MACROLIDES a Chapter 47 MACROLIDES ‘This aroup is charac its Fea sare by the presence of lactone ring in thei structure to which sugar ae ced from Streptomyces Erythrews, Clarithromyein and Azithromy is attached, in are semisynthetic ERYTHROMYCIN MECHANISM OF ACITO! a i MECHANISMLOE imilar to chtoramphenicol, by bindin + Reduced permeability of the drug or active efflux ofthe drug. ‘¢ Modification of the ribosomal binding site. | * _ In Enterobacteriaceae by production ofthe esterase swhiel Cross-resistance is complete b/w erythromycin arul other members. 12 to 50S ribosomal subunit, h hydrolyzes the drug. CLINICAL USES: 1. Drug of choice in Conymebareterial inf (Diphtheria, sepsis, erythrasma). in in allergic pis with Streptococcal, “Preimococeal and Staphylococcal: inf. ta. and other respi ‘ed by Chlamydia, Mycoplasma, Legio) rif (enterocolitis) & Acne. st Spirochetes (Treponema palladium causing sypbi 5. Ithas activity ex HARMACOKINETICS: P eee ramust be administered as enteric coated tablets as itis destroyed by stomach acid Serum T J 1.5 hr. It does not enter CNS but can eross placenta. itis taken up by leukocytes and macrophages. ADVERSE EFFECTS: 7, GIT DISTURBANCES: Anorexia, 2, LIVER TOXICITY: jaundice, fever, 3, Thrombophelibitis at the site of injection, nausea, Vomiting, Diarthes and epigastric distress, cholestatic hepatitis and liver’ dysfunctioning. vovinophilia and superinfecion with candidiasis can ou. DRUG INTERACTIONS: = ‘is metabolites cam inhib fine, oral anticoagulants, cyclosporine ‘& Methylprednisolone. «Inc bjoavailabililty and serum cone of oral digoxin. j CLARI THROMYCIN «Derived from Erythromycin by dition of @ Methyl group & has more sed se 3. J Glinical effects are similar except its more effective against 68, intracellular bacteria M weza and Toxoplasina Gondii, i leprae, Chlamydia, Legionella, H. inf « Gidisturbances ae less common. It has active metabolites: cytochrome P450 system—>ine action of theophyl AZITHROMYCIN Derived from Erythromycin by addition of methylated Nitrogen, Its slightly less active against Gram postive bacteria then Erythromycin ergo metabolism, waxella catarrhalis, H. i T of 2-4 days, Do not und ‘against inf caused by Me” STREPTOGRAMINS: Quinupristin, Dalfopristin Binds to $0 s subunit of ribosome > prevent interaction of (RNA | | from complex ‘Also Dec release of completed polypeptide by blocking its extrusion. | © New drugused IV in VRSA and resistant gram + cocci. * Toxicity not known yet.