metaxalone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
1722 1665-48-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • metaxalone
  • metaxalon
  • metazalone
  • metazolone
  • skelaxin
  • zorane
  • AHR 438
muscle spasm relaxant; structure
  • Molecular weight: 221.26
  • Formula: C12H15NO3
  • CLOGP: 2.15
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 47.56
  • ALOGS: -2.24
  • ROTB: 3
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 0.30 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 2 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 206.61 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK10,MAPK7,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PIM2,PRKDC,SIK2,SIK3,STK33,TEK 37
kinase-selectivity-class AXL,BRAF,CDK9,DDR1,EIF2AK3,EPHB4,ERBB2,GRK2,MAPK7,PDK4,PRKCD,SIK2,SIK3 13
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Aug. 13, 1962 FDA KING PHARMS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Completed suicide 380.57 18.02 190 6109 144868 90477280
Toxicity to various agents 297.15 18.02 206 6093 287640 90334508
Accidental death 278.98 18.02 56 6243 1992 90620156
Drug hypersensitivity 229.91 18.02 216 6083 463393 90158755
Serotonin syndrome 85.51 18.02 45 6254 37842 90584306
Overdose 54.87 18.02 61 6238 157648 90464500
Clonus 47.18 18.02 17 6282 5733 90616415
Foot fracture 42.00 18.02 25 6274 26581 90595567
Drug abuse 41.65 18.02 39 6260 82308 90539840
Purpura senile 39.20 18.02 9 6290 606 90621542
Muscle rigidity 38.07 18.02 19 6280 14290 90607858
Respiratory arrest 34.48 18.02 24 6275 33287 90588861
Tarsal tunnel syndrome 34.41 18.02 8 6291 569 90621579
Concussion 30.31 18.02 15 6284 11076 90611072
Resorption bone increased 28.47 18.02 8 6291 1211 90620937
Autonomic nervous system imbalance 27.55 18.02 10 6289 3440 90618708
Vestibular disorder 26.58 18.02 8 6291 1541 90620607
Suicidal behaviour 25.57 18.02 9 6290 2835 90619313
Ankle fracture 24.23 18.02 16 6283 20354 90601794
Fall 23.33 18.02 80 6219 481730 90140418
Unresponsive to stimuli 23.10 18.02 20 6279 38101 90584047
Hyperreflexia 21.20 18.02 10 6289 6647 90615501
Mydriasis 20.85 18.02 13 6286 14999 90607149
Poisoning 20.69 18.02 13 6286 15204 90606944
Vertigo positional 20.55 18.02 8 6291 3336 90618812
Exposure via ingestion 18.61 18.02 7 6292 2660 90619488
Bronchitis 18.60 18.02 36 6263 152891 90469257

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Toxicity to various agents 170.49 27.08 96 1138 229040 42391061
Completed suicide 170.06 27.08 73 1161 96392 42523709
Accidental death 77.74 27.08 18 1216 3065 42617036
Drug hypersensitivity 63.45 27.08 38 1196 99351 42520750
Cerebral vasoconstriction 27.61 27.08 5 1229 250 42619851

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Completed suicide 589.23 19.70 278 5724 242103 110341194
Toxicity to various agents 462.74 19.70 299 5703 480256 110103041
Accidental death 341.61 19.70 74 5928 4935 110578362
Drug hypersensitivity 252.39 19.70 203 5799 453887 110129410
Serotonin syndrome 101.85 19.70 54 5948 59099 110524198
Overdose 97.54 19.70 89 5913 233705 110349592
Clonus 55.39 19.70 20 5982 8696 110574601
Respiratory arrest 45.28 19.70 32 5970 58267 110525030
Drug abuse 42.13 19.70 50 5952 177361 110405936
Muscle rigidity 41.50 19.70 22 5980 24009 110559288
Hyperreflexia 39.52 19.70 16 5986 9469 110573828
Tarsal tunnel syndrome 36.78 19.70 8 5994 541 110582756
Cardio-respiratory arrest 36.74 19.70 38 5964 115798 110467499
Purpura senile 35.87 19.70 8 5994 607 110582690
Poisoning 34.95 19.70 21 5981 29084 110554213
Intentional overdose 30.87 19.70 37 5965 132464 110450833
Mydriasis 29.25 19.70 17 5985 22140 110561157
Resorption bone increased 28.61 19.70 8 5994 1526 110581771
Vestibular disorder 28.44 19.70 9 5993 2623 110580674
Suicidal behaviour 25.93 19.70 9 5993 3488 110579809
Vertigo positional 21.18 19.70 8 5994 3940 110579357
Unresponsive to stimuli 20.34 19.70 21 5981 63769 110519528

