pilocarpine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tricyclic compounds | 2166 | 92-13-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 15 | mg | O |
| 10 | mg | P |
| 0.40 | ml | None |
| 40 | mg | ointment |
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 29, 1974 | FDA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Limb injury | 70.28 | 50.00 | 13 | 140 | 2497 | 2355435 |
| Wound | 69.20 | 50.00 | 13 | 140 | 2715 | 2355217 |
| Intraocular pressure increased | 63.15 | 50.00 | 11 | 142 | 1498 | 2356434 |
| Asthma | 60.83 | 50.00 | 15 | 138 | 11299 | 2346633 |
| Transient ischaemic attack | 59.03 | 50.00 | 13 | 140 | 5965 | 2351967 |
| Haemorrhage | 56.11 | 50.00 | 14 | 139 | 11025 | 2346907 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Intraocular pressure increased | 121.27 | 94.28 | 18 | 60 | 1163 | 1745540 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N07AX01 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS PARASYMPATHOMIMETICS Other parasympathomimetics |
| ATC | S01EB01 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Parasympathomimetics |
| ATC | S01EB51 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Parasympathomimetics |
| FDA MoA | N0000000104 | Cholinergic Muscarinic Agonists |
| FDA EPC | N0000175884 | Cholinergic Receptor Agonist |
| CHEBI has role | CHEBI:39456 | antiglaucoma drug |
| MeSH PA | D018678 | Cholinergic Agents |
| MeSH PA | D018679 | Cholinergic Agonists |
| MeSH PA | D008916 | Miotics |
| MeSH PA | D018721 | Muscarinic Agonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ocular hypertension | indication | 4210003 | DOID:9282 |
| Open-angle glaucoma | indication | 84494001 | DOID:1067 |
| Aptyalism | indication | 87715008 | |
| Xerostomia Secondary to Sjogren's Syndrome | indication | ||
| Primary Closed Angle Glaucoma | indication | ||
| Xerostomia Secondary to Radiation Therapy | indication | ||
| Bronchospasm | contraindication | 4386001 | |
| Keratitis | contraindication | 5888003 | DOID:4677 |
| Chronic obstructive lung disease | contraindication | 13645005 | DOID:3083 |
| Retinal detachment | contraindication | 42059000 | DOID:5327 |
| Hepatic failure | contraindication | 59927004 | |
| Iritis | contraindication | 65074000 | DOID:1406 |
| Cholecystitis | contraindication | 76581006 | DOID:1949 |
| Kidney stone | contraindication | 95570007 | |
| Disorder of biliary tract | contraindication | 105997008 | DOID:9741 |
| Acute disease of cardiovascular system | contraindication | 128487001 | |
| Calculus in biliary tract | contraindication | 266474003 | |
| Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
| Anterior uveitis | contraindication | 410692006 | DOID:1407 |
| Acute exacerbation of asthma | contraindication | 708038006 | |
| Psychiatric Disturbance | contraindication | ||
| Pupillary Block Glaucoma | contraindication |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.04 | Basic |
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 | EC50 | 6.97 | SCIENTIFIC LITERATURE | IUPHAR | |||
| Muscarinic acetylcholine receptor M2 | GPCR | AGONIST | EC50 | 6.95 | SCIENTIFIC LITERATURE | ||||
| Muscarinic acetylcholine receptor M4 | GPCR | AGONIST | EC50 | 7.15 | SCIENTIFIC LITERATURE | ||||
| Muscarinic acetylcholine receptor M5 | GPCR | AGONIST | EC50 | 7 | SCIENTIFIC LITERATURE | ||||
| Muscarinic acetylcholine receptor M1 | GPCR | AGONIST | EC50 | 7.02 | SCIENTIFIC LITERATURE | ||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 5.01 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 5.51 | CHEMBL | |||||
| Muscarinic acetylcholine receptor DM1 | GPCR | Ki | 5.55 | CHEMBL | |||||
| Muscarinic acetylcholine receptor | GPCR | Ki | 7.08 | CHEMBL | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | EC50 | 5.16 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| C0699930 | UMLSCUI |
| D00525 | KEGG_DRUG |
| 01MI4Q9DI3 | UNII |
| 54-71-7 | SECONDARY_CAS_RN |
| 90356005 | SNOMEDCT_US |
| 4018209 | VANDF |
| 73122 | MMSL |
| 20709 | MMSL |
| 8328 | RXNORM |
| 372895002 | SNOMEDCT_US |
| d04031 | MMSL |
| 001693 | NDDF |
| 5910 | PUBCHEM_CID |
| CHEBI:8207 | CHEBI |
| CHEMBL550 | ChEMBL_ID |
| DB01085 | DRUGBANK_ID |
| CHEMBL611494 | ChEMBL_ID |
| CHEMBL1200330 | ChEMBL_ID |
| 9PL | PDB_CHEM_ID |
| CHEMBL1213136 | ChEMBL_ID |
| D010862 | MESH_DESCRIPTOR_UI |
| 305 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-5911 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 12 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0115-5922 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 12 sections |
| Pilocarpine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0228-2801 | TABLET, FILM COATED | 5 mg | ORAL | NDA AUTHORIZED GENERIC | 12 sections |
| Pilocarpine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0228-2837 | TABLET, FILM COATED | 7.50 mg | ORAL | NDA AUTHORIZED GENERIC | 12 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1313 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 11 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0527-1407 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 11 sections |
| ISOPTO CARPINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0998-0203 | SOLUTION/ DROPS | 10 mg | OPHTHALMIC | NDA | 15 sections |
| ISOPTO CARPINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0998-0204 | SOLUTION/ DROPS | 20 mg | OPHTHALMIC | NDA | 15 sections |
| ISOPTO CARPINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0998-0206 | SOLUTION/ DROPS | 40 mg | OPHTHALMIC | NDA | 15 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-589 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 12 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-590 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 12 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-680 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 13 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-121 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 11 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-122 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 11 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-223 | SOLUTION/ DROPS | 10 mg | OPHTHALMIC | ANDA | 15 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-224 | SOLUTION/ DROPS | 20 mg | OPHTHALMIC | ANDA | 15 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-226 | SOLUTION/ DROPS | 40 mg | OPHTHALMIC | ANDA | 15 sections |
| PILOCARPINE HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-368 | SOLUTION/ DROPS | 10 mg | CONJUNCTIVAL | NDA | 11 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-601 | TABLET | 5 mg | ORAL | ANDA | 12 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-5436 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 11 sections |
| Salagen | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59212-705 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 12 sections |
| Salagen | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59212-775 | TABLET, FILM COATED | 7.50 mg | ORAL | NDA | 12 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59651-224 | TABLET, FILM COATED | 5 mg | ORAL | ANDA | 11 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59651-225 | TABLET, FILM COATED | 7.50 mg | ORAL | ANDA | 11 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61314-203 | SOLUTION/ DROPS | 10 mg | OPHTHALMIC | NDA authorized generic | 15 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61314-204 | SOLUTION/ DROPS | 20 mg | OPHTHALMIC | NDA authorized generic | 15 sections |
| Pilocarpine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 61314-206 | SOLUTION/ DROPS | 40 mg | OPHTHALMIC | NDA authorized generic | 15 sections |
| Salagen | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62856-705 | TABLET, FILM COATED | 5 mg | ORAL | NDA | 12 sections |
| Salagen | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62856-775 | TABLET, FILM COATED | 7.50 mg | ORAL | NDA | 12 sections |
| Pilocarpine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68084-928 | TABLET, FILM COATED | 5 mg | ORAL | NDA authorized generic | 11 sections |