{"id":154,"date":"2023-06-25T09:20:34","date_gmt":"2023-06-25T08:20:34","guid":{"rendered":"https:\/\/microregistrar.com\/?p=154"},"modified":"2023-06-25T09:34:05","modified_gmt":"2023-06-25T08:34:05","slug":"fusidic-acid","status":"publish","type":"post","link":"https:\/\/microregistrar.com\/?p=154","title":{"rendered":"Fusidic acid"},"content":{"rendered":"\n

Fusidic acid was discovered in Copenhagen, Denmark and introduced to clinical practice in the 1960s.
It was derived from a fungus,\u00a0Fusidium coccineum<\/em>.<\/p>\n\n\n\n

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\n
\"\"<\/figure>\n<\/div>\n\n\n\n
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Fusidic acid has a structural similarity with the steroid molecule. You can see in the picture the molecular structure is similar to prednisolone. For this reason, it is called a steroid antibiotic.<\/p>\n\n\n\n

It also has a structural similarity with cephalosporin P. However, the cephalosporin antibiotics we use are derived from cephalosporin C. Hence fusidic acid is not a cephalosporin.<\/p>\n<\/div>\n<\/div>\n\n\n\n

Mechanism of action<\/h2>\n\n\n\n

Fusidic acid inhibits protein synthesis by targeting elongation factor G (EF-G).<\/p>\n\n\n\n

By binding to the EF-G, it prevents\u00a0the translocation of t RNA carrying the amino acid on the ribosomal mRNA complex, hence amino acid fails to be incorporated in the growing peptide chain.<\/strong><\/p>\n\n\n\n

Mechanism of resistance<\/h2>\n\n\n\n

Bacteria can develop resistance to this antibiotic by three mechanisms.<\/p>\n\n\n\n

    \n
  • Reducing the affinity for the elongation factor G.<\/li>\n\n\n\n
  • Enzymatic destruction of the antibiotic and.<\/li>\n\n\n\n
  • Efflux pump, which helps the bacteria to remove antibiotics from its cell.<\/li>\n<\/ul>\n\n\n\n

    The most important resistance mechanism is a mutation in the fus gene<\/strong>, which produces elongation factors with low affinity or protect the EF-G from fusidic acid.<\/p>\n\n\n\n

      \n
    • fusA \u2013 Staph aureus, Staph epidermidis<\/strong><\/li>\n\n\n\n
    • fusB \u2013 Staph aureus<\/strong><\/li>\n\n\n\n
    • fusC, fusD \u2013 Staph aureus, Staph saprophyticus<\/strong><\/li>\n\n\n\n
    • fusE \u2013 Staph aureus (small colony variant)<\/strong><\/li>\n<\/ul>\n\n\n\n

      fusB mutation has been associated with an epidemic impetigo strain.<\/p>\n\n\n\n

      Other types of mechanisms, like enzymatic destruction of acrAB efflux pump, can be seen in some gram-negative bacteria.<\/p>\n\n\n\n

      Properties<\/h2>\n\n\n\n
        \n
      • Oral bioavailability \u2013<\/strong> Suspension and some older preparations  50-70%, while<\/strong> newer film-coated preparation may have IV equivalent bioavailability<\/strong>.<\/li>\n\n\n\n
      • Highly protein-bound >95%<\/strong>.<\/li>\n\n\n\n
      • Wide distribution in the body;  penetrates abscess.<\/strong><\/li>\n\n\n\n
      • Metabolised in the liver \u2013 Some metabolites are active.<\/strong><\/li>\n\n\n\n
      • The main route of excretion is bile.<\/strong><\/li>\n<\/ul>\n\n\n\n

        Adverse effects<\/h2>\n\n\n\n
          \n
        • Local adverse effects \u2013 <\/strong>
          Oral \u2013 gastrointestinal disturbances <\/strong>
          IV \u2013 thrombophlebitis <\/strong>
          Topical (eye) \u2013 dry eye, eye discomfort, conjunctivitis<\/strong>.<\/li>\n\n\n\n
        • Gastro-hepatic \u2013 hyperbilirubinaemia, decreased appetite<\/strong>.<\/li>\n\n\n\n
        • CNS \u2013 dizziness, headache<\/strong>,<\/li>\n\n\n\n
        • Haematological \u2013 anaemia, leukopenia, thrombocytopenia<\/strong>.<\/li>\n\n\n\n
        • Skin \u2013 rash, Toxic epidermal necrolysis, Stevens-Johnson syndrome, DRESS syndrome<\/strong>.<\/li>\n\n\n\n
        • Muscle \u2013 Rhabdomyolysis<\/strong> (avoid using concurrently with statins).<\/li>\n<\/ul>\n\n\n\n

