carbachol indications/contra

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

Drug dosage:

DoseUnitRoute
6 mg O
0.50 mg P
0.40 ml None

Approvals:

DateAgencyCompanyOrphan
Sept. 28, 1972 FDA ALCON

FDA Adverse Event Reporting System

None

Pharmacologic Action:

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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:47958 nicotinic acetylcholine receptor agonist
CHEBI has role CHEBI:38325 muscarinic agonist
CHEBI has role CHEBI:38147 cardiotonic drug
CHEBI has role CHEBI:51068 miotic
CHEBI has role CHEBI:35481 non-narcotic analgesic
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
MeSH PA D001337 Autonomic Agents
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 (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Open-angle glaucoma indication 84494001 DOID:1067
Urinary tract obstruction contraindication 7163005 DOID:5200
Peptic ulcer contraindication 13200003 DOID:750
Abdominal pain contraindication 21522001
Parkinsonism contraindication 32798002 DOID:13548
Hyperthyroidism contraindication 34486009 DOID:7998
Low blood pressure contraindication 45007003
Bradycardia contraindication 48867003
Heart failure contraindication 84114007 DOID:6000
Asthma contraindication 195967001 DOID:2841
Secondary glaucoma off-label use 95717004
Angle-closure glaucoma off-label use 392291006 DOID:13550

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:

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

External reference:

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IDSource
CHEBI:3385 CHEBI
DB00411 DRUGBANK_ID
298 IUPHAR_LIGAND_ID
4018583 VUID
N0000146899 NUI
C0006945 UMLSCUI
D00524 KEGG_DRUG
CHEMBL14 ChEMBL_ID
CHEMBL965 ChEMBL_ID
4018583 VANDF
N0000146899 NDFRT
N0000007437 NDFRT
1999 RXNORM
33675006 SNOMEDCT_US
387183001 SNOMEDCT_US
4349 MMSL
001690 NDDF
8Y164V895Y UNII
383 INN_ID
D002217 MESH_DESCRIPTOR_UI
5831 PUBCHEM_CID
CCE PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
MIOSTAT HUMAN PRESCRIPTION DRUG LABEL 1 0065-0023 SOLUTION 0.10 mg OPHTHALMIC NDA 12 sections