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

Stem definitionDrug idCAS RN
histamine-H1 receptor antagonists, tricyclic compounds 1986 113806-05-6

Description:

MoleculeDescription

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:

PropertyValueReference
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
EoM (Fraction excreted unchanged in urine) 65 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.11 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Dec. 18, 1996 FDA ALCON

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
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
Dry eye 33.07 13.78 39 11559 40722 63436702
Toxicity to various agents 31.54 13.78 4 11594 247246 63230178
Eyelid margin crusting 29.53 13.78 10 11588 1062 63476362
Hepatic function abnormal 29.24 13.78 35 11563 37107 63440317
Upper respiratory tract inflammation 27.58 13.78 12 11586 2511 63474913
Drug intolerance 27.50 13.78 11 11587 308650 63168774
Maternal exposure during pregnancy 27.03 13.78 4 11594 220058 63257366
Systemic lupus erythematosus 25.19 13.78 4 11594 208914 63268510
Alopecia areata 25.12 13.78 10 11588 1675 63475749
Vision blurred 24.77 13.78 53 11545 91871 63385553
Product packaging quantity issue 23.57 13.78 9 11589 1350 63476074
Dermatitis atopic 23.18 13.78 17 11581 9707 63467717
Urticaria aquagenic 21.76 13.78 4 11594 31 63477393
Urticaria cholinergic 21.65 13.78 4 11594 32 63477392
Synovitis 21.61 13.78 4 11594 186914 63290510
Arthropathy 21.51 13.78 8 11590 234784 63242640
Infusion site swelling 20.89 13.78 16 11582 9754 63467670
Glossodynia 20.31 13.78 4 11594 178872 63298552
Lichenification 19.75 13.78 6 11592 450 63476974
Eye swelling 19.59 13.78 23 11575 23895 63453529
Adrenal insufficiency 19.49 13.78 20 11578 17895 63459529
Foreign body sensation in eyes 19.25 13.78 9 11589 2225 63475199
Bronchitis 18.97 13.78 58 11540 124877 63352547
Hypohidrosis 18.77 13.78 4 11594 70 63477354
Burning feet syndrome 18.77 13.78 4 11594 70 63477354
Infusion site pain 18.65 13.78 19 11579 16850 63460574
Infusion site erythema 18.38 13.78 16 11582 11663 63465761
Rheumatoid arthritis 18.20 13.78 12 11586 253807 63223617
Ear infection 17.89 13.78 28 11570 38185 63439239
Infusion site extravasation 17.87 13.78 15 11583 10411 63467013
Eye pain 17.54 13.78 26 11572 33828 63443596
Conjunctivitis 17.03 13.78 20 11578 20776 63456648
Eyelid infection 16.83 13.78 5 11593 347 63477077
Dry skin 16.72 13.78 34 11564 56853 63420571
Renal colic 16.05 13.78 7 11591 1474 63475950
Pulmonary mass 15.70 13.78 20 11578 22576 63454848
Eczema 15.59 13.78 24 11574 32267 63445157
Headache 15.44 13.78 180 11418 633061 62844363
Infusion site pruritus 15.41 13.78 11 11587 6024 63471400
Fulminant type 1 diabetes mellitus 15.36 13.78 5 11593 470 63476954
General physical health deterioration 15.15 13.78 9 11589 201393 63276031
Eye allergy 15.14 13.78 6 11592 993 63476431
Vein collapse 14.89 13.78 6 11592 1038 63476386
Drug eruption 14.81 13.78 22 11576 28672 63448752
Neutrophil count decreased 14.59 13.78 32 11566 56374 63421050
Rhinitis allergic 14.43 13.78 14 11584 11713 63465711
Off label use 14.33 13.78 69 11529 674393 62803031
Cholangitis 13.89 13.78 10 11588 5551 63471873

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
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
Pruritus 30.53 17.93 63 4744 141918 34810206
Drug eruption 28.74 17.93 23 4784 19875 34932249
Interstitial lung disease 27.36 17.93 39 4768 65243 34886881
Sinusitis 27.30 17.93 31 4776 41371 34910753
Eye discharge 26.19 17.93 10 4797 1996 34950128
Dry eye 22.83 17.93 15 4792 9560 34942564
Product delivery mechanism issue 21.91 17.93 5 4802 163 34951961
Conjunctivitis allergic 19.58 17.93 7 4800 1163 34950961
Erythema multiforme 19.29 17.93 13 4794 8636 34943488
Eye pain 18.25 17.93 15 4792 13447 34938677

