Clinical data | |
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Pronunciation |
/vɪˈlæzədoʊn/ vi-LAZ-ə-dohn |
Trade names | Viibryd |
Other names | EMD-68843; SB-659746A |
AHFS/ Drugs.com | Monograph |
MedlinePlus | a611020 |
License data |
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Routes of administration | By mouth |
Drug class | Serotonin modulator [1] |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Bioavailability | 72% (oral, with food) [5] |
Metabolism | Liver via CYP3A4 [5] |
Elimination half-life | 25 hours [5] |
Excretion | Faecal and renal [5] |
Identifiers | |
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CAS Number |
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PubChem CID | |
IUPHAR/BPS | |
DrugBank |
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ChemSpider | |
UNII |
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KEGG | |
ChEBI |
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ChEMBL |
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PDB ligand | |
Chemical and physical data | |
Formula | C26H27N5O2 |
Molar mass | 441.535 g·mol−1 |
3D model ( JSmol) | |
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(what is this?) (verify) |
Vilazodone, sold under the brand name Viibryd among others, is a medication used to treat major depressive disorder. [1] It is classified as a serotonin modulator [1] and is taken by mouth. [1]
Common side effects include nausea, diarrhea, and trouble sleeping. [1] Serious side effects may include increased suicidal thoughts or actions in those under the age of 25, serotonin syndrome, bleeding, mania, pancreatitis, and SIADH. [1] Vilazodone may cause less emotional blunting than typical SSRIs and SNRIs. [6] A withdrawal syndrome may occur if the dose is rapidly decreased. [1] Use during pregnancy and breastfeeding is not generally recommended. [7] It is in the serotonin modulator class of medications and is believed to work both as an SSRI and activator of the 5-HT1A receptor. [1]
Vilazodone was approved for medical use in the United States in 2011 [1] and in Canada in 2018. [8] In 2019, it was the 334th most commonly prescribed medication in the United States, with more than 900 thousand prescriptions. [9] The drug lost patent protection in June 2022 for adults and in July 2023 for pediatrics. [10] Generic versions have been approved by the U.S. Food and Drug Administration (FDA). [11] [12]
Seven controlled efficacy trials were conducted of vilazodone for treatment of major depressive disorder (MDD). [13] Five of these trials showed no significant influence of vilazodone over placebo on depressive symptoms. [13] In the remaining two trials, small but significant advantages of vilazodone over placebo were found. [13] According to these two eight-week trials in adults, vilazodone has an antidepressant response after one week of treatment. [14] After eight weeks it resulted in a 13% greater response than placebo. [14] Remission rates, however, were not significantly different versus placebo. [14]
According to the US Food and Drug Administration (FDA) staff in 2011, "it is unknown whether vilazodone has any advantages compared to other drugs in the antidepressant class." [15] A 2019 review stated that "present studies do not suggest the superiority of vilazodone compared with other antidepressants." [16]
Development of vilazodone for generalized anxiety disorder (GAD) has been stopped as of 2017. [17] While there is tentative evidence of a small benefit in GAD, there is a high rate of side effects. [18]
In September 2016, the FDA wrote a letter to Forest Labs requiring a new warning to be added to the label related to a link between the drug and acute pancreatitis and sleep paralysis. [19]
The most common adverse effects include nausea, diarrhea, vomiting, and insomnia. [5]
After a one-year, open-label study assessing the safety and tolerability of vilazodone in people with major depressive disorder, the most common adverse effects were diarrhea (35.7%), nausea (31.6%), and headache (20.0%); greater than 90% of these adverse effects were mild or moderate. [20] [14] In randomized controlled trials, meanwhile, these rates were 28%, 23.4% and 13.3%, respectively. [14] In contrast to other SSRIs, initial trials showed that vilazodone did not cause decreased sexual desire/function, which often cause people to abandon their use. [21][ unreliable medical source?] Additionally, vilazodone may cause less emotional blunting than typical SSRIs and SNRIs. [6]
Antidepressant exposure (including vilazodone) is associated with shorter average duration of pregnancy (by three days), increased risk of preterm delivery (by 55%), lower birth weight (by 75 g), and lower Apgar scores (by <0.4 points). [22] [23] It is uncertain whether there is an increased rate of septal heart defects among children whose mothers were prescribed an SSRI in early pregnancy. [24] [25]
Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 2.1 nM; Ki = 0.1 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60–70%). [14] [26] It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C, [26] [27] as well as the norepinephrine and dopamine transporters (Ki = 56 nM for NET and 37 nM for DAT). [5] A small clinical study found occupancy of the 5-HT1A receptor with vilazodone, whereas occupancy of the SERT by vilazodone in humans does not seem to have been studied. [28] [29] [30]
Vilazodone is best absorbed with food and has a bioavailability of 72% under fed conditions. The Cmax increased between 147 and 160% and the AUC increased between 64 and 85% of vilazodone when it was administered with either a fatty or light meal. [31]
