Tìm theo
Niacin
Các tên gọi khác (19 ) :
  • 3-carboxypyridine
  • 3-Pyridinecarboxylic acid
  • 3-Pyridylcarboxylic acid
  • Acide Nicotinique
  • Acido nicotinico
  • Acidum Nicotinicum
  • Anti-pellagra vitamin
  • beta-Pyridinecarboxylic acid
  • M-Pyridinecarboxylic Acid
  • Niacin
  • Nicotinic Acid
  • Nikotinsaeure
  • P.P. factor
  • Pellagra preventive factor
  • PP Factor
  • Pyridine-beta-carboxylic acid
  • pyridine-β-carboxylic acid
  • Vitamin B3
  • β-pyridinecarboxylic acid
Vitamin
Thuốc Gốc
Small Molecule
CAS: 59-67-6
ĐG : Abbott Laboratories Ltd. , http://www.abbott.com
CTHH: C6H5NO2
PTK: 123.1094
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]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6H5NO2
Phân tử khối
123.1094
Monoisotopic mass
123.032028409
InChI
InChI=1S/C6H5NO2/c8-6(9)5-2-1-3-7-4-5/h1-4H,(H,8,9)
InChI Key
InChIKey=PVNIIMVLHYAWGP-UHFFFAOYSA-N
IUPAC Name
pyridine-3-carboxylic acid
Traditional IUPAC Name
niacin
SMILES
OC(=O)C1=CN=CC=C1
Độ tan chảy
236.6 °C
Độ hòa tan
1.8E+004 mg/L (at 25 °C)
logP
0.36
logS
-0.84
pKa (strongest acidic)
2.79
pKa (Strongest Basic)
4.19
PSA
50.19 Å2
Refractivity
31.16 m3·mol-1
Polarizability
11.3 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
-1
Number of Rings
1
Bioavailability
1
Rule of Five
true
pKa
4.75 (at 25 °C)
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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] 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.
Dược Động Học :
▧ Absorption :
Both nicotinic acid and nicotinamide are efficiently absorbed from the stomach and small intestine.
▧ Metabolism :
Hepatic
▧ Half Life :
20-45 minutes.
Độc Tính : 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)
Chỉ Định : For the treatment of type IV and V hyperlipidemia. It is indicated as ajunctive therapy.
Tương Tác Thuốc :
  • 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.
Liều Lượng & Cách Dùng : Capsule - Oral
Capsule, extended release - Oral
Powder - Oral
Solution - Intramuscular
Tablet - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Niacor
  • Công ty :
    Sản phẩm biệt dược : Niaspan
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00627
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=938
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507508
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C00253
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00049
ChemSpider
http://www.chemspider.com/Chemical-Structure.913.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=23515
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0245-0067-11
PharmGKB
http://www.pharmgkb.org/drug/PA450617
Wikipedia
http://en.wikipedia.org/wiki/Niacin
RxList
http://www.rxlist.com/cgi/generic3/niacor.htm
Drugs.com
http://www.drugs.com/niacin.html
... loading
... loading