Luhan Pharmachem Co., Ltd.

Luhan pharmachem Co., Ltd. supplies Vilazodone HCl bulk active pharmaceutical ingredient (API) to the pharmaceutical industry. Our Vilazodone HCl is manufactured by cGMP compliant facility. Welcome to contact us for further details including current DMF status for the product and up to date regulatory status of the manufacturing facility. We look forward to assisting you with your research and development projects.

What is Vilazodone hydrochloride?

Vilazodone is a serotonergic antidepressant developed by Clinical Data for the treatment of major depressive disorder. The chemical compound was originally developed by Merck KGaA (Germany). By 2009 two phase III clinical trials with positive results had been completed. Vilazodone was approved by the FDA for use in the United States to treat major depressive disorder on January 21, 2011.

Vilazodone HCl is 2-benzofurancarboxamide, 5-[4-[4-(5-cyano-1H-indol-3-yl)butyl]-1-piperazinyl]-, hydrochloride (1:1). Its molecular weight is 477.99.

Vilazodone hydrochloride Drug Interactions

Central Nervous System (CNS)-Active Agents

The risk of using Vilazodone in combination with other CNS-active drugs has not been systematically evaluated. Consequently, use caution when Vilazodone is prescribed in combination with other CNS-active drugs.

• Monoamine Oxidase Inhibitors (MAOIs)
• Serotonergic Drugs
• Drugs that Interfere with Hemostasis (e.g., NSAIDs, Aspirin, and Warfarin)

Serotonin release by platelets plays an important role in hemostasis. Epidemiological studies of case-control and cohort design have demonstrated an association between use of psychotropic drugs that interfere with serotonin reuptake and the occurrence of upper gastrointestinal bleeding. These studies have also shown that concurrent use of an NSAID or aspirin may potentiate this risk of bleeding. Altered anticoagulant effects, including increased bleeding, have been reported when SSRIs and SNRIs are coadministered with warfarin. Patients receiving warfarin therapy should be carefully monitored when Vilazodone is initiated or discontinued.

• Potential for Other Drugs to Affect Vilazodone

Inhibitors of CYP3A4

Metabolism by CYP3A4 is a major elimination pathway for vilazodone. Concomitant use of Vilazodone and strong inhibitors of CYP3A4 (e.g., ketoconazole) can increase vilazodone plasma concentrations by approximately 50% (see Figure 1).

Inducers of CYP3A4

Concomitant use of Vilazodone with inducers of CYP3A4 has the potential to reduce vilazodone systemic exposure. However, the effect of CYP3A4 inducers on vilazodone plasma concentrations has not been evaluated.

Inhibitors of other CYP enzymes

Concomitant administration of Vilazodone with inhibitors of CYP2C19 and CYP2D6 is not expected to alter plasma concentrations of vilazodone. These isoforms are minor elimination pathways in the metabolism of vilazodone. In vitro studies have shown that CYP1A2, CYP2A6, CYP2C9 and CYP2E1 have minimal contribution to the metabolism of vilazodone.

• Potential for Vilazodone to Affect Other Drugs

Drugs metabolized by CYP1A2, CYP2C9, CYP2D6, CYP3A4 or CYP2C19.

Coadministration of Vilazodone with substrates for CYP1A2, CYP2C9, CYP3A4, or CYP2D6 is unlikely to result in clinically significant changes in the concentrations of the CYP substrates. In vitro studies have shown that Vilazodone is a moderate inhibitor of CYP2C19 and CYP2D6.

• Drugs metabolized by CYP2C8

Coadministration of Vilazodone with a CYP2C8 substrate may lead to an increase in concentration of the other drug.

Induction of CYP isoforms

Vilazodone did not induce CYP1A1, 1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1, 3A4 or 3A5 in an in vitro study in cultured human hepatocytes. Chronic administration of vilazodone is unlikely to induce the metabolism of drugs metabolized by these major CYP isoforms.

• Drugs Highly Bound to Plasma Protein

The interaction between vilazodone and other highly protein-bound drugs has not been evaluated. Because vilazodone is highly bound to plasma protein, administration of Vilazodone to a patient taking another drug that is highly protein bound may cause increased free concentrations of the other drug.

• Triptans

There are postmarketing reports of serotonin syndrome with concomitant use of a serotonergic antidepressant and a triptan.

• Alcohol

As with other psychotropic medications, the use of alcohol by patients taking Vilazodone is not recommended, because of the potential for pharmacodynamic interactions.

Precautions before using Vilazodone hydrochloride

• Clinical Worsening/Suicide Risk: Monitor patients for clinical worsening and suicidal thinking or behavior.
• Serotonin Syndrome : Serotonin syndrome has been reported with SSRIs and SNRIs, including Vilazodone, both when taken alone, but especially when co-administered with other serotonergic agents (including triptans, tricyclic antidepressants, fentanyl, lithium, tramadol, trytophan, buspirone and St. John’s Wort). If such symptoms occur, discontinue Vilazodone and initiate supportive treatment. If concomitant use of Vilazodone with other serotonergic drugs is clinically warranted, patients should be made aware of a potential increased risk for serotonin syndrome, particularly during treatment initiation and dose increases.
• Seizures: Can occur with treatment. Use with caution in patients with a seizure disorder.
• Abnormal Bleeding: Treatment can increase the risk of bleeding. Use with caution in association with nonsteroidal anti-inflammatory drugs (NSAIDs), aspirin, or other drugs that affect coagulation.
• Activation of Mania/Hypomania: Can occur with treatment. Screen patients for bipolar disorder
• Discontinuation of Treatment with Vilazodone: A gradual reduction in dose is recommended rather than an abrupt cessation.
• Hyponatremia: Can occur in association with the syndrome of inappropriate antidiuretic hormone secretion (SIADH).

Vilazodone hydrochloride Side effects

The most common adverse reactions (incidence ? 5% and at least twice the rate of placebo) are: diarrhea, nausea, vomiting, and insomnia

Vilazodone hydrochloride Storage

Vilazodone HCl should be stored at 25°C (77°F) with excursions permitted to 15°C – 30°C (59°F – 86°F) [see USP Controlled Room Temperature].

Disclaimer:

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.