dantrolene 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
780 7261-97-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dantrolene
  • dantrolene sodium
  • dantrium
  • dantrolene sodium salt
Skeletal muscle relaxant that acts by interfering with excitation-contraction coupling in the muscle fiber. It is used in spasticity and other neuromuscular abnormalities. Although the mechanism of action is probably not central, dantrolene is usually grouped with the central muscle relaxants.
  • Molecular weight: 314.26
  • Formula: C14H10N4O5
  • CLOGP: 1.63
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 1
  • TPSA: 120.73
  • ALOGS: -3.59
  • ROTB: 4
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.10 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 2 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 5 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 21.22 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 70 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.37 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.43 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 10 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 15, 1974 FDA PAR STERILE PRODUCTS

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
Neuroleptic malignant syndrome 65.34 25.96 19 1186 12037 63475780
Choluria 38.04 25.96 6 1199 200 63487617
Rhabdomyolysis 32.19 25.96 16 1189 43935 63443882
Respiratory failure 26.48 25.96 19 1186 101839 63385978

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
Neuroleptic malignant syndrome 169.09 24.83 54 1691 17880 34937306
Hyperthermia 60.72 24.83 22 1723 10555 34944631
Muscle rigidity 42.72 24.83 17 1728 10501 34944685
Disseminated intravascular coagulation 36.51 24.83 19 1726 21797 34933389
Respiratory failure 34.09 24.83 34 1711 108538 34846648
Seizure 26.05 24.83 29 1716 104828 34850358
Tachycardia 25.57 24.83 26 1719 84746 34870440

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
Neuroleptic malignant syndrome 221.23 21.25 67 2628 27492 79714201
Hyperthermia 79.91 21.25 28 2667 18009 79723684
Respiratory failure 59.44 21.25 49 2646 180862 79560831
Seizure 40.01 21.25 40 2655 188794 79552899
Disseminated intravascular coagulation 37.36 21.25 20 2675 35822 79705871
Muscle rigidity 35.44 21.25 16 2679 19866 79721827
Rhabdomyolysis 31.87 21.25 27 2668 103104 79638589
Hyperthermia malignant 27.28 21.25 8 2687 2909 79738784
Multiple sclerosis relapse 25.09 21.25 17 2678 46516 79695177
Choluria 24.51 21.25 5 2690 401 79741292
Malignant catatonia 23.83 21.25 5 2690 460 79741233
Autonomic nervous system imbalance 23.64 21.25 8 2687 4622 79737071

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC M03CA01 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, DIRECTLY ACTING AGENTS
Dantrolene and derivatives
FDA PE N0000008953 Decreased Striated Muscle Contraction
CHEBI has role CHEBI:51371 muscle relaxants
CHEBI has role CHEBI:63726 neuroprotective agents
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 N0000175735 Decreased Striated Muscle Tone
FDA EPC N0000175738 Skeletal Muscle Relaxant

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Spasticity indication 221360009
Malignant hyperthermia indication 405501007
Muscle spasticity of spinal origin indication 416830008
Malignant Hyperthermia Prevention indication
Muscle Spasticity of Cerebral Origin indication
Neuroleptic malignant syndrome off-label use 15244003 DOID:14464
Duchenne muscular dystrophy off-label use 76670001 DOID:11723
Glycogen Storage Disease Type V with Muscle Pain off-label use
Disorder of lung contraindication 19829001 DOID:850
Acute hepatitis contraindication 37871000
Disorder of muscle contraindication 129565002 DOID:423
Disease of liver contraindication 235856003 DOID:409
Severe Cardiac Disease contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.28 acidic
pKa2 0.0 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
250MG/VIAL RYANODEX EAGLE PHARMS N205579 July 22, 2014 RX FOR SUSPENSION INTRAVENOUS 8685460 Feb. 15, 2023 FOR USE IN THE TREATMENT OF MALIGNANT HYPERTHERMIA IN CONJUNCTION WITH APPROPRIATE SUPPORTIVE MEASURES AND FOR THE PREVENTION OF MALIGNANT HYPERTHERMIA IN PATIENTS AT HIGH RISK.

