Article: Fluvoxamine

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. weight	318.335
Pharmacokinetic data
Bioavailability	53%
Metabolism	Hepatic
Half life	15.6 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C
Legal status	Unscheduled
Routes	Oral

Fluvoxamine (sold as Luvox®, Faverin®, Fevarin® and Dumyrox®) is a selective serotonin reuptake inhibitor. It is used primarily to treat depression, anxiety and OCD.

Although its effects are similar to other SSRIs, fluvoxamine has different pharmacological effects. For this reason, fluvoxamine can be of benefit to patients who experience unusual or limiting side-effects from other antidepressants. Fluvoxamine also appears to cause fewer side-effects than other SSRIs, particularly in relation to loss of sex-drive.

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.

Effective dosage

For depression and anxiety, dosage normally starts at 50 milligrams per day, rising to 100 milligrams after a few days. It may be raised after evaluation of the effects by a doctor.

Fluvoxamine is generally only effective for OCD at 150 milligrams and above, and dosages can reach 300 milligrams or more for some patients.

Interactions

Fluvoxamine causes many drug-drug interactions due to inhibition of metabolism mediated by several cytochrome P450 oxidases. Examples of substances that have higher serum levels when administered together with fluvoxamine include caffeine, clozapine, olanzapine, tricyclic antidepressants, diazepam, alprazolam, propranolol, warfarin and methadone.

Side effects

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.

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 the 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.