Contributor: Dr. Augustine Provencio, MD, ABFP TEST Xarelto Pill Box CBD and Xarelto explained. The anticoagulant Xarelto can treat clotting disorders, Xarelto And CBD Oil Hi there! The cytochrome p450 system accounts for 70 to 80 percent of the enzymes involved in drug clearance, making it the most important system for drug metabolism. Both
CBD and Xarelto
CBD and Xarelto explained. The anticoagulant Xarelto can treat clotting disorders, which are diseases of the blood. If you take Xarelto and are interested in CBD for health benefits, speak with your doctor first.
CBD is sometimes taken to treat pain or inflammation and may sound like a safer option than prescription medications. But is it safe to combine the two?
Is it Safe to Mix CBD and Xarelto?
It is not safe to combine CBD and Xarelto because CBD changes the way your body metabolizes certain drugs. Some research has shown that CBD affects metabolic enzymes that break down Xarelto. Discuss your plan with your healthcare team before making any medication changes.
What is Xarelto?
Xarelto (Rivaroxaban) is a prescription anticoagulant. It can treat or prevent the formation of blood clots. If clots form in the cardiovascular system, they can become lodged in critical organs. A clot lodged in the veins of the lungs is called a pulmonary embolism, and one stuck in the veins of the legs or arms is called a deep vein thrombosis.
Xarelto can also prevent blood clots after surgery or in those have atrial fibrillation, an irregular heart rhythm.
Why Could it Be Unsafe to Mix CBD and Xarelto?
CBD changes how your body breaks down drugs, which can lead to higher levels of Xarelto in the bloodstream. When your body breaks down drugs more slowly than usual, it is similar to taking more Xarelto than prescribed.
Cytochrome P450 Enzymes
Enzymes are unique proteins that carry out roles in the cells. They can speed up chemical reactions, or they can help to break down waste products, drugs, or medications.
CBD affects a family of metabolic enzymes called cytochrome P450 (CYP450). There are over 50,000 different kinds of CYP450 enzymes, which all break down different things.
Metabolic enzymes are found in tissues all over your body, but this article will focus on the ones found in your gut and liver. CYP450 enzymes break down about 60% of prescription drugs.
Drug Metabolism Basics
When you take a medication by mouth, it travels to the stomach and then the small intestine. CYP450 enzymes in the small intestine may start breaking down the drug before it enters the bloodstream. Most drugs are mostly intact by the time they enter circulation.
One in the bloodstream, Xarelto is first transported to the liver through the hepatic portal vein. The liver has a high concentration of CYP450 enzymes, which break down a larger portion of Xarelto than those in the small intestine.
After passing through the liver, the remaining medication circulates to the rest of the body. After reaching various parts of your body, Xarelto flows through the blood and into the liver again. This process repeats until the drug is eliminated.
The First Pass Effect and Bioavailability
When you swallow a medication, only a percentage reaches your bloodstream. Some drug is broken down by the liver, and this is called the first-pass effect.
The percentage of drug that reaches the bloodstream after the first-pass effect is called bioavailability. If a drug has a bioavailability of 90%, that means 10% of the drug is lost, and 90% makes it into your systemic bloodstream. Bioavailability varies from drug to drug.
Xarelto has a bioavailability of roughly 60% to 100%, depending on the dose and if you take it with food.
Grapefruit and the First Pass Effect
You may have noticed a warning on some medications that reads, “Avoid eating grapefruit or drinking grapefruit juice while taking this medication.” Drugs carry this warning because grapefruit can affect CYP450 enzymes.
Certain compounds in grapefruit can bind to and shut down CYP450 enzymes. When these enzymes are shut down, the drug stays in the bloodstream for longer than usual. Therefore, grapefruit can increase the level of certain drugs to dangerously high amounts.
The compounds in grapefruit can interact with drugs for a long time. They can permanently shut down certain CYP450 enzymes, sometimes as long as 72 hours.
CBD and the First Pass Effect
Just like grapefruit, CBD changes how fast your body breaks down drugs. A study found that CBD is a powerful inhibitor of the CYP450 enzymes CYP3A4 and CYP3A5. Both of these enzymes play a role in breaking down Xarelto.
When CBD inhibits CYP3A4 and CYP3A5, Xarelto stays in the body for longer. Higher levels of Xarelto can lead to side effects, including higher rates of minor and major bleeding events.
Speak with your doctor or pharmacist before taking CBD, especially if you are taking Xarelto.
Increased Side Effects
If higher than normal amounts of Xarelto are in the body, you could be at a higher risk for unwanted side effects.
Side effects of too much Xarelto may include:
- Bleeding in the abdomen
- Bleeding in the brain
- Bleeding in the lungs
- Hemorrhagic stroke
- Liver damage
- Reduced clotting capabilities
- Stomach upset
- Unexplained bruising
Some of these side effects can be life-threatening or even fatal.
It is probably unsafe to combine CBD and Xarelto. CBD changes how fast the body removes Xarelto and causes higher doses in the bloodstream.
Higher levels of Xarelto can increase the rate of dangerous side effects. Some of the side effects of Xarelto can be serious or even fatal. For this reason, CBD should not be combined with Xarelto without the knowledge, consent, and supervision of your healthcare team.
Xarelto And CBD Oil
The cytochrome p450 system accounts for 70 to 80 percent of the enzymes involved in drug clearance, making it the most important system for drug metabolism. Both THC and CBD are competitive inhibitors of three different enzymes in the cytochrome p450 system, two of which are involved in the metabolism of Xarelto (rivaroxaban). This means that CBD and THC are competing for the same receptors as is Xarelto. So when Xarelto is taken concurrently with CBD and/or THC, Xarelto levels could possibly rise. When Xarelto levels rise excessively, blood clotting may become compromised, leading to signs ranging from frequent bloody noses, all the way on up to a potentially fatal event, such as a hemorrhagic stroke or heart attack.
A case report published in 2009 described a patient who was on coumadin (Warfarin) —the most commonly prescribed blood thinner— therapy for eleven years. He was admitted to the hospital for a severe gastrointestinal bleed when he confessed to consuming much more cannabis than was typical for him; his INR was 10.41 (therapeutic range is usually between 2 and 3); after inpatient treatment, his INR normalized; then, fifteen days after being discharged, he was readmitted with an INR of 11.55; after he quit using cannabis, his INR remained between 1.08 and 4.40 and he suffered no further complications.
Another case report suggested that extremely high doses of CBD can lead to markedly elevated coumadin levels. Enrolled in a clinical trial evaluating CBD as a potential treatment for epilepsy, the test subject was given extremely high doses of CBD. He was first given doses averaging 265mg, which resulted in a slightly elevated coumadin level; at doses averaging 528mg, the coumadin levels were markedly elevated; after reducing the coumadin dose, INR results normalized. Relevantly, very few patients, if any, would ever take as much CBD.
However, as previously mentioned, a highly elevated Xarelto level can lead to serious, even fatal, consequences. And because the effects of cannabis on Xarelto levels have yet to be sufficiently studied, you should discuss the matter with your prescribing physician and monitor your INR results with extra vigilance.
You’re very welcome Colly. CBD and Xarelto would still compete for the same p450 isoenzymes. However, because CBD has low affinity to those isoenzyes, it would take much more than 40mg to affect coagulation. Your anesthesiologist will make sure coagulation isn’t compromised with a blood test prior to surgery. Best of luck!