Nicotinic acid: an old drug with a promising future

被引:100
作者
Bodor, E. T. [1 ]
Offermanns, S. [1 ]
机构
[1] Heidelberg Univ, Inst Pharmacol, D-69120 Heidelberg, Germany
关键词
lipid-lowering drugs; HDL cholesterol; lipid metabolism; G-protein-coupled receptor; flushing;
D O I
10.1038/sj.bjp.0707528
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Nicotinic acid has been used for decades to treat dyslipidaemic states. In particular its ability to raise the plasma HDL cholesterol concentration has led to an increased interest in its pharmacological potential. The clinical use of nicotinic acid is somewhat limited due to several harmless but unpleasant side effects, most notably a cutaneous flushing phenomenon. With the recent discovery of a nicotinic acid receptor, it has become possible to better understand the mechanisms underlying the metabolic and vascular effects of nicotinic acid. Based on these new insights into the action of nicotinic acid, novel strategies are currently under development to maximize the pharmacological potential of this drug. The generation of both flush reducing co-medications of nicotinic acid and novel drugs targeting the nicotinic acid receptor will provide future therapeutic options for the treatment of dyslipidaemic disorders.
引用
收藏
页码:S68 / S75
页数:8
相关论文
共 80 条
[1]   NICOTINIC-ACID INHIBITS ADIPOCYTE ADENYLATE-CYCLASE IN A HORMONE-LIKE MANNER [J].
AKTORIES, K ;
JAKOBS, KH ;
SCHULTZ, G .
FEBS LETTERS, 1980, 115 (01) :11-14
[2]   INFLUENCE OF NICOTINIC ACID ON SERUM CHOLESTEROL IN MAN [J].
ALTSCHUL, R ;
HOFFER, A ;
STEPHEN, JD .
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1955, 54 (02) :558-559
[3]  
ANDERSSON RGG, 1977, ACTA PHARMACOL TOX, V41, P1
[4]  
[Anonymous], 1975, JAMA-J AM MED ASSOC, V231, P360
[5]   New insights into renal transport of urate [J].
Anzai, Naohiko ;
Kanai, Yoshikatsu ;
Endou, Hitoshi .
CURRENT OPINION IN RHEUMATOLOGY, 2007, 19 (02) :151-157
[6]   GPR109A (PUMA-G/HM74A) mediates nicotinic acid-induced flushing [J].
Benyó, Z ;
Gille, A ;
Kero, J ;
Csiky, M ;
Suchánková, MC ;
Nüsing, RM ;
Moers, A ;
Pfeffer, K ;
Offermanns, S .
JOURNAL OF CLINICAL INVESTIGATION, 2005, 115 (12) :3634-3640
[7]   Nicotinic acid-induced flushing is mediated by activation of epidermal langerhans cells [J].
Benyo, Zoltan ;
Gille, Andreas ;
Bennett, Clare L. ;
Clausen, Bjoern E. ;
Offermanns, Stefan .
MOLECULAR PHARMACOLOGY, 2006, 70 (06) :1844-1849
[8]   Lipoprotein(a) An elusive cardiovascular risk factor [J].
Berglund, L ;
Ramakrishnan, R .
ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY, 2004, 24 (12) :2219-2226
[9]   HIGH-DENSITY LIPOPROTEIN METABOLISM IN MAN [J].
BLUM, CB ;
LEVY, RI ;
EISENBERG, S ;
HALL, M ;
GOEBEL, RH ;
BERMAN, M .
JOURNAL OF CLINICAL INVESTIGATION, 1977, 60 (04) :795-807
[10]   Niaspan® in the management of dyslipidaemia:: the evidence [J].
Brown, B. Greg .
EUROPEAN HEART JOURNAL SUPPLEMENTS, 2006, 8 (0F) :F60-F67