Mupirocin Calcium

(BANM, USAN, rINNM)
Synonyms: BRL-4910F; Calcii Mupirocinum; Mupirocin vápenatá sůl dihydrát; Mupirocina cálcica; Mupirocine calcique; Mupirocinkalcium; Mupirocin-kalcium; Mupirocino kalcio druska; Mupirocinum calcicum; Mupirocinum Calcicum Dihydricum; Mupirosiinikalsium.
Cyrillic synonym: Кальций Мупироцин.

💊 Chemical information

Chemical formula: C52H86O18Ca,2H2O = 1075.3.
CAS — 104486-81-9 (anhydrous mupirocin calcium); 115074-43-6 (mupirocin calcium dihydrate).
ATC — D06AX09; R01AX06.
ATC Vet — QD06AX09; QR01AX06.

Pharmacopoeias.

In Eur., Jpn, and US.

Ph. Eur. 6.2

(Mupirocin Calcium). A white or almost white powder. Very slightly soluble in water; sparingly soluble in dehydrated alcohol and in dichloromethane.

USP 31

(Mupirocin Calcium). Store in airtight containers at a temperature of 25°, excursions permitted between 15° and 30°.

💊 Adverse Effects and Precautions

Mupirocin is usually well tolerated but local reactions such as burning, stinging, and itching may occur after the application of mupirocin to the skin. Some mupirocin products are formulated in a macrogol base: such formulations are not suitable for application to mucous membranes and should be used with caution in patients with extensive burns or wounds because of the possibility of macrogol toxicity. Care is also required in patients with renal impairment.

💊 Antimicrobial Action

Mupirocin is an antibacterial that inhibits bacterial protein synthesis by binding to isoleucyl transfer RNA synthetase. It is mainly bacteriostatic at low concentrations, although it is usually bactericidal in the high concentrations achieved by topical application to the skin. At these concentrations it may have some activity against organisms reported to be relatively resistant to mupirocin in vitro. It is mainly active against Gram-positive aerobes. Most strains of staphylococci (including meticillin-resistant and multiply-resistant Staph. aureus) and streptococci are susceptible in vitro, although the enterococci are relatively resistant. Mupirocin is also active against Listeria monocytogenes and Erysipelothrix rhusiopathiae. The Gram-negative organisms are generally insensitive, but Haemophilus influenzae, Neisseria spp. and a few others are sensitive. Anaerobic organisms, both Gram-positive and Gram-negative, are generally resistant, and activity against fungi is low. Mupirocin is more active in vitro at acid pH than in alkaline conditions. Naturally resistant strains of Staph. aureus occur rarely but resistance, including high-level plasmid-mediated transferable resistance, has emerged, particularly during long-term use. There has been some concern that inappropriate prescribing of mupirocin has led to this steadily increasing resistance.

Activity against fungi.

Activity of mupirocin 2% in vitro against Candida albicans was comparable to that of other commonly used topical antifungals. Although MICs were considerably in excess of those reported for susceptible bacteria, clinical responses in 10 patients suggested that adequate concentrations of mupirocin were achieved after topical application.1
1. Rode H, et al. Efficacy of mupirocin in cutaneous candidiasis. Lancet 1991; 338: 578.

Resistance.

References.
1. Cookson BD. The emergence of mupirocin resistance: a challenge to infection control and antibiotic prescribing practice. J Antimicrob Chemother 1998; 41: 11–18
2. Schmitz F-J, et al. The prevalence of low- and high-level mupirocin resistance in staphylococci from 19 European hospitals. J Antimicrob Chemother 1998; 42: 489–95
3. Upton A, et al. Mupirocin and Staphylococcus aureus: a recent paradigm of emerging antibiotic resistance. J Antimicrob Chemother 2003; 51: 613–17
4. Kresken M, et al. Prevalence of mupirocin resistance in clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis: results of the Antimicrobial Resistance Surveillance Study of the Paul-Ehrlich-Society for Chemotherapy, 2001. Int J Antimicrob Agents 2004; 23: 577–81
5. Walker ES, et al. A decline in mupirocin resistance in methicillin-resistant Staphylococcus aureus accompanied administrative control of prescriptions. J Clin Microbiol 2004; 42: 2792–5.

💊 Pharmacokinetics

Only very small amounts of topically applied mupirocin are absorbed into the systemic circulation where it is rapidly metabolised to monic acid which is excreted in the urine.

