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Index inducer or just inducer predictably induce metabolism via a given pathway and are commonly used in prospective clinical drug-drug interaction studies. [2]Strong, moderate, and weak inducers are drugs that decreases the AUC of sensitive index substrates of a given metabolic pathway by ≥80%, ≥50% to <80%, and ≥20% to <50%, respectively.
Index inducer or just inducer predictably induce metabolism via a given pathway and are commonly used in prospective clinical drug-drug interaction studies. [ 4 ] Strong, moderate, and weak inducers are drugs that decreases the AUC of sensitive index substrates of a given metabolic pathway by ≥80%, ≥50% to <80%, and ≥20% to <50% ...
An enzyme inducer is a type of drug that increases the metabolic activity of an enzyme either by binding to the enzyme and activating it, or by increasing the expression of the gene coding for the enzyme. [1] [page needed] It is the opposite of an enzyme repressor.
An example of such a transition state inhibitor is the antiviral drug oseltamivir; this drug mimics the planar nature of the ring oxonium ion in the reaction of the viral enzyme neuraminidase. [ 47 ] However, not all inhibitors are based on the structures of substrates.
Following is a table of selected substrates, inducers and inhibitors of CYP1A2. Inhibitors of CYP1A2 can be classified by their potency, such as: Strong inhibitor being one that causes at least a 5-fold increase in the plasma AUC values of sensitive substrates metabolized through CYP1A2, or more than 80% decrease in clearance thereof. [18]
Following is a table of selected substrates, inducers and inhibitors of CYP2B6.. Inhibitors of CYP2B6 can be classified by their potency, such as: . Strong inhibitor being one that causes at least a 5-fold increase in the plasma AUC values, or more than 80% decrease in clearance.
Adding a competitive inhibitor to an enzymatic reaction increases the K m of the reaction, but the V max remains the same. Sulfa drugs also act as competitive inhibitors. For example, sulfanilamide competitively binds to the enzyme in the dihydropteroate synthase (DHPS) active site by mimicking the substrate para-aminobenzoic acid (PABA). [ 15 ]
The ability of glucose-6-phosphate to bind at different places at the same time makes it a non-competitive inhibitor. [7] The most common mechanism of non-competitive inhibition involves reversible binding of the inhibitor to an allosteric site, but it is possible for the inhibitor to operate via other means including direct binding to the ...