Retapamulin

Retapamulin is a topical antibiotic developed by GlaxoSmithKline. It is the first drug in the new class of pleuromutilin antibiotics to be approved for human use. It is marketed as an ointment under the brand names Altabax and Altargo.

Retapamulin
Clinical data
Trade namesAltabax, Altargo
AHFS/Drugs.comMonograph
MedlinePlusa607049
License data
Pregnancy
category
  • US: B (No risk in non-human studies)
    Routes of
    administration    		Topical (ointment)
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    BioavailabilityLow
    Protein binding94%
    MetabolismHepatic, CYP3A4-mediated
    Elimination half-lifeUndetermined
    ExcretionUndetermined
    Identifiers
    CAS Number
    PubChem CID
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEMBL
    ECHA InfoCard100.167.142
    Chemical and physical data
    FormulaC30H47NO4S
    Molar mass517.77 g/mol g·mol−1
    3D model (JSmol)
     NY (what is this?)  (verify)

    Retapamulin was approved by the United States Food and Drug Administration in April 2007 for the treatment of bacterial skin infections such as impetigo. In May 2007, retapamulin received approval in the EU from the European Medicines Agency for the same indication.

    Clinical trials have demonstrated its efficacy against certain Gram-positive bacteria including MRSA.[1]

    Indications

    Retapamulin is indicated for the topical treatment of impetigo due to Staphylococcus aureus (methicillin-susceptible only) or Streptococcus pyogenes.[2]

    Pharmacology

    Mechanism of action

    Retapamulin is an antibacterial agent, specifically a protein synthesis inhibitor. The medication selectively inhibits bacterial protein synthesis by interacting at a site on the 50S subunit of the bacterial ribosome through an interaction that differs from other antibiotics.[2]

    Pharmacokinetics

    Systemic exposure following topical application through intact skin is low.[2]

    Contraindications

    None yet reported.[2]

    Adverse reactions

    The most common reported adverse reaction was irritation at the application site.[2]

    References
    1. Jones R, Fritsche T, Sader H, Ross J (2006). "Activity of retapamulin (SB-275833), a novel pleuromutilin, against selected resistant gram-positive cocci". Antimicrob Agents Chemother. 50 (7): 2583–6. doi:10.1128/AAC.01432-05. PMC 1489758. PMID 16801451.
    2. Borrza, S.; Philippi, E., eds. (2007). Physicians' Desk Reference (62nd ed.). pp. 1318–20. ISBN 1-56363-660-3.
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