Prolongation of nerve and epidural anesthetic blockade by bupivacaine in a lipid emulsion.

UNLABELLED We assessed the effect of a lipid emulsion of bupivacaine on prolonging peripheral nerve and epidural anesthetic blockade in the rat. The intensity and duration of motor and sensory blockade produced by a single injection of aqueous solution (BPV-as) and lipid emulsion (BPV-em) preparations of 0.5% bupivacaine were evaluated by electrophysiological methods. Both preparations induced complete, reversible motor and sensory blockade after injection. The latency time to the maximal blockade and the duration of anesthetic blockade were more prolonged for BPV-em than for BPV-as. The increase in duration of maximal blockade was 1.4 times for nerve and 1.3 times for epidural anesthesia. Histological evaluation of spinal roots and spinal cord sections did not show any abnormalities or differences between animals injected with BPV-as and those injected with BPV-em. Pharmacokinetic studies showed lower plasma peak concentration and a longer elimination half-life for BPV-em than for BPV-as. Thus, BPV-em prolongs the effects of local anesthetics, allows a similar degree of blockade, and reduces the systems toxic effects of anesthetics compared with BPV-as. IMPLICATIONS We assessed a lipid emulsion containing bupivacaine for peripheral nerve and epidural anesthetic blockade in the rat. The emulsion allowed a complete blockade, while increasing the duration of the anesthetic effect (by 30%-40%), compared with the standard bupivacaine aqueous solution.

[1]  D. Anthony,et al.  N-Butyl Tetracaine as a Neurolytic Agent for Ultralong Sciatic Nerve Block , 1996, Anesthesiology.

[2]  B. Castellano,et al.  Electrophysiological evaluation of spinal reflexes during epidural anesthesia in an experimental model , 1996, Muscle & nerve.

[3]  G. Strichartz,et al.  Relation between Functional Deficit and Intraneural Local Anesthetic during Peripheral Nerve Block: A Study in the Rat Sciatic Nerve , 1995, Anesthesiology.

[4]  M. Arboix,et al.  Bupivacaine disposition and pharmacologic effects after intravenous and epidural administrations in dogs. , 1995, American journal of veterinary research.

[5]  X. Navarro,et al.  Comparison of Regenerative and Reinnervating Capabilities of Different Functional Types of Nerve Fibers , 1994, Experimental Neurology.

[6]  H. Turndorf,et al.  Prolonged Analgesia With Liposomal Bupivacaine in a Mouse Model , 1993, Regional Anesthesia & Pain Medicine.

[7]  R. Langer,et al.  Prolonged Regional Nerve Blockade by Controlled Release of Local Anesthetic from a Biodegradable Polymer Matrix , 1993, Anesthesiology.

[8]  R. Myers,et al.  Relative Neural Toxicity of Local Anesthetics , 1993, Journal of neuropathology and experimental neurology.

[9]  H. Renck,et al.  Duration of experimental nerve block by combinations of local anesthetic agents , 1993, Acta anaesthesiologica Scandinavica.

[10]  H. Turndorf,et al.  Prolongation of epidural anesthesia using a lipid drug carrier with procaine, lidocaine, and tetracaine. , 1992, Anesthesia and analgesia.

[11]  G. Cevc,et al.  Noninvasive percutaneous induction of topical analgesia by a new type of drug carrier, and prolongation of local pain insensitivity by anesthetic liposomes. , 1992, Anesthesia and analgesia.

[12]  H. Turndorf,et al.  Prolongation of spinal anesthesia. Differential action of a lipid drug carrier on tetracaine, lidocaine, and procaine. , 1992, Anesthesiology.

[13]  Y. Inagaki,et al.  Prolongation of canine epidural anesthesia by liposome encapsulation of lidocaine. , 1992, Anesthesia and analgesia.

[14]  K. Drasner,et al.  Cauda Equina Syndrome After Continuous Spinal Anesthesia , 1991, Anesthesia and analgesia.

[15]  S. Benita,et al.  Spinal anesthesia: significant prolongation of the pharmacologic effect of tetracaine with lipid solution of the agent. , 1991, Anesthesiology.

[16]  G. Strichartz,et al.  Fundamental Properties of Local Anesthetics. II. Measured Octanol: Buffer Partition Coefficients and pKa Values of Clinically Used Drugs , 1990, Anesthesia and analgesia.

[17]  R. Penn,et al.  The Effect of Chronic Subarachnoid Bupivacaine Infusion in Dogs , 1987, Anesthesiology.

[18]  F. Reynolds Adverse effects of local anaesthetics. , 1987, British journal of anaesthesia.

[19]  R. Penn,et al.  Effect of repetitive lidocaine infusion on peripheral nerve , 1986, Experimental Neurology.

[20]  T. Yaksh,et al.  Epidural Injections of Bupivacaine, Morphine, Fentanyl, Lofentanil, and DADL in Chronically Implanted Rats: A Pharmacologic and Pathologic Study , 1986, Anesthesiology.

[21]  S. M. Sumi,et al.  Neurotoxicity of Intrathecal Local Anesthetics in Rabbits , 1985, Anesthesiology.

[22]  K. van Deyk,et al.  [Delayed respiratory arrest following spinal anesthesia]. , 1984, Regional-Anaesthesie.

[23]  R. E. Kane Neurologic Deficits following Epidural or Spinal Anesthesia , 1981, Anesthesia and analgesia.

[24]  B. Covino,et al.  A Chronic Model for Investigation of Experimental: Spinal Anesthesia in the Dog , 1981, Anesthesiology.

[25]  B. Covino,et al.  Differential Sensitivities of Mammalian Nerve Fibers to Local Anesthetic Agents , 1980, Anesthesiology.

[26]  G A Albright,et al.  Cardiac arrest following regional anesthesia with etidocaine or bupivacaine. , 1979, Anesthesiology.