It was developed by Merck KGaA and licensed by Clinical Data, a biotech company purchased by Forest Laboratories in 2011. [32]
Clinical data | |
---|---|
Pronunciation |
/vɪˈlæzədoʊn/ vi-LAZ-ə-dohn |
Trade names | Viibryd |
Other names | EMD-68843; SB-659746A |
AHFS/ Drugs.com | Monograph |
MedlinePlus | a611020 |
License data |
|
Routes of administration | By mouth |
Drug class | Serotonin modulator [1] |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Bioavailability | 72% (oral, with food) [5] |
Metabolism | Liver via CYP3A4 [5] |
Elimination half-life | 25 hours [5] |
Excretion | Faecal and renal [5] |
Identifiers | |
| |
CAS Number |
|
PubChem CID | |
IUPHAR/BPS | |
DrugBank |
|
ChemSpider | |
UNII |
|
KEGG | |
ChEBI |
|
ChEMBL |
|
PDB ligand | |
Chemical and physical data | |
Formula | C26H27N5O2 |
Molar mass | 441.535 g·mol−1 |
3D model ( JSmol) | |
| |
| |
(what is this?) (verify) |
Vilazodone, sold under the brand name Viibryd among others, is a medication used to treat major depressive disorder. [1] It is classified as a serotonin modulator [1] and is taken by mouth. [1]
Common side effects include nausea, diarrhea, and trouble sleeping. [1] Serious side effects may include increased suicidal thoughts or actions in those under the age of 25, serotonin syndrome, bleeding, mania, pancreatitis, and SIADH. [1] Vilazodone may cause less emotional blunting than typical SSRIs and SNRIs. [6] A withdrawal syndrome may occur if the dose is rapidly decreased. [1] Use during pregnancy and breastfeeding is not generally recommended. [7] It is in the serotonin modulator class of medications and is believed to work both as an SSRI and activator of the 5-HT1A receptor. [1]
Vilazodone was approved for medical use in the United States in 2011 [1] and in Canada in 2018. [8] In 2019, it was the 334th most commonly prescribed medication in the United States, with more than 900 thousand prescriptions. [9] The drug lost patent protection in June 2022 for adults and in July 2023 for pediatrics. [10] Generic versions have been approved by the U.S. Food and Drug Administration (FDA). [11] [12]
Seven controlled efficacy trials were conducted of vilazodone for treatment of major depressive disorder (MDD). [13] Five of these trials showed no significant influence of vilazodone over placebo on depressive symptoms. [13] In the remaining two trials, small but significant advantages of vilazodone over placebo were found. [13] According to these two eight-week trials in adults, vilazodone has an antidepressant response after one week of treatment. [14] After eight weeks it resulted in a 13% greater response than placebo. [14] Remission rates, however, were not significantly different versus placebo. [14]
According to the US Food and Drug Administration (FDA) staff in 2011, "it is unknown whether vilazodone has any advantages compared to other drugs in the antidepressant class." [15] A 2019 review stated that "present studies do not suggest the superiority of vilazodone compared with other antidepressants." [16]
Development of vilazodone for generalized anxiety disorder (GAD) has been stopped as of 2017. [17] While there is tentative evidence of a small benefit in GAD, there is a high rate of side effects. [18]
In September 2016, the FDA wrote a letter to Forest Labs requiring a new warning to be added to the label related to a link between the drug and acute pancreatitis and sleep paralysis. [19]
The most common adverse effects include nausea, diarrhea, vomiting, and insomnia. [5]
After a one-year, open-label study assessing the safety and tolerability of vilazodone in people with major depressive disorder, the most common adverse effects were diarrhea (35.7%), nausea (31.6%), and headache (20.0%); greater than 90% of these adverse effects were mild or moderate. [20] [14] In randomized controlled trials, meanwhile, these rates were 28%, 23.4% and 13.3%, respectively. [14] In contrast to other SSRIs, initial trials showed that vilazodone did not cause decreased sexual desire/function, which often cause people to abandon their use. [21][ unreliable medical source?] Additionally, vilazodone may cause less emotional blunting than typical SSRIs and SNRIs. [6]
Antidepressant exposure (including vilazodone) is associated with shorter average duration of pregnancy (by three days), increased risk of preterm delivery (by 55%), lower birth weight (by 75 g), and lower Apgar scores (by <0.4 points). [22] [23] It is uncertain whether there is an increased rate of septal heart defects among children whose mothers were prescribed an SSRI in early pregnancy. [24] [25]
Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 2.1 nM; Ki = 0.1 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60–70%). [14] [26] It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C, [26] [27] as well as the norepinephrine and dopamine transporters (Ki = 56 nM for NET and 37 nM for DAT). [5] A small clinical study found occupancy of the 5-HT1A receptor with vilazodone, whereas occupancy of the SERT by vilazodone in humans does not seem to have been studied. [28] [29] [30]
Vilazodone is best absorbed with food and has a bioavailability of 72% under fed conditions. The Cmax increased between 147 and 160% and the AUC increased between 64 and 85% of vilazodone when it was administered with either a fatty or light meal. [31]
It was developed by Merck KGaA and licensed by Clinical Data, a biotech company purchased by Forest Laboratories in 2011. [32]