Pharmacokinetics of Local Anaesthetics in Infants and Children

Clinical Pharmacokinetics

Volumn 43, Issue 1, 2004, Pages 17-32

  Mazoit, Jean Xavier ^a   Dalens, Bernard J ^b  

^a BICÊTRE HOSPITAL   (France)

^b UNIVERSITY HOSPITAL OF CLERMONT FERRAND   (France)

Author keywords

[No Author keywords available]

Indexed keywords

ADRENALIN; AMIDE; BUPIVACAINE; ETIDOCAINE; LEVOBUPIVACAINE; LIDOCAINE; LOCAL ANESTHETIC AGENT; OROSOMUCOID; ROPIVACAINE; TETRACAINE;

ABSORPTION; CARDIOTOXICITY; CAUDA EQUINA SYNDROME; CENTRAL NERVOUS SYSTEM; CLINICAL FEATURE; CLINICAL TRIAL; DRUG BLOOD LEVEL; ERYTHROCYTE; HEART FUNCTION; HUMAN; LOCAL ANESTHESIA; NEUROTOXICITY; PHYSICAL CHEMISTRY; POSTOPERATIVE PERIOD; PRIORITY JOURNAL; PROTEIN BINDING; REVIEW; STEREOSPECIFICITY;

ANESTHETICS, LOCAL; BLOOD PROTEINS; CHILD; CHILD, PRESCHOOL; HEART; HUMANS; INFANT; METABOLIC CLEARANCE RATE; PROTEIN BINDING; SEIZURES; TISSUE DISTRIBUTION;

EID: 0442291790     PISSN: 03125963     EISSN: None     Source Type: Journal    
DOI: 10.2165/00003088-200443010-00002     Document Type: Review

References (91)

