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药品详细

Pentoxifylline(己酮可可碱)

化学结构式图
中文名
己酮可可碱
英文名
Pentoxifylline
分子式
C13H18N4O3
化学名
3,7-dimethyl-1-(5-oxohexyl)-2,3,6,7-tetrahydro-1H-purine-2,6-dione
分子量
Average: 278.307
Monoisotopic: 278.137890462
CAS号
6493-05-6
ATC分类
C04A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A methylxanthine derivative that inhibits phosphodiesterase and affects blood rheology. It improves blood flow by increasing erythrocyte and leukocyte flexibility. It also inhibits platelet aggregation. Pentoxifylline modulates immunologic activity by stimulating cytokine production. [PubChem]

生产厂家
  • Actavis elizabeth llc
  • Apotex inc
  • Biovail laboratories inc
  • Heritage pharmaceuticals inc
  • Impax laboratories inc
  • Mylan pharmaceuticals inc
  • Pliva inc
  • Sanofi aventis us llc
  • Teva pharmaceuticals usa inc
  • Upsher smith laboratories inc
  • Watson laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. : European Pentoxifylline Multi-Infarct Dementia Study. Eur Neurol. 1996;36(5):315-21. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Xanthines
Substructures
  • Xanthines
  • Pyrimidines and Derivatives
  • Imidazoles
  • Heterocyclic compounds
  • Aromatic compounds
  • Purines and Purine Derivatives
  • Cyanamides
  • Ketones
适应症
药理
Indication For the treatment of patients with intermittent lameness or immobility arising from chronic occlusive arterial disease of the limbs.
Pharmacodynamics Pentoxifylline, a synthetic dimethylxanthine derivative structurally related to theophylline and caffeine, is used in the treatment of peripheral vascular diseases and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy.
Mechanism of action Pentoxifylline inhibits erythrocyte phosphodiesterase, resulting in an increase in erythrocyte cAMP activity. Subsequently, the erythrocyte membrane becomes more resistant to deformity. Along with erythrocyte activity, pentoxifylline also decreases blood viscosity by reducing plasma fibrinogen concentrations and increasing fibrinolytic activity. It is also a non selective adenosine receptor antagonist.
Absorption Not Available
Volume of distribution Not Available
Protein binding 70%
Metabolism
Not Available
Route of elimination Excretion is almost totally urinary; the main biotransformation product is Metabolite V. Essentially no parent drug is found in the urine.
Half life 0.4-0.8 hours
Clearance Not Available
Toxicity LD50=1385 mg/kg(orally in mice)
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 105 °C Not Available
water solubility 7.7E+004 mg/L (at 25 °C) MERCK INDEX (1996)
logP 0.29 BIOBYTE (1995)
Predicted Properties
Property Value Source
water solubility 5.17e+00 g/l ALOGPS
logP 0.08 ALOGPS
logP 0.23 ChemAxon
logS -1.7 ALOGPS
pKa (strongest acidic) 19.64 ChemAxon
pKa (strongest basic) -0.93 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 4 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 75.51 ChemAxon
rotatable bond count 5 ChemAxon
refractivity 73.52 ChemAxon
polarizability 29.27 ChemAxon
药物相互作用
Drug Interaction
Acenocoumarol Pentoxifylline may increase the anticoagulant effect of acenocoumarol.
Aminophylline Pentoxifylline may increase the effect and toxicity of aminophylline.
Anisindione Pentoxifylline may increase the anticoagulant effect of anisindione.
Dicumarol Pentoxifylline may increase the anticoagulant effect of dicumarol.
Dyphylline Pentoxifylline increases the effect and toxicity of theophylline
Insulin Lispro Concomitant therapy with drugs that may increase the blood-glucose-lowering effect of insulin lispro and thus the chance of hypoglycemia should be monitored closely.
Oxtriphylline Pentoxifylline increases the effect and toxicity of theophylline
Theophylline Pentoxifylline increases the effect and toxicity of theophylline
Warfarin Pentoxifylline may increase the anticoagulant effect of warfarin.
食物相互作用
  • Take with food to reduce irritation. Limit caffeine intake.

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