CAFERGOT- ergotamine tartrate and caffeine tablet, film coated
Serious and/or life-threatening peripheral ischemia has been associated with the coadministration of CAFERGOT® with potent CYP 3A4 inhibitors including protease inhibitors and macrolide antibiotics. Because CYP 3A4 inhibition elevates the serum levels of CAFERGOT®, the risk for vasospasm leading to cerebral ischemia and/or ischemia of the extremities is increased. Hence, concomitant use of these medications is contraindicated (see also CONTRAINDICATIONS and WARNINGS section).
Each tablet for oral administration contains 1 mg ergotamine tartrate, USP, and 100 mg caffeine, USP.
Ergotamine Tartrate Chemical Structure
(click image for full-size original)
Ergotaman-3?,6?,18-trione, 12?-hydroxy-2?-methyl-5?-(phenyl-methyl)-,(5? ?)-, [R-(R*,R*)]-2,3-dihydroxy-butanedioate (2:1) (salt).
Caffeine Chemical Structure
1H -Purine-2,6-dione, 3,7-dihydro-1,3,7-trimethyl-.
Inactive ingredients include black iron oxide, compressible sugar, iron oxide red, magnesium stearate, microcrystalline cellulose, polyethylene glycol, polyvinyl alcohol, sodium starch glycolate, talc, titanium dioxide and yellow iron oxide.
Ergotamine is an alpha adrenergic blocking agent with a direct stimulating effect on the smooth muscle of peripheral and cranial blood vessels and produces depression of central vasomotor centers. The compound also has the properties of serotonin antagonism. In comparison to hydrogenated ergotamine, the adrenergic blocking actions are less pronounced and vasoconstrictive actions are greater.
Caffeine, also a cranial vasoconstrictor, is added to further enhance the vasoconstrictive effect without the necessity of increasing ergotamine dosage.
Many migraine patients experience excessive nausea and vomiting during attacks, making it impossible for them to retain any oral medication. In such cases, therefore, the only practical means of medication is through the rectal route where medication may reach the cranial vessels directly, evading the splanchnic vasculature and the liver.