Sawyer D R, Ludden T M, Crawford M H
Arch Intern Med. 1981 Jan;141(1):43-5.
Recent studies suggest that lidocaine hydrochloride continues to accumulate during prolonged infusions. Plasma levels of lidocaine and monoethylglycinexylidide (MEGX) were measured in 26 patients with cardiac arrhythmias during lidocaine infusions of 15 to 69 hours' duration. Clearance varied, ranging from 3.2 to 14.7 mL/min/kg, and was significantly less in the ten patients with heart failure (5.8 +/- 1.7 mL/min/kg) as compared with the remaining 16 (8.4 +/- 2.6 mL/min/kg; P < .05). The MEGX levels were < 1 microgram/mL. In four patients, steady states were achieved at two different infusion rates, and changes in lidocaine plasma levels were generally proportional to changes in infusion rates. Lidocaine elimination half-lives ranged from 3.2 to 8.7 hours, and no accumulation continued beyond four half-lives. Clearance values, elimination half-lives, apparent volumes of distribution, and, consequently, steady-state levels were widely variable, which can be partly explained by the inclusion of patients with congestive heart failure. Monitoring of serum lidocaine levels may aid in individualization of therapy.
近期研究表明,在长时间输注过程中,盐酸利多卡因会持续蓄积。对26例心律失常患者在持续输注利多卡因15至69小时期间测定了利多卡因和单乙基甘氨酰二甲苯酰胺(MEGX)的血浆水平。清除率各不相同,范围为3.2至14.7 mL/(min·kg),与其余16例患者(8.4±2.6 mL/(min·kg))相比,10例心力衰竭患者的清除率明显更低(5.8±1.7 mL/(min·kg);P<0.05)。MEGX水平<1μg/mL。在4例患者中,以两种不同的输注速率达到了稳态,利多卡因血浆水平的变化通常与输注速率的变化成比例。利多卡因消除半衰期为3.2至8.7小时,在四个半衰期之后未继续蓄积。清除率值、消除半衰期、表观分布容积以及因此的稳态水平差异很大,这部分可以通过纳入充血性心力衰竭患者来解释。监测血清利多卡因水平可能有助于实现个体化治疗。