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Identification
NameFluvoxamine
Accession NumberDB00176  (APRD00425)
Typesmall molecule
Groupsapproved, investigational
Description

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.

Structure
Thumb
Synonyms
SynonymLanguageCode
FluvoxaminaSpanishINN
FluvoxaminumLatinINN
Salts
Name/CAS Structure Properties
Fluvoxamine maleate
Thumb Not applicable DBSALT000879
Brand names
NameCompany
DumiroxNot Available
FaverinNot Available
FevarinNot Available
FloxyfralNot Available
LuvoxNot Available
MaveralNot Available
Brand mixturesNot Available
Categories
CAS number54739-18-3
WeightAverage: 318.3346
Monoisotopic: 318.155512541
Chemical FormulaC15H21F3N2O2
InChI KeyInChIKey=CJOFXWAVKWHTFT-XSFVSMFZSA-N
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+
IUPAC Name
(2-aminoethoxy)({5-methoxy-1-[4-(trifluoromethyl)phenyl]pentylidene})amine
SMILES
COCCCCC(=NOCCN)C1=CC=C(C=C1)C(F)(F)F
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassBenzenoids
ClassBenzene and Substituted Derivatives
SubclassNot Available
Direct parentBenzene and Substituted Derivatives
Alternative parentsOxime Ethers; Polyamines; Ethers; Monoalkylamines; Imines; Organofluorides; Alkyl Fluorides
Substituentsoxime ether; ether; polyamine; organonitrogen compound; primary amine; amine; organofluoride; organohalogen; imine; primary aliphatic amine; alkyl halide; alkyl fluoride
Classification descriptionThis compound belongs to the benzene and substituted derivatives. These are aromatic compounds containing at least one benzene ring.
Pharmacology
IndicationFor management of depression and for Obsessive Compulsive Disorder (OCD). Has also been used in the management of bulimia nervosa.
PharmacodynamicsFluvoxamine, 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.
Mechanism of actionThe 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.
AbsorptionWell absorbed, bioavailability of fluvoxamine maleate is 53%.
Volume of distribution
  • 25 L/kg
Protein binding~77-80% (plasma protein)
Metabolism

