NationMaster - Encyclopedia: Fluvoxamine

Fluvoxamine (brand name as Luvox®, Faverin®, Fevarin® and Dumyrox®) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... Selective serotonin reuptake inhibitors (SSRIs) are a class of antidepressants used in the treatment of depression, anxiety disorders and some personality disorders. ...

History

Fluvoxamine was the first of the SSRI antidepressants to be launched (1984 - Switzerland) and was developed by Solvay Pharmaceuticals. It has been in use in clinical practice since 1983 and has a clinical trial database comprising approximately 35,000 patients. It was launched in the US in December 1994 and in Japan in June 1999. Up to the end of 1995, more than 10 million patients world-wide has been treated with fluvoxamine.^[1] Solvay Pharmaceuticals is one of the top 40 pharmaceutical companies in the world. ...

Fluvoxamine was the first SSRI to be registered for the treatment of OCD in children by FDA in 1997. ^[2]

Fluvoxamine is the first drug approved for the treatment of social anxiety disorder in Japan in 2005. ^[3]

Indication

Approved

Fluvoxamine is widely prescribed to treat depression, and anxiety disorder such as Obsessive-Compulsive Disorder, Obsessive-Compulsive Spectrum Disorder, Panic Disorder, Social Phobia and Post-Traumatic Stress Disorder.^[4] Look up depression in Wiktionary, the free dictionary. ... Anxiety disorder is a blanket term covering several different forms of abnormal, pathological anxiety, fears, phobias and nervous conditions that may come on suddenly or gradually over a period of several years, and may impair or prevent the pursuing of normal daily routines. ... Obsessive-Compulsive Spectrum Disorder comprise a unique category of related disorders, many of which overlap with OCD in symptomatic profile, demographics, family history, neurobiology, comorbidity, clinical course and response to various pharmacotherapies. ... Panic Disorder (also known as cardiac neurosis or neurosis cordis) is a mental condition that causes the sufferer to experience sporadic panic attacks. ... Social anxiety, sometimes known as social phobia or social anxiety disorder (SAD), is a common form of anxiety disorder that causes sufferers to experience intense anxiety in some or all of the social interactions and public events of everyday life. ... It has been suggested that Combat stress reaction be merged into this article or section. ...

Unapproved/Off-label/Investigational

Fluvoxamine is also can be given for the treatment of children and adolescents with social phobia, separation anxiety disorder, or generalized anxiety disorder. ^[6] Separation anxiety disorder (or simply separation anxiety) is a psychological condition in which an individual has excessive anxiety regarding separation from home or from people to whom the individual has a strong emotional attachment. ... General anxiety disorder or generalized anxiety disorder (GAD) is an anxiety disorder that is characterized by uncontrollable worry about everyday things. ...

Mode of Action

Fluvoxamine is the only one of the SSRI class of drugs to have a monocyclic structure.

Although all SSRIs inhibit the reuptake of serotonin, Fluvoxamine has different pharmacological and side effects profiles from other drugs in its class. Fluvoxamine shown to be selective for serotonin reuptake and has little effect on dopamine and noradrenaline uptake systems compared to other SSRI. For this reason, Fluvoxamine can be of benefit to patients who experience unusual or limiting side-effects from other antidepressants. It appears to cause fewer side effects than other SSRIs. In addition, these differences also are a result of the lack of direct effects at other neurotransmitter receptors compared to other SSRIs. Affinity for these receptors, for example cholinergic muscarinic (dry mouth, constipation) sites, histaminergic (sedation) sites, alpha (postural hypertension) sites and dopamine (extrapyramidal)sites, leads to many side effects. Compared to other SSRIs, Fluvoxamine has a very low affinity for all these sites.^[8] An adverse drug reaction (abbreviated ADR) is a term to describe the unwanted, negative consequences sometimes associated with the use of medications. ... Chemical structure of D-Aspartic Acid, a common Amino Acid neurotransmitter. ... Receptor may refer to: In telecommunication, a receiver. ... A synapse is cholinergic if it uses acetylcholine as its neurotransmitter. ... Muscarinic receptors are those membrane bound acetylcholine receptors that are more sensitive to muscarine than to nicotine. ... Alpha may refer to: The Greek letter alpha Alpha (letter), a letter in the Greek alphabet. ... This article or section is in need of attention from an expert on the subject. ... In human anatomy, the extrapyramidal system is a neural network located in the brain that is part of the motor system involved in the coordination of movement. ...

