fabulous Ergotamine and Caffeine Pronunciation (er GOT a meen & KAF een) Index Terms Caffeine and Ergotamine Ergotamine Tartrate and Caffeine Ergotamine Tartrate/Caffeine Dosage Forms Excipient information presented when available (limited, particularly for generics); consult specific product labeling. Suppository, rectal: Migergot: Ergotamine tartrate 2 mg and caffeine 100 mg (12s) Tablet, oral: Cafergot: Ergotamine tartrate 1 mg and caffeine 100 mg Generic: Ergotamine tartrate 1 mg and caffeine 100 mg Brand Names: U.S. Cafergot Migergot Pharmacologic Category Antimigraine Agent Central Nervous System Stimulant Ergot Derivative Pharmacology Has partial agonist and/or antagonist activity against tryptaminergic, dopaminergic and alpha-adrenergic receptors depending upon their site; is a highly active uterine stimulant; it causes constriction of peripheral and cranial blood vessels and produces depression of central vasomotor centers Absorption Ergotamine: Oral, rectal: Erratic (Perrin, 1985) Metabolism Ergotamine: Extensively hepatic, including high first-pass metabolism (Perrin, 1985) Excretion Ergotamine: Feces (90%, primarily as metabolites) (Perrin, 1985) Time to Peak Serum: Ergotamine: 2 hours (Perrin, 1985) Half-Life Elimination 2 to 2.5 hours (Perrin, 1985) Use: Labeled Indications Vascular headache: Prevention or treatment of vascular headaches, such as migraine, migraine variants, or so-called histaminic cephalalgia Contraindications Hypersensitivity to ergotamine, caffeine, or any component of the formulation; peripheral vascular disease; hepatic or renal impairment; coronary heart disease; hypertension; sepsis; concomitant use of ergot alkaloids with strong inhibitors of CYP3A4 (includes HIV and HCV protease inhibitors, cobicistat, azole antifungals, and some macrolide antibiotics); pregnancy Dosing: Adult Vascular headache: Oral: Note: Each tablet contains ergotamine 1 mg and caffeine 100 mg: Ergotamine 2 mg and caffeine 200 mg (2 tablets) at onset of attack; then ergotamine 1 mg and caffeine 100 mg (1 tablet) every 30 minutes as needed Maximum dose: Ergotamine 6 mg and caffeine 600 mg (6 tablets) per attack; do not exceed ergotamine 10 mg and caffeine 1,000 mg (10 tablets) per week Rectal: Ergotamine 2 mg and caffeine 100 mg (1 suppository) at first sign of an attack; follow with second dose after 1 hour, if needed Maximum dose: Ergotamine 4 mg and caffeine 200 mg (2 suppositories) per attack; do not exceed ergotamine 10 mg and caffeine 500 mg (5 suppositories) per week Dosing: Renal Impairment Use is contraindicated. Dosing: Hepatic Impairment Use is contraindicated. Administration Oral: Administer with or without food. Rectal: Suppository: Remove foil from rectal suppository and insert pointed end first. Avoid handling unwrapped suppository for too long. Storage Suppositories: Store refrigerated at 2 C to 8 C (36 F to 46 F) in sealed foil. Tablet: Store at 20 C to 25 C (68 F to 77 F). Protect from light. Drug Interactions Abiraterone Acetate: May increase the serum concentration of CYP1A2 Substrates (High risk with Inhibitors). Monitor therapy Acebrophylline: May enhance the stimulatory effect of CNS Stimulants. Avoid combination Adenosine: Caffeine and Caffeine Containing Products may diminish the therapeutic effect of Adenosine. Management: Monitor for decreased effect of adenosine if patient is receiving caffeine. Discontinue caffeine in advance of scheduled diagnostic use of adenosine whenever possible. Consider therapy modification Alpha-/Beta-Agonists: Ergot Derivatives may enhance the hypertensive effect of Alpha-/Beta-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha-/Beta-Agonists. Avoid combination Alpha1-Agonists: Ergot Derivatives may enhance the hypertensive effect of Alpha1-Agonists. Ergot Derivatives may enhance the vasoconstricting effect of Alpha1-Agonists. Avoid combination Antiemetics (5HT3 Antagonists): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy Antihepaciviral Combination Products: May increase the serum concentration of Ergot Derivatives. Avoid combination Anti-Parkinson Agents (Monoamine Oxidase Inhibitor): May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Monitor for signs and symptoms of serotonin syndrome/serotonin toxicity if selegiline, rasagiline, or safinamide is combined with a serotonin modulator. Use of transdermal selegiline with serotonin modulators is contraindicated. Consider therapy modification Antipsychotic Agents: Serotonin Modulators may enhance the adverse/toxic effect of Antipsychotic Agents. Specifically, serotonin modulators may enhance dopamine blockade, possibly increasing the risk for neuroleptic malignant syndrome. Antipsychotic Agents may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy Aprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy AtoMOXetine: May enhance the hypertensive effect of Sympathomimetics. AtoMOXetine may enhance the tachycardic effect of Sympathomimetics. Monitor therapy Beta-Blockers: May enhance the vasoconstricting effect of Ergot Derivatives. Consider therapy modification Boceprevir: May increase