fluvoxamine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1230 | 54739-18-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A selective serotonin reuptake inhibitor that is used in the treatment of DEPRESSION and a variety of ANXIETY DISORDERS.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 14.87 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 2 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 13.46 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 53 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 23.50 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 31.95 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.20 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 12.50 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 5, 1994 | FDA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Toxicity to various agents | 198.51 | 60.09 | 58 | 339 | 32696 | 2324992 |
| Drug interaction | 151.44 | 60.09 | 46 | 351 | 29117 | 2328571 |
| Completed suicide | 134.26 | 60.09 | 39 | 358 | 20995 | 2336693 |
| Serotonin syndrome | 101.68 | 60.09 | 22 | 375 | 3518 | 2354170 |
| Intentional self-injury | 98.32 | 60.09 | 22 | 375 | 4105 | 2353583 |
| Suicide attempt | 90.02 | 60.09 | 25 | 372 | 11257 | 2346431 |
| Intentional overdose | 71.81 | 60.09 | 21 | 376 | 11300 | 2346388 |
| Depression | 67.54 | 60.09 | 25 | 372 | 28107 | 2329581 |
| Schizophrenia | 65.52 | 60.09 | 13 | 384 | 1346 | 2356342 |
| Electrocardiogram QT prolonged | 65.34 | 60.09 | 18 | 379 | 7796 | 2349892 |
| Anxiety | 62.86 | 60.09 | 24 | 373 | 29335 | 2328353 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Completed suicide | 132.15 | 46.55 | 41 | 366 | 16271 | 1730103 |
| Toxicity to various agents | 131.37 | 46.55 | 47 | 360 | 29094 | 1717280 |
| Serotonin syndrome | 122.68 | 46.55 | 27 | 380 | 2761 | 1743613 |
| Drug interaction | 85.12 | 46.55 | 34 | 373 | 27924 | 1718450 |
| Schizophrenia | 79.86 | 46.55 | 18 | 389 | 2028 | 1744346 |
| Obsessive-compulsive disorder | 65.10 | 46.55 | 13 | 394 | 815 | 1745559 |
| Drug ineffective | 63.81 | 46.55 | 36 | 371 | 63765 | 1682609 |
| Cardio-respiratory arrest | 60.88 | 46.55 | 20 | 387 | 9273 | 1737101 |
| Condition aggravated | 51.44 | 46.55 | 22 | 385 | 21128 | 1725246 |
| Overdose | 49.44 | 46.55 | 20 | 387 | 16681 | 1729693 |
| Intentional overdose | 48.14 | 46.55 | 16 | 391 | 7654 | 1738720 |
| Akathisia | 48.05 | 46.55 | 11 | 396 | 1317 | 1745057 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N06AB08 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Selective serotonin reuptake inhibitors |
| CHEBI has role | CHEBI:50949 | serotonin uptake inhibitor |
| CHEBI has role | CHEBI:35474 | anxiolytic drug |
| CHEBI has role | CHEBI:35469 | antidepressant |
| MeSH PA | D014151 | Anti-Anxiety Agents |
| MeSH PA | D000928 | Antidepressive Agents |
| MeSH PA | D018687 | Antidepressive Agents, Second-Generation |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D065609 | Cytochrome P-450 CYP1A2 Inhibitors |
| MeSH PA | D065689 | Cytochrome P-450 CYP2C19 Inhibitors |
| MeSH PA | D065607 | Cytochrome P-450 Enzyme Inhibitors |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D049990 | Membrane Transport Modulators |
| MeSH PA | D065606 | Metabolic Side Effects of Drugs and Substances |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D014179 | Neurotransmitter Uptake Inhibitors |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D018490 | Serotonin Agents |
| MeSH PA | D017367 | Serotonin Uptake Inhibitors |
| FDA EPC | N0000175696 | Serotonin Reuptake Inhibitor |
| MeSH PA | D014149 | Tranquilizing Agents |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Social phobia | indication | 25501002 | DOID:11257 |
| Obsessive-compulsive disorder | indication | 191736004 | DOID:10933 |
| Depressive disorder | off-label use | 35489007 | |
| Posttraumatic stress disorder | off-label use | 47505003 | DOID:2055 |
| Bipolar affective disorder, current episode depression | off-label use | 191627008 | DOID:3312 |
| Suicidal thoughts | contraindication | 6471006 | |
| Bipolar disorder | contraindication | 13746004 | DOID:3312 |
| Neuroleptic malignant syndrome | contraindication | 15244003 | DOID:14464 |
| Upper gastrointestinal hemorrhage | contraindication | 37372002 | |
| Syndrome of inappropriate vasopressin secretion | contraindication | 55004003 | DOID:3401 |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Hyponatremia | contraindication | 89627008 | |
| Mania | contraindication | 231494001 | |
| Hypomania | contraindication | 231496004 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Serotonin syndrome | contraindication | 371089000 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Poor metabolizer due to cytochrome p450 CYP2D6 variant | contraindication | 423629005 | |
