VENLAFAXINE

Details

Stereochemistry	RACEMIC
Molecular Formula	C17H27NO2
Molecular Weight	277.4018
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=CC=C(C=C1)C(CN(C)C)C2(O)CCCCC2

InChI

InChIKey=PNVNVHUZROJLTJ-UHFFFAOYSA-N

InChI=1S/C17H27NO2/c1-18(2)13-16(17(19)11-5-4-6-12-17)14-7-9-15(20-3)10-8-14/h7-10,16,19H,4-6,11-13H2,1-3H3

HIDE SMILES / InChI

Molecular Formula	C17H27NO2
Molecular Weight	277.4018
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s015lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/16140280

Venlafaxine is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor, which is sold under several brand names; one of them is venlafaxine hydrochloride. Venlafaxine hydrochloride is a venlafaxine extended release tablets, which are indicated for the treatment of major depressive disorder (MDD). Efficacy of venlafaxine in MDD was shown in both short-term trials and a longer-term trial in MDD. A major depressive episode (DSM-IV) implies a prominent and relatively persistent depressed mood or the loss of interest or pleasure in nearly all activities, representing a change from previous functioning, and includes the presence of at least five of the following nine symptoms during the same two-week period. In addition, venlafaxine hydrochloride is indicated for the treatment of social anxiety (SAD), also known as social phobia. Social Anxiety Disorder (DSM-IV) is characterized by a marked and persistent fear of 1 or more social or performance situations in which others expose to unfamiliar people or to possible scrutiny the person. Exposure to the feared situation almost invariably provokes anxiety, which may approach the intensity of a panic attack. The feared situations are avoided or endured with intense anxiety or distress. The mechanism of the antidepressant action of venlafaxine in humans is believed to be associated with its potentiation of neurotransmitter activity in the CNS. Preclinical studies have shown that venlafaxine and its active metabolite, O-desmethylvenlafaxine (ODV), are potent inhibitors of neuronal serotonin and norepinephrine reuptake and weak inhibitors of dopamine reuptake.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Norepinephrine transporter 191 Target ID: CHEMBL222 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16140280	Inhibitor 8297		1.26 µM [Ki]
Serotonin transporter 178 Target ID: CHEMBL228 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16140280	Inhibitor 8297		74.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Major depressive disorder 173 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s015lbl.pdf	Primary		Approved 8429	VENLAFAXINE HYDROCHLORIDE Approved Use Major Depressive Disorder Venlafaxine Extended Release Tablets (venlafaxine hydrochloride) are indicated for the treatment of major depressive disorder (MDD). Efficacy of venlafaxine in MDD was shown in both short-term trials and a longer-term trial in MDD. A major depressive episode (DSM-IV) implies a prominent and relatively persistent (nearly every day for at least 2 weeks) depressed mood or the loss of interest or pleasure in nearly all activities, representing a change from previous functioning, and includes the presence of at least five of the following nine symptoms during the same two-week period: depressed mood, markedly diminished interest or pleasure in usual activities, significant change in weight and/or appetite, insomnia or hypersomnia, psychomotor agitation or retardation, increased fatigue, feelings of guilt or worthlessness, slowed thinking or impaired concentration, a suicide attempt or suicidal ideation. Social Anxiety Disorder Venlafaxine Extended Release Tablets are indicated for the treatment of Social Anxiety Disorder (SAD), also known as Social Phobia, as defined in DSM-IV. Social Anxiety Disorder (DSM-IV) is characterized by a marked and persistent fear of 1 or more social or performance situations in which the person is exposed to unfamiliar people or to possible scrutiny by others. Exposure to the feared situation almost invariably provokes anxiety, which may approach the intensity of a panic attack. The feared situations are avoided or endured with intense anxiety or distress. The avoidance, anxious anticipation, or distress in the feared situation(s) interferes significantly with the person's normal routine, occupational or academic functioning, or social activities or relationships, or there is a marked distress about having the phobias. Lesser degrees of performance anxiety or shyness generally do not require psychopharmacological treatment. Launch Date 2008
Social anxiety disorder 12 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s015lbl.pdf	Primary		Approved 8429	VENLAFAXINE HYDROCHLORIDE Approved Use Major Depressive Disorder Venlafaxine Extended Release Tablets (venlafaxine hydrochloride) are indicated for the treatment of major depressive disorder (MDD). Efficacy of venlafaxine in MDD was shown in both short-term trials and a longer-term trial in MDD. A major depressive episode (DSM-IV) implies a prominent and relatively persistent (nearly every day for at least 2 weeks) depressed mood or the loss of interest or pleasure in nearly all activities, representing a change from previous functioning, and includes the presence of at least five of the following nine symptoms during the same two-week period: depressed mood, markedly diminished interest or pleasure in usual activities, significant change in weight and/or appetite, insomnia or hypersomnia, psychomotor agitation or retardation, increased fatigue, feelings of guilt or worthlessness, slowed thinking or impaired concentration, a suicide attempt or suicidal ideation. Social Anxiety Disorder Venlafaxine Extended Release Tablets are indicated for the treatment of Social Anxiety Disorder (SAD), also known as Social Phobia, as defined in DSM-IV. Social Anxiety Disorder (DSM-IV) is characterized by a marked and persistent fear of 1 or more social or performance situations in which the person is exposed to unfamiliar people or to possible scrutiny by others. Exposure to the feared situation almost invariably provokes anxiety, which may approach the intensity of a panic attack. The feared situations are avoided or endured with intense anxiety or distress. The avoidance, anxious anticipation, or distress in the feared situation(s) interferes significantly with the person's normal routine, occupational or academic functioning, or social activities or relationships, or there is a marked distress about having the phobias. Lesser degrees of performance anxiety or shyness generally do not require psychopharmacological treatment. Launch Date 2008

