Luvox (Fluvoxamine)
Fluvoxamine
Luvox®
Classification:
Psychotropic Agents
- Antidepressants
- Selective serotonin reuptake inhibitors (SSRIs)
Description: Fluvoxamine is an oral antidepressant drug of the selective serotonin reuptake inhibitors (SSRIs) class. The SSRIs are structurally distinct from the tricyclic antidepressants and monoamine oxidase inhibitors. Fluvoxamine has the shortest half-life of all the SSRIs. Sedation is more common with fluvoxamine than with some of the SSRIs (e.g., citalopram, fluoxetine, sertraline). Anorexia and weight loss is less of a concern with fluvoxamine than with fluoxetine. Fluvoxamine is currently approved for use in obsessive-compulsive disorder (OCD), and was the first SSRI approved for use in children. Fluvoxamine has also been used in the treatment of major depression, post traumatic stress disorder, obesity, bulimia nervosa, schizophrenia, panic disorder, and anxiety disorders (including generalized and social anxiety) in both adults and children >= 6 years of age. Fluvoxamine was originally approved by the FDA for treatment of obsessive-compulsive disorder in adults on December 5, 1994; approval for this same indication in children >= 8 years of age and adolescents was granted in March 1997.
On October 15, 2004 the FDA directed manufacturers of all antidepressants to include a Black Box warning, expanded warning statements, and clinical trial results detailing the increased risk of suicidality in children and adolescents. A Patient Medication Guide (MedGuide) will also accompany all prescriptions for antidepressants. The FDA is currently assessing the risk of suicidality in adults taking antidepressants and a final report is expected by mid- to late 2006.
In May 2002, Solvay Pharmaceuticals announced the withdrawal of the Luvox® product from the US market, due to a need to review data related to the chemistry, manufacturing and control (CMC) section of the NDA. The removal of the product from the market is expected to be temporary and the NDA for Luvox® is expected to be refiled. Neither Solvay nor the FDA have any concerns regarding the safety and efficacy of the drug. Generic fluvoxamine products continue to be marketed in the US.
Mechanism of Action: The most important clinical distinction of the SSRIs is their extremely high specificity for blocking the reuptake of serotonin compared to their effects on other known neurotransmitters. The precise action of SSRIs is not fully understood, but it is believed that the most important effect is the potentiation of serotonin due to highly specific blockade of serotonin reuptake at the neuronal membrane. SSRIs have less sedative, anticholinergic, and cardiovascular effects than do the tricyclic antidepressant drugs due to dramatically decreased binding to receptors of histamine, acetylcholine, and norepinephrine. Monoamine oxidase is not inhibited by any of the SSRIs. Anticholinergic activity is virtually absent.
Pharmacokinetics: Fluvoxamine is administered orally as tablets and is rapidly and almost completely absorbed from the gastrointestinal tract. The time to reach peak concentrations occurs within 2 - 8 hours after oral administration. Peak serum concentrations and time to peak are not affected by food. Serum concentrations increase linearly in a dose-dependent manner after oral administration. Steady state serum concentrations are achieved after 10 days of therapy. The excretion of fluvoxamine into breast milk is negligible.
Fluvoxamine is approximately 77% protein bound, which is less than other SSRIs. Fluvoxamine is primarily hepatically metabolized by oxidative demethylation. There are 11 inactive metabolites, which are renally excreted. Only 2% of a dose is excreted renally as unchanged drug. The elimination half-life of fluvoxamine is approximately 15 hours after administration of a single dose, but increases with multiple dosing by 30 - 50%. The elimination half-life increases to 24 hours in patients with cirrhosis. The half-life in patients with renal impairment does not change. In elderly patients, mean maximum plasma concentrations are roughly 40% higher than in young adults; the half-life of fluvoxamine is increased and clearance reduced by about 50%.
References
Institute for Clinical Systems Improvement (ICSI). Major depression in adults for mental health care. Bloomington (MN): Institute for Clinical Systems Improvement (ICSI); 2004 May. Available on the World Wide Web at http://www.guideline.gov
Care Management Institute, Kaiser Permanente. Adult primary care depression guidelines. Oakland (CA): Kaiser Permanente; 2004 Apr. Retrieved October 27, 2005. Available on the World Wide Web at http://www.guidelines.gov
American Psychiatric Association practice guideline for the treatment of patients with major depressive disorder. Am J Psychiatry 2000;157(4 Suppl):1 - 45.
Fluvoxamine Tablets(Tab 50 mg) [1 of 18 - Click here to see more photos]
[ Revised 11/10/2005 4:44:00 PM ]
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