What is the importance of cytochrome P450 in drug metabolism?

Knowledge of the most important drugs metabolized by cytochrome P450 enzymes, as well as the most potent inhibiting and inducing drugs, can help minimize the possibility of adverse drug reactions and interactions.

Do statins inhibit cytochrome P450?

The data regarding statins as a cause of drug interactions is much more limited although statins are known to inhibit drug metabolizing cytochrome P450 2C9 and 3A4 (CYP3A4) enzymes, and drug transporting multidrug transporter protein 1 (MDR1), breast cancer resistance protein (BCRP), and organic anion-transporting …

What do cytochrome P450 enzymes do?

Cytochrome P450 monooxygenases catalyze the oxidation and metabolism of a large number of xenobiotics and endogenous compounds. CYP450 enzymes evolved as the primary defense against xenobiotics and in this process are also responsible for the bioactivation of drugs and toxicants to more reactive intermediates.

What will happen if a drug is administered simultaneously with an enzyme inhibitor?

Enzyme inhibition occurs when 2 drugs sharing metabolism via the same isozyme compete for the same enzyme receptor site. For most drugs, this can lead to increased serum levels of the unmetabolized entity, leading to a greater potential for toxicity.

Is atorvastatin metabolized by CYP450?

Atorvastatin is a 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor that is mainly metabolized by cytochrome P450 (CYP) 3A4.

What drugs are metabolized by cytochrome P450?

Among the drugs metabolized are sedatives such as midazolam, triazolam and diazepam, the antidepressives amitriptyline and imipramine, the anti-arryhthmics amiodarone, quinidine, propafenone and disopyramide, the antihistamines terfenadine, astemizole and loratidine, calcium channel antagonists such as diltiazem and …

What is P450 in cytochrome P450?

Cytochromes P450 (CYPs) are a superfamily of enzymes containing heme as a cofactor that functions as monooxygenases. The term “P450” is derived from the spectrophotometric peak at the wavelength of the absorption maximum of the enzyme (450 nm) when it is in the reduced state and complexed with carbon monoxide.

How do cytochromes differ from hemoglobin?

Cytochrome c is an electron carrying mitochondrial protein that is extremely efficient in transporting electrons. Unlike myoglobin and hemoglobin proteins, cytochrome c does not have the 6th position of the heme ring available to bind with ligands (Faustman et al., 1996).

What is the role of the cytochrome P450 family in statins?

The cytochrome P450 family consists of major enzymes involved in drug metabolism and bioactivation. This article aims to highlight drug interactions involving statins, as well as provide updated recommendations and approaches regarding the safe and appropriate use of statins in the primary care setting.

What is cytochrome P450?

Cytochrome P450 is a family of isozymes responsible for the biotransformation of several drugs. Drug metabolism via the cytochrome P450 system has emerged as an important determinant in the occurrence of several drug interactions that can result in drug toxicities, reduced pharmacological effect, and adverse drug reactions.

What is the role of P450 in drug-drug interactions?

Abstract. Drug metabolism via the cytochrome P450 system has emerged as an important determinant in the occurrence of several drug-drug interactions. A greater degree of interaction predictability has been achieved through the identification of P450 isozymes and some of the drugs that share them.

Can statins cause rhabdomyolysis?

Cytochrome P450 drug interactions with statin therapy Statins are commonly used in the treatment of hyperlipidaemia. Although the benefits of statins are well-documented, they have the potential to cause myopathy and rhabdomyolysis due to the complex interactions of drugs, comorbidities and genetics.