C_max

Value	Dose	Analyte	Population
260 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESVENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
97.9 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	75 mg 1 times / day steady-state, oral dose: 75 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESVENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
26.9 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	75 mg 1 times / day steady-state, oral dose: 75 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
150 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED

AUC

Value	Dose	Co-administered	Analyte	Population
2926 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	75 mg 1 times / day steady-state, oral dose: 75 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		DESVENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
1536.3 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	75 mg 1 times / day steady-state, oral dose: 75 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		VENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED

T_1/2

Value	Dose	Analyte	Population
12.5 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESVENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
12.5 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	75 mg 1 times / day steady-state, oral dose: 75 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESVENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
7.5 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	75 mg 1 times / day steady-state, oral dose: 75 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
10.7 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED

F_unbound

Value	Dose	Analyte	Population
70% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESVENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
70% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	75 mg 1 times / day steady-state, oral dose: 75 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DESVENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
73% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	75 mg 1 times / day steady-state, oral dose: 75 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
73% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s016lbl.pdf	150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VENLAFAXINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED

Doses

Dose	Population	Adverse events
225 mg 1 times / day multiple, oral Recommended Dose: 225 mg, 1 times / day Route: oral Route: multiple Dose: 225 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s015lbl.pdf	unhealthy, adult n = 277 Health Status: unhealthy Condition: Social Anxiety Disorder Age Group: adult Population Size: 277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s015lbl.pdf	Other AEs: Headache, Asthenia... Other AEs: Headache (34%) Asthenia (17%) Flu syndrome (6%) Accidental injury (5%) Abdominal pain (4%) Hypertension (5%) Vasodilatation (3%) Palpitation (3%) Nausea (29%) Anorexia (20%) Constipation (8%) Diarrhea (6%) Vomiting (3%) Eructation (2%) Weight loss (4%) Insomnia (23%) Dry mouth (17%) Dizziness (16%) Somnolence (16%) Nervousness (11%) Libido decreased (9%) Anxiety (5%) Agitation (4%) Tremor (4%) Abnormal dreams (4%) Paresthesia (3%) Twitching (2%) Yawn (5%) Sinusitis (2%) Sweating (13%) Abnormal vision (6%) Abnormal ejaculation (16%) Impotence (10%) Orgasmic disorders and disturbances (8%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s015lbl.pdf
