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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
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

Molecule

Description

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:

Dose	Unit	Route
15	mg	O
10	mg	P
0.40	ml	None
40	mg	ointment

ADMET properties:

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Property	Value	Reference
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

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Approvals:

Date	Agency	Company	Orphan
July 29, 1974	FDA

FDA Adverse Event Reporting System (Female)

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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	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

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FDA Adverse Event Reporting System (Male)

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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
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

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FDA Adverse Event Reporting System (Geriatric)

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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	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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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
CHEBI has role	CHEBI:39456	antiglaucoma agent
FDA EPC	N0000175884	Cholinergic Receptor Agonist
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

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Drug Use | Suggest Off label Use Form| |View source of the data|

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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

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🐶 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)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent 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

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN	AGONIST	EC50	6.97	SCIENTIFIC LITERATURE	IUPHAR
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN	AGONIST	EC50	7.02	SCIENTIFIC LITERATURE
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN	AGONIST	EC50	6.95	SCIENTIFIC LITERATURE
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN	AGONIST	EC50	7.15	SCIENTIFIC LITERATURE
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN	AGONIST	EC50	7	SCIENTIFIC LITERATURE
Muscarinic acetylcholine receptor M1	GPCR		ACM1_RAT		Ki	5.51	CHEMBL
Muscarinic acetylcholine receptor M1	GPCR		ACM1_MOUSE		EC50	5.16	CHEMBL
Muscarinic acetylcholine receptor DM1	GPCR		ACM1_DROME		Ki	5.55	CHEMBL
Muscarinic acetylcholine receptor	GPCR		ACM1_RAT ACM3_RAT ACM4_RAT ACM5_RAT ACM2_RAT		Ki	7.08	CHEMBL
Muscarinic acetylcholine receptor M2	GPCR		ACM2_RAT		Ki	5.01	CHEMBL

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External reference:

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ID	Source
9PL	PDB_CHEM_ID
001693	NDDF
001694	NDDF
001695	NDDF
01MI4Q9DI3	UNII
103244	RXNORM
1396	MMSL
148-72-1	SECONDARY_CAS_RN
20709	MMSL
305	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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 hydrchloride	HUMAN PRESCRIPTION DRUG LABEL	1	0574-0792	TABLET, FILM COATED	5 mg	ORAL	ANDA	20 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

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