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Pronunciation: floo-VOX-a-meen MAL-ee-ate
- Tablets 25 mg
- Tablets 50 mg
- Tablets 100 mg
- Capsules, extended-release 100 mg
- Capsules, extended-release 150 mg
CO Fluvoxamine (Canada)
Sandoz Fluvoxamine (Canada)
Inhibits neuronal reuptake of serotonin in the brain.
Absolute bioavailability is 53%. At steady state, T max is 3 to 8 h and C max is 88 to 546 ng/mL.Extended-release
Bioavailability is 84% and mean C max is 38% lower compared with immediate-release tablets. A 3-fold increase in dose results in a 5.7- and 3-fold increase in AUC and C max , respectively, indicating nonlinear pharmacokinetics.
Mean apparent Vd is about 25 L/kg. Fluvoxamine is about 80% protein bound.
Extensively metabolized by the liver. The main routes are oxidative demethylation and deamination of 9 metabolites; the major metabolite is fluvoxamine acid.
About 2% is excreted unchanged in the urine. Mean t ½ is 15.6 h at steady state.Extended-release
Mean plasma t ½ is 16.3 h.
Special PopulationsHepatic Function Impairment
30% decrease in Cl.Elderly
Cl is reduced by 50% and mean max plasma concentrations are 40% higher.Children
For the immediate-release tablets, AUC and C max were 1.5- and 2.7-fold higher, respectively, in children 6 to 11 yr of age. Female children had significantly higher AUC and C max compared with males. AUC and C max in adolescents 12 to 17 yr of age were similar to adults and there were no gender differences.Gender
The AUC and C max were increased by approximately 60% in healthy women compared with men. The t ½ was not different between men and women.
Indications and UsageImmediate-release tablets
Obsessive-compulsive disorder.Extended-release capsules
Obsessive-compulsive disorder; social anxiety disorder, also known as social phobia.
Bulimia nervosa; depression; panic disorder; nocturnal enuresis.
Coadministration of alosetron, cisapride, MAOIs, pimozide, thioridazine, or tizanidine; hypersensitivity to any component of the product.
Dosage and AdministrationObsessive-compulsive disorder
PO 100 mg once daily as a single dose at bedtime. The dose may be increased in 50 mg increments every 7 days, as tolerated, until max therapeutic benefit is achieved (max, 300 mg/day). Adjust dose to maintain the patient on the lowest effective dosage. Periodically reassess patients to determine the need for continued treatment.Immediate-release
PO 50 mg as a single dose at bedtime initially.Usual range
100 to 300 mg/day. Increase dose in 50 mg increments every 4 to 7 days, as tolerated, until max therapeutic benefit is achieved (max, 300 mg/day). Give total daily doses of more than 100 mg in 2 divided doses; if doses are unequal, give larger dose at bedtime.Maintenance
Dosage is adjusted to maintain patient on lowest effective dosage. Periodically reassess need to continue treatment.Children 8 to 17 yr of age Immediate-release
PO Start with 25 mg as a single daily dose at bedtime.Usual range
50 to 200 mg/day. Increase dose in 25 mg increments every 4 to 7 days, as tolerated, until max therapeutic benefit is achieved (max, 200 mg/day for children 8 to 11 yr of age and 300 mg/day for children 12 to 17 yr of age). Give total daily doses of more than 50 mg in 2 divided doses; if doses are unequal, give larger dose at bedtime.Social Anxiety Disorder
PO 100 mg once daily as a single dose at bedtime. The dose may be increased in 50 mg increments every 7 days, as tolerated, until max therapeutic benefit is achieved (max, 300 mg/day).
- Administer without regard to meals; administer with food if GI upset occurs.
- Extended-release capsules should be swallowed whole; do not break, crush, or chew.
Store at 68° to 77°F. Protect from high humidity. Dispense in a tightly closed, light-resistant container.Extended-release capsules
Store at 59° to 86°F. Protect from high humidity. Avoid exposure to temperatures above 86°F.
