Kinetics of Interaction of Local Anesthetics with Human Serum Albumin

Galenko-Yaroshevskii, A. P.; Fistunenko, P. N.; Dukhanin, A. S.

doi:10.1007/s10517-005-0477-x

Cited by 7 publications

(5 citation statements)

References 5 publications

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“…We previously studied the equilibrium characteristics of HSA-LA interactions using a fluorescent probe (1-anilinonaphthalene-8-sulfonate (ANS) [2]. The LA-HSA complex formation decreases in the following order: bupivacaine>Ru-1117>tetra-caine>>lidocaine>dicaine.…”

Section: Resultsmentioning

confidence: 99%

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Conformation and kinetic characteristics of interactions between local anesthetics and aqueous solutions of hydroxypropylmethylcellulose

Galenko-Yaroshevskii¹,

Варлашкина²,

Тахчиди

et al. 2007

Bull Exp Biol Med

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Conformation and kinetic characteristics of the interactions of local anesthetics lidocaine (xycaine), tetracaine (dicaine), bupivacaine, and new RU-1117 compound with proven anesthetic activity with Visiton (1% hydroxypropylmethylcellulose in phosphate buffer) were studied. It was found that complex formation between the local anesthetics and hydroxypropylmethylcellulose is a time-dependent reversible process. The equilibrium is attained within 2.5-8.0 h and depends on the chemical nature of local anesthetic.

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Section: Resultsmentioning

confidence: 99%

“…human serum albumin (HSA); the results can be used for prediction of the pharmacokinetic and pharmacodynamic characteristics of LA: the degree and duration of the anesthetic effect, rate of metabolism and/ or utilization in peripheral tissues [1,2].…”

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confidence: 99%

Conformation and kinetic characteristics of interactions between local anesthetics and aqueous solutions of hydroxypropylmethylcellulose

Galenko-Yaroshevskii¹,

Варлашкина²,

Тахчиди

et al. 2007

Bull Exp Biol Med

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“…The in vitro experiments of the present study supported the fact that plasma ChE activity could be inhibited by the use of bupivacaine but not by propofol. Local anesthetics, specifically bupivacaine, inhibit the butyryl ChE, which is a form of pseudo-ChE, also known as the plasma ChE (17,35). A recent finding reported reduced plasma ChE activity in women who underwent elective CS with propofol and bupivacaine (7).…”

Section: Discussionmentioning

confidence: 99%

In vitro Effects of Propofol and Bupivacaine on Pregnant Women’s Plasma Cholinesterase Activity and Malondialdehyde Level

Karam,

Mohammad

2024

J Cell Mol Anesth

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Background: Propofol and bupivacaine are commonly used anesthetics for cesarean section (CS), and they might modulate plasma cholinesterase (ChE) activity and oxidative stress during the last stage of pregnancy. This study aimed to assess the in vitro effects of propofol and bupivacaine on plasma ChE activity and malondialdehyde (MDA) levels in pregnant women before undergoing elective CS. Methods: The plasma samples of 20 women set for elective CS were pooled for the in vitro determination of the effects of propofol and bupivacaine separately on plasma ChE activity (10 minutes of incubation with different concentrations at 37ºC) and the MDA level after the in vitro exposure of plasma samples containing different anesthetic concentrations to H2O2 (100 µM, incubated for 1 hour at 37ºC). Results: Bupivacaine at 1.1 and 2.2 µM significantly inhibited plasma ChE in vitro in a concentration-dependent manner by 13% and 20%, respectively. Propofol at 25 and 50 µM did not affect plasma ChE. A unique finding in this study was that both propofol and bupivacaine revealed an antioxidant effect, as both propofol at concentrations of 25, 50, and 100 µM and bupivacaine at 1.1, 2.2, and 4.4 µM reduced the MDA level in a concentration-dependent manner in vitro after the incubation of plasma samples with H2O2 as a source of oxidant. Conclusions: The in vitro findings suggest that bupivacaine exerts anti-ChE activity that should be taken into consideration in CS anesthesia, and both propofol and bupivacaine possess antioxidant properties that need additional clinical studies.

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“…The drug concentration of Group LG was lower than that of Group LS after 10 minutes of treatment ( Figure 1A). Taking into account the toxic effects, as far as plasmatic binding is concerned, some researches consider the gamma globulin as a second site of binding in serum for the lidocaine 19,20 , since it can diminish the free fraction of such drug, and, as a consequence, lead to a lesser adverse effect. However, in the current experiment, the heart rate and blood pressure decreased similarly in Group LS and in Group LG, something that was statistically different of what happened with Groups LE and C, showing what could be considered a limitation of our study.…”

Section: ■ Discussionmentioning

confidence: 99%

“…The pharmacokinetic characteristics of gradual lidocaine application through the trachea are different from that of a single application 19 . The data from testing the bronchoscopic administration of drug showed that the plasma concentration of lidocaine depends on the total amount administered and the peak concentration values, which, in most patients, occurs between 5-30 minutes after drug delivery 20,21 . The peak plasma concentration of Group LS in this experiment was 8.40 ± 7.10 minutes, which was similar to the data from patients who received lidocaine administered through the bronchoscope in clinical practice.…”

Section: ■ Discussionmentioning

confidence: 99%

A study on reducing the absorption of lidocaine from the airway in cats

2017

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Purpose: To determine if the combination of lidocaine with epinephrine or gamma globulin would decrease the rate or reduce the amount of local absorption of lidocaine through the airway. Methods: Twenty adult male cats were randomly and evenly distributed into four groups: 1) Group LG: lidocaine administered with gamma globulin; 2) Group LS: lidocaine administered with physiological saline); 3) Group LE: lidocaine administered with epinephrine; 4) Group C: control group. Invasive blood pressure, heart rate, and concentration of lidocaine were recorded before and after administration. Results: The peak of plasma concentrations appeared difference (Group LG: 1.39 ± 0.23 mg/L; Group LS: 1.47 ± 0.29 mg/L and Group LE: 0.99 ± 0.08 mg/L). Compared to Group C, there were significant differences in the average heart rate of Groups LG, LS, and LE (P < 0.05). The average systolic blood pressures were significantly different when each group was compared to Group C (P < 0.05). The biological half-life, AUC 0-120 , peak time, and half-life of absorption among the three groups have not presented statistically significant differences (P > 0.05). Conclusion: Administering lidocaine in combination with gamma globulin through airway causes significant decrease the rate and reduce the amount of local absorption of lidocaine in cats.

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Kinetics of Interaction of Local Anesthetics with Human Serum Albumin

Cited by 7 publications

References 5 publications

Conformation and kinetic characteristics of interactions between local anesthetics and aqueous solutions of hydroxypropylmethylcellulose

Conformation and kinetic characteristics of interactions between local anesthetics and aqueous solutions of hydroxypropylmethylcellulose

In vitro Effects of Propofol and Bupivacaine on Pregnant Women’s Plasma Cholinesterase Activity and Malondialdehyde Level

A study on reducing the absorption of lidocaine from the airway in cats

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