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

Stem definitionDrug idCAS RN
127 27469-53-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • almitrine
  • almitrine mesylate
  • almitrine mesilate
  • duxil
  • almitrine dimesilate
  • almitrine dimesylate
A respiratory stimulant that enhances respiration by acting as an agonist of peripheral chemoreceptors located on the carotid bodies. The drug increases arterial oxygen tension while decreasing arterial carbon dioxide tension in patients with chronic obstructive pulmonary disease. It may also prove useful in the treatment of nocturnal oxygen desaturation without impairing the quality of sleep.
  • Molecular weight: 477.56
  • Formula: C26H29F2N7
  • CLOGP: 6.59
  • LIPINSKI: 1
  • HAC: 7
  • HDO: 2
  • TPSA: 69.21
  • ALOGS: -4.52
  • ROTB: 10

Drug dosage:

DoseUnitRoute
0.10 g O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 63 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 35.37 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.97 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1344 hours Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AURKB,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK16,CDK19,CDK2,CDK5,CDK7,CDK9,CHEK1,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FLT3,GRK1,GRK2,GSK3B,INSR,ITK,JAK1,JAK2,JAK3,KIT,MAP3K1,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ZAP70 76
kinase-selectivity-class AXL,GRK2,TEK 3
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

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
Lichenoid keratosis 82.28 75.80 10 6 3940 42617379

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
Lichenoid keratosis 87.14 73.60 10 6 6292 110582991

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R07AB07 RESPIRATORY SYSTEM
OTHER RESPIRATORY SYSTEM PRODUCTS
OTHER RESPIRATORY SYSTEM PRODUCTS
Respiratory stimulants
MeSH PA D002491 Central Nervous System Agents
MeSH PA D018696 Neuroprotective Agents
MeSH PA D020011 Protective Agents
MeSH PA D019141 Respiratory System Agents
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:35337 central nervous system stimulant

Related Drugs by ATC class:

R07AB Respiratory stimulants 8 drugs

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

DiseaseRelationSNOMED_IDDOID
Chronic obstructive lung disease indication 13645005 DOID:3083




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.0 Basic
pKa2 5.57 Basic
pKa3 3.77 Basic
pKa4 1.34 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
N0000167166 NUI
D02822 KEGG_DRUG
528 RXNORM
C0002164 UMLSCUI
CHEBI:53778 CHEBI
CHEMBL1183717 ChEMBL_ID
CHEMBL3181957 ChEMBL_ID
D015765 MESH_DESCRIPTOR_UI
DB01430 DRUGBANK_ID
4123 INN_ID
29608-49-9 SECONDARY_CAS_RN
9A1222NBG4 UNII
33887 PUBCHEM_CID
C037558 MESH_SUPPLEMENTAL_RECORD_UI
003689 NDDF
003690 NDDF
418600009 SNOMEDCT_US
734458006 SNOMEDCT_US

Pharmaceutical products:

None