pilocarpine indications/contra

Stem definitionDrug idCAS RN
tricyclic compounds 2166 92-13-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • salagen
  • pilocarpine nitrate
  • pilocarpine
  • ocucarpine
  • pilocarpol
  • pilokarpin
  • syncarpine
  • (+)-Pilocarpine
  • pilocarpine hydrochloride
  • pilocarpine HCl
A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.
  • Molecular weight: 208.26
  • Formula: C11H16N2O2
  • CLOGP: -0.20
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 44.12
  • ALOGS: -2
  • ROTB: 3

Drug dosage:

DoseUnitRoute
15 mg O
10 mg P
0.40 ml None
40 mg ointment

Approvals:

DateAgencyCompanyOrphan
July 29, 1974 FDA

FDA Adverse Event Reporting System

scroll-->
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
Intraocular pressure increased 156.30 63.17 25 154 2397 3383283
Visual acuity reduced 94.04 63.17 20 159 8994 3376686
Angle closure glaucoma 85.47 63.17 13 166 867 3384813
Anterior chamber disorder 76.89 63.17 9 170 75 3385605
Drug ineffective 74.50 63.17 29 150 116061 3269619
Endophthalmitis 71.35 63.17 12 167 1507 3384173

Pharmacologic Action:

scroll-->
SourceCodeDescription
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
CHEBI has role CHEBI:39456 antiglaucoma drug
MeSH PA D001337 Autonomic Agents
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
FDA MoA N0000000104 Cholinergic Muscarinic Agonists
FDA EPC N0000175884 Cholinergic Receptor Agonist

Drug Use (View source of the data)

scroll-->
DiseaseRelationSNOMED_IDDOID
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

scroll-->
Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.04 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

scroll-->
TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA 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:

scroll-->
IDSource
305 IUPHAR_LIGAND_ID
C0699930 UMLSCUI
D00525 KEGG_DRUG
CHEMBL550 ChEMBL_ID
01MI4Q9DI3 UNII
54-71-7 SECONDARY_CAS_RN
DB01085 DRUGBANK_ID
5910 PUBCHEM_CID
4018209 VANDF
73122 MMSL
20709 MMSL
8328 RXNORM
372895002 SNOMEDCT_US
90356005 SNOMEDCT_US
116539001 SNOMEDCT_US
d04031 MMSL
N0000006106 NDFRT
N0000146543 NDFRT
001693 NDDF
CHEBI:8207 CHEBI
CHEMBL611494 ChEMBL_ID
CHEMBL1200330 ChEMBL_ID
CHEMBL1213136 ChEMBL_ID
D010862 MESH_DESCRIPTOR_UI
9PL PDB_CHEM_ID

Pharmaceutical products:

scroll-->
ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
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 0179-0153 TABLET, FILM COATED 5 mg ORAL ANDA 11 sections
Pilocarpine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0228-2801 TABLET, FILM COATED 5 mg ORAL NDA AUTHORIZED GENERIC 11 sections
Pilocarpine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0228-2837 TABLET, FILM COATED 7.50 mg ORAL NDA AUTHORIZED GENERIC 11 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 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
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
Pilocarpine hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 68151-3015 TABLET, FILM COATED 5 mg ORAL NDA AUTHORIZED GENERIC 11 sections