the serum concentration of Ergotamine. Avoid combination Cannabinoid-Containing Products: May enhance the tachycardic effect of Sympathomimetics. Exceptions: Cannabidiol. Monitor therapy Chloroprocaine: May enhance the hypertensive effect of Ergot Derivatives. Monitor therapy Ciprofloxacin (Systemic): May increase the serum concentration of Caffeine. Monitor therapy Clarithromycin: May increase the serum concentration of Ergotamine. Avoid combination CloZAPine: CYP1A2 Inhibitors (Weak) may increase the serum concentration of CloZAPine. Monitor therapy Cobicistat: May increase the serum concentration of Ergotamine. Avoid combination Cocaine: May enhance the hypertensive effect of Sympathomimetics. Management: Consider alternatives to use of this combination when possible. Monitor closely for substantially increased blood pressure or heart rate and for any evidence of myocardial ischemia with concurrent use. Consider therapy modification Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination Crizotinib: May increase the serum concentration of Ergotamine. Avoid combination CYP1A2 Inhibitors (Moderate): May decrease the metabolism of CYP1A2 Substrates (High risk with Inhibitors). Monitor therapy CYP1A2 Inhibitors (Strong): May decrease the metabolism of CYP1A2 Substrates (High risk with Inhibitors). Consider therapy modification CYP3A4 Inhibitors (Moderate): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy CYP3A4 Inhibitors (Strong): May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Consider therapy modification Dapoxetine: May enhance the adverse/toxic effect of Serotonin Modulators. Avoid combination Dasatinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy Deferasirox: May increase the serum concentration of CYP1A2 Substrates (High risk with Inhibitors). Monitor therapy Doxofylline: Caffeine and Caffeine Containing Products may enhance the adverse/toxic effect of Doxofylline. Avoid combination Enzalutamide: May decrease the serum concentration of Ergotamine. Avoid combination Formoterol: Caffeine and Caffeine Containing Products may enhance the adverse/toxic effect of Formoterol. Caffeine and Caffeine Containing Products may enhance the hypokalemic effect of Formoterol. Monitor therapy Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination Guanethidine: May enhance the arrhythmogenic effect of Sympathomimetics. Guanethidine may enhance the hypertensive effect of Sympathomimetics. Monitor therapy Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination Indacaterol: Caffeine and Caffeine Containing Products may enhance the adverse/toxic effect of Indacaterol. Caffeine and Caffeine Containing Products may enhance the hypokalemic effect of Indacaterol. Monitor therapy Iobenguane I 123: Sympathomimetics may diminish the therapeutic effect of Iobenguane I 123. Avoid combination Iohexol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iohexol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iohexol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants. Consider therapy modification Iomeprol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iomeprol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iomeprol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants. Consider therapy modification Iopamidol: Agents With Seizure Threshold Lowering Potential may enhance the adverse/toxic effect of Iopamidol. Specifically, the risk for seizures may be increased. Management: Discontinue agents that may lower the seizure threshold 48 hours prior to intrathecal use of iopamidol. Wait at least 24 hours after the procedure to resume such agents. In nonelective procedures, consider use of prophylactic anticonvulsants. Consider therapy modification Itraconazole: May increase the serum concentration of Ergotamine. Avoid combination Ketoconazole (Systemic): May increase the serum concentration of Ergotamine. Avoid combination Letermovir: May increase the serum concentration of Ergot Derivatives. Avoid combination Linezolid: May enhance the hypertensive effect of Sympathomimetics. Management: Reduce initial doses of sympathomimetic agents, and closely monitor for enhanced pressor response, in patients receiving linezolid. Specific dose adjustment recommendations are not presently available. Consider therapy modification Linezolid: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Management: Due to a risk of serotonin syndrome/serotonin toxicity, discontinue serotonin modulators 2 weeks prior to the administration of linezolid. If urgent initiation of linezolid is needed, discontinue serotonin modulators immediately and monitor closely. Consider therapy modification Lithium: Caffeine and Caffeine Containing Products may decrease the serum concentration of Lithium. Monitor therapy Lorcaserin: May enhance the adverse/toxic effect of Ergot Derivatives. Specifically, use of these drugs together may increase the risk of developing valvular heart disease. Lorcaserin may enhance the serotonergic effect of Ergot Derivatives. This could result in serotonin syndrome. Avoid combination Macrolide Antibiotics: May