225 mg 1 times / day multiple, oral Recommended Dose: 225 mg, 1 times / day Route: oral Route: multiple Dose: 225 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s015lbl.pdf	unhealthy, adult n = 357 Health Status: unhealthy Condition: Major Depressive Disorder Age Group: adult Population Size: 357 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s015lbl.pdf	Other AEs: Asthenia, Vasodilatation... Other AEs: Asthenia (8%) Vasodilatation (4%) Hypertension (4%) Nausea (31%) Constipation (8%) Anorexia (8%) Vomiting (4%) Flatulence (4%) Weight loss (3%) Dizziness (20%) Somnolence (17%) Insomnia (17%) Dry mouth (12%) Nervousness (10%) Abnormal dreams (7%) Tremor (5%) Depression (3%) Paresthesia (3%) Libido decreased (3%) Agitation (3%) Pharyngitis (7%) Yawn (3%) Sweating (14%) Abnormal vision (4%) Abnormal ejaculation (16%) Impotence (4%) Inhibited female orgasm (3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022104s015lbl.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587	substrate 1037	substrate 1217 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
Nav1.5 97 P-gp 1461 CYP1A2 1524 CYP2C 19	CYP2C19 991 P-gp 1537	P-gp 257 BCRP 75 OCT1 35 MRP2 111 OATP1B1 26 CYP1A2 701

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 1692	inhibitor 3277 Sources: https://onlinelibrary.wiley.com/doi/10.1002/(SICI)1520-6394(1998)7:1+%3C24::AID-DA7%3E3.0.CO;2-F	minimal or no
CYP2C 34	inhibitor 3277 Sources: https://onlinelibrary.wiley.com/doi/10.1002/(SICI)1520-6394(1998)7:1+%3C24::AID-DA7%3E3.0.CO;2-F	minimal or no
CYP3A4 1925	inhibitor 3277 Sources: https://onlinelibrary.wiley.com/doi/10.1002/(SICI)1520-6394(1998)7:1+%3C24::AID-DA7%3E3.0.CO;2-F	minimal or no
P-gp 1650	inhibitor 3277 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3268186/	no [IC50 >100 uM]
CYP2D6 1891	inhibitor 3277 Sources: https://onlinelibrary.wiley.com/doi/10.1002/(SICI)1520-6394(1998)7:1+%3C24::AID-DA7%3E3.0.CO;2-F	weak	yes (co-administration study) Comment: info taken from abstract; Coadministration with risperidone increased AUC of risperidone by 32%. See https://pubmed.ncbi.nlm.nih.gov/24964257/ Sources: https://onlinelibrary.wiley.com/doi/10.1002/(SICI)1520-6394(1998)7:1+%3C24::AID-DA7%3E3.0.CO;2-F
BCRP 773	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/23897419/	yes
CYP1A2 1692	inducer 1573 Sources: https://www.tandfonline.com/doi/abs/10.3109/00498254.2014.955831	yes
MRP2 475	inducer 1573 Sources: https://www.tandfonline.com/doi/abs/10.3109/00498254.2014.955831	yes
OATP1B1 803	inducer 1573 Sources: https://www.tandfonline.com/doi/abs/10.3109/00498254.2014.955831	yes
OCT1 543	inducer 1573 Sources: https://www.tandfonline.com/doi/abs/10.3109/00498254.2014.955831	yes
P-gp 1650	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/23897419/	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020699ap_effexor_clinphrmr_admindoc_.pdf#page=7 Page: 7.0	inconclusive	yes (co-administration study) Comment: Coadministration with ketoconazole (CYP3A4 inhibitor) increased AUC by 70%. See https://pubmed.ncbi.nlm.nih.gov/24964257/ Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020699ap_effexor_clinphrmr_admindoc_.pdf#page=7 Page: 7.0
P-gp 1537	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3268186/	no
CYP2C19 991	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/10192828/	yes	weak (co-administration study) Comment: Coadministration with voriconazole (CYP2C9 inhibitor) increased AUC by 31%. See https://pubmed.ncbi.nlm.nih.gov/24964257/ Sources: https://pubmed.ncbi.nlm.nih.gov/10192828/
CYP2C9 1037	substrate 3367 Sources: https://pubmed.ncbi.nlm.nih.gov/10192828/	yes	weak (co-administration study) Comment: Coadministration with voriconazole (CYP2C9 inhibitor) increased AUC by 31%. See https://pubmed.ncbi.nlm.nih.gov/24964257/ Sources: https://pubmed.ncbi.nlm.nih.gov/10192828/
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020699s110s111lbl.pdf#page=27 Page: 27.0	yes	yes (co-administration study) Comment: Coadministration with diphenhydramine increased AUC 2-fold; Coadministration with ketoconazole increased AUc by 70%. See https://pubmed.ncbi.nlm.nih.gov/24964257/ Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020699s110s111lbl.pdf#page=27 Page: 27.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
Nav1.5 100	inhibitor 1626 Sources: https://www.sciencedirect.com/science/article/abs/pii/S0014299916302874?via%3Dihub
hERG 1647	inhibitor 1626 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3002179/

