Tìm theo
Fluvoxamine
Các tên gọi khác (3) :
  • Fluvoxamina
  • Fluvoxamine
  • Fluvoxaminum
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 54739-18-3
ATC: N06AB08
ĐG : Anip Acquisition Co.
CTHH: C15H21F3N2O2
PTK: 318.3346
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H21F3N2O2
Phân tử khối
318.3346
Monoisotopic mass
318.155512541
InChI
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+
InChI Key
InChIKey=CJOFXWAVKWHTFT-XSFVSMFZSA-N
IUPAC Name
(2-aminoethoxy)({5-methoxy-1-[4-(trifluoromethyl)phenyl]pentylidene})amine
Traditional IUPAC Name
(2-aminoethoxy)({5-methoxy-1-[4-(trifluoromethyl)phenyl]pentylidene})amine
SMILES
COCCCCC(=NOCCN)C1=CC=C(C=C1)C(F)(F)F
Độ tan chảy
120-121.5 °C
Độ hòa tan
7.34e-03 g/l
logP
3.2
logS
-4.6
pKa (Strongest Basic)
9.16
PSA
56.84 Å2
Refractivity
79.2 m3·mol-1
Polarizability
32.44 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Fluvoxamine, an aralkylketone-derivative agent, is one of a class of antidepressants known as selective serotonin reuptake inhibitors (SSRIs) that differs structurally from other SSRIs. It is used to treat the depression associated with mood disorders. It is also used on occassion in the treatment of body dysmorphic disorder and anxiety. The antidepressant, antiobsessive-compulsive, and antibulimic actions of Fluvoxamine are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. In vitro studies show that Fluvoxamine is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. Fluvoxamine has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. The chronic administration of Fluvoxamine was found to downregulate brain norepinephrine receptors, as has been observed with other drugs effective in the treatment of major depressive disorder. Fluvoxamine does not inhibit monoamine oxidase.
Cơ Chế Tác Dụng : 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. 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 5HT1A 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 α1- or α2-adrenergic, β-adrenergic, muscarinic, dopamine D2, histamine H1, GABA-benzodiazepine, opiate, 5-HT1, or 5-HT2 receptors.
Dược Động Học :
▧ Absorption :
Well absorbed, bioavailability of fluvoxamine maleate is 53%.
▧ Volume of Distribution :
* 25 L/kg
▧ Protein binding :
~77-80% (plasma protein)
▧ Metabolism :
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
Độc Tính : 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.
Chỉ Định : For management of depression and for Obsessive Compulsive Disorder (OCD). Has also been used in the management of bulimia nervosa.
Tương Tác Thuốc :
  • Acenocoumarol Fluvoxamine may increase the anticoagulant effect of acenocoumarol by increasing its serum concentration.
  • Almotriptan Increased risk of CNS adverse effects
  • Aminophylline Fluvoxamine may increase the effect and toxicity of aminophylline.
  • Amitriptyline The SSRI, fluvoxamine, may increase the serum concentration of the tricyclic antidepressant, amitriptyline, by decreasing its metabolism. Additive modulation of serotonin activity also increases the risk of serotonin syndrome. Monitor for development of serotonin syndrome during concomitant therapy. Monitor for changes in the therapeutic and adverse effects of amitriptyline if fluvoxamine is initiated, discontinued or dose changed.
  • Amoxapine The SSRI, fluvoxamine, may increase the serum concentration of the tricyclic antidepressant, amoxapine, by decreasing its metabolism. Additive modulation of serotonin activity also increases the risk of serotonin syndrome. Monitor for development of serotonin syndrome during concomitant therapy. Monitor for changes in the therapeutic and adverse effects of amoxapine if fluvoxamine is initiated, discontinued or dose changed.
  • Amphetamine Risk of serotoninergic syndrome
  • Anisindione Fluvoxamine may increase the anticoagulant effect of anisindione by increasing its serum concentration.
  • Asenapine Fluvoxamine is a CYP1A2 inhibitor that increases exposure of asenapine by 30%.
  • Astemizole Increased risk of cardiotoxicity and arrhythmias
  • Bendamustine Affects hepatic CYP1A2 metabolism, thus increasing bendamustine levels. Concentration of active metabolites may be decreased due to decreased conversion.
  • Benzphetamine Amphetamines may enhance the adverse/toxic effect of Serotonin Modulators. The risk of serotonin syndrome may be increased. Monitor patients closely for signs and symptoms of serotonin syndrome (e.g., agitation, tremor, tachycardia, etc.) when using amphetamines and serotonin modulators in combination.
  • Carbamazepine Fluvoxamine increases the effect of carbamazepine
  • Carisoprodol Strong CYP2C19 inhibitors such as fluvoxamine may decrease the metabolism of CYP2C19 substrates such as carisoprodol. Consider an alternative for one of the interacting drugs in order to avoid toxicity of the substrate. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of the CYP substrate if a CYP inhibitor is initiated/dose increased, and decreased effects if a CYP inhibitor is discontinued/dose decreased.
