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Fusidic acid is a bacteriostatic antibiotic that is ordinarily used topically in creams and eyedrops, but may also be given systemically as tablets or injections.

Pharmacology

Fusidic acid works by interfering with bacterial protein coalescence, specifically by preventing the translocation of the elongation factor G (EF-G) from the ribosome. Fusidic acid is sole effective on gram-positive bacteria such as Staphylococcus species and Corynebacterium species. Fusidic acid inhibits bacterial replication and does not dispatch the bacteria, and is therefore termed "bacteriostatic".

Fusidic acid is a true antibiotic, derived from the fungus Fusidium coccineum and was developed by Leo Laboratories in Ballerup, Denmark and released for clinical use in the 1960s. It has also been set apart from Mucor ramannianus and Isaria kogana . The drug is not licensed for use in the US, but, as sodium fusidate , it is approved for use at the beck prescription in the UK, Canada, Europe, Israel, Australia and New Zealand.

Uses

Fusidic acid is on the go in vitro against Staphylococcus aureus , most coagulase-negative staphylococci, Corynebacterium species, most clostridium species. Fusidic acid has no functional activity against enterococci or most Gram-negative bacteria (except Neisseria, Moraxella, Legionella pneumophila and Bacteroides fragilis ). Fusidic acid is vigorous in vitro and clinically against Mycobacterium leprae but has only marginal activity against Mycobacterium tuberculosis .

One eminent use of fusidic acid clinically is its activity against methicillin-resistant Staphylococcus aureus. Sundry strains of MRSA remain sensitive to fusidic acid, but because there is a low genetic frontier to resistance (a single point mutation is all that is required), fusidic acid obligated to never be used on its own to treat serious MRSA infection and should be combined with another antimicrobial such as rifampicin.

Fusidic acid is instances found in topical skin and eye preparations (e.g., Fucibet), a use which has been contested.

Dosing

Fusidic acid should not be tempered to on its own to treat Staph. aureus infections. The use of topical preparations (skin creams and eye ointments) containing fusidic acid is strongly associated with the incident of resistance, and there are voices agitating against the continued use of fusidic acid monotherapy in the community. Local preparations used in Europe often contain fusidic acid and gentamicin in conspiracy, which helps to prevent the development of resistance.

Depending on the reason for which sodium fusidate is prescribed the adult measure can be 250 mg twice a day and or up to 750 mg three times a day. (Skin conditions normally desideratum the smaller dose). It is available in tablet and suspension form. There is an intravenous preparation handy but it is irritant to veins, causing phlebitis. Most people absorb the drug very well after taking it orally so, if a patient can swallow, there is not much constraint to administer it intravenously, including endocarditis (infection of the heart chambers).

Pregnancy counsel

There is inadequate evidence of safety in human pregnancy. Animal studies and numerous years of clinical experience suggest that fusidic acid is devoid of teratogenic effects (start defects)...fusidic acid can cross the placental barrier.

Side Effects

• Fucidin Tablets and Rejection can occasionally cause liver upsets which can produce jaundice (yellowing of a forbearing's skin and the whites of his or her eyes). This condition will almost always get change one's mind after you finish taking Fucidin Tablets or Suspension. Other related side effects file dark urine, lighter-than-usual feces. These, too should conform when the course of treatment is completed.
• Patients taking the drug should announce their doctors if they notice that their urine is 'very drab', their feces are 'very pale' or if their skin or the whites of their eyes becomes yellow, the Australian matter sheet for patients adds.

Resistance

Because the drug is not licensed for use in the US, there are no Clinical and Laboratory Standards Society standard definitions of fusidic acid resistance.

In the UK and Australia, susceptibility is defined as an least inhibitory concentration (MIC) of 0.25mg/l or 0.5mg/l or less. Resistance is defined as an MIC of 2mg/l or more. In laboratories using disc diffusion methods, susceptibility for a 2.5µg disc is defined as a zone of 22 mm or more, and guerilla movement is defined as a zone of 17 mm or less; intermediate values are defined as intermediate refusal.