Drug InteractionsAlosetron, cisapride, MAOIs, pimozide, thioridazine, tizanidine
Coadministration with fluvoxamine is contraindicated.Aspirin, heparin, NSAIDs, warfarin
Risk of bleeding may be increased.Benzodiazepines (eg, alprazolam, diazepam, midazolam, triazolam), carbamazepine, clozapine, lidocaine, methadone, metoprolol, mexiletine, phenytoin, phosphodiesterase type 5 inhibitors (eg, sildenafil), propranolol, proton pump inhibitors, quinidine, ropivacaine, tacrine, theophylline, tricyclic antidepressants
Plasma levels of these drugs may be increased.Cyproheptadine
Pharmacologic effects of fluvoxamine may be decreased.Grapefruit
Fluvoxamine plasma levels may be elevated.Diltiazem
Bradycardia may occur.MAOIs
Similar SSRIs can cause serious (sometimes fatal) reactions. Do not give fluvoxamine in combination with MAOIs or within 14 days of discontinuation of MAOIs. After stopping fluvoxamine, wait at least 2 wk before starting MAOIs.Ramelteon
Ramelteon plasma levels may be greatly elevated, increasing the risk of adverse reactions. Do not coadminister with fluvoxamine.Serotonergic drugs (eg, 5-HT 1 agonists, linezolid, lithium, St. John's wort, tramadol), sympathomimetics, tryptophan
Risk of serotonin syndrome may be increased.Smoking
Increases metabolism of fluvoxamine.
Laboratory Test Interactions
None well documented.
Palpitations, vasodilation (3%); hypertension, hypotension, syncope, tachycardia (at least 1%); ventricular tachycardia, including torsades de pointes (postmarketing).Extended-release capsules
Palpitation (3%); hypertension, vasodilation (2%).
Headache, somnolence (22%); insomnia (21%); asthenia (14%); nervousness (12%); dizziness (11%); anxiety, tremor (5%); agitation, decreased libido, depression, hypertonia, stimulation (2%); amnesia, apathy, hyperkinesia, hypokinesia, malaise, manic reaction, psychotic reaction (at least 1%); myoclonus neuropathy, serotonin syndrome (postmarketing).Extended-release capsules
Headache, insomnia (35%); somnolence (27%); asthenia (26%); dizziness (15%); dry mouth (11%); nervousness (10%); anxiety, tremor (8%); decreased libido (6%); abnormal dreams, abnormal thinking, agitation, apathy, paresthesia (3%); hypertonia, neurosis, twitching (2%).
Sweating (7%); bullous eruption, Henoch-Schönlein purpura, Stevens-Johnson syndrome, toxic epidermal necrolysis (postmarketing).Extended-release capsules
Sweating (7%); acne (2%).
Amblyopia, taste perversion (3%); laryngismus (postmarketing).Extended-release capsules
Pharyngitis (6%); laryngitis (3%); amblyopia, epistaxis (2%).
Nausea (40%); dry mouth (14%); diarrhea (11%); constipation, dyspepsia (10%); anorexia (6%); vomiting (5%); flatulence (4%); tooth disorder (3%); dysphagia (2%); abdominal pain (1%); ileus, pancreatitis (postmarketing).Extended-release capsules
Nausea (39%); diarrhea (18%); anorexia (14%); dyspepsia (10%); constipation, vomiting (6%); abdominal pain (5%); gingivitis, taste perversion, tooth disorder (2%).
Abnormal ejaculation (8%); urinary frequency (3%); anorgasmia, impotence (2%); urinary retention (1%); acute renal failure, priapism (postmarketing).Extended-release capsules
Abnormal ejaculation (11%); anorgasmia (5%); abnormal sexual function, menorrhagia (3%); impotence, polyuria, UTI (2%).
Agranulocytosis, aplastic anemia (postmarketing).Extended-release capsules
Hepatitis (postmarketing).Extended-release capsules
Abnormal LFTs (2%).
Anaphylactic reaction, angioedema (postmarketing).
Lab TestsImmediate-release tablets
Elevated liver transaminases (at least 1%).
Edema, weight gain, weight loss (at least 1%); hyponatremia (postmarketing).Extended-release capsules
Weight loss (2%).
