DGIdb - VENLAFAXINE Drug Record

VENLAFAXINE chembl:CHEMBL637 Approved

Alternate Names:

SUNVENIZ XL
VAXALIN XL
VEXARIN XL
RANFAXINE XL
EFFEXOR
ALVENTA XL
VENLABLUE XL
EFEXOR
FORAVEN XL
TIFAXIN XL
VENLANEO XL
RODOMEL XL
VENSIR XL
VIEPAX
MENTAVEN XL
TONPULAR XL
BONILUX XL
VENLADEX XL
VENAXX XL
TRIXAT XL
AMPHERO XL
DEPEFEX XL
TARDCAPS XL
WINFEX XL
EFEXOR XL
VENLAFAXINE
VENLALIC XL
VIEPAX XL
POLITID XL
TREVILOR
WY-45030
VENLAFAXIN
ELAFAX
EFECTIN
VENLAFEXINE
1-[2-(DIMETHYLAMINO)-1-(4-METHOXYPHENYL)ETHYL]CYCLOHEXAN-1-OL
EFFEXOR®
rxcui:39786
drugbank:00285
pubchem.compound:5656
chembl:CHEMBL637
chemidplus:93413-69-5

Drug Info:

Drug Categories	serotonin and noradrenaline reuptake inhibitors
Drug Categories	fatty alcohols
Drug Categories	cyclohexanols
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antidepressant
Drug Class	antidepressive agents, second-generation
Year of Approval	1993
Drug Categories	agents producing tachycardia
Drug Categories	agents that reduce seizure threshold
Drug Categories	bcrp/abcg2 inducers
Drug Categories	central nervous system depressants
Drug Categories	combined inhibitors of serotonin/norepinephrine reuptake
Drug Categories	cytochrome p-450 cyp2d6 inhibitors (weak)
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	drugs that are mainly renally excreted
Drug Categories	hypoglycemia-associated agents
Drug Categories	norepinephrine uptake inhibitors
Drug Categories	p-glycoprotein inhibitors
Drug Categories	p-glycoprotein substrates
Drug Categories	potential qtc-prolonging agents
Drug Categories	qtc prolonging agents
Drug Categories	serotonergic drugs shown to increase risk of serotonin syndrome
Drug Categories	serotonin agents

(5 More Sources)

Publications:

