Dose‐Independent Pharmacokinetics of Intravenous Lidocaine in Humans

Ochs, H R; Knüchel, Martin; Abernethy, Darrell R.; Greenblatt, David J.

doi:10.1002/j.1552-4604.1983.tb02723.x

Cited by 19 publications

(6 citation statements)

References 4 publications

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“…1), with clearance values in humans consistent with earlier reports [22]. Clearance of intra venously injected lidocaine has been used as an index of hepatic blood flow in humans [10].…”

Section: Discussionsupporting

confidence: 70%

Antipyrine and Lidocaine Are Cleared Faster in Horses than in Humans: Acetaminophen May Be Handled Similarly

Engelking¹,

Löfstedt

Blyden

et al. 1987

Pharmacology

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The following studies were designed to evaluate plasma elimination kinetics of intravenously administered antipyrine, acetaminophen and lidocaine among 9 healthy adult horses and 9 healthy drug-free humans (3 each per drug group), in order to compare potential species differences in drug-metabolizing ability. Acetaminophen is largely biotransformed in humans by hepatic glucuronide and sulfate conjugation, whereas both antipyrine and lidocaine are oxidized by hepatic microsomal mixed-function oxidases. Thus, plasma clearances of these drugs are thought to reflect differences in hepatic oxidative and conjugative activity, and possibly hepatic blood flow in the case of lidocaine. Results showed that mean ( ± SD, n = 3) acetaminophen clearance was similar in both horses (4.84 ± 0.637 ml/min/kg) and humans (4.68 ± 0.691 ml/min/kg). However, antipyrine clearance was 10 times greater in horses (5.83 ± 2.21 ml/min/kg) than in humans (0.536 ± 0.110 ml/min/kg), which may reflect enhanced hepatic microsomal activity in horses. Although lidocaine clearance in humans was similar to estimated hepatic blood flow (20.6 ± 5.81 ml/min/kg), clearance in horses was more than 2 times greater (52.0 ± 11.7 ml/min/kg). The cause of the higher clearance of lidocaine in horses (like dogs) remains unexplained, and may involve significant metabolism of lidocaine at extrahepatic, extravascular sites, for intravascular degradation and renal excretion of intact lidocaine in horses was negligible. Although precise biochemical mechanisms underlying pharmacokinetic parameters for these drugs in horses were not determined, it is nonetheless concluded from antipyrine results that horses may have an enhanced ability (compared with humans) to clear drugs from the circulation that are primarily metabolized in the liver by phase I oxidative reactions. On the other hand, drugs (like acetaminophen) which require biotransformation by hepatic glucuronide and sulfate conjugation, may be handled similarly in horses and humans.

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“…1), with clearance values in humans consistent with earlier reports [22]. Clearance of intra venously injected lidocaine has been used as an index of hepatic blood flow in humans [10].…”

Section: Discussionsupporting

confidence: 70%

Antipyrine and Lidocaine Are Cleared Faster in Horses than in Humans: Acetaminophen May Be Handled Similarly

Engelking¹,

Löfstedt

Blyden

et al. 1987

Pharmacology

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“…The half-time of IV lidocaine is approximately 2 hours. 54,55 This may explain why a cough-suppressing effect may last until the end of a short surgical procedure. It has also been suggested that the cough pathway is sensitized in a way similar to pain.…”

Section: Discussionmentioning

confidence: 99%

Intravenous Lidocaine for the Prevention of Cough: Systematic Review and Meta-analysis of Randomized Controlled Trials

Clivio

Putzu

Tramèr

2019

Anesthesia &Amp; Analgesia

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“…Furthermore, the comparison of observed and predicted changes is not complicated by any non-linearity in the kinetics of lignocaine since dose-independency over the range of plasma drug concentrations encountered has been established for both i.v. and oral administration (Bennett et al, 1982;Ochs et al, 1983a).…”

Section: Discussionmentioning

confidence: 99%

The impairment of lignocaine clearance by propranolol‐major contribution from enzyme inhibition.

Bax¹,

Tucker²,

Lennard³

et al. 1985

Brit J Clinical Pharma

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1 To account for a 40% lowering of the systemic clearance of lignocaine by propranolol treatment it has been proposed that propranolol reduces liver blood flow by 25% and causes a 50% decrease in the intrinsic clearance of lignocaine by enzyme inhibition. 2 In theory, the contribution of direct enzyme inhibition is best evaluated using oral administration of lignocaine when models of hepatic drug clearance predict that propranolol could increase the AUCP0 of lignocaine by 100-140%.3 This hypothesis was tested in six healthy men who received 200 mg lignocaine HCl.H20 orally with and without propranolol pre-treatment (80 mg twice daily for 3 days). Propranolol treatment increased the mean plasma AUCpO of lignocaine by 113 ± 58 s.d.% (P < 0.005); it increased the peak plasma lignocaine concentration by 79 ± 50 s.d.% (P < 0.025) and it prolonged the elimination half-life of lignocaine by 20 + 13 s.d.% (P < 0.05). 4 Propranolol treatment lowered indocyanine green clearance by 11 + 15 s.d.%, but this change was not significant statistically. 5 These experimental results are in accord with the theoretical predictions suggesting that propranolol lowers the systemic clearance of lignocaine mainly by direct inhibition of its metabolism rather than by a lowering of the hepatic blood flow.

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Dose‐Independent Pharmacokinetics of Intravenous Lidocaine in Humans

Cited by 19 publications

References 4 publications

Antipyrine and Lidocaine Are Cleared Faster in Horses than in Humans: Acetaminophen May Be Handled Similarly

Antipyrine and Lidocaine Are Cleared Faster in Horses than in Humans: Acetaminophen May Be Handled Similarly

Intravenous Lidocaine for the Prevention of Cough: Systematic Review and Meta-analysis of Randomized Controlled Trials

The impairment of lignocaine clearance by propranolol‐major contribution from enzyme inhibition.

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