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:

PropertyValueReference
fu (Fraction unbound in plasma) 0.92 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

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
Limb injury 54.49 16.48 35 7341 25442 63456204
Vitreous detachment 51.75 16.48 16 7360 2011 63479635
Occult blood 49.56 16.48 14 7362 1287 63480359
Angioplasty 48.63 16.48 14 7362 1378 63480268
Glaucoma 42.98 16.48 27 7349 18878 63462768
Vitreous floaters 41.34 16.48 18 7358 5948 63475698
Choking 41.22 16.48 21 7355 9858 63471788
Eye pain 41.18 16.48 33 7343 33821 63447825
Peripheral vascular disorder 41.14 16.48 18 7358 6017 63475629
Vitreoretinal traction syndrome 38.71 16.48 6 7370 24 63481622
Vision blurred 37.97 16.48 50 7326 91874 63389772
Dry eye 37.82 16.48 34 7342 40727 63440919
Visual impairment 34.98 16.48 46 7330 84400 63397246
Eye irritation 34.63 16.48 25 7351 21946 63459700
Transient ischaemic attack 34.06 16.48 31 7345 37722 63443924
Crepitations 33.28 16.48 17 7359 8023 63473623
Acute myocardial infarction 28.24 16.48 26 7350 32098 63449548
Spinal osteoarthritis 26.85 16.48 19 7357 16167 63465479
Iritis 26.72 16.48 11 7365 3164 63478482
Sputum discoloured 26.68 16.48 19 7357 16328 63465318
Iron deficiency 26.24 16.48 14 7362 7216 63474430
Hot flush 26.19 16.48 31 7345 51128 63430518
Coronary artery disease 26.14 16.48 25 7351 32352 63449294
Tanning 25.86 16.48 5 7371 85 63481561
Haemorrhage 24.89 16.48 33 7343 60989 63420657
Urinary retention 23.72 16.48 23 7353 30278 63451368
Accommodation disorder 23.50 16.48 6 7370 375 63481271
Body temperature fluctuation 22.98 16.48 9 7367 2276 63479370
Conjunctival hyperaemia 22.63 16.48 9 7367 2370 63479276
Pulmonary congestion 21.22 16.48 17 7359 17401 63464245
Cardiac failure congestive 20.81 16.48 38 7338 92395 63389251
Blood pressure systolic decreased 20.51 16.48 12 7364 7385 63474261
Intraocular pressure increased 19.92 16.48 11 7365 6067 63475579
Blood pressure diastolic increased 19.55 16.48 13 7363 9997 63471649
Corneal oedema 19.06 16.48 7 7369 1486 63480160
Toxicity to various agents 18.99 16.48 3 7373 247247 63234399
Dry mouth 18.79 16.48 33 7343 77830 63403816
Asthma 18.76 16.48 44 7332 127517 63354129
Myocardial infarction 18.73 16.48 38 7338 99855 63381791
Blood pressure increased 17.73 16.48 50 7326 162012 63319634
Open fracture 17.72 16.48 5 7371 458 63481188
Ocular hyperaemia 17.67 16.48 18 7358 25126 63456520
Epstein-Barr virus associated lymphoma 17.16 16.48 5 7371 513 63481133
Photopsia 17.12 16.48 9 7367 4500 63477146
Pulmonary oedema 16.95 16.48 26 7350 54847 63426799
Platelet count increased 16.87 16.48 15 7361 17696 63463950
Productive cough 16.85 16.48 28 7348 63180 63418466
Increased tendency to bruise 16.61 16.48 12 7364 10540 63471106

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
Vitreous detachment 91.46 28.81 17 1128 871 34954915
Visual impairment 88.98 28.81 36 1109 35766 34920020
Retinal tear 72.51 28.81 14 1131 879 34954907
Retinal detachment 70.22 28.81 19 1126 5372 34950414
Vitreous floaters 62.86 28.81 16 1129 3569 34952217
Intraocular pressure increased 60.97 28.81 17 1128 5366 34950420
Vision blurred 41.42 28.81 23 1122 45940 34909846
Photopsia 40.55 28.81 10 1135 1958 34953828
Treatment failure 35.71 28.81 21 1124 46676 34909110
Ocular hyperaemia 33.54 28.81 13 1132 11439 34944347

