- Overview
- Properties
- Genetics
- Related Genes
- Pathways
- Related Drugs
- Related Diseases
- Datasets
- Downloads/LinkOuts
Overview
| Generic Names: | Fluoxetina [INN-Spanish]; Fluoxetina [Spanish]; Fluoxetine Hcl; Fluoxetine Hydrochloride; Fluoxetinum [INN-Latin] |
|---|---|
| Trade Names: | Adofen; Animex-On; Deprex; Eufor; Fluctin; Fluoxeren; Fluval; Fontex; Foxetin; Portal; Prozac; Prozac Weekly; Pulvules; Reneuron; Sarafem |
| PharmGKB Accession Id: | PA449673 |
Description
The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants. PubChem (source: Drug Bank)
Indication
For the treatment of depression, obsessive compulsive disorder, and bulimia nervosa. (source: Drug Bank)
ATC Therapeutic Category
- N06AB:Selective serotonin reuptake inhibitors
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Metabolized to norfluoxetine, fluoxetine is a selective serotonin-reuptake inhibitor (SSRI), it 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
Fluoxetine, an antidepressant agent belonging to the selective serotonin reuptake inhibitors (SSRIs), is used to treat depression, bulimia nervosa, premenstrual dysphoric disorder, panic disorder and post-traumatic stress. According to the amines hypothesis, a functional decrease in the activity of amines, such as serotonin and norepinephrine, would result in depression; a functional increase of the activity of these amines would result in mood elevation. Fluoxetine's effects are thought to be associated with the inhibition of 5HT receptor, which leads to an increase of serotonin level. (source: Drug Bank)
Food Interactions
Avoid alcohol.
Take with food to reduce irritation and nausea.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic. (source: Drug Bank)
Protein Binding
94.5% (source: Drug Bank)
Absorption
72% (source: Drug Bank)
Toxicity
Symptoms of overdose include agitation, restlessness, hypomania, and other signs of CNS excitation. LD<sub>50</sub>=284mg/kg (orally in mice). (source: Drug Bank)
Isomeric SMILES Code:
CNCCC(c1ccccc1)Oc2ccc(cc2)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 (
)
-
rs2296840
at chr1:149638671
in
PSMB4
Based on an study on 284 Mexican Americans, this variant in the 5' UTR of PSMB4 is significantly associated with major depressive disorder (MDD). The results implicate that the specific UTR variation increases the risks for a T-cell dysfunction in MDD in the studied population.- Related Drugs:
- desipramine, fluoxetine
- Related Diseases:
- Depression
- Evidence:
-
PMID:18504423
-
rs6808874
at chr3:121040541
in
GSK3B
This variant is associated with antidepressant treatment response in Chinese major depressive disorder. In a four-locus haplotype analysis (rs334558; rs13321783; rs2319398; rs6808874), the GSK3B TAGT carriers showed a poorer response to antidepressants than carriers with other haplotype groups.- Variant Name:
- GSK3B: IVS11+4251 T>A
- Related Drugs:
- citalopram, fluoxetine
- Related Diseases:
- Depression, Depressive Disorder, Major
- Evidence:
-
PMID:18195730
-
rs2319398
at chr3:121095632
in
GSK3B
This variant is associated with antidepressant treatment response in Chinese major depressive disorder. In a four-locus haplotype analysis (rs334558; rs13321783; rs2319398; rs6808874), the GSK3B TAGT carriers showed a poorer response to antidepressants than carriers with other haplotype groups.- Variant Name:
- GSK3B: IVS7+9227 A>G
- Related Drugs:
- citalopram, fluoxetine
- Related Diseases:
- Depression, Depressive Disorder, Major
- Evidence:
-
PMID:18195730
-
rs13321783
at chr3:121098065
in
GSK3B