1. Fortuna A. Caudal analgesia: a simple and safe technique in paediatric surgery. Br J Anaesth 1967; 39: 165-70
2. Schulte-Steinberg O, Rahlfs VW. Caudal anaesthesia in children and spread of 1 per cent lignocaine: a statistical study. Br J Anaesth 1970; 42: 1093-9
3. Giaufre E, Dalens B, Gombert A. Epidemiology and morbidity of regional anesthesia in children: a one-year prospective survey of the French-Language Society of Pediatric Anesthesiologists. Anesth Analg 1996; 83: 904-12
4. Schulte-Steinberg O, Rahlfs VW. Caudal anesthesia in children and the distribution of 0.25 per cent bupivacaine solution: a statistical study. Anaesthesist 1972; 21: 94-100
5. Eyres RL. Kild J, Oppenheim R, et al. Local anaesthetic plasma levels in children. Anaesth Intensive Care 1978; 6: 243-7
6. Rigler ML, Drasner K, Krejcie TC, et al. Cauda equina syndrome after continuous spinal anesthesia. Anesth Analg 1991; 72: 275-81
7. Lambert DH, Hurley RJ. Cauda equina syndrome and continuous spinal anesthesia. Anesth Analg 1991; 72: 817-9
8. Hampl KF, Schneider MC, Ummenhofer W, et al. Transient neurologic symptoms after spinal anesthesia. Anesth Analg 1995; 81: 1148-53
9. Freedman JM, Li DK, Drasner K, et al. Transient neurologic symptoms after spinal anesthesia: an epidemiologic study of 1,863 patients. Anesthesiology 1998; 89: 633-41
10. Markey JR, Naseer OB, Bird DJ, et al. Transient neurologic symptoms after epidural analgesia. Anesth Analg 2000; 90: 437-9
11. Bourlon-Figuet S, Dubousset A-M, Benhamou D, et al. Transient neurologic symptoms after epidural analgesia in a five-year-old child. Anesth Analg 2000; 91: 856-7
12. Flandin-Bléty C, Barrier G. Accidents following extradural analgesia in children: the results of a retrospective study. Paediatr Anaesth 1995; 5: 41-6
13. Bouaziz H, Okubo N, Malinovsky JM, et al. The age-related effects of epidural lidocaine, with and without epinephrine, on spinal cord blood flow in anesthetized rabbits. Anesth Analg 1999; 88: 1302-7
14. Maxwell LG, Martin LD, Yaster M. Bupivacaine-induced cardiac toxicity in neonates: successful treatment with intravenous phenytoin. Anesthesiology 1994; 80: 682-6
15. Hellstrom-Westas L, Westgren U, Rosen I, et al. Lidocaine for treatment of severe seizures in newborn infants: I. clinical effects and cerebral electrical activity monitoring. Acta Paediatr Scand 1988; 77: 79-84
16. Salas S, Johannessen SI, Hoem NO, et al. Lidocaine pharmacokinetics and toxicity in newborn pigs. Anesth Analg 1997; 85: 306-12
17. Kohane DS, Sankar WN, Shubina M, et al. Sciatic nerve blockade in infant, adolescent, and adult rats: a comparison of ropivacaine with bupivacaine. Anesthesiology 1998; 89: 1199-208
18. Brown DL, Ransom DM, Hall JA, et al. Regional anesthesia and local anesthetic-induced systemic toxicity: seizure frequency and accompanying cardiovascular changes. Anesth Analg 1995; 81: 321-8
19. Albright GA. Cardiac arrest following regional anesthesia with etidocaine and bupivacaine. Anesthesiology 1979; 51: 285-7
20. de La Coussaye J, Brugada J, Allessie MA. Electrophysiologic and arrhythmogenic effects of bupivacaine: a study with high-resolution ventricular epicardial mapping in rabbit hearts. Anesthesiology 1992; 77: 32-41
21. Mazoit JX, Decaux A, Bouaziz H, et al. Comparative ventricular electrophysiologic effect of racemic bupivacaine, levobupivacaine, and ropivacaine on the isolated rabbit heart. Anesthesiology 2000; 93: 784-92
22. Bardsley H, Gristwood R, Baker H, et al. A comparison of the cardiovascular effects of levobupivacaine and rac-bupivacaine following intravenous administration to healthy volunteers. Br J Clin Pharmacol 1998; 46: 245-9
23. Chang DH, Ladd LA, Copeland S, et al. Direct cardiac effects of intracoronary bupivacaine, levobupivacaine and ropivacaine in the sheep. Br J Pharmacol 2001; 132: 649-58
24. Freysz M, Timour Q, Mazze RI, et al. Potentiation by mild hypothermia of ventricular conduction disturbances and reentrant arrhythmias induced by bupivacaine in dogs. Anesthesiology 1989; 70: 799-804
25. Timour Q, Freysz M, Mazze R, et al. Enhancement by hyponatremia and hyperkalemia of ventricular conduction and rhythm disorders caused by bupivacaine. Anesthesiology 1990; 72: 1051-6
26. Freysz M, Timour Q, Bertrix L, et al. Enhancement by ischemia of the risk of cardiac disorders, especially fibrillation, in regional anesthesia with bupivacaine. Acta Anaesthesiol Scand 1993; 37: 350-6
27. Tucker GT, Boyes RN, Bridenbaugh PO, et al. Binding of anilide-type local anesthetics in human plasma: 1. relationships between binding, physicochemical properties, and anesthetic activity. Anesthesiology 1970; 33: 287-303
28. Meunier JF, Goujard E, Dubousset AM, et al. Pharmacokinetics of bupivacaine after continuous epidural infusion in infants with and without biliary atresia. Anesthesiology 2001; 95: 87-95
29. Lönnqvist PA, Herngren L. Effects of pronounced haemodilution on the plasma protein binding of lidocaine. Perfusion 1995; 10: 17-20
30. Burm AG, van der Meer AD, van Kleef JW, et al. Pharmacokinetics of the enantiomers of bupivacaine following intravenous administration of the racemate. Br J Clin Pharmacol 1994; 38: 125-9
31. Emanuelsson BM, Persson J, Alm C, et al. Systemic absorption and block after epidural injection of ropivacaine in healthy volunteers. Anesthesiology 1997; 87: 1309-17
32. Lonnqvist 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
33. Mazoit JX, Denson DD, Samii K. Pharmacokinetics of bupivacaine following caudal anesthesia in infants. Anesthesiology 1988; 68: 387-91
34. Hansen TG, Ilett KF, Reid C, et al. Caudal ropivacaine in infants: population pharmacokinetics and plasma concentrations. Anesthesiology 2001; 94: 579-84
35. Kremer JMH, Wilting J, Jansen LHM. Drug binding to human alpha-1-acid glycoprotein in health and disease. Pharmacol Rev 1988; 40: 1-47
36. Burm AG, Cohen IM, van Kleef JW, et al. Pharmacokinetics of the enantiomers of mepivacaine after intravenous administration of the racemate in volunteers. Anesth Analg 1997; 84: 85-9
37. Veering BT, Burm AG, Feyen HM, et al. Pharmacokinetics of bupivacaine during postoperative epidural infusion: enantioselectivity and role of protein binding. Anesthesiology 2002; 96: 1062-9
38. Mazoit JX, Cao LS, Samii K. Binding of bupivacaine to serum proteins, isolated albumin and isolated α1-acid glycoprotein: differences between the two enantiomers are partly due to cooperativity. J Pharmacol Exp Ther 1996; 256: 109-15
39. Booker PD, Taylor C, Saba G. Perioperative changes in α1-acid glycoprotein concentrations in infants undergoing major surgery. Br J Anaesth 1996; 76: 365-8
40. Denson D, Coyle D, Thompson G, et al. Alpha 1-acidglycoprotein and albumin in human serum bupivacaine binding. Clin Pharmacol Ther 1984; 35: 409-15
41. Rolan PE. Plasma protein binding displacement interactions: why are they still regarded as clinically important? Br J Clin Pharmacol 1994 Feb; 37 (2): 125-8
42. Denson DD, Mazoit JX. Physiology and pharmacology of local anesthetics. In: Sinatra RS, editor. Acute pain mechanisms and management. St Louis (MO): Mosby, 1992: 124-39
43. Gjonaj ST, Lowenthal DB, Dozor AJ. Nebulized lidocaine administered to infants and children undergoing flexible bronchoscopy. Chest 1997; 112: 1665-9
44. Sitbon P, Laffon M, Lesage V, et al. Lidocaine plasma concentrations in pediatric patients after providing airway topical anesthesia from a calibrated device. Anesth Analg 1996; 82: 1003-6
45. Day RO, Chalmers DR, Williams KM, et al. The death of a healthy volunteer in a human research project: implications for Australian clinical research. Med J Aust 1998; 168: 449-51
