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药品详细

Vilazodone(维拉佐)

化学结构式图
中文名
维拉佐
英文名
Vilazodone
分子式
C26H27N5O2
化学名
5-{4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl}-1-benzofuran-2-carboxamide
分子量
Average: 441.5249
Monoisotopic: 441.216475133
CAS号
163521-12-8
ATC分类
N06A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Vilazodone is a novel compound with combined high affinity and selectivity for the 5-hydroxytryptamine (5-HT) transporter and 5-HT receptors. It has been shown to be equally efficacious as other antidepressants with similar gastrointestinal side effects and possibly with reduced sexual side effects and weight gain. Vilazodone is an antidepressant agent that can used as an alternative for patients who cannot tolerate therapy with other antidepressant classes such as selective serotonin reuptake inhibitors or serotonin norepinephrine reuptake inhibitors. Treatment should be titrated towards the target dose, which is 40mg per day.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Khan A, Cutler AJ, Kajdasz DK, Gallipoli S, Athanasiou M, Robinson DS, Whalen H, Reed CR: A randomized, double-blind, placebo-controlled, 8-week study of vilazodone, a serotonergic agent for the treatment of major depressive disorder. J Clin Psychiatry. 2011 Apr;72(4):441-7. Pubmed
    2. Traynor K: Vilazodone approved for major depression. Am J Health Syst Pharm. 2011 Mar 1;68(5):366. Pubmed
    3. Howland RH: Vilazodone: another novel atypical antidepressant drug. J Psychosoc Nurs Ment Health Serv. 2011 Mar;49(3):19-22. doi: 10.3928/02793695-20110203-98. Epub 2011 Feb 16. Pubmed
    4. Dawson LA, Watson JM: Vilazodone: a 5-HT1A receptor agonist/serotonin transporter inhibitor for the treatment of affective disorders. CNS Neurosci Ther. 2009 Summer;15(2):107-17. Pubmed
    5. de Paulis T: Drug evaluation: Vilazodone—a combined SSRI and 5-HT1A partial agonist for the treatment of depression. IDrugs. 2007 Mar;10(3):193-201. Pubmed
    6. Page ME, Cryan JF, Sullivan A, Dalvi A, Saucy B, Manning DR, Lucki I: Behavioral and neurochemical effects of 5-(4-[4-(5-Cyano-3-indolyl)-butyl)-butyl]-1-piperazinyl)-benzofuran-2-carb oxamide (EMD 68843): a combined selective inhibitor of serotonin reuptake and 5-hydroxytryptamine(1A) receptor partial agonist. J Pharmacol Exp Ther. 2002 Sep;302(3):1220-7. Pubmed
    7. Wang SM, Han C, Lee SJ, Patkar AA, Pae CU: A review of current evidence for vilazodone in major depressive disorder. Int J Psychiatry Clin Pract. 2013 Apr 12. Pubmed
    8. Dopheide JA: Vilazodone’s comparative merits yet to be demonstrated. Am J Health Syst Pharm. 2012 Sep 15;69(18):1549. doi: 10.2146/ajhp110570. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes Not Available
    Substructures Not Available
    适应症
    药理
    Indication Vilazodone is approved for treatment of acute episodes of major depression. Labeling of vilazodone describes an increased risk of suicidal thoughts in children, adolescents and young adults. The use of vilazodone in pediatrics is not indicated. Its use with monoamine oxidase inhibitors (MAOI) is contraindicated due to increased risk of serotonin syndome. Once the MAOI is discontinued, a 14-day washout period must pass before starting vilazodone.
    Pharmacodynamics Vilazodone increases serotonin levels in the brain by inhibiting the reuptake of serotonin while acting as a partial agonist on serotonin-1A receptors. It has therefore been coined by scientists as a selective partial agonist and reuptake inhibitor (SPARI). Because of its partial agonist activity for serotonin-1A, vilazodone helps to reduce anxiety.
