Pharmacokinetics of Lidocaine and Bupivacaine Following Subarachnoid Administration in Surgical Patients

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

doi:10.1097/00132582-198907000-00033

Cited by 5 publications

(11 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…This effect has been observed with lignocaine, bupivacaine and etidocaine (Bromage et al 1964;Burm 1985;Murphy et al 1976). Furthermore, it may speed the onset of action; this has been demonstrated with dilute solutions of bupivacaine (Eisenach et al 1987) and with etidocaine (Murphy et al 1976), although others have observed a slowing of the onset with lignocaine (Bromage et al 1964).…”

Section: Additivesmentioning

confidence: 71%

“…With all 3 agents a rapid initial absorption was followed by a much slower second phase. This biphasic absorption pattern was confirmed later by studies using stable isotope methods in surgical patients (Burm 1985;Burm et al 1987b) [ infusion after epidural administration of the unlabelled drug. Data on the systemic disposition were then derived from the plasma concentration-time profiles of the deuterium-labelled analogues, which had been shown previously to have disposition characteristics similar to the unlabelled drugs (Burm et al 1988a).…”

Section: Epidural Blockmentioning

confidence: 76%

“…Studies after epidural and subarachnoid administration of lignocaine and bupivacaine in man (Burm 1985;Burm et al 1987bBurm et al , 1988b and subarachnoid administration oflignocaine in monkeys (Denson et al 1981) showed that at least 95% of the dose ultimately entered the general circulation. This indicates that little or no metabolism occurs within the epidural and subarachnoid spaces.…”

Section: Extent Of Absorptionmentioning

confidence: 99%

“…Studies in surgical patients have demonstrated that the initial absorption rate of both lignocaine and bupivacaine was much slower after subarachnoid than after epidural administration (Burm 1985;Burm et al 1988b) [table II]. In fact, no rapid absorption phase was detected after subarachnoid injection oflignocaine in most patients.…”

Section: Subarachnoid Blockmentioning

confidence: 99%

“…In general, the addition of adrenaline (usually 5 lLg/ml, but smaller amounts are used in obstetrics) prolonged the duration of epidural anaesthesia to a greater extent with lignocaine and mepivacaine than with prilocaine; comparatively little prolongation was noted with bupivacaine and etidocaine (Abboud et al 1984(Abboud et al , 1985(Abboud et al , 1987AbdelSalam et al 1975;Bridenbaugh et al 1974;Bromage et al 1964;Buckley et al 1978;Burm 1985;Covino 1986;Littlewood et al 1979;Murphy et al 1976;Sinclair & Scott 1984). The effect of adrenaline may be greater when lower doses of local anaesthetics are administered (Covino 1986;Littlewood et al 1979).…”

Section: Additivesmentioning

confidence: 99%

See 4 more Smart Citations

Clinical Pharmacokinetics of Epidural and Spinal Anaesthesia

Burm

1989

Clinical Pharmacokinetics

View full text Add to dashboard Cite

Epidural and spinal anaesthesia results from the interaction of local anaesthetics with nerve structures, primarily those located within the subarachnoid space. Local anaesthetics can reach the sites of action along various distribution pathways. Uptake into extraneural tissues (in particular epidural fat) and systemic absorption compete with neural tissue distribution and thereby affect the clinical potency and duration of action. Consequently, epidural doses must be much higher than spinal doses. The systemic absorption of lignocaine (lidocaine), bupivacaine and etidocaine following lumbar epidural administration has been shown to be biphasic, with a rapid initial absorption phase followed by a much slower absorption phase. Initial absorption rates of lignocaine and bupivacaine following subarachnoid injection are much slower, but the late absorption rates are similar to those after epidural administration. The tissue distribution characteristics of various amide-type agents are similar, because more extensive plasma binding offsets the greater tissue affinity of the more lipophilic compounds bupivacaine and etidocaine. The amide-type agents are predominantly eliminated by hepatic metabolism, except prilocaine, which is also metabolised elsewhere in the body. Ester-type agents are rapidly hydrolysed in blood and liver and are eliminated much faster than amide-type agents. The blood concentrations attained depend primarily upon the dose administered. The addition of adrenaline (epinephrine) reduces the peak plasma drug concentrations; similarly, the age of the patient, disease states and drug interactions may alter the pharmacokinetics to various extents. Because of the low dose requirements, systemic toxicity is not a problem during spinal anaesthesia. During epidural anaesthesia, however, the safety margin is relatively small, and systemic toxicity is very likely to occur after inadvertent intravascular injection of an epidural dose.

