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药品详细

Triamcinolone(曲安奈德)

化学结构式图
中文名
曲安奈德
英文名
Triamcinolone
分子式
C21H27FO6
化学名
(1R,2S,10S,11S,13R,14S,15S,17S)-1-fluoro-13,14,17-trihydroxy-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
分子量
Average: 394.4339
Monoisotopic: 394.179166801
CAS号
124-94-7
ATC分类
A01A 未知;D07A 未知;D07X 未知;H02A 未知;R01A 未知;R03B 未知;S01B 抗炎药;C05A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A glucocorticoid given, as the free alcohol or in esterified form, orally, intramuscularly, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. (From Martindale, The Extra Pharmacopoeia, 30th ed, p739)

生产厂家
  • Abbott laboratories
  • Actavis mid atlantic llc
  • Akorn inc
  • Alcon inc
  • Allergan inc
  • Alpharma us pharmaceuticals division
  • Altana inc
  • Ambix laboratories div organics corp america
  • Apothecon inc div bristol myers squibb
  • Astellas pharma us inc
  • Barr laboratories inc
  • Bristol myers squibb co
  • Bristol myers squibb co pharmaceutical research institute
  • Carolina medical products co
  • Del ray laboratories inc
  • G and w laboratories inc
  • Impax laboratories inc
  • Ivax pharmaceuticals inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Lupin atlantis holding sa switzerland
  • Lyne laboratories inc
  • Morton grove pharmaceuticals inc
  • Mylan pharmaceuticals inc
  • Parnell pharmaceuticals inc
  • Perrigo new york inc
  • Pharmaderm div altana inc
  • Pharmafair inc
  • Purepac pharmaceutical co
  • Ranbaxy laboratories inc
  • Roxane laboratories inc
  • Sandoz canada inc
  • Sandoz inc
  • Sanofi aventis us llc
  • Savage laboratories inc div altana inc
  • Solvay pharmaceuticals
  • Taro pharmaceuticals inc
  • Taro pharmaceuticals usa inc
  • Teva pharmaceuticals usa inc
  • Topiderm inc
  • Vintage pharmaceuticals llc
  • Watson laboratories inc
  • Wockhardt eu operations (swiss) ag
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
  • Steroids and Steroid Derivatives
Substructures
  • Steroids and Steroid Derivatives
  • Hydroxy Compounds
  • Alkanes and Alkenes
  • Alkyl Halides
  • Alcohols and Polyols
  • Ketones
适应症
药理
Indication For the treatment of perennial and seasonal allergic rhinitis.
Pharmacodynamics Triamcinolone and its derivatives are synthetic glucocorticoids that are used for their antiinflammatory or immunosuppressive properties.
Mechanism of action The antiinflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition of arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Firstly, however, these glucocorticoids bind to the glucocorticoid receptors which translocate into the nucleus and bind DNA (GRE) and change genetic expression both positively and negatively. The immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.
Absorption Rapid absorption following oral administration
Volume of distribution Not Available
Protein binding 68%
Metabolism
Hepatic.
Route of elimination Not Available
Half life 88 minutes
Clearance Not Available
Toxicity LD50=>500mg/kg (in rats)
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 270 °C PhysProp
water solubility 80 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP 1.16 HANSCH,C ET AL. (1995)
logS -3.69 ADME Research, USCD
Predicted Properties
Property Value Source
water solubility 8.47e-01 g/l ALOGPS
logP 0.84 ALOGPS
logP 0.24 ChemAxon
logS -2.7 ALOGPS
pKa (strongest acidic) 11.75 ChemAxon
pKa (strongest basic) -3.3 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 6 ChemAxon
hydrogen donor count 4 ChemAxon
polar surface area 115.06 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 99.38 ChemAxon
polarizability 39.79 ChemAxon
药物相互作用
Drug Interaction
Acenocoumarol The corticosteroid, triamcinolone, alters the anticoagulant effect, acenocoumarol.
Acetylsalicylic acid The corticosteroid, triamcinolone, may decrease the effect of the salicylate, acetylsalicylic acid.
Ambenonium The corticosteroid, triamcinolone, may decrease the effect of the anticholinesterase, ambenonium.
Amobarbital The barbiturate, amobarbital, may decrease the effect of the corticosteroid, triamcinolone.
Anisindione The corticosteroid, triamcinolone, alters the anticoagulant effect of anisindione.
Aprobarbital The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, triamcinolone.
Bismuth Subsalicylate The corticosteroid, triamcinolone, may decrease the effect of the salicylate, bismuth subsalicylate.
Butabarbital The barbiturate, butabarbital, may decrease the effect of the corticosteroid, triamcinolone.
Butalbital The barbiturate, butalbital, may decrease the effect of the corticosteroid, triamcinolone.
Butethal The barbiturate, butethal, may decrease the effect of the corticosteroid, triamcinolone.
Dicumarol The corticosteroid, triamcinolone, alters the anticoagulant effect of dicumarol.
Dihydroquinidine barbiturate The barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, triamcinolone.
Edrophonium The corticosteroid, triamcinolone, may decrease the effect of the anticholinesterase, edrophonium.
Ethotoin The enzyme inducer, ethotoin, may decrease the effect of the corticosteroid, triamcinolone.
Fosphenytoin The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, triamcinolone.
Heptabarbital The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, triamcinolone.
Hexobarbital The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, triamcinolone.
Magnesium salicylate The corticosteroid, triamcinolone, may decrease the effect of magnesium salicylate.
Mephenytoin The enzyme inducer, mephenytoin, may decrease the effect of the corticosteroid, triamcinolone.
Methohexital The barbiturate, methohexital, may decrease the effect of the corticosteroid, triamcinolone.
Methylphenobarbital The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, triamcinolone.
Midodrine Increased arterial pressure
Neostigmine The corticosteroid, triamcinolone, may decrease the effect of the anticholinesterase, neostigmine.
Pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, triamcinolone.
Phenobarbital The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, triamcinolone.
Phenytoin The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, triamcinolone.
Primidone The barbiturate, primidone, may decrease the effect of the corticosteroid, triamcinolone.
Pyridostigmine The corticosteroid, triamcinolone, may decrease the effect of the anticholinesterase, pyridostigmine.
Quinidine barbiturate The barbiturate, quinidine barbiturate, may decrease the effect of the corticosteroid, triamcinolone.
Rifampin The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, triamcinolone.
Salicylate-sodium The corticosteroid, triamcinolone, may decrease the effect of the salicylate, salicylate-sodium.
Salsalate The corticosteroid, triamcinolone, may decrease the effect of the salicylate, salsalate.
Secobarbital The barbiturate, secobarbital, may decrease the effect of the corticosteroid, triamcinolone.
Tacrine Tacrine and Triamcinolone may independently exacerbate muscle weakness in myasthenia gravis patients. Monitor for additive muscle weakness effects.
Talbutal The barbiturate, talbutal, may decrease the effect of the corticosteroid, triamcinolone.
Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Trisalicylate-choline The corticosteroid, triamcinolone, may decrease the effect of the salicylate, trisalicylate-choline.
Vecuronium Vecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Triamcinolone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.
Warfarin The corticosteroid, triamcinolone, alters the anticoagulant effect of warfarin.
食物相互作用
Not Available

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