Mechanisms of resistance have only been extensively studied in Staphylococcus aureus . The most critical mechanism is the development of point mutations in fusA , the chromosomal gene which codes for EF-G. The varying alters EF-G so that fusidic acid is no longer able to bind to it. Resistance is eagerly acquired when fusidic acid is used alone and commonly develops during the lecture of treatment, but resistance does not occur when fusidic acid is used in conjunction with other antibiotics. For this reason, fusidic acid should not be utilized on its own to treat serious Staph. aureus infections. However, at least in Canadian hospitals, facts collected between 1999-2005 showed rather low rate of resistance of MSSA and MRSA to fusidic acid, and mupirocin was more disputed topical antibiotics from this point of view.

Some bacteria also mediate defiance via the fusB gene, which is carried on a plasmid; the mechanism by which fusB causes intransigence is unknown.

Interactions

Fusidic acid should not be used with quinolones, with which they are antagonistic. When combined with rifampicin, the deportment of fusidic acid is additive or synergistic.
It has been reported on August 8th 2008, that the Irish Medicines Surface is investigating the death of a 59-year-old Irish man who developed rhabdomyolysis after combining Lipitor and Fusidic Acid, and three nearly the same cases.

It is delivered as an ointment, a cream, eye drops or in tablet form.

Trade names and preparations

• Fusidin (of Leo in Canada)
• Fucidin (of Leo in UK/ Leo-Ranbaxy-Croslands in India)
• Fucidine (of Leo in France)
• Fucithalmic (of Leo in UK and Denmark)
• Fucicort (local mixture with hydrocortisone)
• Fucibet (topical mixture with betamethasone)
• fuci(of pharopharm in Egypt)
• fucizon(local mixture with hydrocortisone of pharopharm in Egypt)
• fusiderm (topical cream and mediocre by indi pharma in india)

References

1. ^ Existing drug will cure polyclinic superbug MRSA, say scientists – The Guardian, 17 January 2007.Accessed 2008-01-17.
2. ^ ^{a b} Howden BP, Grayson ML (2006). "Quiet and dumber—the potential waste of a useful antistaphylococcal agent: emerging fusidic acid guerrilla in Staphylococcus aureus ". Clin Infect Dis 42 (3): 394–400. doi: 10.1086/499365 .  
3. ^ Mason BW, Howard AJ, Magee JT (2003). "Fusidic acid opposition in community isolates of methicillin-susceptible Staphylococcus aureus and fusidic acid prescribing". J Antimicrob Chemother 51 : 300–3. doi: 10.1093/jac/dkg190 . PMID 12654748.  
4. ^ Fucidin matter sheet archived by New Zealand government. December 2005.Accessed: 2007-09-09.
5. ^ Fucidin) UK statistics sheet archived at the electronic Medicines Compendium. June 1997.Accessed: 2007-09-09.
6. ^ Fucidin unaggressive information leaflet, archived by Government of Victoira, Australia .Accessed: 2007-09-09.
7. ^ Turnidge J, Collignon P (1999). "Stubbornness to fusidic acid". Int J Antimicrob Agents 12 (Suppl 2): S35–44. doi: 10.1016/S0924-8579(98)00072-7 .  
8. ^ Besier S, Ludwig A, Brade V, Wichelhaus TA (2003). "Molecular division of fusidic acid resistance in Staphylococcus aureus ". Mol Microbiol 47 : 463–9. doi: 10.1046/j.1365-2958.2003.03307.x .  
9. ^ Fantin B, Leclerq R, Duval J, Carbon C (1993). "Fusidic acid toute seule or in combination with vancomycin for therapy of experimental endocarditis due to methicillin-resistant Staphylococcus aureus ". Antimicrob Agents Chemother 37 : 2466–69.  
10. ^ Rennie RP (2006). "Susceptibility of Staphylococcus aureus to fusidic acid:Canadian materials". J Cutan Med Surg 10 : 277-280.  
11. ^ Collignon P, Turnidge J (1999). "Fusidic acid in vitro work". Int J Antimicrob 12 (Suppl 2): S45–58. doi: 10.1016/S0924-8579(98)00073-9 .  
12. ^ http:
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