nursing infants

            Owing to the potential serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug, considering the importance of the drug to the mother

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

            Previous
            Next:

            Pharmacology

            Mechanism of Action

            Ergotamine: Alpha-adrenergic blocking agent with direct stimulating effect on smooth muscle of peripheral and cranial blood vessels; also elicits serotonin antagonism

            Caffeine: Cranial vasoconstrictor; added to further enhance vasoconstrictive effect without increasing ergotamine dosage

            Absorption

            Bioavailability: <5%

            Peak plasma time: 2 hr (PO)

            Distribution

            Vd: 1.85 L/kg

            Metabolism

            Extensively metabolized in liver hepatic metabolism

            Elimination

            Half-life: 2-2.5 hr

            Excretion: Feces (90%, mostly as metabolites)

            Previous
            Next:

            Administration

            Oral Administration

            May take with or without food

            Rectal Administration

            Remove suppository from foil wrap

            Lay on side and insert pointed end of suppository into rectum; remain on side to allow suppository to dissolve and absorb

            Avoid handling unwrapped suppository for too long

            If needed, may cut suppository lengthwise

            Storage

            Tablets

            • Store at 20-25ºC (68-77ºF)
            • Dispense in tight, light-resistant container

            Suppositories

            • Refrigerate at 2-8ºC (36-46ºF) in sealed foil
            Previous
            Next:

            Images

            No images available for this drug.
            Previous
            Next:

            Patient Handout

            A Patient Handout is not currently available for this monograph.
            Previous
            Next:

            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Additional Offers
            Email to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Email Forms to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Previous
            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.