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药品详细

Niacin(烟酸)

化学结构式图
中文名
烟酸
英文名
Niacin
分子式
C6H5NO2
化学名
pyridine-3-carboxylic acid
分子量
Average: 123.1094
Monoisotopic: 123.032028409
CAS号
59-67-6
ATC分类
C04A 未知;C10A 未知
药物类型
small molecule
阶段
approved, nutraceutical
商品名
同义名
基本介绍

A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has pellagra-curative, vasodilating, and antilipemic properties. [PubChem]

生产厂家
  • Abbott laboratories
  • Barr laboratories inc
  • Everylife
  • Halsey drug co inc
  • Impax laboratories inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Medpointe pharmaceuticals medpointe healthcare inc
  • Mk laboratories inc
  • Purepac pharmaceutical co
  • Sandoz inc
  • Sanofi aventis us llc
  • Tablicaps inc
  • Upsher smith laboratories inc
  • Watson laboratories inc
  • West ward pharmaceutical corp
  • Wockhardt ltd
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Gopal E, Fei YJ, Miyauchi S, Zhuang L, Prasad PD, Ganapathy V: Sodium-coupled and electrogenic transport of B-complex vitamin nicotinic acid by slc5a8, a member of the Na/glucose co-transporter gene family. Biochem J. 2005 May 15;388(Pt 1):309-16. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Amino Acids
  • Pyridines and Derivatives
Substructures
  • Amino Acids
  • Hydroxy Compounds
  • Acetates
  • Pyridines and Derivatives
  • Carboxylic Acids and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
适应症
药理
Indication For the treatment of type IV and V hyperlipidemia. It is indicated as ajunctive therapy.
Pharmacodynamics Niacin and niacinamide are indicated for prevention and treatment of vitamin B3 deficiency states. Vitamin B3 (Niacin) also acts to reduce LDL cholesterol, triglycerides, and HDL cholesterol. The magnitude of individual lipid and lipoprotein responses may be influenced by the severity and type of underlying lipid abnormality. The increase in total HDL is associated with a shift in the distribution of HDL subfractions (as defined by ultra-centrifugation) with an increase in the HDL2:HDL3 ratio and an increase in apolipoprotein A-I content. Vitamin B3 (Niacin) treatment also decreases the serum levels of apolipoprotein B-100 (apo B), the major protein component of the VLDL (very low-density lipoprotein) and LDL fractions, and of lipoprotein-a, a variant form of LDL independently associated with coronary risk.
Mechanism of action Niacin binds to Nicotinate D-ribonucleotide phyrophsopate phosphoribosyltransferase, Nicotinic acid phosphoribosyltransferase, Nicotinate N-methyltransferase and the Niacin receptor. Niacin is the precursor to nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP), which are vital cofactors for dozens of enzymes. The mechanism by which niacin exerts its lipid lowering effects is not entirely understood, but may involve several actions, including a decrease in esterification of hepatic triglycerides. Niacin treatment also decreases the serum levels of apolipoprotein B-100 (apo B), the major protein component of the VLDL (very low-density lipoprotein) and LDL fractions.
Absorption Both nicotinic acid and nicotinamide are efficiently absorbed from the stomach and small intestine.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Hepatic
Route of elimination Not Available
Half life 20-45 minutes.
Clearance Not Available
Toxicity Nicotinic acid can cause vasodilation of cutaneous blood vessels resulting in increased blood flow, principally in the face, neck and chest. This produces the niacin- or nicotinic acid-flush. The niacin-flush is thought to be mediated via the prostaglandin prostacyclin. Histamine may also play a role in the niacin-flush. Flushing is the adverse reaction first observed after intake of a large dose of nicotinic acid, and the most bothersome one. LD50 7000 mg/kg (Rat)
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 236.6 °C PhysProp
water solubility 1.8E+004 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP 0.36 SANGSTER (1993)
logS -0.84 ADME Research, USCD
pKa 4.75 (at 25 °C) DEAN,JA (1985)
Predicted Properties
Property Value Source
water solubility 8.31e+01 g/l ALOGPS
logP 0.29 ALOGPS
logP -0.17 ChemAxon
logS -0.17 ALOGPS
pKa (strongest acidic) 2.79 ChemAxon
pKa (strongest basic) 4.19 ChemAxon
physiological charge -1 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 50.19 ChemAxon
rotatable bond count 1 ChemAxon
refractivity 31.16 ChemAxon
polarizability 11.3 ChemAxon
药物相互作用
Drug Interaction
Colesevelam Bile Acid Sequestrants may decrease the absorption of Niacin. It may be prudent to separate the administration times of niacin and bile acid sequestrants by a few hours in order to reduce the potential for reduced efficacy of these agents. The manufacturer of colesevelam recommends that drugs should be administered at least 1 hour before or 4 hours after colesevelam.
Lovastatin Risk of severe myopathy/rhabdomyolysis with this combination
Pitavastatin Increased incidence of adverse drug reactions (ie. rhabdomyolysis) of both niacin and pitavastatin via pharmacodynamic synergism. Use alternative therapy.
食物相互作用
  • Avoid alcohol.
  • Take with food.

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