Antibiotics and Antivirals Flashcards
What is meant by
a) Bacteriostatic
b) Bacteriocidal
a) Inhibits bacterial growth/replication
b) Kills the bacteria
In the gram-stain what colour are organisms that are
a) gram +ve
b) gram -ve
c) Have thick peptidoglycan wall
a) Purple
b) Pink
c) Purple (gram +ve)
What is the mechanism of action of the Beta-lactams e.g. penicillin, cephalosporins, carbapenems
Inhibition of peptidoglycan synthesis by irreversibly binding to the enzyme (penicillin binding proteins) that catalyses the crosslinking of peptidoglycan subunits
Ie prevents cell wall synthesis
What is the mechanism of action of vancomycin?
Disruption of peptidoglycan cross-linkage by binding to peptidoglycan monomers (n-acetylmuramic acid)
What is the mechanism of action of bacitracin?
Disrupts lipid carrier require for glycan transport across the bacterial cell membrane
Which drugs work by altering the cell/plasma membrane, causing depolarisation of the cell and leakage of its contents?
- Polymyxins (B+E)
- Daptomycin
Which drugs act on the 30s ribosome site to prevent protein synthesis and what actions do they inhibit?
Tetracyclines - entry of incoming acetyl tRNA
Aminoglycosides e.g. gentamycin - correct reading of mRNA
Which drugs act on the 50s ribosome site to prevent protein synthesis and what actions do they inhibit?
Macrolides e.g. erythromycin - Translocation
Chloramphenicol - Transpeptidation
Clindamycin - Translocation
What do Quinalones (e.g. Ciprofloxacin) effect?
DNA
They inhibit DNA gyrases or topoisomerases required for supercoiling of DNA
What does Metronidazole effect?
DNA
Cause inhibition of DNA replication, loss of DNA helical structure and fragmentation of existing DNA and mutates bacterial genome
What does Rifampicin effect?
RNA (transcription)
Binds to RNA polymerase
What pathway is a target for the drugs sulphonamides, trimethoprim and dapsone?
Folate synthesis leading to the synthesis of DNA
What is the MOA of sulphonamides in the folic acid pathway?
Prevent PABA being converted to dihydrofolic acid by dihydropterote synthetase - enzyme not active in humans
What is the MOA of trimethoprim?
Inhibits dihydrofolate
What is MRSA treated with?
- Vancomycin
- Teicoplanin
- Linezolid (inhibit protein synthesis)
What are the mechanisms bacteria have adopted to prevent the action of antibiotics (ie resistance)?
- Efflux of antibiotic - reverse transport systems in the membrane e.g. tetracycline transported out
- Enzyme modification
- Enzyme degredation - e.g. penicillinases cleave beta-lactam ring on penicillin
What is the acquired resistance mechanism ‘Vertical gene transfer’?
Spontanous mutation causing resistance genes which are transferred directly to all bacteria progeny during DNA replication
What are the 3 forms of horizontal gene transfer?
1) Conjugation - direct cell to cell contact transferring plasmids
2) Transformation - DNA taken up from external environment
3) Transduction - Bacteriophages transfer DNA
What antibiotics are contraindicated in pts with liver disease?
- Tetracyclines (can cause jaundice, fever and fatty liver)
- Macrolides e.g. erythromycin (bile retention and jaundice)
- Metronidazole (metabolised in liver by p450 so half life and clearance prolonged and adverse reaction)
What is the safest antibiotic to use in pts with liver disease?
Penicillin
What antibiotics are contraindicated in pts with kidney disease?
- Tetracycline
- Reduce dose of amoxicillin and erythromycin
What antibiotics are contraindicated in pts with glandular fever/infectious mononucleosis?
Ampicillin and amoxicillin as they cause rashes
What antibiotics are contraindicated in pts with lymphocytic leukaemia?
Ampicillin and amoxicillin as they cause rashes
What antibiotics are contraindicated in pts with pre-existing diarrhoea?
Clindamycin and co-amoxiclav