chlorzoxazone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 626 | 95-25-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1.50 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.25 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 196.38 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 15, 1958 | FDA | JANSSEN R AND D |
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 |
|---|---|---|---|---|---|---|
| Intentional overdose | 108.18 | 23.07 | 48 | 1628 | 74104 | 63413242 |
| Intentional self-injury | 108.05 | 23.07 | 36 | 1640 | 25651 | 63461695 |
| Completed suicide | 48.68 | 23.07 | 36 | 1640 | 145637 | 63341709 |
| Stress cardiomyopathy | 34.77 | 23.07 | 12 | 1664 | 9438 | 63477908 |
| Toxicity to various agents | 34.00 | 23.07 | 37 | 1639 | 247213 | 63240133 |
| Pulmonary renal syndrome | 31.32 | 23.07 | 6 | 1670 | 448 | 63486898 |
| Depressed level of consciousness | 29.29 | 23.07 | 19 | 1657 | 62059 | 63425287 |
| Stevens-Johnson syndrome | 26.48 | 23.07 | 13 | 1663 | 24937 | 63462409 |
| Anti-neutrophil cytoplasmic antibody positive vasculitis | 24.70 | 23.07 | 7 | 1669 | 2892 | 63484454 |
| Loss of consciousness | 24.21 | 23.07 | 22 | 1654 | 118099 | 63369247 |
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 |
|---|---|---|---|---|---|---|
| Secondary adrenocortical insufficiency | 84.27 | 42.28 | 14 | 291 | 1456 | 34955170 |
| Spinal column injury | 50.45 | 42.28 | 8 | 297 | 616 | 34956010 |
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 |
|---|---|---|---|---|---|---|
| Intentional self-injury | 89.63 | 24.80 | 31 | 1574 | 32388 | 79710395 |
| Intentional overdose | 88.82 | 24.80 | 43 | 1562 | 105917 | 79636866 |
| Secondary adrenocortical insufficiency | 62.30 | 24.80 | 14 | 1591 | 3000 | 79739783 |
| Completed suicide | 48.94 | 24.80 | 40 | 1565 | 245727 | 79497056 |
| Stress cardiomyopathy | 36.00 | 24.80 | 12 | 1593 | 11154 | 79731629 |
| Spinal column injury | 33.65 | 24.80 | 8 | 1597 | 2190 | 79740593 |
| Pulmonary renal syndrome | 30.89 | 24.80 | 6 | 1599 | 634 | 79742149 |
| Loss of consciousness | 30.59 | 24.80 | 26 | 1579 | 167917 | 79574866 |
| Sensory disturbance | 28.83 | 24.80 | 11 | 1594 | 15066 | 79727717 |
| Toxicity to various agents | 27.74 | 24.80 | 38 | 1567 | 421502 | 79321281 |
| Dizziness | 26.75 | 24.80 | 42 | 1563 | 526399 | 79216384 |
| Anti-neutrophil cytoplasmic antibody positive vasculitis | 24.84 | 24.80 | 7 | 1598 | 3722 | 79739061 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | M03BB03 | MUSCULO-SKELETAL SYSTEM MUSCLE RELAXANTS MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS Oxazol, thiazine, and triazine derivatives |
| ATC | M03BB53 | MUSCULO-SKELETAL SYSTEM MUSCLE RELAXANTS MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS Oxazol, thiazine, and triazine derivatives |
| ATC | M03BB73 | MUSCULO-SKELETAL SYSTEM MUSCLE RELAXANTS MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS Oxazol, thiazine, and triazine derivatives |
| CHEBI has role | CHEBI:35717 | hypnotics |
| CHEBI has role | CHEBI:51371 | muscle relaxants |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D009125 | Muscle Relaxants, Central |
| MeSH PA | D009465 | Neuromuscular Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| FDA PE | N0000175730 | Centrally-mediated Muscle Relaxation |
| FDA EPC | N0000175737 | Muscle Relaxant |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Spasticity | indication | 221360009 | |
| Muscle Spasm with Pain | indication | ||
| Alcoholism | contraindication | 7200002 | |
| Hepatic failure | contraindication | 59927004 | |
| Poisoning by acetaminophen | contraindication | 70273001 | |
| Liver function tests abnormal | contraindication | 166603001 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Drug-induced hepatitis | contraindication | 235876009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.22 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Calcium-activated potassium channel subunit alpha-1 | Ion channel | OPENER | EC50 | 4.52 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Intermediate conductance calcium-activated potassium channel protein 4 | Ion channel | ACTIVATOR | EC50 | 4 | IUPHAR | ||||
