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Fusidic acid
Fusidic acid, sold under the brand name Fucidin among others, is an antibiotic that is often used topically in creams or ointments and eyedrops but may also be given systemically as tablets or injections. As of October 2008[update], the global problem of advancing antimicrobial resistance has led to a renewed interest in its use.
Fusidic acid is active in vitro against Staphylococcus aureus, most coagulase-positive staphylococci, Beta-hemolytic streptococci, Corynebacterium species, and most clostridium species.[medical citation needed] Fusidic acid has no known useful activity against enterococci or most Gram-negative bacteria (except Neisseria, Moraxella, Legionella pneumophila, and Bacteroides fragilis).[medical citation needed] Fusidic acid is active in vitro and clinically against Mycobacterium leprae but has only marginal activity against Mycobacterium tuberculosis.[medical citation needed]
One use of fusidic acid is its activity against methicillin-resistant Staphylococcus aureus (MRSA). Although many strains of MRSA remain sensitive to fusidic acid, there is a low genetic barrier to drug resistance (a single point mutation is all that is required), fusidic acid should never be used on its own to treat serious MRSA infection and should be combined with another antimicrobial such as rifampicin when administering oral or topical dosing regimens approved in Europe, Canada, and elsewhere. However, resistance selection is low when pathogens are challenged at high drug exposure.
Topical fusidic acid is occasionally used as a treatment for acne vulgaris. As a treatment for acne, fusidic acid is often partially effective at improving acne symptoms. However, research studies have indicated that fusidic acid is not as highly active against Cutibacterium acnes as many other antibiotics that are commonly used as acne treatments. Fusidic acid is also found in several additional topical skin and eye preparations (e.g., Fucibet), although its use for these purposes is controversial.
Fucidin tablets and suspension, whose active ingredient is sodium fusidate, occasionally cause liver damage, which can produce jaundice (yellowing of the skin and the whites of the eyes). This condition will almost always get better after the patient finishes taking Fucidin tablets or suspension. Other related side-effects include dark urine and lighter-than-usual feces. These, too, should normalize when the course of treatment is completed.
Fusidic acid acts as a bacterial protein synthesis inhibitor by preventing the turnover of elongation factor G (EF-G) from the ribosome. Fusidic acid is effective primarily on Gram-positive bacteria such as Staphylococcus, Streptococcus and Corynebacterium species.
Fusidic acid is a tetracyclic, naturally occurring steroid derived from the fungus Fusidium coccineum. It was first isolated in 1960 and developed by Leo Pharma in Ballerup, Denmark, being used clinically from 1962 onwards. It has also been isolated from Mucor ramannianus, an Acremonium species, and Isaria kogana. The drug is licensed for use as its sodium salt sodium fusidate, and it is approved for use under prescription in Australia, Canada, Colombia, the European Union, India, Japan, New Zealand, South Korea, Taiwan, Thailand,[citation needed] and the United Kingdom.
Fusidic acid binds to EF-G after translocation and GTP (guanosine-5'-triphosphate) hydrolysis. This interaction prevents the necessary conformational changes for EF-G release from the ribosome, effectively blocking the protein synthesis process. Fusidic acid can only bind to EF-G in the ribosome after GTP hydrolysis.
Fusidic acid
Fusidic acid, sold under the brand name Fucidin among others, is an antibiotic that is often used topically in creams or ointments and eyedrops but may also be given systemically as tablets or injections. As of October 2008[update], the global problem of advancing antimicrobial resistance has led to a renewed interest in its use.
Fusidic acid is active in vitro against Staphylococcus aureus, most coagulase-positive staphylococci, Beta-hemolytic streptococci, Corynebacterium species, and most clostridium species.[medical citation needed] Fusidic acid has no known useful activity against enterococci or most Gram-negative bacteria (except Neisseria, Moraxella, Legionella pneumophila, and Bacteroides fragilis).[medical citation needed] Fusidic acid is active in vitro and clinically against Mycobacterium leprae but has only marginal activity against Mycobacterium tuberculosis.[medical citation needed]
One use of fusidic acid is its activity against methicillin-resistant Staphylococcus aureus (MRSA). Although many strains of MRSA remain sensitive to fusidic acid, there is a low genetic barrier to drug resistance (a single point mutation is all that is required), fusidic acid should never be used on its own to treat serious MRSA infection and should be combined with another antimicrobial such as rifampicin when administering oral or topical dosing regimens approved in Europe, Canada, and elsewhere. However, resistance selection is low when pathogens are challenged at high drug exposure.
Topical fusidic acid is occasionally used as a treatment for acne vulgaris. As a treatment for acne, fusidic acid is often partially effective at improving acne symptoms. However, research studies have indicated that fusidic acid is not as highly active against Cutibacterium acnes as many other antibiotics that are commonly used as acne treatments. Fusidic acid is also found in several additional topical skin and eye preparations (e.g., Fucibet), although its use for these purposes is controversial.
Fucidin tablets and suspension, whose active ingredient is sodium fusidate, occasionally cause liver damage, which can produce jaundice (yellowing of the skin and the whites of the eyes). This condition will almost always get better after the patient finishes taking Fucidin tablets or suspension. Other related side-effects include dark urine and lighter-than-usual feces. These, too, should normalize when the course of treatment is completed.
Fusidic acid acts as a bacterial protein synthesis inhibitor by preventing the turnover of elongation factor G (EF-G) from the ribosome. Fusidic acid is effective primarily on Gram-positive bacteria such as Staphylococcus, Streptococcus and Corynebacterium species.
Fusidic acid is a tetracyclic, naturally occurring steroid derived from the fungus Fusidium coccineum. It was first isolated in 1960 and developed by Leo Pharma in Ballerup, Denmark, being used clinically from 1962 onwards. It has also been isolated from Mucor ramannianus, an Acremonium species, and Isaria kogana. The drug is licensed for use as its sodium salt sodium fusidate, and it is approved for use under prescription in Australia, Canada, Colombia, the European Union, India, Japan, New Zealand, South Korea, Taiwan, Thailand,[citation needed] and the United Kingdom.
Fusidic acid binds to EF-G after translocation and GTP (guanosine-5'-triphosphate) hydrolysis. This interaction prevents the necessary conformational changes for EF-G release from the ribosome, effectively blocking the protein synthesis process. Fusidic acid can only bind to EF-G in the ribosome after GTP hydrolysis.
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