, Cefalosporines Binding PBP (transpeptidase/ carboxypeptidase) Resistent tgn beta-lactamase
(b-lactam) => inhibitie PG synthese (bactericide) - Lage microbiële activiteit
=> chemische modificatie
=> 4 generaties
Carbapenems Binding PBP (transpeptidase/ carboxypeptidase) BREEDSTE SPECTRUM
(b-lactam) => inhibitie PG synthese (bactericide) bij multiresistente pseudomonas
Monobactam Binding PBP3 van G- aeroben - Eng spectrum: G- aeroben
= Aztreonam => inhibitie PG synthese (bactericide) <> G+ & anaeroben
(b-lactam) bij pseudomonas
Verstoring buitenste membraan G-
Polymyxines Hydrofobe staart gaat in OM - Eng spectrum: aerobe G- bacillen
=> positief geladen kop: bij pseudomonas
competitie met bivalente kationen - Geen absorptie, trage excretie
=> destabilisatie/ verstoring OM => lysis G- slechte distributie (bindt eiwitten)
bacterie => lokaal: in zalven bij huidinfectie,
oraal voor diarree
- Resistentie zeldzaam
- Synergie met penicilline, macroliden, …
=> inhibitie G- & G+
Inhibitoren replicatie en transcriptie
Quinolonen Inhibitor replicatie: - Concentratie-afh. bactericide
& Fluoroquinolonen Bindt in actieve site DNA gyrase (G-) & - Breed spectrum (FQ), atypische bact.
(topoisomerase (G+)) bij mycoplasma, Chlamidia,
=> geen herstel ds breuken DNA pseudomonas, S.aureus,
=> lysis bacterie (bactericide) !! mycobacterium tuberculosis
- Snelle resistentie:
mutatie gyrase, #gyrase DAALT,
effluxpompen, opname ↓,
qnr determinanten
- Goede absorptie, distributie, niet dr BBB,
eliminatie dr nier & lever
- Fototoxiciteit; GI neveneffecten
Rifampicine Inhibitor transcriptie: - Breed spectrum
Bindt beta-subunit RNA polymerase bij mycobacterium tuberculosis
=> inhibitie initiatie TXN bij fungi/ gisten
- Rode kleur; affiniteit plastic
- Rifabutine & rifapentine (varianten)
=> tragere excretie => # toediening ↓
- SNELLE resistentie (mutatie RNA pol)
=> combinatie therapie !!
- Goede absorptie, distribie, kan dr BBB
- Eliminatie: lever & feces
- Neveneffect: inductie oxidase
=> interactie andere medicatie
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