increase the serum concentration of Ergot Derivatives. Cabergoline and Clarithromycin may interact, see specific monograph for full details. Exceptions: Azithromycin (Systemic); Fidaxomicin; Spiramycin. Consider therapy modification Metaxalone: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy Methylene Blue: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Avoid combination Methylphenidate: May enhance the adverse/toxic effect of Serotonin Modulators. Specifically, the risk of serotonin syndrome or serotonin toxicity may be increased. Monitor therapy Metoclopramide: Serotonin Modulators may enhance the adverse/toxic effect of Metoclopramide. This may be manifest as symptoms consistent with serotonin syndrome or neuroleptic malignant syndrome. Monitor therapy MiFEPRIStone: May increase the serum concentration of Ergotamine. Management: Avoid ergotamine during and 2 weeks following mifepristone for treatment of hyperglycemia in Cushing's syndrome. The interaction magnitude could be lower with single doses used to terminate pregnancy, but neither effect has been studied clinically. Avoid combination Netupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy Nitroglycerin: Ergot Derivatives may diminish the vasodilatory effect of Nitroglycerin. This is of particular concern in patients being treated for angina. Nitroglycerin may increase the serum concentration of Ergot Derivatives. Avoid combination Norfloxacin: May increase the serum concentration of Caffeine and Caffeine Containing Products. Monitor therapy Obeticholic Acid: May increase the serum concentration of CYP1A2 Substrates (High risk with Inhibitors). Monitor therapy Olodaterol: Caffeine and Caffeine Containing Products may enhance the adverse/toxic effect of Olodaterol. Caffeine and Caffeine Containing Products may enhance the hypokalemic effect of Olodaterol. Monitor therapy Opioid Analgesics: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy Palbociclib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy Peginterferon Alfa-2b: May increase the serum concentration of CYP1A2 Substrates (High risk with Inhibitors). Monitor therapy Pipemidic Acid: May increase the serum concentration of Caffeine and Caffeine Containing Products. Monitor therapy Posaconazole: May increase the serum concentration of Ergotamine. Avoid combination Protease Inhibitors: May increase the serum concentration of Ergot Derivatives. Avoid combination Reboxetine: May enhance the hypertensive effect of Ergot Derivatives. Monitor therapy Regadenoson: Caffeine and Caffeine Containing Products may diminish the vasodilatory effect of Regadenoson. Management: Avoiding using caffeine or other methylxanthine containing products (e.g., theophylline) for at least 12 hours prior to the administration of regadenoson. Consider therapy modification Roxithromycin: May increase the serum concentration of Ergot Derivatives. Avoid combination Serotonin 5-HT1D Receptor Agonists: Ergot Derivatives may enhance the vasoconstricting effect of Serotonin 5-HT1D Receptor Agonists. Serotonin 5-HT1D Receptor Agonists may enhance the vasoconstricting effect of Ergot Derivatives. Avoid combination Serotonin Modulators: May enhance the adverse/toxic effect of other Serotonin Modulators. The development of serotonin syndrome may occur. Exceptions: Nicergoline; Tedizolid. Monitor therapy Simeprevir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy Stiripentol: May increase the serum concentration of Caffeine and Caffeine Containing Products. Avoid combination Sympathomimetics: May enhance the adverse/toxic effect of other Sympathomimetics. Monitor therapy Tedizolid: May enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy Tedizolid: May enhance the hypertensive effect of Sympathomimetics. Tedizolid may enhance the tachycardic effect of Sympathomimetics. Monitor therapy Telaprevir: May increase the serum concentration of Ergotamine. Avoid combination Teriflunomide: May decrease the serum concentration of Caffeine and Caffeine Containing Products. Monitor therapy TiZANidine: CYP1A2 Inhibitors (Weak) may increase the serum concentration of TiZANidine. Management: Avoid these combinations when possible. If combined use is necessary, initiate tizanidine at an adult dose of 2 mg and increase in 2 to 4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions. Consider therapy modification TraMADol: Serotonin Modulators may enhance the adverse/toxic effect of TraMADol. The risk of seizures may be increased. TraMADol may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Monitor therapy Vemurafenib: May increase the serum concentration of CYP1A2 Substrates (High risk with Inhibitors). Management: Consider alternatives to such combinations whenever possible, particularly if the CYP1A2 substrate has a relatively narrow therapeutic index. Consider therapy modification Voriconazole: May increase the serum concentration of Ergotamine. Avoid combination Adverse Reactions Frequency not defined. Cardiovascular: Bradycardia, cold extremities, ECG changes, edema, hypertension, ischemia, tachycardia, valvular