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
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
Ocular hyperaemia 35.51 14.01 31 11705 28175 79704477
Adrenal insufficiency 31.31 14.01 29 11707 28458 79704194
Interstitial lung disease 31.31 14.01 58 11678 112542 79620110
Platelet count decreased 30.92 14.01 80 11656 194584 79538068
Neutrophil count decreased 30.77 14.01 52 11684 93907 79638745
Conjunctivitis allergic 30.75 14.01 11 11725 1709 79730943
Cerebral infarction 29.50 14.01 35 11701 45641 79687011
Urticaria 26.26 14.01 73 11663 185128 79547524
Erythema multiforme 25.50 14.01 21 11715 17630 79715022
Pruritus 23.88 14.01 118 11618 394530 79338122
Drug intolerance 23.67 14.01 5 11731 264114 79468538
Eye pruritus 22.72 14.01 21 11715 20549 79712103
Urticaria aquagenic 22.63 14.01 4 11732 31 79732621
Urticaria cholinergic 22.51 14.01 4 11732 32 79732620
Dry eye 21.74 14.01 27 11709 36904 79695748
Pyrexia 21.59 14.01 172 11564 678537 79054115
Lichenification 21.44 14.01 7 11729 826 79731826
Completed suicide 21.32 14.01 5 11731 245762 79486890
Malaise 20.70 14.01 133 11603 489736 79242916
Erythema 20.66 14.01 76 11660 223214 79509438
Bronchitis 20.02 14.01 53 11683 130591 79602061
Off label use 19.82 14.01 68 11668 907147 78825505
Hypohidrosis 18.74 14.01 5 11731 292 79732360
Rash 18.06 14.01 146 11590 578212 79154440
Concomitant disease aggravated 17.64 14.01 15 11721 13152 79719500
Eye discharge 17.58 14.01 11 11725 6023 79726629
Eyelid infection 17.41 14.01 5 11731 384 79732268
Eye pain 16.77 14.01 24 11712 37554 79695098
Eczema 16.67 14.01 25 11711 40793 79691859
Rhinitis allergic 16.49 14.01 14 11722 12255 79720397
Cardiac disorder 15.97 14.01 32 11704 65725 79666927
Headache 15.76 14.01 156 11580 653616 79079036
Vein collapse 15.69 14.01 6 11730 1122 79731530
Syphilis 15.66 14.01 5 11731 549 79732103
Burning feet syndrome 15.60 14.01 4 11732 200 79732452
Myofascial pain syndrome 15.36 14.01 7 11729 2030 79730622
Anaphylactic reaction 14.94 14.01 36 11700 83707 79648945
Fulminant type 1 diabetes mellitus 14.10 14.01 6 11730 1477 79731175
Alopecia universalis 14.10 14.01 4 11732 294 79732358
Dry skin 14.08 14.01 31 11705 67964 79664688
Contraindicated product administered 14.07 14.01 3 11733 157535 79575117
Cholangitis 14.02 14.01 13 11723 12763 79719889

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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 MoA N0000000190 Histamine H1 Receptor Antagonists
FDA EPC N0000175519 Histamine-1 Receptor Inhibitor
FDA EPC N0000175587 Histamine-1 Receptor Antagonist
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
MeSH PA D018926 Anti-Allergic Agents
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D018501 Antirheumatic Agents
MeSH PA D018494 Histamine Agents
MeSH PA D006633 Histamine Antagonists
MeSH PA D006634 Histamine H1 Antagonists
MeSH PA D039563 Histamine H1 Antagonists, Non-Sedating
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
FDA PE N0000175628 Decreased Histamine Release
FDA EPC N0000175630 Mast Cell Stabilizer

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

DiseaseRelationSNOMED_IDDOID
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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.89 acidic
pKa2 8.66 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
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
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

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.025MG/SPRAY;0.665MG/SPRAY RYALTRIS GLENMARK SPECIALTY N211746 Jan. 13, 2022 RX SPRAY, METERED NASAL Jan. 13, 2025 NEW PRODUCT

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histamine H1 receptor GPCR ANTAGONIST Ki 8.28 WOMBAT-PK CHEMBL
Histamine H1 receptor GPCR Ki 7.80 CHEMBL

External reference:

