Antibiotics Flashcards
The 5 main target sites for antibacterial agents:
- cell wall synthesis
- cytoplasmic membrane function
- protein synthesis
- nucleic acid synthesis
- metabolic pathway
Which antibacterial agent has the best selective toxicity?
Antibacterial agent targeting cell wall synthesis because human cells do not have cell wall
Famileis of drugs that inhibit Send wall synthesis
- Beta lactams including monobactams, carbapenem, penicillin and cephalosporins.
- Glycopeptides including vancomycin
- bacitracin
- subactams
Antibiotics inhibiting cell wall synthesis are bactericidal or bacteriostatic?
Bactericidal
What is the target beta lactams?
Penicillin binding proteins
What is beta-lactamase?
An enzyme produced by bacteria that provides multi resistance to beta-lactam antibiotics
Bacteria that beta-lactam can’t act on:
Bacteria that do not have a cell wall like mycoplasma and intracellular bacteria
Inhibitors of beta lactamase:
Clavulanic acid and sulbactam
Mechanism of action of beta-lactams
They will bind to transpeptidase active site of penicillin binding proteins thus inhibiting the formation of cross linking and cell wall synthesis
All penicillin antibiotics are sensitive to the acidity of the stomach except those two:
Amoxicillin and penicillin V
Penicillins that are resistant to beta lactamase:
Nafcillin, oxacillin and methicilin
Penicillin V:
Active against gram-positive bacteria
Sensitive to Beta lactamase
Oxacillin methicillin and nafcillin:
Less active against gram-positive and inactive against gram negative
Resistant to beta lactamase
Ampicillin and piperacillin:
Active against gram positive and gram negative bacteria
Sensitive against beta lactamase
Amoxicillin
Less sensitive to beta lactamase
Taken orally
Better absorbed than ampicillin
Penicillin V
Acts like penicillin G but taken orally
MRSE
Methicillin resistant staphylococcus epidermidis
MRSA
Methicillin resistant staphylococcus aureus
How resistance is acquired by staphylococcus bacteria?
They have a MECA gene which will Produce new penicillin binding proteins that have a lesser affinity to penicillin and at the same time inactivating normal penicillin binding proteins.
ESBL
Extended spectrum beta lactamase
How beta lactamase inactivate penicillin?
By converting the 6-aminopenicilanic acid which is the compound that has the anti-bacterial activity, into 6-aminopenicilloic acid inactive against bacteria but have a property of an hapten
Hapten:
It is a molecule that has lost its capacity to produce disease but has preserved its antigenicity and can stimulate the immune system causing an allergic reaction
manifestations of an allergic reaction due to penicillin;
Skin rash and edema
Clavulanic acid
It’s a suicide inhibitor that has the capacity to inhibit the activity of beta lactamase.
It can’t be administered alone since it has o anti-microbial or antibacterial properties so it should be combined with another antibiotic and the junction with beta lactamase will make this antibiotic more effective.
First generation of cephalosporins
Activity similar to ampicillin
More active against gram-positive and less against gram-negative