| Smokes tobacco daily | contraindication | 449868002 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.36 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| 100MG **Federal Register determination that product was not discontinued or withdrawn for safety or efficacy reasons** | LUVOX CR | JAZZ PHARMS | N022033 | Feb. 28, 2008 | DISCN | CAPSULE, EXTENDED RELEASE | ORAL | 7465462 | May 10, 2020 | TREATMENT OF OBSESSIVE COMPULSIVE DISORDER TREATABLE WITH AN SSRI |
| 150MG **Federal Register determination that product was not discontinued or withdrawn for safety or efficacy reasons** | LUVOX CR | JAZZ PHARMS | N022033 | Feb. 28, 2008 | DISCN | CAPSULE, EXTENDED RELEASE | ORAL | 7465462 | May 10, 2020 | TREATMENT OF OBSESSIVE COMPULSIVE DISORDER TREATABLE WITH AN SSRI |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sodium-dependent serotonin transporter | Transporter | INHIBITOR | Ki | 8.51 | WOMBAT-PK | CHEMBL | |||
| Sodium-dependent dopamine transporter | Transporter | Ki | 8.84 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 7.44 | CHEMBL | |||||
| Cytochrome P450 1A2 | Enzyme | Ki | 5.07 | WOMBAT-PK | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.95 | PDSP | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 7.44 | CHEMBL | |||||
| Sodium-dependent serotonin transporter | Transporter | INHIBITOR | Ki | 8.19 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4023976 | VUID |
| N0000021981 | NUI |
| C0085228 | UMLSCUI |
| D00824 | KEGG_DRUG |
| 5LGN83G74V | UNII |
| 61718-82-9 | SECONDARY_CAS_RN |
| 96213009 | SNOMEDCT_US |
| 4023976 | VANDF |
| 003633 | NDDF |
| 42355 | RXNORM |
| d03804 | MMSL |
| 372905008 | SNOMEDCT_US |
| CHEMBL814 | ChEMBL_ID |
| CHEMBL1409 | ChEMBL_ID |
| DB00176 | DRUGBANK_ID |
| 3879 | INN_ID |
| FVX | PDB_CHEM_ID |
| CHEBI:5138 | CHEBI |
| 5324346 | PUBCHEM_CID |
| D016666 | MESH_DESCRIPTOR_UI |
| 7189 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Fluvoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0228-2848 | CAPSULE, EXTENDED RELEASE | 100 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0228-2849 | CAPSULE, EXTENDED RELEASE | 150 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-0407 | TABLET, FILM COATED | 25 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-0412 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-0414 | TABLET, FILM COATED | 100 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-7569 | TABLET, FILM COATED | 100 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0832-1670 | TABLET, FILM COATED | 25 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0832-1671 | TABLET, FILM COATED | 50 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0832-1672 | TABLET, FILM COATED | 100 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10370-175 | CAPSULE, EXTENDED RELEASE | 100 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10370-176 | CAPSULE, EXTENDED RELEASE | 150 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-270 | TABLET | 25 mg | ORAL | NDA | 11 sections |
| fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 33261-683 | TABLET, COATED | 50 mg | ORAL | NDA AUTHORIZED GENERIC | 21 sections |
| Fluvoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-0164 | TABLET | 25 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-0165 | TABLET | 50 mg | ORAL | ANDA | 20 sections |
| Fluvoxamine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60505-0166 | TABLET | 100 mg | ORAL | ANDA | 20 sections |
| fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-158 | TABLET, COATED | 25 mg | ORAL | NDA authorized generic | 20 sections |
| fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-159 | TABLET, COATED | 50 mg | ORAL | NDA authorized generic | 20 sections |
| fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-160 | TABLET, COATED | 100 mg | ORAL | NDA authorized generic | 20 sections |
| fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-8018 | TABLET, COATED | 25 mg | ORAL | NDA authorized generic | 21 sections |
| fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68151-0637 | TABLET, COATED | 50 mg | ORAL | NDA authorized generic | 21 sections |
| fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68788-7219 | TABLET, COATED | 100 mg | ORAL | NDA authorized generic | 21 sections |
| fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-1057 | TABLET, COATED | 100 mg | ORAL | NDA authorized generic | 21 sections |
| fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-1643 | TABLET, COATED | 50 mg | ORAL | NDA authorized generic | 21 sections |
| fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70518-1789 | TABLET, COATED | 25 mg | ORAL | NDA authorized generic | 21 sections |
| fluvoxamine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-0264 | TABLET, COATED | 100 mg | ORAL | NDA authorized generic | 20 sections |