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

Stem definitionDrug idCAS RN
4667 151-73-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • betamethasone phosphate
  • betamethasone sodium phosphate
  • betamethasone disodium phosphate
  • betnesol
  • durabetason
phosphate ester of betamethasone; RN given refers to the di-Na salt (11beta,16beta)-isomer; structure in Negwer,5th ed, 4975
  • Molecular weight: 472.45
  • Formula: C22H30FO8P
  • CLOGP: 0.32
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 4
  • TPSA: 141.36
  • ALOGS: -2.21
  • ROTB: 4
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
S (Water solubility) 0.06 mg/mL Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,JAK3,KDR,MAP2K6,MAP3K14,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PIK3CG,PIM2,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,ZAP70 45
kinase-selectivity-class AXL,CDK4,CDK9,GRK2,MAP2K6,SYK,TEK,ZAP70 8
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 0.296 Moderate 0.78
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 0 Moderate 0.78
rat-kpuu-brain Rat brain Kpuu 0.002 % Moderate 0.78

Approvals:

DateAgencyCompanyOrphan
March 3, 1965 FDA MERCK SHARP DOHME

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
Erythema 71.64 24.37 58 2735 229188 90396466
Macular degeneration 59.04 24.37 27 2766 37943 90587711
Libido increased 42.33 24.37 10 2783 1734 90623920
Face oedema 40.75 24.37 18 2775 23300 90602354
Soft tissue injury 40.52 24.37 10 2783 2082 90623572
Hostility 39.70 24.37 10 2783 2263 90623391
Post-traumatic neck syndrome 38.70 24.37 10 2783 2504 90623150
Sternal fracture 37.33 24.37 10 2783 2877 90622777
Vaginal flatulence 33.02 24.37 13 2780 12625 90613029
Paraesthesia oral 32.61 24.37 17 2776 31642 90594012
Female genital tract fistula 31.88 24.37 14 2779 17854 90607800
Radiculopathy 31.41 24.37 14 2779 18491 90607163
Chronic sinusitis 31.04 24.37 15 2778 23787 90601867
Throat tightness 30.84 24.37 16 2777 29468 90596186
Proctitis 30.65 24.37 13 2780 15246 90610408
Pharyngeal oedema 28.55 24.37 12 2781 13759 90611895
Vaginal discharge 27.62 24.37 13 2780 19451 90606203
Colitis 24.56 24.37 19 2774 69923 90555731

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
Enamel anomaly 40.68 23.22 7 1362 234 42619732
Tooth hypoplasia 40.15 23.22 7 1362 253 42619713
Sopor 31.98 23.22 13 1356 13189 42606777
Mucormycosis 24.28 23.22 9 1360 7134 42612832
Intentional self-injury 23.79 23.22 11 1358 15191 42604775

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
Erythema 69.68 22.19 69 4064 291378 110293788
Paraesthesia oral 48.08 22.19 24 4109 33647 110551519
Face oedema 42.38 22.19 22 4111 33447 110551719
Enamel anomaly 39.52 22.19 7 4126 237 110584929
Soft tissue injury 37.77 22.19 10 4123 2266 110582900
Tooth hypoplasia 36.86 22.19 7 4126 350 110584816
Libido increased 36.68 22.19 10 4123 2529 110582637
Post-traumatic neck syndrome 36.47 22.19 10 4123 2585 110582581
Hostility 36.09 22.19 10 4123 2686 110582480
Sternal fracture 34.04 22.19 10 4123 3306 110581860
Vaginal flatulence 31.09 22.19 13 4120 12131 110573035
Pharyngeal oedema 30.41 22.19 14 4119 16414 110568752
Female genital tract fistula 30.34 22.19 14 4119 16505 110568661
Sopor 29.82 22.19 18 4115 36528 110548638
Radiculopathy 28.24 22.19 14 4119 19322 110565844
Chronic sinusitis 27.55 22.19 15 4118 25069 110560097
Proctitis 26.95 22.19 13 4120 16914 110568252
Macular degeneration 26.74 22.19 14 4119 21645 110563521
Vaginal discharge 26.25 22.19 13 4120 17895 110567271
Throat tightness 26.05 22.19 16 4117 33473 110551693

