2747 Fluvoxamine Fluvoxamine is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor. Though it is in the same class as other SSRI drugs, it is most often used to treat obsessive-compulsive disorder. Fluvoxamine has been in use in clinical practice since 1983 and has a clinical trial database comprised of approximately 35,000 patients. It was launched in the US in December 1994 and in Japan in June 1999. As of the end of 1995, more than 10 million patients worldwide have been treated with fluvoxamine. 54739-18-3 5324346 C15H21F3N2O2 318.155510 White powder. 120-121.5°C 7.34e-03 g/L Oral. Well absorbed, bioavailability of fluvoxamine maleate is 53%. The exact mechanism of action of fluvoxamine has not been fully determined, but appears to be linked to its inhibition of CNS neuronal uptake of serotonin. Fluvoxamine blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT_1A autoreceptors. In-vitro studies suggest that fluvoxamine is more potent than clomipramine, fluoxetine, and desipramine as a serotonin-reuptake inhibitor. Studies have also demonstrated that fluvoxamine has virtually no affinity for alpha₁- or alpha₂-adrenergic, beta-adrenergic, muscarinic, dopamine D₂, histamine H₁, GABA-benzodiazepine, opiate, 5-HT₁, or 5-HT₂ receptors. Hepatic Route of Elimination: The main human metabolite was fluvoxamine acid which, together with its N-acetylated analog, accounted for about 60% of the urinary excretion products. Approximately 2% of fluvoxamine was excreted in urine unchanged. Following a 14C-labelled oral dose of fluvoxamine maleate (5 mg), an average of 94% of drug-related products was recovered in the urine within 71 hours. Half Life: 15.6 hours No indication of carcinogenicity to humans (not listed by IARC). For management of depression and for Obsessive Compulsive Disorder (OCD). Has also been used in the management of bulimia nervosa. Side effects include anorexia, constipation, dry mouth, headache, nausea, nervousness, skin rash, sleep problems, somnolence, liver toxicity, mania, increase urination, seizures, sweating increase, tremors, or Tourette's syndrome. Treatment should consist of those general measures employed in the management of overdosage with any antidepressant. Ensure an adequate airway, oxygenation, and ventilation. Monitor cardiac rhythm and vital signs. General supportive and symptomatic measures are also recommended. Induction of emesis is not recommended. Gastric lavage with a large-bore orogastric tube with appropriate airway protection, if needed, may be indicated if performed soon after ingestion, or in symptomatic patients. Activated charcoal should be administered. Due to the large volume of distribution of this drug, forced diuresis, dialysis, hemoperfusion and exchange transfusion are unlikely to be of benefit. No specific antidotes for fluvoxamine are known. (L1712) 2009-07-21T20:26:13Z 2026-05-14T16:24:29Z Fluvoxamine C07571 5138 Fluvoxamine DB00176 FVX true COCCCC\C(=N/OCCN)C1=CC=C(C=C1)C(F)(F)F C15H21F3N2O2 InChI=1S/C15H21F3N2O2/c1-21-10-3-2-4-14(20-22-11-9-19)12-5-7-13(8-6-12)15(16,17)18/h5-8H,2-4,9-11,19H2,1H3/b20-14+ InChIKey=CJOFXWAVKWHTFT-XSFVSMFZSA-N 318.3346 318.155512541 Exogenous Solid 3.2 HMDB14322 CHEMBL814 3287 <p>Welle, H.B.A. and Claassen, V.; U.S. Patent 4,085,225; April 18, 1978; assigned to U.S. Phillips Corp.</p> CHEM002137 DTXSID2044002 NS00001955 (E)-(2-aminoethoxy)({5-methoxy-1-[4-(trifluoromethyl)phenyl]pentylidene})amine 56.84 79.19710000000003 32.43969539227251 10 4 1 9.163029545122631 1 1 2.89 -4.64 7.34e-03 g/l