CYP2C19 catalyzes the metabolism of several drugs, including proton pump inhibitors (PPIs) (e.g., omeprazole, lansoprazole, pantoprazole), antidepressants (e.g., citalopram and amitriptyline), antiplatelet drugs (e.g., clopidogrel), antifungals (e.g., voriconazole), and anticancer compounds (e.g., cyclophosphamide).
Who is a CYP2C19 poor metabolizer?
Individuals who carry 2 non-functional copies of the CYP2C19 gene are classified as CYP2C19 poor metabolizers. They have no enzyme activity and cannot activate clopidogrel via the CYP2C19 pathway, which means the drug will have no effect.
What is a poor drug metabolizer?
Poor metabolizer: Patients who are poor metabolizers experience a very slow breakdown of medications, making side effects more pronounced. That means standard doses of certain medications may not work as intended.
What drugs are metabolized by CYP2D6?
The CYP2D6 enzyme catalyses the metabolism of a large number of clinically important drugs including antidepressants, neuroleptics, some antiarrhythmics, lipophilic β-adrenoceptor blockers and opioids.
What does it mean if you are a rapid metabolizer?
Rapid or Ultrarapid Metabolizers. These enzymes are very active, often breaking down drugs before they can have any effect. If you metabolize a drug in this way, you may require a higher dose in order for the drug to work properly.
Why do I metabolize drugs so slow?
Because of their genetic makeup, some people process (metabolize) drugs slowly. As a result, a drug may accumulate in the body, causing toxicity. Other people metabolize drugs so quickly that after they take a usual dose, drug levels in the blood never become high enough for the drug to be effective.
How common is poor metabolizer?
Poor Metabolizer (PM) – This means there are two copies of low or no activity genes. This results in very little to no CYP2C19 activity. About 2 out of 100 people have this gene status.
What happens when you can’t metabolize a drug?
Patients who do not metabolize the drug well can be switched to a higher dose or a new antiplatelet drug. However, the majority of clopidogrel users do not need to change their current prescription. Antiplatelet medicines plus aspirin have been shown to achieve excellent outcomes in the vast majority of patients.
What is a normal metabolizer?
Normal Metabolizer (NM) – This means there are two copies of a normal activity CYP2C19 gene. This results in normal CYP2C19 activity. About 4 out of 10 people have this gene status.
Does a FAst metabolism affect medication?
If your body metabolizes a drug too quickly, you may not get any benefit from the prescribed dose. Your dose may need to be increased to reach a therapeutic effect.
What inhibits CYP2D6?
Selective serotonin reuptake inhibitors inhibit CYP2D6 to varying degrees . Paroxetine and fluoxetine are the strongest inhibitors, with paroxetine irreversibly inhibiting CYP2D6 activity, whereas fluvoxamine and citalopram are weaker inhibitors.
What foods inhibit CYP2D6?
Considerable evidence from both in vitro and animal studies suggests that CYP2D6 activity can be inhibited by goldenseal [59, 60], milk thistle [61, 62], kava kava [59, 63-65], Echinacea , and St. John’s wort [59, 66-68].
What is the CYP2D6 enzyme?
Cytochrome P450 2D6 (CYP2D6) is an enzyme that in humans is encoded by the CYP2D6 gene. CYP2D6 is primarily expressed in the liver. It is also highly expressed in areas of the central nervous system, including the substantia nigra.
What does it mean to be a CYP2C19 rapid MEtabolizer?
Ultrarapid Metabolizer (UM) – This means there are two copies of a CYP2C19 gene with increased activity. This results in very high CYP2C19 activity. About 5 out of 100 people have this gene status. Certain drugs should be used with caution and patients may need to have their doses of some medications adjusted.
How does CYP2C19 affect metabolism?
Most often, changes in the CYP2C19 gene lead to impaired metabolism of these drugs, which reduces their effectiveness. One change in the CYP2C19 gene (known as CYP2C19*17) increases the enzyme’s ability to metabolize drugs.
What does CYP2D6 do in the human body?
Cytochrome P450 2D6 (CYP2D6) is part of the cytochrome P450 family of proteins in the body. It is responsible for breaking down many medicines that are commonly used.