Mupirocin

Mupirocin(BRL-4910A) is an antibiotic of the monoxycarbolic acid class; effective against Gram-positive bacteria, including MRSA.(In Vitro):Mupirocin (BRL-4910A, Pseudomonic acid) (0-100 μM; 48 h) shows antibacterial effect against staphylococci, streptococci and certain gram-negative bacteria, with MIC values range from 0.06-0.25 μg/mL (MIC50 =0.12 μg/mL, MIC90 =0.25 μg/mL).Mupirocin is highly bound (95% bound) to human serum protein, thus results in activity inhibition in the presence of human serum.Mupirocin apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis.Mupirocin (2% ointment) reduces pro-inflammatory cytokines IL-1β and IL-17 level, decreases tumor necrosis factor-alpha (TNF-α) expression, and increases the leavel of vascular endothelial growth factor (VEGF).Mupirocin inhibits MS (S. epidermidis ATCC 12228), MR (S. epidermidis (Se56-99)), and VIR (S. epidermidis (Se43-98)) with MICs of 0.25, 1.26, 1.59 mg/L.(In Vivo):MRSA: Meticillin-resistant Staphylococcus aureusMupirocin (BRL-4910A, Pseudomonic acid) is well absorbed after oral and parenteral administration but serum antibiotic concentrations were short-lived as a result of extensive degradation to the antibacterially inactive metabolite, monic acid A.Mupirocin (2% ointment; external administration; twice daily; 3-6 d) decreases the total bacterial loads in the skin lesions with either topical treatment.Mupirocin (2% ointment; external administration; 4 d) alleviates MRSA-infected pressure ulcers in mice.Mupirocin (100 mg/mL; s.c.; 7 d) exerts prevention efficacy against vascular prosthetic graft infection due to Staphylococcus epidermidis.