What causes flushing with Tecfidera?
40% of people report flushing as a side effect of Tecfidera and although experts aren’t sure how Tecfidera causes flushing they suggest it may be due to one of the pathways affected by Tecfidera called HCAR2. When the metabolite of Tecfidera, MMF binds to HCAR2, it induces prostanoid-forming enzymes in different cell types. These enzymes form prostaglandins which, in addition to other effects, signal capillaries to open, which causes flushing.
The incidence of flushing with Tecfidera can be greatly reduced by:
- Taking Tecfidera with food. Research has shown taking Tecfidera with food reduced the incidence of flushing by about 25%
- Taking a small dose of non-enteric coated aspirin (up to a dose of 325 mg) 30 minutes before taking Tecfidera. Aspirin reduces prostaglandin synthesis which reduces flushing.
Flushing is one of the most common side effects of Tecfidera with symptoms may include a feeling of warmth, redness, itching, and/or a burning sensation. These symptoms generally begin soon after initiating Tecfidera and usually improve or resolve over time. For most patients, symptoms are mild or moderate but less than 1% have serious flushing symptoms that led to hospitalization. 3% discontinue Tecfidera because of flushing.
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How does Tecfidera cause flushing?
Experts are not sure exactly how Tecfidera (dimethyl fumarate) causes flushing but they know it has antioxidant and immunomodulating (affecting the immune system) properties.
The antioxidant potential of Tecfidera appears to be mediated through two different pathways, one being the Nrf2 (Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway, which is activated during oxidative stress. The other pathway involves a receptor for nicotinic acid/niacin and HCAR2.
HCAR2 is thought to be involved in the flushing reaction. When the metabolite of Tecfidera, monomethyl fumarate (MMF) binds to HCAR2, it induces prostanoid forming enzymes in different cell types. These enzymes form prostaglandins which signal capillaries to open, which causes flushing. Taking aspirin reduces prostaglandin synthesis which reduces flushing.
References
- Tecfidera (dimethyl fumarate) 02/2020 Biogen Inc. https://www.drugclasses.com/pro/tecfidera.html
- Phillips JT, Selmaj K, Gold R, et al. Clinical Significance of Gastrointestinal and Flushing Events in Patients with Multiple Sclerosis Treated with Delayed-Release Dimethyl Fumarate. Int J MS Care. 2015;17(5):236-243. doi:10.7224/1537-2073.2014-069
- Prosperini L, Pontecorvo S. Dimethyl fumarate in the management of multiple sclerosis: appropriate patient selection and special considerations. Ther Clin Risk Manag. 2016;12:339-350. Published 2016 Mar 2. doi:10.2147/TCRM.S85099
Read next
Can you drink alcohol while taking Tecfidera?
Although there is no direct interaction between alcohol and Tecfidera (dimethyl fumarate), you should not drink excessive quantities of alcohol while you are taking Tecfidera, because it may increase the risk of side effects such as inflammation of the stomach (gastritis), especially in those with a history of stomach problems. You should avoid drinking alcohol, especially strong spirits, for at least an hour after taking Tecfidera; however, one glass of alcohol, now and then at a different time of day to your Tecfidera dose is considered OK. Continue reading
Gilenya vs Tecfidera. How do they compare?
Gilenya and Tecfidera are both disease-modifying oral medications approved for the treatment of MS. Both are equally effective although Tecfidera is more likely than Gilenya to be discontinued within 24 months. Gilenya is approved to treat adults and children aged 10 and older and Tecfidera is only approved for adults over the age of 18. Common side effects of Gilenya include heart rhythm disturbances, diarrhea, infections, and elevations in liver enzymes and common side effects of Tecfidera include flushing, gastrointestinal disturbances, and infections. Tecfidera is slightly more expensive than Gilenya. Continue reading
How long can you take Tecfidera?
Tecfidera can be taken for as long as it continues to have a clinical benefit and you are not experiencing intolerable or severe side effects. Continue reading
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