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Venlafaxine

Product Name
Venlafaxine
CAS No.
93413-69-5
Chemical Name
Venlafaxine
Synonyms
Velafax;Trevilor;Wy-45030;Wy-45651;AKOS 92111;VENLAFAXIN;venlafexine;Venlafaxine;Venlafaxin HCL;VENLAFAXINE HCL
CBNumber
CB7136180
Molecular Formula
C17H27NO2
Formula Weight
277.4
MOL File
93413-69-5.mol
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Venlafaxine Property

Melting point:
72-74°C
Boiling point:
397.6±27.0 °C(Predicted)
Density 
1.060±0.06 g/cm3(Predicted)
storage temp. 
Keep in dark place,Inert atmosphere,2-8°C
pka
pKa 9.5 (Uncertain)
Water Solubility 
<0.1g/L(room temperature)
CAS DataBase Reference
93413-69-5(CAS DataBase Reference)
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Safety

Hazardous Substances Data
93413-69-5(Hazardous Substances Data)
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC
Product number
V119995
Product name
D,L-Venlafaxine
Packaging
250mg
Price
$520
Updated
2021/12/16
Medical Isotopes, Inc.
Product number
D4421
Product name
DL-Venlafaxine-d10Hydrochloride
Purity
99.9%
Packaging
5 mg
Price
$900
Updated
2021/12/16
Activate Scientific
Product number
AS146607
Product name
Venlafaxine
Purity
98%
Packaging
5 g
Price
$1173
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0004581
Product name
VENLAFAXINE
Purity
95.00%
Packaging
1G
Price
$284.55
Updated
2021/12/16
Ambeed
Product number
A901971
Product name
Venlafaxine
Purity
98+%
Packaging
1g
Price
$1797
Updated
2021/12/16
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Venlafaxine Chemical Properties,Usage,Production

Chemical Properties

White Solid

Uses

A optically active version of Venlafaxine, a selective serotonin noradrenaline reuptake inhibitor. Used as an antidepressant

Uses

antidepressant;serotonin-norepinephrine reuptake inhibitor

Uses

A selective serotonin noradrenaline reuptake inhibitor. Used as an antidepressant.

Definition

ChEBI: A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group.

brand name

Effexor (Wyeth).

Biological Functions

Venlafaxine (Effexor) inhibits the reuptake of both serotonin and norepinephrine at their respective presynaptic sites.This drug does not have significant effects at muscarinic, histamine, or α-adrenergic receptors and therefore is devoid of many of the side effects associated with the TCAs.Venlafaxine and its active metabolite O-desmethyl-venlafaxine, have half lives of 5 and 11 hours respectively, so dosing twice a day is necessary. However, an extended release preparation (Effexor XR) now allows for once-daily dosing and better tolerance. Venlafaxine has a side effect profile similar to that of the SSRIs. Higher doses of venlafaxine result in modest increases in blood pressure in approximately 5% of patients.Venlafaxine has minimal effects on the cytochrome P450 enzyme system.

General Description

The structure and activity of venlafaxine (Effexor) are in accordwith the general SARs for the group. As expected, it isan effective antidepressant. Venlafaxine is a serotonin–norepinephrinereuptake inhibitor (SNRI).

Pharmaceutical Applications

Venlafaxine is a serotonin and noradrenalin reuptake inhibitor (SNRI) and is used as an antidepressant. Compared to tricyclic antidepressants, it lacks the antimuscarinic and sedative side effects. Nevertheless, treatment with venlafaxine can lead to a higher risk of withdrawal symptoms.

Mechanism of action

Venlafaxine and its active metabolite, O-desmethylvenlafaxine (ODV), have dual mechanisms of action, with preferential affinity for 5-HT reuptake and weak inhibition of NE and dopamine reuptake. Venlafaxine is approximately 30 times more potent as an inhibitor of SERT than of NET. Because of the 30 times difference in transporter affinities, increasing the dose of venlafaxine from 75 to 375 mg/day can sequentially inhibit SERT and NERT . Thus, venlafaxine displays an ascending dose-dependent antidepressant response in contrast to the flat dose–antidepressant response curve observed with the SSRIs. This sequential action for venlafaxine also is consistent with its dose-dependent adverse-effect profile. Its mechanism of action is similar to imipramine.
Venlafaxine is rapidly and well absorbed, but with a bioavailability of 45%, which has been attributed to first-pass metabolism. Food delays its absorption but does not impair the extent of absorption. Venlafaxine is distributed into breast milk. Venlafaxine is primarily metabolized in the liver by CYP2D6 to its primary metabolite, ODV, which is approximately equivalent in pharmacological activity and potency to venlafaxine. In vitro studies indicate that CYP3A4 also is involved in the metabolism of venlafaxine to its minor and less active metabolite, N-desmethylvenlafaxine. Protein binding for venlafaxine and ODV is low and is not a problem for drug interactions. In patients with hepatic impairment, elimination half-lives were increased by approximately 30% for venlafaxine and approximately 60% for ODV. In patients with renal function impairment, elimination half-lives were increased by approximately 40 to 50% for venlafaxine and for ODV. At steady-state doses, venlafaxine and ODV exhibit dose-proportional linear pharmacokinetics over the dose range of 75 to 450 mg/day. Steady-state concentrations of venlafaxine and ODV are attained within 3 days with regular oral dosing. Venlafaxine and its metabolites are excreted primarily in the urine (87%).

Clinical Use

Venlafaxine is a methoxyphenylethylamine antidepressant that resembles an open TCA with one of the aromatic rings replaced by a cyclohexanol ring and a dimethylaminomethyl group rather than a dimethylaminopropyl chain.

