Dimethyl fumarate


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Chống chỉ định
Hypersensitivity.
Thận trọng
Patient w/ severe GI disorders, serious infection. Severe renal and hepatic impairment. Pregnancy and lactation.
Phản ứng phụ
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.
Thông tin tư vấn bệnh nhân
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).
Tương tác
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.
Tác dụng
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).
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Dimethyl fumarate, CID=637568, https://pubchem.ncbi.nlm.nih.gov/compound/Dimethyl-fumarate (accessed on Jan. 21, 2020)

Bảo quản
Store between 15-30°C. Protect from light.
Phân loại ATC
L04AX07 - dimethyl fumarate ; Belongs to the class of other immunosuppressants.
References
Anon. Dimethyl Fumarate. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/09/2017.

Buckingham R (ed). Fumaric Acid. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/09/2017.

Joint Formulary Committee. Dimethyl Fumarate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/09/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Dimethyl Fumarate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 04/09/2017.

Tecfidera Capsule (Biogen Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/09/2017.

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