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 |
|---|---|
|
Synonyms:
|
An antihistamine with mast-cell stabilizing properties used as eye drops in the treatment of ALLERGIC CONJUNCTIVITIS.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 18, 1996 | FDA | ALCON |
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 |
|---|---|---|---|---|---|---|
| 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 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 | 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 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 | 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:
| 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 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)
| 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 |
🐶 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)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 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 |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | GPCR | ANTAGONIST | Ki | 8.28 | WOMBAT-PK | CHEMBL | |||
| Histamine H1 receptor | GPCR | Ki | 7.80 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |