Adult: Available preparation:
Ergotamine 1 mg and caffeine 100 mg
Initially, 2 tab at onset of attack, then 1 tab every 30 min, if necessary. Max: 6 tab/day; 10 tab/wk.
Rectal Acute migraine attacks
Adult: Available preparation:
Ergotamine 2 mg and caffeine 100 mg
Initially, 1 supp at onset of attack, then 1 supp after 1 hr, if necessary. Max: 2 supp/day; 5 supp/wk.
Renal Impairment
Severe: Contraindicated.
Hepatic Impairment
Severe: Contraindicated.
Administration
May be taken with or without food.
Contraindications
Peripheral vascular disease, obliterative vascular disease, CHD, HTN, septic condition e.g. shock, temporal arteritis, hemiplegic or basilar migraine. Concomitant use w/ potent CYP3A4 inhibitors (e.g. azole antifungals, protease inhibitors, macrolide antibiotics. Severe renal and hepatic impairment. Pregnancy and lactation.
This drug may cause visual disturbances, dizziness, or other CNS disturbances, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor BUN, serum creatinine, LFT.
Overdosage
Symptoms: Nausea, vomiting, drowsiness, confusion, tachycardia, dizziness, resp depression, hypotension, convulsion, shock, coma, symptoms and complications of ergotism. Management: Symptomatic and supportive treatment. Employ activated charcoal. Gastric lavage may be considered for recent ingestion. Maintain adequate pulmonary ventilation, correction of hypotension and control or BP and convulsions. Keep the extremities warm to treat peripheral vasospasm. Vasodilators may be beneficial.
Increased serum concentration w/ grapefruit and grapefruit juice.
Action
Description: Ergotamine is an ergot alkaloid that has marked vasoconstrictor effects and partial agonistic action at serotonin (5-HT) receptors. It causes central vasomotor depression, stimulates vasoconstriction of peripheral smooth muscles and cranial blood vessels thus alleviating migraine. It also has significant oxytocic action on the uterus.
Caffeine is a methylxanthine that inhibits phosphodiesterase enzyme causing increased levels of intracellular cyclic 3’,5’-adenosine monophosphate(cAMP). It enhances vasoconstrictive effect and increases ergotamine enteral absorption. It also exerts analgesic activity by blocking peripheral pronociceptive action of adenosine and activating central noradrenergic pathway that constitute endogenous pain suppressing system. Additionally, it antagonises central adenosine receptors thus stimulating the CNS and resp center, producing wakefulness, increased mental activity, increased rate and depth of respiration. Pharmacokinetics: Absorption: Ergotamine: Poorly absorbed from the GI tract. Bioavailability: Approx ≤5%. Time to peak plasma concentration: W/in 0.5-3 hr.
Caffeine: Well absorbed from the GI tract (oral); slow and erratic (rectal). Time to peak plasma concentration: 30-120 min. Distribution: Crosses blood-brain barrier and enters breast milk.
Ergotamine: Plasma protein binding: Approx 93-98%.
Caffeine: Rapidly distributed throughout the body tissues. Crosses placenta. Volume of distribution: 0.6 L/kg. Plasma protein binding: Approx 17-36%. Metabolism: Ergotamine: Undergoes extensive metabolism in the liver by CYP3A4 isoenzyme including first-pass effect.
Caffeine: Rapidly metabolised in the liver into 1-methyluric acid, 1-methylxanthine and 7-methylxanthine metabolites. Excretion: Ergotamine: Via faeces (90%, mainly as metabolites); urine (approx 4%). Elimination half-life: Biphasic: Approx 2 hr (initial phase); 21 hr (terminal phase).
Caffeine: Via urine (1% as unchanged drug). Elimination half-life: 3-5 hr.
Chemical Structure
Ergotamine Source: National Center for Biotechnology Information. PubChem Database. Ergotamine, CID=8223, https://pubchem.ncbi.nlm.nih.gov/compound/Ergotamine (accessed on Jan. 22, 2020)
Caffeine Source: National Center for Biotechnology Information. PubChem Database. Caffeine, CID=2519, https://pubchem.ncbi.nlm.nih.gov/compound/Caffeine (accessed on Jan. 22, 2020)
Storage
Tab: Store below 25°C. Protect from light. Supp: Store between 2-8°C.
N02CA52 - ergotamine, combinations excl. psycholeptics ; Belongs to the class of ergot alkaloids preparations. Used to relieve migraine.
References
AFT Pharmaceuticals Ltd. Cafergot Tablets data sheet 24 Nov 2016. Medsafe. http://www.medsafe.govt.nz/. Accessed 31/07/2017.Anon. Ergotamine and Caffeine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 31/07/2017.Buckingham R (ed). Caffeine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 31/07/2017.Buckingham R (ed). Ergotamine Tartrate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 31/07/2017.McEvoy GK, Snow EK, Miller J et al (eds). Caffeine; Caffeine and Sodium Benzoate Injection; Caffeine, Citrated. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 31/07/2017.McEvoy GK, Snow EK, Miller J et al (eds). Ergotamine Tartrate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 31/07/2017.Migergot Suppository (Crealta Pharmaceuticals LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 31/07/2017.
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