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- Approved, Withdrawn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
Structure for Floctafenine (DB08976)
- 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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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Mild acute pain •••••••••••• Management of Moderate acute pain •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Floctafenine may decrease the excretion rate of Abacavir which could result in a higher serum level. Abciximab The risk or severity of bleeding and hemorrhage can be increased when Floctafenine is combined with Abciximab. Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with Floctafenine. Aceclofenac The risk or severity of adverse effects can be increased when Aceclofenac is combined with Floctafenine. Acemetacin The risk or severity of adverse effects can be increased when Floctafenine is combined with Acemetacin. - 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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- Diralgan / Idalon / Novodolan
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Floctafenine Tablet 400 mg Oral Aa Pharma Inc 2001-11-14 Not applicable Canada 
Floctafenine Tablet 200 mg Oral Aa Pharma Inc 2001-11-14 Not applicable Canada Idarac Tablet 200 mg Oral Sanofi Synthelabo 1985-12-31 2004-08-05 Canada Idarac Tablet 400 mg Oral Sanofi Synthelabo 1988-12-31 2004-08-05 Canada
Categories
- ATC Codes
- N02BG04 — Floctafenine
- Drug Categories
- Acids, Carbocyclic
- Agents causing hyperkalemia
- Agents that produce hypertension
- Aminobenzoates
- Analgesics
- Analgesics, Non-Narcotic
- Anti-Inflammatory Agents
- Anti-Inflammatory Agents, Non-Steroidal
- Antirheumatic Agents
- Benzene Derivatives
- Benzoates
- Miscellaneous Analgesics and Antipyretics
- Nephrotoxic agents
- Nervous System
- Non COX-2 selective NSAIDS
- Peripheral Nervous System Agents
- Sensory System Agents
- 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
- External Links
- PubChem Compound
- 76958517
- PubChem Substance
- 310264938
- ChemSpider
- 3243
- 4444
- ChEBI
- 31612
- ChEMBL
- CHEMBL2105075
- Wikipedia
- Floctafenine
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet Oral 200 mg Tablet Oral 400 mg Tablet Oral - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 179-180 U.S. Patent 3,644,368. - Predicted Properties
Property Value Source Water Solubility 0.0346 mg/mL ALOGPS logP 3.05 ALOGPS logP 4.43 Chemaxon logS -4.1 ALOGPS pKa (Strongest Acidic) 13.62 Chemaxon pKa (Strongest Basic) 5.84 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 91.68 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 98.72 m3·mol-1 Chemaxon Polarizability 37.76 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0009000000-16ea1f7ceba4e5de6a79 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-001u-7059000000-50e219356b6b8157ee4e Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0009000000-c04328bf9f15c7a71717 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-03ei-1059000000-d5819f127dfb2ec055fb Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-0091000000-02c083b25c65d5fa8022 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-014j-0089000000-fd1b7c0631c2988a8339 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 186.40678 predictedDeepCCS 1.0 (2019) [M+H]+ 188.76479 predictedDeepCCS 1.0 (2019) [M+Na]+ 195.80959 predictedDeepCCS 1.0 (2019)
Drug created at June 09, 2014 20:37 / Updated at April 24, 2024 14:30