Drug information of Dimethyl Fumarate
Dimethyl fumarate is used to treat relapsing-remitting forms of multiple sclerosis (MS; a condition in which the nerves do not function properly and people may experience weakness, numbness, loss of muscle coordination, and problems with vision, speech, and bladder control).
Mechanism of effect
Dimethyl fumarate is in a class of medications called Nrf2 activators. It may work by decreasing inflammation and preventing nerve damage that may cause symptoms of multiple sclerosis.
Dimethyl fumarate is a fumaric acid derivative . Exactly how it works to treat MS is not known.
• Absorption: Peak Plasma Time: 2-2.5 hr (MMF)
• Distribution: Protein Bound: 27-45% (MMF), Vd: 53-73 L
• Metabolism: Metabolized rapidly by presystemic hydrolysis by esterases in GI tract, blood, and tissues (before it reaches systemic circulation) and is converted to its active metabolite, monomethylfumarate (MMF)
• Further metabolism of MMF occurs via tricarboxylic acid (TCA) cycle with no involvement of CYP450 system
• Metabolites: MMF, fumaric acid, citric acid, and glucose
• Elimination: Excretion: 60% by exhalation of CO2; 16% renal; 1% feces
Drug indicationspsoriasis treatment , Control multiple sclerosis
- Initial dose: 120 mg orally twice a day for 7 days
- Maintenance dose: 240 mg orally twice a day
Drug contraindicationshypersensitivity to drug or its components.
Side effectsnausea , vomiting , flushing , Diarrhea , stomach pain , indigestion
InteractionsDuloxetine , Cetirizine , Levothyroxine , Lisinopril , Metoprolol , Vitamin D3 , Multi Prenatal , Mirabegron , Lactobacillus Acidophilus , Dalfampridine , Magnesium aspartate , Zoster Vaccines , Yellow fever vaccine , Meningococcal conjugate vaccine
• Dimethyl fumarate may lower the ability of your body to fight infection. Avoid contact with people who have colds or infections. Tell your doctor if you notice signs of infection like fever, sore throat, rash, or chills.
• A very bad brain problem called progressive multifocal leukoencephalopathy (PML) has happened with dimethyl fumarate . It may cause disability or death. Tell your doctor right away if you have symptoms like confusion, memory problems, depression, change in the way you act, one-sided weakness, trouble speaking or thinking, balance changes, or vision changes.
Points of recommendation
• Swallow capsule whole and intact; do not chew, crush, or sprinkle on food
• May take with or without food
• Administration with food may reduce incidence of flushing by ~25%
• Dimethyl fumarate may cause flushing. Taking dimethyl fumarate with food or taking aspirin 30 minutes before dimethyl fumarate may decrease how often flushing happens.
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