Population pharmacokinetic analysis of ropivacaine and its metabolite 2′,6′-pipecoloxylidide from pooled data in neonates, infants, and children

British Journal of Anaesthesia

Volumn 107, Issue 3, 2011, Pages 409-424

  Aarons, L ^a   Sadler, B ^b   Pitsiu, M ^b   Sjovall J ^c   Henriksson, J ^d   Molnar V ^e  

^a UNIVERSITY OF MANCHESTER   (United Kingdom)

^b ICON Development Solutions   (United States)

^c ASTRAZENECA R AND D   (Sweden)

^d ASTRAZENECA R AND D   (Sweden)

^e Clinical Pharmacology Consulting Ltd   (Australia)

Author keywords

local anaesthetics; metabolite kinetics; paediatric anaesthesia; population pharmacokinetics; regional anaesthetic techniques; ropivacaine

Indexed keywords

2',6' PIPECOLOXYLIDIDE; OROSOMUCOID; ROPIVACAINE; UNCLASSIFIED DRUG;

ARTICLE; CAUDAL ANESTHESIA; CHILD; CONTINUOUS INFUSION; DRUG BINDING; DRUG BLOOD LEVEL; DRUG EXCRETION; DRUG HALF LIFE; DRUG METABOLISM; FEMALE; GROUPS BY AGE; HUMAN; INFANT; MAJOR CLINICAL STUDY; MALE; MODEL; NEWBORN; PEDIATRIC ANESTHESIA; PRESCHOOL CHILD; PRIORITY JOURNAL; RECOMMENDED DRUG DOSE; SCHOOL CHILD; URINARY EXCRETION;

EID: 80051775860     PISSN: 00070912     EISSN: 14716771     Source Type: Journal    
DOI: 10.1093/bja/aer154     Document Type: Article

References (40)

