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PubMed2004

Possible mechanism of irreversible nerve injury caused by local anesthetics: detergent properties of local anesthetics and membrane disruption.

BACKGROUND: Irreversible nerve injury may result from neural membrane lysis due to the detergent properties of local anesthetics. This study aimed to investigate whether local anesthetics display the same properties as detergents and whether they disrupt the model membrane at high concentrations. METHODS: Concentrations at which dodecyltrimethylammonium chloride and four local anesthetic (dibucaine, tetracaine, lidocaine, and procaine) molecules exhibit self-aggregation in aqueous solutions were measured using an anesthetic cation-sensitive electrode. Light-scattering measurements in a model membrane solution were also performed at increasing drug concentrations. The concentration at which drugs caused membrane disruption was determined as the point at which scattering intensity decreased. Osmotic pressures of anesthetic agents at these concentrations were also determined. RESULTS: Concentrations of dodecyltrimethylammonium chloride, dibucaine, tetracaine, lidocaine, and procaine at which aggregation occurred were 0.15, 0.6, 1.1, 5.3, and 7.6%, respectively. Drug concentrations causing membrane disruption were 0.09% (dodecyltrimethylammonium chloride), 0.5% (dibucaine), 1.0% (tetracaine), 5.0% (lidocaine), 10.2% (procaine), and 20% (glucose), and osmotic pressures at these concentrations were 278, 293, 329, 581, 728, and 1,868 mOsm/kg H2O, respectively. CONCLUSIONS: These results show that all four local anesthetics form molecular aggregations in the same manner as dodecyltrimethylammonium chloride, a common surfactant. At osmotic pressures insufficient to affect the membrane, local anesthetics caused membrane disruption at the same concentrations at which molecular aggregation occurred. This shows that disruption of the model membrane results from the detergent nature of local anesthetics. Nerve membrane solubilization by highly concentrated local anesthetics may cause irreversible neural injury.

Anesthetics, Local↗
PubMedDate not supplied

Alkalinization of local anesthetics. Which block, which local anesthetic?

BACKGROUND AND OBJECTIVES: A number of clinical studies have been performed in an attempt to establish the effects of alkalinization on potency of local anesthetics. Conflicting results were obtained probably because different studies used different methods as well as different definitions of the effects. To determine the efficacy of alkalinization using different local anesthetic solutions and different regional blocks, 180 patients were studied in a randomized, double-blind fashion. The local anesthetic solutions studied were bupivacaine, mepivacaine, and lidocaine; the regional blocks studied were epidural block, axillary brachial plexus block, and femoral and sciatic nerve block. MATERIALS AND METHODS: In this study, 180 patients receiving epidural block (n = 60), sciatic and femoral nerve block (n = 60), and brachial plexus block (n = 60) were randomized to receive, in a double-blind fashion, a plain or a pH-adjusted solution of 2% mepivacaine, 2% lidocaine, or 0.5% bupivacaine. Onset of sensory analgesia, onset of maximum effect (peak effect or complete analgesia), duration of the block, onset, duration and density of motor block were evaluated using pinprick (Hollmen scale) and a 10-point decimal scale (Seow scale). RESULTS: concerning epidural block, the alkalinization of the local anesthetic shortened significantly the onset of sensory analgesia in the dermatome corresponding to the lumbar interspace used for epidural puncture (L3-L4) and increased the spread of the epidural block in all the groups. The onset of sensory analgesia at L4 level ranged from 10 minutes for plain bupivacaine to 3 minutes for alkalinized lidocaine, whereas the onset at T10 level ranged from 16 minutes for plain bupivacaine and mepivacaine to 12.3 minutes for alkalinized lidocaine. The effects of alkalinization were more evident with lidocaine and bupivacaine. Concerning femoral and sciatic nerve blocks, a statistically significant shorter onset of sensory analgesia and motor block were observed with mepivacaine. Concerning brachial plexus axillary block, the effects of alkalinization were more evident with lidocaine. CONCLUSIONS: Alkalinization produced the best results with lidocaine and bupivacaine for epidural block, with lidocaine for brachial plexus block, and with mepivacaine for sciatic and femoral nerve blocks.

Adult↗
PubMed2006

Randomized clinical trial of local anesthetic versus a combination of local anesthetic with self-hypnosis in the management of pediatric procedure-related pain.

A prospective controlled trial was conducted to compare the efficacy of an analgesic cream (eutectic mixture of local anesthetics, or EMLA) with a combination of EMLA with hypnosis in the relief of lumbar puncture-induced pain and anxiety in 45 pediatric cancer patients (age 6-16 years). The study also explored whether young patients can be taught and can use hypnosis independently as well as whether the therapeutic benefit depends on hypnotizability. Patients were randomized to 1 of 3 groups: local anesthetic, local anesthetic plus hypnosis, and local anesthetic plus attention. Results confirmed that patients in the local anesthetic plus hypnosis group reported less anticipatory anxiety and less procedure-related pain and anxiety and that they were rated as demonstrating less behavioral distress during the procedure. The level of hypnotizability was significantly associated with the magnitude of treatment benefit, and this benefit was maintained when patients used hypnosis independently.

