What is a CYP 450 substrate?

Cytochromes P450 (CYPs) are a superfamily of enzymes containing heme as a cofactor that functions as monooxygenases. In mammals, these proteins oxidize steroids, fatty acids, and xenobiotics, and are important for the clearance of various compounds, as well as for hormone synthesis and breakdown.

What drugs are substrates of cytochrome P450?

CYP2C19 has a number of commonly used substrates including the benzodiazepine diazepam, the proton pump inhibitor omeprazole, propanolol and the antidepressive amitriptyline [19]. A number of important abnormal variants of this enzyme exist, one of these has important clinical consequences.

What are CYP3A4 substrates?

Cytochrome P450 enzymes metabolize approximately 60% of prescribed drugs, with CYP3A4 responsible for about half of this metabolism; substrates include acetaminophen, codeine, ciclosporin (cyclosporin), diazepam, and erythromycin. The enzyme also metabolizes some steroids and carcinogens.

What are CYP 450 enzymes?

The superfamily of proteins called cytochrome P450 (CYP) enzymes are involved in the synthesis and metabolism of a range of internal and external cellular components. These enzymes have been identified in many organisms, including animals, plants, bacteria, and even in a few viruses.

What does it mean if a drug is a substrate?

Definitions. substrates are drugs or other substances (xenobiotics) which are metabolized by cytochrome enzymes including 1. pharmacologically active drugs which require metabolism to inactive form for clearance from the body. metabolically activated drugs (prodrugs) which require conversion to active drug.

Is alcohol an inducer?

Alcohol is a substrate of CYP2E1, and depending on the frequency of alcohol intake, it can also be either an inducer or inhibitor of CYP2E1.

What inhibits cyp450?

Cytochrome P450 enzymes can be inhibited or induced by drugs, resulting in clinically significant drug-drug interactions that can cause unanticipated adverse reactions or therapeutic failures. Interactions with warfarin, antidepressants, antiepileptic drugs, and statins often involve the cytochrome P450 enzymes.

What is the ingredient in grapefruit that interacts with medications?

Grapefruit and a few of its close relatives, such as Seville oranges, tangelos, pomelos, and Minneolas, contain a class of chemicals called furanocoumarins. Furanocoumarins disrupt the normal function of CYPs. In fact, studies show that they increase the blood levels of over 85 medications (1).

Why grapefruit is bad for you?

Grapefruit has vitamin C and potassium, nutrients your body needs to work properly. Grapefruit juice and grapefruit can affect the way your medicines work, and that food and drug interaction can be a concern.

What is the function of cytochrome P450 CYP1A2?

Function. CYP1A2 is a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. CYP1A2 localizes to the endoplasmic reticulum and its expression is induced by some polycyclic aromatic…

What are the substrates of CYP1A2 in humans?

CYP1A2 substrates include drugs, industrial chemicals, and environmental toxicants. The enzyme activity is variable in humans due to a combination of genetic polymorphism and environmental factors affecting enzyme expression level and activity.

Are there any sensitive index substrates for CYP2B6?

DDI data were collected based on a search of the University of Washington Metabolism and Transport Drug Interaction Database [Hachad et al. (2010), Hum Genomics, 5 (1):61], and the list of references is available here. (a) We currently do not have sensitive index substrates for CYP2B6.

What causes drug interactions in the cytochrome P450 pathway?

The characterization of drug interactions by metabolic pathways is complex. Just because a medication interacts with one substrate of a particular cytochrome P450 pathway, does not mean it affects all substrates of that isozyme. Genetics, age, nutrition, stress, liver disease, hormones, and other endogenous chemicals also influence drug metabolism.