Dawson et al., 1999, Effects of venlafaxine on extracellular concentrations of 5-HT and noradrenaline in the rat frontal cortex: augmentation via 5-HT1A receptor antagonism., Neuropharmacology
Lemke, 2007, [Antidepressant effects of dopamine agonists. Experimental and clinical findings]., Nervenarzt
Barkin et al., 2000, The management challenges of chronic pain: the role of antidepressants., Am J Ther
Bourin, 1999, [Psychopharmacological profile of venlafaxine]., Encephale
Van Ameringen et al., 2009, Pharmacotherapy for social anxiety disorder: an update., Isr J Psychiatry Relat Sci
Shang et al., 2007, Displacement of serotonin and dopamine transporters by venlafaxine extended release capsule at steady state: a [123I]2beta-carbomethoxy-3beta-(4-iodophenyl)-tropane single photon emission computed tomography imaging study., J Clin Psychopharmacol
Westenberg, 2009, Recent advances in understanding and treating social anxiety disorder., CNS Spectr
Malizia et al., 1997, Demonstration of clomipramine and venlafaxine occupation at serotonin reuptake sites in man in vivo., J. Psychopharmacol. (Oxford)
Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
Sindrup et al., 2005, Antidepressants in the treatment of neuropathic pain., Basic Clin. Pharmacol. Toxicol.
Gould et al., 2006, A comparison of the chronic treatment effects of venlafaxine and other antidepressants on serotonin and norepinephrine transporters., Biol. Psychiatry
Béïque et al., 2000, Effects of sustained administration of the serotonin and norepinephrine reuptake inhibitor venlafaxine: I. in vivo electrophysiological studies in the rat., Neuropharmacology
Bymaster et al., 2001, Comparative affinity of duloxetine and venlafaxine for serotonin and norepinephrine transporters in vitro and in vivo, human serotonin receptor subtypes, and other neuronal receptors., Neuropsychopharmacology
Chen et al., 2005, The S-enantiomer of R,S-citalopram, increases inhibitor binding to the human serotonin transporter by an allosteric mechanism. Comparison with other serotonin transporter inhibitors., Eur Neuropsychopharmacol
Béïque et al., 1998, Affinities of venlafaxine and various reuptake inhibitors for the serotonin and norepinephrine transporters., Eur. J. Pharmacol.
Mitchell et al., 2006, The effects of norepinephrine transporter inactivation on locomotor activity in mice., Biol. Psychiatry
Vaishnavi et al., 2004, Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity., Biol. Psychiatry
Marshe VS et al., 2017, Norepinephrine Transporter Gene Variants and Remission From Depression With Venlafaxine Treatment in Older Adults., Am J Psychiatry
Pu M et al., 2013, Influence of genetic polymorphisms in the glutamatergic and GABAergic systems and their interactions with environmental stressors on antidepressant response., Pharmacogenomics
Millan et al., 2004, S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: III. Actions in models of potential antidepressive and anxiolytic activity in comparison with ropinirole., J. Pharmacol. Exp. Ther.
Tzvetkov MV et al., 2008, Common genetic variations in human brain-specific tryptophan hydroxylase-2 and response to antidepressant treatment., Pharmacogenet Genomics
Perroud N et al., 2011, Clinical and genetic correlates of suicidal ideation during antidepressant treatment in a depressed outpatient sample., Pharmacogenomics
Kirchheiner J et al., 2008, Genetic variants in FKBP5 affecting response to antidepressant drug treatment., Pharmacogenomics
Zou YF et al., 2010, Meta-analysis of FKBP5 gene polymorphisms association with treatment response in patients with mood disorders., Neurosci Lett
Sarginson JE et al., 2010, FKBP5 polymorphisms and antidepressant response in geriatric depression., Am J Med Genet B Neuropsychiatr Genet
Binder EB et al., 2004, Polymorphisms in FKBP5 are associated with increased recurrence of depressive episodes and rapid response to antidepressant treatment., Nat Genet
Niitsu T et al., 2013, Pharmacogenetics in major depression: a comprehensive meta-analysis., Prog Neuropsychopharmacol Biol Psychiatry
Papiol S et al., 2007, Genetic variability at HPA axis in major depression and clinical response to antidepressant treatment., J Affect Disord
Lohoff FW et al., 2013, Serotonin receptor 2A (HTR2A) gene polymorphism predicts treatment response to venlafaxine XR in generalized anxiety disorder., Pharmacogenomics J
Huang X et al., 2013, ABCB6, ABCB1 and ABCG1 genetic polymorphisms and antidepressant response of SSRIs in Chinese depressive patients., Pharmacogenomics
Uhr M et al., 2008, Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression., Neuron
Breitenstein B et al., 2016, Association of ABCB1 gene variants, plasma antidepressant concentration, and treatment response: Results from a randomized clinical study., J Psychiatr Res
Moresco M et al., 2016, Pharmacogenetics and Treatment Response in Narcolepsy Type 1: Relevance of the Polymorphisms of the Drug Transporter Gene ABCB1., Clin Neuropharmacol
de Klerk OL et al., 2013, ABCB1 gene variants influence tolerance to selective serotonin reuptake inhibitors in a large sample of Dutch cases with major depressive disorder., Pharmacogenomics J
Jeleń AM et al., 2015, The Influence of C3435T Polymorphism of the ABCB1 Gene on Genetic Susceptibility to Depression and Treatment Response in Polish Population - Preliminary Report., Int J Med Sci
Narasimhan S et al., 2012, Variation in the catechol-O-methyltransferase (COMT) gene and treatment response to venlafaxine XR in generalized anxiety disorder., Psychiatry Res
Taranu A et al., 2017, The Catechol-O-methyltransferase Val(108/158)Met Genetic Polymorphism cannot be Recommended as a Biomarker for the Prediction of Venlafaxine Efficacy in Patients Treated in Psychiatric Settings., Basic Clin Pharmacol Toxicol
Hopkins SC et al., 2013, Catechol-O-methyltransferase genotype as modifier of superior responses to venlafaxine treatment in major depressive disorder., Psychiatry Res
Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem

VENLAFAXINE FKBP5

Interaction Score: 2.37

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18597649 21449676 20709156 19676097 15565110 23733030 17467808

Sources:
PharmGKB
VENLAFAXINE TPH2

Interaction Score: 0.89

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18496129

Sources:
PharmGKB
VENLAFAXINE SLC6A2

Interaction Score: 0.64

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Effexor

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
19728573 9669506 16893531 14744476 19238127 15910402 10884561 11750180 28068779

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology
VENLAFAXINE SLC6A4

Interaction Score: 0.56

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
19728573 17224717 19238127 9305421 9537821 15910402 16140280 10884561 11750180 15695064

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology
VENLAFAXINE COMT

Interaction Score: 0.37

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22417933 28627776 23706899

Sources:
PharmGKB
VENLAFAXINE GRIA3

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23394390

Sources:
PharmGKB
VENLAFAXINE SLC6A3

Interaction Score: 0.22

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10462128 17187269 11319571 10434156

Sources:
DrugBank
VENLAFAXINE GABRQ

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23394390

Sources:
PharmGKB
VENLAFAXINE GABRP

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23394390

Sources:
PharmGKB
VENLAFAXINE ABCB1

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24192121 18215618 21449676 26704739 26757307 22641028 26664259

Sources:
PharmGKB
VENLAFAXINE BDNF

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14978196

Sources:
NCI
VENLAFAXINE HTR1B

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21449676

Sources:
PharmGKB
VENLAFAXINE GABRA6

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23394390

Sources:
PharmGKB
VENLAFAXINE CYP3A5

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18695978

Sources:
PharmGKB
VENLAFAXINE HTR2A

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22006095

Sources:
PharmGKB
VENLAFAXINE CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA

DrugBank: DB00285

Version: 5.1.7

Alternate Names:

93413-69-5 CAS Number

Act Venlafaxine XR Drug Brand

Apo-venlafaxine XR Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories agents producing tachycardia

Publications:

Dawson et al., 1999, Effects of venlafaxine on extracellular concentrations of 5-HT and noradrenaline in the rat frontal cortex: augmentation via 5-HT1A receptor antagonism., Neuropharmacology

Lemke, 2007, [Antidepressant effects of dopamine agonists. Experimental and clinical findings]., Nervenarzt

Barkin et al., 2000, The management challenges of chronic pain: the role of antidepressants., Am J Ther

TdgClinicalTrial: VENLAFAXINE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antidepressant

Drug Class Small Molecule

FDA Approval approved

Publications:
TEND: VENLAFAXINE
- Version: 01-August-2011
Alternate Names:

Drug Info:

Year of Approval 1993

Drug Class antidepressive agents, second-generation

Publications:

NCI: VENLAFAXINE

Version: 14-September-2017

Alternate Names:

C1278 NCI drug code

Drug Info:

Publications:

Millan et al., 2004, S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: III. Actions in models of potential antidepressive and anxiolytic activity in comparison with ropinirole., J. Pharmacol. Exp. Ther.

PharmGKB: venlafaxine

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Tzvetkov MV et al., 2008, Common genetic variations in human brain-specific tryptophan hydroxylase-2 and response to antidepressant treatment., Pharmacogenet Genomics

Pu M et al., 2013, Influence of genetic polymorphisms in the glutamatergic and GABAergic systems and their interactions with environmental stressors on antidepressant response., Pharmacogenomics

Marshe VS et al., 2017, Norepinephrine Transporter Gene Variants and Remission From Depression With Venlafaxine Treatment in Older Adults., Am J Psychiatry

TTD: Venlafaxine
- Version: 2020.06.01
Alternate Names:

D0P1UX TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL637
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
GuideToPharmacology: 178103894
- Version: 29-September-2020
Alternate Names:

Drug Info:

Publications:
FDA: Venlafaxine
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

Trial Name	Effexor
Novel drug target	Established target
Specific Action of the Ligand	Inhibition

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	True

93413-69-5	CAS Number
Act Venlafaxine XR	Drug Brand
Apo-venlafaxine XR	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	agents producing tachycardia

VENLAFAXINE Drug Record

VENLAFAXINE chembl:CHEMBL637 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18597649 21449676 20709156 19676097 15565110 23733030 17467808

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18496129

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Effexor Novel drug target Established target Specific Action of the Ligand Inhibition

PMIDs: 19728573 9669506 16893531 14744476 19238127 15910402 10884561 11750180 28068779

Sources: TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

PMIDs: 19728573 17224717 19238127 9305421 9537821 15910402 16140280 10884561 11750180 15695064

Sources: TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22417933 28627776 23706899

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23394390

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 10462128 17187269 11319571 10434156

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23394390

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23394390

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24192121 18215618 21449676 26704739 26757307 22641028 26664259

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14978196

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 21449676

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23394390

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18695978

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22006095

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA

DrugBank: DB00285

Alternate Names: 93413-69-5 CAS Number Act Venlafaxine XR Drug Brand Apo-venlafaxine XR Drug Brand

Drug Info: Drug Type small molecule Drug Groups approved Drug Categories agents producing tachycardia

TdgClinicalTrial: VENLAFAXINE

Alternate Names:

Drug Info: Drug Indications antidepressant Drug Class Small Molecule FDA Approval approved

Publications:

TEND: VENLAFAXINE

Alternate Names:

Drug Info: Year of Approval 1993 Drug Class antidepressive agents, second-generation

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
18597649 21449676 20709156 19676097 15565110 23733030 17467808

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18496129

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Effexor

Novel drug target Established target

Specific Action of the Ligand Inhibition

PMIDs:
19728573 9669506 16893531 14744476 19238127 15910402 10884561 11750180 28068779

Sources:
TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
19728573 17224717 19238127 9305421 9537821 15910402 16140280 10884561 11750180 15695064

Sources:
TEND TdgClinicalTrial DrugBank GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
22417933 28627776 23706899

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23394390

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
10462128 17187269 11319571 10434156

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
23394390

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23394390

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
24192121 18215618 21449676 26704739 26757307 22641028 26664259

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
14978196

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
21449676

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23394390

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
18695978

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
22006095

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA

Alternate Names:

93413-69-5 CAS Number

Act Venlafaxine XR Drug Brand

Apo-venlafaxine XR Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories agents producing tachycardia

Drug Info:

Drug Indications antidepressant

Drug Class Small Molecule

FDA Approval approved

Drug Info:

Year of Approval 1993

Drug Class antidepressive agents, second-generation

Alternate Names:

C1278 NCI drug code

Publications:

Millan et al., 2004, S32504, a novel naphtoxazine agonist at dopamine D3/D2 receptors: III. Actions in models of potential antidepressive and anxiolytic activity in comparison with ropinirole., J. Pharmacol. Exp. Ther.

Alternate Names:

D0P1UX TTD Drug ID