sclerosis, vasospasm Central nervous system: Numbness, paresthesia, precordial pain, vertigo Dermatologic: Gangrene of skin or other tissue, pruritus Gastrointestinal: Anal fissure (with overuse of suppository), nausea, rectal ulcer (with overuse of suppository), vomiting Genitourinary: Retroperitoneal fibrosis Neuromuscular & skeletal: Myalgia, weakness Respiratory: Cyanosis, pleuropulmonary fibrosis ALERT: U.S. Boxed Warning Concurrent drug therapy: Serious and/or life-threatening peripheral ischemia has been associated with the coadministration of ergotamine/caffeine with potent CYP 3A4 inhibitors including protease inhibitors and macrolide antibiotics. Because CYP 3A4 inhibition elevates the serum levels of ergotamine/caffeine, the risk for vasospasm leading to cerebral ischemia and/or ischemia of the extremities is increased. Hence, concomitant use of these medications is contraindicated. Warnings/Precautions Concerns related to adverse effects: Cardiac valvular fibrosis: Ergot alkaloids have been associated (rarely) with fibrotic valve thickening (eg, aortic, mitral, tricuspid); usually associated with long-term, chronic use. Cardiovascular effects: Vasospasm or vasoconstriction can occur, possibly resulting in cyanosis, decreased cerebral blood flow, bradycardia or tachycardia, asystole, and hypertension; sustained vasoconstriction may also lead to intermittent claudication, precordial distress, and pain. Do not use in any patient at risk or predisposed to vascular effects of ergot alkaloids. Ergotism: Ergot alkaloid use may result in ergotism (intense vasoconstriction) resulting in peripheral vascular ischemia and possible gangrene. Ergotism is usually associated with overdosage or prolonged chronic use; do not exceed dosing guidelines and avoid prolonged administration. Pleural/retroperitoneal fibrosis: Rare cases of pleural and/or retroperitoneal fibrosis have been reported with prolonged daily administration. Concurrent drug therapy issues: CYP3A4 inhibitors: [U.S. Boxed Warning]: Ergot alkaloids are contraindicated with potent inhibitors of CYP3A4 (includes protease inhibitors and some macrolide antibiotics). Serum levels of ergotamines may be elevated, leading to increased risk of vasospasm leading to cerebral ischemia and/or ischemia of extremities. Serious and/or life-threatening peripheral ischemia has been associated with concomitant use. Drug-drug interactions: Additional potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information. Special populations: Elderly: Avoid use in the elderly due to the vasoconstrictive properties and cardiovascular adverse effects associated with ergot alkaloids. Dosage form specific issues: Rectal suppositories: Solitary rectal or anal ulcers have occurred rarely when suppositories are used in higher than recommended doses or with continual use of recommended doses for prolonged periods of time. After discontinuation, spontaneous healing occurs within 4 to 8 weeks. Other warnings/precautions: Appropriate use: Do not use for prolonged daily administration; serious adverse effects are associated with long-term continuous use. Use caution and remain within recommended dosage limits. Medication-overuse headache/Withdrawal: Discontinuation even after limited use may result in withdrawal symptoms (ie, rebound headache, nausea, vomiting). Monitoring Parameters BUN, serum creatinine, liver function tests at baseline, signs of peripheral ischemia (eg, vasospasm, digit coldness, and pallor), numbness, muscle pains, extremity weakness, chest pain, tachycardia or bradycardia, hypersensitivity reactions. Pregnancy Risk Factor X Pregnancy Considerations Animal reproduction studies have not been conducted with this combination. Ergotamine and caffeine both cross the placenta and may cause prolonged constriction of the uterine vessels and/or increased myometrial tone leading to reduced placental blood flow. Use is contraindicated in pregnant women. Patient Education Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?) Patient may experience nausea or vomiting. Have patient report immediately to prescriber angina, bradycardia, tachycardia, abnormal heartbeat, edema, severe dizziness, passing out, severe headache, vision changes, muscle weakness, muscle pain, change in color of hands or feet from pale to blue or red, burning or numbness of hands or feet, rectal sores, rectal pain, or wounds on fingers or toes (HCAHPS). Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions. Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients. Print this page} Recently Approved Lonhala Magnair Lonhala Magnair (glycopyrrolate) is a long-acting muscarinic antagonist (LAMA) bronchodilator for... Ozempic Ozempic (semaglutide) is a glucagon-like peptide-1 (GLP-1) analog administered once-weekly for the... Ogivri Ogivri (trastuzumab-dkst) is a HER2 / neu receptor antagonist biosimilar to Herceptin indicated for... Sublocade Sublocade (buprenorphine) is a once-monthly injectable partial opioid agonist formulation for the... More} } past love
treatments Ergotamine and Caffeine land up
EmoticonEmoticon