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Metabolism is by enzymes in the liver, and to a lesser extent in the kidneys. Excretion occurs via the kidneys but only a small percentage of the drug appears in the urine in its original form. Therefore, the risk of adverse effects is increased in patients with hepatic or renal disorders. In addition to their action as local anaesthetics, the following actions on other parts of the body are possible.

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An inhibitor of GABA has not been identified, but it has been tentatively called GABA modulin.

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