Desipramin

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Achtung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H336：Kann Schläfrigkeit und Benommenheit verursachen.

  H370：Schädigt die Organe.

• Sicherheit

  P260：Dampf/Aerosol/Nebel nicht einatmen.

  P261：Einatmen von Staub vermeiden.

  P264：Nach Gebrauch gründlich waschen.

  P264：Nach Gebrauch gründlich waschen.

  P270：Bei Gebrauch nicht essen, trinken oder rauchen.

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

  P301+P312：BEI VERSCHLUCKEN: Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

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

  P307+P311：BEI Exposition: GIFTINFORMATIONSZENTRUM oder Arzt anrufen.

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

  P321：Besondere Behandlung

  P330：Mund ausspülen.

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

  P405：Unter Verschluss aufbewahren.

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

DESIPRAMINE Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R20/21/22:Gesundheitsschädlich beim Einatmen,Verschlucken und Berührung mit der Haut.

• S-Sätze Betriebsanweisung:

  S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.

• Originator

  Pertofran,Geigy,UK,1963

• Verwenden

  Desipramine is used for depression of various etiology and in particular for endogenous depression.

• Verwenden

  Antidepressant.

• Definition

  ChEBI: A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group.

• Manufacturing Process

  Oxidative coupling of o-nitrotoluene gives 4,4'-dinitrodibenzyl which is reduced with hydrogen to the diamine. The diamine is pyrolyzed to give dihydrobenzazepine. This is reacted with N-(3-chloropropyl)-Nmethylbenzamine to give N-benzyldesipramine. This is debenzylated by reductive cleavage and then reacted with HCl.

• Trademarks

  Norpramin (Sanofi Aventis); Pertofrane (Sanofi Aventis).

• Therapeutic Function

  Psychostimulant

• Mechanism of action

  Its antidepressant effect results from increases in the level of NE in CNS synapses, and long-term administration causes a downregulation of α1-adrenoceptors and desensitization of presynaptic α2-receptors, equilibrating the noradrenergic system and, thus, correcting the dysregulated output of depressed patients. The SSRIs do not produce this effect. Desipramine also downregulates the NET, but not the 5-SERT . Substantial loss of NE transporter–binding sites takes 15 days to occur and is accompanied by a marked reduction of NET function in vivo. Desipramine has weak effects on 5-HT reuptake.

• Synthese

  Desipramine, 10,11-dihydro-5-[3-(methylamino)propyl]-5H-dibenz[b,f] azepine (7.1.13), differs from imipramine in that it contains only one methyl group on the nitrogen atom of the propylamine side chain. The suggested methods of desipramine synthesis are very simple, and the difference lies only in the manner in which the secondary methylamine group is introduced into the structure of the drug.
  The first way of synthesis is by the alkylation of 10,11-dihydro-5H-dibenz[b,f]azepine using 1-bromo-3-chloropropane in the presence of sodium amide into a chloro derivative (7.1.12) and the subsequent reaction of this with methylamine, giving desipramine (7.1.13) [18–20].
  
  Finally, a second way of synthesis is from imipramine (7.1.1), which undergoes demethylation by successive reaction with ethyl chloroformate, giving 5-[3-(N-carbethoxy-N-methyl)aminopropyl]-10,11-dihydro-5H-dibenz[b,f]azepine (7.1.15), the alkaline hydrolysis of which leads to desipramine (7.1.13) [23,24].
  

• Stoffwechsel

  Desipramine is a dihydrodibenzazepine secondary amine TCA that also is the active metabolite of imipramine. Desipramine appears to have a bioavailability comparable to the other secondary TCAs. Desipramine is distributed into milk in concentrations similar to those present at steady state in maternal plasma. This drug is metabolized primarily by CYP2D6 to its 2-hydroxy metabolite and by CYP1A2 and CYP2C19 to its N-demethylated (primary amine) metabolite . Desipramine exhibits a greater potency and selectivity for the NET than the other secondary TCAs do.

DESIPRAMINE Upstream-Materialien And Downstream Produkte

Desipramin Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(56)Suppliers

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