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Ryanodine receptor 1 Ion channel ANTAGONIST Ki 6.76 WOMBAT-PK CHEMBL
Ryanodine receptor 3 Ion channel ANTAGONIST CHEMBL CHEMBL
CDGSH iron-sulfur domain-containing protein 1 Unclassified Ki 5.68 CHEMBL

External reference:

IDSource
4019703 VUID
N0000147795 NUI
D02347 KEGG_DRUG
24868-20-0 SECONDARY_CAS_RN
3104 RXNORM
4018876 VANDF
4019703 VANDF
C0010976 UMLSCUI
CHEBI:4317 CHEBI
CHEMBL1201288 ChEMBL_ID
DB01219 DRUGBANK_ID
CHEMBL928 ChEMBL_ID
D003620 MESH_DESCRIPTOR_UI
6914273 PUBCHEM_CID
4172 IUPHAR_LIGAND_ID
2317 INN_ID
F64QU97QCR UNII
4534 MMSL
629 MMSL
66073 MMSL
d00968 MMSL
001675 NDDF
004679 NDDF
372819007 SNOMEDCT_US
69107004 SNOMEDCT_US
81946009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0115-4411 CAPSULE 25 mg ORAL ANDA 24 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0115-4411 CAPSULE 25 mg ORAL ANDA 24 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0115-4422 CAPSULE 50 mg ORAL ANDA 24 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0115-4422 CAPSULE 50 mg ORAL ANDA 24 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0115-4433 CAPSULE 100 mg ORAL ANDA 24 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0115-4433 CAPSULE 100 mg ORAL ANDA 24 sections
Dantrolene HUMAN PRESCRIPTION DRUG LABEL 1 0143-9297 INJECTION, POWDER, FOR SOLUTION 20 mg INTRAVENOUS ANDA 17 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-3219 CAPSULE 25 mg ORAL ANDA 24 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-3220 CAPSULE 25 mg ORAL ANDA 24 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-3221 CAPSULE 25 mg ORAL ANDA 24 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0904-7211 CAPSULE 25 mg ORAL ANDA 24 sections
Revonto HUMAN PRESCRIPTION DRUG LABEL 1 27505-003 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 20 mg INTRAVENOUS ANDA 22 sections
Dantrium HUMAN PRESCRIPTION DRUG LABEL 1 42023-123 INJECTION 20 mg INTRAVENOUS NDA 22 sections
Dantrium HUMAN PRESCRIPTION DRUG LABEL 1 42023-124 CAPSULE 25 mg ORAL NDA 24 sections
Dantrium HUMAN PRESCRIPTION DRUG LABEL 1 42023-125 CAPSULE 50 mg ORAL NDA 24 sections
Dantrium HUMAN PRESCRIPTION DRUG LABEL 1 42023-126 CAPSULE 100 mg ORAL NDA 24 sections
RYANODEX dantrolene sodium HUMAN PRESCRIPTION DRUG LABEL 1 42367-540 INJECTION, SUSPENSION 250 mg INTRAVENOUS NDA 24 sections
dantrolene sodium HUMAN PRESCRIPTION DRUG LABEL 1 49884-362 CAPSULE 25 mg ORAL NDA AUTHORIZED GENERIC 23 sections
dantrolene sodium HUMAN PRESCRIPTION DRUG LABEL 1 49884-363 CAPSULE 50 mg ORAL NDA AUTHORIZED GENERIC 23 sections
dantrolene sodium HUMAN PRESCRIPTION DRUG LABEL 1 49884-364 CAPSULE 100 mg ORAL NDA AUTHORIZED GENERIC 23 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 50268-217 CAPSULE 25 mg ORAL ANDA 24 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 50268-217 CAPSULE 25 mg ORAL ANDA 24 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 55154-7140 CAPSULE 25 mg ORAL ANDA 24 sections
Dantrolene Sodium HUMAN PRESCRIPTION DRUG LABEL 1 55154-7140 CAPSULE 25 mg ORAL ANDA 24 sections
dantrolene sodium HUMAN PRESCRIPTION DRUG LABEL 1 63629-2168 CAPSULE 25 mg ORAL NDA AUTHORIZED GENERIC 22 sections
dantrolene sodium HUMAN PRESCRIPTION DRUG LABEL 1 63629-2168 CAPSULE 25 mg ORAL NDA AUTHORIZED GENERIC 22 sections
dantrolene sodium HUMAN PRESCRIPTION DRUG LABEL 1 63629-2168 CAPSULE 25 mg ORAL NDA AUTHORIZED GENERIC 22 sections
dantrolene sodium HUMAN PRESCRIPTION DRUG LABEL 1 63629-2169 CAPSULE 50 mg ORAL NDA AUTHORIZED GENERIC 22 sections
dantrolene sodium HUMAN PRESCRIPTION DRUG LABEL 1 63629-2169 CAPSULE 50 mg ORAL NDA AUTHORIZED GENERIC 22 sections
dantrolene sodium HUMAN PRESCRIPTION DRUG LABEL 1 63629-2169 CAPSULE 50 mg ORAL NDA AUTHORIZED GENERIC 22 sections