Antibiotics mupirocin

Mupirocin calcium cream 2% contains the dihydrate crystalline calcium hemisalt of the antibiotic mupirocin. Chemically, it is ((alpha) E,2 5,3 R,4 R,5 5)-5-[(2 5,3 5,4 5,5 5) -2,3 -epoxy-5-hydroxy-4-methylhexyl]tetra-hydro-3, 4-dihydroxy-(beta)-methyl-2//-pyran-2-crotonic acid, ester with 9-hydroxynonanoic acid, calcium salt (2 1),... 

El-Sayed, A.K., Hothersall, J., and Thomas, C.M. Quorum sensing-dependent regnlation of the biosynthesis of the polyketide antibiotic mupirocin in Pseudomonas fluorescens. Microbiology, 147, 2127-2139, 2001. 

Nakama T, Nureki O, Yokoyama S Structural basis for the recognition of iso-leucyl-adenylate and an antibiotic, mupirocin, by isoleucyl-tRNA synthetase. J Biol Chem 2001, 276(50) 47387-47393. 

Fig. 5.14 Miscellaneous antibiotics A, chloramphenicol B, fusidic acid C, lincomycin D, clindamycin E, mupirocin (pseudomonic acid A).

Mupirocin is a topical antibiotic that inhibits isoleucyl tRNA synthetase with the subsequent inhibition of protein synthesis. Mupirocin has become a mainstay in the treatment of Staph, aureus infection and colonization during hospital outbreaks, and it is in this organism that acquired resistance has arisen (Gilbart etal. 1993). 

Gilbart J., Perry CR. Slocombe B. (1993) High-level mupirocin resistance in Staphylococcus aureus evidence for two distinct isoleucyl-tRNA synthetases. Antimicrob Agents Chemother, 31, 32-38. Godfrey A.J. Bryan L.E. (1984) Intrinsic resistance and whole cell factors contributing to antibiotic resistance, hv. Antimicrobial Drug Resistance (ed. L.E. Bryan), pp. 113-145. New York Academic Press. 

O Impetigo is a skin infection that most commonly afflicts young children. It is caused by group A streptococci or Staphylococcus aureus and is characterized by the development of numerous blisters that rupture and form crusts. Dicloxacillin, cephalexin, and topical mupirocin are considered the antibiotics of choice for treatment of impetigo. 

A topical antibiotic or antifungal may be used to control the spread of infection but generally is unnecessary. For staphylococcal or streptococcal folliculitis, antibiotic ointments such as mupirocin might be administered three times daily. Antifungal shampoo can be used for dermatophytes. 

Systemic therapy with a variety of (3-lactams, macro-lides and lincosamides (clindamycin) has been the cornerstone of skin infection therapy for many years [17]. However, topical antibiotics can play an important role in both treatment and prevention of many primary cutaneous bacterial infections commonly seen in the dermatological practice [18], Indeed, while systemic antimicrobials are needed in the complicated infections of skin and skin structure, the milder forms can be successfully treated with topical therapy alone [18], The topical agents used most often in the treatment of superficial cutaneous bacterial infections are tetracyclines, mupirocin, bacitracin, polymyxin B, and neomycin. 

Mupirocin (Bactroban) Topical antibiotic Oint 2% [15,30gm] Nasal oint 2% [1 gm] Apply to affected areas tid. Active against gram positive cocci 0.5 gm ( 4 tube) in each nostril bid x 5daysfor MRSA nasal carriers... 

Mupirocin is a broad spectrum antibiotic available as a 2% ointment. 

Mupirocin is an antibiotic agent available only for topical use. It is indicated for use in Gram-positive skin infections. Mupirocin should not be used for more than 10 days, to prevent the emergence of resistance. 

As a group, the protein biosynthesis inhibitors comprise the second largest class of antibiotics available for clinical use. Natural product classes of antibiotics that inhibit the protein biosynthesis are aminoglycosides, tetracyclines, chloramphenicol, macrolides, lincosamides, fusidic acid, streptogramins and mupirocin (Fig. 7). 

Mupirocin is not related to any of the sys-temically used antibiotics. It is an inhibitor of bacterial protein synthesis and is especially active against gram-positive aerobic bacteria, e.g. methicillin-resistant S. aureus and group A beta-hemolytic streptococci. Absorption through the skin is minimal. Intranasal application may be associated with irritation of mucous membranes. 

Topical antibiotics with a narrow spectrum of action and low toxicity (eg, bacitracin and mupirocin) can be used for temporary control of bacterial growth and are generally preferred to antiseptics. Methenamine mandelate releases formaldehyde in a low antibacterial concentration at acid pH and can be an effective urinary antiseptic for long-term control of urinary tract infections. 

