1. Introduction: what cyp enzymes metabolize teriflunomide
Cytochrome P450 (CYP) enzymes are widely distributed in the body, with a greater abundance in the liver than in other tissues. They metabolize drugs and some xenobiotics and link up with neurotransmitters to create various pharmacological effects. This article will discuss the role of CYP enzymes in drug metabolism.
2. What are CYP enzymes?
For years, scientists have been excited about a new class of drugs that interferes with the metabolism of drugs, such as chemotherapy, steroids, and anti-depressants. The hope is that this new class of medications will enable patients to take fewer pills and thus be less dependent on them.
And here’s the rub: these drugs have side effects. What if those side effects are equally problematic? What if those side effects make you feel worse than you used to? What if they interfere with your ability to live a healthy life?
What are cytochrome P450 enzymes?
They are a family of enzymes (enzymes) that detoxify specific classes of chemicals such as alcohol, nicotine, caffeine, and more. Once activated by a particular chemical like an addictive drug or environmental pollutant in our bodies, cytochrome P450 enzymes remove it from the body by converting it into other chemicals, a process called metabolism.
CYP enzymes metabolize drugs like chemotherapy medicines (usually administered orally), blood pressure medications, and many others. CYP enzymes can also metabolize many prescription medications (including antidepressants), over-the-counter medicines, vitamins (including vitamin supplements), herbs, and homeopathic remedies.
So what exactly happens when someone uses drugs like teriflunomide? How does it affect the liver? How does it interact with one’s body chemistry? How does it get into our system in the first place? In this article, I’ll answer these questions and more about how teriflunomide affects CYP enzyme activity in the human body. I will also provide some information about how your body may react to this drug at different times during treatment; so that you can choose whether or not to become concerned about its effect on your life in terms of health.
First off — let’s look at some essential facts about teriflunomide: More than 100 million people worldwide take it yearly for medical reasons. It is often used to treat epilepsy, cancer, HIV/AIDS, depression, rheumatoid arthritis — even for weight loss. One common mechanism by which teriflunomide works is through interfering with CYP enzyme genes called CYP2D6 or ‘CYP2D6*1A2’ genes. These genes regulate how much of various chemical reactions occur within our bodies, both internal reactions (metabolism) that occur inside our cells and external.
3. What does teriflunomide do?
Teriflunomide is an orally administered antibiotic that acts as a selective and irreversible inhibitor of CYP3A enzymes (cytochrome P450), which are answerable for metabolizing multiple essential pills, including most antibiotics.
The metabolism of teriflunomide is highly dependent on the cytochrome p450 system. For example, suppose a patient has a moderate hepatic impairment (as measured by AST/ALT ratio). In that issue, there is a grown risk that CYP3A4 will metabolize teriflunomide to its active drug metabolite, alanine, or inactive metabolite, N-acetyl-beta-alanine (2-deoxyaldol).
4. How does teriflunomide work?
What is teriflunomide, and what does it do?
Teriflunomide is a drug used to treat a variety of different diseases. It is one of the most commonly prescribed medications in the United States and is also marketed under Atrovent, Travaflunomide, or Virlunomide. However, it has been available only since 1987.
The chemical name of teriflunomide is 2-[1-(3-test-butoxy carbonyl-4-hydroxy benzoyl)-2-(hydroxymethyl)-2H-pyrazol-5-yl]-1,1-dihydro quinoxaline sulfonamide dihydrate. It belongs to a class of drugs understood as quinazolines – compounds with at least one nitrogen atom in the ring that can be oxidized with an electrophile (such as oxygen or sulfur) to form a quinoline ring.
Janssen Pharmaceutica initially synthesized Teriflunomide as an agent used to treat hepatitis B and C infections. Later, it was also used to treat cancer (such as melanoma) and other types of kidney disorders. Teriflunomide’s use for these purposes prompted its development into another class of antineoplastic drugs known as cytotoxic antibiotics; these drugs are generally given intravenously or through the skin.
