How does CYP1A2 metabolize caffeine?

The liver enzyme cytochrome P450 1A2 (CYP1A2) is responsible for 90% of caffeine metabolism, while caffeine exerts many of its effects via antagonist binding to adenosine A2a receptors (ADORA2A).

Is caffeine a CYP1A2 inducer or inhibitor?

Results from rat studies have shown that caffeine is an inducer of CYP1A2, the enzyme responsible for caffeine’s metabolism.

What is CYP1A2 ultrarapid metabolizer?

CYP1A2 metabolizes some pro-carcinogens from tobacco smoke into carcinogens. It also helps to turn aflatoxins (molds found in grains) into active compounds involved in liver cancer. Once CYP1A2 metabolizes these carcinogens, the body must eliminate them.

What the CYP1A2 enzyme is why it is important and what it does in the body?

CYP1A2 is an important detox enzyme that breaks down toxic chemicals, drugs, hormones, and other products of metabolism in order to eliminate them from your body. It’s found mainly in the liver [1, 2]. This enzyme is one of the cytochrome P450 monooxygenases (CYPs).

What are CYP1A2 inhibitors?

Strong inhibitor of CYP1A2 and CYP2C19, and moderate inhibitor of CYP2D6 and CYP3A….

	CYP1A2
Strong inhibitors	ciprofloxacin, enoxacin, fluvoxamine(a)
Moderate inhibitors	methoxsalen, mexiletine ,oral contraceptives
Weak inhibitors	acyclovir, allopurinol, cimetidine, peginterferon alpha-2a, piperine, zileuton

What is CYP1A2 and caffeine?

In humans, CYP1A2, encoded by the CYP1A2 gene, is responsible for ∼13% of the cytochrome P450 activity of the liver (3). CYP1A2 is the main enzyme responsible for the metabolism of caffeine (1,3,7-trimethylxanthine, 137X), a purine alkaloid that occurs naturally in coffee beans.

What does it mean to be a fast metabolizer of caffeine?

People who inherit two copies of the “fast” variant – one from each parent – are generally referred to as fast metabolizers. Their bodies metabolize caffeine about four times more quickly than people who inherit one or more copies of the slow variant of the gene.

What are strong CYP1A2 inhibitors?

A selective serotonin-reuptake inhibitor used to treat obsessive-compulsive disorder. An antiandrogen used in the treatment of prostate cancer.

What drugs are CYP1A2 substrates?

Typical CYP1A2 substrates generally contain planar ring that can fit the narrow and planar active site of the enzyme, such as propranolol, clozapine, guanabenz, flutamide, imatinib, thalidomide, carbamazepine, lidocaine, theophylline, tacrine, tizanidine, zolpidem, riluzole, zileuton, and leflunomide.

How do you know if you’re a fast caffeine metabolizer?

Slow metabolizers can get jittery and stay wired up to nine hours after drinking caffeine, according to Precision Nutrition. Meanwhile, fast metabolizers simply feel more energetic and alert for a couple hours.

What gene metabolizes caffeine?

CYP1A2
CYP1A2 produces a liver enzyme that metabolizes roughly 95 percent of all ingested caffeine. AHR controls how much of that enzyme you produce. Together, these genes control how much caffeine circulates in your bloodstream, and for how long.

What are the metabolites of caffeine?

The primary metabolites of caffeine, paraxanthine, theobromine, and theophylline are biologically active.

What is a CYP1A2 inhibitor?

Like many of other CYPs, CYP1A2 is subject to induction and inhibition by a number of compounds. In particular, several therapeutic drugs including antofloxacin, carbamazepine, dihydralazine, furafylline, isoniazid, rofecoxib, clorgyline, thiabendazole, and zileuton are mechanism-based inhibitors of CYP1A2.

What is CYP1A2 gene mutation?

CYP1A2 (Cytochrome P450 Family 1 Subfamily A Member 2) is a Protein Coding gene. Diseases associated with CYP1A2 include Porphyria Cutanea Tarda and Acetaminophen Metabolism. Among its related pathways are 2-Naphthylamine and 2-Nitronaphtalene metabolism and Clomipramine Pathway, Pharmacokinetics.

What is the CYP1A2 * 1F?

The CYP1A2*1F polymorphism (rs762551) is a common C to A transition in intron 1 of the CYP1A2 gene at position 734 downstream of the first transcribed nucleotide and termed C-163A according to the human cytochrome P450 (CYP) Allele Nomenclature Committee with the A allele being the highly inducible allele.

Are the effects of caffeine ingestion different for different CYP1A2 genotypes?

It might be that the effects of caffeine ingestion are similar between different CYP1A2 genotypes, at least for the performance tests used in the present study. The results reported herein are generally in line with the current body of evidence.

What is the speed of caffeine metabolism affected by?

The speed of caffeine metabolism is affected by a single nucleotide polymorphism, rs762551, within this gene [8].

How many CYP1A2 polymorphisms are there?

As of 2010, over 40 haplotypes have been identified, affecting the expression of the gene and its enzyme activity. The wild type (or the most common variant) CYP1A2 polymorphism is CYP1A2*1A. The major allele variant is *1F. The *1F variant is well-studied, but is not the only gene that affects caffeine metabolism.

What enzyme converts caffeine into paraxanthine?

In the liver, the cytochrome P450 oxidase enzyme system and specifically CYP1A2 metabolizes caffeine into paraxanthine to increase lipolysis and increase free fatty acids and glycerol levels in the blood, theobromine to dilate blood vessels and increase urine volume and theophylline which relaxes bronchi smooth muscles.