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) 2 mg/mL Benet LZ, Broccatelli F, Oprea TI
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 1713.34 14.76 704 8274 136933 50459213
Eye irritation 110.34 14.76 56 8922 17084 50579062
Eye pruritus 55.60 14.76 32 8946 12502 50583644
Asthma 47.04 14.76 68 8910 89269 50506877
Ocular hyperaemia 41.56 14.76 32 8946 20260 50575886
Sinusitis 37.47 14.76 89 8889 170469 50425677
Conjunctivitis allergic 33.76 14.76 10 8968 708 50595438
Dry eye 32.50 14.76 34 8944 32061 50564085
Urticarial vasculitis 31.36 14.76 9 8969 570 50595576
Eye discharge 30.81 14.76 16 8962 5107 50591039
Eyelid margin crusting 29.33 14.76 9 8969 719 50595427
Upper respiratory tract inflammation 28.55 14.76 12 8966 2377 50593769
Hepatic function abnormal 25.14 14.76 30 8948 32651 50563495
Toxicity to various agents 24.79 14.76 4 8974 212495 50383651
Product packaging quantity issue 22.05 14.76 8 8970 1072 50595074
Eye pain 20.07 14.76 25 8953 28424 50567722
Eye swelling 19.78 14.76 21 8957 20123 50576023
Vision blurred 19.40 14.76 43 8935 78604 50517542
Infusion site swelling 18.49 14.76 13 8965 7163 50588983
Foreign body sensation in eyes 18.04 14.76 8 8970 1803 50594343
Adrenal insufficiency 17.94 14.76 17 8961 14226 50581920
Eye allergy 17.22 14.76 6 8972 715 50595431
Drug intolerance 16.75 14.76 9 8969 219095 50377051
Maternal exposure during pregnancy 16.55 14.76 4 8974 159774 50436372
Arthropathy 16.26 14.76 4 8974 157902 50438244
Lichenification 16.06 14.76 5 8973 419 50595727
Cholangitis 15.92 14.76 10 8968 4569 50591577
Systemic lupus erythematosus 15.62 14.76 3 8975 140619 50455527

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 818.70 20.49 264 3425 36675 29534163
Eye irritation 56.98 20.49 23 3666 5875 29564963
Asthma 39.19 20.49 33 3656 33816 29537022
Drug eruption 31.95 20.49 22 3667 16719 29554119
Cerebral infarction 30.51 20.49 25 3664 24650 29546188
Rash 29.85 20.49 70 3619 189749 29381089
Alopecia areata 26.93 20.49 6 3683 194 29570644
Hypersensitivity 26.81 20.49 33 3656 52870 29517968
Pruritus 25.15 20.49 49 3640 116800 29454038
Hepatic function abnormal 22.36 20.49 26 3663 39233 29531605

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 65.73 14.00 74 9051 95151 64394456
Hepatic function abnormal 51.38 14.00 54 9071 64259 64425348
Drug eruption 41.40 14.00 37 9088 36099 64453508
Upper respiratory tract inflammation 35.55 14.00 15 9110 3767 64485840
Alopecia areata 32.45 14.00 11 9114 1517 64488090
Platelet count decreased 30.67 14.00 71 9054 167640 64321967
Eye irritation 30.49 14.00 22 9103 15834 64473773
Cerebral infarction 30.19 14.00 33 9092 41011 64448596
Interstitial lung disease 29.47 14.00 51 9074 97681 64391926
Neutrophil count decreased 28.29 14.00 44 9081 77152 64412455
Adrenal insufficiency 25.70 14.00 23 9102 22464 64467143
Ocular hyperaemia 25.63 14.00 23 9102 22541 64467066
Urticaria 25.44 14.00 61 9064 147256 64342351
Erythema multiforme 24.02 14.00 19 9106 15682 64473925
Sinusitis 21.61 14.00 57 9068 145871 64343736
Urticarial vasculitis 21.33 14.00 6 9119 445 64489162
Pyrexia 21.05 14.00 143 8982 558501 63931106
Conjunctivitis allergic 20.25 14.00 7 9118 1023 64488584
Pruritus 19.04 14.00 91 9034 312309 64177298
Completed suicide 17.55 14.00 5 9120 224409 64265198
Dry eye 17.40 14.00 21 9104 28998 64460609
Drug intolerance 17.08 14.00 3 9122 187989 64301618
Eczema 17.00 14.00 21 9104 29699 64459908
Dermatitis atopic 16.74 14.00 9 9116 3867 64485740
Malaise 16.46 14.00 104 9021 396143 64093464
Rash 16.43 14.00 116 9009 458433 64031174
Eye pain 15.96 14.00 21 9104 31604 64458003
Anaphylactic reaction 15.89 14.00 32 9093 68632 64420975
Headache 15.64 14.00 128 8997 529339 63960268
Concomitant disease aggravated 15.61 14.00 13 9112 11529 64478078
Bronchitis 15.60 14.00 42 9083 108701 64380906
Lichenification 14.70 14.00 5 9120 697 64488910
Eyelid margin crusting 14.59 14.00 5 9120 713 64488894
Cholangitis 14.26 14.00 12 9113 10790 64478817
Nasopharyngitis 14.09 14.00 60 9065 196013 64293594

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 (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
0.665MG/SPRAY PATANASE NOVARTIS N021861 April 15, 2008 RX SPRAY, METERED NASAL 8399508 Sept. 17, 2022 ALLERGIC RHINITIS
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 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
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 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
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 0536-1308 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
Olopatadine Hydrochloride Ophthalmic Solution Human OTC Drug Label 1 21130-105 SOLUTION 2 mg OPHTHALMIC ANDA 12 sections
OLOPATADINE HYDROCHLORIDE Human OTC Drug Label 1 30142-026 SOLUTION 2 mg OPHTHALMIC ANDA 13 sections
OLOPATADINE HYDROCHLORIDE Human OTC Drug Label 1 30142-064 SOLUTION 1 mg OPHTHALMIC ANDA 13 sections
Once Daily Relief Human OTC Drug Label 1 37808-045 SOLUTION 2 mg OPHTHALMIC ANDA 12 sections
Olopatadine Hydrochloride Ophthalmic Solution Human OTC Drug Label 1 43598-764 SOLUTION 2 mg OPHTHALMIC ANDA 12 sections
Olopatadine Hydrochloride Ophthalmic Solution Human OTC Drug Label 1 43598-765 SOLUTION/ DROPS 1 mg OPHTHALMIC ANDA 14 sections