Upper respiratory tract infection (9%); dyspnea, yawn (2%); increased cough, sinusitis (at least 1%).Extended-release capsules
Yawning (5%); bronchitis (2%).
Flu-like syndrome (3%); chills (2%); accidental injury (at least 1%); porphyria, vasculitis (postmarketing).Extended-release capsules
Pain (10%); accidental injury (5%); chest pain (3%); viral infection (2%).
Increased risk of suicidal thinking and behavior in children, adolescents, and young adults taking antidepressants for major depressive disorders and other psychiatric disorders. Appropriately monitor patients of all ages who are started on antidepressant therapy and closely observe for clinical worsening, suicidality, or unusual changes in behavior. Advise families and caregivers of the need for close observation and communication with the prescriber.
Frequently assess patient for response to treatment. Periodically review therapy to determine if a dose change is indicated.
Category C .
Excreted in breast milk.
Safety and efficacy not established for children younger than 8 yr of age.Extended-release capsules
Safety and efficacy not established.
Because of decreased drug Cl, titrate the dosage slowly after the initial dose.
Because of decreased drug Cl, titrate the dosage slowly after the initial dose
Bleeding episodes can occur in patients treated with drugs that interfere with serotonin reuptake.
Screen for bipolar disorder prior to initiating therapy.
Cognitive and motor performance
Caution patients in operating potentially hazardous machinery (eg, cars) until they know whether the drug impairs their ability. Advise patients to avoid use of alcohol.
Caution is advised in patients with diseases or conditions that could affect hemodynamic responses or metabolism (eg, liver dysfunction).
When discontinuing or reducing dose, gradually decrease dose and monitor the patient for adverse reactions (eg, abnormal skin sensations, agitation, anxiety, confusion, dizziness, dysphoric mood, irritability, nausea, sweating). If intolerable symptoms occur, consider reinstating therapy at previous dose and attempt to decrease dose at a more gradual rate.
Hyponatremia and SIADH have been reported and appear to be reversible when fluvoxamine is discontinued.
Fluvoxamine may activate hypomania or mania. Use cautiously in patients with history of mania.
Neuroleptic malignant syndrome
Has occurred and is potentially fatal. Signs and symptoms include altered mental status, diaphoresis, hyperpyrexia, irregular BP, irregular pulse, muscle rigidity, or tachycardia.
Use with caution in patients with history of seizures. Seizures have been reported in small numbers of patients given this drug.
Life-threatening serotonin syndrome may occur, particularly with coadministration of serotonergic drugs.
Supervise depressed patients at risk during initial therapy. Prescribe the smallest quantity consistent with good patient management to reduce the risk of overdose.
Bradycardia, coma, diarrhea, ECG abnormalities, hypokalemia, hypotension, increased reflexes, nausea, respiratory difficulties, seizures, somnolence, tachycardia, tremor, vomiting.
- Advise patient to read patient information leaflet before starting therapy and with each refill.
- Advise patient that medication is usually started at a low dose and then gradually increased until max benefit is obtained.
- Advise patient taking once-daily dose to take at bedtime.
- Advise patient to take prescribed dose without regard to meals, but to take with food if stomach upset occurs.
- Inform patient that it may take 1 to 4 wk to note improvement in symptoms and to continue with prescribed therapy once improvement has been noted.
- Instruct patient to contact health care provider if symptoms do not appear to be getting better or are getting worse, or if bothersome adverse reactions (eg, changes in sexual function, diarrhea, drowsiness, headache, insomnia, nausea, nervousness, unusual sweating) occur.
- Advise patient to take frequent sips of water, suck on ice chips or sugarless hard candy, or chew sugarless gum if dry mouth occurs.
- Instruct patient to avoid alcoholic beverages and other depressants while taking this medication.
- Advise patient that drug may impair judgment, thinking, or reflexes, and to use caution while driving or performing other tasks requiring mental alertness until tolerance is determined.
- Advise patients and family to be alert for the emergence of agitation, irritability, and unusual changes in behavior as well as the emergence of suicidality, and to report such symptoms immediately to health care provider.
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