Department of Dermatology, Asahikawa Medical College, Asahikawa, Hokkaido, Japan.
J Dermatolog Treat. 2012 Apr;23(2):112-5. doi: 10.3109/09546634.2010.507702. Epub 2011 Jan 22.
Although ciclosporin is useful for atopic dermatitis (AD), appropriate dosage and therapeutic drug monitoring (TDM) has been performed only by post-prandial ciclosporin administration. We administered ciclosporin pre-prandially to eight severe adult AD patients (four cases of erythrodermic AD, three cases of AD recalcitrant to standard therapy, and one AD case with numerous pruriginous lesions). Blood concentrations of ciclosporin at various dosages were measured and appropriate dosage in terms of therapeutic efficacy was analyzed by using the area under the concentration curve (AUC). AUC was estimated by the C1 (obtained serum concentration of ciclosporin at 1 hour after ciclosporin administration), C2 (concentration of ciclosporin at 2 hours) and C4 (concentration of ciclosporin at 4 hours) concentrations of ciclosporin. The trough levels of ciclosporin with 200 mg/day, 150 mg/day, and 100 mg/day administration were 96.5 ng/ml, 66.4 ng/ml, and 75.3 ng/ml, respectively. The peak serum concentration (C(max)) was obtained at 1 hour (C1) in most cases. The AUC of 0-4 hours (AUC 0-4) were 2099.5 ng · h/ml (200 mg/day), 1782.6 ng · h/ml (150 mg/day) and 1696.2 ng · h/ml (100 mg/day). VAS scores of itching and blood eosinophil counts were decreased significantly by the ciclosporin treatment. Pre-prandial administration of a relatively low dose of ciclosporin for severe atopic dermatitis resulted in a favorable subjective and objective clinical response and the measurement of blood concentration mostly correlated with the effective dosage assessment.
虽然环孢素对特应性皮炎(AD)有效,但仅通过餐后给药进行适当的剂量和治疗药物监测(TDM)。我们给 8 例严重成人 AD 患者(4 例红皮病 AD,3 例标准治疗难治性 AD,1 例伴有大量瘙痒性皮损的 AD)进行餐前环孢素给药。测量了不同剂量的环孢素血药浓度,并通过浓度曲线下面积(AUC)分析了治疗效果的适当剂量。AUC 通过环孢素的 C1(给药后 1 小时获得的环孢素血清浓度)、C2(环孢素 2 小时时的浓度)和 C4(环孢素 4 小时时的浓度)浓度来估算。200 mg/天、150 mg/天和 100 mg/天给药的环孢素谷浓度分别为 96.5ng/ml、66.4ng/ml 和 75.3ng/ml。大多数情况下,在 1 小时(C1)时可获得最高血清浓度(C(max))。0-4 小时(AUC 0-4)的 AUC 分别为 2099.5ng·h/ml(200 mg/天)、1782.6ng·h/ml(150 mg/天)和 1696.2ng·h/ml(100 mg/天)。环孢素治疗后瘙痒 VAS 评分和血嗜酸性粒细胞计数明显降低。对于严重特应性皮炎,餐前给予相对低剂量的环孢素可获得良好的主观和客观临床反应,并且血药浓度的测量大多与有效剂量评估相关。