What are examples of enzyme inducers?

What are examples of enzyme inducers?

Enzyme Inducer

• Carbamazepine.
• Anticonvulsant.
• Sodium Valproate.
• Rifampicin.
• Metabolism.
• Enzyme.
• Phenytoin.
• Phenobarbital.

Which drug is microsomal enzyme inhibitor?

Several drugs, including fluconazole, spironolactone, and metronidazole, can inhibit cytochrome P450 enzyme activity. This inhibition reduces the metabolism of potential substrates and secondarily delays their elimination.

Is rifampicin a microsomal enzyme inducer?

These results demonstrate that rifampicin administration for only 6 days leads to the induction of the microsomal mixed function oxidase system in liver.

What is microsomal enzyme induction?

Microsomal enzyme inducing drugs such as phenytoin, phenobarbital and carbamazepine, and also alcohol, influence serum lipid and apoprotein concentrations. The inducers increase the concentrations of hepatic microsomal enzyme and apo A-I mRNA, and also proteins and phospholipids.

What drugs are inducers?

Examples of enzyme inducers include aminoglutethimide, barbiturates, carbamazepine, glutethimide, griseofulvin, phenytoin, primidone, rifabutin, rifampin, and troglitazone. Some drugs, such as ritonavir, may act as either an enzyme inhibitor or an enzyme inducer, depending on the situation.

Does cimetidine induce microsomal enzyme?

Cimetidine: an inhibitor and an inducer of rat liver microsomal cytochrome P-450. Xenobiotica. 1991 Feb;21(2):193-203.

What are microsomal enzymes?

There are several microsomal enzymes, including flavin monooxygenases, cytochrome P450, NADPH cytochrome c reductase, UDP Glucoronosyl transferases (UGT), glutathione-S-transferases, epoxide hydrolases, etc. Cytochrome P450 and NADPH cytochrome c reductase are the two main enzymes in this system.

Is Tegretol an enzyme inducer?

The dose of Tegretol may have to be adjusted. Carbamazepine is a potent inducer of CYP3A4 and other phase I and phase II enzyme systems in the liver, and may therefore reduce plasma concentrations of co-medications mainly metabolized by CYP3A4 by induction of their metabolism.

Is cimetidine an enzyme inducer or inhibitor?

Cimetidine is a potent inhibitor of certain cytochrome P450 (CYP) enzymes, including CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4. The drug appears to primarily inhibit CYP1A2, CYP2D6, and CYP3A4, of which it is described as a moderate inhibitor.

What enzyme does phenobarbital induce?

Pharmacokinetics. Phenobarbital is completely absorbed after oral administration and extensively metabolized by the liver. The average t½,elim is 100 h (range 50–150 h). Phenobarbital is a potent cytochrome P450 enzyme inducer, leading to interactions with other drugs by increasing their clearance.

What is the role of microsomal enzymes?

Inducers of microsomal enzymes stimulate the metabolism or synthesis of several normal body substrates such as steroid hormones, pyridine nucleotides, cytochromes, and bilirubin. Recent studies suggest that inducers of liver microsomal enzymes enhance the hydroxylation of steroids in man.

Microsomal Enzyme Induction. Electron microscopic analysis by Remmer and Merker (1963, 1965) demonstrated that phenobarbital treatment caused proliferation of the hepatic smooth endoplasmic reticulum, which is the intracellular location of the drug metabolizing enzymes. Treatment with phenobarbital increased CYP450 ( Reichert and Remmer,…

What do hepatic microsomal cytochrome P450 (CYP) and Phase 2 enzyme induction data show?

Availability of hepatic microsomal cytochrome P450 (CYP) and phase 2 enzyme induction data can be useful to account for otherwise unexplained mild to moderate elevations in serum enzyme activities, increased liver weight and hepatocellular hypertrophy/hyperplasia, and hepatic and thyroid tumor formation after chronic xenobiotic administration.

Does microsomal enzyme induction in rodents predict tumorgenicity?

Hepatic microsomal enzyme induction in rodents may be predictive of non-genotoxic tumorgenicity in long-term studies in mice and rats.

Does PB induce hepatic microsomal enzymes in the liver?

Hepatic microsomal enzyme induction by PB in the rat was accompanied by significant increase of liver TG content. This occurred whether the animals were sacrificed without fasting, or after an 18-hr fast.