Taskinen M R, Nikkilä E A
Second Department of Medicine, University of Helsinki, Finland.
Atherosclerosis. 1988 Feb;69(2-3):249-55. doi: 10.1016/0021-9150(88)90021-4.
Two separate studies were carried out with acipimox, a new antilipolytic agent with long-lasting activity. First, in a randomized, double-blind, cross-over study a dose of 750 mg/day of acipimox versus placebo was employed for 60 days in 11 patients with type IV hyperlipoproteinemia. Mean plasma triglyceride levels were reduced after acipimox compared to placebo (434 +/- 60 vs 777 +/- 224 mg/dl, P less than 0.01). Serum total cholesterol fell also significantly after acipimox compared to placebo. No significant alteration was observed in the HDL2/HDL3 ratio or in the concentration or composition of the HDL subfractions. Six patients with severe hypertriglyceridemia (2 type IV and 4 type V) and low lipoprotein lipase (LPL) activity took part in a second, open study, lasting for 9 months. Acipimox was given at a dose of 750 mg/day for the first 6 months and 1200 mg/day for the last period. The response of serum total and VLDL triglycerides was inconsistent. HDL cholesterol was significantly raised (+33.3%) after 9 months of treatment due to changes of HDL2 and HDL3 cholesterol, phospholipid and protein concentrations. LPL activity was markedly reduced in adipose tissue at 9 months. No significant changes occurred in postheparin plasma LPL activity. In contrast, hepatic lipase activity showed a reduction of about 25% from 6 months of treatment onwards.
使用阿西莫司（一种具有长效活性的新型抗脂解剂）进行了两项独立研究。首先，在一项随机、双盲、交叉研究中，11名IV型高脂蛋白血症患者服用750毫克/天的阿西莫司，与安慰剂对照，持续60天。与安慰剂相比，服用阿西莫司后平均血浆甘油三酯水平降低（434±60对777±224毫克/分升，P<0.01）。与安慰剂相比，服用阿西莫司后血清总胆固醇也显著下降。HDL2/HDL3比值或HDL亚组分的浓度或组成未观察到显著变化。6名重度高甘油三酯血症患者（2名IV型和4名V型）且脂蛋白脂肪酶（LPL）活性较低，参与了第二项为期9个月的开放研究。阿西莫司在前6个月的剂量为750毫克/天，最后阶段为1200毫克/天。血清总甘油三酯和VLDL甘油三酯的反应不一致。由于HDL2和HDL3胆固醇、磷脂和蛋白质浓度的变化，治疗9个月后HDL胆固醇显著升高（+33.3%）。9个月时脂肪组织中的LPL活性显著降低。肝素后血浆LPL活性未发生显著变化。相反，从治疗6个月起，肝脂酶活性降低了约25%。
