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

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

  • Status: OFP

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

Drug dosage:

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

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
July 29, 1974 FDA

FDA Adverse Event Reporting System (Female)

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
Occult blood 49.81 15.73 14 6211 1193 50597706
Limb injury 47.21 15.73 30 6195 20220 50578679
Angioplasty 36.09 15.73 11 6214 1244 50597655
Dry eye 30.85 15.73 28 6197 32067 50566832
Peripheral vascular disorder 29.19 15.73 14 6211 5453 50593446
Transient ischaemic attack 28.82 15.73 27 6198 32183 50566716
Iritis 28.55 15.73 11 6214 2517 50596382
Iron deficiency 28.26 15.73 14 6211 5848 50593051
Spinal osteoarthritis 28.25 15.73 19 6206 14073 50584826
Hot flush 26.74 15.73 30 6195 44139 50554760
Tanning 26.04 15.73 5 6220 77 50598822
Choking 26.02 15.73 15 6210 8483 50590416
Crepitations 24.60 15.73 13 6212 6206 50592693
Glaucoma 21.94 15.73 17 6208 15669 50583230
Asthma 21.45 15.73 39 6186 89298 50509601
Acute myocardial infarction 21.45 15.73 22 6203 29251 50569648
Dry mouth 21.00 15.73 30 6195 56148 50542751
Haemorrhage 20.66 15.73 29 6196 53412 50545487
Body temperature fluctuation 20.21 15.73 8 6217 1965 50596934
Blood pressure systolic decreased 19.92 15.73 11 6214 5728 50593171
Conjunctival hyperaemia 19.79 15.73 8 6217 2074 50596825
Sputum discoloured 19.79 15.73 15 6210 13380 50585519
Coronary artery disease 19.39 15.73 21 6204 29705 50569194
Open fracture 19.20 15.73 5 6220 319 50598580
Platelet count increased 18.70 15.73 15 6210 14525 50584374
Eye pain 18.38 15.73 20 6205 28429 50570470
Urinary retention 17.96 15.73 19 6206 26171 50572728
Epstein-Barr virus associated lymphoma 17.37 15.73 5 6220 464 50598435
Increased tendency to bruise 17.29 15.73 12 6213 9344 50589555
Blood pressure diastolic increased 17.27 15.73 11 6214 7432 50591467
Cardiac failure congestive 16.77 15.73 34 6191 84348 50514551
Toxicity to various agents 16.69 15.73 3 6222 212496 50386403
Exposure to communicable disease 16.63 15.73 5 6220 540 50598359
Eye irritation 16.55 15.73 15 6210 17125 50581774

FDA Adverse Event Reporting System (Male)

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 60.72 25.33 16 816 4773 29568922
Treatment failure 43.41 25.33 21 811 36918 29536777
Ocular surface disease 27.67 25.33 4 828 48 29573647
Visual impairment 26.40 25.33 14 818 29694 29544001

FDA Adverse Event Reporting System (Geriatric)

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
Limb injury 57.55 17.00 32 5690 23473 64469537
Occult blood 52.27 17.00 14 5708 1388 64491622
Angioplasty 40.79 17.00 12 5710 1673 64491337
Intraocular pressure increased 40.29 17.00 18 5704 8284 64484726
Glaucoma 36.61 17.00 21 5701 16327 64476683
Transient ischaemic attack 35.04 17.00 30 5692 44152 64448858
Hot flush 31.88 17.00 29 5693 46206 64446804
Choking 30.39 17.00 16 5706 10522 64482488
Iron deficiency 29.92 17.00 14 5708 7163 64485847
Peripheral vascular disorder 29.76 17.00 14 5708 7247 64485763
Crepitations 28.61 17.00 14 5708 7901 64485109
Tanning 27.80 17.00 5 5717 75 64492935
Wound 27.65 17.00 34 5688 76443 64416567
Iritis 26.17 17.00 10 5712 3106 64489904
Asthma 24.70 17.00 36 5686 95189 64397821
Dry eye 23.60 17.00 20 5702 28999 64464011
Haemorrhage 23.55 17.00 32 5690 79319 64413691
Spinal osteoarthritis 23.30 17.00 15 5707 14326 64478684
Weight increased 22.71 17.00 55 5667 213293 64279717
Sputum discoloured 22.60 17.00 16 5706 17840 64475170
Conjunctival hyperaemia 20.68 17.00 9 5713 3890 64489120
Ocular surface disease 20.66 17.00 4 5718 91 64492919
Cardiac failure congestive 19.99 17.00 39 5683 130541 64362469
Open fracture 19.90 17.00 5 5717 385 64492625
Urinary retention 19.62 17.00 23 5699 49178 64443832
Body temperature fluctuation 18.77 17.00 8 5714 3290 64489720
Exposure to communicable disease 18.71 17.00 5 5717 491 64492519
Platelet count increased 17.54 17.00 14 5708 18682 64474328

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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
FDA MoA N0000000104 Cholinergic Muscarinic Agonists
FDA MoA N0000175369 Cholinergic Agonists
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
CHEBI has role CHEBI:39456 antiglaucoma agent
FDA EPC N0000175884 Cholinergic Receptor Agonist

Drug Use (View source of the data)

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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.04 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
1.25% VUITY ABBVIE INC N214028 Oct. 28, 2021 RX SOLUTION OPHTHALMIC 10610518 April 24, 2039 USE OF VUITY FOR THE TREATMENT OF PRESBYOPIA IN ADULTS
1.25% VUITY ABBVIE INC N214028 Oct. 28, 2021 RX SOLUTION OPHTHALMIC 11285134 April 24, 2039 USE OF VUITY FOR THE TREATMENT OF PRESBYOPIA IN ADULTS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
1.25% VUITY ABBVIE INC N214028 Oct. 28, 2021 RX SOLUTION OPHTHALMIC Oct. 28, 2024 NEW PRODUCT