    Mechanism of action Since serotonin is believed to be one of the three main neurotransmitters that is low or imbalanced in patients with depression- pathways seeking to increase serotonin levels are targeted by pharmaceutical companies. As a selective serotonin reuptake inhibitor, vilazodone prevents serotonin from re-entering cell bodies. Hence, they will remain longer in the synapse. Vilazodone also has an inherent selectivity for serotonin-1A receptors, acting as a partial agonist which stimulates the production of serotonin. The end result is increased serotonin in the synaptic cleft, allowing serotonin to resume its action on nearby cells. The mechanism of the antidepressant effect of vilazodone is not fully understood, but is thought to be related to its enhancement of serotonergic activity in the CNS through selective inhibition of serotonin reuptake.
    Absorption Vilazodone's absorption is improved when taken with food to 72%.
    Volume of distribution Not Available
    Protein binding 96-99% protein bound
    Metabolism
    Major: CYP3A4. Minor: CYP2C19 and CYP2D6
    Route of elimination 1% recovered in urine. 2% unchanged in feces.
    Half life 25.4h
    Clearance

    21.1L/h
    Toxicity Vomiting, serotonin syndrome.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    water solubility Aqueous solubility is 0.32 mg/mL Not Available
    pKa 7.1 Not Available
    Predicted Properties
    Property Value Source
    water solubility 1.23e-01 g/l ALOGPS
    logP 4.21 ALOGPS
    logP 3.72 ChemAxon
    logS -3.6 ALOGPS
    pKa (strongest acidic) 14.19 ChemAxon
    pKa (strongest basic) 8.6 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 102.29 ChemAxon
    rotatable bond count 7 ChemAxon
    refractivity 129.71 ChemAxon
    polarizability 50.02 ChemAxon
    药物相互作用
    Drug Interaction
    Amitriptyline Monitor for toxic effects of tricyclic antidepressants if a selective serotonin reuptake inhibitor (SSRI) is initiated or the dose is increased. The influence of the SSRI may take several days or weeks to be fully realized or resolved.
    Atazanavir CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vilazodone. imit maximum adult vilazodone dose to 20 mg/day in patients receiving strong CYP3A4 inhibitors.
    Carbamazepine Carbamazepine may increase the metabolism of Selective Serotonin Reuptake Inhibitors (SSRI). Specifically those agents metabolized via CYP1A2, 2C, and/or 3A4 isoenzymes. Selective Serotonin Reuptake Inhibitors may decrease the metabolism of Carbamazepine. Specifically those SSRIs that inhibit CYP3A4 isoenzymes.
    Celecoxib Selective Serotonin Reuptake Inhibitors may enhance the antiplatelet effect of NSAID (COX-2 Inhibitor). To minimize the risk of bleeding associated with this combination, consider using alternative analgesics, when appropriate, and/or addition of an gastroprotective agent, such as a proton pump inhibitor for the time that combined selective serotonin reuptake inhibitor (SSRIs) and nonsteroidal anti-inflammatory drugs (NSAIDs) is necessary.
    Cimetidine Cimetidine may decrease the metabolism of Selective Serotonin Reuptake Inhibitors. Consider using an alternative H2-antagonist to avoid the risk of selective serotonin reuptake inhibitor (SSRI) toxicity. Monitor for increased therapeutic or toxic effects of SSRI if cimetidine is initiated/dose increased, or decreased effects if cimetidine is discontinued/dose decreased.
    Clarithromycin CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vilazodone. imit maximum adult vilazodone dose to 20 mg/day in patients receiving strong CYP3A4 inhibitors.
    Clozapine Selective Serotonin Reuptake Inhibitors may decrease the metabolism of clozapine. If concurrent use of these agents is employed, monitor for increased toxic effects of clozapine if a selective serotonin reuptake inhibitor (SSRI) is initiated/dose increased, or decreased effects if a SSRI is discontinued/dose decreased.
    Conivaptan CYP3A4 Inhibitors (Strong) such as conivaptan may increase the serum concentration of Vilazodone. Limit maximum adult vilazodone dose to 20 mg/day in patients receiving strong CYP3A4 inhibitors.
