Le Pelley E, Klossek J M, Bouquet S, Ferrier B, Fusciardi J
Département d'Anesthésie-Réanimation Chirurgicale, CHU la Milétrie, Poitiers.
Ann Fr Anesth Reanim. 1995;14(6):472-7. doi: 10.1016/s0750-7658(05)80487-3.
To assess the pharmacokinetics and clinical tolerance of a 33% cocaine solution administered topically for intranasal surgery.
Clinical prospective open trial.
Twelve ASA I patients scheduled for intranasal surgery were sedated with midazolam 2 mg and fentanyl 50 micrograms. Topical anaesthesia was obtained with aqueous 33% cocaine HCl 360 mg, lidocaine HCl 140 mg, adrenaline 0.04 mg and naphazoline 0.4 mg. Venous blood samples were taken before cocaine application and 15, 30, 45, 60, 90, 120, 150, 180, 240 min later. The plasma was immediately separated and the samples were frozen. The concentration of cocaine was measured by HPLC. Potential cardiotoxic and neurotoxic effects were clinically monitored.
The mean dose of cocaine applied was 5.85 +/- 1.3 mg.kg-1 and the dose actually delivered was 4 +/- 1.5 mg.kg-1. The Cmax was 859 +/- 503 ng.mL-1 after a Tmax to 47 +/- 17 min. The mean elimination half-life was 87 +/- 19 min (mean +/- SD). The total clearance and the volume of distribution were respectively 4,521 +/- 1,858 mL.min-1 and 568 +/- 273 L. No clinical evidence of toxicity was found.
This study shows that it is possible to perform major intranasal surgery under topical anaesthesia with a concentrated solution (33%) of cocaine at a high dose (6 mg.kg-1). These results differ completely with data obtained in addicts.
评估用于鼻内手术的33%可卡因溶液的药代动力学及临床耐受性。
临床前瞻性开放试验。
12例计划行鼻内手术的ASA I级患者，用2 mg咪达唑仑和50微克芬太尼镇静。用含360 mg 33%盐酸可卡因、140 mg盐酸利多卡因、0.04 mg肾上腺素和0.4 mg萘甲唑啉的水溶液进行局部麻醉。在应用可卡因前及应用后15、30、45、60、90、120、150、180、240分钟采集静脉血样。血浆立即分离，样本冷冻。用高效液相色谱法测定可卡因浓度。临床监测潜在的心脏毒性和神经毒性作用。
可卡因的平均应用剂量为5.85±1.3 mg·kg-1，实际给药剂量为4±1.5 mg·kg-1。达峰时间（Tmax）为47±17分钟后，峰浓度（Cmax）为859±503 ng·mL-1。平均消除半衰期为87±19分钟（平均值±标准差）。总清除率和分布容积分别为4521±1858 mL·min-1和568±273 L。未发现临床毒性证据。
本研究表明，使用高剂量（6 mg·kg-1）的浓缩（33%）可卡因溶液进行局部麻醉，有可能实施大型鼻内手术。这些结果与在成瘾者中获得的数据完全不同。
