- Overview
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- Related Drugs
- Related Diseases
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Overview
| Generic Names: | Fluvoxamina [INN-Spanish]; Fluvoxamine maleate; Fluvoxaminum [INN-Latin]; fluvoxamine; fluvoxamine-CR |
|---|---|
| Trade Names: | Dumirox; Faverin; Fevarin; Floxyfral; Luvox; Maveral |
| PharmGKB Accession Id: | PA449690 |
Description
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.
Fluvoxamine 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.
(source:
Drug Bank)
Indication
For treatment of depression and for Obsessive Compulsive Disorder (OCD) (source: Drug Bank)
ATC Therapeutic Category
- N06AB:Selective serotonin reuptake inhibitors
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
The antidepressant, antiobsessive-compulsive, and antibulimic actions of Fluvoxamine are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. Fluvoxamine blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT<sub>1A</sub> autoreceptors. SSRIs bind with significantly less affinity to histamine, acetylcholine, and norepinephrine receptors than tricyclic antidepressant drugs. (source: Drug Bank)
Pharmacology
Fluvoxamine is one of a class of antidepressants known as selective serotonin reuptake inhibitors (SSRIs). It is used to treat the depression associated with mood disorders. It is also used on occassion in the treatment of body dysmorphic disorder and anxiety. The antidepressant, antiobsessive-compulsive, and antibulimic actions of Fluvoxamine are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin. <i>In vitro</i> studies show that Fluvoxamine is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. Fluvoxamine has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT<sub>1A</sub>, 5HT<sub>1B</sub>, 5HT<sub>2</sub>), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs. The chronic administration of Fluvoxamine was found to downregulate brain norepinephrine receptors, as has been observed with other drugs effective in the treatment of major depressive disorder. Fluvoxamine does not inhibit monoamine oxidase. (source: Drug Bank)
Food Interactions
Avoid alcohol.
Avoid high doses of caffeine.
Grapefruit and grapefruit juice should be avoided throughout treatment as grapefruit can significantly increase serum levels of this product.
Take without regard to meals.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Protein Binding
~77-80% (plasma protein) (source: Drug Bank)
Absorption
Well absorbed, bioavailability of fluvoxamine maleate is 53%. (source: Drug Bank)
Toxicity
Side effects include anorexia, constipation, dry mouth, headache, nausea, nervousness, skin rash, sleep problems, somnolence, liver toxicity, mania, increase urination, seizures, sweating increase, tremors, or Tourette's syndrome. (source: Drug Bank)
Isomeric SMILES Code:
COCCCC/C(=N\OCCN)/C1=CC=C(C=C1)C(F)(F)F (source: Drug Bank)
In-Depth Annotations (
)
-
rs59421388
at chr22:40853554
in
CYP2D6
This variant is part of the reduced functioning haplotype CYP2D6*29, which is found at an estimated allele frequency of 20% in African Tanzanians.- Variant Name:
- CYP2D6: 3183G>A; 3271G>A
- Related Drugs:
- citalopram, codeine, desipramine, fluoxetine, fluvoxamine, gefitinib, haloperidol, imipramine, morphine, tramadol
- Related Diseases:
- Cystic Fibrosis, Depression, Hypertension, Neoplasms, Pain, Parkinson Disease, Schizophrenia
- Evidence:
-
http://www.pharmgkb.org/.../variant.jsp
-
rs61736512
at chr22:40855078
in
CYP2D6
This variant is part of the reduced functioning haplotype CYP2D6*29, which is found at an estimated allele frequency of 20% in African Tanzanians.- Variant Name:
- CYP2D6: 1659G>A; 1747G>A
- Related Drugs:
- citalopram, codeine, desipramine, fluoxetine, fluvoxamine, gefitinib, haloperidol, imipramine, morphine, tramadol
- Related Diseases:
- Cystic Fibrosis, Depression, Hypertension, Neoplasms, Pain, Parkinson Disease, Schizophrenia
- Evidence:
-
http://www.pharmgkb.org/.../variant.jsp
Curated Annotations (
)
-
rs1364043
at chr5:63286607
