Infectious Disease Book

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MacrolideAka: Erythromycin

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  1. Mechanism of action
    1. Reversibly binds 50S ribosomal subunit
    2. Inhibits protein synthesis
  2. Bacterial resistance mechanisms
    1. Impermeability of bacterial outer membranes
      1. Especially Gram Negative Organisms
    2. Production of enzymes that alter ribosomal targets
  3. Adverse Effects
    1. Gastrointestinal upset
    2. Nausea
    3. Cholestatic Jaundice
    4. Multiple drug interactions
  4. Complications
    1. Candida Vaginitis infection
    2. Gram Negative Folliculitis
  5. Pharmacokinetics
    1. Half life: 1.5 hours
  6. Drug Interactions
    1. Interactions may also occur with extended spectrum
      1. Clarithromycin
      2. Telithromycin
      3. Less likely to occur with Azithromycin
    2. QT Prolongation (erythromycin with an agent below)
      1. Calcium Channel Blockers increase erythromycin level
        1. Verapamil
        2. Diltiazem
      2. Other potent CYP3A4 inhibitors
        1. Ketoconazole
        2. Itraconazole
        3. Nefazodone
        4. Protease Inhibitors
    3. References
      1. Ray (2004) N Engl J Med 351:1089
  7. Oral Preparations (Take with food to reduce GI Upset)
    1. Erythromycin base 1000 mg/day PO divided bid-qid
    2. Erythromycin ethyl succinate (EES)
      1. Adult: 400 mg PO qid
      2. Child: 30-50 mg/kg/day PO divided qid
  8. Parenteral Preparation: Erythromycin lactobionate
    1. Dose: 15 to 20 mg/kg/day IV divided every 6 hours
    2. Maximum: 4 grams
  9. Activity Spectrum
    1. Major indications for Erythromycin
      1. Chlamydia pneumoniae
      2. Chlamydia trachomatis
        1. Pneumoniae or Conjunctivitis
        2. Pelvic infection in pregnancy
      3. Legionella pneumophila
      4. Mycoplasma pneumoniae
      5. Bordetella pertussis
      6. Corynebacterium diphtheriae
      7. Campylobacter jejuni
    2. Other organisms covered
      1. Ureaplasma urealyticum
      2. Treponema pallidum (Syphilis)
      3. Staphylococcus
      4. Streptococcus
      5. Bacillus anthracis
      6. Clostridium species

Erythromycin (C0014806)

Definition (MSH)A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.
Definition (CSP)bacteriostatic antibiotic macrolide produced by Streptomyces erythreus; in sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits; this binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.
Definition (PDQ)A broad-spectrum, topical macrolide antibiotic with antibacterial activity. Erythromycin diffuses through the bacterial cell membrane and reversibly binds to the 50S subunit of the bacterial ribosome. This prevents bacterial protein synthesis. Erythromycin may be bacteriostatic or bactericidal in action, depending on the concentration of the drug at the site of infection and the susceptibility of the organism involved. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39234&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39234&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C476" NCI Thesaurus)
Definition (NCI)A broad-spectrum, macrolide antibiotic with antibacterial activity. Erythromycin diffuses through the bacterial cell membrane and reversibly binds to the 50S subunit of the bacterial ribosome. This prevents bacterial protein synthesis. Erythromycin may be bacteriostatic or bactericidal in action, depending on the concentration of the drug at the site of infection and the susceptibility of the organism involved.
ConceptsOrganic Chemical (T109) , Antibiotic (T195)
EnglishErythromycin, Erythromycin A, Erythromycin base, ERYTHROMYCIN PREPARATION, Erythromycin product, Erythromycins
Spanisheritromicina
CreditsDerived from the NIH UMLS (Unified Medical Language System)


Macrolides (C0282563)

Definition (MSH)A group of macrocyclic compounds formed by chain extension of multiple PROPIONATES and cyclized into a large (typically 12, 14, 16) membered lactone. They are often glycosylated. Many of them are ANTIBIOTICS.
Definition (NCI)A term used to describe a chemical structure of a compound containing a large lactone ring, usually with a 14 or 16-membered ring structure. The prototypical compounds within the macrolide class are the erythromycin-based antibiotics; however, many compounds with this chemical structure are being developed for other diseases.
ConceptsOrganic Chemical (T109)
EnglishMacrolide, Macrolides
CreditsDerived from the NIH UMLS (Unified Medical Language System)



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