For a few medications, the parent drug has low therapeutic activity until it is biotransformed by a CYP enzyme. In such cases, the substrate is called a prodrug, and the biotransformation process can be referred to as bioactivation.
For most medications (active parent drug to inactive metabolite) inDuction decreases (D for Down) effect of the drug and inHibition (H for High) amplifies the therapeutic effect and/or side effects.
With prodrugs, the opposite effect is observed clinically. Induction increases and inhibition decreases the medication’s effect(s).
Don’t let prodrugs confuse you. InHibitors increase and InDucers decrease the levels of substrate regardless of whether the parent drug is pharmacologically active.
PRODRUGS
Phase I metabolism typically involves biotransformation of an active drug to an inactive (or less active) chemical.
