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Class: Selective serotonin reuptake inhibitor, Serotonin 5HT 1A receptor agonist
- Tablets, oral 10 mg
- Tablets, oral 20 mg
- Tablets, oral 40 mg
- Tablets, oral Starter kit contains seven 10 mg, seven 20 mg, and sixteen 40 mg tablets (total of 30 tablets)
Undetermined; thought to be related to potentiation of serotonergic activity in the CNS. Vilazodone is also a partial agonist at serotonergic 5-HT 1A receptors.
T max is 4 to 5 h, C max is 156 ng/mL, and AUC is 1,645 ng•h/mL under fed conditions. Steady state is achieved in approximately 3 days. Absolute bioavailability is 72% with food. Administration with food increases C max by approximately 147% to 160% and AUC by approximately 64% to 85%.
96% to 99% protein bound.
Extensively metabolized through CYP (primarily 3A4) and non-CYP pathways. Only 1% of the dose recovered in the urine and 2% of the dose recovered in the feces is unchanged vilazodone.
Terminal half-life is approximately 25 h.
Special PopulationsRenal Function Impairment
Mild or moderate renal impairment did not affect the apparent Cl of vilazodone.Hepatic Function Impairment
Mild or moderate hepatic impairment did not affect the apparent Cl of vilazodone.
Indications and Usage
Treatment of major depressive disorder (MDD).
Concomitant use in patients taking MAOIs or in patients who have taken MAOIs within the preceding 14 days.
Dosage and AdministrationMajor depressive disorder
PO Titrate, starting with 10 mg once daily for 7 days, followed by 20 mg once daily for 7 days, and then increase to 40 mg once daily.
- Administer with food.
- If discontinuation of therapy is required, gradual dose reduction is recommended, instead of abrupt discontinuation, whenever possible.
Store between 56° and 86°F.
Drug InteractionsAspirin, NSAIDs (eg, naproxen)
Concomitant use may increase the risk of bleeding.CNS-acting drugs
The risk of using vilazodone with other CNS-active drugs has not been systematically evaluated. Use with caution.CYP2C8 substrates (eg, paclitaxel)
Coadministration of the CYP2C8 substrates may be increased; however, the effect of vilazodone on CYP2C8 has not been studied.CYP3A4 inducers (eg, phenytoin)
Vilazodone plasma concentrations may be reduced. However, the effects of CYP3A4 inducers have not been evaluated.CYP3A4 moderate inhibitors (eg, erythromycin)
Vilazodone plasma concentrations may be increased. Reduce the vilazodone dosage to 20 mg once daily for patients experiencing intolerable adverse events. No dosage adjustment is recommended with coadministration of mild CYP3A4 inhibitors (eg, cimetidine).CYP3A4 strong inhibitors (eg, ketoconazole)
Vilazodone plasma concentrations may be increased by approximately 50%. If vilazodone is administered with a strong CYP3A4 inhibitor, reduce the vilazodone dosage to 20 mg once daily.Food
Coadministration increases vilazodone C max and AUC. Vilazodone should be taken with food.MAOIs (eg, phenelzine, rasagiline, selegiline)
Coadministration is contraindicated. Serious, sometimes fatal, reactions may occur. It is recommended that vilazodone not be used in combination with an MAOI or within at least 14 days of discontinuing treatment with an MAOI. Allow at least 14 days after stopping vilazodone before starting an MAOI.Serotonergic drugs (eg, buspirone, SNRIs, SSRIs, tramadol, tryptophan)
Potential for serotonin toxicity, also known as serotonin syndrome (eg, agitation, altered consciousness, ataxia, myoclonus, overactive reflexes, shivering), may be increased. Use with caution.Triptans (eg, almotriptan, eletriptan, naratriptan, sumatriptan)
Risk of NMS-like reactions or serotonin syndrome (eg, agitation, altered consciousness, ataxia, myoclonus, overactive reflexes, shivering) may be increased. If coadministration cannot be avoided, closely monitor patients for emergence of serotonin syndrome or NMS-like signs or symptoms. If signs or symptoms occur, discontinue both drugs immediately and initiate supportive symptomatic treatment.Warfarin
Altered anticoagulant effects, including increased bleeding, have been reported. Carefully monitor warfarin therapy when vilazodone is initiated or discontinued.