This variant is associated with antidepressant treatment response in Chinese major depressive disorder. In a four-locus haplotype analysis (rs334558; rs13321783; rs2319398; rs6808874), the GSK3B TAGT carriers showed a poorer response to antidepressants than carriers with other haplotype groups.- Variant Name:
- GSK3B: IVS7+11660 G>T
- Related Drugs:
- citalopram, fluoxetine
- Related Diseases:
- Depression, Depressive Disorder, Major
- Evidence:
-
PMID:18195730
-
rs334558
at chr3:121295972
in
GSK3B
This variant is in the promoter region of GSK3B. T allele is associated with greater transcription activity compared with the A allele. This variant is associated with antidepressant treatment response in Chinese major depressive disorder. In a four-locus haplotype analysis (rs334558; rs13321783; rs2319398; rs6808874), the GSK3B TAGT carriers showed a poorer response to antidepressants than carriers with other haplotype groups.- Variant Name:
- GSK3B: -50 T>C
- Related Drugs:
- citalopram, fluoxetine
- Related Diseases:
- Depression, Depressive Disorder, Major, Parkinsonian Disorders
- Evidence:
-
PMID:16315267
PMID:18195729
-
rs3800373
at chr6:35650454
in
FKBP5
This variant is associated with higher chance of response to anti-depressant drugs.- Related Drugs:
- desipramine, fluoxetine, mirtazapine, venlafaxine
- Related Diseases:
- Depression
- Evidence:
-
PMID:15565110
PMID:18349090
PMID:18597649
-
rs1360780
at chr6:35715549
in
FKBP5
This variant is associated with higher chance of response to anti-depressant drugs.- Related Drugs:
- desipramine, fluoxetine, mirtazapine, venlafaxine
- Related Diseases:
- Depression
- Evidence:
-
PMID:15565111
PMID:18349090
PMID:18597649
-
rs2227631
at chr7:100556258
in
SERPINE1
This variant was shown to be assoicated with antidepressant treatment response in a study consisting of 188 Chinese MDD patients and 346 controls.The G allele was less frequent in responders than nonresponders- Related Drugs:
- citalopram, fluoxetine
- Related Diseases:
- Depression, Depressive Disorder, Major
- Evidence:
-
PMID:18794724
-
rs1799889
at chr7:100556430
in
SERPINE1
This variant was shown to be assoicated with antidepressant treatment response in a study consisting of 188 Chinese MDD patients and 346 controls.The G allele was less frequent in responders than nonresponders- Related Drugs:
- citalopram, fluoxetine
- Related Diseases:
- Depression, Depressive Disorder, Major
- Evidence:
-
PMID:18794724
-
rs6314
at chr13:46307035
in
HTR2A
In a study in a unipolar depressive population (n=166) this variant showed an association with remission and response following paroxetine therapy. HTR2A C1354T heterozygotes were significantly associated with improved response to paroxetine therapy. The SNP was also studied as a modifier of antidepressant response in a study in depressed patients (n=173) given a variety of antidepressant treatments with no association found, however another report found the HTR2A T1354 allele to be associated with response to fluoxetine.- Variant Name:
- HTR2A: C1354T
- Related Drugs:
- fluoxetine, paroxetine
- Related Diseases:
- Depression
- Evidence:
-
PMID:11311507
PMID:15052272
PMID:18253134
-
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
-
rs17244587
at chr17:43178034
in
TBX21
Based on an study on 284 Mexican Americans, this variant in the 3' UTR of TBX21 is significantly associated with major depressive disorder (MDD). The results implicate that the specific UTR variation increases the risks for a T-cell dysfunction in MDD in the studied population.- Related Drugs:
- desipramine, fluoxetine
- Related Diseases:
- Depression
- Evidence:
-
PMID:18504423
The following genes are in curated knowledge about this drug.
