Venlafaxine Hydrochloride
VENLAFAXINE HCL · D,L-VENLAFAXINE · D,L-VENLAFAXINE, HYDROCHLORIDE · Vexor · Venlift · AKOS 92111 · VENLAFAXINEHCL · Venlaffaxine HCL
Identifikatoren & physikalische Daten
| CAS No. | 99300-78-4 |
|---|---|
| Summenformel | C17H28ClNO2 |
| Durchschnittliche Molmasse | 313,9 g/mol |
| Monoisotopische Masse | 313,18085682 g/mol |
| SMILES | COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1.Cl |
| InChIKey | QYRYFNHXARDNFZ-UHFFFAOYSA-N |
| PubChem CID | 62923 |
| ChEMBL | CHEMBL1201066 |
| EC No. | 619-421-1 |
| DTXSID | DTXSID8047397 |
Chemische & physikalische Eigenschaften
| Polarare Oberfläche (TPSA) | 32,7 |
|---|---|
| H-Brücken-Donoren | 2 |
| H-Brücken-Akzeptoren | 3 |
| Frei drehbare Bindungen | 5 |
| Schwere Atome | 21 |
| Formalladung | 0 |
| Komplexität | 279 |
| Human Drugs | FDA approved drugs -> Active ingredient |
| Schmelzpunkt | 207-209°C |
| Flammpunkt | 9℃ |
| Lagerbedingungen | 2-8°C |
| Löslichkeit | H2O: >10mg/mLwater: 100mMDMSO: 50mM |
| Aggregatzustand | powder |
| Farbe | white |
| Merck | 14,9946 |
| BCS Class | 1 |
| Hauptanwendungen | pharmaceutical (small molecule) |
| InChI | InChI=1S/C17H27NO2.ClH/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,4-6,11-13H2,1-3H31H |
| InChIKey | QYRYFNHXARDNFZ-UHFFFAOYSA-N |
| SMILES | OC1(CCCCC1)C(C1=CC=C(OC)C=C1)CN(C)C.[H]Cl |
| CAS Datenbank | 99300-78-4(CAS DataBase Reference) |
| EPA chemische Informationen | Cyclohexanol, 1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]-, hydrochloride (1:1 (99300-78-4) |
Sicherheit & Vorschriften
| GHS-Einstufung | This chemical does not meet GHS hazard criteria for 0.9% (1 of 113) of reports.WarningH302 (15.9%): Harmful if swallowed [Warning Acute toxicity, oral]P264, P264+P265, P270, P280, P301+P317, P305+P351+P338, P330, P337+P317, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 113 reports by companies from 15 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies. |
|---|---|
| Hazard Classes and Categories | Acute Tox. 4 (15.9%) |
| Treatment | Treatment should consist of those general measures employed in the management of overdosage with any antidepressant. Ensure an adequate airway, oxygenation, and ventilation. Monitor cardiac rhythm and vital signs. General supportive and symptomatic measures are also recommended. Induction of emesis is not recommended. Gastric lavage with a large bore orogastric tube with appropriate airway protection, if needed, may be indicated if performed soon after ingestion or in symptomatic patients. Activated charcoal should be administered. Due to the large volume of distribution of this drug, forced diuresis, dialysis, hemoperfusion, and exchange transfusion are unlikely to be of benefit. No specific antidotes for venlafaxine are known. (L1712) |
| Expositionspfade | Oral. Venlafaxine is well absorbed. Food does not effect the absorption of venlafaxine or its subsequent metabolism into ODV. Bioavailability is 45% following oral administration. Time to steady state = 3 days. |
| Toxizitätsübersicht | The exact mechanism of action of venlafaxine is unknown, but appears to be associated with the its potentiation of neurotrasmitter activity in the CNS. Venlafaxine and its active metabolite, O-desmethylvenlafaxine (ODV), inhibit the reuptake of both serotonin and norepinephrine with a potency greater for the 5-HT than for the NE reuptake process. Both venlafaxine and the ODV metabolite have weak inhibitory effects on the reuptake of dopamine but, unlike the tricyclics and similar to SSRIs, they are not active at histaminergic, muscarinic, or alpha(1)-adrenergic receptors. |
| Signs and Symptoms | Most patients overdosing with venlafaxine develop only mild symptoms. However, severe toxicity is reported with the most common symptoms being CNS depression, serotonin toxicity, seizure, or cardiac conduction abnormalities. |
Anwendungen & Verwendung
Beschreibung
Venlafaxine hydrochloride, a novel phenethylamine derivative, was introduced in the U.S.A. as an antidepressant. Venlafaxine is reported to be the first in the class of the second-generation of antidepressants with dual serotonidnorepinephrine reuptake inhibitory activity. Venlafaxine lacks any affinity for muscarinic, cholinergic, histaminergic and noradrenergic receptors and therefore, has an unusually favorable side effect profile compared with classical tricyclic antidepressants and shows less cardiotoxicity. In addition, venlafaxine has a rapid onset of action that makes it unique among the antidepressant agents. Other indications for venlafaxine include the treatment of obsessive and panic disorders, and obesity. Both enantiomers of venlafaxine were reported to have similar biological activity.
Verwenden
A selective serotonin noradrenaline reuptake inhibitor. Used as an antidepressant