Dizziness (9%); insomnia (6%); libido increased (5%); abnormal dreams, abnormal orgasm, fatigue (4%); paresthesia, restlessness, somnolence (3%); feeling jittery, sexual dysfunction, tremor (2%); migraine, sedation (at least 1%).
Hyperhidrosis, night sweats (at least 1%).
Blurred vision, dry eye (at least 1%).
Diarrhea (28%); nausea (23%); dry mouth (8%); vomiting (5%); dyspepsia, flatulence, gastroenteritis (3%).
Delayed ejaculation, erectile dysfunction (2%).
Increased appetite (2%); decreased appetite (at least 1%).
Antidepressants increase the risk compared with placebo of suicidal thinking and behavior in short-term studies in children, adolescents, and young adults with MDD and other psychiatric disorders. Closely observe patients who are started on therapy for clinical worsening, suicidality, or unusual changes in behavior.
Vilazodone is not approved for use in children.
Appropriately monitor all patients being treated with antidepressants for any indication and closely observe for clinical worsening, suicidality, and unusual changes in behavior, especially during the initial few months of a course of drug therapy or at times of dosage changes, either increases or decreases. Monitor patients for the emergence of serotonin syndrome or NMS-like signs and symptoms. Monitor patients closely for discontinuation symptoms when discontinuing therapy with vilazodone.
Safety and efficacy not established.
Use with caution. Antidepressants have been associated with cases of clinically significant hyponatremia in elderly patients who may be at greater risk for this adverse reaction.
Bleeding events, ranging from ecchymosis, hematoma, epistaxis, petechiae, and life-threatening hemorrhage, have been reported with other medications that interfere with serotonin reuptake. Aspirin, NSAIDs, and warfarin may add to this risk.
Activation of mania/hypomania
Has been reported. Use cautiously in patients with history of bipolar disorder, hypomania, or mania.
Screen patients with depression for risk of bipolar disorder prior to initiating therapy.
Adverse events, some serious, have been reported to occur upon discontinuation of serotonergic antidepressants. Reduce dose gradually before complete discontinuation of treatment.
May occur. Use with caution in elderly patients, volume-depleted patients, and patients taking diuretics.
Use with caution in patients with a seizure disorder.
Serotonin syndrome/NMS-like reaction
Life-threatening serotonin syndrome or NMS-like reactions may occur, particularly with coadministration of serotonergic drugs.
Disorientation, hallucinations, lethargy, restlessness, serotonin syndrome.
- Advise patients to read the Medication Guide before starting therapy and with each refill.
- Advise patient, family, and caregiver to be alert to changes in behavior, worsening of depression, and suicidal thinking, especially during initiation of therapy and when the dose is increased or decreased. Advise them to report such symptoms to their health care provider.
- Instruct patients not to take vilazodone with an MAOI or within 14 days of stopping an MAOI, and to allow 14 days after stopping vilazodone before starting an MAOI.
- Inform patients that serotonin syndrome or NMS-like reactions may occur with use, especially with concomitant use of triptans, tramadol, tryptophan supplements, other serotonergic agents, or antipsychotic drugs.
- Caution patients about using vilazodone if they have a history of seizure disorder.
- Inform patients of the potential risk of bleeding and bleeding-related events, including life-threatening hemorrhages, with the concomitant use of vilazodone and NSAIDs, aspirin, warfarin, or other drugs that affect coagulation or bleeding.
- Inform patients not to discontinue therapy with vilazodone abruptly without discussing it with their health care provider. Discontinuation effects may occur when suddenly stopping vilazodone.
- Advise patients that if they are treated with diuretics, or are otherwise volume depleted, or are elderly, they may be at greater risk of developing hyponatremia while taking vilazodone.
- Advise patients to notify their health care provider if they develop an allergic reaction, such as rash, hives, swelling, or difficulty breathing.
- Advise patients to notify their health care provider if they become pregnant or intend to become pregnant during therapy.
- Advise patients to notify their health care provider if they are breast-feeding and would like to continue taking or start vilazodone.
- Caution patients about operating hazardous machinery, including automobiles, until they are reasonably certain that vilazodone therapy does not adversely affect their ability to engage in such activities.
- Instruct patients to take daily dose with food.
Copyright © 2009 Wolters Kluwer Health.