Side effects

The potential for cardiotoxicity with venlafaxine during normal use and for various toxicities in overdose situations are key concerns. Venlafaxine displays minimal in vitro affinity for the other neural neurotransmitter receptors and, thus, a low probability for adverse effects. To minimize GI upset (e.g., nausea), venlafaxine can be taken with food without affecting its GI absorption. Venlafaxine should be administered as a single daily dose with food at approximately the same time each day. The extended-release capsules should be swallowed whole with fluid and should not be divided, crushed, chewed, or placed in water.
Whenever venlafaxine is being discontinued after more than 1 week of therapy, it generally is recommended that the patient be closely monitored and the dosage of the drug be tapered gradually to reduce the risk of withdrawal symptoms.
Although venlafaxine is a weak inhibitor of CYP2D6, variability has been observed in the pharmacokinetic parameters of venlafaxine in patients with hepatic or renal function impairment. As a precaution, elderly patients taking venlafaxine concurrently with a drug that has a narrow therapeutic index and also is metabolized by CYP2D6 should be carefully monitored. Concurrent use of CYP3A4 inhibitors with venlafaxine has been shown to interfere with its metabolism and clearance. Similar to the other antidepressants that block 5-HT reuptake, venlafaxine may interact pharmacodynamically to cause toxic levels of 5-HT to accumulate, leading to the 5-HT syndrome.

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Venlafaxine Suppliers

Chengdu Saint - Kay Biotechnology Co., Ltd.
Email
676046971@qq.com
Country
China
ProdList
4510
Advantage
58
J & K SCIENTIFIC LTD.
Tel
010-82848833- ;010-82848833-
Fax
86-10-82849933
Email
jkinfo@jkchemical.com;market6@jkchemical.com
Country
China
ProdList
96815
Advantage
76
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15877
Advantage
69
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
1938
Advantage
70
Nanjing Chemlin Chemical Co., Ltd
Tel
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
20007
Advantage
64
Chemsky(shanghai)International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
32358
Advantage
50
Syntechem Co.,Ltd
Tel
Please Email
Fax
E-Mail Inquiry
Email
info@syntechem.com
Country
China
ProdList
13009
Advantage
57
BOC Sciences
Email
info@bocsci.com
Country
United States
ProdList
21113
Advantage
65
BioBioPha Co., Ltd.
Tel
0871-65217109-
Fax
0871-65215563
Email
sales@mail.biobiopha.com
Country
China
ProdList
5688
Advantage
65
Beijing HuaMeiHuLiBiological Chemical
Tel
010-56205725;010-86181995
Fax
010-65763397
Email
waley188@sohu.com
Country
China
ProdList
12341
Advantage
58
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View Lastest Price from Venlafaxine manufacturers

Hong Kong Tiansheng New Material Trading Co., Ltd
Product
Venlafaxine 93413-69-5
Price
US $16.55/Kg/Bag
Min. Order
1Kg/Bag
Purity
99%
Supply Ability
20tons
Release date
2022-01-11
Hong Kong Tiansheng New Material Trading Co., Ltd
Product
Venlafaxine 93413-69-5
Price
US $4.60/KG
Min. Order
1KG
Purity
99%
Supply Ability
1000tons
Release date
2021-12-27
Hebei Crovell Biotech Co Ltd
Product
Venlafaxine 93413-69-5
Price
US $19.00/KG
Min. Order
1KG
Purity
99.%
Supply Ability
50 ton
Release date
2022-01-07

93413-69-5, VenlafaxineRelated Search:


  • D,L-VENLAFAXINE, HYDROCHLORIDE
  • 1-[2-(DIMETHYLAMINO)-1-(4-METHOXYPHENYL)ETHYL]CYCLOHEXANOL, HCL
  • 1-[2-(DIMETHYLAMINO)-1-(4-METHOXYPHENYL)ETHYL]CYCLOHEXANOL HYDROCHLORIDE
  • AKOS 92111
  • (?-1-[a-[(dimethylamino)methyl]-p-methoxybenzyl]cyclohexanol
  • N,N-dimethyl-2-(1-hydroxycyclohexyl)-2-(4-methoxyphenyl)ethylamine
  • venlafexine
  • VENLAFAXINE HCL
  • VENALAFAXINE HCL
  • Venlafaxin HCL
  • 1-[2-dimethylamino-1-(4-methoxyphenyl)ethyl]cyclohexan-1-ol
  • VENLAFAXIN
  • [2-Dimethylamino-1-(4-methoxyphenyl)-ethyl]cyclohexan-1-ol
  • Venlafaxine
  • 1-[(1S)-2-(Dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol
  • 1-[(1R)-2-(Dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol
  • Trevilor
  • Velafax
  • Wy-45030
  • Wy-45651
  • 1-[1-(4-Methoxyphenyl)-2-(dimethylamino)ethyl]cyclohexanol
  • 1-[1-(4-Methoxyphenyl)-2-dimethylaminoethyl]cyclohexanol
  • 1-[α-(Dimethylaminomethyl)-4-methoxybenzyl]cyclohexanol
  • Venlafaxine API
  • Cyclohexanol,1-[2-(diMethylaMino)-1-(4-Methoxyphenyl)ethyl]-
  • Venlafaxine for system suitability CRS
  • Venlafaxine USP/EP/BP
  • Venlafaxine (Wy 45030)
  • 93413-69-5
  • C17H17D10NO2
  • Venlafaxine
  • Pharmaceutical material and intermeidates
  • Pharmaceutical raw material
  • Effexor, Efexor
  • PROZAC
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Chiral Reagents