💊 Uses and Administration

Mupirocin is an antibacterial produced by Pseudomonas fluorescens. It is applied topically as a 2%
ointment in a macrogol base, or as a cream containing mupirocin calcium equivalent to 2% mupirocin, in the treatment of various bacterial skin infections. These preparations should be applied up to 3 times daily for up to 10 days; treatment should be re-evaluated if there is no response after 3 to 5 days. They are not suitable for application to mucous membranes, and therefore a nasal ointment containing mupirocin calcium equivalent to 2% mupirocin in a paraffin basis is used for eradication of the nasal carriage of Staphylococcus aureus, particularly epidemic meticillin-resistant strains. The nasal ointment should be applied into each nostril 2 or 3 times daily for a maximum of 7 days. For further details of skin infections and staphylococcal infections and their treatment, see under Choice of Antibacterial.
1. Roth VR, et al. Should we routinely use mupirocin to prevent staphylococcal infections? Infect Control Hosp Epidemiol 2000; 21: 745–9
2. Perl TM, et al. Mupirocin and the Risk of Staphylococcus Aureus Study Team. Intranasal mupirocin to prevent postoperative Staphylococcus aureus infections. N Engl J Med 2002; 346: 1871–7
3. Takahashi S, et al. The preventive effects of mupirocin against nasotracheal intubation-related bacterial carriage. Anesth Analg 2003; 97: 222–5
4. Laupland KB, Conly JM. Treatment of Staphylococcus aureus colonization and prophylaxis for infection with topical intranasal mupirocin: an evidence-based review. Clin Infect Dis 2003; 37: 933–8
5. Tacconelli E, et al. Mupirocin prophylaxis to prevent Staphylococcus aureus infection in patients undergoing dialysis: a metaanalysis. Clin Infect Dis 2003; 37: 1629–38
6. Wertheim HF, et al. Mupirocin prophylaxis against nosocomial Staphylococcus aureus infections in nonsurgical patients: a randomized study. Ann Intern Med 2004; 140: 419–25
7. Kallen AJ, et al. Perioperative intranasal mupirocin for the prevention of surgical-site infections: systematic review of the literature and meta-analysis. Infect Control Hosp Epidemiol 2005; 26: 916–22
8. Unemura Y, et al. Impact of prophylactic mupirocin for radical esophagectomy. J Infect Chemother 2006; 12: 257–63
9. Sit D, et al. Prophylactic intranasal mupirocin ointment in the treatment of peritonitis in continuous ambulatory peritoneal dialysis patients. Adv Therapy 2007; 24: 387–93.

💊 Preparations

BP 2008: Mupirocin Ointment; USP 31: Mupirocin Cream; Mupirocin Ointment.

Proprietary Preparations

Arg.: Bactroban; Mupax; Mupirox; Paldar; Vidox; Austral.: Bactroban; Austria: Bactroban; Belg.: Bactroban; Braz.: Bacrocin; Bactocin; Bactroban; Bactroneo; Canad.: Bactroban; Chile: Bactroban; Bantix; Ultrabiotic; Underan; Cz.: Bactroban; Denm.: Bactroban; Fin.: Bactroban; Fr.: Bactroban; Mupiderm; Ger.: InfectoPyoderm; Turixin; Gr.: Bactroban; Bactrocine; Hevronaz; Micoban; Mupider; Mupiran; Veltion; Hong Kong: Bactroban; Hung.: Bactroban; India: Bactroban; Supirocin; Indon.: Bactoderm; Bactroban; Pibaksin; Irl.: Bactroban; Israel: Bactoderm†; Bactroban; Ital.: Bactroban; Mupiskin; Jpn: Bactroban; Malaysia: Bactroban; Muprin; Mex.: Bactroban; Sinpebac; Neth.: Bactroban; NZ: Bactroban; Philipp.: Bactifree; Bactroban; Foskina; Pol.: Bactroban; Mupirox; Port.: Bactroban; Rus.: Bactroban (Бактробан); S.Afr.: Bactroban; Singapore: Bactroban; Supirocin; Spain: Bactroban; Plasimine; Swed.: Bactroban; Switz.: Bactroban; Thai.: Bactex; Bactroban; Muporin; Turk.: Bactroban; UK: Bactroban; USA: Bactroban; Centany; Venez.: Bactroban; Bactrobandos†. Multi-ingredient: India: Supirocin-B.
Published May 08, 2019.