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By Duy Thai
ANTIBIOTICS 2
• Often, aminoglycosides and beta lactams are used in conjunction because they have a synergistic
effect. Beta lactams can inhibit the production of the cell wall, producing a weakened cell wall which
allows aminoglycosides to enter more easily in higher concentrations. The time to kill the bacteria is
thus reduced
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1997 Clinical pharmacology
By Duy Thai
• Tetracyclines
• e.g. doxycycline minocycline
• Can work on G- and G+ bacteria
• Drug of choice for Rickettsia infections
• Thought to interfere with the energy released by T factors
• Binds to the 30s subunit and prevents the binding of tRNA to the A site
• The effect is reversible, so it acts as a bacteristatic agent.
• Not used in pregnancy because the drug can deposit in teeth of foetus and young children.
• Metronidazole
• Given as an inactive form. It is activated by nitro reductase (present in anaerobic bacteria to
break down oxygen)
Page 2 of 3
1997 Clinical pharmacology
By Duy Thai
• Quinolones
• e.g. Nalidixic acid
• Interferes with gyrase, which is involved in folding of the bacterial chromosome.
• It is secreted unchanged in the urine, and hence it is effective against urinary tract infections.
• By adding an extra FIuoride, you get Ciprofloxacin which can be used to treat more systemic
infections. It has a broader spectrum and is antimycobacterial and pseudomonas.
• Rifampicin
• Inhibits the bacterial for of RNA polymerase
• Drug of choice for treating TB
• Broad spectrum, can be used against G-ve, G+ rods and cocci. Also antiviral
• If used to treat trivial infections, and the person has latent TB, then the low doses may get rid of
the trivial infection but may result in the formation of resistant TB. Therefore, when the TB flares
up again, it will be very difficult to treat.
• Sulphonamides
• Analogue of pABA
• Interferes with the uptake of pABA into the bacteria and also interferes with the first step of
tetrahydrofolate production pABA + pteridine)
• If sulphonamides are added bacterial growth does not stop immediately because the bacteria
have folic acid stores
• Trimethoprim
• Inhibits the enzyme dihydrofolate reductase, which is involved in the synthesis of
tetrahydrofolate.
• Present in both humans and bacteria, although trimethoprim is selective for the bacterial form.
• Methotrexate is selective for the human form, and is used in cancer therapy.
• Often given in conjunction with sulphonamides (cotrimoxazole) - trimethoprim + sulphonamide.
• There is no evidence that these drugs have any real synergistic effect, because by blocking the
first step, there is no real reason to block further steps. However, there may be some molecules
which can leak past the initial blockage. and so this may be the rationale for this.
• Izoniazid
• Bactericidal
• An analogue of pyridoxine
• A prodrug which is converted to its active form by Mycobacterium (therefore it is highly specific
for these bacteria)
• It interferes with pyridoxine metabolism
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