felbamate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tranquillizers, propanediol and pentanediol derivatives | 1140 | 25451-15-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A PEGylated phenylcarbamate derivative that acts as an antagonist of NMDA RECEPTORS. It is used as an anticonvulsant, primarily for the treatment of SEIZURES in severe refractory EPILEPSY.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 2.40 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.74 mg/mL | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 45 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 251.84 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 90 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 29, 1993 | FDA | MEDA PHARMS |
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 |
|---|---|---|---|---|---|---|
| Seizure | 169.16 | 60.16 | 64 | 791 | 132570 | 63355597 |
| Unmasking of previously unidentified disease | 76.77 | 60.16 | 13 | 842 | 963 | 63487204 |
| Electrocardiogram ST segment elevation | 75.60 | 60.16 | 16 | 839 | 3911 | 63484256 |
| Laryngeal stenosis | 75.48 | 60.16 | 13 | 842 | 1065 | 63487102 |
| Electrocardiogram repolarisation abnormality | 66.31 | 60.16 | 12 | 843 | 1305 | 63486862 |
| Tachycardia | 66.18 | 60.16 | 32 | 823 | 118124 | 63370043 |
| Systolic dysfunction | 63.98 | 60.16 | 12 | 843 | 1587 | 63486580 |
| Electrocardiogram QRS complex prolonged | 63.72 | 60.16 | 15 | 840 | 5923 | 63482244 |
| Cardiotoxicity | 63.42 | 60.16 | 16 | 839 | 8422 | 63479745 |
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 |
|---|---|---|---|---|---|---|
| Seizure | 298.24 | 51.68 | 104 | 688 | 104753 | 34851386 |
| Generalised tonic-clonic seizure | 82.75 | 51.68 | 27 | 765 | 21147 | 34934992 |
| Drug ineffective | 66.75 | 51.68 | 65 | 727 | 456686 | 34499453 |
| Benzodiazepine drug level decreased | 55.36 | 51.68 | 7 | 785 | 35 | 34956104 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Seizure | 305.73 | 51.11 | 116 | 1268 | 188718 | 79554286 |
| Generalised tonic-clonic seizure | 88.72 | 51.11 | 32 | 1352 | 43878 | 79699126 |
| Laryngeal stenosis | 72.03 | 51.11 | 13 | 1371 | 1075 | 79741929 |
| Drug ineffective | 68.56 | 51.11 | 88 | 1296 | 1080825 | 78662179 |
| Unmasking of previously unidentified disease | 63.77 | 51.11 | 13 | 1371 | 2044 | 79740960 |
| Multiple-drug resistance | 63.35 | 51.11 | 17 | 1367 | 8791 | 79734213 |
| Electrocardiogram ST segment elevation | 59.41 | 51.11 | 16 | 1368 | 8381 | 79734623 |
| Benzodiazepine drug level decreased | 57.21 | 51.11 | 7 | 1377 | 35 | 79742969 |
| Electrocardiogram repolarisation abnormality | 56.74 | 51.11 | 12 | 1372 | 2255 | 79740749 |
| Petit mal epilepsy | 55.44 | 51.11 | 14 | 1370 | 5713 | 79737291 |
| Cardiotoxicity | 53.45 | 51.11 | 16 | 1368 | 12223 | 79730781 |
| Toxicity to various agents | 52.14 | 51.11 | 49 | 1335 | 421491 | 79321513 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N03AX10 | NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Other antiepileptics |
| FDA PE | N0000008486 | Decreased Central Nervous System Disorganized Electrical Activity |
| CHEBI has role | CHEBI:35623 | anticonvulsants |
| CHEBI has role | CHEBI:63726 | neuroprotective agents |
| MeSH PA | D000927 | Anticonvulsants |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D018691 | Excitatory Amino Acid Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| FDA EPC | N0000175753 | Anti-epileptic Agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Epilepsy | indication | 84757009 | DOID:1826 |
| Lennox-Gastaut syndrome | indication | 230418006 | |
| Simple partial seizure | indication | 117891000119100 | |
| Suicidal thoughts | contraindication | 6471006 | |
| Torsades de pointes | contraindication | 31722008 | |
| Depressive disorder | contraindication | 35489007 | |
| Hepatic failure | contraindication | 59927004 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Prolonged QT interval | contraindication | 111975006 | |
| Liver function tests abnormal | contraindication | 166603001 | |
| Disease of blood AND/OR blood-forming organ | contraindication | 191124002 | DOID:74 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Aplastic anemia | contraindication | 306058006 | DOID:12449 |