Hepatic

SubstrateEnzymesProduct
Fluvoxamine
fluvoxamino acidDetails
Route of eliminationThe 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 life15.6 hours
ClearanceNot Available
ToxicitySide 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.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 1.0
Blood Brain Barrier + 0.9775
Caco-2 permeable - 0.5149
P-glycoprotein substrate Substrate 0.6079
P-glycoprotein inhibitor I Inhibitor 0.7883
P-glycoprotein inhibitor II Non-inhibitor 0.8382
Renal organic cation transporter Non-inhibitor 0.5325
CYP450 2C9 substrate Non-substrate 0.8595
CYP450 2D6 substrate Substrate 0.8919
CYP450 3A4 substrate Non-substrate 0.6723
CYP450 1A2 substrate Inhibitor 0.9107
CYP450 2C9 substrate Inhibitor 0.8949
CYP450 2D6 substrate Inhibitor 0.8932
CYP450 2C19 substrate Inhibitor 0.8994
CYP450 3A4 substrate Inhibitor 0.7959
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8481
Ames test Non AMES toxic 0.5
Carcinogenicity Non-carcinogens 0.637
Biodegradation Not ready biodegradable 1.0
Rat acute toxicity 2.6997 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.8427
hERG inhibition (predictor II) Inhibitor 0.7995
Pharmacoeconomics
Manufacturers
  • Jazz pharmaceuticals
  • Actavis elizabeth llc
  • Apotex inc
  • Barr laboratories inc
  • Caraco pharmaceutical laboratories ltd
  • Genpharm inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Synthon pharmaceuticals ltd
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Ani pharmaceuticals inc
  • Solvay pharmaceuticals
Packagers
Dosage forms
FormRouteStrength
Tablet, film coatedOral100 mg
Tablet, film coatedOral25 mg
Tablet, film coatedOral50 mg
Prices
Unit descriptionCostUnit
Luvox CR 150 mg 24 Hour Capsule6.34USDcapsule
Luvox cr 150 mg capsule6.24USDcapsule
Luvox CR 100 mg 24 Hour Capsule6.05USDcapsule
Luvox cr 100 mg capsule5.82USDcapsule
Fluvoxamine maleate 100 mg tablet2.69USDtablet
Fluvoxamine mal 100 mg tablet2.63USDtablet
Fluvoxamine maleate 50 mg tablet2.61USDtablet
Fluvoxamine maleate 25 mg tablet2.34USDtablet
Luvox 100 mg Tablet1.7USDtablet
Luvox 50 mg Tablet0.95USDtablet
Apo-Fluvoxamine 100 mg Tablet0.93USDtablet
Co Fluvoxamine 100 mg Tablet0.93USDtablet
Novo-Fluvoxamine 100 mg Tablet0.93USDtablet
Nu-Fluvoxamine 100 mg Tablet0.93USDtablet
Pms-Fluvoxamine 100 mg Tablet0.93USDtablet
Ratio-Fluvoxamine 100 mg Tablet0.93USDtablet
Sandoz Fluvoxamine 100 mg Tablet0.93USDtablet
Apo-Fluvoxamine 50 mg Tablet0.52USDtablet
Co Fluvoxamine 50 mg Tablet0.52USDtablet
Novo-Fluvoxamine 50 mg Tablet0.52USDtablet
Nu-Fluvoxamine 50 mg Tablet0.52USDtablet
Pms-Fluvoxamine 50 mg Tablet0.52USDtablet
Ratio-Fluvoxamine 50 mg Tablet0.52USDtablet
Sandoz Fluvoxamine 50 mg Tablet0.52USDtablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States74654622000-05-102020-05-10
Properties
Statesolid
Experimental Properties
PropertyValueSource
melting point120-122.5 °CNot Available
logP3.2Not Available
Predicted Properties
PropertyValueSource
water solubility7.34e-03 g/lALOGPS
logP2.89ALOGPS
logP2.8ChemAxon
logS-4.6ALOGPS
pKa (strongest basic)9.16ChemAxon
physiological charge1ChemAxon
hydrogen acceptor count4ChemAxon
hydrogen donor count1ChemAxon
polar surface area56.84ChemAxon
rotatable bond count10ChemAxon
refractivity79.2ChemAxon
polarizability32.44ChemAxon
number of rings1ChemAxon
bioavailability1ChemAxon
rule of fiveYesChemAxon
Ghose filterYesChemAxon
Veber's ruleNoChemAxon
MDDR-like ruleNoChemAxon
Spectra
SpectraNot Available
References
Synthesis ReferenceNot Available
General Reference
  1. Dell’Osso B, Allen A, Hollander E: Fluvoxamine: a selective serotonin re-uptake inhibitor for the treatment of obsessive-compulsive disorder. Expert Opin Pharmacother. 2005 Dec;6(15):2727-40. Pubmed
  2. Irons J: Fluvoxamine in the treatment of anxiety disorders. Neuropsychiatr Dis Treat. 2005 Dec;1(4):289-99. Pubmed
External Links
ResourceLink
KEGG CompoundC07571
PubChem Compound5324346
PubChem Substance46507588
ChemSpider3287
ChEBI5138
ChEMBLCHEMBL814
Therapeutic Targets DatabaseDNC000897
PharmGKBPA449690
Drug Product Database2262630
RxListhttp://www.rxlist.com/cgi/generic/fluvox.htm
Drugs.comhttp://www.drugs.com/cdi/fluvoxamine.html
PDRhealthhttp://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/flu1660.shtml
WikipediaFluvoxamine
ATC CodesN06AB08
AHFS Codes
  • 28:16.04.20
PDB EntriesNot Available
FDA labelshow(633 KB)
MSDSshow(48.5 KB)
Interactions
Drug Interactions
Drug
AcenocoumarolFluvoxamine may increase the anticoagulant effect of acenocoumarol by increasing its serum concentration.
AlmotriptanIncreased risk of CNS adverse effects
AminophyllineFluvoxamine may increase the effect and toxicity of aminophylline.
AmitriptylineThe 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.
AmoxapineThe 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.
AmphetamineRisk of serotoninergic syndrome
AnisindioneFluvoxamine may increase the anticoagulant effect of anisindione by increasing its serum concentration.
AsenapineFluvoxamine is a CYP1A2 inhibitor that increases exposure of asenapine by 30%.
AstemizoleIncreased risk of cardiotoxicity and arrhythmias
BendamustineAffects hepatic CYP1A2 metabolism, thus increasing bendamustine levels. Concentration of active metabolites may be decreased due to decreased conversion.
BenzphetamineAmphetamines 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.
CarbamazepineFluvoxamine increases the effect of carbamazepine
CarisoprodolStrong 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.
CilostazolFluvoxamine increases the effect of cilostazol