Adolescent↗
PubMed2005

Estimation of the effect of the acidosis and alkalosis on the anesthetic potency of local anesthetics by biopartitioning micellar chromatography and micellar electrokinetic chromatography.

Local anesthetics are hydrophobic compounds and weak bases with protonation constants ranged between 7.5 and 8.8. These drugs block reversibly nerve conduction near their site of application or injection and thus produce temporary loss of feeling or sensation in a limited area of the body. The efficacy of anesthetic blockade of local anesthetics depends on the charged/uncharged form ratio and the hydrophobicity of the compounds. In addition their toxicological effects have been reported to be highly dependent on the physiological pH. Biopartitioning micellar chromatography (BMC) and micellar electrokinetic chromatography (MEKC), that use micellar solutions as mobile phases, have proven to be useful for describing the biological behavior of different kind of compounds. In this paper, relationships between the retention data in BMC and MEKC using Brij35 as surfactant (at pH 7.4) and some pharmacodynamic parameters of local anesthetics are obtained. These models are compared with those obtained using an immobilized artificial column (IAM). Finally, the effect of the corporal pH in situations of acidosis and alkalosis on the pharmacological and toxicological properties of local anesthetics is studied using the retention of compounds in BMC at different mobile phase pH values.

Acidosis↗
PubMed2005

The role of molecular structure in the crystal polymorphism of local anesthetic drugs: crystal polymorphism of local anesthetic drugs, part X.

PURPOSE: This report is the résumé of a comprehensive investigation on the solid-state properties and the crystal polymorphism of the structurally homogenous class of local anesthetic drugs. The goal is to explore the relationship between crystal polymorphism and molecular structural features. METHODS: A salt form (mostly the hydrochloride) as well as the free base of 24 local anesthetics has been characterized by means of thermomicroscopy, differential scanning calorimetry, pycnometry, Fourier transform infrared, Fourier transform Raman, and solid-state NMR spectroscopies, as well as X-ray diffraction methods (single crystal, powder). RESULTS: Based on the thermochemical data, the relative thermodynamic stabilities of the different crystal forms of each polymorphic system were evaluated and visualized as semiquantitative energy/temperature diagrams. CONCLUSION: This study is the first step in recognizing relationships between the structure and the solid-state properties within this limited group of active substances with common structural elements. The results clearly show that there are certain relationships, but, to understand the phenomenological behavior in more detail on a molecular level, more structural information must be collected and analyzed by computational methods.

Adsorption↗
PubMed1992

[Local anesthetics. 99. Synthesis and local anesthetic actions of alkoxyphenylcarbamates].

Within the framework of studying the influence of alterations of the connecting chain in the group of local anaesthetics a series of 24 compounds of 1-propoxymethyl-2-(1-pyrrolidinyl), 2-(1-piperidino)-, and 2-(1-perhydroazepinyl)-ethyl esters of o- and m-alkoxyphenylcarbamic acid were prepared. Studied compounds show a high index of relative local anaesthetic activity as compared to the standards cocaine and procaine, at a relatively low acute toxicity.

Anesthetics, Local↗
PubMed1994

The partition coefficient as a predictor of local anesthetic potency for spinal anesthesia: evaluation of five local anesthetics in a mouse model.

Local anesthetic partition coefficients correlate with drug potencies in vitro, but in vivo data have not always complimented in vitro results. Despite extensive studies on intrathecal anesthetic action, whether there is correlation between the partition coefficient and local anesthetic potency has not been addressed. Mice (n = 150) were randomly allocated into 15 groups. Intrathecal injections of etidocaine (E), tetracaine (T), bupivacaine (B), lidocaine (L), or procaine (P) were administered and analgetic effect was measured using tail-flick (TF) test. Concentration-response regressions were constructed for each drug; EC50 values were calculated and compared at 95% confidence intervals. The EC50 values between E (0.017%), T (0.019%), and B (0.012%) were not significantly variant. The EC50 of L (0.098%) and P (0.229%) were significantly different from each other and from E, T, and B. The EC50 values were converted to ED50 in nmols. Relative anesthetic potency, defined as the inverse value of ED50 of drug was 23:16:15:2.4:1 for B, E, T, L, and P, respectively. ED50 showed high correlation (R = 0.978) with partition coefficients of local anesthetics. This study implies that the partition coefficient is a predictor of intrathecal local anesthetic potency. We suggest that the mouse model is reliable for evaluation of intrathecal local anesthetic action.

Anesthesia, Spinal↗