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Drug Info:

Fluvoxamine

Brand names: Luvox®

Chemical formula:



Fluvoxamine Maleate Oral capsule, extended-release

What is this medicine?

FLUVOXAMINE is an antidepressant. It is used to treat obsessive-compulsive disorder and social phobia.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• bipolar disorder
• liver disease
• seizures
• suicidal thoughts
• an unusual or allergic reaction to fluvoxamine, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Do not cut, crush or chew this medicine. You can take this medicine with or without food. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on your doctor's advice.

A special MedGuide will be given to you by the pharmacist with each prescription and refill. Be sure to read this information carefully each time.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
• alosetron
• certain diet drugs like dexfenfluramine, fenfluramine, and phentermine
• cisapride
• MAOIs like Carbex, Eldepryl, Marplan, Nardil, and Parnate
• phenothiazines like chlorpromazine, mesoridazine, prochlorperazine, thioridazine
• pimozide
• procarbazine
• ramelteon
• ranolazine
• SSRIs like citalopram, escitalopram, fluoxetine, paroxetine and sertraline
• St. John's Wort
• tizanidine
• tryptophan

This medicine may also interact with the following medications:
• aspirin and aspirin-like medicines
• carbamazepine
• clozapine
• diltiazem
• lithium
• migraine headache medicines
• medicines for anxiety or sleep problems like alprazolam or diazepam
• medicines that treat or prevent blood clots like warfarin, enoxaparin, and dalteparin
• metoprolol
• mexiletine
• NSAIDS, medicines for pain and inflammation, like ibuprofen or naproxen
• other medicines used for mental problems like depression or psychosis
• phenytoin
• propranolol
• tacrine
• theophylline

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress. Continue to take your medicine even if you do not immediately feel better. It can take several weeks before you feel the full effect of this medicine.

Patients and their families should watch out for depression or thoughts of suicide that get worse. Also watch out for sudden or severe changes in feelings such as feeling anxious, agitated, panicky, irritable, hostile, aggressive, impulsive, severely restless, overly excited and hyperactive, or not being able to sleep. If this happens, especially at the beginning of treatment or after a change in dose, call your doctor.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol can make you more drowsy and dizzy. Avoid alcoholic drinks.

Do not treat yourself for coughs, colds or allergies without asking your doctor or health care professional for advice. Some ingredients can increase possible side effects.

Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
• allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• fast talking and excited feelings or actions that are out of control
• hallucination, loss of contact with reality
• irregular, pounding heartbeat
• muscle spasms or weakness
• seizures
• suicidal thoughts or other mood changes
• unusual bleeding or bruising
• unusually tired or weak
• vomiting

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
• change in sex drive or performance
• diarrhea or constipation
• difficulty sleeping
• headache
• increased sweating
• loss of appetite
• tremors

This list may not describe all possible side effects.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Protect from humidity. Keep container tightly closed. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

 
 

A selective serotonin reuptake inhibitor (SSRI) antidepressant.

 
Wikipedia: fluvoxamine
Fluvoxamine_structure.svg
Fluvoxamine
Systematic (IUPAC) name
2-[(5-methoxy-1- [4-(trifluoromethyl) phenyl]pentylidene) amino]oxyethanamine
Identifiers
CAS number 54739-18-3
ATC code N06AB08
PubChem 5324346
DrugBank APRD00425
Chemical data
Formula C15H21F3N2O2 
Mol. mass 318.335
Pharmacokinetic data
Bioavailability 77%
Metabolism Hepatic
Half life 15.6 hours
Excretion Renal
Therapeutic considerations
Pregnancy cat.

C

Legal status

Schedule VI US

Routes Oral

Fluvoxamine (brand name as Luvox®, Faverin®, Fevarin® and Dumyrox®) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor. Though it is in the same class as other SSRI drugs, it is most often used to treat obsessive-compulsive disorder.

History

Fluvoxamine was one of 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 comprised of approximately 35,000 patients. It was launched in the US in December 1994 and in Japan in June 1999. As of the end of 1995, more than 10 million patients worldwide have been treated with fluvoxamine.[1]

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

Fluvoxamine was 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 disorders such as Obsessive-Compulsive Disorder, Obsessive-Compulsive Spectrum Disorder, Panic Disorder, Social Phobia, and Post-Traumatic Stress Disorder.[4]

Fluvoxamine is indicated for children and adolescents with OCD.[5]

Unapproved/Off-label/Investigational

Fluvoxamine is also used for the treatment of children and adolescents with social phobia, separation anxiety disorder, or generalized anxiety disorder.[6]

Fluvoxamine may help in the treatment of Irritable Bowel Syndrome.[7]

Mode of Action

Fluvoxamine is one of the few 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 has been 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 to all of these sites.[8]

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]

Pharmacokinetics

Absorption

The oral absorption of fluvoxamine is equal to or more than 94%.

Distribution

The plasma protein binding is only about 77%.

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.

Dosage & Administration

The normal dosage for depression and anxiety 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, dextromethorphan, 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 enzymez.

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: common decreased sex drive or ability, drowsiness, tiredness, diarrhea, dizziness or light-headedness, constipation, headache, nausea, nervousness, sleep problems, increased sweating, tremors, serious skin rash and other allergic problems such as difficulty breathing, fever, confusion, severe weakness, intense agitation or anxiety, restlessness, hypomania, mania, seizures.

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. What was not made public however was that Solvay concealed from the public the fact that a homicide occurred during the clinical trials involving adults. 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.

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.


References

  1. ^ (1999) "". Fluvoxamine Product Monograph. 
  2. ^ "Luvox Approved For Obsessive Compulsive Disorder in Children and Teens". http://www.pslgroup.com/dg/2261a.htm. 
  3. ^ "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. 
  4. ^ 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. 
  5. ^ (March 2005) "US-FDA Fluvoxamine Product Insert". 
  6. ^ 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. 
  7. ^ Emmanuel, et al. (1997). "Treatment of Irritable Bowel Syndrome with Fluvoxamine". Am J Psychiatry 154: 711-712. 
  8. ^ J., Hyttel (1993). "Comparative pharmacology of selective serotonin reuptake inhibitors (SSRIs)". Nordisk Journal of Psychiatric 47 (Suppl 30): 5-12. 
  9. ^ 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. 
  10. ^ 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. 
  11. ^ P., Baumann (1996). "Pharmacokinetic-pharmacodynamic relationship of the Selective serotonin reuptake inhibitors". Clinical Pharmacokinetics 31: 444-469. 
  12. ^ Gill HS, DeVane CL (1997). "Clinical Pharmacokinetics of Fluvoxamine: applications to dosage regime design". Journal of Clinical Psychiatric 58 (Suppl 5): 7-14. 
  13. ^ DeVane, CL (1998). "Translational pharmacokinetics: current issues with newer antidepressants". Depression and Anxiety 8 (Suppl 1): 64-70. 
  14. ^ 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. 

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Copyrights:

Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
Wikipedia. This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Fluvoxamine" Read more

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