pilocarpine 🐶 Veterinary Use | 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 |
|---|---|---|---|---|---|---|
| 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 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 | 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 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 | 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:
| 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 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|
| 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 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
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)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 1.25% | VUITY | ABBVIE INC | N214028 | Oct. 28, 2021 | RX | SOLUTION | OPHTHALMIC | Oct. 28, 2024 | NEW PRODUCT |
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 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |