Pharmacokinetics of Lidocaine and Bupivacaine following Subarachnoid Administration in Surgical Patients

Burm, A. G. L.; Kleef, Jack W. van; Vermeulen, Nico; Olthof, G.; Breimer, D.D.; Spierdijk, J.

doi:10.1097/00000542-198810000-00020

Cited by 30 publications

(16 citation statements)

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“…After subarachnoid administration the half-life of the slow absorption process and the mean absorption time decreased with age, because of a higher late absorption rate. In fact, the late absorption rate of bupivacaine after subarachnoid administration has been found to be similar to that after epidural administration in younger patients (Burm et al 1987(Burm et al , 1988b. In keeping with this observation, the values of the slow absorption half-lives obtained 83 in this study were in the same ranges as those obtained in the spinal study (Veering et al 1991).…”

Section: Discussionsupporting

confidence: 86%

“…Consequently, data on the absorption rate cannot be derived from the plasma concentration curves unless a detailed description of the disposition is avail-able. Therefore, Burm et al (1987Burm et al ( , 1988b developed a stable isotope method, using deuteriumlabelled analogues of bupivacaine, which enabled simultaneous determination of the absorption and disposition characteristics of the drug. We have used this approach to investigate the effects of age on the systemic absorption and disposition following epidural administration of bupivacaine.…”

Section: Discussionmentioning

confidence: 99%

“…The initial absorption is believed to occur predominantly by uptake into blood vessels from the dense venous plexus within the epidural space, resulting in a rather high Cmax and absorption rate. The late absorption phase has been suggested to be due to slow uptake of local anaesthetics sequestered in epidural fat (Burm et al 1988b;Tucker 1986). The present study showed that the half-lives of the fast and slow absorption processes and the corresponding absorbed fraction were unaffected by age.…”

Section: Discussionmentioning

confidence: 99%

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The Effect of Age on the Systemic Absorption, Disposition and Pharmacodynamics of Bupivacaine After Epidural Administration

Veering

Burm

Vletter

et al. 1992

Clinical Pharmacokinetics

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The influence of age on the systemic absorption and disposition of bupivacaine following epidural administration in 20 male patients (22 to 81 years) was examined using a stable isotope method to determine whether pharmacokinetics play a role in age-related pharmacodynamic changes seen with the drug. After epidural bupivacaine administration a deuterium-labelled analogue was administered intravenously. Bi- and triexponential functions were fitted to plasma concentration-time data of deuterium-labelled bupivacaine. The systemic absorption was described by 2 parallel first-order absorption processes. The upper level of analgesia and the duration of analgesia at dermatome T-12 increased with age (r = 0.68, p less than 0.001; r = 0.56, p less than 0.01, respectively). The time to maximal caudad spread of analgesia and the time to onset of motor block decreased with age (r = -0.76, p less than 0.0001; r = -0.72, p less than 0.001, respectively). Age did not influence systemic absorption or disposition of bupivacaine. We conclude that the changes in the clinical profile of bupivacaine with age are not due to altered pharmacokinetics, but may be related to changes in the pharmacodynamics of the drug.

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Section: Discussionsupporting

confidence: 86%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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The Effect of Age on the Systemic Absorption, Disposition and Pharmacodynamics of Bupivacaine After Epidural Administration

Veering

Burm

Vletter

et al. 1992

Clinical Pharmacokinetics

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“…The total concentrations (lignocaine + lignocaine-D3 or bupivacaine + bupivacaine-D3) of the local anaesthetics in the plasma samples were determined using capillary gas chromatography (Burm 1985;Burm et al 1982;De Boer et al 1979). The ratios of the concentrations of lignocaine and lignocaine-D3 were determined using electron impact mass fragmentography (Burm 1985;Vermeulen et al 1986), whereas the ratios of the concentrations of bupivacaine and bupivacaine-D3 were determined using positive-ion chemical ionisation mass fragmentography (Burm 1985;Vermeulen et al 1986).…”

Section: Blood Samples and Assaysmentioning

confidence: 99%

Pharmacokinetics of Lignocaine and Bupivacaine in Surgical Patients Following Epidural Administration

