Dimethylfumarat

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H312：Gesundheitsschädlich bei Hautkontakt.

  H315：Verursacht Hautreizungen.

  H317：Kann allergische Hautreaktionen verursachen.

  H335：Kann die Atemwege reizen.

  H411：Giftig für Wasserorganismen, mit langfristiger Wirkung.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

  P264：Nach Gebrauch gründlich waschen.

  P264：Nach Gebrauch gründlich waschen.

  P271：Nur im Freien oder in gut belüfteten Räumen verwenden.

  P273：Freisetzung in die Umwelt vermeiden.

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

Dimethyl fumarate Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R21:Gesundheitsschädlich bei Berührung mit der Haut.
  R38:Reizt die Haut.
  R41:Gefahr ernster Augenschäden.
  R43:Sensibilisierung durch Hautkontakt möglich.
  R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.

• S-Sätze Betriebsanweisung:

  S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
  S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.

• Aussehen Eigenschaften

  C6H8O4; Dimethylfumarat. Farblose Kristalle ohne Geruch.

• Gefahren für Mensch und Umwelt

  Gesundheitsschädlich bei Berührung mit der Haut. Reizt die Atmungsorgane, Augen und die Haut.
  Resorption führt zu Übelkeit und Erbrechen, Blutbildveränderungen, Nierenschäden und Schwächung des Immunsystems.
  LD₅₀ (oral, Ratte): 2240 mg/kg

• Schutzmaßnahmen und Verhaltensregeln

  Geeignete Schutzhandschuhe als kurzzeitiger Staubschutz.

• Verhalten im Gefahrfall

  Vorsichtig trocken aufnehmen. Der Entsorgung zuführen.
  Kohlendioxid, Schaum, Pulver.
  Brennbar. Im Brandfall Entstehung gefährlicher Dämpfe möglich.

• Erste Hilfe

  Nach Hautkontakt: Mit reichlich Wasser abwaschen. Abtupfen mit Polyethylenglycol 400.
  Nach Augenkontakt: Mit reichlich Wasser bei geöffnetem Lidspalt mindestens 10 Minuten ausspülen. Sofort Augenarzt hinzuziehen.
  Nach Einatmen: Frischluft.
  Nach Verschlucken: Reichlich Wasser trinken lassen. Erbrechen auslösen. Arzt hinzuziehen.
  Nach Kleidungskontakt: Kontaminierte Kleidung entfernen.
  Ersthelfer: siehe gesonderten Anschlag

• Sachgerechte Entsorgung

  Als feste Laborchemikalienabfälle.

• Beschreibung

  In March 2013, the US FDA approved dimethyl fumarate for the treatment of relapsing forms of multiple sclerosis (MS). Dimethyl fumarate is the newest oral therapeutic for MS. While its mechanism is not completely understood, dimethyl fumarate increases anti-inflammatory cytokines (IL-10, IL-4, and IL-6), decreases proinflammatory cytokines (IL-1β, IL-6, and TNF-α), and activates the Nrf2 pathway to protect neuronal cells. Nrf2 is activated by covalent bond-forming electrophiles such as dimethyl fumarate, a Michael acceptor. Dimethyl fumarate has been used for the treatment of psoriasis in Europe since 1994 and has a favorable long-term safety profile. An exploratory study in patients with relapsing remitting MS showed significant reductions in MS lesions after 18 weeks of treatment with 720 mg/day of dimethyl fumarate. Evaluation of dimethyl fumarate in a mouse experimental autoimmune encephalomyelitis model of MS resulted in reduced spinal cord macrophage inflammation. Dimethyl fumarate is obtained in high purity by esterification of fumaric acid with methanol and catalytic sulfuric acid.

• Chemische Eigenschaften

  fine white crystalline powder

• Originator

  Biogen Idec (United States)

• Verwenden

  Dimethyl fumarate acts as an immunomodulator. It is also used in cycloaddition reactions involving ylides, benzenes and amino acids. It is added to food grains,tobacco,leather and preservation. Clothing

• Definition

  ChEBI: Dimethyl fumarate is an enoate ester resulting from the formal condensation of both carboxy groups of fumaric acid with methanol. Used for treatment of adults with relapsing forms of multiple sclerosis. It has a role as an immunomodulator and an antipsoriatic. It is an enoate ester, a methyl ester and a diester. It is functionally related to a methanol and a fumaric acid.