1. Knudsen K, Beckman Suurkula M, Blomberg S, Sjovall J, Edvardsson N. Central nervous and cardiovascular effects of i.v. infusions of ropivacaine, bupivacaine, and placebo in volunteers. Br J Anaesth 1997;78:507-14 (Pubitemid 27226361)
2. Groban L, Deal DD, Vernon JC, James RL, Butterworth J. Cardiac resuscitation after incremental overdosage with lidocaine, bupivacaine, levobupivacaine, and ropivacaine in anesthetized dogs. Anesth Analg 2001;92:37-43 (Pubitemid 32039174)
3. Zaric D, Nydahl PA, Philipson L, Samuelsson L, Heierson A, Axelsson K. The effect of continuous lumbar epidural infusion of ropivacaine (0.1%, 0.2%, and 0.3%) and 0.25% bupivacaine on sensory and motor block in volunteers: a double-blind study. Reg Anesth 1996;21:14-25 (Pubitemid 26042520)
4. Ekström G, Gunnarsson UB. Ropivacaine, a new amide-type local anesthetic agent, is metabolized by cytochromes P450 1A and 3A in human liver microsomes. Drug Metab Dispos 1996;24:955-61 (Pubitemid 26314546)
5. Halldin MM, Bredberg E, Angelin B, et al. Metabolism and excretion of ropivacaine in humans. Drug Metab Dispos 1996;24:962-8 (Pubitemid 26314547)
6. Lönnqvist PA, Westrin P, Larsson BA, et al. Ropivacaine pharmacokinetics after caudal block in 1-8 year old children. Br J Anaesth 2000;85:506-11
7. Burm AG, Stienstra R, Brouwer RP, Emanuelsson BM, van Kleef JW. Epidural infusion of ropivacaine for postoperative analgesia after major orthopedic surgery: pharmacokinetic evaluation. Anesthesiology 2000;93:395-403 (Pubitemid 30620312)
8. Ekatodramis G, Borgeat A, Huledal G, Jeppsson L, Westman L, Sjovall J. Continuous interscalene analgesia with ropivacaine 2 mg/ml after major shoulder surgery. Anesthesiology 2003;98:143-50 (Pubitemid 36043420)
9. Tucker GT. Safety in numbers. The role of pharmacokinetics in local anesthetic toxicity: the 1993 ASRA Lecture. Reg Anesth 1994;19:155-63
10. Luz G, Wieser C, Innerhofer P, Frischhut B, Ulmer H, Benzer A. Free and total bupivacaine plasma concentrations after continuous epidural anaesthesia in infants and children. Paediatr Anaesth 1998;8:473-8 (Pubitemid 28523407)
11. McCloskey JJ, Haun SE, Deshpande JK. Bupivacaine toxicity secondary to continuous caudal epidural infusion in children. Anesth Analg 1992;75:287-90
12. Booker PD, Taylor C, Saba G. Perioperative changes in alpha 1-acid glycoprotein concentrations in infants undergoing major surgery. Br J Anaesth 1996;76:365-8 (Pubitemid 26068826)
13. Erichsen CJ, Sjovall J, Kehlet H, Hedlund C, Arvidsson T. Pharmacokinetics and analgesic effect of ropivacaine during continuous epidural infusion for postoperative pain relief. Anesthesiology 1996;84:834-42 (Pubitemid 26105246)
14. Arlander E, Ekstrom G, Alm C, et al. Metabolism of ropivacaine in humans is mediated by CYP1A2 and to a minor extent by CYP3A4: an interaction study with fluvoxamine and ketoconazole as in vivo inhibitors. Clin Pharmacol Ther 1998;64:484-91 (Pubitemid 28531592)
15. Benet LZ, Hoener BA. Changes in plasma protein binding have little clinical relevance. Clin Pharmacol Ther 2002;71:115-21 (Pubitemid 34271114)
16. Berde CB, Yaster M, Meretoja O, et al. Stable plasma concentrations of unbound ropivacaine during postoperative epidural infusion for 24-72 hours in children. Eur J Anaesthesiol 2008;25:410-7 (Pubitemid 351465527)
17. Bösenberg AT, Thomas J, Cronje L, et al. Pharmacokinetics and efficacy of ropivacaine for continuous epidural infusion in neonates and infants. Paediatr Anaesth 2005;15:739-49 (Pubitemid 43960890)
18. Bösenberg AT, Thomas J, Lopez T, Huledal G, Jeppsson L, Larsson LE. Plasma concentrations of ropivacaine following a single-shot caudal block of 1, 2 or 3 mg kg21 in children. Acta Anaesthesiol Scand 2001;45:1276-80 (Pubitemid 33063415)
19. Rapp HJ, Molnar V, Austin S, et al. Ropivacaine in neonates and infants: a population pharmacokinetic evaluation following single caudal block. Paediatr Anaesth 2004;14:724-32 (Pubitemid 39223083)
