Why you should take Xarelto in the evening? (3+ precautions)

In this article, we will discuss the dosing instructions of Xarelto. Why you should take Xarelto in the evening? Additionally, we will talk about the precautionary measures while taking Xarelto.

Why you should take Xarelto in the evening? 

When Xarelto is taken in the evening, it stays in the system for a long time, which reduces the risk of thrombosis (blockage of arteries due to clot) when compared to Xarelto taken in the morning. (1)

Xarelto is usually administered as a single dose in the evening. If your physician has prescribed you a dose of Xarelto twice a day, you can take it in the morning and evening. Xarelto is an anticoagulant that acts by thinning the blood to prevent clot formation in blood vessels. 

Do not alter the course of your treatment without consulting your physician. Sudden discontinuation of Xarelto before completion of the treatment can increase the risk of stroke, blockage in arteries and myocardial infarction. Seek immediate medical help if you notice any unwanted changes, easy bruising, uncontrolled bleeding, altered mental status, etc. 

What does the research suggest? 

A comparison study between the impact of morning and evening dosing of Xarelto by Ziegler et al. found that evening dosing of Xarelto led to prolonged exposure to Xarelto concentration in the system. (1)

The dose of Xarelto ranges from 2.5mg twice a day to 20mg once daily, depending upon your condition. Xarelto is a novel direct anticoagulant that inhibits factor Xa, which prevents coagulation cascade and clot formation. The half-life of Xarelto is 5 to 9 hours, and in some individuals, it can range from 11 to 13 hours. Xarelto can be taken with or without food. (2,3)

A pharmacokinetics-based study about the effect of food and meal timing on Xarelto was analysed. The study compared clinical phase trials and concluded that the meal-time intake did not influence the pharmacokinetic properties of Xarelto. (4)

What are the things you should know before taking Xarelto? 

Xarelto is an anticoagulant that prevents clot formation by thinning the blood. Xarelto decreases the clotting factor in your body, which reduces your body’s ability to form clots. 

In conditions such as stroke, atrial fibrillation, deep venous thrombosis, etc, the risk of artery blockage is high, which can cut the blood supply to a particular part of the body and lead to life-threatening conditions. Hence, anticoagulants/blood thinning agents are prescribed to avoid blockage of arteries. 

When anticoagulants are used, there is a higher chance of bleeding. If the dose of the drug is higher than usual or if you accidentally consume a double dose of the drug, it can increase the risk of bleeding. 

The use of Xarelto can cause easy bruising and excessive bleeding in some cases. If you are planning for any dental surgery or any invasive procedure, make sure you inform the respective physician about your anticoagulant therapy in order to prevent uncontrolled bleeding. It is not recommended to get tattoos, piercings or any procedure which can cause cuts on your skin. 

When not to take Xarelto? 

There are a few conditions and situations where you have to avoid taking Xarelto, such as: 

Allery: If you are allergic to the medication, you may experience swelling, hives, itching, fever, trouble breathing, vomiting, wheezing, congestion, etc. If you experience these side effects, stop taking the drug and seek medical help immediately.

Active pathological bleeding: If you have active bleeding in your body, such as bleeding gums, GI bleeding, open wounds, etc., it is not recommended to take Xarelto.

Hepatic impairment: The role of the liver in metabolising Xarelto is very important. If you have severe liver damage, Xarelto is not recommended. 

Renal impairment: A proper dose adjustment is necessary if you have renal impairment. Xarelto is not recommended if you have end-stage renal disease. 

Valvular disease:  Xarelto is not recommended if you have prosthetic heart valves, rheumatic heart disease, severe mitral stenosis or mechanical valves. 

Patients with an increased risk of bleeding: In conditions such as acquired bleeding disorder, severe arterial hypertension, ulcerative GI disease, vascular retinopathy, etc. 

What to avoid while taking Xarelto? 

Xarelto is primarily metabolised by the enzymes CYP3A4/5 and CYPJ2 and also through P-glycoprotein (P-gp); some foods and herbal medications inhibit these enzymes, leading to an increased concentration of Xarelto in the blood and increase the risk of bleeding. Here are certain foods, fruits and herbal supplements to avoid while taking Xarelto. (2,5)

Foods Action
Oats Inhibits P-gp
Gingko Inhibits CYP (3A4, 1A1, 1A2, 2B6, 2C9, 2E1) and P-gp.
Cinnamon, ginger and turmeric It has antiplatelet activity, enhances anticoagulant properties and increases the risk of bleeding. 
Capsicum, grapefruit Inhibits CYP3A4 and P-gp.
St John’s wort Inhibits CYP450 (1A2, 2C9, 3A4) and P-gp.
Mango  Inhibits CYP450 enzymes and P-gp
Fish oil Has antiplatelet activities. 
Black and long pepper Increases plasma concentration of Xarelto

Unlike warfarin, Xarelto does not interact with vitamin K supplements or foods that contain vitamin K. Hence, it is safe to take multivitamins and food that contains vitamin K. 

Drugs such as antidepressants (sertraline, fluoxetine), NSAIDs (ibuprofen, naproxen), aspirin, etc can interact with Xarelto and can increase or decrease its action. Always consult a physician before taking any medication to avoid the risk of bleeding and other complications. 

In my experience 

As per my knowledge, the duration of the drug in the body increases when Xarelto is administered in the evening, which is beneficial in reducing the risk of clot formation. If you miss a dose of Xarelto, take it as soon as you remember on the same day and avoid taking double doses at a time. 

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References

1.-

Brunner‐Ziegler S, Jilma B, Schörgenhofer C, Winkler F, Jilma‐Stohlawetz P, Koppensteiner R, Quehenberger P, Seger C, Weigel G, Griesmacher A, Brunner M. Comparison between the impact of morning and evening doses of rivaroxaban on the circadian endogenous coagulation rhythm in healthy subjects. Journal of Thrombosis and Haemostasis. 2016 Feb 1;14(2):316-23. Available from: https://pubmed.ncbi.nlm.nih.gov/26644369/  

2.-

Perzborn E, Kubitza D, Misselwitz F. Rivaroxaban. Hämostaseologie. 2007;27(04):282-9. Available from: https://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-0037-1617095  

3.-

Xarelto [package insert].  Leverkusen, Germany: Janssen Pharmaceuticals, Inc. 2011. Available from: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/202439s001lbl.pdf  

4.-

Zhang L, Peters G, Haskell L, Patel P, Nandy P, Moore KT. A cross‐study analysis evaluating the effects of food on the pharmacokinetics of rivaroxaban in clinical studies. The Journal of Clinical Pharmacology. 2017 Dec;57(12):1607-15. Available from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5697651/  

5.-

Grześk G, Rogowicz D, Wołowiec Ł, Ratajczak A, Gilewski W, Chudzińska M, Sinkiewicz A, Banach J. The clinical significance of drug–food interactions of direct oral anticoagulants. International Journal of Molecular Sciences. 2021 Aug 8;22(16):8531. Available from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8395160/