Askmark H, Aquilonius S M, Gillberg P G, Hartvig P, Hilton-Brown P, Lindström B, Nilsson D, Stålberg E, Winkler T
Department of Neurology, University Hospital, Uppsala, Sweden.
Acta Neurol Scand. 1990 Oct;82(4):253-8. doi: 10.1111/j.1600-0404.1990.tb01615.x.
Assuming the presence of clinically significant cholinergic hypofunction in amyotrophic lateral scleroses (ALS), seven patients with ALS were treated with 100-200 mg tetrahydroaminoacridine (THA) together with 11 g lecithin daily for up to 7 weeks. In a separate experiment pharmacokinetics and effects on muscle strength and neurophysiological parameters were studied following the injection of 30 mg THA intravenously. Following the injection of THA an increase in muscle strength was observed in two patients. There were no consistent pharmacokinetic differences that could explain the effect on intravenous THA on muscle strength in these two patients. The plasma clearance of THA was high and the oral bioavailability low with large interindividual differences (6-36%). No beneficial effect was seen during oral medication and side-effects were common. There were no conclusive changes observed regarding neurophysiological parameters after drug administration. THA has probably no place in the treatment of ALS.
假设肌萎缩侧索硬化症（ALS）存在具有临床意义的胆碱能功能减退，7例ALS患者每日接受100 - 200毫克他克林（THA）联合11克卵磷脂治疗，为期7周。在另一项实验中，静脉注射30毫克THA后，研究了其药代动力学以及对肌肉力量和神经生理参数的影响。注射THA后，两名患者的肌肉力量有所增加。在这两名患者中，没有一致的药代动力学差异可以解释静脉注射THA对肌肉力量的影响。THA的血浆清除率高，口服生物利用度低，个体差异大（6 - 36%）。口服给药期间未见有益效果，且副作用常见。给药后神经生理参数未见决定性变化。THA可能在ALS治疗中没有地位。
