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

Stem definitionDrug idCAS RN
488 51-83-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • carbachol
  • carbastat
  • carboptic
  • isopto carbachol
  • miostat
A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.
  • Molecular weight: 147.20
  • Formula: C6H15N2O2
  • CLOGP: -4.32
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 52.32
  • ALOGS: -2.41
  • ROTB: 4

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
6 mg O
0.50 mg P
0.40 ml None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 28, 1972 FDA ALCON

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 N07AB01 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
PARASYMPATHOMIMETICS
Choline esters
ATC S01EB02 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Parasympathomimetics
CHEBI has role CHEBI:38147 cardiotonic drugs
CHEBI has role CHEBI:38325 muscarinic agonists
CHEBI has role CHEBI:51068 Miotico
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
MeSH PA D002316 Cardiotonic Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D018678 Cholinergic Agents
MeSH PA D018679 Cholinergic Agonists
MeSH PA D008916 Miotics
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D020011 Protective Agents
MeSH PA D018689 Sensory System Agents

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

DiseaseRelationSNOMED_IDDOID
Open-angle glaucoma indication 84494001 DOID:1067
Secondary glaucoma off-label use 95717004
Angle-closure glaucoma off-label use 392291006 DOID:13550
Urinary tract obstruction contraindication 7163005 DOID:5200
Peptic ulcer contraindication 13200003 DOID:750
Abdominal pain contraindication 21522001
Parkinsonism contraindication 32798002
Hyperthyroidism contraindication 34486009 DOID:7998
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Heart failure contraindication 84114007 DOID:6000
Asthma contraindication 195967001 DOID:2841




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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
Muscarinic acetylcholine receptor M3 GPCR AGONIST EC50 8.70 WOMBAT-PK CHEMBL
Muscarinic acetylcholine receptor M2 GPCR EC50 7.92 WOMBAT-PK
Muscarinic acetylcholine receptor M4 GPCR EC50 7.58 WOMBAT-PK
Muscarinic acetylcholine receptor M5 GPCR EC50 8.10 WOMBAT-PK
Neuronal acetylcholine receptor subunit alpha-7 Ion channel Ki 4.18 CHEMBL
Neuronal acetylcholine receptor; alpha4/beta2 Ion channel Ki 6.12 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR EC50 8.52 WOMBAT-PK
Muscarinic acetylcholine receptor M2 GPCR Ki 8.40 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 7.51 CHEMBL
Acetylcholine receptor subunit delta Ion channel Ki 6.35 CHEMBL
Acetylcholinesterase Enzyme Ki 8.10 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 7.70 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 8.10 CHEMBL
Muscarinic acetylcholine receptor M4 GPCR Ki 5.59 CHEMBL
Muscarinic acetylcholine receptor GPCR Kd 4.74 CHEMBL
Acetylcholine receptor subunit alpha Ion channel IC50 5.12 CHEMBL
Neuronal acetylcholine receptor; alpha2/beta2 Ion channel Ki 6.68 CHEMBL
Neuronal acetylcholine receptor; alpha3/beta2 Ion channel Ki 5.96 CHEMBL
Neuronal acetylcholine receptor; alpha3/beta4 Ion channel Ki 5.32 CHEMBL
Neuronal acetylcholine receptor; alpha4/beta2 Ion channel Ki 6.23 CHEMBL
Neuronal acetylcholine receptor; alpha4/beta4 Ion channel Ki 5.89 CHEMBL
Muscarinic acetylcholine receptor GPCR Ki 8.89 CHEMBL

External reference:

IDSource
4018583 VUID
N0000146899 NUI
D00524 KEGG_DRUG
1999 RXNORM
C0006945 UMLSCUI
CHEBI:3385 CHEBI
CHEMBL965 ChEMBL_ID
CHEMBL14 ChEMBL_ID
D002217 MESH_DESCRIPTOR_UI
5831 PUBCHEM_CID
383 INN_ID
298 IUPHAR_LIGAND_ID
8Y164V895Y UNII
1101 MMSL
1253 MMSL
177672 MMSL
4349 MMSL
4801 MMSL
33675006 SNOMEDCT_US
387183001 SNOMEDCT_US
CCE PDB_CHEM_ID
DB00411 DRUGBANK_ID
4018583 VANDF
001690 NDDF

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
MIOSTAT HUMAN PRESCRIPTION DRUG LABEL 1 0065-0023 SOLUTION 0.10 mg OPHTHALMIC NDA 15 sections
MIOSTAT HUMAN PRESCRIPTION DRUG LABEL 1 0065-0023 SOLUTION 0.10 mg OPHTHALMIC NDA 15 sections
MIOSTAT HUMAN PRESCRIPTION DRUG LABEL 1 0065-0023 SOLUTION 0.10 mg OPHTHALMIC NDA 15 sections