• Trademarks

  Tecfidera

• Synthesis Reference(s)

  Synthetic Communications, 21, p. 223, 1991 DOI: 10.1080/00397919108020815
  The Journal of Organic Chemistry, 55, p. 329, 1990 DOI: 10.1021/jo00288a056

• Allgemeine Beschreibung

  Dimethyl fumarate is a novel oral therapeutic agent, which can be used for patients suffering from relapsing-remitting multiple sclerosis. It shows an effective inhibition of mould in bread and can also serve as a potential candidate for the treatment of psoriasis, a chronic autoimmune condition.

• Kontakt-Allergie

  Dimethylfumarate, a strong irritant, is used as an industrial wide spectrum biocide in Asia and mainly in China, for textiles, leather, seeds, food, and cosmetic ingredients. It provoked a worldwide epidemic of severe contact dermatitis, initially from Chinese sofas sold in Finland, Great Britain, and France. It also induced severe burning and contact allergy due to shoes, and to contaminated clothing as well. This chemical, presents as is (white powder) or as tablets contained in little bags disposed in/or around the materials to protect, progressively evaporates and contaminates the environment. It is forbidden in the European Union since 2008

• Clinical Use

  Treatment of relapsing-remitting multiple sclerosis
  Treatment of moderate to severe plaque psoriasis

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Aminophylline and theophylline: enhanced effect of aminophylline and theophylline.
  Anaesthetics: enhanced hypotensive effect.
  Anti-arrhythmics: increased risk of bradycardia, AV block and myocardial depression with amiodarone; increased risk of bradycardia and myocardial depression with dronedarone.
  Antibacterials: metabolism increased by rifampicin; metabolism possibly inhibited by clarithromycin, erythromycin and telithromycin.
  Antidepressants: enhanced hypotensive effect with MAOIs; concentration of imipramine and possibly other trycyclics increased
  Antiepileptics: effect probably reduced by barbiturates, fosphenytoin, phenytoin, and primidone; enhanced effect of carbamazepine; increased levels of fosphenytoin and phenytoin.
  Antifungals: negative inotropic effect possibly increased with itraconazole.
  Antihypertensives: enhanced hypotensive effect; increased risk of first dose hypotensive effect of postsynaptic alpha-blockers
  Antipsychotics: concentration of lurasidone increased.
  Antivirals: concentration increased by atazanavir and ritonavir - reduce dose of diltiazem with atazanavir; concentration reduced by efavirenz; use telaprevir with caution.
  Avanafil: possibly increases avanafil concentration.
  Beta-blockers: risk of bradycardia and AV block if co-prescribed with beta-blockers.
  Cardiac glycosides: increased digoxin concentration.
  Ciclosporin: increased ciclosporin concentrations.
  Cilostazol: increased cilostazol concentration - avoid.
  Colchicine: possibly increased risk of colchicine toxicity - suspend or reduce colchicine, avoid concomitant use in renal or hepatic failure.
  Cytotoxics: concentration of bosutinib, ibrutinib and olaparib possibly increased - avoid or reduce dose; possibly increased risk of bradycardia with crizotinib.
  Fingolimod: increased risk of bradycardia.
  Ivabradine: concentration of ivabradine increased - avoid.
  Lipid lowering drugs: concentration of lomitapide possibly increased - avoid.
  Sirolimus: sirolimus concentration increased.

• Stoffwechsel

  Diltiazem is almost completely absorbed from the gastrointestinal tract after oral doses, but undergoes extensive first-pass hepatic metabolism resulting in a bioavailability of about 40%. It is extensively metabolised in the liver, mainly by the cytochrome P450 isoenzyme CYP3A4; one of the metabolites, desacetyldiltiazem, has been reported to have 25-50% of the activity of the parent compound.
  About 2-4% of a dose is excreted in urine as unchanged diltiazem with the remainder excreted as metabolites in bile and urine.

Dimethyl fumarate Upstream-Materialien And Downstream Produkte

Dimethylfumarat Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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