ClomipramineThe 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.
ClozapineThe antidepressant increases the effect of clozapine
DesipramineThe 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.
DesvenlafaxineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
DexfenfluramineRisk of serotoninergic syndrome
DextroamphetamineRisk of serotoninergic syndrome
DicoumarolFluvoxamine may increase the anticoagulant effect of dicumarol by increasing its serum concentration.
DiethylpropionRisk of serotoninergic syndrome
DihydroergotaminePossible ergotism and severe ischemia with this combination
DoxepinThe 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.
DuloxetineFluvoxamine increases the effect and toxicity of duloxetine
DyphyllineIncreases the effect and toxicity of theophylline
EletriptanIncreased risk of CNS adverse effects
EltrombopagAffects hepatic enzyme CYP1A2 metabolism and may increase the level of eltrombopag.
EltrombopagAffects hepatic CYP2C9/10 metabolism, will increase effect/level of eltrombopag.
ErgotaminePossible ergotism and severe ischemia with this combination
EthotoinIncreases the effect of hydantoin
FenfluramineRisk of serotoninergic syndrome
FosphenytoinFluvoxamine may increase the therapeutic and adverse effects of fosphenytoin.
FrovatriptanIncreased risk of CNS adverse effects
Ginkgo bilobaAdditive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
ImipramineThe 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.
IsocarboxazidPossible severe adverse reaction with this combination
KetoprofenConcomitant therapy may result in additive antiplatelet effects and increase the risk of bleeding. Monitor for increased risk of bleeding during concomitant therapy.
LinezolidCombination associated with possible serotoninergic syndrome
LithiumThe SSRI, fluvoxamine, increases serum levels of lithium.
MazindolRisk of serotoninergic syndrome
MephenytoinIncreases the effect of hydantoin
MesoridazineIncreased risk of cardiotoxicity and arrhythmias
MethadoneFluvoxamine increases the effect and toxicity of methadone
MethamphetamineRisk of serotoninergic syndrome
MexiletineFluvoxamine may increase the therapeutic and adverse effects of mexiletine.
MirtazapineFluvoxamine may increase the therapeutic and adverse effects of mirtazapine.
MoclobemideIncreased incidence of adverse effects with this association
NaratriptanIncreased risk of CNS adverse effects
NortriptylineThe 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.
OlanzapineFluvoxamine increases the effect and toxicity of olanzapine
OxtriphyllineFluvoxamine may increase the therapeutic and adverse effects of oxtriphylline.
OxycodoneIncreased risk of serotonin syndrome
PhendimetrazineRisk of serotoninergic syndrome
PhenelzinePossible severe adverse reaction with this combination
PhentermineRisk of serotoninergic syndrome
PhenylpropanolamineRisk of serotoninergic syndrome
PhenytoinFluvoxamine may increase the therapeutic effect of phenytoin.
ProtriptylineThe 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.
RamelteonFluvoxamine may increase the serum level and toxicity of ramelteon.
RasagilinePossible severe adverse reaction with this combination
RizatriptanIncreased risk of CNS adverse effects
RoflumilastIncreases roflumilast levels.
RopiniroleIncreases the effect and toxicity of ropinirole
RopivacaineIncreases the effect and toxicity of ropivacaine
SelegilinePossible severe adverse reaction with this combination
SibutramineRisk of serotoninergic syndrome
St. John's WortSt. John's Wort increases the effect and toxicity of the SSRI, fluvoxamine.
SumatriptanIncreased risk of CNS adverse effects
TacrineFluvoxamine, 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.
TerbinafineTerbinafine 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.
TerfenadineIncreased risk of cardiotoxicity and arrhythmias
TheophyllineFluvoxamine may increase the therapeutic and adverse effects of theophylline.
ThiabendazoleThe 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.
ThioridazineIncreased risk of cardiotoxicity and arrhythmias
ThiothixeneThe 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 acidAdditive antiplatelet effects increase the risk of bleeding. Consider alternate therapy or monitor for increased bleeding.
TizanidineFluvoxamine inhibits the metabolism and clearance of tizanidine. Concomitant therapy is contraindicated.
TolmetinIncreased antiplatelet effects may enhance the risk of bleeding. Alternate therapy may be considered or monitor for inreased bleeding during concomitant therapy.
TramadolTramadol may increase the risk of serotonin syndrome and seizures.
TranylcypromineIncreased 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.
TrazodoneIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
TreprostinilThe prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Fluvoxamine. Monitor for increased bleeding during concomitant thearpy.
TrimipramineThe 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.
TriprolidineThe CNS depressants, Triprolidine and Fluvoxamine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
VenlafaxineIncreased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
WarfarinFluvoxamine may increase the anticoagulant effect of warfarin by increasing its serum concentration.
ZolmitriptanUse 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.
Food Interactions
  • Avoid alcohol.
  • Avoid high doses of caffeine.
  • Grapefruit and grapefruit juice should be avoided throughout treatment as grapefruit can significantly increase serum levels of this product.
  • Take without regard to meals.

