Domperidon

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Sicherheit

  P201：Vor Gebrauch besondere Anweisungen einholen.

  P202：Vor Gebrauch alle Sicherheitshinweise lesen und verstehen.

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

  P308+P313：BEI Exposition oder falls betroffen: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

  P405：Unter Verschluss aufbewahren.

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

Domperidone Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R62:Kann möglicherweise die Fortpflanzungsfähigkeit beeinträchtigen.
  R63:Kann das Kind im Mutterleib möglicherweise schädigen.

• S-Sätze Betriebsanweisung:

  S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
  S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.

• Chemische Eigenschaften

  White or almost white powder.

• Originator

  Motilium,Cilag,Switz.,1979

• Verwenden

  A novel peripheral dopamine receptor antagonist that does not cross the blood-brain barrier; anti-emetic. Domperidone(Motilium) is a dopamine blocker and an antidopaminergic reagent.

• Verwenden

  For management of dyspepsia, heartburn, epigastric pain, nausea, and vomiting.

• Verwenden

  COX2 inhibitor, antiinflammatory, antiarthritic

• Definition

  ChEBI: 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used s an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet reparations.

• Manufacturing Process

  A mixture of 2.3 parts of 1-(3-chloropropyl)-1,3-dihydro-2H-benzimidazol-2- one, 2.5 parts of 5-chloro-1,3-dihydro-l-(4-piperidinyl)-2H-benzimidazol-2- one, 3.2 parts of sodium carbonate, 0.1 part of potassium iodide and 80 parts of 4-methyl-2-pentanone is stirred and refluxed for 24 hours. The reaction mixture is cooled to room temperature and water is added. The undissolved product is filtered off and purified by column chromatography over silica gel using a mixture of trichloromethane and 10% methanol as eluent. The pure fractions are collected and the eluent is evaporated. The residue is crystallized from 4-methyl-2-pentanone. The product is filtered off and recrystallized from a mixture of N,N-dimethylformamide and water, yielding 1.3 parts (30%) of 5- chloro-1-[1-[3-(1,3-dihydro-2-oxo-2H-benzimidazol-1-yl)propyl]-4- piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one; MP 242.5°C.

• Trademarks

  Motilium (Janssen);Evixub;Kw 5338;Moperidona;Neta662;R 33812;Tametil;Touristic.

• Therapeutic Function

  Antiemetic

• Weltgesundheitsorganisation (WHO)

  Domperidone, a peripheral dopaminergic antagonist, was introduced in 1979 for the symptomatic relief of acute nausea and vomiting. The major manufacturer became aware that the injectable formulation was being used in some countries in much higher doses than those recommended to combat nausea and vomiting in cancer patients treated with cytostatic agents. Such use - which was not in conformity with the approved indications - was associated with cardiotoxicity, which in some cases was fatal, and the manufacturer decided to withdraw the injectable dosage form from the market worldwide in January 1985. Suppositories, tablets and a suspension remain available and the manufacturer continues to supply the injection for the treatment of a named patient at the written request of a doctor on the understanding that the appropriate dosage recommendations will be followed.

• Biologische Aktivität

  Peripheral dopamine D 2 -like receptor antagonist that does not readily cross the blood brain barrier. Displays gastroprokinetic and antiemetic properties; increases the frequency and duration of antral and duodenal contractions and protects from apomorphine-induced emesis (ED 50 values are 0.003 and 0.03 mg/kg for i.v. and oral administration respectively).

• Clinical Use

  Acute nausea and vomiting (including that caused by levodopa and bromocriptine)
  Gastro-oesophageal reflux
  Dyspepsia

• Veterinary Drugs and Treatments

  Domperidone may be useful for treatment of fescue toxicosis in pregnant mares or as a prokinetic or antiemetic agent in small animals. It has more effect on conditions with delayed gastric emptying than other GI hypomotility conditions.
  Via its effects on prolactin, domperidone may also be used to stimulate milk production in horses and small animals.
  Domperidone has been shown to increase plasma ACTH in horses with equine pituitary pars intermedia dysfunction (Equine Cushing’s) and may be useful in helping diagnose this condition.

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Antibacterials: possible increased risk of ventricular arrhythmias with clarithromycin, delamanid and erythromycin - avoid with clarithromycin and erythromycin.
  Antifungals: possibly increased risk of ventricular arrhythmias with itraconazole, ketoconazole and voriconazole - avoid.
  Antimalarials: possible increased risk of ventricular arrhythmias with piperaquine with artenimol - avoid.
  Antivirals: possible increased risk of ventricular arrhythmias with boceprevir; possible increased risk of ventricular arrhythmias with ritonavir, saquinavir and telaprevir - avoid
  Apomorphine: possible increased risk of ventricular arrhythmias.
  Cobicistat: possible increased risk of ventricular arrhythmias - avoid.
  Cytotoxics: increased risk of ventricular arrhythmias with bosutinib and ceritinib - avoid with bosutinib.

• Stoffwechsel

  Domperidone undergoes extensive first-pass hepatic and intestinal metabolism. It undergoes rapid and extensive hepatic metabolism. The main metabolic pathways are N-dealkylation by cytochrome P450 isoenzyme CYP3A4, and aromatic hydroxylation by CYP3A4, CYP1A2, and CYP2E1.
  About 30% of an oral dose is excreted in urine within 24 hours, almost entirely as metabolites; the remainder of a dose is excreted in faeces over several days, about 10% as unchanged drug.

• Lager

  Room temperature

Domperidone Upstream-Materialien And Downstream Produkte

Domperidon Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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