Vilazodone

Các tên gọi khác (2) :

Vilazodona
Vilazodonum

serotonin uptake inhibitors, serotonin receptor agonists, antidepressive agents

Thuốc Gốc

Small Molecule

CAS: 163521-12-8

ATC: N06AX24

CTHH: C₂₆H₂₇N₅O₂

PTK: 441.5249

Vilazodone is a novel compound with combined high affinity and selectivity for the 5-hydroxytryptamine (5-HT) transporter and 5-HT(1A) 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.

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₂₆H₂₇N₅O₂

Phân tử khối

441.5249

Monoisotopic mass

441.216475133

InChI

InChI=1S/C26H27N5O2/c27-16-18-4-6-23-22(13-18)19(17-29-23)3-1-2-8-30-9-11-31(12-10-30)21-5-7-24-20(14-21)15-25(33-24)26(28)32/h4-7,13-15,17,29H,1-3,8-12H2,(H2,28,32)

InChI Key

InChIKey=SGEGOXDYSFKCPT-UHFFFAOYSA-N

IUPAC Name

5-{4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl}-1-benzofuran-2-carboxamide

Traditional IUPAC Name

5-{4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl}-1-benzofuran-2-carboxamide

SMILES

NC(=O)C1=CC2=C(O1)C=CC(=C2)N1CCN(CCCCC2=CNC3=C2C=C(C=C3)C#N)CC1

Độ hòa tan

Aqueous solubility is 0.32 mg/mL

logP

3.72

logS

-3.6

pKa (strongest acidic)

14.19

pKa (Strongest Basic)

8.6

PSA

102.29 Å²

Refractivity

129.71 m³·mol^-1

Polarizability

50.02 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

Ghose Filter

true

MDDR-Like Rule

true

pKa

7.1

Dược Lực Học : 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.

Cơ Chế Tác Dụng : Vilazodone is a novel compound with combined high affinity and selectivity for the 5-hydroxytryptamine (5-HT) transporter and 5-HT(1A) 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. 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.

Dược Động Học :

▧ Absorption :
Vilazodone's absorption is improved when taken with food to 72%.
▧ 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

Độc Tính : Vomiting, serotonin syndrome.

Chỉ Định : 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.

Tương Tác Thuốc :

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.

Liều Lượng & Cách Dùng : Tablet - Oral - 10mg
Tablet - Oral - 20mg
Tablet - Oral - 40mg

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty : Forest Laboratories, Inc.

Sản phẩm biệt dược : Viibryd

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB06684

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D09698

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0456-1110-30

Wikipedia

http://en.wikipedia.org/wiki/Vilazodone

RxList

http://www.rxlist.com/viibryd-drug.htm

Drugs.com

http://www.drugs.com/cdi/vilazodone.html

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