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Muscarinic acetylcholine receptor M3 GPCR AGONIST EC50 6.97 SCIENTIFIC LITERATURE IUPHAR
Muscarinic acetylcholine receptor M1 GPCR AGONIST EC50 7.02 SCIENTIFIC LITERATURE
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 Ki 5.51 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR EC50 5.16 CHEMBL
Muscarinic acetylcholine receptor DM1 GPCR Ki 5.55 CHEMBL
Muscarinic acetylcholine receptor GPCR Ki 7.08 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 5.01 CHEMBL

External reference:

IDSource
D00525 KEGG_DRUG
148-72-1 SECONDARY_CAS_RN
54-71-7 SECONDARY_CAS_RN
4018207 VANDF
4018208 VANDF
4018209 VANDF
4020904 VANDF
C0031923 UMLSCUI
CHEBI:8207 CHEBI
9PL PDB_CHEM_ID
CHEMBL550 ChEMBL_ID
CHEMBL611494 ChEMBL_ID
DB01085 DRUGBANK_ID
CHEMBL1200330 ChEMBL_ID
CHEMBL1213136 ChEMBL_ID
D010862 MESH_DESCRIPTOR_UI
5910 PUBCHEM_CID
305 IUPHAR_LIGAND_ID
01MI4Q9DI3 UNII
103244 RXNORM
1396 MMSL
20709 MMSL
3317 MMSL
44345 MMSL
5299 MMSL
5300 MMSL
72427 MMSL
73122 MMSL
d04031 MMSL
001693 NDDF
001694 NDDF
001695 NDDF
372895002 SNOMEDCT_US
387035001 SNOMEDCT_US
395827004 SNOMEDCT_US
90356005 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
VUITY HUMAN PRESCRIPTION DRUG LABEL 1 0074-7098 SOLUTION/ DROPS 12.50 mg OPHTHALMIC NDA 24 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0115-5911 TABLET, FILM COATED 7.50 mg ORAL ANDA 23 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0115-5922 TABLET, FILM COATED 5 mg ORAL ANDA 23 sections
Pilocarpine hydrochloride Human Prescription Drug Label 1 0228-2801 TABLET, FILM COATED 5 mg ORAL NDA AUTHORIZED GENERIC 21 sections
Pilocarpine hydrochloride Human Prescription Drug Label 1 0228-2837 TABLET, FILM COATED 7.50 mg ORAL NDA AUTHORIZED GENERIC 21 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0527-1313 TABLET, FILM COATED 5 mg ORAL ANDA 24 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0527-1407 TABLET, FILM COATED 7.50 mg ORAL ANDA 24 sections
pilocarpine hydrchloride HUMAN PRESCRIPTION DRUG LABEL 1 0574-0792 TABLET, FILM COATED 5 mg ORAL ANDA 20 sections
ISOPTO CARPINE HUMAN PRESCRIPTION DRUG LABEL 1 0998-0203 SOLUTION/ DROPS 10 mg OPHTHALMIC NDA 24 sections
ISOPTO CARPINE HUMAN PRESCRIPTION DRUG LABEL 1 0998-0204 SOLUTION/ DROPS 20 mg OPHTHALMIC NDA 24 sections
ISOPTO CARPINE HUMAN PRESCRIPTION DRUG LABEL 1 0998-0206 SOLUTION/ DROPS 40 mg OPHTHALMIC NDA 24 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10135-589 TABLET, FILM COATED 5 mg ORAL ANDA 22 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10135-590 TABLET, FILM COATED 7.50 mg ORAL ANDA 22 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 10135-680 TABLET, FILM COATED 5 mg ORAL ANDA 23 sections
Pilocarpine Hydrochloride Human Prescription Drug Label 1 16714-121 TABLET, FILM COATED 5 mg ORAL ANDA 20 sections
Pilocarpine Hydrochloride Human Prescription Drug Label 1 16714-122 TABLET, FILM COATED 7.50 mg ORAL ANDA 20 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-223 SOLUTION/ DROPS 10 mg OPHTHALMIC ANDA 24 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-224 SOLUTION/ DROPS 20 mg OPHTHALMIC ANDA 24 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 17478-226 SOLUTION/ DROPS 40 mg OPHTHALMIC ANDA 24 sections
PILOCARPINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 21695-368 SOLUTION/ DROPS 10 mg CONJUNCTIVAL NDA 14 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 21695-601 TABLET 5 mg ORAL ANDA 23 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 50268-652 TABLET, FILM COATED 5 mg ORAL ANDA 24 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 54868-5436 TABLET, FILM COATED 5 mg ORAL ANDA 24 sections
Salagen Human Prescription Drug Label 1 59212-705 TABLET, FILM COATED 5 mg ORAL NDA 21 sections
Salagen Human Prescription Drug Label 1 59212-775 TABLET, FILM COATED 7.50 mg ORAL NDA 21 sections
Pilocarpine Hydrochloride Human Prescription Drug Label 1 59651-224 TABLET, FILM COATED 5 mg ORAL ANDA 20 sections
Pilocarpine Hydrochloride Human Prescription Drug Label 1 59651-225 TABLET, FILM COATED 7.50 mg ORAL ANDA 20 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 60219-1745 SOLUTION/ DROPS 10 mg OPHTHALMIC ANDA 23 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 60219-1746 SOLUTION/ DROPS 20 mg OPHTHALMIC ANDA 23 sections
Pilocarpine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 60219-1747 SOLUTION/ DROPS 40 mg OPHTHALMIC ANDA 23 sections