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

Stem definition	Drug id	CAS RN
histamine-H1 receptor antagonists, tricyclic compounds	1986	113806-05-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: olopatadine olopatadine hydrochloride opatanol pataday patanol olopatadine HCl	An antihistamine with mast-cell stabilizing properties used as eye drops in the treatment of ALLERGIC CONJUNCTIVITIS. Molecular weight: 337.42 Formula: C21H23NO3 CLOGP: 1.09 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 49.77 ALOGS: -4.03 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

olopatadine
olopatadine hydrochloride
opatanol
pataday
patanol
olopatadine HCl

An antihistamine with mast-cell stabilizing properties used as eye drops in the treatment of ALLERGIC CONJUNCTIVITIS.

Molecular weight: 337.42
Formula: C21H23NO3
CLOGP: 1.09
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 49.77
ALOGS: -4.03
ROTB: 5

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
EoM (Fraction excreted unchanged in urine)	65 %	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	28.04 mg/mL	Bocci G, Oprea TI, Benet LZ
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.11 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

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Approvals:

Date	Agency	Company	Orphan
Dec. 18, 1996	FDA	ALCON

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
Treatment failure	1438.18	13.78	704	10894	198339	63279085
Eye irritation	114.63	13.78	63	11535	21908	63455516
Asthma	67.76	13.78	99	11499	127462	63349962
Eye pruritus	61.95	13.78	40	11558	18631	63458793
Sinusitis	51.52	13.78	122	11476	226531	63250893
Conjunctivitis allergic	47.76	13.78	14	11584	928	63476496
Urticarial vasculitis	47.61	13.78	13	11585	666	63476758
Ocular hyperaemia	38.69	13.78	34	11564	25110	63452314
Total cholesterol/HDL ratio abnormal	35.88	13.78	7	11591	77	63477347
Eye discharge	33.31	13.78	18	11580	6045	63471379

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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
Treatment failure	730.57	17.93	264	4543	46433	34905691
Eye irritation	68.64	17.93	29	4778	7532	34944592
Hypersensitivity	47.81	17.93	50	4757	60985	34891139
Ocular hyperaemia	43.00	17.93	24	4783	11428	34940696
Asthma	42.78	17.93	40	4767	42616	34909508
Hepatic function abnormal	34.10	17.93	36	4771	44327	34907797
Dermatitis atopic	34.04	17.93	16	4791	5331	34946793
Rash	32.70	17.93	85	4722	222667	34729457
Cerebral infarction	31.94	17.93	28	4779	27427	34924697
Alopecia areata	30.60	17.93	7	4800	231	34951893

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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
Asthma	88.26	14.01	104	11632	134991	79597661
Hepatic function abnormal	62.80	14.01	65	11671	73042	79659610
Alopecia areata	49.52	14.01	16	11720	1827	79730825
Dermatitis atopic	47.18	14.01	25	11711	10031	79722621
Eye irritation	44.03	14.01	31	11705	20650	79712002
Drug eruption	41.25	14.01	41	11695	43894	79688758
Urticarial vasculitis	37.66	14.01	10	11726	574	79732078
Total cholesterol/HDL ratio abnormal	37.31	14.01	7	11729	78	79732574
Upper respiratory tract inflammation	37.30	14.01	16	11720	4019	79728633
Sinusitis	35.98	14.01	85	11651	195416	79537236

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	R01AC08	RESPIRATORY SYSTEM NASAL PREPARATIONS DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE Antiallergic agents, excl. corticosteroids
ATC	S01GX09	SENSORY ORGANS OPHTHALMOLOGICALS DECONGESTANTS AND ANTIALLERGICS Other antiallergics
FDA EPC	N0000175519	Histamine-1 Receptor Inhibitor
FDA EPC	N0000175587	Histamine-1 Receptor Antagonist
FDA EPC	N0000175630	Mast Cell Stabilizer
FDA MoA	N0000000190	Histamine H1 Receptor Antagonists
FDA PE	N0000175628	Decreased Histamine Release
MeSH PA	D000700	Analgesics
MeSH PA	D018712	Analgesics, Non-Narcotic
MeSH PA	D018926	Anti-Allergic Agents

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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
Allergic rhinitis	indication	61582004
Seasonal allergic rhinitis	indication	367498001
Allergic conjunctivitis	indication	473460002	DOID:11204
Epistaxis	contraindication	12441001
Perforation of nasal septum	contraindication	80142000
Nasal Lesions	contraindication
Nasal Septal Ulcers	contraindication

