clomethiazole 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 602 | 533-45-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A sedative and anticonvulsant often used in the treatment of alcohol withdrawal. Chlormethiazole has also been proposed as a neuroprotective agent. The mechanism of its therapeutic activity is not entirely clear, but it does potentiate GAMMA-AMINOBUTYRIC ACID receptors response and it may also affect glycine receptors.
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Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.50 | g | O |
| 1.50 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 10 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.05 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 33.94 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 25 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 6.60 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 33 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.36 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 4.50 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1981 | YEAR INTRODUCED |
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 |
|---|---|---|---|---|---|---|
| Vascular encephalopathy | 58.68 | 53.57 | 9 | 698 | 432 | 63487883 |
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 |
|---|---|---|---|---|---|---|
| Drug withdrawal convulsions | 63.95 | 45.87 | 12 | 631 | 1165 | 34955123 |
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 |
|---|---|---|---|---|---|---|
| Drug interaction | 64.83 | 39.41 | 55 | 1329 | 415128 | 79327876 |
| Drug withdrawal convulsions | 56.99 | 39.41 | 12 | 1372 | 2208 | 79740796 |
| Depressed level of consciousness | 52.75 | 39.41 | 28 | 1356 | 96624 | 79646380 |
| Vascular encephalopathy | 51.56 | 39.41 | 9 | 1375 | 614 | 79742390 |
| Joint hyperextension | 49.94 | 39.41 | 8 | 1376 | 323 | 79742681 |
| Persecutory delusion | 42.60 | 39.41 | 11 | 1373 | 4898 | 79738106 |
| Cogwheel rigidity | 42.38 | 39.41 | 10 | 1374 | 3078 | 79739926 |
| Subileus | 41.05 | 39.41 | 11 | 1373 | 5643 | 79737361 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N05CM02 | NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Other hypnotics and sedatives |
| ATC | N05CX04 | NERVOUS SYSTEM PSYCHOLEPTICS HYPNOTICS AND SEDATIVES Hypnotics and sedatives in combination, excl. barbiturates |
| MeSH PA | D000927 | Anticonvulsants |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D002492 | Central Nervous System Depressants |
| MeSH PA | D018682 | GABA Agents |
| MeSH PA | D018757 | GABA Modulators |
| MeSH PA | D006993 | Hypnotics and Sedatives |
| MeSH PA | D018696 | Neuroprotective Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D020011 | Protective Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Alcohol withdrawal syndrome | indication | 191480000 | |
| Insomnia | indication | 193462001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.16 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| GABA-A receptor alpha-1/beta-3/gamma-2 | Ion channel | WOMBAT-PK |
External reference:
| ID | Source |
|---|---|
| N0000167093 | NUI |
| D07330 | KEGG_DRUG |
| 20802 | RXNORM |
| C0008221 | UMLSCUI |
| CHEBI:92875 | CHEBI |
| CHEMBL315795 | ChEMBL_ID |
| DB06470 | DRUGBANK_ID |
| 10783 | PUBCHEM_CID |
| 1717 | INN_ID |
| 0C5DBZ19HV | UNII |
| 003691 | NDDF |
| 003692 | NDDF |
| 354039005 | SNOMEDCT_US |
| 395978007 | SNOMEDCT_US |
| 395988008 | SNOMEDCT_US |
| D002719 | MESH_DESCRIPTOR_UI |
Pharmaceutical products:
None