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药品详细

Phytonadione(植物甲萘醌)

化学结构式图
中文名
植物甲萘醌
英文名
Phytonadione
分子式
C31H46O2
化学名
2-methyl-3-[(2E,7R,11R)-3,7,11,15-tetramethylhexadec-2-en-1-yl]-1,4-dihydronaphthalene-1,4-dione
分子量
Average: 450.6957
Monoisotopic: 450.349780716
CAS号
84-80-0
ATC分类
B02B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Phytonadione is often called vitamin K1. It is a fat-soluble vitamin that is stable to air and moisture but decomposes in sunlight. It is found naturally in a wide variety of green plants. Phylloquinone is also an antidote for coumatetralyl. Vitamin K is needed for the posttranslational modification of certain proteins, mostly required for blood coagulation.

生产厂家
  • Aton pharma inc
  • Eli lilly and co
  • Glaxosmithkline
  • Hoffmann la roche inc
  • Hospira inc
  • International medication system
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes Not Available
Substructures Not Available
适应症
药理
Indication For the treatment of haemorrhagic conditions in infants, antidote for coumarin anticoagulants in hypoprothrombinaemia
Pharmacodynamics Phytonadione is a vitamin, indicated in the treatment of coagulation disorders which are due to faulty formation of factors II, VII, IX and X when caused by vitamin K deficiency or interference with vitamin K activity. Phytonadione aqueous colloidal solution of vitamin K1 for parenteral injection, possesses the same type and degree of activity as does naturally-occurring vitamin K, which is necessary for the production via the liver of active prothrombin (factor II), proconvertin (factor VII), plasma thromboplastin component (factor IX), and Stuart factor (factor X).
Mechanism of action Vitamin K is an essential cofactor for the gamma-carboxylase enzymes which catalyze the posttranslational gamma-carboxylation of glutamic acid residues in inactive hepatic precursors of coagulation factors II (prothrombin), VII, IX and X. Gamma-carboxylation converts these inactive precursors into active coagulation factors which are secreted by hepatocytes into the blood. Supplementing with Phytonadione results in a relief of vitamin K deficiency symptoms which include easy bruisability, epistaxis, gastrointestinal bleeding, menorrhagia and hematuria.
Absorption Oral phytonadione is adequately absorbed from the gastrointestinal tract only if bile salts are present. After absorption, phytonadione is initially concentrated in the liver, but the concentration declines rapidly. Very little vitamin K accumulates in tissues.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
Route of elimination Almost no free unmetabolized vitamin K appears in bile or urine.
Half life Not Available
Clearance Not Available
Toxicity The intravenous LD50 of phytonadione in the mouse is 41.5 and 52 mL/kg for the 0.2% and 1% concentrations, respectively.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State liquid
Experimental Properties
Property Value Source
melting point -20 °C PhysProp
boiling point 142.5 °C at 1.00E-03 mm Hg PhysProp
water solubility Insoluble in water Not Available
logP 9.3 Not Available
Predicted Properties
Property Value Source
water solubility 5.92e-05 g/l ALOGPS
logP 8.48 ALOGPS
logP 9.7 ChemAxon
logS -6.9 ALOGPS
pKa (strongest basic) -7.2 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 34.14 ChemAxon
rotatable bond count 14 ChemAxon
refractivity 142.96 ChemAxon
polarizability 55.92 ChemAxon
药物相互作用
Drug Interaction
Warfarin Phytonadione (vitamin K) may antagonize the anticoagulant effects of warfarin. Monitor for changes in prothrombin time if phytonadione intake (either via supplements or vitamin K-rich foods) is increased or decreased.
食物相互作用
Not Available

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