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药品详细

Tirofiban(替罗非班)

化学结构式图
中文名
替罗非班
英文名
Tirofiban
分子式
C22H36N2O5S
化学名
(2S)-2-(butane-1-sulfonamido)-3-{4-[4-(piperidin-4-yl)butoxy]phenyl}propanoic acid
分子量
Average: 440.597
Monoisotopic: 440.234492962
CAS号
144494-65-5
ATC分类
B01A 抗血栓药
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Tirofiban prevents the blood from clotting during episodes of chest pain or a heart attack, or while the patient is undergoing a procedure to treat a blocked coronary artery. It is a non-peptide reversible antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor, and inhibits platelet aggregation.

生产厂家
  • Medicure international inc
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
  • Phenethylamines
  • Amino Acids
  • Amphetamines
Substructures
  • Hydroxy Compounds
  • Acetates
  • Aliphatic and Aryl Amines
  • Phenols and Derivatives
  • Sulfonyls
  • Ethers
  • Benzene and Derivatives
  • Carboxylic Acids and Derivatives
  • Phenethylamines
  • Heterocyclic compounds
  • Aromatic compounds
  • Anisoles
  • Sulfonamides
  • Amino Acids
  • Phenyl Esters
  • Amphetamines
  • Piperidines
适应症
药理
Indication For treatment, in combination with heparin, of acute coronary syndrome, including patients who are to be managed medically and those undergoing PTCA or atherectomy.
Pharmacodynamics Tirofiban prevents the blood from clotting during episodes of chest pain or a heart attack, or while the patient is undergoing a procedure to treat a blocked coronary artery. It is a non-peptide antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor, and inhibits platelet aggregation. When administered intravenously, tirofiban inhibits ex vivo platelet aggregation in a dose- and concentration-dependent manner. When given according to the recommended regimen, >90% inhibition is attained by the end of the 30-minute infusion. Tirofiban has been recently shown in patients with unstable angina to reduce ischemic events at 48 hours following infusion when compared to standard heparin therapy.
Mechanism of action Tirofiban is a reversible antagonist of fibrinogen binding to the GP IIb/IIIa receptor, the major platelet surface receptor involved in platelet aggregation. Platelet aggregation inhibition is reversible following cessation of the infusion of tirofiban.
Absorption Not Available
Volume of distribution
  • 22 to 42 L
Protein binding 65%
Metabolism
Metabolism appears to be limited.
Route of elimination It is cleared from the plasma largely by renal excretion, with about 65% of an administered dose appearing in urine and about 25% in feces, both largely as unchanged tirofiban.
Half life 2 hours
Clearance
  • 213 – 314 mL/min [Healthy subjects]
  • 152 – 267 mL/min [patients with coronary artery disease]
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00267 Tirofiban Pathway SMP00267
理化性质
Properties
State solid
Experimental Properties
Property Value Source
water solubility Very slightly soluble Not Available
logP 1.4 Not Available
Predicted Properties
Property Value Source
water solubility 3.17e-03 g/l ALOGPS
logP 1.78 ALOGPS
logP 0.6 ChemAxon
logS -5.1 ALOGPS
pKa (strongest acidic) 3.17 ChemAxon
pKa (strongest basic) 10.21 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 6 ChemAxon
hydrogen donor count 3 ChemAxon
polar surface area 104.73 ChemAxon
rotatable bond count 13 ChemAxon
refractivity 117.48 ChemAxon
polarizability 49.27 ChemAxon
药物相互作用
Drug Interaction
Abciximab Additive effects. Concomitant use is contraindicated.
Eptifibatide Additive effects. Concomitant use is contraindicated.
Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
Treprostinil The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Tirofiban. Monitor for increased bleeding during concomitant thearpy.
食物相互作用
Not Available

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