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药品详细

Suprofen(舒洛芬)

化学结构式图
中文名
舒洛芬
英文名
Suprofen
分子式
C14H12O3S
化学名
2-{4-[(thiophen-2-yl)carbonyl]phenyl}propanoic acid
分子量
Average: 260.308
Monoisotopic: 260.05071494
CAS号
40828-46-4
ATC分类
M01A 未知
药物类型
small molecule
阶段
approved
商品名
Maldocil;Masterfen;Profenal;Srendam;Sulproltin;Suprocil;Suprol;Sutoprofen;Topalgic;
同义名
Suprofene [INN-French];Suprofenum [INN-Latin];
基本介绍

An ibuprofen-type anti-inflammatory analgesic and antipyretic. It inhibits prostaglandin synthesis and has been proposed as an anti-arthritic. [PubChem]

生产厂家
  • Alcon laboratories 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
  • Phenylacetates
Substructures
  • Hydroxy Compounds
  • Acetates
  • Carboxylic Acids and Derivatives
  • Phenylacetates
  • Benzene and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • Benzoyl Derivatives
  • Thiophenes
  • Ketones
适应症
ANTIINFLAMMATORY AND ANTIRHEUMATIC 消炎抗风湿;
药理
Indication Used as eye drops to inhibit the miosis (pupil constriction) that may occur during ocular surgery.
Pharmacodynamics Suprofen is a non-steroidal anti-inflammatory analgesic and antipyretic. Ophthalmic anti-inflammatory medicines are used in the eye to lessen problems that can occur during or after some kinds of eye surgery. Sometimes, the pupil of the eye gets smaller during an operation (pupil constriction), making it more difficult for the surgeon to reach some areas of the eye. Suprofen is used to help prevent this.
Mechanism of action Suprofen binds to the cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) isoenzymes, preventing the synthesis of prostaglandins and reducing the inflammatory response. Cyclooxygenase catalyses the formation of prostaglandins and thromboxane from arachidonic acid (itself derived from the cellular phospholipid bilayer by phospholipase A2). Prostaglandins act (among other things) as messenger molecules in the process of inflammation. The overall result is a reduction in pain and inflammation in the eyes and the prevention of pupil constriction during surgery. Normally trauma to the anterior segment of the eye (especially the iris) increases endogenous prostaglandin synthesis which leads to constriction of the iris sphincter.
Absorption Not Available
Volume of distribution Not Available
Protein binding 20%
Metabolism
Primarily hepatic (mainly via cytochrome P450 isozyme 2C9).

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Suprofen
Suprofen S-oxide Details
Suprofen
Thiophene-4,5-epoxide Details
Suprofen
Suprofen glucuronide Details
Route of elimination Not Available
Half life Not Available
Clearance Not Available
Toxicity Symptoms of overdose include bleeding in the eye or redness or swelling of the eye or the eyelid, blurred vision or other change in vision, fever or chills, itching or tearing, nausea or vomiting, pain, sensitivity to light, shortness of breath, sticky or matted eyelashes, swelling of face, throbbing pain, tightness in chest, troubled breathing, and wheezing.
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00101 Suprofen Pathway SMP00101
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 124.3 °C PhysProp
water solubility limited solubility Not Available
logP 2.2 Not Available
pKa 3.91 MERCK INDEX (1996)
Predicted Properties
Property Value Source
water solubility 4.22e-02 g/l ALOGPS
logP 3.16 ALOGPS
logP 3.53 ChemAxon
logS -3.8 ALOGPS
pKa (strongest acidic) 4.01 ChemAxon
pKa (strongest basic) -7.8 ChemAxon
physiological charge -1 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 54.37 ChemAxon
rotatable bond count 4 ChemAxon
refractivity 69.41 ChemAxon
polarizability 26.84 ChemAxon
药物相互作用
食物相互作用
Not Available

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