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
FDA MoA N0000175450 Corticosteroid Hormone Receptor Agonists
FDA EPC N0000175576 Corticosteroid
CHEBI has role CHEBI:35472 anti-inflammatory drug
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35705 immunosuppressive agent
CHEBI has role CHEBI:35845 gout suppressant
CHEBI has role CHEBI:39456 antiglaucoma drug
CHEBI has role CHEBI:49201 anti-ulcer drug
CHEBI has role CHEBI:50177 dermatologic drug
CHEBI has role CHEBI:50748 antipsoriatic
CHEBI has role CHEBI:51177 antitussive
CHEBI has role CHEBI:65023 anti-asthmatic agent
CHEBI has role CHEBI:66981 ophthalmology drug
CHEBI has role CHEBI:77715 nasal decongestant
CHEBI has role CHEBI:67079 anti-inflammatory agent
MeSH PA D005938 Glucocorticoids
MeSH PA D006728 Hormones
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D018927 Anti-Asthmatic Agents
MeSH PA D019141 Respiratory System Agents

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

None




🐶 Veterinary Drug Use

SpeciesUseRelation
Cats Pruritus associated with dermatoses Indication
Dogs Pruritus associated with dermatoses Indication
Horses Inflammatory joint conditions Indication

🐶 Veterinary products

ProductApplicantIngredients
Betavet Soluspan Suspension Intervet Inc. 2
Betasone Aqueous Suspension Intervet Inc. 2
BetaVet American Regent Inc. 2

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 1.75 acidic
pKa2 6.8 acidic
pKa3 11.06 acidic
pKa4 13.94 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Glucocorticoid receptor Nuclear hormone receptor AGONIST Ki 8.43 DRUG MATRIX CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 5.78 DRUG MATRIX
Muscarinic acetylcholine receptor M3 GPCR Ki 5.87 DRUG MATRIX
Histamine H1 receptor GPCR Ki 5.93 DRUG MATRIX
Muscarinic acetylcholine receptor M5 GPCR Ki 5.25 DRUG MATRIX
Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 Enzyme Kd 5.66 CHEMBL
Muscarinic acetylcholine receptor M4 GPCR Ki 5.78 DRUG MATRIX

External reference:

IDSource
D00972 KEGG_DRUG
4018646 VUID
N0000179655 NUI
360-63-4 SECONDARY_CAS_RN
4018644 VANDF
4018646 VANDF
CHEMBL1201207 ChEMBL_ID
CHEMBL1200762 ChEMBL_ID
DB14669 DRUGBANK_ID
YJO1F9W10R UNII
DB00443 DRUGBANK_ID
1514 RXNORM
10006 MMSL
3292 MMSL
33290 MMSL
4270 MMSL
4277 MMSL
d00628 MMSL
002168 NDDF
002172 NDDF
116571008 SNOMEDCT_US
116573006 SNOMEDCT_US
29896003 SNOMEDCT_US
C2698382 UMLSCUI
C0005308 UMLSCUI
65478 PUBCHEM_CID
9782 PUBCHEM_CID
1045 INN_ID
C028994 MESH_SUPPLEMENTAL_RECORD_UI
D001623 MESH_DESCRIPTOR_UI
CHEBI:3077 CHEBI
YJO1F9W10R INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Betamethasone Sodium Phosphate and Betamethasone Acetate HUMAN PRESCRIPTION DRUG LABEL 2 0517-0720 INJECTION, SUSPENSION 3 mg INTRA-ARTICULAR ANDA 21 sections
Betamethasone Sodium Phosphate and Betamethasone Acetate HUMAN PRESCRIPTION DRUG LABEL 2 0517-0791 INJECTION, SUSPENSION 3 mg INTRA-ARTICULAR ANDA 21 sections
Betamethasone Sodium Phosphate and Betamethasone Acetate HUMAN PRESCRIPTION DRUG LABEL 2 0517-0799 INJECTION, SUSPENSION 3 mg INTRA-ARTICULAR ANDA 21 sections
Betamethasone Sodium Phosphate and Betamethasone Acetate HUMAN PRESCRIPTION DRUG LABEL 2 76420-007 INJECTION, SUSPENSION 3 mg INTRA-ARTICULAR ANDA 21 sections
Betaloan SUIK HUMAN PRESCRIPTION DRUG LABEL 2 76420-240 INJECTION, SUSPENSION 3 mg INTRA-ARTICULAR unapproved drug other 21 sections
CELESTONE SOLUSPAN HUMAN PRESCRIPTION DRUG LABEL 2 78206-118 INJECTION, SUSPENSION 3 mg INTRAMUSCULAR NDA 22 sections
Betaloan SUIK HUMAN PRESCRIPTION DRUG LABEL 2 80425-0347 INJECTION, SUSPENSION 3 mg INTRA-ARTICULAR unapproved drug other 21 sections
CELESTONE SOLUSPAN HUMAN PRESCRIPTION DRUG LABEL 2 85766-070 INJECTION, SUSPENSION 3 mg INTRAMUSCULAR NDA 22 sections