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

Stem definitionDrug idCAS RN
953 309-29-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • doxapram hydrochloride hydrate
  • dopram
  • doxapram
  • doxapram hydrochloride
  • doxapram HCl
A central respiratory stimulant with a brief duration of action. (From Martindale, The Extra Pharmocopoeia, 30th ed, p1225)
  • Molecular weight: 378.52
  • Formula: C24H30N2O2
  • CLOGP: 3.04
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 32.78
  • ALOGS: -4.04
  • ROTB: 6
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.40 g P

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 10.57 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 64 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.20 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 5.30 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.10 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 25 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 2.125 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 1.517 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 34.834 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 31.769 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 44.720 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 57.370 % High 1
herg hERG pIC50 4.778 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 6.714 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 116.145 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 44.100 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK4,PRKDC,SIK3 17
kinase-selectivity-class AXL,FLT3,GRK2,MAPK7,PDK4,SIK2 6
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 1.644 High 1
mh-clint Mouse hepatocyte intrinsic clearance 86.896 High 1
mppb Mouse plasma protein binding (% unbound) 45.750 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 6.442 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pld-class Phospholipidosis risk class (1 = positive, 0 = negative) 1 High 1
pppb Pig plasma protein binding (% unbound) 66.410 % High 1
rh-clint Rat hepatocyte intrinsic clearance 155.239 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 83.110 % High 1
rppb Rat plasma protein binding (% unbound) 49.420 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 986.279 uM High 1

Approvals:

DateAgencyCompanyOrphan
June 23, 1965 FDA HIKMA MAPLE

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R07AB01 RESPIRATORY SYSTEM
OTHER RESPIRATORY SYSTEM PRODUCTS
OTHER RESPIRATORY SYSTEM PRODUCTS
Respiratory stimulants
FDA PE N0000009393 Increased Medullary Respiratory Drive
MeSH PA D000697 Central Nervous System Stimulants
MeSH PA D019141 Respiratory System Agents
FDA EPC N0000175716 Respiratory Stimulant
CHEBI has role CHEBI:35337 central nervous system stimulant
CHEBI has role CHEBI:35469 antidepressant

Related Drugs by ATC class:

R07AB Respiratory stimulants 8 drugs
almitrinebemegridedimeflineetamivanmepixanoxnikethamidepentetrazolprethcamide

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

DiseaseRelationSNOMED_IDDOID
Decreased respiratory function indication 80954004
Post-Anesthesia Respiratory Depression indication
Apnea in the newborn off-label use 13094009
Cerebral edema contraindication 2032001
Chronic obstructive lung disease contraindication 13645005 DOID:3083
Hyperthyroidism contraindication 34486009 DOID:7998
Pneumothorax contraindication 36118008
Artificial respiration contraindication 40617009
Paralysis contraindication 44695005
Conduction disorder of the heart contraindication 44808001
Low blood pressure contraindication 45007003
Fibrosis of lung contraindication 51615001 DOID:3770
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Neuromuscular block, function contraindication 55394004
Flail chest contraindication 78011002
Injury of head contraindication 82271004
Epilepsy contraindication 84757009 DOID:1826
Leukopenia contraindication 84828003 DOID:615
Kidney disease contraindication 90708001 DOID:557
Decompensated cardiac failure contraindication 195111005
Asthma contraindication 195967001 DOID:2841
Cerebrovascular accident contraindication 230690007
Pulmonary thromboembolism contraindication 233935004
Disease of liver contraindication 235856003 DOID:409
Pheochromocytoma contraindication 302835009
Hypertensive urgency contraindication 443482000
Acute exacerbation of asthma contraindication 708038006
Physical Obstruction of Respiratory Tract contraindication




🐶 Veterinary Drug Use

SpeciesUseRelation
Cats Stimulation of respiration during and after general anesthesia Indication
Cats Acceleration of awakening and return of reflexes after anesthesia Indication
Cats To initiate respiration following dystocia or caesarean section Indication
Cats Stimulation of respiration following dystocia or caesarean section Indication
Dogs Stimulation of respiration during and after general anesthesia Indication
Dogs Acceleration of awakening and return of reflexes after anesthesia Indication
Dogs To initiate respiration following dystocia or caesarean section Indication
Dogs Stimulation of respiration following dystocia or caesarean section Indication
Horses Stimulation of respiration during and after general anesthesia Indication
Horses Acceleration of awakening and return of reflexes after anesthesia Indication

🐶 Veterinary products

ProductApplicantIngredients
Dopram-V Injectable Boehringer lngelheim Animal Health USA Inc. 1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.03 Basic

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
Potassium channel subfamily K member 3 Ion channel BLOCKER CHEMBL CHEMBL
Potassium channel subfamily K member 9 Ion channel BLOCKER CHEMBL CHEMBL
Cytochrome P450 2D6 Enzyme IC50 7 DRUG MATRIX
Potassium channel subfamily K member 3 Ion channel IC50 6.39 CHEMBL
Potassium channel subfamily K member 9 Ion channel IC50 4.80 CHEMBL

External reference:

IDSource
D07873 KEGG_DRUG
7081-53-0 SECONDARY_CAS_RN
4018416 VANDF
4019734 VANDF
C0013084 UMLSCUI
CHEBI:681848 CHEBI
CHEMBL1754 ChEMBL_ID
CHEMBL3989519 ChEMBL_ID
DB00561 DRUGBANK_ID
D004315 MESH_DESCRIPTOR_UI
3156 PUBCHEM_CID
7169 IUPHAR_LIGAND_ID
1462 INN_ID
94F3830Q73 UNII
202987 RXNORM
3192 MMSL
332 MMSL
4636 MMSL
d00802 MMSL
001383 NDDF
004577 NDDF
28235004 SNOMEDCT_US
373339005 SNOMEDCT_US
84748003 SNOMEDCT_US
94F3830Q73 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Dopram HUMAN PRESCRIPTION DRUG LABEL 1 0641-6018 INJECTION 20 mg INTRAVENOUS NDA 20 sections
DOXAPRAM HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 51662-1404 INJECTION 20 mg INTRAVENOUS NDA 12 sections