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All about: Fluvoxamine Maleate

Big Image Pronouncation: (floo-VOX-a-meen MAL-ee-ate)
Class: SSRI

Trade Names:
Fluvoxamine Maleate
- Tablets 25 mg
- Tablets 50 mg
- Tablets 100 mg

Apo-Fluvoxamine (Canada)
Novo-Fluvoxamine (Canada)
Nu-Fluvoxamine (Canada)
PMS-Fluvoxamine (Canada)
ratio-Fluvoxamine (Canada)

Mechanism of Action

Pharmacology

Inhibits neuronal reuptake of serotonin in brain.

Pharmacokinetics

Absorption

Absolute bioavailability is 53%. At steady state, T max is 3 to 8 h and C max is 88 to 546 ng/mL.

Distribution

Mean apparent Vd is about 25 L/kg. Fluvoxamine is about 80% protein bound.

Metabolism

Extensively metabolized by the liver. The main routes are oxidative demethylation and deamination of 9 metabolites; the major metabolite is fluvoxamine acid.

Elimination

About 2% is excreted unchanged in the urine. Mean t ½ is 15.6 h at steady state.

Special Populations

Hepatic Function Impairment

30% decrease in Cl.

Elderly

Cl is reduced by 50% and mean max plasma concentrations are 40% higher.

Indications and Usage

Obsessive-compulsive disorder.

Contraindications

Coadministration of alosetron, cisapride, MAOIs, pimozide, thioridazine, or tizanidine; hypersensitivity to any component of the product.

Dosage and Administration

Adults

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 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

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). Give total daily doses of more than 50 mg in 2 divided doses; if doses are unequal, give larger dose at bedtime.

General Advice

  • Administer without regard to meals; administer with food if GI upset occurs.

Storage/Stability

Store at 68° to 77°F. Protect from high humidity. Dispense in a tight, light-resistant container.

Drug Interactions

Alosetron, 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, glimepiride, haloperidol, lidocaine, methadone, metoprolol, mexiletine, phenytoin, propranolol, proton pump inhibitors, quinidine, ropivacaine, tacrine, theophylline, tolbutamide, tricyclic antidepressants, warfarin

Plasma levels of these drugs may be increased.

Grapefruit

Fluvoxamine plasma levels may be elevated.

Diltiazem

Bradycardia may occur.

Lithium, tryptophan

May enhance serotonergic effects of fluvoxamine.

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.

Metoclopramide, serotonergic drugs (eg, 5-HT 1 agonists, linezolid, lithium, St. John's wort, tramadol), sympathomimetics

Risk of serotonin syndrome may be increased.

Smoking

Increases metabolism of fluvoxamine.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitations, vasodilation (3%); hypertension, hypotension, syncope, tachycardia (at least 1%); ventricular tachycardia, including torsades de pointes (postmarketing).

CNS

Headache, somnolence (22%); insomnia (21%); nervousness (12%); dizziness (11%); anxiety, tremor (5%); agitation, decreased libido, depression, hypertonia, stimulation (2%); amnesia, apathy, hyperkinesia, hypokinesia, malaise, manic reaction, myoclonus neuropathy, psychotic reaction (at least 1%).

Dermatologic

Sweating (7%); bullous eruption, Henoch-Schönlein purpura, Stevens-Johnson syndrome, toxic epidermal necrolysis (postmarketing).

EENT

Amblyopia, taste perversion (3%); laryngismus (postmarketing).

GI

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).

Genitourinary

Abnormal ejaculation (8%); urinary frequency (3%); anorgasmia, impotence (2%); urinary retention (1%); acute renal failure, priapism (postmarketing).

Hematologic-Lymphatic

Agranulocytosis, aplastic anemia (postmarketing).

Hepatic

Hepatitis (postmarketing).

Hypersensitivity

Anaphylactic reaction, angioedema (postmarketing).

Lab Tests

Elevated liver transaminases (at least 1%).

Metabolic-Nutritional

Edema, weight gain, weight loss (at least 1%); hyponatremia (postmarketing).

Respiratory

Upper respiratory tract infection (9%); dyspnea, yawn (2%); increased cough, sinusitis (at least 1%).

Miscellaneous

Asthenia (14%); flu-like syndrome (3%); chills (2%); accidental injury (at least 1%); porphyria, serotonin syndrome, vasculitis (postmarketing).

Precautions

Warnings

Antidepressants increased the risk of suicidal thinking and behavior in short-term studies in children and adolescents with major depressive disorder and other psychiatric disorders. Closely observe patients who are started on therapy for clinical worsening, suicidality, or unusual changes in behavior.


Monitor

Frequently assess patient for response to treatment. Periodically review therapy to determine if therapy needs to be continued without change or if a dose change is indicated.


Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established for children younger than 8 yr of age.

Elderly

Because of decreased drug Cl, reduce initial dose and titrate slowly.

Hepatic Function

Because of decreased drug Cl, reduce initial dose and titrate slowly.

Abnormal bleeding

Bleeding episodes can occur in patients treated with drugs that interfere with serotonin reuptake.

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.

Concomitant illness

Caution is advised in patients with diseases or conditions that could affect hemodynamic responses or metabolism (eg, liver dysfunction).

Discontinuation

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

Hyponatremia and SIADH have been reported and appear to be reversible when fluvoxamine is discontinued.

Mania/Hypomania

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.

Seizures

Use with caution in patients with history of seizures. Seizures have been reported in small numbers of patients given this drug.

Serotonin syndrome

Life-threatening serotonin syndrome may occur, particularly with coadministration of serotonergic drugs.

Suicide

Supervise depressed patients at risk during initial therapy. Prescribe the smallest quantity consistent with good patient management to reduce the risk of overdose.

Overdosage

Symptoms

Bradycardia, coma, diarrhea, ECG abnormalities, hypokalemia, hypotension, increased reflexes, nausea, respiratory difficulties, seizures, somnolence, tachycardia, tremor, vomiting.

Patient Information

  • 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.
  • Advise patient to not change the dose or stop taking unless advised by health care provider.
  • 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.

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