| Nitric oxide synthase, brain | Enzyme | IC50 | 4.30 | CHEMBL | |||||
| Nitric oxide synthase, inducible | Enzyme | IC50 | 4.85 | CHEMBL | |||||
| Nitric oxide synthase, endothelial | Enzyme | IC50 | 5.06 | CHEMBL | |||||
| Nitric oxide synthase, brain | Enzyme | IC50 | 5.55 | DRUG MATRIX | |||||
| Small conductance calcium-activated potassium channel protein 2 | Ion channel | ACTIVATOR | EC50 | 4.10 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4017882 | VUID |
| N0000146235 | NUI |
| D00771 | KEGG_DRUG |
| 2410 | RXNORM |
| 4017882 | VANDF |
| C0008296 | UMLSCUI |
| CHEBI:3655 | CHEBI |
| CLW | PDB_CHEM_ID |
| CHEMBL1371 | ChEMBL_ID |
| DB00356 | DRUGBANK_ID |
| D002753 | MESH_DESCRIPTOR_UI |
| 2733 | PUBCHEM_CID |
| 748 | INN_ID |
| 2322 | IUPHAR_LIGAND_ID |
| H0DE420U8G | UNII |
| 4369 | MMSL |
| 4433 | MMSL |
| d00962 | MMSL |
| 001671 | NDDF |
| 400361007 | SNOMEDCT_US |
| 44908000 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0254-2005 | TABLET | 750 mg | ORAL | ANDA | 11 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0254-2053 | TABLET | 375 mg | ORAL | ANDA | 11 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-2520 | TABLET | 500 mg | ORAL | ANDA | 12 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-2520 | TABLET | 500 mg | ORAL | ANDA | 12 sections |
| chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13811-717 | TABLET | 375 mg | ORAL | ANDA | 12 sections |
| chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13811-717 | TABLET | 375 mg | ORAL | ANDA | 12 sections |
| chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13811-718 | TABLET | 750 mg | ORAL | ANDA | 12 sections |
| chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 13811-718 | TABLET | 750 mg | ORAL | ANDA | 12 sections |
| CHLORZOXAZONE | Human Prescription Drug Label | 1 | 16571-725 | TABLET | 375 mg | ORAL | ANDA | 11 sections |
| CHLORZOXAZONE | Human Prescription Drug Label | 1 | 16571-725 | TABLET | 375 mg | ORAL | ANDA | 11 sections |
| CHLORZOXAZONE | Human Prescription Drug Label | 1 | 16571-726 | TABLET | 500 mg | ORAL | ANDA | 11 sections |
| CHLORZOXAZONE | Human Prescription Drug Label | 1 | 16571-726 | TABLET | 500 mg | ORAL | ANDA | 11 sections |
| CHLORZOXAZONE | Human Prescription Drug Label | 1 | 16571-727 | TABLET | 750 mg | ORAL | ANDA | 11 sections |
| CHLORZOXAZONE | Human Prescription Drug Label | 1 | 16571-727 | TABLET | 750 mg | ORAL | ANDA | 11 sections |
| CHLORZOXAZONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-478 | TABLET | 500 mg | ORAL | ANDA | 12 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-569 | TABLET | 500 mg | ORAL | ANDA | 12 sections |
| CHLORZOXAZONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24470-923 | TABLET | 250 mg | ORAL | ANDA | 12 sections |
| CHLORZOXAZONE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24470-923 | TABLET | 250 mg | ORAL | ANDA | 12 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 33261-021 | TABLET | 500 mg | ORAL | ANDA | 12 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42254-076 | TABLET | 500 mg | ORAL | ANDA | 12 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42494-425 | TABLET | 375 mg | ORAL | ANDA | 14 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42494-426 | TABLET | 500 mg | ORAL | ANDA | 14 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42494-427 | TABLET | 500 mg | ORAL | ANDA | 14 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42494-428 | TABLET | 750 mg | ORAL | ANDA | 14 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 45865-434 | TABLET | 500 mg | ORAL | ANDA | 12 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 49999-044 | TABLET | 500 mg | ORAL | ANDA | 12 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-0315 | TABLET | 500 mg | ORAL | ANDA | 12 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-0315 | TABLET | 500 mg | ORAL | ANDA | 12 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-0316 | TABLET | 500 mg | ORAL | ANDA | 12 sections |
| Chlorzoxazone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51862-338 | TABLET | 375 mg | ORAL | ANDA | 14 sections |