|AHFS/Drugs.com||Consumer Drug Information|
|Bioavailability||72% (oral, with food)|
|Metabolism||Hepatic via CYP3A4|
|Elimination half-life||25 hours|
|Excretion||Faecal and renal|
|Chemical and physical data|
|Molar mass||441.524 g/mol|
|3D model (JSmol)|
|‹See TfM› (what is this?)|
Vilazodone (United States trade name Viibryd) is a serotonergic antidepressant developed by Merck KGaA and licensed by Clinical Data, a biotech company purchased by Forest Laboratories in 2011. Vilazodone was approved in 2011 by the FDA for use in the United States to treat major depressive disorder. Its mechanism of action is believed to be a combination of SSRI-like activity (SERT inhibition) and 5HT1AR partial agonism, like the structurally related anxiolytic buspirone. As such it can be compared to vortioxetine, and these two drugs are sometimes used as the prototypical members of the class of serotonin modulator/stimulator antidepressants.
According to two eight-week, randomized, double-blind, placebo-controlled trials in adults, vilazodone elicits an antidepressant response after one week of treatment. After eight weeks, subjects assigned to vilazodone 40 mg daily dose (titrated over two weeks) experienced a higher response rate than the group given placebo (44% vs 30%, P = .002). Remission rates for vilazodone were not significantly different versus placebo.
According to an article on the United States approval of vilazodone written by FDA staff, "it is unknown whether [vilazodone] has any advantages compared to other drugs in the antidepressant class."
On September 6, 2016, the FDA wrote a letter to Forest Labs about Viibryd. New warnings will be added to the Viibryd label related to a link between the drug and acute pancreatitis. Acute pancreatitis can lead to serious injury and even death. Pancreatitis, especially if it reoccurs, can lead to pancreatic cancer, which is almost always fatal.
Additionally, it is expected that new warnings related to sleep paralysis will also be added to the Viibryd label and prescribing information. Sleep paralysis is a condition in which a person is awake but cannot move or speak. Generally, sleep paralysis occurs upon waking and lasts less than one minute. Although sleep paralysis is a serious condition, and can cause psychological harm in the most severe cases, the condition is generally not life threatening.
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. Whereas in randomized controlled trials these rates were 28%, 23.4% and 13.3%, respectively. In contrast to other SSRIs currently on the market, initial clinical trials showed that vilazodone did not cause significant decreased sexual desire/function as with many other antidepressants, which often cause people to abandon their use.
Incidence of adverse effects
Incidence of adverse effects include:
- Very common adverse effects (incidence >10%)
- Common adverse effects (1–10% incidence)
- Dry mouth
- Uncommon adverse effects (0.1–1% incidence)
- Abnormal dreams
- Libido decreased
- Restless legs syndrome
- Abnormal orgasms (male persons only)
- Delayed ejaculations (male persons only)
- Erectile dysfunction (male persons only)
- Feeling jittery
- Ventricular premature contractions
- Increased appetite
- Rare adverse effects (<0.1% incidence)
- Serotonin syndrome—a serious adverse effect characterised by:
- Mental status change (e.g. confusion, hallucinations, agitation, coma, stupor)
- Muscle rigidity
- Hyperreflexia—overresponsive/overactive reflexes
- Hyperthermia—elevated body temperature
- Autonomic instability (e.g. tachycardia, dizziness, abnormally excessive sweating, etc.)
- Mania/hypomania—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.
- 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.
- Syndrome of inappropriate antidiuretic hormone secretion (SIADH)—a condition characterised by an abnormally excessive secretion of antidiuretic hormone causing potentially-fatal electrolyte abnormalities (such as hyponatraemia).
- Hyponatraemia (a complication of the former)—low blood sodium.
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%). It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C. It also exhibits clinically unimportant inhibitory activity at the norepinephrine and dopamine transporters (Ki = 56 nM for NET and 37 nM for DAT). Vilazdone is best absorbed with food and has a bioavailability of 72% under fed conditions. The Cmax increased between 147%-160% and the AUC increased between 64%-85% of vilazodone when it was administered with either a fatty or light meal.
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