Mupirocin (calcium)

Mupirocin (BRL-4910A, Pseudomonic acid) calcium is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin calcium apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis^[1][2]. In Vitro: Mupirocin (BRL-4910A, Pseudomonic acid) calcium (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)^[1].
Mupirocin calcium is highly bound (95% bound) to human serum protein, thus results in activity inhibition in the presence of human serum^[1].
Mupirocin calcium apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis^[2].
Mupirocin calcium (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)^[4].
Mupirocin calcium 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^[5].
Note: MIC, the minimum inhibition concentration. In Vivo: MRSA: Meticillin-resistant Staphylococcus aureus
Mupirocin (BRL-4910A, Pseudomonic acid) calcium 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^[1].
Mupirocin calcium (2% ointment; external administration; twice daily; 3-6 d) decreases the total bacterial loads in the skin lesions with either topical treatment^[3].
Mupirocin calcium (2% ointment; external administration; 4 d) alleviates MRSA-infected pressure ulcers in mice^[4].
Mupirocin calcium (100 mg/mL; s.c.; 7 d) exerts prevention efficacy against vascular prosthetic graft infection due to Staphylococcus epidermidis^[5].