16. Bactericidal Antibiotics Flashcards
Which are the bactericide antibiotics? (4)
- BETALACTAMS
- AMINOGLYCOSIDES
- QUINOLONES
- GLYCOPEPTIDES
What defines betalactams?
beta lactam ring
What is the therapuetic index of beta lactams?
wide: very safe
What is the toxicity of beta lactams?
low
What are the side effects of beta lactams? (4)
digestive system (most common orally):
- nausea
- vomiting
- ab pain
- dyspepsia
Teratogenicity with beta lactams?
none
MOA of beta lactams? (2)
inhibit bacterial cell wall synthesis:
-inhibit transpeptidase activity of penicilin binding protiends (PBP)
What drugs are betalactams?
- penicillins
- cephalosporins
- monobactams
- carbapenems
- clavulanic acid
What is PBP? (2)
penicilin binding protein
-enz involved in synthesis of bacterial wall
What is the mechanism of action for resistence for bacteria against betalactams? (3)
- INACTIVATION of the ANTIBIOTIC: producing BETA-LACTAMASES to bind to beta- lactams
- REDUCE UPTAKE INTO THE CELL: loss/modification of porins and pumps of influx or active efflux from the cells
- ALTERATION OF THE TARGET ENZYME: they produce enzymes (mutated PBP) with less affinity for beta-lactams
What can you do to a bacteria that starts producing beta lactamase inhibitors?
Prescribe beta lactamase inhibitors so that the antibiotic will work again
ex. clavulanic acid
How are betalactams administered? (2)
orally
parenterally
Do betalactams cross BBB?
yes
Distribution of betalactams?
good/wide distribution
Betalactams cross placenta?
yes but still safe
Betalactam metabolism?
remain active until eliminated
Beta lactam elimination?
renal
Betalactam short term adverse effects?
- hypersensitivity reactions (urticaria, angioedema)
- anaphylactic shock: bronchospasm, severe dyspneoa
- GI intolerance: oral candida, diarrhea, nausea, vomit
Betalactam long term adverse effects?
Less frequent
- Hematologic: fever, eosinophilia, haemolytic anaemia
- Renal toxicity: Renal failure
What is angioedema?
swelling (usually localized) of the subcutaneous tissues due to increased vascular permeability and extravasation of intravascular fluid.
What mediates angioedema? (2)
Mast cell derived mediators (eg, histamine, leukotrienes, prostaglandins)
Bradykinin and complement-derived mediators