1. Sodium-dependent serotonin transporter

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Sodium-dependent serotonin transporter P31645 Details

References:

  1. Kakiuchi T, Tsukada H, Fukumoto D, Nishiyama S: Effects of aging on serotonin transporter availability and its response to fluvoxamine in the living brain: PET study with [(11)C](+)McN5652 and [(11)C](-)McN5652 in conscious monkeys. Synapse. 2001 Jun 1;40(3):170-9. Pubmed
  2. Yoshida K, Ito K, Sato K, Takahashi H, Kamata M, Higuchi H, Shimizu T, Itoh K, Inoue K, Tezuka T, Suzuki T, Ohkubo T, Sugawara K, Otani K: Influence of the serotonin transporter gene-linked polymorphic region on the antidepressant response to fluvoxamine in Japanese depressed patients. Prog Neuropsychopharmacol Biol Psychiatry. 2002 Feb;26(2):383-6. Pubmed
  3. Miolo G, Caffieri S, Levorato L, Imbesi M, Giusti P, Uz T, Manev R, Manev H: Photoisomerization of fluvoxamine generates an isomer that has reduced activity on the 5-hydroxytryptamine transporter and does not affect cell proliferation. Eur J Pharmacol. 2002 Aug 30;450(3):223-9. Pubmed
  4. Suhara T, Takano A, Sudo Y, Ichimiya T, Inoue M, Yasuno F, Ikoma Y, Okubo Y: High levels of serotonin transporter occupancy with low-dose clomipramine in comparative occupancy study with fluvoxamine using positron emission tomography. Arch Gen Psychiatry. 2003 Apr;60(4):386-91. Pubmed
  5. Inoue K: [Analysis and its application for prevention of side-effects of drugs and for evaluation of drug responsiveness] Yakugaku Zasshi. 2004 Jun;124(6):293-9. Pubmed
  6. McMahon LR, Cunningham KA: Role of 5-HT and 5-HT receptors in the behavioral interactions between serotonin and catecholamine reuptake inhibitors. Neuropsychopharmacology. 2001 Mar;24(3):319-29. Pubmed
  7. Millan MJ, Veiga S, Girardon S, Brocco M: Blockade of serotonin 5-HT1B and 5-HT2A receptors suppresses the induction of locomotor activity by 5-HT reuptake inhibitors, citalopram and fluvoxamine, in NMRI mice exposed to a novel environment: a comparison to other 5-HT receptor subtypes. Psychopharmacology (Berl). 2003 Aug;168(4):397-409. Epub 2003 Apr 30. Pubmed
  8. Dell’Osso B, Allen A, Hollander E: Fluvoxamine: a selective serotonin re-uptake inhibitor for the treatment of obsessive-compulsive disorder. Expert Opin Pharmacother. 2005 Dec;6(15):2727-40. Pubmed
  9. Irons J: Fluvoxamine in the treatment of anxiety disorders. Neuropsychiatr Dis Treat. 2005 Dec;1(4):289-99. Pubmed
  10. Williams K, Wheeler DM, Silove N, Hazell P: Selective serotonin reuptake inhibitors (SSRIs) for autism spectrum disorders (ASD). Cochrane Database Syst Rev. 2010 Aug 4;8:CD004677. Pubmed

1. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Baumann P: Pharmacokinetic-pharmacodynamic relationship of the selective serotonin reuptake inhibitors. Clin Pharmacokinet. 1996 Dec;31(6):444-69. Pubmed
  2. Rasmussen BB, Brosen K: Is therapeutic drug monitoring a case for optimizing clinical outcome and avoiding interactions of the selective serotonin reuptake inhibitors? Ther Drug Monit. 2000 Apr;22(2):143-54. Pubmed
  3. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  4. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  5. Lexicomp.

2. Cytochrome P450 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

References:

  1. Rasmussen BB, Nielsen TL, Brosen K: Fluvoxamine is a potent inhibitor of the metabolism of caffeine in vitro. Pharmacol Toxicol. 1998 Dec;83(6):240-5. Pubmed
  2. Baumann P: Pharmacokinetic-pharmacodynamic relationship of the selective serotonin reuptake inhibitors. Clin Pharmacokinet. 1996 Dec;31(6):444-69. Pubmed
  3. Brosen K: Drug interactions and the cytochrome P450 system. The role of cytochrome P450 1A2. Clin Pharmacokinet. 1995;29 Suppl 1:20-5. Pubmed
  4. Micallef J, Fakra E, Blin O: [Use of antidepressant drugs in schizophrenic patients with depression] Encephale. 2006 Mar-Apr;32(2 Pt 1):263-9. Pubmed
  5. Rasmussen BB, Brosen K: Is therapeutic drug monitoring a case for optimizing clinical outcome and avoiding interactions of the selective serotonin reuptake inhibitors? Ther Drug Monit. 2000 Apr;22(2):143-54. Pubmed
  6. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  7. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  8. Yasui-Furukori N, Inoue Y, Kaneko S, Otani K: Determination of fluvoxamine and its metabolite fluvoxamino acid by liquid-liquid extraction and column-switching high-performance liquid chromatography. J Pharm Biomed Anal. 2005 Feb 7;37(1):121-5. Pubmed
  9. Lexicomp.

3. Cytochrome P450 2E1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2E1 P05181 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

4. Cytochrome P450 1A1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 1A1 P04798 Details

References:

  1. Baumann P: Pharmacokinetic-pharmacodynamic relationship of the selective serotonin reuptake inhibitors. Clin Pharmacokinet. 1996 Dec;31(6):444-69. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

5. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Baumann P: Pharmacokinetic-pharmacodynamic relationship of the selective serotonin reuptake inhibitors. Clin Pharmacokinet. 1996 Dec;31(6):444-69. Pubmed
  2. Micallef J, Fakra E, Blin O: [Use of antidepressant drugs in schizophrenic patients with depression] Encephale. 2006 Mar-Apr;32(2 Pt 1):263-9. Pubmed
  3. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  4. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  5. Lexicomp.

6. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

7. Cytochrome P450 3A7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A7 P24462 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

8. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

References:

  1. Micallef J, Fakra E, Blin O: [Use of antidepressant drugs in schizophrenic patients with depression] Encephale. 2006 Mar-Apr;32(2 Pt 1):263-9. Pubmed
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed
  3. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  4. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  5. Lexicomp.

9. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

References:

  1. Baumann P: Pharmacokinetic-pharmacodynamic relationship of the selective serotonin reuptake inhibitors. Clin Pharmacokinet. 1996 Dec;31(6):444-69. Pubmed
  2. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  3. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  4. Lexicomp.

10. Cytochrome P450 2B6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2B6 P20813 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  2. Lexicomp.

1. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. Pubmed
  2. Weiss J, Dormann SM, Martin-Facklam M, Kerpen CJ, Ketabi-Kiyanvash N, Haefeli WE: Inhibition of P-glycoprotein by newer antidepressants. J Pharmacol Exp Ther. 2003 Apr;305(1):197-204. Pubmed

Comments
Drug created on June 13, 2005 07:24 / Updated on September 23, 2013 23:37