          Spectrum<\/h2>\n\n\n\n
            \n
          • Fusidic acid is mainly used for\u00a0Staphylococcus<\/strong>\u00a0infection. It has activity against Staphylococcus aureus, including MRSA. Some coagulase-negative Staphylococcus are also susceptible.<\/li>\n\n\n\n
          • Streptococcus<\/strong>\u00a0are less susceptible, and\u00a0Enterococcus\u00a0<\/strong>are often resistant.<\/li>\n\n\n\n
          • Fusidic acid has activity against Corynebacterium spp<\/strong>, and some Mycobacteria<\/strong>.<\/li>\n\n\n\n
          • It is mostly resistant to gram-negative bacteria<\/strong>. However, it retains some activity against Neisseria, Moraxella, Legionella<\/strong> etc.<\/li>\n\n\n\n
          • It has a good anti-anaerobe <\/strong>spectrum and is active against C difficile. However, Fusobacterium and some anaerobes tend to have high MIC.<\/li>\n<\/ul>\n\n\n\n

            Indication<\/h2>\n\n\n\n
              \n
            • Staphylococcal skin infection<\/strong> \u2013 Non-bullous impetigo, bacterial superinfection<\/strong><\/li>\n\n\n\n
            • Staphylococcal eye infection<\/strong><\/li>\n\n\n\n
            • Deep staphylococcal infection \u2013 osteomyelitis, endocarditis<\/strong>.<\/li>\n<\/ul>\n\n\n\n

              Systemic monotherapy is not recommended as resistance may develop quickly.<\/p>\n","protected":false},"excerpt":{"rendered":"

              Fusidic acid was discovered in Copenhagen, Denmark and introduced to clinical practice in the 1960s.It was derived from a fungus,\u00a0Fusidium […]<\/p>\n","protected":false},"author":1,"featured_media":155,"comment_status":"open","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"site-sidebar-layout":"default","site-content-layout":"","ast-site-content-layout":"default","site-content-style":"default","site-sidebar-style":"default","ast-global-header-display":"","ast-banner-title-visibility":"","ast-main-header-display":"","ast-hfb-above-header-display":"","ast-hfb-below-header-display":"","ast-hfb-mobile-header-display":"","site-post-title":"","ast-breadcrumbs-content":"","ast-featured-img":"","footer-sml-layout":"","ast-disable-related-posts":"","theme-transparent-header-meta":"","adv-header-id-meta":"","stick-header-meta":"","header-above-stick-meta":"","header-main-stick-meta":"","header-below-stick-meta":"","astra-migrate-meta-layouts":"default","ast-page-background-enabled":"default","ast-page-background-meta":{"desktop":{"background-color":"var(--ast-global-color-5)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"tablet":{"background-color":"","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"mobile":{"background-color":"","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""}},"ast-content-background-meta":{"desktop":{"background-color":"var(--ast-global-color-4)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"tablet":{"background-color":"var(--ast-global-color-4)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""},"mobile":{"background-color":"var(--ast-global-color-4)","background-image":"","background-repeat":"repeat","background-position":"center center","background-size":"auto","background-attachment":"scroll","background-type":"","background-media":"","overlay-type":"","overlay-color":"","overlay-opacity":"","overlay-gradient":""}},"ngg_post_thumbnail":0,"footnotes":""},"categories":[9],"tags":[28,35],"class_list":["post-154","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-antibiotic","tag-antibiotic","tag-fusidic-acid"],"_links":{"self":[{"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/posts\/154","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/users\/1"}],"replies":[{"embeddable":true,"href":"https:\/\/microregistrar.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=154"}],"version-history":[{"count":1,"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/posts\/154\/revisions"}],"predecessor-version":[{"id":156,"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/posts\/154\/revisions\/156"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/microregistrar.com\/index.php?rest_route=\/wp\/v2\/media\/155"}],"wp:attachment":[{"href":"https:\/\/microregistrar.com\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=154"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/microregistrar.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=154"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/microregistrar.com\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=154"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}