20. Dalens B, Ecoffey C, Joly A, et al. Pharmacokinetics and analgesic effect of ropivacaine following ilioinguinal/iliohypogastric nerve block in children. Paediatr Anaesth 2001;11:415-20 (Pubitemid 32635318)
21. Beal S, Sheiner LB, Boeckmann A, Bauer RJ. NONMEM User's Guides. (1989-2009). Ellicott City, MD: Icon Development Solutions, 2009
22. Engle WA. Age terminology during the perinatal period. Pediatrics 2004;114:1362-4 (Pubitemid 41647702)
23. Grasela T, Sheiner L. Pharmacostatistical modeling for observational data. J Pharmacokinet Biopharm 1991;19:25s-6s
24. Anderson BJ, van Lingen RA, Hansen TG, Lin YC, Holford NH. Acetaminophen developmental pharmacokinetics in premature neonates and infants: a pooled population analysis. Anesthesiology 2002;96:1336-45 (Pubitemid 34587201)
25. Bouwmeester NJ, Anderson BJ, Tibboel D, Holford NH. Developmental pharmacokinetics of morphine and its metabolites in neonates, infants and young children. Br J Anaesth 2004;92:208-17 (Pubitemid 38159658)
26. Holford NH. The visual predictive check-superiority to standard diagnostic (Rorschach) plots. Population Approach Group in Europe (PAGE), Pamplona, Spain, 2005. Available from www.page-meeting.org/?abstract=738
27. Seta N, Chalan-Belval I, de Crepy A, Giai-Brueri M, Feger J, Durand G. Comparison of glycan microheterogeneities of alpha1-acid glycoprotein between mothers and their newborns, alpha1-acid glycoprotein. Progr Clin Biol Res 1989;300:139-42
28. Müller W. Drug binding sites of human a-1-acid glycoprotein, alpha1-acid glycoprotein. Progr Clin Biol Res 1989;300:363-78
29. UK Medicines and Healthcare Products Regulatory Agency (MHRA), European Medicines Agency (EMEA). electronic Medicines Compendium (eMC). Available from thttp://www.medicines.org.uk/EMC/searchresults.aspx?term=ropivacaine& searchtype=QuickSearch (accessed November 20, 2010)
30. Hansen TG, Ilett KF, Reid C, Lim SI, Hackett LP, Bergesio R. Caudal ropivacaine in infants: population pharmacokinetics and plasma concentrations. Anesthesiology 2001;94:579-84 (Pubitemid 32249615)
31. Alcorn J, McNamara PJ. Ontogeny of hepatic and renal systemic clearance pathways in infants: part I. Clin Pharmacokinet 2002;41:959-98 (Pubitemid 35168438)
32. Van Obbergh LJ, Roelants FA, Veyckemans F, Verbeeck RK. In children, the addition of epinephrine modifies the pharmacokinetics of ropivacaine injected caudally. Can J Anaesth 2003;50:593-8 (Pubitemid 37038477)
33. Tod M, Jullien V, Pons G. Facilitation of drug evaluation in children by population methods and modelling. Clin Pharmacokinet 2008;47:231-43 (Pubitemid 351367434)
34. Anderson BJ, Holford NH. Mechanism-based concepts of size and maturity in pharmacokinetics. Ann Rev Pharmacol Toxicol 2008;48:303-32 (Pubitemid 351738156)
35. Emanuelsson BM, Persson J, Sandin S, Alm C, Gustafsson LL. Intraindividual and interindividual variability in the disposition of the local anesthetic ropivacaine in healthy subjects. Ther Drug Monitor 1997;19:126-31 (Pubitemid 28056021)
36. Habre W, Bergesio R, Johnson C, Hackett P, Joyce D, Sims C. Pharmacokinetics of ropivacaine following caudal analgesia in children. Paediatr Anaesth 2000;10:143-7 (Pubitemid 30148638)
37. McCann ME, Sethna NF, Mazoit JX, et al. The pharmacokinetics of epidural ropivacaine in infants and young children. Anesth Analg 2001;93:893-7 (Pubitemid 32905974)
38. Chalkiadis GA, Anderson BJ, Tay M, Bjorksten A, Kelly JJ. Pharmacokinetics of levobupivacaine after caudal epidural administration in infants less than 3 months of age. Br J Anaesth 2005;95:524-9 (Pubitemid 41418750)
39. Irestedt L, Ekblom A, Olofsson C, Dahlstrom AC, Emanuelsson BM. Pharmacokinetics and clinical effect during continuous epidural infusion with ropivacaine 2.5 mg/ml or bupivacaine 2.5 mg/ml for labour pain relief. Acta Anaesthesiol Scand 1998;42:890-6 (Pubitemid 28416858)
40. Datta S, Camann W, Bader A, VanderBurgh L. Clinical effects and maternal and fetal plasma concentrations of epidural ropivacaine versus bupivacaine for cesarean section. Anesthesiology 1995;82:1346-52