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Clinical - Enzymes
Enzyme inhibitors
Enzyme inhibitors act mainly in the
liver to inhibit the action of the cytochrome P450
enzyme. Inhibition of cytochrome P450 cause decreased
metabolism of other drugs. In most cases this causes the
drug to stay in the body for longer in its active form,
and therefore have increased action. When enzyme
inhibitors are taken at the same time as drugs with
narrow therapeutic ranges (warfarin, theophylline,
phenytoin) this significantly increases the risk of
toxicity or adverse effects. The effects of enzyme
inhibitors will be seen approximately 2-3 days.
Important enzyme inhibitors are listed below:
1. Isoniazid
2. Cimetidine
3. Grapefruit juice
3. Dilsulfuram
4. Sulphonamides
5. Quinolones (Erythromycin and Ciprofloxacin)
6. Fluconazole
7. Sodium Valporate
others include, omeprazole, verapamil, itraconazole,
ketoconazole, fluoxetine, allopurinol, metronidazole,
clarithromycin.
Enzyme inducers
Enzyme inducers have the opposite effect from enzyme
inhibitors, they induce enzyme activity in the liver,
therefore more active drugs are being changed into their
inactive form, this causes a decrease in the action of
other medication being taken at the same time. As with
enzyme inducers this is particularly important in drugs
with low a therapeutic range, e.g Rifampicin may
decrease the effectiveness of an anti-epileptic drug,
therefore reducing its action and leading to an increase
risk of convulsions in the patient.
1. Phenytoin
2. Carbamazepine
3. Rifampicin
4. Griseofulvin
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