  • Cilostazol Fluvoxamine increases the effect of cilostazol
  • Clomipramine The SSRI, fluvoxamine, may increase the serum concentration of the tricyclic antidepressant, clomipramine, by decreasing its metabolism. Additive modulation of serotonin activity also increases the risk of serotonin syndrome. Monitor for development of serotonin syndrome during concomitant therapy. Monitor for changes in the therapeutic and adverse effects of clomipramine if fluvoxamine is initiated, discontinued or dose changed.
  • Clozapine The antidepressant increases the effect of clozapine
  • Desipramine The SSRI, fluvoxamine, may increase the serum concentration of the tricyclic antidepressant, desipramine, by decreasing its metabolism. Additive modulation of serotonin activity also increases the risk of serotonin syndrome. Monitor for development of serotonin syndrome during concomitant therapy. Monitor for changes in the therapeutic and adverse effects of desipramine if fluvoxamine is initiated, discontinued or dose changed.
  • Desvenlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Dexfenfluramine Risk of serotoninergic syndrome
  • Dextroamphetamine Risk of serotoninergic syndrome
  • Dicoumarol Fluvoxamine may increase the anticoagulant effect of dicumarol by increasing its serum concentration.
  • Diethylpropion Risk of serotoninergic syndrome
  • Dihydroergotamine Possible ergotism and severe ischemia with this combination
  • Doxepin The SSRI, fluvoxamine, may increase the serum concentration of the tricyclic antidepressant, doxepin, by decreasing its metabolism. Additive modulation of serotonin activity also increases the risk of serotonin syndrome. Monitor for development of serotonin syndrome during concomitant therapy. Monitor for changes in the therapeutic and adverse effects of doxepin if fluvoxamine is initiated, discontinued or dose changed.
  • Duloxetine Fluvoxamine increases the effect and toxicity of duloxetine
  • Dyphylline Increases the effect and toxicity of theophylline
  • Eletriptan Increased risk of CNS adverse effects
  • Eltrombopag Affects hepatic enzyme CYP1A2 metabolism and may increase the level of eltrombopag.
  • Eltrombopag Affects hepatic CYP2C9/10 metabolism, will increase effect/level of eltrombopag.
  • Ergotamine Possible ergotism and severe ischemia with this combination
  • Ethotoin Increases the effect of hydantoin
  • Fenfluramine Risk of serotoninergic syndrome
  • Fosphenytoin Fluvoxamine may increase the therapeutic and adverse effects of fosphenytoin.
  • Frovatriptan Increased risk of CNS adverse effects
  • Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
  • Imipramine The SSRI, fluvoxamine, may increase the serum concentration of the tricyclic antidepressant, imipramine, by decreasing its metabolism. Additive modulation of serotonin activity also increases the risk of serotonin syndrome. Monitor for development of serotonin syndrome during concomitant therapy. Monitor for changes in the therapeutic and adverse effects of imipramine if fluvoxamine is initiated, discontinued or dose changed.
  • Isocarboxazid Possible severe adverse reaction with this combination
  • Ketoprofen Concomitant therapy may result in additive antiplatelet effects and increase the risk of bleeding. Monitor for increased risk of bleeding during concomitant therapy.
  • Linezolid Combination associated with possible serotoninergic syndrome
  • Lithium The SSRI, fluvoxamine, increases serum levels of lithium.
  • Mazindol Risk of serotoninergic syndrome
  • Mephenytoin Increases the effect of hydantoin
  • Mesoridazine Increased risk of cardiotoxicity and arrhythmias
  • Methadone Fluvoxamine increases the effect and toxicity of methadone
  • Methamphetamine Risk of serotoninergic syndrome
  • Mexiletine Fluvoxamine may increase the therapeutic and adverse effects of mexiletine.
  • Mirtazapine Fluvoxamine may increase the therapeutic and adverse effects of mirtazapine.
  • Moclobemide Increased incidence of adverse effects with this association
  • Naratriptan Increased risk of CNS adverse effects
  • Nortriptyline The SSRI, fluvoxamine, may increase the serum concentration of the tricyclic antidepressant, nortriptyline, by decreasing its metabolism. Additive modulation of serotonin activity also increases the risk of serotonin syndrome. Monitor for development of serotonin syndrome during concomitant therapy. Monitor for changes in the therapeutic and adverse effects of nortriptyline if fluvoxamine is initiated, discontinued or dose changed.
  • Olanzapine Fluvoxamine increases the effect and toxicity of olanzapine
  • Oxtriphylline Fluvoxamine may increase the therapeutic and adverse effects of oxtriphylline.
  • Oxycodone Increased risk of serotonin syndrome
  • Phendimetrazine Risk of serotoninergic syndrome
  • Phenelzine Possible severe adverse reaction with this combination
  • Phentermine Risk of serotoninergic syndrome
  • Phenylpropanolamine Risk of serotoninergic syndrome
  • Phenytoin Fluvoxamine may increase the therapeutic effect of phenytoin.
