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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.
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.
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.
Methylphenidate, one of the most widely used NDRIs.. A norepinephrine–dopamine reuptake inhibitor (NDRI) is a type of drug that inhibits the reuptake of the monoamine neurotransmitters norepinephrine and dopamine and thereby increases extracellular levels of these neurotransmitters and noradrenergic and dopaminergic neurotransmission. [1]
Nevirapine is an inducer of cytochrome P450 isoenzymes CYP3A4 and CYP2B6. It may reduce levels of several co-administered drugs including the antiretrovirals efavirenz, indinavir, lopinavir, nelfinavir and saquinavir, as well as clarithromycin, ketoconazole, forms of hormonal contraception, and methadone. [25]
Avasimibe is a potent activator of the pregnane X receptor and, consequently, an indirect inducer of CYP3A4 and P-glycoprotein, as well as a potent inhibitor of several cytochrome P450 isoenzymes, including CYP1A2, CYP2C9, and CYP2C19; its spectrum of CYP induction and inhibition is similar to that of rifampicin. [7] [8]
When two drugs affect each other, it is a drug–drug interaction (DDI). The risk of a DDI increases with the number of drugs used. [1] A large share of elderly people regularly use five or more medications or supplements, with a significant risk of side-effects from drug–drug interactions. [2] Drug interactions can be of three kinds: