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tiagabine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| gabamimetic agents | 2648 | 115103-54-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
The precise mechanism by which tiagabine exerts its antiseizure effect is unknown, although it is believed to be related to its ability to block GABA uptake into presynaptic neurons, permitting more GABA to be available for receptor binding on the surfaces of post-synaptic cells.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 30 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 2.85 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| S (Water solubility) | 11 mg/mL | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 2 % | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 90 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 1.10 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 1.60 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.04 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 10 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.011 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 5.559 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 28.510 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.420 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 6.860 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 6.510 | % | High | 1 |
| herg | hERG pIC50 | 5.356 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.151 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.373 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 6.390 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAP3K7,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKDC,STK33,TEK,TGFBR1,ZAP70 | 34 | |||
| kinase-selectivity-class | AXL,BRAF,CDK9,EIF2AK3,EPHB4,GRK2,MAP2K6,MAPK7,SIK2,STK33,TEK | 11 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 10.864 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 12.474 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 9.908 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 7.840 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 41.687 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 0 | High | 1 | |
| pppb | Pig plasma protein binding (% unbound) | 7.040 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.040 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 14.997 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 54.880 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 8.480 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 993.116 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 30, 1997 | FDA | CEPHALON |
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 |
|---|---|---|---|---|---|---|
| Myoclonus | 123.22 | 68.58 | 25 | 303 | 19143 | 90608976 |
| Encephalopathy | 96.13 | 68.58 | 24 | 304 | 46420 | 90581699 |
| Seizure | 71.80 | 68.58 | 25 | 303 | 152604 | 90475515 |
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 |
|---|---|---|---|---|---|---|
| Status epilepticus | 48.38 | 47.15 | 14 | 443 | 15564 | 42605314 |
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 |
|---|---|---|---|---|---|---|
| Myoclonus | 92.54 | 39.22 | 24 | 619 | 32974 | 110555682 |
| Drug ineffective | 80.29 | 39.22 | 67 | 576 | 1520473 | 109068183 |
| Encephalopathy | 75.23 | 39.22 | 25 | 618 | 81030 | 110507626 |
| Seizure | 60.11 | 39.22 | 28 | 615 | 221157 | 110367499 |
| Drug withdrawal convulsions | 49.12 | 39.22 | 9 | 634 | 2440 | 110586216 |
| Status epilepticus | 47.01 | 39.22 | 14 | 629 | 31557 | 110557099 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N03AG06 | NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Fatty acid derivatives |
| FDA PE | N0000008486 | Decreased Central Nervous System Disorganized Electrical Activity |
| MeSH PA | D000927 | Anticonvulsants |
| MeSH PA | D014179 | Neurotransmitter Uptake Inhibitors |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018682 | GABA Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| MeSH PA | D058805 | GABA Uptake Inhibitors |
| FDA EPC | N0000175753 | Anti-epileptic Agent |
| CHEBI has role | CHEBI:35474 | anxiolytic drug |
| CHEBI has role | CHEBI:35476 | antipsychotic agent |
| CHEBI has role | CHEBI:35623 | anticonvulsant |
| CHEBI has role | CHEBI:85384 | GABA reuptake inhibitor |
Related Drugs by ATC class:
N03AG Fatty acid derivatives 5 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Epilepsy characterized by intractable complex partial seizures | indication | 442481002 | |
| Simple partial seizure | indication | 117891000119100 | |
| Suicidal thoughts | contraindication | 6471006 | |
| Depressive disorder | contraindication | 35489007 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.31 | acidic |
| pKa2 | 8.82 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Sodium- and chloride-dependent GABA transporter 1 | Transporter | INHIBITOR | Ki | 7.77 | CHEMBL | CHEMBL | |||
| Sodium- and chloride-dependent GABA transporter 1 | Transporter | Ki | 7.17 | CHEMBL | |||||
| Sodium- and chloride-dependent GABA transporter 1 | Transporter | Ki | 7.41 | CHEMBL | |||||
| Sodium- and chloride-dependent betaine transporter | Transporter | IC50 | 6.74 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4024093 | VUID |
| N0000022098 | NUI |
| D02097 | KEGG_DRUG |
| 145821-59-6 | SECONDARY_CAS_RN |
| 4021068 | VANDF |
| 4024093 | VANDF |
| C0068897 | UMLSCUI |
| CHEBI:9586 | CHEBI |
| TGI | PDB_CHEM_ID |
| CHEMBL1027 | ChEMBL_ID |
| CHEMBL1695 | ChEMBL_ID |
| DB00906 | DRUGBANK_ID |
| D000078308 | MESH_DESCRIPTOR_UI |
| 60648 | PUBCHEM_CID |
| 4818 | IUPHAR_LIGAND_ID |
| 6306 | INN_ID |
| Z80I64HMNP | UNII |
| 236875 | RXNORM |
| 53205 | MMSL |
| 5580 | MMSL |
| d04221 | MMSL |
| 007057 | NDDF |
| 007058 | NDDF |
| 108403006 | SNOMEDCT_US |
| 108404000 | SNOMEDCT_US |
| 372485004 | SNOMEDCT_US |
| Z80I64HMNP | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Tiagabine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-5030 | TABLET, FILM COATED | 2 mg | ORAL | NDA authorized generic | 27 sections |
| Tiagabine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-5031 | TABLET, FILM COATED | 4 mg | ORAL | NDA authorized generic | 27 sections |
| Tiagabine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-8072 | TABLET, FILM COATED | 12 mg | ORAL | NDA authorized generic | 27 sections |
| Tiagabine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-8076 | TABLET, FILM COATED | 16 mg | ORAL | NDA authorized generic | 27 sections |
| GABITRIL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-832 | TABLET | 12 mg | ORAL | NDA | 16 sections |
| TIAGABINE HYDROCHLORIDE | Human Prescription Drug Label | 1 | 62756-200 | TABLET, FILM COATED | 2 mg | ORAL | ANDA | 25 sections |
| TIAGABINE HYDROCHLORIDE | Human Prescription Drug Label | 1 | 62756-224 | TABLET, FILM COATED | 4 mg | ORAL | ANDA | 25 sections |
| GABITRIL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68151-4235 | TABLET, FILM COATED | 4 mg | ORAL | NDA | 26 sections |
| Tiagabine Hydrochloride | Human Prescription Drug Label | 1 | 72205-084 | TABLET | 2 mg | ORAL | ANDA | 22 sections |
| Tiagabine Hydrochloride | Human Prescription Drug Label | 1 | 72205-085 | TABLET | 4 mg | ORAL | ANDA | 22 sections |
| Tiagabine Hydrochloride | Human Prescription Drug Label | 1 | 72205-086 | TABLET | 12 mg | ORAL | ANDA | 22 sections |
| Tiagabine Hydrochloride | Human Prescription Drug Label | 1 | 72205-087 | TABLET | 16 mg | ORAL | ANDA | 22 sections |