    Desipramine Monitor for toxic effects of tricyclic antidepressants if a selective serotonin reuptake inhibitor (SSRI) is initiated or the dose is increased. The influence of the SSRI may take several days or weeks to be fully realized or resolved.
    Dextromethorphan Consideration should be given to avoiding the concomitant use of dextromethorphan and selective serotonin reuptake inhibitors (SSRI). Monitor for toxic effects of dextromethorphan (eg, CNS, Cardiovascular) if an SSRI is initiated or the dose is increased. SSRIs, other than fluoxetine and paroxetine, may be safer alternatives due to lesser CYP2D6 inhibition; however, the mechanism for the interaction is not fully understood, and caution is still advised.
    Diclofenac Increased risk of bleeding with concomitant use of NSAIDs with vilazodone.
    Drotrecogin alfa Increase monitoring for signs/symptoms of bleeding during concomitant therapy. If possible, avoid use of drotrecogin within 7 days of use of any IIb/IIIa antagonists, higher dose aspirin (more than 650 mg/day), or use of other antiplatelet agents.
    Ibuprofen Increased risk of bleeding with concomitant use of non-steroidal anti-inflammatory drugs with vilazodone.
    Isocarboxazid MAO Inhibitors may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Avoid combination.
    Ketoconazole CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vilazodone. imit maximum adult vilazodone dose to 20 mg/day in patients receiving strong CYP3A4 inhibitors.
    Ketorolac Increased risk of bleeding with concomitant use of vilazodone and ketorolac
    L-Tryptophan Due to risks of enhanced serotonin activity and/or adverse reactions (e.g., serotonin syndrome), concomitant use of selective serotonin reuptake inhibitors (SSRIs) and tryptophan is not recommended. Avoid combination.
    Linezolid MAO Inhibitors may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Avoid combination.
    Metoclopramide Seek alternatives to this combination when possible. Monitor patients receiving metoclopramide with selective serotonin reuptake inhibitors for signs of extrapyramidal symptoms, neuroleptic malignant syndrome, and serotonin syndrome.
    Mexiletine Monitor for increased serum concentrations/toxic effects of mexiletine if a selective serotonin reuptake inhibitor (SSRI) is initiated/dose increased, or decreased concentrations/effects if an SSRI is discontinued/dose decreased.
    Naproxen Increased risk of bleeding with concomitant use of NSAIDs with vilazodone.
    Naratriptan Increased risk of serotonin syndrome
    Nortriptyline Monitor for toxic effects of tricyclic antidepressants if a selective serotonin reuptake inhibitor (SSRI) is initiated or the dose is increased. The influence of the SSRI may take several days or weeks to be fully realized or resolved.
    Phenelzine MAO Inhibitors may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome.
    Piroxicam Increased risk of bleeding with concomitant use of NSAIDs and vilazodone
    Quinidine CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vilazodone. imit maximum adult vilazodone dose to 20 mg/day in patients receiving strong CYP3A4 inhibitors.
    Selegiline MAO Inhibitors may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Avoid combination.
    Sibutramine Sibutramine may enhance the serotonergic effect of Serotonin Modulators. This may cause serotonin syndrome. Avoid combination.
    Sumatriptan Increased risk of serotonin syndrome
    Thioridazine Thioridazine prescribing information contraindicates the concomitant use of agents that inhibit CYP2D6 isoenzymes. Avoid combination.
    Tranylcypromine MAO Inhibitors may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome.
    Voriconazole CYP3A4 Inhibitors (Strong) may increase the serum concentration of Vilazodone. imit maximum adult vilazodone dose to 20 mg/day in patients receiving strong CYP3A4 inhibitors.
    Warfarin Increased risk of bleeding with concomitant use of warfarin and vilazodone.
    食物相互作用
    • Caution taking vilazodone with foods/herbal product with antiplatelet/anticoagulant properties
    • Gingko bilboa, ginger, garlic, green tea, licorice, horseradish

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