Action and Spectrum

Actions and spectrum: 

vilazodone is selective serotonin reuptake inhibitor (SSRI) and partial agonist of the serotonin 5-HT1A receptor. It acts by increasing the levels of serotonin, a neurotransmitter in the brain that regulates mood, anxiety, and other emotional states.

vilazodone is primarily used for the treatment of the major depressive disorder (MDD) in adults. It may also be effective in the treatment of anxiety disorders. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Nausea (23%) 

Diarrhea (28%)  

1-10% 

Dizziness (9%) 

Insomnia (6%) 

Fatigue (4%) 

Libido decreased (4%) 

Dyspepsia (3%) 

Gastroenteritis (3%) 

Paresthesia (3%) 

Restlessness/akathisia (3%) 

Tremor (2%) 

Erectile dysfunction (2%) 

Xerostomia (8%) 

Vomiting (5%) 

Abnormal dreams (4%) 

Abnormal orgasm (3%) 

Flatulence (3%) 

Somnolence (3%) 

Arthralgia (3%) 

Jittery sensation (2%) 

Delayed ejaculation (2%) 

Increased appetite (2%) 

Post marketing Reports 

Gastrointestinal disorders 

Nervous system disorders 

Psychiatric disorders 

Black Box Warning

Black Box Warning:  

It has an increased risk of suicidal behavior and thinking in children, adolescents, and young adults with psychiatric disorders and major depressive disorders. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

vilazodone is contraindicated in individuals with known hypersensitivity to vilazodone or any component of the formulation. It is also contraindicated in individuals who have taken monoamine oxidase inhibitors (MAOIs) within the past 14 days, as concurrent use with MAOIs can lead to serotonin syndrome, a potentially life-threatening condition. Additionally, the use of vilazodone is contraindicated in individuals taking pimozide due to the risk of QT prolongation.  

Caution: 

• Suicidal thoughts or behaviors: vilazodone can increase the risk of suicidal thinking or behavior in some individuals, especially those under the age of 24. 
• Serotonin syndrome: vilazodone can cause a potentially life-threatening condition known as serotonin syndrome, which can be characterized by symptoms such as hallucinations, fever, agitation, sweating,  fast heart rate, twitching, muscle stiffness, loss of coordination, diarrhoea, nausea and vomiting. 
• Hypersensitivity: vilazodone may cause allergic reactions in some individuals, especially those who are allergic to other medications that work by increasing serotonin levels. 
• Bleeding disorders: vilazodone may increase the risk of bleeding, especially in individuals with a history of bleeding disorders or those taking other medications that increase the risk of bleeding. 
• Mania/hypomania: vilazodone may cause or worsen symptoms of mania or hypomania in individuals with a history of bipolar disorder. 
• Hyponatremia: vilazodone may cause low levels of sodium in the blood, which can be characterized by symptoms such as headache, confusion, weakness, and seizures. 
• Angle-closure glaucoma: vilazodone may cause an increase in eye pressure, which can lead to a condition called angle-closure glaucoma. Individuals with a history of glaucoma or those at risk for the condition should use vilazodone with caution.

Comorbidities: 

• History of mania/hypomania: vilazodone may trigger a manic episode in patients with a history of mania or hypomania. 
• Suicidal ideation: As with all antidepressant medications, vilazodone may have an increased risk of suicidal thoughts or behavior, particularly in young adults (18-24 years of age). 
• Seizure disorders: vilazodone should be used with caution in patients with seizure disorders, as it may lower the seizure threshold. 
• Renal/hepatic impairment: Dosage adjustments may be required in patients with renal or hepatic impairment. 
• Bleeding disorders: vilazodone may increase the risk of bleeding in patients with bleeding disorders or those taking anticoagulant medications. 
• Hyponatremia: SSRIs, including vilazodone, have been associated with the development of hyponatremia (low blood sodium levels), particularly in elderly patients and those taking diuretics. 
• Pregnancy/breastfeeding: The safety of vilazodone during pregnancy and breastfeeding is not well established. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category C 

Lactation: safety and efficacy not established

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

vilazodone is selective serotonin reuptake inhibitor (SSRI) and a partial agonist of the 5-HT1A receptor. It acts by increasing the levels of serotonin in the brain, which helps to improve mood and relieve symptoms of depression. vilazodone is rapidly absorbed after oral administration and reaches peak plasma concentration within 4 to 5 hours.

It has an elimination half-life of approximately 25 hours and is primarily metabolized in the liver by cytochrome P450 enzymes. The pharmacological effects of vilazodone include the inhibition of serotonin reuptake, which leads to increased levels of serotonin in the synaptic cleft. This in turn leads to increased activation of post-synaptic 5-HT1A receptors, which are thought to be involved in the antidepressant effects of the drug.

The partial agonist activity of vilazodone at 5-HT1A receptors may contribute to its efficacy and may also reduce the incidence of side effects commonly associated with SSRIs. vilazodone has also been shown to have anxiolytic effects in preclinical studies, although the exact mechanism of action for this is not well understood.  

Pharmacodynamics: 

vilazodone is selective serotonin reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist. The medication works by blocking the reuptake of serotonin, a neurotransmitter that regulates mood, by binding to the serotonin transporter, increasing its concentration in the synaptic cleft, and enhancing serotonin neurotransmission.

It also acts as a partial agonist at the 5-HT1A receptor, which is involved in the modulation of mood, anxiety, and other functions in the central nervous system. The precise mechanism by which vilazodone produces its antidepressant effects is not fully understood, but it is thought to involve the modulation of multiple neurotransmitter systems.  

Pharmacokinetics: 

Absorption 

vilazodone is rapidly absorbed after oral administration, with peak plasma concentrations reached within 4 to 5 hours. Food does not have a significant effect on its absorption. 

Distribution 

vilazodone has a high protein binding of about 96%. The apparent volume of distribution is approximately 4200 L. 

Metabolism 

vilazodone is primarily metabolized by CYP3A4 and, to a lesser extent, by CYP2C19. The major metabolite is an inactive N-demethylated compound. 

Elimination and excretion 

vilazodone is eliminated mainly through hepatic metabolism, with the majority of the dose excreted in the feces. The elimination half-life is about 25 hours. It is not known whether vilazodone is excreted in human milk. 

Adminstartion

Administration: 

vilazodone is available in tablet form for oral administration. It is recommended to take vilazodone with food to increase its oral bioavailability. The duration and dosage of treatment may vary depending on the individual’s condition and response to treatment. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: vilazodone 

Pronounced: [vil-az-oh-done]  

Why do we use vilazodone? 

vilazodone is primarily used for the treatment of the major depressive disorder (MDD) in adults. It is a selective serotonin reuptake inhibitor (SSRI) and serotonin receptor partial agonist, which means it acts by increasing serotonin levels, thereby improving mood, appetite, and sleep patterns. It is also used off-label to treat anxiety disorders, such as generalized anxiety disorder (GAD).