A study, investigating the response of SSRI in 137 Japanese major depression subjects, observed a significant association of better response to antidepressant in rs10042486 (P < 0.0001), rs6295 (P < 0.0001) and rs1364043 (P = 0.018) genotype carriers (minor allele homozygotes), independently from clinical variables. The rs6295 variant has been found to affect the expression and function of HTR1A. rs6295 is in strong linkage disequilibrium with other polymorphisms of HTR1A.- Related Drugs:
- fluvoxamine, paroxetine
- Related Diseases:
- Depression
- Evidence:
-
PMID:18484082
-
rs6295
at chr5:63294321
in
HTR1A
The variant in the HTR1A gene has been found to affect the expression and function of HTR1A. rs6295 is in strong linkage disequilibrium with other polymorphisms of HTR1A. A study, investigating the response of SSRI in 137 Japanese major depression subjects, observed a significant association of better response to antidepressant in rs10042486 (P < 0.0001), rs6295 (P < 0.0001) and rs1364043 (P = 0.018) genotype carriers (minor allele homozygotes), independently from clinical variables.- Related Drugs:
- fluvoxamine, paroxetine
- Related Diseases:
- Depression
- Evidence:
-
PMID:18484082
-
rs10042486
at chr5:63297085
in
HTR1A
A study, investigating the response of SSRI in 137 Japanese major depression subjects, observed a significant association of better response to antidepressant in rs10042486 (P < 0.0001), rs6295 (P < 0.0001) and rs1364043 (P = 0.018) genotype carriers (minor allele homozygotes), independently from clinical variables. The rs6295 variant has been found to affect the expression and function of HTR1A. rs6295 is in strong linkage disequilibrium with other polymorphisms of HTR1A.- Related Drugs:
- fluvoxamine, paroxetine
- Related Diseases:
- Depression
- Evidence:
-
PMID:18484082
-
rs57098334
at chr17:25572722
in
SLC6A4
In a study in a unipolar depressive population (n=166), the frequency of individuals carrying two copies of the 12-copy repeat was significantly associated with lack of remission and lack of response, suggesting that individuals homozygous for the 12-copy repeat are more likely to have a poor therapeutic outcome following antidepressant treatment. Another study found the 12-copy repeat to be associated with paroxetine and fluoxetine response in 120 depressed Koreans, although a Japanese study found no association with this polymorphism and fluvoxamine response. The 12-copy allele of the SLC6A4 intron 2 polymorphism has been associated with increased gene transcription.- Variant Name:
- SLC6A4: (GGGTGGGCT)9/10/12
- Related Drugs:
- fluoxetine, fluvoxamine, paroxetine
- Related Diseases:
- Depression
- Evidence:
-
PMID:10481059
PMID:10611371
PMID:10683861
PMID:12374640
PMID:18253134
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
CREB1 |
|
Publications |
|
CYP1A2 |
|
Publications |
|
CYP2C19 |
|
Publications |
|
|
CYP2C9 |
|
Publications |
|
|
CYP2D6 |
|
Publications, Variants |
|
|
HTR1A |
|
Publications, Variants |
|
|
HTR2A |
|
Publications |
|
|
HTR3A |
|
Publications |
|
|
HTR3B |
|
Publications |
|
|
KCNH2 |
|
Publications |
|
|
MAOA |
|
Publications |
|
|
SLC6A4 |
|
Publications, Variants |
|
|
TPH1 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
|
|
alprazolam |
|
Publications |
|
|
bupropion |
|
Publications |
|
|
tamoxifen |
|
Publications |
|
|
warfarin |
|
Publications |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| acenocoumarol |
|
Fluvoxamine increases the effect of the anticoagulant (source: Drug Bank) |
| almotriptan |
|
Increased risk of CNS adverse effects (source: Drug Bank) |
| amitriptyline |
|
Fluvoxamine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| amoxapine |
|
Fluvoxamine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| amphetamine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| astemizole |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| benzphetamine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| carbamazepine |
|
Fluvoxamine increases the effect of carbamazepine (source: Drug Bank) |
