Vilazodone, sold under the brand name Viibryd among others, is a

medication A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy ( pharmacotherapy) is an important part of the medical field and ...

used to treat

major depressive disorder Major depressive disorder (MDD), also known as clinical depression, is a mental disorder characterized by at least two weeks of pervasive low mood, low self-esteem, and loss of interest or pleasure in normally enjoyable activities. Intro ...

. It is taken by mouth. Common side effects include nausea, diarrhea, and trouble sleeping. Serious side effects may include increased suicidal thoughts or actions in those under the age of 25, serotonin syndrome, bleeding, mania,

pancreatitis Pancreatitis is a condition characterized by inflammation of the pancreas. The pancreas is a large organ behind the stomach that produces digestive enzymes and a number of hormones. There are two main types: acute pancreatitis, and chronic p ...

, and SIADH. Vilazodone may cause less

emotional blunting Reduced affect display, sometimes referred to as emotional blunting or emotional numbing, is a condition of reduced emotional reactivity in an individual. It manifests as a failure to express feelings (affect display) either verbally or nonverba ...

than typical

SSRIs Selective serotonin reuptake inhibitors (SSRIs) are a class of drugs that are typically used as antidepressants in the treatment of major depressive disorder, anxiety disorders, and other psychological conditions. SSRIs increase the extracellu ...

and SNRIs. A

withdrawal syndrome Drug withdrawal, drug withdrawal syndrome, or substance withdrawal syndrome, is the group of symptoms that occur upon the abrupt discontinuation or decrease in the intake of pharmaceutical or recreational drugs. In order for the symptoms of with ...

may occur if the dose is rapidly decreased. Use during

pregnancy Pregnancy is the time during which one or more offspring develops ( gestates) inside a woman's uterus (womb). A multiple pregnancy involves more than one offspring, such as with twins. Pregnancy usually occurs by sexual intercourse, but ...

and

breastfeeding Breastfeeding, or nursing, is the process by which human breast milk is fed to a child. Breast milk may be from the breast, or may be expressed by hand or pumped and fed to the infant. The World Health Organization (WHO) recommends that bre ...

is not generally recommended. It is in the serotonin modulator class of medications and is believed to work both as an SSRI and activator of the 5-HT_1A receptor. Vilazodone was approved for medical use in the United States in 2011 and in Canada in 2018. In 2019, it was the 334th most commonly prescribed medication in the United States, with more than 900thousand prescriptions. The drug lost patent protection in June 2022 for adults, and is scheduled to lose exclusivity for pediatrics in July 2023. Generic versions have been approved by the U.S.

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food ...

(FDA).

Medical uses

Seven controlled efficacy trials were conducted of vilazodone for treatment of

(MDD). Five of these trials showed no significant influence of vilazodone over

placebo A placebo ( ) is a substance or treatment which is designed to have no therapeutic value. Common placebos include inert tablets (like sugar pills), inert injections (like Saline (medicine), saline), sham surgery, and other procedures. In general ...

on depressive symptoms. In the remaining two trials, small but significant advantages of vilazodone over placebo were found. According to these two eight-week trials in adults, vilazodone has an

antidepressant Antidepressants are a class of medication used to treat major depressive disorder, anxiety disorders, chronic pain conditions, and to help manage addictions. Common Side effect, side-effects of antidepressants include Xerostomia, dry mouth, weig ...

response after one week of treatment. After eight weeks it resulted in a 13% greater response than placebo. Remission rates, however, were not significantly different versus placebo. According to FDA staff in 2011, "it is unknown whether vilazodone has any advantages compared to other drugs in the antidepressant class." A 2019 review stated that "present studies do not suggest the superiority of vilazodone compared with other antidepressants." Development of vilazodone for generalized anxiety disorder (GAD) has been stopped as of 2017. While there is tentative evidence of a small benefit in GAD, there is a high rate of side effects.

Adverse effects

On September 6, 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. 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 Diarrhea, also spelled diarrhoea, is the condition of having at least three loose, liquid, or watery bowel movements each day. It often lasts for a few days and can result in dehydration due to fluid loss. Signs of dehydration often begin w ...

(35.7%),

nausea Nausea is a diffuse sensation of unease and discomfort, sometimes perceived as an urge to vomit. While not painful, it can be a debilitating symptom if prolonged and has been described as placing discomfort on the chest, abdomen, or back of th ...

(31.6%), and

headache Headache is the symptom of pain in the face, head, or neck. It can occur as a migraine, tension-type headache, or cluster headache. There is an increased risk of depression in those with severe headaches. Headaches can occur as a result ...

(20.0%); greater than 90% of these adverse effects were mild or moderate. In randomized controlled trials, meanwhile, these rates were 28%, 23.4% and 13.3%, respectively. 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. Additionally, Vilazodone may cause less

than typical

and SNRIs. Incidence of adverse effects include: ;Very common adverse effects (incidence >10%): * Nausea * Diarrhea * Headache ;Common adverse effects (1–10% incidence) * Vomiting * Dry mouth * Dizziness *

Insomnia Insomnia, also known as sleeplessness, is a sleep disorder in which people have trouble sleeping. They may have difficulty falling asleep, or staying asleep as long as desired. Insomnia is typically followed by daytime sleepiness, low energy, ...

