Question

36. If a biologically active drug in a tablet formulation after being swallowed is metabolized to an inactive metabolite. What are the 2 alternatives to minimizing metabolic inactivation ________ & _________?

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Answer 1

The liver is the primary site for drug metabolism. In liver detoxification of xenobiotics which are foreign compunds to our body, metabolic pathways modify their chemical structure via xenobiotics metabolism. The liver enzymes convert prodrugs to active drugs or convert active drugs to inactive forms. This conversion is regulated by drug metabolizing mechanism of liver by a specific group of Cytochrome P-450 enzymes. In some cases, the active drug when swallowed is metabolized to an inactive metabolite, where the addition of drug essentially induces the rate of enzyme action and thus it able to break the drug and decrease its action. Contrary, enzyme inhibition also may result with the intake of drug resulting in increase activity.

So the metabolic inactivation of the drug can be minimized when sublingual and buccal administration of drug is taken. On administering like this, as an alternative pathway, the drugs are directly absorbed into the blood through the tissue and further these drugs do not enter the digestive system, so are not metabolized by liver. Hence, two alternatives to minimize metabolic inactivation are Buccal and Sublingual forms of drug intake.