title: Pharmacokinetics of ropivacaine in uremic and nonuremic patients after axillary brachial plexus block.
abstract: Reports on the efficacy and pharmacokinetics of local anesthetics in uremic patients have been controversial. Our study involved 29 uremic and 28 nonuremic patients. We performed axillary block with ropivacaine 300 mg (50 mL). Venous blood samples were drawn for 24 h for assay of total and unbound plasma ropivacaine, 3-hydroxyropivacaine, pipecoloxylidide (PPX), and serum alpha(1)-acid glycoprotein (AAG). Block quality was similar in both groups. No toxicity occurred. Plasma clearance of ropivacaine was smaller and the area under the concentration-time curve of ropivacaine, 3-hydroxyropivacaine, and PPX larger in the uremic patients. The plasma concentration of PPX increased until 24 h in uremic patients whose AAG concentrations were also larger throughout the study. The free fraction of ropivacaine in plasma was smaller in the uremic group when measured 60 min and 12 h after the block, but the unbound concentration of ropivacaine was larger in the uremic group at 12 h. Enhanced absorption of ropivacaine into circulation, increased binding to AAG, and probably reduced urinary excretion of the metabolites lead to larger total plasma concentrations of ropivacaine and its main metabolites in uremic patients.
authors.affiliation: Department of Anesthesiology and Intensive Care Medicine, Helsinki University Central Hospital, Helsinki, Finland. pertti.pere@hus.fi
authors.forename: Pertti
authors.initials: P
authors.lastname: Pere
authors.forename: Merja
authors.initials: M
authors.lastname: Salonen
authors.forename: Mika
authors.initials: M
authors.lastname: Jokinen
authors.forename: Per H
authors.initials: PH
authors.lastname: Rosenberg
authors.forename: Pertti J
authors.initials: PJ
authors.lastname: Neuvonen
authors.forename: Juhani
authors.initials: J
authors.lastname: Haasio
mesh_terms: D000368:Aged; D000577:Amides / Q000097:blood / Q000493:pharmacokinetics*; D000779:Anesthetics, Local / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001711:Biotransformation; D001917:Brachial Plexus; D002045:Bupivacaine / Q000031:analogs & derivatives* / Q000097:blood; D005260:Female; D005542:Forearm / Q000294:innervation; D006225:Hand / Q000294:innervation; D018737:Hand Strength / Q000502:physiology; D006801:Humans; D008297:Male; D008875:Middle Aged; D009407:Nerve Block; D009961:Orosomucoid / Q000378:metabolism; D010147:Pain Measurement / Q000187:drug effects; D011485:Protein Binding; D000077212:Ropivacaine; D014511:Uremia / Q000378:metabolism*
chemical_list: D000577:Amides; D000779:Anesthetics, Local; D009961:Orosomucoid; D000077212:Ropivacaine; C025149:2',6'-pipecoloxylidide; D002045:Bupivacaine