Among the SSRIs, Fluvoxamine has the highest affinity for sigma receptor subtype 1 (σ₁receptors)^[9] , suggesting that it may have particular benefits in the treatment of depressed patients who show features of anxiety/stress and for whom memory impairment is particularly undesirable (such as in depressed elderly patients, and also in treating psychotic depression).^[10] Opioid receptors are a group of G-protein coupled receptors with opioids as ligands. ...

Pharmacokinetics

Absorption

Distribution

Metabolism

Fluvoxamine is extensively metabolised in the liver. It has no active metabolites.

Elimination

Fluvoxamine has the shortest half-life of all the SSRIs. Its mean serum half-life is 15 hours after a single dose, and 17 to 22 hours after repeated doses. Half-Life For a quantity subject to exponential decay, the half-life is the time required for the quantity to fall to half of its initial value. ... Look up Serum in Wiktionary, the free dictionary. ...

Dosage & Administration

The normal dosage for depression and anxiety is to starts at 50mg per day, rising to 100mg after a few days. It may be raised after evaluation of the effects by a doctor.

Fluvoxamine has shown generally effective for OCD at 150mg and above, and dosages can reach 300mg or more for some patients.

Drug Interactions

Fluvoxamine has a low potential for drug interactions. In terms of inhibition of enzyme Cytochrome P450 CYP2D6, Fluvoxamine is the cleanest among all the SSRI because importantly it does not inhibit CYP2D6. ^[11] ^[12] ^[13] Drugs that interacts with CYP2D6 will have more interactions with TCAs, antiarrythmics, B-blockers, phenytoin, opiates (eg. codeine, dextromethophon, morphine, tramadol) and neuroleptics (eg. haloperidol, risperidon). It does, however, inhibit Cytochrome P450 enzyme CYP1A2, which metabolises theophylline, caffeine, phenacetin, tacrine, clozapine, and olanzapine, . These substances can cause increased serum levels when administered together with fluvoxamine. It has only modest effects on CYP2C and CYP3A3/4. Therefore, different SSRI have different level of drug interactions depending on the inhibition of Cytochrome P450 enzyme. Drug interaction is a situation in which two or more separate drugs have been absorbed into the body and their effects are affected by each other, i. ... Cytochrome P450 Oxidase (CYP2E1) Cytochrome P450 oxidase (commonly abbreviated CYP) is a generic term for a large number of related, but distinct, oxidative enzymes (EC 1. ... Cytochrome P450 2D6 (abbreviated CYP2D6, EC 1. ... This page is a candidate for speedy deletion. ... Theophylline is a methylxanthine drug used in therapy for respiratory diseases such as COPD or asthma under a variety of brand names. ... Caffeine is a xanthine alkaloid compound that acts as a stimulant in humans. ... Phenacetin, introduced in 1887, is used principally as an analgesic. ... Chemical structure of tacrine Tacrine is a parasympathomimetic and a centrally acting cholinesterase inhibitor (anticholinesterase). ... Clozapine (sold as ClozarilÂ®, LeponexÂ®, FazacloÂ®) was the first of the atypical antipsychotics to be developed. ... Olanzapine (oh-LAN-za-peen, sold as ZyprexaÂ®, ZydisÂ®, or in combination with fluoxetine, as SymbyaxÂ®) was the third atypical antipsychotic to gain approval by the Food and Drug Administration (FDA) and has become one of the most commonly used atypical antipsychotics. ...

In addition, Fluvoxamine has relatively short plasma half life, roughly 15 hours, and has no active metabolites. With these properties, Fluvoxamine has less of a chance of drug accumulations and interactions.

The plasma protein binding of Fluvoxamine is only about 77%. Drugs with low protein binding are less likely to displace other protein bound drugs, and therefore have a lower potential to cause drug interactions.

Side effects

Fluvoxamine has the least incidence of side effects on sexual dysfunctions, or loss of sex drive of all the SSRIs.^[14]

