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含1:100,000和1:200,000肾上腺素的高剂量阿替卡因的药代动力学及心血管效应

The pharmacokinetics and cardiovascular effects of high-dose articaine with 1:100,000 and 1:200,000 epinephrine.

作者信息

Hersh Elliot V, Giannakopoulos Helen, Levin Lawrence M, Secreto Stacey, Moore Paul A, Peterson Carrie, Hutcheson Matthew, Bouhajib Mohammed, Mosenkis Ari, Townsend Raymond R

机构信息

Oral and Maxillofacial Surgery and Pharmacology, School of Dental Medicine, University of Pennsylvania, 240 South 40th St., Philadelphia, PA 19104-6003, USA.

出版信息

J Am Dent Assoc. 2006 Nov;137(11):1562-71. doi: 10.14219/jada.archive.2006.0092.

Abstract

OBJECTIVES

The authors conducted a randomized, double-blind, two-way crossover clinical trial to compare the pharmacokinetics and cardiovascular effects of 11.9 milliliters of 4 percent articaine hydrochloride (HCl) plus 1:100,000 epinephrine (A100) with those of 11.9 mL of 4 percent articaine HCl plus 1:200,000 epinephrine (A200).

METHODS

During two testing sessions, the authors administered injections of A100 and A200 over a seven-minute period (in one-cartridge doses unless otherwise noted): maxillary right first molar infiltration, maxillary left first molar infiltration, maxillary right first premolar infiltration, maxillary left first premolar infiltration, right inferior alveolar injection, left inferior alveolar injection, right long buccal infiltration (one-half cartridge) and left long buccal infiltration (one-half cartridge). They analyzed venous blood samples for articaine levels. They used noninvasive acoustic tonometry to measure a variety of cardiovascular parameters over a two-hour period.

RESULTS

Plasma concentration curves of articaine over time were similar for both solutions, with peak concentrations and times to maximum concentration being 2,037 nanograms per milliliter and 22 minutes for A100 and 2,145 ng/mL and 22 minutes for A200. At the 10-minute point, the mean systolic blood pressure and heart rate were significantly elevated (P < .05) with A100 versus A200.

CONCLUSIONS

Maximum dose recommendations for the A100 solution also can be applied to the A200 solution. A200 produces less cardiovascular stimulation than does A100.

CLINICAL IMPLICATIONS

A200 is as safe as A100, and may be preferable to A100 in patients with cardiovascular disease and in those taking drugs that reportedly enhance the systemic effects of epinephrine.

摘要

目的

作者进行了一项随机、双盲、双向交叉临床试验,以比较11.9毫升4%盐酸阿替卡因加1:100,000肾上腺素(A100)与11.9毫升4%盐酸阿替卡因加1:200,000肾上腺素(A200)的药代动力学和心血管效应。

方法

在两个测试阶段,作者在7分钟内注射A100和A200(除非另有说明,均为单支剂量):右上颌第一磨牙浸润、左上颌第一磨牙浸润、右上颌第一前磨牙浸润、左上颌第一前磨牙浸润、右下牙槽注射、左下牙槽注射、右长颊侧浸润(半支)和左长颊侧浸润(半支)。他们分析静脉血样中的阿替卡因水平。他们使用无创声反射测压法在两小时内测量各种心血管参数。

结果

两种溶液中阿替卡因的血浆浓度随时间变化曲线相似,A100的峰值浓度和达到最大浓度的时间分别为每毫升2037纳克和22分钟,A200为每毫升2145纳克和22分钟。在10分钟时,与A200相比,A100使平均收缩压和心率显著升高(P < .05)。

结论

A100溶液的最大剂量推荐也可应用于A200溶液。A200产生的心血管刺激比A100少。

临床意义

A200与A100一样安全,对于心血管疾病患者和服用据报道可增强肾上腺素全身作用药物的患者,A200可能比A100更可取。

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