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:9943	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:9943
ChemicalBook	CB42567671	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB42567671
ChemicalBook	CB7136180	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB7136180
MolPort	MolPort-003-666-534	https://www.molport.com/shop/molecule-link/MolPort-003-666-534
eMolecules	902654	https://www.emolecules.com/cgi-bin/more?vid=902654

PubMed

Title	Date	PubMed
Antidepressant efficacy of venlafaxine.	2000	11098413
Attaining remission in generalized anxiety disorder: venlafaxine extended release comparative data.	2001	11577788
Hormone replacement in women with a history of breast cancer.	2001	11524554
Venlafaxine extended-release: a review of its use in the management of major depression.	2001	11524036
Separation anxiety disorder in children and adolescents: epidemiology, diagnosis and management.	2001	11460893
Mania resulting from continuous positive airways pressure in a depressed man with sleep apnea syndrome.	2001	11287803
Possible neurobiological mechanisms underlying faster onset of antidepressant action.	2001	11229789
Incidence of sexual dysfunction associated with antidepressant agents: a prospective multicenter study of 1022 outpatients. Spanish Working Group for the Study of Psychotropic-Related Sexual Dysfunction.	2001	11229449
Asymptomatic QTc prolongation associated with quetiapine fumarate overdose in a patient being treated with risperidone.	2001 Apr	11393275
Specific effect of venlafaxine on single and repetitive experimental painful stimuli in humans.	2001 Apr	11309553
Anti-Inflammatory effects of antidepressants through suppression of the interferon-gamma/interleukin-10 production ratio.	2001 Apr	11270917
[Serotonin-noradrenaline reuptake inhibitors(SNRIs)].	2001 Aug	11519152
[14C]Serotonin uptake and [O-methyl-11C]venlafaxine kinetics in porcine brain.	2001 Aug	11518644
Flushing in a menopausal woman taking venlafaxine.	2001 Aug	11481177
Screening for detection of new antidepressants, neuroleptics, hypnotics, and their metabolites in urine by GC-MS developed using rat liver microsomes.	2001 Feb	11206046
In vitro effects of St. John's wort extract and hyperforin on 5 HT uptake and efflux in human blood platelets.	2001 Jul	11518065
[Depressive disorders and antidepressive therapy. A comparison of neurology practice and psychiatric clinic].	2001 Jul	11478223
Neuroimaging profiles and the differential therapies of depression.	2001 Jul	11448371
Functional brain circuits in major depression and remission.	2001 Jul	11448370
Even low-dose treatment of venlafaxine may provoke recurrence of hypertension in an Asian patient?	2001 Jul-Aug	11569474
The health economic impact of antidepressant usage from a payer's perspective: a multinational study.	2001 Jun	11452675
Antidepressant discontinuation (withdrawal) symptoms presenting as 'stroke'.	2001 Jun	11448088
Venlafaxine withdrawal syndrome not prevented by maprotiline, but resolved by sertraline.	2001 Mar	11343628
[Psychiatric manifestations of a new variant of Creutzfeldt-Jakob disease. Apropos of a case].	2001 Mar-Apr	11407273
Recurrent depression with vagus nerve stimulation.	2001 May	11329411
The combined use of bupropion, lithium, and venlafaxine during ECT: a case of prolonged seizure activity.	2001 Sep	11528316
Long-term outcome after ECT for catatonic depression.	2001 Sep	11528308
Postmortem tissue concentrations of venlafaxine.	2001 Sep 15	11516890
Critical use of venlafaxine serology to uncover genetic rapid metabolism.	2001 Winter	11207339

