dimethyl fumarate (dye-meth-il fue-ma-rate ) Tecfidera

 Indications

Treatment of relapsing forms of multiple sclerosis.

Action

Activates nuclear factor (Nrf2) pathway involved in cellular

response to oxidative stress. Therapeutic Effects:

Decreased incidence/severity of relapse with decreased

progression of lesions and disability.

Pharmacokinetics

Absorption: Following oral administration rapidly

converted to active metabolite monomethyl fumarate

(MMF) by enzymes in GI tract, blood, and tissue.

Distribution: Unknown.

Metabolism and Excretion: MMF is metabolized

by the tricarboxylic acid (TCA) cycle. 60% eliminated

via exhalation of CO2. Minor amounts eliminated by renal (16%) and fecal (1%) routes, trace amounts in

urine.

Half-life: MMF—1 hr.

TIME/ACTION PROFILE (effects on disability)

ROUTE ONSET PEAK DURATION

PO 24 wk 60 wk Unk

Contraindications/Precautions

Contraindicated in: Hypersensitivity.

Use Cautiously in: Serious infections (treatment

may be withheld); OB: Use during pregnancy only if potential

benefit justifies potential risk to fetus; Lactation:

Use cautiously if breast feeding; Pedi: Safety and effectiveness

not established.

Adverse Reactions/Side Effects

CNS: PROGRESSIVE MULTIFOCAL LEUKOENCEPHALOPATHY.

GI: HEPATOTOXICITY, abdominal pain, diarrhea, nausea,

dyspepsia,qliver enzymes, vomiting. Derm: flushing,

erythema, pruritus, rash. Hemat: lymphopenia.

Misc: hypersensitivity reactions including ANAPHYLAXIS

and ANGIOEDEMA.

Interactions

Drug-Drug: None noted.

Route/Dosage

PO (Adults): 120 mg twice daily for one week, then

240 mg twice daily.

Availability

Extended-release capsules: 120 mg, 240 mg.