Stem definition | Drug id | CAS RN |
---|---|---|
gabamimetic agents | 2648 | 115103-54-3 |
Dose | Unit | Route |
---|---|---|
30 | mg | O |
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) | 0.03 mg/mL | Hosey CM, Chan R, 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 |
Date | Agency | Company | Orphan |
---|---|---|---|
Sept. 30, 1997 | FDA | CEPHALON |
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 | 175.66 | 27.03 | 85 | 1533 | 122969 | 46561475 |
Epilepsy | 35.39 | 27.03 | 17 | 1601 | 23721 | 46660723 |
Serotonin syndrome | 35.06 | 27.03 | 17 | 1601 | 24203 | 46660241 |
Status epilepticus | 33.63 | 27.03 | 14 | 1604 | 13965 | 46670479 |
Focal dyscognitive seizures | 31.80 | 27.03 | 9 | 1609 | 2819 | 46681625 |
Confusional state | 31.66 | 27.03 | 33 | 1585 | 159859 | 46524585 |
Tremor | 30.62 | 27.03 | 28 | 1590 | 115611 | 46568833 |
Generalised tonic-clonic seizure | 27.55 | 27.03 | 15 | 1603 | 27107 | 46657337 |
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 | 84.02 | 36.27 | 47 | 915 | 98428 | 29853088 |
Status epilepticus | 77.74 | 36.27 | 24 | 938 | 11048 | 29940468 |
Generalised tonic-clonic seizure | 60.71 | 36.27 | 23 | 939 | 19528 | 29931988 |
Completed suicide | 47.71 | 36.27 | 33 | 929 | 99459 | 29852057 |
Drug withdrawal convulsions | 40.47 | 36.27 | 9 | 953 | 1150 | 29950366 |
Source | Code | Description |
---|---|---|
ATC | N03AG06 | NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Fatty acid derivatives |
FDA PE | N0000008486 | Decreased Central Nervous System Disorganized Electrical Activity |
FDA EPC | N0000175753 | Anti-epileptic Agent |
MeSH PA | D000927 | Anticonvulsants |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D018682 | GABA Agents |
MeSH PA | D058805 | GABA Uptake Inhibitors |
MeSH PA | D049990 | Membrane Transport Modulators |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D014179 | Neurotransmitter Uptake Inhibitors |
CHEBI has role | CHEBI:35623 | antiepileptic |
CHEBI has role | CHEBI:85384 | gamma-aminobutyric acid re-uptake inhibitors |
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 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 3.31 | acidic |
pKa2 | 8.82 | Basic |
None
None
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 | Unclassified | IC50 | 6.74 | CHEMBL |
ID | Source |
---|---|
4024093 | VUID |
N0000022098 | NUI |
D02097 | KEGG_DRUG |
145821-59-6 | SECONDARY_CAS_RN |
4021068 | VANDF |
4024093 | VANDF |
C0068897 | UMLSCUI |
CHEBI:9586 | CHEBI |
60648 | PUBCHEM_CID |
CHEMBL1027 | ChEMBL_ID |
CHEMBL1695 | ChEMBL_ID |
D000078308 | MESH_DESCRIPTOR_UI |
6306 | INN_ID |
DB00906 | DRUGBANK_ID |
Z80I64HMNP | UNII |
4818 | IUPHAR_LIGAND_ID |
236875 | RXNORM |
53205 | MMSL |
5580 | MMSL |
d04221 | MMSL |
007057 | NDDF |
007058 | NDDF |
108403006 | SNOMEDCT_US |
108404000 | SNOMEDCT_US |
372485004 | SNOMEDCT_US |
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 | 52536-350 | TABLET | 2 mg | ORAL | ANDA | 29 sections |
tiagabine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52536-355 | TABLET | 4 mg | ORAL | ANDA | 29 sections |
tiagabine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52536-360 | TABLET | 12 mg | ORAL | ANDA | 29 sections |
tiagabine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 52536-365 | TABLET | 16 mg | ORAL | ANDA | 29 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 | 63459-402 | TABLET, FILM COATED | 2 mg | ORAL | NDA | 26 sections |
GABITRIL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63459-404 | TABLET, FILM COATED | 4 mg | ORAL | NDA | 26 sections |
GABITRIL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63459-412 | TABLET, FILM COATED | 12 mg | ORAL | NDA | 26 sections |
GABITRIL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63459-416 | TABLET, FILM COATED | 16 mg | ORAL | NDA | 26 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 | 69238-1104 | TABLET | 2 mg | ORAL | ANDA | 25 sections |
Tiagabine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1105 | TABLET | 4 mg | ORAL | ANDA | 25 sections |
Tiagabine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1106 | TABLET | 12 mg | ORAL | ANDA | 25 sections |
Tiagabine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1107 | TABLET | 16 mg | ORAL | ANDA | 25 sections |