Fluvoxamine maleate

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

Fluvoxamine maleate Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R22:Gesundheitsschädlich beim Verschlucken.
  R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.

• S-Sätze Betriebsanweisung:

  S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
  S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
  S27:Beschmutzte, getränkte Kleidung sofort ausziehen.
  S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.

• Beschreibung

  Fluvoxamine maleate is the most recent of the serotonin-specific antidepressants to reach the market. In vitro and in vivo animal experiments have shown fluvoxamine to have a marked effect on 5-HT mediated processes and little effect on norepinephrine. Clinical trials suggest similar efficacy to imipramine and clomipramine with a somewhat lower incidence of side effects, especially anticholinergic effects. Fluvoxamine, in contrast to the tricyclic antidepressants, does not appear to produce heart rate increase, postural hypotension or prolongation of the intraventricular conduction time and QT interval.

• Chemische Eigenschaften

  Crystalline Solid

• Originator

  Duphar (Netherlands)

• Verwenden

  Anxiety disorder

• Verwenden

  nonsteroidal anti-inflammatory reduces pain and inflammation in eyes

• Verwenden

  A selective serotonin reuptake inhibitor (SSRI) used as an anti-depressant. Antiobsessional.

• Verwenden

  estrogen

• Verwenden

  Fluvoxamine maleate has been used as a test compound to determine the solubility and effective blood-brain barrier permeability.(2)

• Definition

  ChEBI: Fluvoxamine maleate is a member of (trifluoromethyl)benzenes.

• Manufacturing Process

  20.4 mmol (5.3 g) of 5-methoxy-4'-trifluoromethylvalerophenone (MP 43°C to 44°C), 20.5 mmol (3.1 g) of 2-aminooxyethylamine dihydrochloride and 10 ml of pyridine were refluxed for 15 hr in 20 ml of absolute ethanol. After evaporating the pyridine and the ethanol in vacuo, the residue was dissolved in water. This solution was washed with petroleum ether and 10 ml of 50% sodium hydroxide solution were then added. Then three extractions with 40 ml of ether were carried out. The ether extract was washed successively with 20 ml of 5% sodium bicarbonate solution and 20 ml of water. After drying on sodium sulfate, the ether layer was evaporated in vacuo. Toluene was then evaporated another three times (to remove the pyridine) and the oil thus obtained was dissolved in 15 ml of absolute ethanol. An equimolar quantity of maleic acid was added to the solution and the solution was then heated until a clear solution was obtained. The ethanol was then removed in vacuo and the residue was crystallized from 10 ml of acetonitrile at +5°C. After sucking off and washing with cold acetonitrile, it was dried in air. The MP of the resulting compound was 120°C to 121.5°C.

• Trademarks

  Luvox (Solvay Pharmaceuticals);FLOXYFRAL.

• Therapeutic Function

  Antidepressant

• Allgemeine Beschreibung

  Pharmaceutical secondary standards for application in quality control provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards

• Hazard

  A poison by ingestion. Human systemic effects.

• Biologische Aktivität

  Selective serotonin reuptake inhibitor; antidepressant. Binds to the human 5-HT transporter with a K i of 1.6 nmol/l. Also available as part of the Serotonin Uptake Inhibitor Tocriset™ .

• Biochem/physiol Actions

  Fluvoxamine maleate is a selective neuronal serotonin reuptake inhibitor. It functions as an antidepressant and anti-obsessive agent. It is useful in treating obsessive compulsive disorder and panic disorder.

• Clinical Use

  SSRI antidepressant:
  Depression
  Obsessive compulsive disorder

• Veterinary Drugs and Treatments

  Fluvoxamine may be considered for use in treating a variety of behavior- related diagnoses in dogs and cats, including aggression and stereotypic behaviors (and other obsessive-compulsive behaviors).

• Arzneimittelwechselwirkung

  Potentially hazardous interactions with other drugs
  Aminophylline and theophylline: increased aminophylline and theophylline concentrations - avoid; if not possible, halve aminophylline or theophylline dose and monitor levels.
  Analgesics: increased risk of bleeding with aspirin and NSAIDs; risk of CNS toxicity increased with tramadol; concentration of methadone possibly increased.
  Anti-arrhythmics: increased risk of toxicity with mexiletine.
  Anticoagulants: effect of coumarins possibly enhanced; possibly increased risk of bleeding with dabigatran.
  Antidepressants: avoid with reboxetine, MAOIs, moclobemide and St John’s wort; possibly enhanced serotonergic effects with mirtazapine; fluvoxamine inhibits metabolism of duloxetine - avoid; can increase tricyclics concentration; metabolism of agomelatine reduced; possible increased risk of convulsions with vortioxetine.
  Antiepileptics: antagonise anticonvulsant threshold; concentration of carbamazepine, fosphenytoin and phenytoin increased.
  Antimalarials: avoid with artemether/lumefantrine and piperaquine with artenimol.
  Antipsychotics: concentration of asenapine, haloperidol, clozapine and olanzapine increased; increased risk of ventricular arrhythmias with droperidol and possibly pimozide - avoid.
  Antivirals: concentration possibly increased by ritonavir.
  Ciclosporin: may increase ciclosporin concentration.
  Clopidogrel: possibly reduced antiplatelet effect.
  Cytotoxics: concentration of pomalidomide increased
  Dapoxetine: possible increased risk of serotonergic effects - avoid.
  Dopaminergics: increased risk of CNS toxicity with rasagiline - avoid; hypertension and CNS excitation with selegiline - avoid.
  5HT1 agonists: risk of CNS toxicity increased with sumatriptan; possibly increased risk of serotonergic effects with naratriptan; inhibits metabolism of frovatriptan; possibly inhibits metabolism of zolmitriptan - reduce zolmitriptan dose.
  Linezolid: use with care, possibly increased risk of side effects.
  Lithium: increased risk of CNS effects - monitor levels.
  Melatonin: concentration of melatonin increased - avoid.
  Methylthioninium: risk of CNS toxicity - avoid if possible.
  Muscle relaxants: increased risk of toxicity with tizanidine - avoid
  Pirfenidone: concentration of pirfenidone increased - avoid.

• Stoffwechsel

  Fluvoxamine undergoes extensive hepatic transformation by CYP2D6, mainly via oxidative demethylation, into at least 9 metabolites. The 2 major metabolites showed negligible pharmacological activity. The other metabolites are not expected to be pharmacologically active.
  Excretion is mainly in the urine; about 2% of a dose is excreted as unchanged drug.

• Lager

  +4°C (desiccate)

Fluvoxamine maleate Upstream-Materialien And Downstream Produkte

Fluvoxamine maleate Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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