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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	3.89	acidic
pKa2	8.66	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
0.025MG/SPRAY;0.665MG/SPRAY	RYALTRIS	GLENMARK SPECIALTY	N211746	Jan. 13, 2022	RX	SPRAY, METERED	NASAL	10016443	Sept. 4, 2034	TREATMENT OF SEASONAL ALLERGIC RHINITIS BY NASALY ADMINISTERING A COMBINATION OF OLOPATADINE HYDROCHLORIDE AND MOMETASONE FUROATE
0.025MG/SPRAY;0.665MG/SPRAY	RYALTRIS	GLENMARK SPECIALTY	N211746	Jan. 13, 2022	RX	SPRAY, METERED	NASAL	10517880	Sept. 4, 2034	TREATMENT OF SEASONAL ALLERGIC RHINITIS BY NASALY ADMINISTERING A COMBINATION OF OLOPATADINE HYDROCHLORIDE AND MOMETASONE FUROATE
0.025MG/SPRAY;0.665MG/SPRAY	RYALTRIS	GLENMARK SPECIALTY	N211746	Jan. 13, 2022	RX	SPRAY, METERED	NASAL	10548907	Sept. 4, 2034	TREATMENT OF SEASONAL ALLERGIC RHINITIS BY NASALY ADMINISTERING A COMBINATION OF OLOPATADINE HYDROCHLORIDE AND MOMETASONE FUROATE
0.025MG/SPRAY;0.665MG/SPRAY	RYALTRIS	GLENMARK SPECIALTY	N211746	Jan. 13, 2022	RX	SPRAY, METERED	NASAL	10646500	Sept. 4, 2034	TREATMENT OF SEASONAL ALLERGIC RHINITIS BY NASALY ADMINISTERING A COMBINATION OF OLOPATADINE HYDROCHLORIDE AND MOMETASONE FUROATE
0.025MG/SPRAY;0.665MG/SPRAY	RYALTRIS	GLENMARK SPECIALTY	N211746	Jan. 13, 2022	RX	SPRAY, METERED	NASAL	10758550	Sept. 4, 2034	TREATMENT OF SEASONAL ALLERGIC RHINITIS BY NASALY ADMINISTERING A COMBINATION OF OLOPATADINE HYDROCHLORIDE AND MOMETASONE FUROATE TO A PEDIATRIC PATIENT
0.025MG/SPRAY;0.665MG/SPRAY	RYALTRIS	GLENMARK SPECIALTY	N211746	Jan. 13, 2022	RX	SPRAY, METERED	NASAL	10765686	Sept. 4, 2034	METHOD OF DELIVERING A COMBINATION OF OLOPATADINE HYDROCHLORIDE AND MOMETASONE FUROATE TO A NASAL AIRWAY
0.025MG/SPRAY;0.665MG/SPRAY	RYALTRIS	GLENMARK SPECIALTY	N211746	Jan. 13, 2022	RX	SPRAY, METERED	NASAL	11400101	Sept. 4, 2034	TREATMENT OF SEASONAL ALLERGIC RHINITIS BY NASALY ADMINISTERING A COMBINATION OF OLOPATADINE HYDROCHLORIDE AND MOMETASONE FUROATE
0.025MG/SPRAY;0.665MG/SPRAY	RYALTRIS	GLENMARK SPECIALTY	N211746	Jan. 13, 2022	RX	SPRAY, METERED	NASAL	9078923	Sept. 4, 2034	TREATMENT OF SEASONAL ALLERGIC RHINITIS BY NASALY ADMINISTERING A COMBINATION OF OLOPATADINE HYDROCHLORIDE AND MOMETASONE FUROATE
0.025MG/SPRAY;0.665MG/SPRAY	RYALTRIS	GLENMARK SPECIALTY	N211746	Jan. 13, 2022	RX	SPRAY, METERED	NASAL	9750754	Sept. 4, 2034	TREATMENT OF SEASONAL ALLERGIC RHINITIS BY NASALY ADMINISTERING A COMBINATION OF OLOPATADINE HYDROCHLORIDE AND MOMETASONE FUROATE
EQ 0.7% BASE	PATADAY ONCE DAILY RELIEF	ALCON LABS INC	N206276	Jan. 30, 2015	OTC	SOLUTION/DROPS	OPHTHALMIC	8791154	May 19, 2032	TREATMENT OF OCULAR ITCHING ASSOCIATED WITH ALLERGIC CONJUNCTIVITIS

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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
0.025MG/SPRAY;0.665MG/SPRAY	RYALTRIS	GLENMARK SPECIALTY	N211746	Jan. 13, 2022	RX	SPRAY, METERED	NASAL	Jan. 13, 2025	NEW PRODUCT

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	8.28		WOMBAT-PK	CHEMBL
Histamine H1 receptor	GPCR		HRH1_CAVPO		Ki	7.80		CHEMBL

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External reference:

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ID	Source
006403	NDDF
006404	NDDF
10342	MMSL
107496	MMSL
108843008	SNOMEDCT_US
108845001	SNOMEDCT_US
135391	RXNORM
140462-76-6	SECONDARY_CAS_RN
230004	MMSL
372550002	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Olopatadine	HUMAN PRESCRIPTION DRUG LABEL	1	17478-105	SOLUTION/ DROPS	1 mg	OPHTHALMIC	ANDA	17 sections
Olopatadine	HUMAN PRESCRIPTION DRUG LABEL	1	17478-305	SOLUTION/ DROPS	2 mg	OPHTHALMIC	ANDA	24 sections
Olopatadine	HUMAN PRESCRIPTION DRUG LABEL	1	17478-305	SOLUTION/ DROPS	2 mg	OPHTHALMIC	ANDA	24 sections
Olopatadine	HUMAN OTC DRUG LABEL	1	17478-308	SOLUTION/ DROPS	1 mg	OPHTHALMIC	ANDA	13 sections
Olopatadine	HUMAN OTC DRUG LABEL	1	17478-312	SOLUTION/ DROPS	2 mg	OPHTHALMIC	ANDA	13 sections
Olopatadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7684	SOLUTION/ DROPS	2 mg	OPHTHALMIC	ANDA	22 sections
Olopatadine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7684	SOLUTION/ DROPS	2 mg	OPHTHALMIC	ANDA	22 sections
OLOPATADINE HYDROCHLORIDE	Human OTC Drug Label	1	0363-0200	SOLUTION	1 mg	OPHTHALMIC	ANDA	13 sections
OLOPATADINE HYDROCHLORIDE	Human OTC Drug Label	1	0363-8022	SOLUTION	2 mg	OPHTHALMIC	ANDA	13 sections
Olopatadine Hydrochloride Ophthalmic Solution	Human OTC Drug Label	1	0363-7130	SOLUTION/ DROPS	1 mg	OPHTHALMIC	ANDA	13 sections

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