Flumethasone (CAS 2135-17-3)

Flumethasone (Flumethasone) Comprehensive Information

​Chemical Properties

1. ​Basic Parameters
   • ​Chemical Formula: C₂₂H₂₈F₂O₅
   • ​Molecular Weight: 410.45
   • ​CAS Number: 2135-17-3
   • ​EINECS Number: 218-370-9
   • ​Melting Point: 237–240°C
   • ​Boiling Point: 569.8 ± 50.0°C (Predicted)
   • ​Density: 1.1621 (estimated)
   • ​Solubility: Soluble in acetic acid (10 mg/mL); practically insoluble in water (1 mg/L at 20°C)
   • ​Appearance: White solid
   • ​Optical Activity: [α]²⁵/D 67.0–71.0°, c = 1 in dioxane
   • ​Storage Temperature: 2–8°C
2. ​Structural Features
   A synthetic difluorinated corticosteroid derivative of prednisolone, featuring 6α,9α-difluoro and 16α-methyl substitutions. These modifications enhance anti-inflammatory activity while reducing mineralocorticoid effects.

​Pharmacological Actions and Clinical Applications

1. ​Mechanism of Action
   • ​Glucocorticoid Receptor Agonist: Binds to glucocorticoid receptors, inhibiting phospholipase A₂ activity and reducing prostaglandin/leukotriene synthesis.
   • ​Anti-inflammatory: Suppresses immune cell activity and cytokine production (e.g., IL-1, TNF-α).
2. ​Indications
   • ​Veterinary Use: Treats inflammatory skin conditions (dermatitis, eczema) and respiratory infections in cattle.
   • ​Human Use: Topical application for psoriasis, allergic dermatitis, and insect bites.
   • ​Combination Therapy: Used with antibiotics (e.g., ceftiofur) for bacterial pneumonia in livestock.
3. ​Dosage Forms
   • ​Topical: Creams, ointments (1–2% concentrations).
   • ​Injectable: Solutions for systemic anti-inflammatory effects.

​Safety and Precautions

1. ​Adverse Effects
   • ​Local: Skin atrophy, telangiectasia with prolonged use.
   • ​Systemic: Cushing’s syndrome, HPA axis suppression.
2. ​Contraindications
   • Fungal/bacterial infections at application sites.
   • Pregnancy (risk-benefit assessment required).
3. ​Regulatory Status
   • Approved for veterinary and human use globally; classified as a prescription drug.

​Manufacturing and Quality Control

1. ​Synthesis
   Derived via fluorination and methylation of prednisolone derivatives.
2. ​Analytical Standards
   • ​HPLC: C18 column with methanol-water (60:40) mobile phase; UV detection at 240 nm.
   • ​Impurity Limits: Total impurities ≤1.0% of main peak area.

​Research and Market

1. ​Scientific Use
   • Models for studying glucocorticoid receptor signaling and anti-inflammatory pathways.
   • Investigated for enhancing chemotherapy efficacy in lung cancer 6.
2. ​Market Overview
   • ​Suppliers: Major manufacturers include Shanghai Synchem Pharma, Wuhan Dongkangyuan Biotech.
   • ​Price: ~50–100 per gram (research-grade).

For detailed toxicological data or formulation protocols, consult specialized pharmacological references.