| clomipramine |
|
Fluvoxamine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| clozapine |
|
The antidepressant increases the effect of clozapine (source: Drug Bank) |
| desipramine |
|
Fluvoxamine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| dextroamphetamine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| dicumarol |
|
Fluvoxamine increases the effect of the anticoagulant (source: Drug Bank) |
| doxepin |
|
Fluvoxamine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| duloxetine |
|
Fluvoxamine increases the effect and toxicity of duloxetine (source: Drug Bank) |
| eletriptan |
|
Increased risk of CNS adverse effects (source: Drug Bank) |
| fenfluramine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| imipramine |
|
Fluvoxamine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| isocarboxazid |
|
Possible severe adverse reaction with this combination (source: Drug Bank) |
| linezolid |
|
Combination associated with possible serotoninergic syndrome (source: Drug Bank) |
| lithium |
|
The SSRI increases serum levels of lithium (source: Drug Bank) |
| mazindol |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| mephenytoin |
|
Increases the effect of hydantoin (source: Drug Bank) |
| mesoridazine |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| methadone |
|
Fluvoxamine increases the effect and toxicity of methadone (source: Drug Bank) |
| methamphetamine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| mexiletine |
|
Increases the effect and toxicity of mexiletine (source: Drug Bank) |
| mirtazapine |
|
Increases the effect adn toxicity of mirtazapine (source: Drug Bank) |
| moclobemide |
|
Increased incidence of adverse effects with this association (source: Drug Bank) |
| naratriptan |
|
Increased risk of CNS adverse effects (source: Drug Bank) |
| nortriptyline |
|
Fluvoxamine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| olanzapine |
|
Fluvoxamine increases the effect and toxicity of olanzapine (source: Drug Bank) |
| oxycodone |
|
Increased risk of serotonin syndrome (source: Drug Bank) |
| phendimetrazine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| phenelzine |
|
Possible severe adverse reaction with this combination (source: Drug Bank) |
| phenytoin |
|
Increases the effect of hydantoin (source: Drug Bank) |
| protriptyline |
|
Fluvoxamine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| rizatriptan |
|
Increased risk of CNS adverse effects (source: Drug Bank) |
| ropivacaine |
|
Increases the effect and toxicity of ropivacaine (source: Drug Bank) |
| selegiline |
|
Possible severe adverse reaction with this combination (source: Drug Bank) |
| sibutramine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| sumatriptan |
|
Increased risk of CNS adverse effects (source: Drug Bank) |
| tacrine |
|
Fluvoxamine increases the effect of tacrine (source: Drug Bank) |
| terfenadine |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| theophylline |
|
Increases the effect and toxicity of theophylline (source: Drug Bank) |
| thioridazine |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| tizanidine |
|
Fluvoxamine increases the effect/toxicity of tizanidine (source: Drug Bank) |
| tramadol |
|
Increased risk of serotonin syndrome (source: Drug Bank) |
| tranylcypromine |
|
Possible severe adverse reaction with this combination (source: Drug Bank) |
| trimipramine |
|
Fluvoxamine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| warfarin |
|
Fluvoxamine increases the effect of the anticoagulant (source: Drug Bank) |
| zolmitriptan |
|
Increased risk of CNS adverse effects (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Breast Neoplasms |
|
Publications |
|
|
Death |
|
Publications |
|
|
Depression |
|
Publications, Variants |
|
|
Depressive Disorder |
|
Publications |
|
|
Obsessive-Compulsive Disorder |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
Common Searches
Search PubMed
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Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.