Patents

Sample Use Guides

In Vivo Use Guide

Major Depressive Disorder: for most patients, the recommended starting dose for Venlafaxine Extended Release Tablets is 75 mg/day, administered in a single dose. In the clinical trials establishing the efficacy of venlafaxine hydrochloride extended-release capsules in moderately depressed outpatients, the initial dose of venlafaxine was 75 mg/day. For some patients, it may be desirable to start at 37.5 mg/day for 4 to 7 days, to allow new patients to adjust to the medication before increasing to 75 mg/day. While the relationship between dose and antidepressant response for venlafaxine hydrochloride extended-release capsules has not been adequately explored, patients not responding to the initial 75 mg/day dose may benefit from dose increases to a maximum of approximately 225 mg/day. Dose increases should be in increments of up to 75 mg/day, as needed, and should be made at intervals of not less than 4 days, since steady state plasma levels of venlafaxine and its major metabolites are achieved in most patients by day 4. In the clinical trials establishing efficacy, upward titration was permitted at intervals of 2 weeks or more; the average doses were about 140 to 180 mg/day. It should be noted that, while the maximum recommended dose for moderately depressed outpatients is also 225 mg/day for venlafaxine hydrochloride immediate-release tablets, more severely depressed inpatients in one study of the development program for that product responded to a mean dose of 350 mg/day (range of 150 to 375 mg/day). Whether or not higher doses of Venlafaxine Extended Release Tablets are needed for more severely depressed patients is unknown; however, the experience with venlafaxine hydrochloride extended-release capsule doses higher than 225 mg/day is very limited. Social Anxiety Disorder (Social Phobia): the recommended dose is 75 mg/day, administered in a single dose. There was no evidence that higher doses confer any additional benefit.

Route of Administration: Oral

In Vitro Use Guide

In vitro radioligand binding studies were carried out in rat brain membranes to assess the affinity of various reuptake inhibitors for the serotonin (5-hydroxytryptamine, 5-HT) and the norepinephrine transporters using the selective ligands [3H]cyanoimipramine and [3H]nisoxetine, respectively. Venlafaxine, a dual 5-HT and norepinephrine reuptake inhibitor, displayed only a moderate affinity for the 5-HT transporter (Ki = 74 nM) and a very low affinity for the norepinephrine transporter (Ki = 1.26 microM). The relatively low affinities of venlafaxine contrast with its potent in vivo 5-HT and norepinephrine reuptake blocking properties. These results raise the possibility that the in vivo effects on the 5-HT and norepinephrine reuptake observed with venlafaxine may not be mediated solely by its binding to the [3H]cyanoimipramine and [3H]nisoxetine binding sites.

Substance Class	Chemical Created by `admin` on `Fri Dec 15 15:56:35 GMT 2023` Edited by `admin` on `Fri Dec 15 15:56:35 GMT 2023`
Record UNII	GRZ5RCB1QG
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

VENLAFAXINE

Official Name

English

VENLOR

Common Name

English

CYCLOHEXANOL, 1-(2-(DIMETHYLAMINO)-1-(4-METHOXYPHENYL)ETHYL)-

Systematic Name

English

VENLAFAXINE [VANDF]

Common Name

English

venlafaxine [INN]

Common Name

English

NSC-758676

Code

English

TREVILOR

Common Name

English

EFECTIN

Brand Name

English

Venlafaxine [WHO-DD]

Common Name

English

(±)-1-(.ALPHA.-((DIMETHYLAMINO)METHYL)-P-METHOXYBENZYL)CYCLOHEXANOL

Common Name

English

VENLAFAXINE [MI]

Common Name

English

KANGHONG

Common Name

English

VELAFAX

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C265