46. Burm AGL, Vermeulen NPE, Van Kleef JW, et al. Pharmacokinetics of lidocaine and bupivacaine in surgical patients following epidural administration: simultaneous investigation of absorption and disposition kinetics using stable isotopes. Clin Pharmacokinet 1987; 13: 191-203
47. Burm AGL. Clinical pharmacokinetics of epidural and spinal anaesthesia. Clin Pharmacokinet 1989; 16: 283-311
48. Karmakar MK, Aun CS, Wong EL, et al. Ropivacaine undergoes slower systemic absorption from the caudal epidural space in children than bupivacaine. Anesth Analg 2002; 94: 259-65
49. McCann ME, Sethna NF, Mazoit JX, et al. The pharmacokinetics of epidural ropivacaine in infants and young children. Anesth Analg 2001; 93: 893-7
50. Emanuelsson B-MK, Zaric D, Nydahl P-A, et al. Pharmacokinetics of ropivacaine and bupivacaine during 21 hours of continuous epidural infusion in healthy male volunteers. Anesth Analg 1995; 81: 1163-8
51. Ecoffey C, Desparmet J, Berdeaux A, et al. Bupivacaine in children: pharmacokinetics following caudal anesthesia. Anesthesiology 1985; 63: 447-8
52. Ecoffey C, Dubousset AM, Samii K. Lumbar and thoracic epidural anesthesia for urologic and upper abdominal surgery in infants and children. Anesthesiology 1986; 65: 87-90
53. Murat I, Montay G, Delleur MM, et al. Bupivacaine pharmacokinetics during epidural anaesthesia in children. Eur J Anaesthesiol 1988; 5: 113-20
54. Smith T, Moratin P, Wulf H. Smaller children have greater bupivacaine plasma concentrations after ilioinguinal block. Br J Anaesth 1996; 76: 452-5
55. 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
56. Burm AG, de Boer AG, van Kleef JW, et al. Pharmacokinetics of lignocaine and bupivacaine and stable isotope labelled analogues: a study in healthy volunteers. Biopharm Drug Dispos 1988; 9: 85-95
57. Veering BT, Burm AG, Vletter AA, et al. The effect of age on the systemic absorption, disposition and pharmacodynamics of bupivacaine after epidural administration. Clin Pharmacokinet 1992; 22: 75-84
58. Morrison LMM, Emanuelsson BM, McClure JH, et al. Efficacy and kinetics of extradural ropivacaine: comparison with bupivacaine. Br J Anaesth 1994; 72: 164-9
59. Weston PJ, Bourchier D. The pharmacokinetics of bupivacaine following interpleural nerve block in infants of very low birthweight. Paediatr Anaesth 1995; 5: 219-22
60. Desparmet J, Meistelman C, Barre J, et al. Continuous epidural infusion of bupivacaine for postoperative pain relief in children. Anesthesiology 1987; 67: 108-10
61. Emanuelsson BM, Persson J, Sandin S, et al. Intraindividual and interindividual variability in the disposition of the local anaesthetic ropivacaine in healthy subjects. Ther Drug Monit 1997; 19: 126-31
62. Burm AG, Stienstra R, Brouwer RP, et al. Epidural infusion of ropivacaine for postoperative analgesia after major orthopedic surgery: pharmacokinetic evaluation. Anesthesiology 2000; 93: 395-403
63. Hansen TG, Ilett KF, Lim SI, et al. Pharmacokinetics and clinical efficacy of long-term epidural ropivacaine infusion in children. Br J Anaesth 2000; 85: 347-53
64. Iida H, Watanabe Y, Dohi S, et al. Direct effects of ropivacaine and bupivacaine on spinal pial vessels in canine: assessment with closed spinal window technique. Anesthesiology 1997; 87: 75-81
65. Iida H, Ohata H, Iida M, et al. The differential effects of stereoisomers of ropivacaine and bupivacaine on cerebral pial arterioles in dogs. Anesth Analg 2001; 93: 1552-6
66. Burm AGL, Van Kleef JW, Gladines MPRR, et al. Epidural anesthesia with lidocaine and bupivacaine: effects of epinephrine on the plasma concentration profiles. Anesth Analg 1986; 65: 1281-4
