STREPTOGRAMINES
Contents
1. 7 Q pharmacocin tique 1 Q pharmacocin tique 2 Q posologie mode d emploi O indications Mod le d endocardite lapin O tol rance Inhibition CYP 4503A4 BE H yperbilirubin mie Rapport s apr s l utilisation chez 2300 patients Rubinstein AC 1999 Topic A 44 37 Utilisation Q D chez l homme Nouvelle mol cule Eliopoulos AAC 2005 49 3034 Inhibition of Protein Synthesis by Antibiotics Growing peptide C Ophardt c 2003 H E oo p aA phenylalanine a i i 1 i Ae TOS Ribosome RNA magenta protein green protein green RNA magenta mEMA red IRMA gray 505 subRibosome grayirR Ai magenta protein 305 subRibosome cyan RNA blue protein 1b is 7 NN IRMA red orange yellow ae NS C Ophardt c 2003 macrolides Uc macrolides G GA UC2. NA in the P site 4 y Anticodon pairs with codon Formation of the correct complex triggers hydrolysis of GTP which alters the conformation of EF Tu EF Tu dissociates leaving behind a correctly inserted aminoacviARNA Et Tu GTP aminoacyl tRN A 1 Aminoacyl tRNA is delivered to the ribosome and GTP is hydrolyzed causing the EP Te GDP complex 10 dissociate 4 Regenerated EE Tu GTP binds another Ami tRNA aminoacyl tRNA mol cule EF Tu GTP complex EE Tu GDP complex 3 The EF Tu EF Ts i 2 The inactive EF Tu GDP pi Vida STE N f complex is recognized by pr r elongation factor EP Ts to dissociate which promotes dissociation of GDP GTP GDP EF Tu ET Ts complex Q D m canisme d action 1 Cocito J AC 1997 39 Suppl 7 13 50 S 0 D m canisme d action 2 Q spectre d activit 1 d apr s E Bergogne B r zin Antibiotiques 2001 3 111 Cam de Tosa m 77 Q spectre d activit 2 d apr s E Bergogne B r zin Antibiotiques 2001 3 111 O r sistances des ent rocoques Hershberger CID 2004 38 92 O D r sistances des staphylocoques Hershberger CID 2004 38 92 Q r sistance staphylocoques ent rocoques Utilisation de virgniamycine chez l animal Cons quences de l utilisation des ATB chez l animal Aarestrup AAC 2001 45 2054 R sistance de E f aecium en Allemagne Werner Microb Drug Resist 2000 6 3
3. S TREPTOGRAMINES GROUPE A GROUPE B Macrolactones cycliques Hexadepsipeptides cycliques polyinsatur s O ulnupristine Dalf opristine a A 70 30 peu soluble 70S ribosome 37 A site Tunnel tRNA with amino acid peptide chain AUS subunit ay TES and TET bind to the 308 subunit preventing premature assembly of the 708 complex 708 initiation complex 2 IF 2 GTP binds to the AUS 3 The 50S subunit then joins gene the AUS initiation complex nding OANA IF 1 and TF 3 are released The 30S complex interacts and the GTP bound 1 1 2 is pica by eee og hydrolyzed to GDP and P the Shine Dalgarno sequence 1F 2 GDP dissociates and the inttiavon codon leaving the 7US initiation complex with IMelARNA 1 r positioned in the P site 308 imitation complex SUS subunit IMEI IRNA Y mRNA y Aminoucyl1RNA is positioned in the A site Following synthesis of the peptide bond the newly formed peplidyltRNA is partly in the A site and partly in the P site Deaminoucylated RNA 2G GDP is ejected Ms z eem Translocation shifts the peptidyl tRNA completely into the P site leaving the A site empty and vjecting the deamino acylated tRNA from the E site Ternary complex AminoacyI RNA The ternary complex enters the A site If the codon and anticodon match EF Tu forms contacts with the ribosome and the peptidyl tR
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