OPC-67683

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• 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.

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

  P302+P352：BEI BERÜHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckmäßig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.

  P304+P340：BEI EINATMEN: Die Person an die frische Luft bringen und für ungehinderte Atmung sorgen.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

  P312：Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

  P321：Besondere Behandlung

  P332+P313：Bei Hautreizung: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

  P337+P313：Bei anhaltender Augenreizung: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

  P403+P233：An einem gut belüfteten Ort aufbewahren. Behälter dicht verschlossen halten.

  P405：Unter Verschluss aufbewahren.

  P501：Inhalt/Behälter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

OPC-67683 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  Marketed by Otsuka, delamanid was approved in both the European Union and Japan in 2014 as part of combination therapies for multi-drug resistant tuberculosis (TB). Because delamanid exhibited no adverse drug–drug interactions, it has found utility as a combination therapy with standard antiretroviral drugs indicated for TB. Delamanid blocks mycolic acid biosynthesis in Mycobacterium tuberculosis, which allows its cell wall to be penetrated by small molecule antivirals.

• Verwenden

  Delamanid is a novel anti-tuberculosis medication that inhibits mycolic acid synthesis and shows potent in vitro and in vivo activity against drug-resistant strains of Mycobacterium tuberculosis.

• Definition

  ChEBI: Delamanid is a member of piperidines.

• Clinical Use

  Treatment of multi-drug resistant tuberculosis

• Synthese

  Piperidine 81 was concurrently prepared by first generating biaryl ether 79, which arose from a substitution reaction between pyridine N-oxide 77 and phenol 78 that proceeded in 86% yield. Next, removal of the N-oxide functionality by means of catalytic hydrogenation under mild pressure and neutral conditions afforded diaryl ether 80 in excellent yield. Reduction of the pyridine to the corresponding piperidine (81) was affected through the use of catalytic hydrogenation as well, this time under acidic conditions and elevated pressures relative to the N-oxide reduction. At this juncture, subjection of piperidine 81 to Buchwald¨C Hartwig conditions in the presence of diol subunit 82 delivered diol 83. A two-step elimination to deliver enantiopure epoxide 84 set the stage for an interesting cascade reaction to arrive at delamanid (XI) directly?a the initial alkylation of the epoxide by imidazole 85 proceeded under basic conditions with sodium acetate which then underwent an intramolecular nucleophilic substitution reaction by the liberated alcohol on the pendant imidazole chloride in the presence of sodium hydroxide. The reaction sequence proceeded in 73% yield to provide delamanid (XI) as a free base.

  

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Analgesics: increased risk of ventricular arrhythmias with methadone
  Anti-arrhythmics: increased risk of ventricular arrhythmias with amiodarone and disopyramide
  Antibacterials: possible increased risk of ventricular arrhythmias with clarithromycin, erythromycin and moxifloxacin; increased risk of ventricular arrhythmias with pentamidine; concentration reduced by rifampicin
  Antidepressants: possible increased risk of ventricular arrhythmias with tricyclics.
  Antiepileptics: avoid with carbamazepine.
  Antipsychotics: increased risk of ventricular arrhythmias with droperidol, haloperidol, phenothiazines that prolong the QT interval and pimozide.
  Antivirals: increased risk of ventricular arrhythmias with saquinavir
  Beta-blockers: increased risk of ventricular arrhythmias with sotalol.
  Cytotoxics: increased risk of ventricular arrhythmias with arsenic trioxide and possibly vinblastine, vincristine, vindesine, vinflunine and vinorelbine
  Domperidone: possible increased risk of ventricular arrhythmias.

• Stoffwechsel

  Delamanid is mainly metabolised in plasma by albumin and to a lesser extent by CYP3A4. The complete metabolic profile of delamanid has not yet been elucidated. The identified metabolites do not show anti-mycobacterial activity but some contribute to QT prolongation, mainly DM-6705.

OPC-67683 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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