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药品详细

Fenoprofen (非诺洛芬 )

化学结构式图
中文名
非诺洛芬
英文名
Fenoprofen
分子式
Not Available
化学名
2-(3-phenoxyphenyl)propanoic acid
分子量
Average: 242.2699
Monoisotopic: 242.094294314
CAS号
34597-40-5
ATC分类
M01A 未知
药物类型
small molecule
阶段
商品名
Nalfon;
同义名
Feneprofen calcium salt dihydrate;Fenoprofen calcium;Fenoprofen calcium hydrate;
基本介绍

An anti-inflammatory analgesic and antipyretic highly bound to plasma proteins. It is pharmacologically similar to aspirin, but causes less gastrointestinal bleeding. [PubChem]

生产厂家
  • Actavis elizabeth llc
  • American therapeutics inc
  • Clonmel healthcare ltd
  • Dista products co div eli lilly and co
  • Halsey drug co inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • Pedinol pharmacal inc
  • Quantum pharmics ltd
  • Sandoz inc
  • Usl pharma inc
  • Warner chilcott div warner lambert co
  • Watson laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
Form Route Strength
Capsule Oral
规格
Unit description Cost Unit
Fenoprofen calcium powder 1.59 USD g
Fenoprofen Calcium 600 mg tablet 1.01 USD tablet
Nalfon 200 mg capsule 0.91 USD capsule
Fenoprofen 600 mg tablet 0.88 USD tablet
化合物类型
Type small molecule
Classes
  • Phenylacetates
Substructures
  • Hydroxy Compounds
  • Acetates
  • Phenols and Derivatives
  • Carboxylic Acids and Derivatives
  • Phenylacetates
  • Ethers
  • Benzene and Derivatives
  • Aromatic compounds
  • Anisoles
  • Phenyl Esters
适应症
ANTIINFLAMMATORY AND ANTIRHEUMATIC 消炎抗风湿;
药理
Indication For relief of the signs and symptoms of rheumatoid arthritis and osteoarthritis. Also for the relief of mild to moderate pain.
Pharmacodynamics Fenoprofen is a propionic acid derivative with analgesic, antiinflammatory and antipyretic properties. Fenoprofen inhibits prostaglandin synthesis by decreasing the enzyme needed for biosynthesis. In patients with rheumatoid arthritis, the anti-inflammatory action of fenoprofen has been evidenced by relief of pain, increase in grip strength, and reductions in joint swelling, duration of morning stiffness, and disease activity (as assessed by both the investigator and the patient). In patients with osteoarthritis, the anti-inflammatory and analgesic effects of fenoprofen have been demonstrated by reduction in tenderness as a response to pressure and reductions in night pain, stiffness, swelling, and overall disease activity (as assessed by both the patient and the investigator). These effects have also been demonstrated by relief of pain with motion and at rest and increased range of motion in involved joints. In patients with rheumatoid arthritis and osteoarthritis, clinical studies have shown fenoprofen to be comparable to aspirin in controlling the aforementioned measures of disease activity, but mild gastrointestinal reactions (nausea, dyspepsia) and tinnitus occurred less frequently in patients treated with fenoprofen than in aspirin-treated patients. It is not known whether fenoprofen causes less peptic ulceration than does aspirin. In patients with pain, the analgesic action of fenoprofen has produced a reduction in pain intensity, an increase in pain relief, improvement in total analgesia scores, and a sustained analgesic effect.
Mechanism of action Fenoprofen's exact mode of action is unknown, but it is thought that prostaglandin synthetase inhibition is involved. Fenoprofen has been shown to inhibit prostaglandin synthetase isolated from bovine seminal vesicles.
Absorption Rapidly absorbed under fasting conditions, and peak plasma levels of 50 µg/mL are achieved within 2 hours after oral administration of 600 mg doses.
Volume of distribution Not Available
Protein binding 99% to albumin.
Metabolism

About 90% of a single oral dose is eliminated within 24 hours as fenoprofen glucuronide and 4'-hydroxyfenoprofen glucuronide, the major urinary metabolites of fenoprofen.

Route of elimination Not Available
Half life Plasma half-life is approximately 3 hours.
Clearance Not Available
Toxicity Symptoms of overdose appear within several hours and generally involve the gastrointestinal and central nervous systems. They include dyspepsia, nausea, vomiting, abdominal pain, dizziness, headache, ataxia, tinnitus, tremor, drowsiness, and confusion. Hyperpyrexia, tachycardia, hypotension, and acute renal failure may occur rarely following overdose. Respiratory depression and metabolic acidosis have also been reported following overdose with certain NSAIDs.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Melting point Not Available
Experimental Properties
Property Value Source
water solubility Slight (calcium salt) PhysProp
logP 3.1 PhysProp
pKa 4.5 Various sources
Predicted Properties
Property Value Source
water solubility 8.11e-02 g/l ALOGPS
logP 3.87 ALOGPS
logP 3.65 ChemAxon Molconvert
logS -3.48 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 2 ChemAxon Molconvert
hydrogen donor count 1 ChemAxon Molconvert
polar surface area 46.53 ChemAxon Molconvert
rotatable bond count 4 ChemAxon Molconvert
refractivity 68.18 ChemAxon Molconvert
polarizability 25.30 ChemAxon Molconvert
药物相互作用
Drug Interaction
Acenocoumarol The NSAID, fenoprofen, may increase the anticoagulant effect of acenocoumarol.
Alendronate Increased risk of gastric toxicity
Anisindione The NSAID, fenoprofen, may increase the anticoagulant effect of anisindione.
Cyclosporine Monitor for nephrotoxicity
Dicumarol The NSAID, fenoprofen, may increase the anticoagulant effect of dicumarol.
Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
Methotrexate The NSAID, fenoprofen, may decrease the renal excretion of methotrexate. Increased risk of methotrexate toxicity.
Telmisartan Concomitant use of Telmisartan and Fenoprofen may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment.
Timolol The NSAID, Fenoprofen, may antagonize the antihypertensive effect of Timolol.
Trandolapril The NSAID, Fenoprofen, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Fenoprofen is initiated, discontinued or dose changed.
Treprostinil The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Fenoprofen. Monitor for increased bleeding during concomitant thearpy.
Warfarin The antiplatelet effects of fenoprofen may increase the bleed risk associated with warfarin. Consider alternate therapy or monitor for signs and symptoms of bleeding during concomitant therapy.
食物相互作用
  • Avoid alcohol.
  • Take with food to reduce irritation.

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