Vilazodone

Vilazodone
Clinical data
Pronunciation /ˈvaɪbrɪd/ VY-brid
Trade names Viibryd
Synonyms EMD-68843; SB-659746A
AHFS/Drugs.com Consumer Drug Information
MedlinePlus a611020
License data
Pregnancy
category
  • US: C (Risk not ruled out)
    Routes of
    administration    		 Oral
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Bioavailability 72% (oral, with food)[1]
    Metabolism Hepatic via CYP3A4[1]
    Elimination half-life 25 hours[1]
    Excretion Faecal and renal[1]
    Identifiers
    CAS Number
    PubChem CID
    IUPHAR/BPS
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    Chemical and physical data
    Formula C26H27N5O2
    Molar mass 441.524 g/mol
    3D model (JSmol)
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    Vilazodone (United States trade name Viibryd) is a serotonergic antidepressant developed by Merck KGaA[2] and licensed by Clinical Data, a biotech company purchased by Forest Laboratories in 2011.[3] Vilazodone was approved in 2011 by the FDA for use in the United States to treat major depressive disorder.[4][5][6] 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.

    Medical uses

    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.[7]

    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."[8]

    Adverse effects

    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.[7] Whereas in randomized controlled trials these rates were 28%, 23.4% and 13.3%, respectively.[7] 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.[4]

    Incidence of adverse effects

    Incidence of adverse effects include:[1]

    Very common adverse effects (incidence >10%)
    • Nausea
    • Diarrhea
    • Headache
    Common adverse effects (1–10% incidence)
    Uncommon adverse effects (0.1–1% incidence)
    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—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.[9]
    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.[9][10][11]
    • Seizures
    • 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.

    Pharmacology

    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%).[7][12] It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C.[12][13] It also exhibits clinically unimportant inhibitory activity at the norepinephrine and dopamine transporters (Ki = 56 nM for NET and 37 nM for DAT).[1] 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.[14]

    See also

    References

    1. 1 2 3 4 5 6 "VIIBRYD (vilazodone hydrochloride) tablet VIIBRYD (vilazodone hydrochloride) kit [Forest Laboratories, Inc.]". DailyMed. Forest Laboratories, Inc. December 2012. Archived from the original on 29 October 2013. Retrieved 28 October 2013.
    2. ↑ "Clinical Data's Vilazodone Patient Enrollment Over One Third Complete". Business Wire. Berkshire Hathaway. 17 August 2006. Archived from the original on 13 April 2014. Retrieved 12 April 2014.
    3. ↑ "Xconomy: Blend Therapeutics Taps Former Clinical Data Chief Fromkin As New CEO". xconomy.com. 13 April 2015. Archived from the original on 9 September 2017. Retrieved 6 May 2018.
    4. 1 2 "FDA approves Clinical Data Inc's antidepressant". Reuters. January 22, 2011. Archived from the original on January 27, 2011.
    5. ↑ "FDA approves Clinical Data Inc's antidepressant". Reuters. January 22, 2011. Archived from the original on 27 January 2011. Retrieved 12 April 2014.
    6. ↑ "Clinical Data, Inc. - Clinical Data, Inc. Submits New Drug Application for Vilazodone for the Treatment of Major Depressive Disorder". Archived from the original on 18 August 2011. Retrieved 12 April 2014.
    7. 1 2 3 4 Wang, SM; Han, C; Lee, SJ; Patkar, AA; Masand, PS; Pae, CU (August 2013). "A review of current evidence for vilazodone in major depressive disorder". International Journal of Psychiatry in Clinical Practice. 17 (3): 160–9. doi:10.3109/13651501.2013.794245. PMID 23578403.
    8. ↑ Laughren TP, Gobburu J, Temple RJ, Unger EF, Bhattaram A, Dinh PV, Fossom L, Hung HM, Klimek V, Lee JE, Levin RL, Lindberg CY, Mathis M, Rosloff BN, Wang SJ, Wang Y, Yang P, Yu B, Zhang H, Zhang L, Zineh I (September 2011). "Vilazodone: clinical basis for the US Food and Drug Administration's approval of a new antidepressant". The Journal of Clinical Psychiatry. 72 (9): 1166–73. doi:10.4088/JCP.11r06984. PMID 21951984.
    9. 1 2 Australian Medicines Handbook 2013. The Australian Medicines Handbook Unit Trust; 2013.
    10. ↑ Taylor D, Paton C, Kapur S, Taylor D. The Maudsley prescribing guidelines in psychiatry. 11th ed. Chichester, West Sussex: John Wiley & Sons; 2012.
    11. ↑ Wang Y-P, Chen Y-T, Tsai C-F, Li S-Y, Luo J-C, Wang S-J, et al. Short-Term Use of Serotonin Reuptake Inhibitors and Risk of Upper Gastrointestinal Bleeding. Am J Psychiatry [Internet]. 2013 Sep 13 [cited 2013 Oct 6]; Available from: http://ajp.psychiatryonline.org/article.aspx?articleid=1738031
    12. 1 2 Hughes ZA, Starr KR, Langmead CJ, et al. (March 2005). "Neurochemical evaluation of the novel 5-HT1A receptor partial agonist/serotonin reuptake inhibitor, vilazodone". European Journal of Pharmacology. 510 (1–2): 49–57. doi:10.1016/j.ejphar.2005.01.018. PMID 15740724.
    13. ↑ Page ME, Cryan JF, Sullivan A, et al. (September 2002). "Behavioral and neurochemical effects of 5-(4-[4-(5-Cyano-3-indolyl)-butyl)-butyl]-1-piperazinyl)-benzofuran-2-carboxamide (EMD 68843): a combined selective inhibitor of serotonin reuptake and 5-hydroxytryptamine(1A) receptor partial agonist". The Journal of Pharmacology and Experimental Therapeutics. 302 (3): 1220–7. doi:10.1124/jpet.102.034280. PMID 12183683.
    14. ↑ Cruz MP (2012). "Vilazodone HCl (Viibryd): A Serotonin Partial Agonist and Reuptake Inhibitor For the Treatment of Major Depressive Disorder". P T. 37 (1): 28–31. PMC 3278186. PMID 22346333.
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