Site and mode of action

o
Inhibition of cell wall synthesis - penicillins, cephalosporins

Prevention of crosslinking of polymers due to interference of

synthesis of peptidoglycan. Most active against gram positive
bacteria. Natural penicillins susceptible to penicilinase which
cleaves the b lactam ring

Semisynthetic penicillins. Affective against gram positive and

gram negative bacteria. Different B lactam rings sensitive to other
types of B lactamase.

B lactams have low toxicity to eucaryotes as they do not

produce peptidoglycan

B lactamase resistance is one of the most common.

Destruction of lactamase ring allows both resistant and non
resistant bacteria to grow as penicillin within serum is decreased

Cephalosporins 2,3 and 4 generation more effective against

gram negatives

Interference with synthesis of peptidoglycan by preventing

elongation of polymer glycopeptides such as vancomycin are
relatively toxic to host. Clinical use in post-operative procedures
o
Inhibition of protein synthesis - chloramphenicol, erythromycin

Interference with protein synthesis by binding ribosomes

preventing attachment of tRNA and therefore arresting translation.
Difference in ribosome structure allows drugs to inhibit activity of
bacterial protein synthesis although some organelles such as
mitochondria also have the 70x ribosome

Selective permeabiltiy is important

Aminoglycosides - groups of amino sugars linked by glycoside

bonds. Affect 30s ribosomal subunit

Tetracycline have a cyclic 4 ring strucuture which prevents

attachment of tRNA. Broad spectrum.

Chloramphenicol affects 50s ribosomal subunit. Adverse

reaction in host

Macrolides possess macrocyclic lactone ring. Erythromycin

narrow spectrum affecting 50S ribosomal subunit. Non permeable
to gram negative bacteria.
o
Inhibition of nucleic acid replication and transcription - Quinolones,
rifampin

Inhibit mRNA synthesis. Effective against mycobacteria

Quinolones affect function of DNA gyrase. Mutase in gyrase

gene raises resistance to quinolones