IDSource
4021024 VUID
N0000148491 NUI
D01192 KEGG_DRUG
140462-76-6 SECONDARY_CAS_RN
4021024 VANDF
4021040 VANDF
C0527189 UMLSCUI
CHEBI:7769 CHEBI
CHEMBL1189432 ChEMBL_ID
DB00768 DRUGBANK_ID
CHEMBL1719 ChEMBL_ID
D000069605 MESH_DESCRIPTOR_UI
5281071 PUBCHEM_CID
7249 IUPHAR_LIGAND_ID
7257 INN_ID
D27V6190PM UNII
135391 RXNORM
10342 MMSL
107496 MMSL
230004 MMSL
5199 MMSL
006403 NDDF
006404 NDDF
108843008 SNOMEDCT_US
108845001 SNOMEDCT_US
372550002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
PATANASE HUMAN PRESCRIPTION DRUG LABEL 1 0065-0332 SPRAY, METERED 600 ug NASAL NDA 29 sections
PATANASE HUMAN PRESCRIPTION DRUG LABEL 1 0065-0332 SPRAY, METERED 600 ug NASAL NDA 29 sections
PATADAY ONCE DAILY RELIEF HUMAN OTC DRUG LABEL 1 0065-0816 SOLUTION 7 mg OPHTHALMIC NDA 12 sections
PATADAY ONCE DAILY RELIEF HUMAN OTC DRUG LABEL 1 0065-0816 SOLUTION 7 mg OPHTHALMIC NDA 12 sections
Pazeo HUMAN PRESCRIPTION DRUG LABEL 1 0065-4273 SOLUTION 7 mg OPHTHALMIC NDA 22 sections
PATADAY TWICE A DAY RELIEF HUMAN OTC DRUG LABEL 1 0065-4274 SOLUTION 1 mg OPHTHALMIC NDA 12 sections
PATADAY TWICE A DAY RELIEF HUMAN OTC DRUG LABEL 1 0065-4274 SOLUTION 1 mg OPHTHALMIC NDA 12 sections
PATADAY ONCE DAILY RELIEF HUMAN OTC DRUG LABEL 1 0065-8150 SOLUTION 2 mg OPHTHALMIC NDA 12 sections
PATADAY ONCE DAILY RELIEF HUMAN OTC DRUG LABEL 1 0065-8150 SOLUTION 2 mg OPHTHALMIC NDA 12 sections
PATANASE HUMAN PRESCRIPTION DRUG LABEL 1 0078-0834 SPRAY, METERED 600 ug NASAL NDA 29 sections
PATANASE HUMAN PRESCRIPTION DRUG LABEL 1 0078-0834 SPRAY, METERED 600 ug NASAL NDA 29 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 Ophthalmic Solution Human OTC Drug Label 1 0363-7130 SOLUTION/ DROPS 1 mg OPHTHALMIC ANDA 13 sections
Olopatadine Hydrochloride Ophthalmic Solution Human OTC Drug Label 1 0363-7131 SOLUTION 2 mg OPHTHALMIC ANDA 11 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 0536-1307 SOLUTION 2 mg OPHTHALMIC ANDA 11 sections
Olopatadine Hydrochloride Ophthalmic Solution Human OTC Drug Label 1 0536-1307 SOLUTION 2 mg OPHTHALMIC ANDA 11 sections
Olopatadine Hydrochloride Ophthalmic Solution Human OTC Drug Label 1 0536-1308 SOLUTION/ DROPS 1 mg OPHTHALMIC ANDA 13 sections
Olopatadine Hydrochloride Ophthalmic Solution Human OTC Drug Label 1 0536-1308 SOLUTION/ DROPS 1 mg OPHTHALMIC ANDA 13 sections
Olopatadine Hydrochloride Ophthalmic Solution Human OTC Drug Label 1 11673-688 SOLUTION 2 mg OPHTHALMIC ANDA 11 sections
Olopatadine Hydrochloride Ophthalmic Solution Human OTC Drug Label 1 11673-689 SOLUTION/ DROPS 1 mg OPHTHALMIC ANDA 13 sections
Olopatadine Hydrochloride Ophthalmic Solution Human OTC Drug Label 1 11822-9975 SOLUTION 2 mg OPHTHALMIC ANDA 11 sections
Olopatadine Hydrochloride Ophthalmic Solution Human OTC Drug Label 1 11822-9976 SOLUTION/ DROPS 1 mg OPHTHALMIC ANDA 13 sections
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