Pharmacology of Antibiotics Flashcards
Antibacterial Chemotherapy Targets
Bacterial cell walls
Bacterial ribosomes
Bacterial folate metabolism
Bacterial DNA gyrases
Antibacterials vs antibiotics
Antibiotics are antibacterials that are produced by an organism to attack other organisms (e.g. penicillin) while antibacterials are more of an umbrella
Beta lactam ring
Feature of penicillins
can be a weakness and be targeted by bacteria since it is unstable
Mode of action of penicillins
Target bacterial cell wall synthesis by binding irreversibly to the transpeptidase which cross links peptidoglycans in the bacterial cell wall
Thus it is only effective against dividing organisms as division requires cell walls synthesis, leading to lysis
Is penicillin bactericidal (also what is bactericidal)
Penicillins are bactericidal
They cause lysis of the bacteria
Beta-lactamase
Enzymes produced by bacteria that cause cleavage in the beta lactam rings
Note that some penicillins are resistant to beta lactamases
Clavulanic acid
An acid that is included with some agents to inhibit the beta lactamases
Immunogenic
Relating to or denoting substances able to produce an immune response.
Penicillin allergies
Penicillin is immunogenic so about 10% of patients treated with it can develop allergies
Cephalosporins
Beta-lactam antibiotics that act in a very similar way to penicillin
Do not prescribe them to patients who are allergic to penicillin as a small percentage of them would also be sensitive to cephalosporins
Glycopeptides
Antibacterials used against very resistant bacteria like MRSA
Inhibit bacterial cell wall synthesis by inhibiting the growth of the peptidoglycan chain
Are glycopeptides bactericidal
Yes (mostly)
Example of a glycopeptide
Vancomycin
Tetracyclines
Antibacterials that inhibit protein synthesis by binding to the 30S subunit of bacterial ribosomes and preventing tRNA from binding at the A(cceptor) site
Actively accumulate in bacterial cells
Have decreased use due to resistance
Bacteriostatic
Prevents the growth of bacteria
Are tetracyclines bacteriostatic
Yes
Macrolides
Antibacterials that prevent the translocation of the 50S subunit of the bacterial ribosome along the mRNA (prevents protein synthesis)
Example of macrolide
Erythromycin
Are macrolides bacteriostatic or bactericidal
They are bacteriostatic
Which antibacterials are used as a common alternative to penicillins in resistant patients
Macrolides
What is the difficulty of using macrolides
They are cytochrome inhibitors associated with a range of drug interactions (e.g. decreasing drug clearance and causing toxicity)
Aminoglycocide
Antibacterials that bind irreversibly to the 30S subunit of bacterial ribosomes leading to mRNA being misread; interferes with protein synthesis
Example of aminoglycoside
Gentamicin
Are aminoglycosides bactericidal or bactereostatic
Bactericidal - used to manage gram-negative bacteria
What antibacterial does aminoglycoside work with
They synergise with penicillins (breaks down cell wall, increasing aminoglycoside uptake)
Otoxicity
When a person develops hearing or balance problems due to a medicine
Difficulties of using aminoglycosides/gentamicin
Ototoxicity/Nephrotoxicity
When used, dose it in a way that there is a sub-therapeutic blood concentration at some points
Quinolones
Inhibitors of DNA gyrase (g -) and topoisomerase IV (g +)
Inhibits the function of DNA by preventing supercoiling (g -) or interfering with the separation of strands on replication (g +)
Example of quinolones
Ciprofloxacin
Are quinolones bactericidal or bactereostatic
Bactericidal
Folic acid
Precursors needed by bacteria for growth and DNA synthesis
Trimethoprim
Analogue folic acid; interferes with folate activity in bacteria (affecting bacterial DNA synthesis) while leaving human DNA alone
Folate antagonist; inhibitor of bacterial dihydrofolate reductase which converts folate to tetrahyrofolate
Usually go-to drug for UTIs
Is trimethoprim bactericidal or bactereostatic
Bacteriostatic
Sulphonamides
Antibacterials that are analogues of p-aminobenzoic acid (PABA) and inhibit bacterial growth by competitively inhibiting the enzyme dihydripteroate synthase involved in folate synthesis from PABA
Basically a competitive inhibitor of an enzyme involved in folate synthesis from PABA
Reduces DNA and RNA precursors that are available
Metronidazole
Antibacterial activated by anaerobic bacteria to cytotoxic products which damages the helical structure of DNA, protein and cell membrane
Used against anaerobic bacteria and protozoa
Commonly used for lower GI bacteria
Why not to drink alcohol on metronidazole
Metronidazole is an inhibitor of aldehyde dehydrogenase (alcohol is converted into the toxic chemical aldehyde which needs to be metabolised)
How to select antibacterials
BNF
Different trusts/areas have slightly different recommendations
Take consideration of allergies and the bacteria’s sensitivity
Pharamacokinetics (IV for rapid effects or oral route occasionally)
Drug Interactions
Tell patient to complete the course of antibacterials
Seriously, this is important >:(
Even if they’re ok before the course is over