Side effects of fluvoxamine can include: anorexia, constipation, dry mouth, headache, nausea, nervousness, skin rash, sleep problems, somnolence, liver toxicity, mania, increased urination, seizures, increased sweating, tremors, or Tourette's syndrome. Anorexia (deriving from the Greek Î±(Î½)- (a(n)-, a prefix that denotes absence) + ÏŒÏÎµÎ¾Î· (orexe) = appetite) is the decreased sensation of appetite. ... Constipation or irregularity, is a condition of the digestive system where a person (or animal) experiences hard feces that are difficult to eliminate; it may be extremely painful, and in severe cases (fecal impaction) lead to symptoms of bowel obstruction. ... Xerostomia is the medical term for a dry mouth due to a lack of saliva. ... A headache (medically known as cephalalgia, sometimes spelled as cephalgia) is a condition of pain in the head; sometimes neck or upper back pain may also be interpreted as a headache. ... For other uses, see Nausea (disambiguation). ... Anxiety is a complex combination of the feeling of fear, apprehension and worry often accompanied by physical sensations such as palpitations, chest pain and/or shortness of breath. ... For the manga by Tsukasa Hôjô, see Rash. ... Sleep is the state of natural rest observed in most mammals, birds, fish, as well as invertebrates such as the fruitfly Drosophila. ... Somnolence (or drowsiness, or hypersomnia) is a state of near-sleep, a strong desire for sleep, or sleeping unusually long periods. ... Hepatotoxicity (from hepatic toxicity) is chemical-driven liver damage. ... Mania is a medical condition characterized by severely elevated mood. ... Urination, also called micturition, is the process of disposing urine from the urinary bladder through the urethra to the outside of the body. ... This article is about the medical condition. ... Sweating (also called perspiration or sometimes transpiration) is the loss of a watery fluid, consisting mainly of sodium chloride (commonly known as salt) and urea in solution, that is secreted by the sweat glands in the skin of mammals. ... Fred Ward as Earl Bassett in the 1990 film Tremors. ... Tourette syndrome — also called Tourettes syndrome, Tourette Spectrum (TS), Tourettes disorder, or Gilles de la Tourette syndrome (after its discoverer, Georges Gilles de la Tourette) — is a neurological or neurochemical disorder characterized by tics — involuntary, rapid, sudden movements or vocalizations that occur repeatedly in the...

Historical relevance

In 1999, fluvoxamine came under great public scrutiny after it was discovered that Eric Harris, one of the two teenaged shooters involved in the Columbine High School massacre, had been taking the drug as treatment for depression. Many immediately pointed fingers at fluvoxamine and its manufacturer Solvay Pharmaceuticals (which sells fluvoxamine under the widely known brandname Luvox), since Solvay's own clinical trials indicated the drug had the propensity to induce mania in 4% of the youth who took it. Solvay, while acknowledging the risks inherent in taking an SSRI medication like fluvoxamine, downplayed any role the drug may have had in the killings. The American Psychiatric Association (A.P.A.) took a similar stance; Rodrigo Munoz, M.D., President of the A.P.A., said: "Despite a decade of research, there is little valid evidence to prove a causal relationship between the use of anti-depressant medications and destructive behavior. On the other hand, there is ample evidence that undiagnosed and untreated mental illness exacts a heavy toll on those who suffer from these disorders as well as those around them." It was also pointed out by many that Luvox was often safer than the other SSRI medications available--for example, fluoxetine (Prozac) caused mania in 6% of youth tested on the drug (versus fluvoxamine's 4%). Nonetheless, the reputation of Luvox was irreparably damaged. Sales fell, and Solvay withdrew the medication from the U.S. market in 2002; the company maintains, however, that this move had nothing to do with the safety profile of fluvoxamine, which they still sell in many countries around the world. In the United States, fluvoxamine can only be purchased generically. 1999 (MCMXCIX) was a common year starting on Friday, and was designated the International Year of Older Persons by the United Nations. ... Yearbook photographs of the two perpetrators. ... Staff and students evacuate Columbine High School shortly after the shooting. ... The American Psychiatric Association is a professional organization of psychiatrists whose members are American and international physicians who are trained in psychiatry. ...

The FDA currently issues the following warning with Luvox: Taking antidepressants may increase suicidal thoughts and actions in about 1 out of 50 people 18 years or younger.[1] The UK and Health Canada have taken similar actions.

Appearance in popular culture

The drug was given visibility in the American television series The Sopranos produced by HBO, in the second season, episode 10. Dr. Jennifer Melfi, the psychiatrist treating the character named Tony Soprano, is prescribed Luvox by her own psychiatrist, to treat a strong inclination toward alcohol.