show abstract

Section: Additivesmentioning

confidence: 71%

Section: Epidural Blockmentioning

confidence: 76%

Section: Extent Of Absorptionmentioning

confidence: 99%

Section: Subarachnoid Blockmentioning

confidence: 99%

Section: Additivesmentioning

confidence: 99%

See 3 more Smart Citations

Clinical Pharmacokinetics of Epidural and Spinal Anaesthesia

Burm

1989

Clinical Pharmacokinetics

View full text Add to dashboard Cite

show abstract

Investigations into distribution of lidocaine in human autopsy material

Oertel

Arenz

Zeitz

et al. 2015

Biomedical Chromatography

View full text Add to dashboard Cite

With screening methods in the legal medicine drugs were often detected in autopsy material. In this study the antiarrhythmic and the local anesthetic drug lidocaine could be proved in fifty-one cases and determined in different autopsy materials. For the first time the comparison of so many distribution patterns of lidocaine in human compartments was possible. A liquid-liquid extraction procedure, a standard addition method and LC/MS/MS were used for analytics. The measured concentrations in blood were in the therapeutic range or lower. The time between lidocaine application and death was given in twenty-nine cases. These data were very helpful to estimate and interpret the distribution process of lidocaine between application and death. This time exerted a crucial influence on the distribution of lidocaine in the compartments. Most of the intravenous applicated lidocaine was found in heart blood after a very short time of distribution. Afterwards the highest concentrations were measured in brain. Later the highest concentration was found in the kidney samples or in urine. If the time between lidocaine application and death is known, the results of this study can be used to deepen the knowledge of its pharmacokinetics. If this time is unknown, the circumstances and the causes of death can be better explained.

show abstract

Pharmacokinetics of lidocaine and bupivacaine and stable isotope labelled analogues: A study in healthy volunteers

Burm

Boer

Kleef

et al. 1988

Biopharm & Drug Disp

Self Cite

View full text Add to dashboard Cite

The pharmacokinetics of lidocaine and bupivacaine and tri-deuteromethyl-labelled lidocaine and bupivacaine were investigated in healthy volunteers. The deuterium-labelled and the unlabelled form of the drug to be investigated were simultaneously infused in 10 min. Plasma concentrations were determined using a combination of capillary gas chromatography and mass fragmentography. Bi-exponential functions were fitted to the plasma concentration-time data. The mean distribution and elimination half-lives were 8.4 +/- 5.9 min and 96 +/- 26 min for lidocaine, 9.2 +/- 7.0 min and 98 +/- 27 min for deuterium-labelled lidocaine, 15.3 +/- 9.9 min and 111 +/- 32 min for bupivacaine, and 15.2 +/- 10.9 min and 109 +/- 31 min for deuterium-labelled bupivacaine, respectively. The mean volumes of the central compartment and mean steady state volumes of distribution were: lidocaine 37 +/- 151 and 97 +/- 201, deuterium-labelled lidocaine 39 +/- 161 and 98 +/- 181, bupivacaine 27 +/- 111 and 66 +/- 231 and deuterium-labelled bupivacaine 28 +/- 121, and 65 +/- 221, respectively. The respective mean plasma clearances were 0.88 +/- 0.181 min-1, 0.87 +/- 0.181 min-1, 0.61 +/- 0.151 min-1, and 0.62 +/- 0.171 min-1. The results of the study indicate that substitution of a deuterated methyl group does not alter the pharmacokinetics of lidocaine and bupivacaine in healthy subjects.

show abstract

Pharmacokinetics of Lidocaine and Bupivacaine Following Subarachnoid Administration in Surgical Patients

Cited by 5 publications

References 0 publications

Clinical Pharmacokinetics of Epidural and Spinal Anaesthesia

Clinical Pharmacokinetics of Epidural and Spinal Anaesthesia

Investigations into distribution of lidocaine in human autopsy material

Pharmacokinetics of lidocaine and bupivacaine and stable isotope labelled analogues: A study in healthy volunteers

Contact Info

Product

Resources

About