Pharmacokinetics, metabolism, and renal excretion of articaine and its metabolite articainic acid in patients after epidural administration.
Articaine is metabolized into articainic acid. The half-lives of articaine are 0.54 +/- 0.05 and 2.44 +/- 0.30 h and that of its metabolite, 2.44 +/- 0.30 h. Of the administered dose approximately 2-5% is excreted unchanged, 40-70% is excreted as articainic acid, and 4-15% as articainic acid glucoronide. The percentage of the total dose recovered in the urine varies between 50% and 91%. Protein binding of articaine in patients varies between 50% and 70%, and that of articainic acid between 60% and 90%. Renal clearance of articaine varies between 12 and 28 ml min-1, while that of articainic acid is between 84 and 160 ml min-1.
van Oss
G E
GE
Department of Anesthesiology, Hervormd Diaconessen Huis, Arnhem, The Netherlands.
Vree
T B
TB
Baars
A M
AM
Termond
E F
EF
Booij
L H
LH
D000368:Aged; D000767:Anesthesia, Epidural; D000777:Anesthetics / Q000378:metabolism* / Q000493:pharmacokinetics / Q000652:urine; D002355:Carticaine / Q000031:analogs & derivatives / Q000378:metabolism* / Q000493:pharmacokinetics / Q000652:urine; D005260:Female; D006207:Half-Life; D006801:Humans; D007668:Kidney / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D011485:Protein Binding; D013876:Thiophenes / Q000378:metabolism*
D000777:Anesthetics; D013876:Thiophenes; C055853:2-carboxyarticaine; D002355:Carticaine