Identification

Summary

Floctafenine is an anti-inflammatory analgesic used to manage mild to moderate acute pain.

Generic Name
Floctafenine
DrugBank Accession Number
DB08976
Background

Floctafenine is an anti-inflammatory analgesic similar in action to aspirin. Floctafenine inhibits prostaglandin synthesis.

Type
Small Molecule
Groups
Approved, Withdrawn
Structure
Weight
Average: 406.3552
Monoisotopic: 406.114041657
Chemical Formula
C20H17F3N2O4
Synonyms
  • Floctafenina
  • Floctafenine
  • Floctafeninum
External IDs
  • R 4318
  • R-4138
  • R-4318
  • RU 15750

Pharmacology

Indication

Not Available

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Not Available

Mechanism of action
Not Available
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbacavirFloctafenine may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbciximabThe risk or severity of bleeding and hemorrhage can be increased when Floctafenine is combined with Abciximab.
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol is combined with Floctafenine.
AceclofenacThe risk or severity of adverse effects can be increased when Aceclofenac is combined with Floctafenine.
AcemetacinThe risk or severity of adverse effects can be increased when Floctafenine is combined with Acemetacin.
AcenocoumarolThe risk or severity of bleeding and hemorrhage can be increased when Floctafenine is combined with Acenocoumarol.
AcetaminophenThe risk or severity of adverse effects can be increased when Acetaminophen is combined with Floctafenine.
AcetohexamideThe protein binding of Acetohexamide can be decreased when combined with Floctafenine.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Floctafenine.
AclidiniumFloctafenine may decrease the excretion rate of Aclidinium which could result in a higher serum level.
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Food Interactions
  • Avoid alcohol. Consuming alcohol increases the risk of gastrointestinal irritation.
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Herbs with anticoagulant effects may increase the risk of gastrointestinal bleeding. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • Take after a meal. Food reduces gastric irritation.
  • Take with a full glass of water.

Products

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International/Other Brands
Diralgan / Idalon / Novodolan
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
FloctafenineTablet400 mgOralAa Pharma Inc2001-11-14Not applicableCanada flag
FloctafenineTablet200 mgOralAa Pharma Inc2001-11-14Not applicableCanada flag
IdaracTablet400 mgOralSanofi Synthelabo1988-12-312004-08-05Canada flag
IdaracTablet200 mgOralSanofi Synthelabo1985-12-312004-08-05Canada flag

Categories

ATC Codes
N02BG04 — Floctafenine
Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
O04HVX6A9Q
CAS number
23779-99-9
InChI Key
APQPGQGAWABJLN-UHFFFAOYSA-N
InChI
InChI=1S/C20H17F3N2O4/c21-20(22,23)15-6-3-5-13-17(8-9-24-18(13)15)25-16-7-2-1-4-14(16)19(28)29-11-12(27)10-26/h1-9,12,26-27H,10-11H2,(H,24,25)
IUPAC Name
2,3-dihydroxypropyl 2-{[8-(trifluoromethyl)quinolin-4-yl]amino}benzoate
SMILES
OCC(O)COC(=O)C1=CC=CC=C1NC1=CC=NC2=C(C=CC=C12)C(F)(F)F

References

Synthesis Reference

U.S. Patent 3,644,368.

General References
Not Available
PubChem Compound
76958517
PubChem Substance
310264938
ChemSpider
3243
RxNav
4444
ChEBI
31612
ChEMBL
CHEMBL2105075
Wikipedia
Floctafenine

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral200 mg
TabletOral400 mg
TabletOral
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)179-180U.S. Patent 3,644,368.
Predicted Properties
PropertyValueSource
Water Solubility0.0346 mg/mLALOGPS
logP3.05ALOGPS
logP4.43ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)13.62ChemAxon
pKa (Strongest Basic)5.84ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area91.68 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity98.72 m3·mol-1ChemAxon
Polarizability37.76 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Drug created at June 09, 2014 20:37 / Updated at August 07, 2022 05:31