Mupirocin is a naturally occurring antibiotic available as a cream or ointment, and is unusual in its origin and mechanism of action. It inhibits protein synthesis, actively preventing the incorporation... 

Recurrent impetigo, furunculosis, or other staphylococcal infections may be a result of pathogenic nasal carriage of S. aureus. To reduce postoperative complications, eradication of nasal colonization of S. aureus has been extended to colonized health care workers and other susceptible patients.14 Mupirocin has been found to be the most effective topical antibiotic for the elimination and is effective in reducing subsequent infections. When applied intranasally four times daily for five days, it has been shown to reduce nasal carriage for up to 1 year.77... 

Topical Antibiotic Monotherapy Localized impetiginized eczema lesions can be treated successfully with topical fusidic acid or mupirocin, whereas topical application of other antibiotics (neomycin as obsolete aminoglycosid, tetracyclines, or polymyxines) should be avoided.84 Especially in children with AD, fusidic acid resistance seems to be a particular problem reflecting the chronicity and the extent of the disease (see Section 30.2.2). 

White, D.G., Collins, P.O., and Rowsell, R.B., Topical antibiotics in the treatment of superficial skin infections in general practice — a comparison of mupirocin with sodium fusidate. J. Infect. 18, 221-229, 1989. 

The lincosamides, lincomycin and clindamycin are active against Grampositive bacteria. Plasmid-mediated inactivation from enzymatic nucleo-tidylation occurs in some staphylococci. Plasmid-encoded enzymes can modify streptogramin A (O-acetyltransferase enzyme) and streptogramin B (hydrolase enzyme involved) in S. aureus [198, 199], There is no evidence that bacteria can circumvent the action of other antibiotics for example, mupirocin is not degraded [200]. 

Mupirocin Antibiotic Treat certain skin infections (e.g., impetigo) Bactroban 2.0... 

Enzymes in the aaRS family are a promising target for the development of novel antibiotics (17). Selective inhibition of just one essential aaRS would be lethal to the pathogen. The best example is mupirocin, a commercially marketed IleRS inhibitor. Mupirocin, also known as pseudomonic acid, originally was isolated from Pseudomonas fluorescens and is used as a topical antibiotic against gram-positive bacteria, particularly Staphylococcus aureus. It binds directly to the first lysine of the conserved KMSKS sequence in the amino acylation active site (18). 

Mupirocin is an antibiotic that inhibits bacterial protein synthesis by binding to isoleucyl transfer RNA synthetase. It is primarily bacteriostatic at low concentrations, but is bactericidal in the high concentrations and can have activity against organisms reported to be relatively resistant in vitro. 

Mupirodn, USP, Mupirocin (pseudomonic acid A.Bac-troban) is the major component of a family of. stnictuiullv related antibiotics, pseudomonic acids A to D, produced In the submerged fermentation of Pseudomonas fluoresceia. Although the antimicrobial properties of P.fUiorescemvttK recorded as early as 1887, it was not until 1971 that Fuller et al. identified the metabolites responsible for this activity. The. structure of the major and most potent metaboliK. pseudomonic acid A (which represents 90 to 95% of the active fraction from P. fhtore. cem). was later confirmed b) chemical sy nthesis to be the 9-hydroxynonanoic acid ester of monic acid. 

Mupirocin interferes with RNA synthesis and protein svit-thesis in susceptible bacteria. " It specifically and reversibly binds with bacterial isolcucyl transfer-RNA svrr thase to prevent the incorporation of isoleucine into bacletui proteins. High-level, pla-smid-mediated mupirocin nsLv tance in S. aureus has been attributed to the elaboration d a modified isoleucyl tRNA that does not bind mupirocin. Inherent re.sistance in bacilli is likely due to poor cellubi penetration of the antibiotic. " ... 

Mupirocin is supplied in u wulcr-miscible ointment con-uming 2Vo of the antibiotic in polyethylene glycols 400 and 350. 

Parent , M. A., Hatfield, S. M., Leyden, J. J. Mupirocin a topical antibiotic with a unique structure and mechanism of action. Clin. Pharm. 1987, 6, 761-770. 

Impetigo, a superficial skin infection characterized by fluid-filled vesicles that develop rapidly into pus-filled blisters that rupture to form golden-yellow crusts, is caused by S. aureus and/or S. pyogenes and occurs most commonly in children. Dicloxacillin is used commonly for treatment, although topical antibiotics such as mupirocin are also effective. 

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