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
Spasticity indication 221360009
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Hemolytic anemia contraindication 61261009 DOID:583
Acute hepatic failure contraindication 197270009
Chronic Hepatic Disease contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.45 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
800MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** SKELAXIN KING PHARMS N013217 Aug. 30, 2002 DISCN TABLET ORAL 7122566 Feb. 6, 2026 TREATMENT OF MUSCULOSKELETAL CONDITIONS
640MG **Federal Register determination that product was not discontinued or withdrawn for safety or effectiveness reasons** METAXALONE PRIMUS PHARMS N022503 June 1, 2015 RX TABLET ORAL 12485111 May 14, 2043 METAXALONE IS INDICATED AS AN ADJUNCT TO REST, PHYSICAL THERAPY, AND OTHER MEASURES FOR THE RELIEF AND DISCOMFORT ASSOCIATED WITH ACUTE, PAINFUL MUSCULOSKELETAL CONDITIONS

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
4018807 VUID
N0000147110 NUI
D00773 KEGG_DRUG
4018807 VANDF
C0163055 UMLSCUI
CHEBI:6797 CHEBI
CHEMBL1079604 ChEMBL_ID
DB00660 DRUGBANK_ID
15459 PUBCHEM_CID
C011301 MESH_SUPPLEMENTAL_RECORD_UI
7609 IUPHAR_LIGAND_ID
1027 INN_ID
1NMA9J598Y UNII
204315 RXNORM
1680 MMSL
172287 MMSL
5062 MMSL
d00964 MMSL
001673 NDDF
404863006 SNOMEDCT_US
87599003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 0115-1745 TABLET 400 mg ORAL ANDA 25 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 0276-0508 TABLET 400 mg ORAL ANDA 20 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 0527-1435 TABLET 800 mg ORAL ANDA 25 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 0591-2341 TABLET 800 mg ORAL ANDA 24 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 0904-6831 TABLET 800 mg ORAL ANDA 26 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 10544-002 TABLET 800 mg ORAL NDA 20 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 10544-144 TABLET 800 mg ORAL ANDA 20 sections
SKELAXIN HUMAN PRESCRIPTION DRUG LABEL 1 10544-524 TABLET 800 mg ORAL NDA 20 sections
SKELAXIN HUMAN PRESCRIPTION DRUG LABEL 1 16590-207 TABLET 800 mg ORAL NDA 20 sections
METAXALONE HUMAN PRESCRIPTION DRUG LABEL 1 16590-346 TABLET 800 mg ORAL NDA 20 sections
Skelaxin HUMAN PRESCRIPTION DRUG LABEL 1 21695-123 TABLET 800 mg ORAL NDA 21 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 21695-585 TABLET 800 mg ORAL ANDA 19 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 33261-724 TABLET 800 mg ORAL ANDA 20 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 42254-040 TABLET 800 mg ORAL NDA 20 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 42291-985 TABLET 800 mg ORAL ANDA 25 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 42291-985 TABLET 800 mg ORAL ANDA 25 sections
METAXALONE HUMAN PRESCRIPTION DRUG LABEL 1 42549-650 TABLET 800 mg ORAL NDA 20 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 45865-161 TABLET 800 mg ORAL ANDA 17 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 45865-942 TABLET 800 mg ORAL ANDA 19 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 45865-985 TABLET 800 mg ORAL ANDA 20 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 50090-3174 TABLET 800 mg ORAL ANDA 20 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 50090-3650 TABLET 800 mg ORAL ANDA 26 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 50090-3670 TABLET 800 mg ORAL ANDA 19 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 50090-4448 TABLET 800 mg ORAL ANDA 21 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 50228-323 TABLET 800 mg ORAL ANDA 20 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 50228-323 TABLET 800 mg ORAL ANDA 20 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 50228-474 TABLET 400 mg ORAL ANDA 25 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 50268-530 TABLET 800 mg ORAL ANDA 20 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 50436-0449 TABLET 800 mg ORAL ANDA 19 sections
Metaxalone HUMAN PRESCRIPTION DRUG LABEL 1 51655-162 TABLET 800 mg ORAL ANDA 5 sections