  • Protriptyline The SSRI, fluvoxamine, may increase the serum concentration of the tricyclic antidepressant, protriptyline, by decreasing its metabolism. Additive modulation of serotonin activity also increases the risk of serotonin syndrome. Monitor for development of serotonin syndrome during concomitant therapy. Monitor for changes in the therapeutic and adverse effects of protriptyline if fluvoxamine is initiated, discontinued or dose changed.
  • Ramelteon Fluvoxamine may increase the serum level and toxicity of ramelteon.
  • Rasagiline Possible severe adverse reaction with this combination
  • Rizatriptan Increased risk of CNS adverse effects
  • Roflumilast Increases roflumilast levels.
  • Ropinirole Increases the effect and toxicity of ropinirole
  • Ropivacaine Increases the effect and toxicity of ropivacaine
  • Selegiline Possible severe adverse reaction with this combination
  • Sibutramine Risk of serotoninergic syndrome
  • St. John's Wort St. John's Wort increases the effect and toxicity of the SSRI, fluvoxamine.
  • Sumatriptan Increased risk of CNS adverse effects
  • Tacrine Fluvoxamine, a strong CYP1A2 inhibitor, may decrease the metabolism and clearance of tacrine, a CYP1A2 substrate. Concomitant therapy should be avoided as it could lead to severe toxic effects such as hepatotoxicity. If concomitant therapy is used, monitor for altered efficacy and toxic effects, such as gastrointestinal and hepatic effects, of tacrine.
  • Terbinafine Terbinafine may reduce the metabolism and clearance of Fluvoxamine. Consider alternate therapy or monitor for therapeutic/adverse effects of Fluvoxamine if Terbinafine is initiated, discontinued or dose changed.
  • Terfenadine Increased risk of cardiotoxicity and arrhythmias
  • Theophylline Fluvoxamine may increase the therapeutic and adverse effects of theophylline.
  • Thiabendazole The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Fluvoxamine by decreasing Fluvoxamine metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Fluvoxamine if Thiabendazole is initiated, discontinued or dose changed.
  • Thioridazine Increased risk of cardiotoxicity and arrhythmias
  • Thiothixene The strong CYP1A2 inhibitor, Fluvoxamine, may decrease the metabolism and clearance of Thiothixene, a CYP1A2 substrate. Consider alternate therapy or monitor for changes in Thiothixene therapeutic and adverse effects if Fluvoxamine is initiated, discontinued or dose changed.
  • Tiaprofenic acid Additive antiplatelet effects increase the risk of bleeding. Consider alternate therapy or monitor for increased bleeding.
  • Tizanidine Fluvoxamine inhibits the metabolism and clearance of tizanidine. Concomitant therapy is contraindicated.
  • Tolmetin Increased antiplatelet effects may enhance the risk of bleeding. Alternate therapy may be considered or monitor for inreased bleeding during concomitant therapy.
  • Tramadol Tramadol may increase the risk of serotonin syndrome and seizures.
  • Tranylcypromine Increased risk of serotonin syndrome. Concomitant therapy should be avoided. A significant washout period, dependent on the half-lives of the agents, should be employed between therapies.
  • Trazodone Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Treprostinil The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Fluvoxamine. Monitor for increased bleeding during concomitant thearpy.
  • Trimipramine The strong CYP2C19 inhibitor, fluvoxamine, may decrease the metabolism and clearance of trimipramine, a CYP2C19 substrate. Additive modulation of serotonin activity may also increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome and changes in therapeutic and adverse effects of trimipramine if fluvoxamine is initiated, discontinued or dose changed.
  • Triprolidine The CNS depressants, Triprolidine and Fluvoxamine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Venlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Warfarin Fluvoxamine may increase the anticoagulant effect of warfarin by increasing its serum concentration.
  • Zolmitriptan Use of two serotonin modulators, such as zolmitriptan and fluvoxamine, may increase the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
Liều Lượng & Cách Dùng : Tablet, film coated - Oral - 100 mg
Tablet, film coated - Oral - 25 mg
Tablet, film coated - Oral - 50 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Abbott
    Sản phẩm biệt dược : Dumirox
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    Sản phẩm biệt dược : Faverin
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    Sản phẩm biệt dược : Fevarin
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    Sản phẩm biệt dược : Floxyfral
  • Công ty : Abbott
    Sản phẩm biệt dược : Luvox
  • Công ty : Abbott
    Sản phẩm biệt dược : Maveral
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00176
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5324346
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507588
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07571
ChemSpider
http://www.chemspider.com/Chemical-Structure.3287.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/57664-357-88
PharmGKB
http://www.pharmgkb.org/drug/PA449690
Wikipedia
http://en.wikipedia.org/wiki/Fluvoxamine
RxList
http://www.rxlist.com/cgi/generic/fluvox.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/flu1660.shtml
Drugs.com
http://www.drugs.com/cdi/fluvoxamine.html
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