| Bone marrow depression | contraindication | 307762000 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Porphyria | contraindication | 418470004 | |
| Congenital long QT syndrome | contraindication | 442917000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.24 | acidic |
| pKa2 | 13.84 | acidic |
Orange Book patent data (new drug applications)
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| Glutamate receptor ionotropic, NMDA 2A | Ion channel | ANTAGONIST | DRUGBANK | CHEMBL | |||||
| Glutamate receptor ionotropic, NMDA 2B | Ion channel | ANTAGONIST | IC50 | 4.28 | WOMBAT-PK | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4020832 | VUID |
| N0000148344 | NUI |
| D00536 | KEGG_DRUG |
| 4020832 | VANDF |
| C0060135 | UMLSCUI |
| CHEBI:4995 | CHEBI |
| CHEMBL1094 | ChEMBL_ID |
| DB00949 | DRUGBANK_ID |
| D000078328 | MESH_DESCRIPTOR_UI |
| 3331 | PUBCHEM_CID |
| 5473 | IUPHAR_LIGAND_ID |
| 5686 | INN_ID |
| X72RBB02N8 | UNII |
| 224900 | RXNORM |
| 185493 | MMSL |
| 3074 | MMSL |
| 4715 | MMSL |
| d03170 | MMSL |
| 004277 | NDDF |
| 371387009 | SNOMEDCT_US |
| 96194006 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Felbatol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0037-0430 | TABLET | 400 mg | ORAL | NDA | 31 sections |
| Felbatol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0037-0430 | TABLET | 400 mg | ORAL | NDA | 31 sections |
| Felbatol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0037-0431 | TABLET | 600 mg | ORAL | NDA | 31 sections |
| Felbatol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0037-0431 | TABLET | 600 mg | ORAL | NDA | 31 sections |
| Felbatol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0037-0442 | SUSPENSION | 600 mg | ORAL | NDA | 31 sections |
| Felbatol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0037-0442 | SUSPENSION | 600 mg | ORAL | NDA | 31 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0121-0891 | SUSPENSION | 600 mg | ORAL | ANDA | 33 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-601 | TABLET | 400 mg | ORAL | ANDA | 28 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-602 | TABLET | 600 mg | ORAL | ANDA | 28 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-775 | SUSPENSION | 600 mg | ORAL | ANDA | 33 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47781-627 | TABLET | 400 mg | ORAL | ANDA | 32 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47781-627 | TABLET | 400 mg | ORAL | ANDA | 32 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47781-630 | TABLET | 600 mg | ORAL | ANDA | 32 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 47781-630 | TABLET | 600 mg | ORAL | ANDA | 32 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51525-0430 | TABLET | 400 mg | ORAL | NDA authorized generic | 31 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51525-0430 | TABLET | 400 mg | ORAL | NDA authorized generic | 31 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51525-0431 | TABLET | 600 mg | ORAL | NDA authorized generic | 31 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51525-0431 | TABLET | 600 mg | ORAL | NDA authorized generic | 31 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51525-0442 | SUSPENSION | 600 mg | ORAL | NDA authorized generic | 31 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51525-0442 | SUSPENSION | 600 mg | ORAL | NDA authorized generic | 31 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-4172 | SUSPENSION | 600 mg | ORAL | ANDA | 33 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-4185 | TABLET | 400 mg | ORAL | ANDA | 34 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-4185 | TABLET | 400 mg | ORAL | ANDA | 34 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-4186 | TABLET | 600 mg | ORAL | ANDA | 34 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51672-4186 | TABLET | 600 mg | ORAL | ANDA | 34 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53746-734 | TABLET | 400 mg | ORAL | ANDA | 15 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53746-735 | TABLET | 600 mg | ORAL | ANDA | 15 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-730 | TABLET | 400 mg | ORAL | ANDA | 31 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-730 | TABLET | 400 mg | ORAL | ANDA | 31 sections |
| Felbamate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-731 | TABLET | 600 mg | ORAL | ANDA | 31 sections |