67. Warner MA, Kunkel SE, Offord KO, et al. The effects of age, epinephrine, and operative site on duration of caudal analgesia in pediatric patients. Anesth Analg 1987; 66: 995-8
68. Doyle E, Morton NS, McNicol LR. Plasma bupivacaine levels after fascia iliaca compartment block with and without adrenaline. Paediatr Anaesth 1997; 7: 121-4
69. Hansen TG, Morton NS, Cullen PM, et al. Plasma concentrations and pharmacokinetics of bupivacaine with and without adrenaline following caudal anaesthesia in infants. Acta Anaesthesiol Scand 2001; 45: 42-7
70. Mather LE. Anatomical-physiological approaches in pharmacokinetics and pharmacodynamics. Clin Pharmacokinet 2001; 40: 707-22
71. Luz G, Innerhofer P, Haussler B, et al. Comparison of ropivacaine 0.1% and 0.2% with bupivacaine 0.2% for single-shot caudal anaesthesia in children. Paediatr Anaesth 2000; 10: 499-504
72. Hines RN, McCarver DG. The ontogeny of human drug-metabolizing enzymes: phase I oxidative enzymes. J Pharmacol Exp Ther 2002; 300: 355-60
73. Tateishi T, Nakura H, Asoh M, et al. A comparison of hepatic cytochrome P450 protein expression between infancy and postinfancy. Life Sci 1997; 61: 2567-74
74. Tanaka E. In vivo age-related changes in hepatic drug-oxidizing capacity in humans. J Clin Pharm Ther 1998; 23: 247-55
75. Kuhnert BR, Zuspan KJ, Kuhnert PM, et al. Bupivacaine disposition in mother, fetus, and neonate after spinal anesthesia for cesarean section. Anesth Analg 1987; 66: 407-12
76. Gantenbein M, Attolini L, Bruguerolle B, et al. Oxidative metabolism of bupivacaine into pipecolylxylidine in humans is mainly catalyzed by CYP3A. Drug Metab Dispos 2000; 28: 383-5
77. Oda Y, Furuichi K, Tanaka K, et al. Metabolism of a new local anesthetic, ropivacaine, by human hepatic cytochrome P450. Anesthesiology 1995; 82: 214-20
78. Ekstrom 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
79. 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
80. Tucker GT. Pharmacokinetics of local anaesthetics. Br J Anaesth 1986; 58: 717-31
81. Bax NDS, Tucker GT, Lennard MS, et al. The impairment of lignocaîne clearance by propranolol: major contribution from enzyme inhibition, Br J Clin Pharmacol 1985; 9: 597-603
82. le Lorrier J, Gredin D, Lapout Y, et al. Pharmacokinetics of lidocaine after intravenous infusions in uncomplicated myocardial infarction. Ann Intern Med 1977; 87: 700-2
83. Mazoit JX, Lambert C, Berdeaux A, et al. Pharmacokinetics of bupivacaine after short and prolonged infusions in conscious dogs. Anesth Analg 1988; 67: 961-6
84. Scott DB, Lee A, Fagan D, et al. Acute toxicity of ropivacaine compared with that of bupivacaine. Anesth Analg 1989; 69: 563-9
85. Knudsen K, Beckman Suurkula M, Blomberg S, et al. Central nervous and cardiovascular effects of i.v. infusions of ropivacaine, bupivacaine and placebo in volunteers. Br J Anaesth 1997; 78: 507-14
86. Xu YQ, Pickoff AS, Clarkson CW. Developmental changes in the effects of lidocaine on sodium channels in rat cardiac myocytes. J Pharmacol Exp Ther 1992; 262: 670-6
87. Sun LS, Rosen MR. The electrophysiologic effects of bupivacaine on adult, neonatal, and fetal guinea pig papillary muscles. Anesthesiology 1991; 74: 893-39
88. Giaufre E, Bruguerolle B, Rastello C, et al. New regimen for interpleural block in children. Paediatr Anaesth 1995; 5: 125-8
89. Elman A, Debaene B, Magny-Metrot C, et al. Interpleural analgesia with bupivacaine following thoracotomy: ineffective results of a controlled study and pharmacokinetics. J Clin Anesth 1993; 5: 118-21
90. Luz G, Wieser C, Innerhofer P, et al. Free and total bupivacaine plasma concentrations after continuous epidural anaesthesia in infants and children. Paediatr Anaesth 1998; 8: 473-8
91. Luz G, Innerhofer P, Bachmann B, et al. Bupivacaine plasma concentrations during continuous epidural anesthesia in infants and children. Anesth Analg 1996; 82: 231-4