Burm

Vermeulen

Kleef

et al. 1987

Clinical Pharmacokinetics

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The pharmacokinetics of lignocaine (lidocaine) and bupivacaine following epidural administration were studied in 12 surgical patients using a stable isotope method. Shortly after epidural administration of the agent to be evaluated, a deuterium-labelled analogue was administered intravenously. Plasma concentrations of the unlabelled and the deuterium-labelled local anaesthetics were determined using gas chromatography and mass fragmentography. The pharmacokinetic behaviour of both agents was consistent with a 2-compartment open model and two parallel first-order absorption processes. The mean distribution and elimination half-lives were 12 minutes and 100 minutes for lignocaine, and 22 minutes and 143 minutes for bupivacaine. The mean volumes of the central compartment and the mean steady-state volumes of distribution were: lignocaine, 43L and 99L; bupivacaine, 33L and 68L. Total plasma clearances averaged 0.95 L/min (57 L/h) for lignocaine and 0.52 L/min (31.2 L/h) for bupivacaine. The half-lives, characterising the fast and slow absorption processes, were 9.3 and 82 minutes for lignocaine, and 7.0 minutes and 362 minutes for bupivacaine; the fractions of the doses absorbed in the fast and slow processes were lignocaine 0.38 and 0.58, bupivacaine 0.28 and 0.66, respectively. The results indicate that the local anaesthetics are completely absorbed from the epidural space into the general circulation. The initial absorption rates of both local anaesthetics appear to be similar, but, later, the absorption of bupivacaine proceeds much more slowly than the absorption of lignocaine.

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“…The clearance of lidocaine in this study population was 7.9 ± 1.32 mL/kg/min, ~20% less than the estimate used when formulating the dosage regimen 23. This study found that an infusion rate of 33 µg/kg/min (2 mg/kg/h) resulted in mean steady state serum concentration of 4.1 mg/L.…”

Section: Discussionmentioning

confidence: 59%

The analgesic efficacy of intravenous lidocaine infusion after laparoscopic fundoplication: a prospective, randomized, double-blind, placebo-controlled trial

Dale¹,

Phillips²,

Falk³

2016

LRA

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This study aimed to determine if intravenous lidocaine infusion reduces postoperative pain intensity following laparoscopic fundoplication surgery and to also validate the safety of intravenous lidocaine at the dose tested. This was an equally randomized, double-blind, placebo-controlled, parallel-group, single center trial. Adult patients undergoing laparoscopic fundoplication were recruited. The intervention group received 1 mg/kg intravenous lidocaine bolus prior to induction of anesthesia, then an intravenous infusion at 2 mg/kg/h for 24 hours. The primary outcome was pain, measured using a numeric rating scale for 30 hours postoperatively. Secondary outcomes were nausea and vomiting, opioid requirements, adverse events, serum lidocaine concentration, and length of hospital stay. The study was terminated after an interim analysis of 24 patients showed evidence of futility. There was no difference in postoperative pain scores (lidocaine versus control, mean ± standard deviation) at rest (2.0 ± 2.7 vs 2.1 ± 2.4, P=0.286) or with movement (2.0 ± 2.6 vs 2.6 ± 2.7, P=0.487). Three adverse events occurred in the lidocaine group (25% of patients). Intravenous lidocaine did not provide clinically significant analgesia to patients undergoing laparoscopic fundoplication. The serum lidocaine concentration of patients who experienced adverse events were within the therapeutic range. This trial cannot confirm the safety of intravenous lidocaine at the dose tested.

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Pharmacokinetics of Lidocaine and Bupivacaine following Subarachnoid Administration in Surgical Patients

Cited by 30 publications

References 0 publications

The Effect of Age on the Systemic Absorption, Disposition and Pharmacodynamics of Bupivacaine After Epidural Administration

The Effect of Age on the Systemic Absorption, Disposition and Pharmacodynamics of Bupivacaine After Epidural Administration

Pharmacokinetics of Lignocaine and Bupivacaine in Surgical Patients Following Epidural Administration

The analgesic efficacy of intravenous lidocaine infusion after laparoscopic fundoplication: a prospective, randomized, double-blind, placebo-controlled trial

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