Contrasting effects of unmodified and time-release forms of niacin on lipoproteins in hyperlipidemic subjects: clues to mechanism of action of niacin.
Contrasting effects of unmodified and time-release forms of niacin on lipoproteins in hyperlipidemic subjects: clues to mechanism of action of niacin.
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烟酸的未修饰形式和缓释形式对高脂血症受试者脂蛋白的影响对比：烟酸作用机制的线索。
DOI：
10.1016/0026-0495(85)90092-7
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发表时间：
1985
期刊：
影响因子：
--
通讯作者：
Poole,M
中科院分区：
文献类型：
--
作者：
Knopp,RH;Ginsberg,J;Albers,JJ;Hoff,C;Ogilvie,JT;Warnick,GR;Burrows,E;Retzlaff,B;Poole,M
为了最小化与烟酸使用相关的皮肤潮红症状，已经配制了烟酸的定时释放胶囊形式。因此，研究比较了定时释放烟酸与未修饰烟酸对脂蛋白脂质（包括HDL 2和HDL 3）、载脂蛋白A-I和A-II、临床化学、症状性副作用和药物治疗方案依从性的影响。71名原发性高胆固醇血症受试者被随机分配至未修饰的烟酸或缓释烟酸组，并服用药物6个月。两组在拟人和血脂变量上非常接近。在治疗的第一个月，两组对1.5 g/d剂量治疗方案的依从性相似。此后，在剂量为3.0 g/d时，服用未修饰烟酸的受试者的依从性超过90%，但服用缓释烟酸的受试者仅为64%，主要是因为胃肠道症状加重;然而，皮肤潮红副作用在缓释烟酸中稍不常见。在这些粘附水平下，未修饰的烟酸使LDL胆固醇（C）降低21%，缓释形式降低13%。血浆总甘油三酯减少与未修饰的烟酸（27%）比时间释放烟酸（8%最大），HDL-C和HDL 2-C显着增加与未修饰的烟酸（26%和36%），并没有显着改变的时间释放烟酸。两种治疗方案升高程度相似的是HDL 3-C（≥ 35%）和apoA-I（≥ 12%）。ApoA-II不受任何药物方案的影响。除了缓释组SGOT和碱性磷酸酶水平略高外，两种方案对临床化学检查的影响无差异。我们的结论是，未修饰的烟酸可能是最好的高脂血症，特别是在合并甘油三酯和胆固醇升高的受试者开始治疗，但时间释放烟酸可能是有价值的受试者严重潮红症状和高胆固醇血症的主要障碍。烟酸降低甘油三酯和升高HDL的机制似乎与降低LDL胆固醇的机制不同，升高HDL 2和HDL 3胆固醇的机制也不同。这两种形式的烟酸可以作为研究脂蛋白相互关系的探针。
To minimize the cutaneous flushing symptoms associated with niacin use, a time-release capsule form of niacin has been formulated. Thus study compares the effects of time-release niacin with those of unmodified niacin on lipoprotein lipids, including HDL2and HDL3, apoproteins A-I and A-II, clinical chemistries, symptomatic side effects, and adherence to the medication regimen. Seventy-one primarily hypercholesterolemic subjects were randomized to either unmodified niacin or time-release niacin and took medication for a six-month period. The two groups were closely matched on anthropomorphic and lipid variables. Adherence to the therapeutic regimen at a dose of 1.5 g/d in the first month of treatment was similar in the two groups. Thereafter, at a dose of 3.0 g/d, adherence was in excess of 90% among subjects taking unmodified niacin but only 64% among those taking time-release niacin, chiefly because of aggravated gastrointestinal symptoms; cutaneous flushing side effects, however, were slightly less common with time-release niacin. At these levels of adherence, LDL cholesterol (C) was reduced 21% by unmodified niacin and 13% by the time release form. Plasma total triglyceride was reduced more with unmodified niacin (27%) than with time-release niacin (8% maximum), and HDL-C and HDL2-C were increased significantly with unmodified niacin (26% and 36%) and were not significantly changed by time-release niacin. Increased to a similar degree on both regimens were HDL3-C (∼35%) and apoA-I (∼12%). ApoA-II was not affected by either drug regimen. There were no differences in the effects of the two regimens on clinical chemistry tests except for slightly higher SGOT and alkaline phosphatase levels in the time-release group. We conclude that unmodified niacin may be preferable in initiating therapy for hyperlipidemia, particularly in subjects with combined elevations of triglyceride and cholesterol, but that time-release niacin may be of value in subjects with severe flushing symptoms and hypercholesterolemia as the primary disorder. The mechanism whereby niacin lowers triglyceride and raises HDL appears to differ from the mechanism of LDL cholesterol lowering, as do the mechanisms increasing HDL2and HDL3cholesterol. The two forms of niacin can serve as probes in studying lipoprotein interrelationships.