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 65.36 17.20 37 6701 29491 79708159
Glaucoma 55.51 17.20 29 6709 19732 79717918
Angioplasty 53.53 17.20 15 6723 1848 79735802
Occult blood 50.09 17.20 14 6724 1709 79735941
Intraocular pressure increased 49.02 17.20 21 6717 9184 79728466
Choking 46.57 17.20 22 6716 12079 79725571
Vitreous detachment 46.34 17.20 14 6724 2245 79735405
Vitreous floaters 43.47 17.20 18 6720 7238 79730412
Peripheral vascular disorder 41.71 17.20 18 6720 8012 79729638
Transient ischaemic attack 39.64 17.20 34 6704 52661 79684989
Crepitations 37.90 17.20 18 6720 9999 79727651
Sputum discoloured 29.61 17.20 20 6718 21723 79715927
Hot flush 28.85 17.20 29 6709 54848 79682802
Dry eye 28.11 17.20 24 6714 36907 79700743
Tanning 27.56 17.20 5 6733 83 79737567
Haemorrhage 27.29 17.20 36 6702 91082 79646568
Visual impairment 26.97 17.20 36 6702 92095 79645555
Urinary retention 26.29 17.20 28 6710 56602 79681048
Vitreoretinal traction syndrome 25.88 17.20 4 6734 23 79737627
Iron deficiency 25.33 17.20 14 6724 10640 79727010
Wound 24.68 17.20 39 6699 116140 79621510
Iritis 24.58 17.20 10 6728 3845 79733805
Vision blurred 24.53 17.20 37 6701 105861 79631789
Cardiac failure congestive 23.87 17.20 43 6695 142359 79595291
Conjunctival hyperaemia 23.27 17.20 10 6728 4403 79733247
Asthma 22.91 17.20 41 6697 135054 79602596
Weight increased 22.85 17.20 63 6675 277323 79460327
Eye pain 21.87 17.20 21 6717 37557 79700093
Spinal osteoarthritis 21.70 17.20 15 6723 16912 79720738
Pulmonary congestion 21.42 17.20 18 6720 27082 79710568
Body temperature fluctuation 21.31 17.20 9 6729 3798 79733852
Ocular surface disease 19.82 17.20 4 6734 119 79737531
Coronary artery disease 19.80 17.20 26 6712 65448 79672202
Acne 19.34 17.20 17 6721 27173 79710477
Blood pressure diastolic increased 18.91 17.20 13 6725 14529 79723121
Open fracture 18.86 17.20 5 6733 500 79737150
Exposure to communicable disease 18.49 17.20 5 6733 539 79737111
Accommodation disorder 18.03 17.20 5 6733 593 79737057
Corneal oedema 17.40 17.20 7 6731 2613 79735037
Blood pressure increased 17.38 17.20 48 6690 211312 79526338
Toxicity to various agents 17.29 17.20 7 6731 421533 79316117

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 | Suggest Off label Use Form| |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 N214028 Oct. 28, 2021 RX SOLUTION OPHTHALMIC 10610518 April 24, 2039 TREATMENT OF PRESBYOPIA IN ADULTS BY ADMINISTRATION OF PILOCARPINE HCI FORMULATION ONCE DAILY
1.25% VUITY ABBVIE N214028 Oct. 28, 2021 RX SOLUTION OPHTHALMIC 10610518 April 24, 2039 TREATMENT OF PRESBYOPIA IN ADULTS BY ADMINISTRATION OF PILOCARPINE HCI FORMULATION TWICE DAILY
1.25% VUITY ABBVIE 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 N214028 Oct. 28, 2021 RX SOLUTION OPHTHALMIC 11285134 April 24, 2039 TREATMENT OF PRESBYOPIA IN ADULTS BY ADMINISTRATION OF PILOCARPINE HCI FORMULATION ONCE DAILY
1.25% VUITY ABBVIE N214028 Oct. 28, 2021 RX SOLUTION OPHTHALMIC 11285134 April 24, 2039 TREATMENT OF PRESBYOPIA IN ADULTS BY ADMINISTRATION OF PILOCARPINE HCI FORMULATION TWICE DAILY
1.25% VUITY ABBVIE 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 N214028 Oct. 28, 2021 RX SOLUTION OPHTHALMIC Oct. 28, 2024 NEW PRODUCT
1.25% VUITY ABBVIE N214028 Oct. 28, 2021 RX SOLUTION OPHTHALMIC March 28, 2026 ADDITION OF SECOND DOSE FOR TREATMENT OF PRESBYOPIA IN ADULTS

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 26 sections
VUITY HUMAN PRESCRIPTION DRUG LABEL 1 0074-7098 SOLUTION/ DROPS 12.50 mg OPHTHALMIC NDA 26 sections
VUITY HUMAN PRESCRIPTION DRUG LABEL 1 0074-7098 SOLUTION/ DROPS 12.50 mg OPHTHALMIC NDA 26 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 0527-1313 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 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 16714-121 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 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 17478-223 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 17478-224 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 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