Articles: anesthetics.
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Neurotoxicity after subarachnoid infusion of bupivacaine, lignocaine and 2-chloroprocaine was studied in a chronic rat model. Hartmann's solution 100 microliter h-1 was infused as a control, and 0.5% bupivacaine, 1.5% lignocaine and 2.0% 2-chloroprocaine were infused at 100 microliter h-1 for 3, 6 or 24 h, to five rats in each group. ⋯ Abnormal histology, in the form of neuronal vacuolation, was not a sensitive index, being present in control rats, but more intense in those receiving lignocaine and 2-chloroprocaine than in those given bupivacaine; no correlation with clinical findings could be established. The neurotoxic effects of each local anaesthetic tested as a continuous intrathecal infusion were dose related in the rat, which may be a useful model for screening other local anaesthetics.
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[3H]Batrachotoxinin A benzoate ( [3H]BTX-B) binds with high affinity to sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex. In this preparation, local anesthetics competitively antagonize the binding of [3H]BTX-B. The potencies of some 40 classical local anesthetics and a variety of catecholamine, histamine, serotonin, adenosine, GABA, glycine, acetylcholine, and calcium antagonists, tranquilizers, antidepressants, barbiturates, anticonvulsants, steroids, vasodilators, antiinflammatories, anticoagulants, analgesics, and other agents have been determined. An excellent correlation with the known local anesthetic activity of many of these agents indicate that antagonism of binding of [3H]BTX-B binding provides a rapid, quantitative, and facile method for the screening and investigation of local anesthetic activity.
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Randomized Controlled Trial Clinical Trial
Clinical study of a lignocaine-prilocaine cream to relieve the pain of venepuncture.
The efficacy of a topical anaesthetic formulation, EMLA 5% cream (Eutectic Mixture of Local Anaesthetics) in obtunding the pain produced by venepuncture, was determined in a double-blind randomized, cross-over study in 31 adult volunteers. Pain was registered on a 10-cm visual analogue scale. ⋯ Transient skin reactions (blanching, erythema and oedema) were observed with both formulations. These reactions were not found to be aggravated by repeated applications.
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One century after the clinical introduction of cocaine, local anesthesia remains the most important method of pain control in dentistry. Many local anesthetics have been marketed since 1884, and it is likely that attempts to produce drugs that enhance anesthetic efficacy, reduce systemic and local toxicity, and increase nociceptive selectivity, will continue. ⋯ Of fundamental importance to such improvements are investigations into the pharmacology of drugs with local anesthetic activity and anatomical and physiologic studies pertaining to the reasons why local anesthetics sometimes fail to achieve desired results. This paper reviews recent advances in our understanding of these drugs and their clinical use.