When given intravenously, teriflunomide has a half-life (the time it takes to get half its initial dose back when administered) of about 6 hours.
In 2017, teriflunomide became available in Canada under the generic name Aristocort® [generic name: mesalamine]. In addition, several generic versions have been approved in Europe since late 2014 under the trade name Virlixa™ [generic name: virlupine] and in Japan since January 2015 under the trade name Dynacort™ [generic name: miglustat]. These products are manufactured by Janssen Pharmaceutica GmbH & Co KGaA for use in Germany and China.
5. What are the side effects of teriflunomide?
Teriflunomide, an anti-viral medication, is used to treat HIV/AIDS patients in some parts of the world. It is a powerful drug used to treat HIV and acquired immunodeficiency syndrome (AIDS) since the late 1980s. Teriflunomide stood supported by the U.S. Food and Drug Administration (FDA) for treating this disease in 2002, but its use is not yet widespread. In the United States, it is available only in combination with other medications such as nevirapine or atovaquone prophylaxis for hepatitis B or with azithromycin for tuberculosis treatment.
Teriflunomide has caused severe liver failure in patients who were previously on other medications that contained cytochrome P450 enzymes that metabolize teriflunomide (CYP1A2, CYP2B6, CYP2D6), including drugs such as carbamazepine and amiodarone.
The most common side effects are:
Excessively high blood pressure;
Hyperventilation and dry mouth; and
Weight changes due to reduced appetite.
It may also cause Precipitation of blood, Blood clots; Cardiac arrhythmias; Abnormal bone development or formation, bone marrow suppression; Seizures. In sporadic cases, it may cause Liver damage. Teriflunomide can increase your risk of death from a heart attack or stroke by 53% when taken with medications to lower cholesterol levels because they metabolize teriflunomide differently than how it metabolizes itself (this is called “reverse metabolism”).
However, this risk applies only after you take another medication that lowers your cholesterol level first. Suppose you are already taking a drug that lowers your cholesterol level. In that case, this risk will be even more significant because the chance that you will need another medication to lower your cholesterol level is higher than if you took no medicine when you take teriflunomide.
If you are concerned about these probable side effects, talk with your doctor about whether teriflunomide should be used concomitantly with other drugs for known risks. Learn more about these potential side effects. Discuss any concerns about trifle.
6. Who should take teriflunomide?
Cytochrome P450 enzymes are the body’s central drug-metabolizing system. Cytochrome P450 enzymes are answerable for the metabolism of thousands of other molecules, including drugs, alcohol, and over-the-counter drugs.
Most of these substances are broken down by cytochrome P450 enzymes into their primary metabolites, which have a broad range of results on the body. These metabolites can be excreted from a person’s body in urine, sweat, or feces.
Treatment with teriflunomide is often indicated when there is an abnormality in metabolism caused by one or more of these enzyme deficiencies:
Cytochrome P450 (CYP) 1A2 Cytochrome P450 (CYP) 2D6 Cytochrome P450 (CYP) 3A4
Even if the enzyme deficiency is found to be due to an inherited genetic defect, it is possible that teriflunomide can still be prescribed as it has been shown to work well in patients where other therapy options have failed and where different medications have not worked effectively.
Some people genetically predisposed to having a deficiency in one or several of these enzymes may not respond well to other drugs that control liver function but will respond well to teriflunomide since it contains most liver function problems associated with having deficiencies in some or all of these enzymes.
7. Conclusion: what cyp enzymes metabolize teriflunomide
Cytochrome P450 enzymes are interested in the metabolism of many drugs and chemicals. During the last decade, more than 300 cyp enzymes have been identified. Of these, more than 30 were involved in the metabolism of alprazolam and clozapine. However, few studies have been conducted on the role of cyp enzymes in drug metabolism and its adverse effects.
This review article will discuss the clinical implications of cytochrome P450 enzymes from a pharmacological perspective. We will also provide details about how cyp-enzymes metabolize different drug classes and their action on human physiology.