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
PharmGKB Curated Pathways
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
|
alprazolam |
|
Publications |
|
|
antipsychotics |
|
Publications |
|
|
benzodiazepine derivatives |
|
Publications |
|
|
bupropion |
|
Publications |
|
|
diazepam |
|
Publications |
|
|
galantamine |
|
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 |
|
The SSRI increases the effect of anticoagulant (source: Drug Bank) |
| almotriptan |
|
Increased risk of CNS adverse effects (source: Drug Bank) |
| amitriptyline |
|
Fluoxetine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| amoxapine |
|
Fluoxetine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| amphetamine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| anisindione |
|
The SSRI increases the effect of anticoagulant (source: Drug Bank) |
| astemizole |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| atomoxetine |
|
The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine (source: Drug Bank) |
| benzphetamine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| carbamazepine |
|
Increases the effect of carbamazepine (source: Drug Bank) |
| carvedilol |
|
The SSRI increases the effect of the beta-blocker (source: Drug Bank) |
| cilostazol |
|
Increases the effect of cilostazol (source: Drug Bank) |
| clarithromycin |
|
Possible serotoninergic syndrome with this combination (source: Drug Bank) |
| clomipramine |
|
Fluoxetine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| clozapine |
|
The antidepressant increases the effect of clozapine (source: Drug Bank) |
| cyclosporine |
|
The antidepressant increases the effect and toxicity of cyclosporine (source: Drug Bank) |
| cyproheptadine |
|
Possible antagonism of action (source: Drug Bank) |
| desipramine |
|
Fluoxetine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| dexfenfluramine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| dextroamphetamine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| dextromethorphan |
|
Combination associated with possible serotoninergic syndrome (source: Drug Bank) |
| dicumarol |
|
The SSRI increases the effect of anticoagulant (source: Drug Bank) |
| diethylpropion |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| dihydroergotamine |
|
Possible ergotism and severe ischemia with this combination (source: Drug Bank) |
| doxepin |
|
Fluoxetine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| eletriptan |
|
Increased risk of CNS adverse effects (source: Drug Bank) |
| ergotamine |
|
Possible ergotism and severe ischemia with this combination (source: Drug Bank) |
| erythromycin |
|
Possible serotoninergic syndrome with this combination (source: Drug Bank) |
| ethotoin |
|
Fluoxetine increases the effect of phenytoin (source: Drug Bank) |
| fenfluramine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| fosphenytoin |
|
Fluoxetine increases the effect of phenytoin (source: Drug Bank) |
| frovatriptan |
|
Increased risk of CNS adverse effects (source: Drug Bank) |
| imipramine |
|
Fluoxetine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| isocarboxazid |
|
Possible severe adverse reaction with this combination (source: Drug Bank) |
| josamycin |
|
Possible serotoninergic syndrome 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 |
|
Fluoxetine increases the effect of phenytoin (source: Drug Bank) |
| mesoridazine |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| methamphetamine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| metoprolol |
|
The SSRI increases the effect of the beta-blocker (source: Drug Bank) |
| moclobemide |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| naratriptan |
|
Increased risk of CNS adverse effects (source: Drug Bank) |
| nortriptyline |
|
Fluoxetine increases the effect and toxicity of tricyclics (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) |
| phentermine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| phenylpropanolamine |
|
Risk of serotoninergic syndrome (source: Drug Bank) |
| phenytoin |
|
Fluoxetine increases the effect of phenytoin (source: Drug Bank) |
| propafenone |
|
Increases the effect and toxicity of propafenone (source: Drug Bank) |
| propranolol |
|
The SSRI increases the effect of the beta-blocker (source: Drug Bank) |
| protriptyline |
|
Fluoxetine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| rasagiline |
|
Possible severe adverse reaction with this combination (source: Drug Bank) |
| risperidone |
|
The SSRI increases the effect and toxicity of risperidone (source: Drug Bank) |
| ritonavir |
|
Increased risk of serotonin syndrome (source: Drug Bank) |
| rizatriptan |
|
Increased risk of CNS adverse effects (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) |
| terfenadine |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| thioridazine |
|
Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank) |
| tramadol |
|
Increased risk of serotonin syndrome (source: Drug Bank) |
| tranylcypromine |
|
Possible severe adverse reaction with this combination (source: Drug Bank) |
| trimipramine |
|
Fluoxetine increases the effect and toxicity of tricyclics (source: Drug Bank) |
| troleandomycin |
|
Possible serotoninergic syndrome with this combination (source: Drug Bank) |
| warfarin |
|
The SSRI increases the effect of 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 | |
|---|---|---|---|
|
|
Amblyopia |
|
Publications |
|
|
Anxiety Disorders |
|
Publications |
|
|
Breast Neoplasms |
|
Publications |
|
|
Death |
|
Publications |
|
|
Depression |
|
Publications, Variants |
|
|
Depression, Postpartum |
|
Publications |
|
|
Depressive Disorder |
|
Publications |
|
|
Depressive Disorder, Major |
|
Publications, Variants |
|
|
Long QT Syndrome |
|
Publications |
|
|
Obsessive-Compulsive Disorder |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Curated Phenotype Datasets
These datasets are sorted alphabetically by title.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
- Depression in Mexican-Americans - CRHR1
- Genetic Associations in Drug-induced QT Prolongation and Torsades
- Genetic Variants in Selective Serotonin Reuptake Inhibitors (SSRIs) associated Adverse Events
- PDEs and Depression in Mexican-Americans
- The Connectivity Map: using gene-expression signatures to connect small molecules, genes, and disease
Downloads
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LinkOuts
Common Searches
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Search Medline Plus
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Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.