;Uncommon adverse effects (0.1–1% incidence): *

Somnolence Somnolence (alternatively sleepiness or drowsiness) is a state of strong desire for sleep, or sleeping for unusually long periods (compare hypersomnia). It has distinct meanings and causes. It can refer to the usual state preceding falling asleep ...

* Paraesthesia * Tremor * Abnormal dreams * Libido decreased * Restlessness * Akathisia * Restless legs syndrome * Abnormal orgasms (men only) * Delayed ejaculations (men only) * Erectile dysfunction (men only) * Fatigue * Feeling jittery * Palpitations * Ventricular premature contractions * Arthralgia * Increased appetite ;Rare adverse effects (<0.1% incidence): * Serotonin syndrome—a serious adverse effect characterised by: **Nausea **Vomiting **Mental status change (e.g. confusion, hallucinations, agitation, coma, stupor) **Muscle rigidity **Tremor ** Myoclonus ** Hyperreflexia—overresponsive/overactive reflexes **Hyperthermia—elevated body temperature **Autonomic instability (e.g. tachycardia, dizziness, abnormally excessive sweating, etc.) * Mania/

hypomania Hypomania (literally "under mania" or "less than mania") is a mental and behavioural disorder, characterised essentially by an apparently non-contextual elevation of mood (euphoria) that contributes to persistently disinhibited behaviour. Th ...

—a potentially dangerously elated/agitated mood. Every antidepressant has the potential to induce these psychiatric reactions. They are particularly problematic in those with a history of hypomania/mania such as those with

bipolar disorder Bipolar disorder, previously known as manic depression, is a mental disorder characterized by periods of Depression (mood), depression and periods of abnormally elevated Mood (psychology), mood that last from days to weeks each. If the elevat ...

.Australian Medicines Handbook 2013. The Australian Medicines Handbook Unit Trust; 2013. ;Unknown-incidence adverse effects: * Suicidal ideation—all antidepressants can cause suicidal ideation especially in young adults and adolescents under the age of 25. * Abnormal bleeding—the SSRIs are known for their ability to increase the incidence of gastrointestinal bleeds and other bleeding abnormalities.Taylor D, Paton C, Kapur S, Taylor D. The Maudsley prescribing guidelines in psychiatry. 11th ed. Chichester, West Sussex: John Wiley & Sons; 2012. * Seizures * Syndrome of inappropriate antidiuretic hormone secretion (SIADH)—a condition characterised by an abnormally excessive secretion of

antidiuretic hormone Human vasopressin, also called antidiuretic hormone (ADH), arginine vasopressin (AVP) or argipressin, is a hormone synthesized from the AVP gene as a peptide prohormone in neurons in the hypothalamus, and is converted to AVP. It then travel ...

causing potentially-fatal electrolyte abnormalities (such as hyponatraemia). * Hyponatraemia (a complication of the former)—low blood sodium.

Pregnancy

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 score The Apgar score is a quick way for doctors to evaluate the health of all newborns at 1 and 5 minutes after birth and in response to resuscitation. It was originally developed in 1952 by an anesthesiologist at Columbia University, Virginia Apgar ...

s (by <0.4 points). It is uncertain whether there is an increased rate of septal heart defects among children whose mothers were prescribed an SSRI in early pregnancy.

Pharmacology

Pharmacodynamics

Vilazodone acts as a serotonin reuptake inhibitor (IC₅₀ = 2.1 nM; K_i = 0.1 nM) and 5-HT_1A receptor

partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonis ...

(IC₅₀ = 0.2 nM; IA = ~60–70%). It has negligible affinity for other

serotonin receptor 5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in the central and peripheral nervous systems. They mediate both excitatory and inhibitory ne ...

s such as 5-HT_1D, 5-HT_2A, and 5-HT_2C. It also exhibits inhibitory activity at the norepinephrine and dopamine transporters (K_i = 56 nM for NET and 37 nM for DAT). A small clinical study found

occupancy Within the context of building construction and building codes, "occupancy" refers to the use, or intended use, of a building, or portion of a building, for the shelter or support of persons, animals or property. A closely related meaning is ...

of the 5-HT_1A receptor with vilazodone, whereas occupancy of the SERT by vilazodone in humans does not seem to have been studied.

Pharmacokinetics

Vilazodone is best absorbed with food and has a bioavailability of 72% under fed conditions. The C_max increased between 147 to 160% and the AUC increased between 64 to 85% of vilazodone when it was administered with either a fatty or light meal.

History

It was developed by Merck KGaA and licensed by Clinical Data, a biotech company purchased by

Forest Laboratories Forest Laboratories was a company in the pharmaceutical industry incorporated in Delaware, with its principal office in New York City. It was known for licensing European pharmaceuticals for sale in the United States. On July 1, 2014, the comp ...

in 2011.

Research

While it was being studied for generalized anxiety disorder, such research had stopped as of 2017.

References

External links

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