References

^ (1999) "". Fluvoxamine Product Monograph.
^ "Luvox Approved For Obsessive Compulsive Disorder in Children and Teens". http://www.pslgroup.com/dg/2261a.htm.
^ "Solvay’s Fluvoxamine maleate is first drug approved for the treatment of social anxiety disorder in Japan". http://www.solvaypress.com/pressreleases/0,,33713-2-83,00.htm.
^ Karen J. McClellan, David P. Figgit (Drugs Oct 2000). "Fluvoxamine An Updated Review of its Use in the Management of Adults with Anxiety Disorders". Adis Drug Evaluation 60 (4): 925-954.
^ (March 2005) "US-FDA Fluvoxamine Product Insert".
^ John T Walker MD, Michael J. Labelarte MD et.al. (April 26, 2001). "Fluvoxamine for the treatment of anxiety disorders in children and adolescents". The New England Journal of Medicine 344: 1279-1285.
^ Emmanuel, et al. (1997). "Treatment of Irritable Bowel Syndrome with Fluvoxamine". Am J Psychiatry 154: 711-712.
^ J., Hyttel (1993). "Comparative pharmacology of selective serotonin reuptake inhibitors (SSRIs)". Nordisk Journal of Psychiatric 47 (Suppl 30): 5-12.
^ Hashimoto K et al., Narita N (1996). "Interactions of selective reuptake inhibitors with subtypes of sigma receptor in rat brain". Eur J Pharmacol 307: 117-9.
^ C.Sandner, Carrasco JL (December 2005). "Clinical effects of pharmacological variations in selective serotonin reuptake inhibitors: an overview". International Journal of Clinical Practice 59 (12): 1428-1434.
^ P., Baumann (1996). "Pharmacokinetic-pharmacodynamic relationship of the Selective serotonin reuptake inhibitors". Clinical Pharmacokinetics 31: 444-469.
^ Gill HS, DeVane CL (1997). "Clinical Pharmacokinetics of Fluvoxamine: applications to dosage regime design". Journal of Clinical Psychiatric 58 (Suppl 5): 7-14.
^ DeVane, CL (1998). "Translational pharmacokinetics: current issues with newer antidepressants". Depression and Anxiety 8 (Suppl 1): 64-70.
^ Hengeveld VW et al., Waldinger MD (1998). "Effect of SSRI antidepressants on ejaculation: a double blind, randomised, placebo-controlled study with fluoxetine, fluvoxamine, paroxetine and sertraline". Journal of Clinical Psychopharmacology 18: 274-281.

External links

Category: Selective serotonin reuptake inhibitors An antidepressant is a medication designed to treat or alleviate the symptoms of clinical depression. ... A section of the Anatomical Therapeutic Chemical Classification System. ... Monoamine oxidase inhibitors (MAOIs) are a class of antidepressant drugs prescribed for the treatment of depression. ... Harmala, also known at various times as Telepathine and Banisterine, is a blanket term for a group of naturally occurring beta-carbolines including harmine, harmaline, and others. ... Iproclozide is a monoamine oxidase inhibitor antidepressant. ... Iproniazid is a monamine oxidase inhibitor (MAOI) that was developed as the first anti-depressant (Also first psychiatric drug). ... Isocarboxazid is a nonselective hydrazine-derived monoamine oxidase inhibitor used in treatment resistant depression. ... 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Reboxetine has two chiral centers, but it only exists as two enantiomers, (R,R)-(-)- and (S,S)-(+)-reboxetine. ... Viloxazine is a bicyclic antidepressants[2] that inhibits the reuptake of serotonin, and to a lesser extent, dopamine and norepinephrine. ... Serotonin-norepinephrine reuptake inhibitors (SNRIs) are a class of antidepressant used in the treatment of clinical depression and other affective disorders. ... Duloxetine hydrochloride (brand names: Cymbalta/Yentreve and in parts of Europe known as Xeristar) is a medically used drug that primarily targets major depressive disorders (MDD), pain related to diabetic peripheral neuropathy and stress urinary incontinence (SUI). ... Milnacipran is an antidepressant of the serotonin-norepinephrine reuptake inhibitor class. ... Venlafaxine hydrochloride is a prescription antidepressant first introduced by Wyeth in 1993. ... 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Trimipramine is an tricyclic antidepressant with sedative and anxiolytic properties. ... The structure of the tetracyclic antidepressant mirtazapine A tetracyclic antidepressant is an antidepressant drug from the tetracyclic drug group. ... To meet Wikipedias quality standards, this article may require cleanup. ... Mianserin is a tetracyclic antidepressant that has an antihistaminic and hypnosedative, but almost no anticholinergic effect. ... // Introduction Serzone (nefazodone) Serzone ( Nefazodone HCl ) is an antidepressant drug formerly marketed by Bristol-Myers Squibb. ... Trazodone (DesyrelÂ®, TritticoÂ®, ThombranÂ®, TrialodineÂ®) is a psychoactive compound with sedative, anxiolytic, and antidepressant properties. ... Noradrenergic and specific serotonergic antidepressants (abbreviated: NaSSAs) are a relatively new class of antidepressants. ... To meet Wikipedias quality standards, this article or section may require cleanup. ...

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