Antibiotics a logical approach Flashcards
Gram +ve
Thick peptidoglycan cell wall
Gram -ve
Thin peptidoglycan cell wall
B lactam examples
Penicillin, cephalosporins, vancomycin
B-lactam antibiotic method of action
Inhibit cell wall synthesis
Macrolides and clindamycin
Inhibit 50S subunit + protein synthesis
Aminoglycosides and tetracyclines
Inhibit 30S subunit + protein synthesis
MOA of quinolones
Inhibit DNA gyrase and stop nucleic acid synthesis
MOA of trimethoprim
Inhibit folate synthesis to stop nucleic acid synthesis
MOA of nitrofurantoin
Create free radicals and inhibit nucleic acid synthesis
Penecillin MoA
Inhibit cell wall synthesis by preventing peptidoglycan cross-linkage which weakens wall
Irreversible binding to transpeptidase enzymes in cell wall
B-lactamase MoA
Hydrolyses the B-lactam ring to stop penicillin activity
Clavulanic acid MoA
Re-activates penicillin by inactivating B-lactamase
S/e of penicillin
Rash, nausea, vomiting, diarrhoea
Cephalosporin structure
B-lactam ring fuses with dihydrothiazine ring to produce cephem nucleus
How do cephalosporins work?
Disrupts the integrity of the peptidoglycan cell wall
Why are cephalosporins less susceptible to B-lactamase
Modified B-lactam ring is more stable
Where are cephalosporins excreted?
Liver
MoA vancomycin
Inhibits cell wall synthesis but non B-lactam bactericidal
When will vancomycin be used?
Aerobic and anaerobic gram -ve bacteria inc MRSA
C.diff and endocarditis
MoA macrolides
Inhibits bacterial protein synthesis
Stops translocation movement of ribosomes so it can’t create protein chain
Macrolides example
Erythromycin
S/e macrolides
Nausea, vomiting, diarrhoea
Why are macrocodes dangerous
Interacts with warfarin, simvastatin and carbamazepine
MoA gentamicin
Inhibits protein synthesis by binding to S30 tRNA
Why does gentamicin need to be administered via IV
Large polar molecule
Low protein binding - water soluble
How is gentamicin excreted
urine
side effects gentamicin
Ototoxicity and nephrotoxicity
MoA ciprofloxacin
Blocks DNA replication - circular DNA rings need topoisomerase to unwind two strands to replicate. Fluroquinolones inhibit this process - bacteriostatic
MoA trimethoprim sulfamethoxazole
Inhibits folic acid synthesis in bacteria but huge amount needed to affect human cells
STevens-Johnson side effect
Skin reaction
Metronidazole
Effective against anaerobes, little resistance
Enters bacteria by passive diffusion
Metronidazole MOA
Induces DNA breakage
Where is metronidazole metabolised and excreted?
liver and kidney
What is MRSA
Methicillin resistant staphylococcus aureus