Chauvin M
Département d'Anesthésie-Réanimation, Hôpital Ambroise-Paré, Boulogne.
Ann Fr Anesth Reanim. 1988;7(3):216-23. doi: 10.1016/s0750-7658(88)80114-x.
A patient's condition may alter the pharmacokinetic and pharmacodynamic characteristics of local anaesthetics and so increase the risk of toxicity. In the elderly patient, the elimination half-life is increased for both lidocaine and bupivacaine; the risk of overdose is therefore increased when the local anaesthetic agent is given in repeated doses and as a continuous infusion. Cardiotoxicity due to bupivacaine seems to be worsened by pregnancy. In the foetus and newborn, local anaesthetic toxicity gives the same clinical picture as in the adult and is increased in the presence of acidosis and anoxia. Bupivacaine depressive effects are increased by tachycardias, intraventricular blocks and all the conditions which are known to depolarize the cardiac cell membrane (e.g. hyperkaliemia, acidosis, severe hypoxia, myocardial ischaemia). Drug interactions may also potentiate the toxicity of lidocaine and bupivacaine, such as calcium blockers and diazepam. The effects of other conditions (cirrhosis, renal failure, epilepsy) and other drug interactions, specially those modifying free fraction and elimination of local anaesthetics, are also discussed.
患者的病情可能会改变局部麻醉药的药代动力学和药效学特性，从而增加毒性风险。对于老年患者，利多卡因和布比卡因的消除半衰期均会延长；因此，当局部麻醉药重复给药或持续输注时，过量用药的风险会增加。布比卡因所致的心脏毒性在妊娠时似乎会加重。在胎儿和新生儿中，局部麻醉药毒性的临床表现与成人相同，且在存在酸中毒和缺氧的情况下会增加。心动过速、室内传导阻滞以及所有已知会使心肌细胞膜去极化的情况（如高钾血症、酸中毒、严重缺氧、心肌缺血）都会增强布比卡因的抑制作用。药物相互作用也可能增强利多卡因和布比卡因的毒性，如钙通道阻滞剂和地西泮。文中还讨论了其他情况（肝硬化、肾衰竭、癫痫）以及其他药物相互作用的影响，特别是那些改变局部麻醉药游离分数和消除的相互作用。
