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methacholine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1726 | 55-92-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A quaternary ammonium parasympathomimetic agent with the muscarinic actions of ACETYLCHOLINE. It is hydrolyzed by ACETYLCHOLINESTERASE at a considerably slower rate than ACETYLCHOLINE and is more resistant to hydrolysis by nonspecific CHOLINESTERASES so that its actions are more prolonged. It is used as a parasympathomimetic bronchoconstrictor agent and as a diagnostic aid for bronchial asthma. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1116)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,JAK2,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1 | 54 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,CAMK2D,CDK4,GRK2,MAPK7 | 7 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 31, 1986 | FDA | METHAPHARM |
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:
| Source | Code | Description |
|---|---|---|
| ATC | V04CX03 | VARIOUS DIAGNOSTIC AGENTS OTHER DIAGNOSTIC AGENTS Other diagnostic agents |
| FDA MoA | N0000175369 | Cholinergic Agonists |
| CHEBI has role | CHEBI:35620 | vasodilator agent |
| CHEBI has role | CHEBI:38324 | cholinergic agonist |
| CHEBI has role | CHEBI:38325 | muscarinic agonist |
| CHEBI has role | CHEBI:50141 | bronchoconstrictor agent |
| CHEBI has role | CHEBI:53000 | epitope |
| CHEBI has role | CHEBI:65023 | anti-asthmatic agent |
| MeSH PA | D008916 | Miotics |
| MeSH PA | D010277 | Parasympathomimetics |
| MeSH PA | D016085 | Bronchoconstrictor Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D018679 | Cholinergic Agonists |
| MeSH PA | D018721 | Muscarinic Agonists |
| MeSH PA | D019141 | Respiratory System Agents |
| FDA EPC | N0000175884 | Cholinergic Receptor Agonist |
Related Drugs by ATC class:
V04CX Other diagnostic agents 9 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Diagnostic Test for Asthma | indication | ||
| Gastritis | contraindication | 4556007 | DOID:4029 |
| Urinary tract obstruction | contraindication | 7163005 | DOID:5200 |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Disorder of thyroid gland | contraindication | 14304000 | DOID:50 |
| Increased gastric tonus | contraindication | 18644006 | |
| Gastrointestinal ulcer | contraindication | 40845000 | |
| Body fluid retention | contraindication | 43498006 | |
| Bradycardia | contraindication | 48867003 | |
| Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
| Vitamin K deficiency | contraindication | 52675005 | DOID:11249 |
| Nasal polyp | contraindication | 52756005 | |
| Hepatic failure | contraindication | 59927004 | |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Factor II deficiency | contraindication | 73975000 | |
| Gastrointestinal hemorrhage | contraindication | 74474003 | |
| Thrombotic thrombocytopenic purpura | contraindication | 78129009 | DOID:10772 |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Thyrotoxicosis | contraindication | 90739004 | DOID:7997 |
| Hemophilia | contraindication | 90935002 | |
| Anemia due to enzyme deficiency | contraindication | 111577008 | |
| Gastroesophageal reflux disease | contraindication | 235595009 | DOID:8534 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Pregnancy, function | contraindication | 289908002 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Breastfeeding (mother) | contraindication | 413712001 |
🐶 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M3 | GPCR | AGONIST | CHEMBL | CHEMBL | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 7.23 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 5.80 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 7.64 | PDSP | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 7.23 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | AGONIST | EC50 | 6.40 | IUPHAR | ||||
| Muscarinic acetylcholine receptor M3 | GPCR | AGONIST | EC50 | 6.92 | IUPHAR | ||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 5.80 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4020262 | VUID |
| N0000148153 | NUI |
| D04970 | KEGG_DRUG |
| 62-51-1 | SECONDARY_CAS_RN |
| 4020262 | VANDF |
| 4020540 | VANDF |
| C0600370 | UMLSCUI |
| CHEBI:6804 | CHEBI |
| CHEMBL978 | ChEMBL_ID |
| DB06709 | DRUGBANK_ID |
| CHEMBL1200764 | ChEMBL_ID |
| D016210 | MESH_DESCRIPTOR_UI |
| 1993 | PUBCHEM_CID |
| 7438 | IUPHAR_LIGAND_ID |
| 03V657ZD3V | UNII |
| 155080 | RXNORM |
| 5064 | MMSL |
| 72376 | MMSL |
| d03667 | MMSL |
| 001688 | NDDF |
| 001689 | NDDF |
| 109196007 | SNOMEDCT_US |
| 372766003 | SNOMEDCT_US |
| 53584007 | SNOMEDCT_US |
| 3161 | INN_ID |
| 03V657ZD3V | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Provocholine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64281-100 | POWDER, FOR SOLUTION | 100 mg | RESPIRATORY (INHALATION) | NDA | 24 sections |
| Provocholine Inhalation Solution | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64281-116 | SOLUTION | 48 mg | RESPIRATORY (INHALATION) | NDA | 24 sections |