Dimethyl fumarate


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Relapsing-remitting multiple sclerosis Initial: 120 mg bid. Increase dose to 240 mg bid after 7 days. Adjust dose according to tolerance. Moderate to severe plaque psoriasis Wk 1: 30 mg once daily. Wk 2: 30 mg bid. Wk 3: 30 mg tid. Wk 4: 120 mg once daily. Wk 5: 120 mg bid. Wk 6: 120 mg tid. Wk 7: 120 mg in the morning and at midday, and 240 mg in the evening. Wk 8: 240 mg in the morning, 120 mg at midday, 240 mg in the evening. Wk 9 onwards: 240 mg tid. Dosage adjustments may be required based on tolerance. Max: 720 mg/day.
Dosage Details
Oral
Relapsing-remitting multiple sclerosis
Adult: Initially, 120 mg bid, increase to 240 mg bid after 7 days. Adjust dose according to tolerance.

Oral
Plaque psoriasis
Adult: Moderate to severe cases: Wk 1: 30 mg once daily (evening). Wk 2: 30 mg bid (morning and evening). Wk 3: 30 mg tid (morning, midday, evening). Wk 4: 120 mg once daily (evening). Wk 5: 120 mg bid (morning and evening). Wk 6: 120 mg tid (morning, midday, evening). Wk 7: 120 mg in the morning and at midday, and 240 mg (2 tab of 120 mg) in the evening. Wk 8: 240 mg in the morning, 120 mg at midday, and 240 mg in the evening. Wk 9 onwards: 240 mg in the morning, at midday, and in the evening. Dosage adjustments may be required based on tolerance. Max: 720 mg daily.
Renal Impairment
Severe: Not recommended.
Hepatic Impairment
Severe: Not recommended.
Contraindications
Hypersensitivity.
Special Precautions
Patient w/ severe GI disorders, serious infection. Severe renal and hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Anaphylaxis, angioedema, leucopenia, lymphopenia, opportunistic infections, hepatic injury, flushing, GI disturbances (e.g. diarrhoea, abdominal distension, abdominal pain, nausea, vomiting, dyspepsia, constipation, abdominal discomfort, flatulence), proteinuria, ketonuria, albuminuria.
Nervous: Headache, paraesthesia, fatigue, asthenia.
GI: Decreased appetite.
Hepatic: Increased hepatic enzymes.
Endocrine: Hot flush.
Haematologic: Eosinophilia, leukocytosis.
Dermatologic: Erythema, burning sensation, pruritus, rash.
Potentially Fatal: Progressive multifocal leukoencephalopathy.
Patient Counseling Information
This drug may cause fatigue or dizziness, if affected, do not drive or operate machinery.
MonitoringParameters
Monitor CBC including lymphocytes, renal and hepatic function prior to initiation and periodically during treatment; signs or symptoms of hypersensitivity, infections (e.g. progressive multifocal encephalopathy).
Drug Interactions
Increased renal adverse reactions w/ nephrotoxic agents (e.g. methotrexate, ciclosporin, aminoglycosides, lithium). Increased risk of infection w/ live vaccine.
Food Interaction
Increased tolerance to flushing and GI adverse reactions w/ food intake. Increased frequency of GI adverse reactions w/ alcoholic beverages.
Action
Description: Dimethyl fumarate (DMF) is a fumaric acid derivative w/ anti-inflammatory and immunomodulating effects. It decreases immune cell activation and subsequent release of pro-inflammatory cytokines. In patients w/ multiple sclerosis, DMF activates the nuclear factor (erythroid-derived 2)-like 2 (Nrf2) transcriptional pathway thereby upregulating Nrf2-dependent antioxidant genes which may protect various cells and tissues, including some in the CNS, from oxidative stress. DMF also interacts w/ the intracellular reduced glutathione of cells involved in the pathogenesis of psoriasis.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: 2-2.5 hr.
Distribution: Volume of distribution: 53-73 L [monomethyl fumarate (MMF)]. Plasma protein binding: 27-45% (MMF).
Metabolism: Rapidly metabolised in the GI tract, blood and tissues via presystemic hydrolysis by esterases into MMF (active metabolite). MMF is further metabolised via oxidation in the tricarboxylic acid cycle.
Excretion: Mainly via exhalation of CO2 (approx 60%); urine (16%); faeces (1%). Terminal elimination half-life: Approx 1 hr (MMF).
Chemical Structure

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Storage
Store between 15-30°C. Protect from light.
ATC Classification
L04AX07 - dimethyl fumarate ; Belongs to the class of other immunosuppressants.
Disclaimer: This information is independently developed by MIMS based on Dimethyl fumarate from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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