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Samenvatting alle antibiotica

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Alle antibiotica samengevat: eigenschappen, spectrum, werkingsmechanisme, type, ...

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  • July 31, 2022
  • 7
  • 2021/2022
  • Summary
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Antibioticum Werking Eigenschappen
Inhibitoren PG synthese
Fosfomycine Structuur ~PEP - Breed spectrum (klein)
=> inhibitie UDP-NAG EP transferase - Goede penetratie
=> inhibitie PG synthese (bactericide) - Resistentie:
+ ringspanning => irriversibele inhibitie mutatie transporter of doelwit
- Niet toxisch
D-cycloserine Structuur ~Ala - Breed spectrum (kleinste AB)
= oxamycine => inhibitie racemase & D-ala-D-ala ligase - Lage therapeuthische index (CZS)
=> inhibitie PG synthese (bactericide)  bij multiresistente tuberculose
Bactiracine Bindt fosfaat van Udc-P-P - Eng spectrum (groot): G+
=> inhibitie defosforylase - Niet vaak resistentie
=> inhibitie PG synthese (bactericide) - Synergie met aminoglycoside &
polymycines => G- OM gaten
- Oraal gebruik, GEEN absorptie
 bij pseudomembraneuze colitis
- Niet IV => toxiciteit
Vancomycine Bindt EC de eindstandige D-ala-D-ala - Eng spectrum (groot): G+
= Glycopeptide AB (via 5 H-bruggen)  MRSA !!
=> inhibitie transglycosylase & transpeptidase  bij C. difficile (pseudom. colitis)
=> inhibitie PG synthese (bactericide)  bij beta-lactam allergie vr G+
- ! Resistentie:
door wijziging PG (lactaat)
- GEEN absorptie darm
 enkel oraal bij colitis
- IV toediening, goede distributie
- Slechte penetratie BBB
- Red-Man Syndroom
b-lactam AB: Binding PBP (transpeptidase/ carboxypeptidase)
=> inhibitie PG synthese (bactericide)
- Concentratie-onafhankelijke afdoding (wel boven MIC) & tijdsafhankelijk
- Absoptie: vaak afgebroken door lage pH => variabele orale inname; voedsel => opname ↓
- Brede distributie + kan door BBB !!!
- Eliminatie door nier
- Hypersensiviteit/ allergie; GI neveneffecten; interstitiële Nephritis

Penicillines Structuur ~Ala-Ala - Korte eliminatie halfwaardetijd
(b-lactam) => inhibitie transpeptidase (PBP) - Resistentie:
+ ringspanning => irreversibele inhibitie beta-lactamase productie;
=> inhibitie PG synthese mutatie of overproductie PBP,
∆permeabiliteit OM
- Eventueel in combi
b-lactamase inhibitoren
(clavulaanzuur & sulbactam)
Klassen penicillines:
- Natuurlijke: eng, gevoelig
- Penicillase-resistente: eng (G+)
- Aminopen.: breed, gevoelig
- Carboxypen.: breder, gevoelig
 bij pseudomonas

, 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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