Ergotamine:(6aR,9R)-N-((2R,5S,10aS,10bS)- 5-benzyl-10b-hydroxy-2-methyl- 3,6-dioxooctahydro-2H-oxazolo[3,2-a] pyrrolo[2,1-c]pyrazin-2-yl) -7-methyl-4,6,6a,7,8,9-hexahydroindolo[4,3-fg] quinoline-9-carboxamide
Caffeine:1,3,7-trimethyl-1H-purine-2,6(3H,7H)-dione
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Ergotamine: Absorption Poorly absorbed following GI and SL administration.
Metabolism Metabolized by the liver.
Elimination T ½ is approximately 2 h; 90% of metabolites are excreted in the bile. Unmetabolized ergotamine is erratically excreted in the saliva and trace amounts are excreted in the feces and urine.
Caffeine: Absorption 99% absorbed orally. C max is 5 to 25 mcg/mL; T max is 15 to 120 min.
Distribution Rapidly distributed throughout tissues; crosses the blood-brain barrier and placenta; excreted in breast milk. 17% to 36% protein bound. Vd is 0.64 kg.
Metabolism Rapidly metabolized in the liver to 1-methyluric acid, 1-methylxanthine, and 7-methylxanthine; CYP1A2 is involved in the biotransformation.
Elimination The t ½ is 3 to 5 h. Approximately 1% is excreted in the urine as unchanged drug.
Special Populations Pregnancy, smoking, and cirrhosis The t ½ is increased.
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