olopatadine hydrochloride 665 ug Spray
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Histamine-1 Receptor Inhibitor class.
Where does this data come from?
🏭 Manufacturer & labeler
Where does this data come from?
🩺 Clinical
Olopatadine nasal spray is used to relieve sneezing and a stuffy, runny or itchy nose caused by allergic rhinitis (hay fever). Olopatadine is in a class of medications called antihistamines. It works by blocking the effects of histamine, a substance in the body that causes allergy symptoms.
Read the full MedlinePlus article ↗- It does both, but with different products. The eye drops are for allergy-related itchy and red eyes. The nasal spray — brands like Patanase — is for seasonal allergic rhinitis, mea...
- What exactly does olopatadine treat — is it just for eyes, or can it help my runny nose too?
- You need to take your contacts out before you put the drops in. Wait at least 10 minutes after using the drops before you put them back in. Also, don't wear contacts at all if your...
- Can I wear my contact lenses while using olopatadine eye drops?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Olopatadine Hydrochloride — tap one for details:
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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UNII F5UM2KM3W7
Benzalkonium chloride is a chemical compound that works as a preservative and antimicrobial agent in medications. It prevents bacterial and fungal growth in liquid formulations to keep the product safe during storage and use.
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UNII 7FLD91C86K
Edetate disodium is a chemical compound that binds and removes certain metal ions. In medicines, it acts as a preservative and stabilizer by preventing metals like calcium from interfering with the product's shelf life and consistency.
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UNII QTT17582CB
A strong acid used to adjust and maintain the proper pH level in liquid medicines, ensuring stability and preventing breakdown of active ingredients.
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UNII 451W47IQ8X
Sodium chloride is common table salt. It's used in medicines as a buffer to maintain proper pH, as a filler to add bulk, or to adjust the osmotic balance in liquid formulations.
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UNII 55X04QC32I
A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
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UNII GR686LBA74
Sodium phosphate, dibasic is a salt derived from phosphoric acid. It acts as a buffer to help maintain the medicine's pH balance and may serve as a binder or filler in tablets and capsules.
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UNII 059QF0KO0R
Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
7 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $2.07 | — |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| olopatadine hydrochloride 665 ug 45802-0104-01 | Padagis | 1 bottle | $0.868 | AB | Availability likely | — |
| Olopatadine Hydrochloride 665 ug 60505-0845-05 | Apotex | 1 bottle | $0.868 | AB | Availability likely | — |
| Olopatadine Hydrochloride 665 ug 65162-0890-23 | Amneal | 1 bottle | $0.868 | AB | Availability likely | — |
| olopatadine hydrochloride 665 ugthis 63629-8434-01 | Bryant | 1 bottle | — | AB | FDA listed | — |
| olopatadine hydrochloride 665 ug 72162-1390-02 | Bryant | 1 bottle | — | AB | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 63629-8434-01 You're viewing this | 1 BOTTLE in 1 CARTON (63629-8434-1) / 240 SPRAY in 1 BOTTLE | 2021-04-28 | Active |
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
Questions about this listing
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Olopatadine hydrochloride nasal solution (nasal spray) is indicated for the relief of the symptoms of seasonal allergic rhinitis in adults and pediatric patients 6 years of age and older. Olopatadine hydrochloride nasal solution (nasal spray) is an H 1 receptor antagonist indicated for the relief of the symptoms of seasonal allergic rhinitis in adults and pediatric patients 6 years of age and older.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION For nasal use only. Recommended dosages: • Adults and Adolescents ≥ 12 Years : Two sprays per nostril (665 mcg per spray) twice daily ( 2.1 ). • Pediatric Patients 6 to 11 Years : One spray per nostril (665 mcg per spray) twice daily ( 2.2 ). • Priming Information : Prime olopatadine hydrochloride nasal solution (nasal spray) before initial use and when olopatadine hydrochloride nasal solution (nasal spray) has not been used for more than 7 days ( 2.3 ).
2.1Adults and Adolescents Twelve Years of Age and Older The recommended dosage is two sprays per nostril twice daily.
2.2Pediatric Patients Six to Eleven Years of Age The recommended dosage is one spray per nostril twice daily.
2.3Administration Information Administer olopatadine hydrochloride nasal solution (nasal spray) by the nasal route only. Priming : Before initial use, prime olopatadine hydrochloride nasal solution (nasal spray) by releasing 5 sprays or until a fine mist appears. The correct amount of medication cannot be assured before the initial priming.
Re-priming (as needed): When olopatadine hydrochloride nasal solution (nasal spray) has not been used for more than 7 days, re-prime by releasing 2 sprays. Avoid spraying olopatadine hydrochloride nasal solution (nasal spray) into the eyes. Discard Instructions : Discard nasal device after 240 sprays (enough for 30 days of dosing) have been used even though the bottle is not completely empty.
The correct amount of medication cannot be assured after 240 sprays have been used.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Nasal spray: 665 mcg olopatadine hydrochloride per spray supplied in a white plastic bottle with a metered-dose manual spray pump, a white nasal applicator, a blue overcap and a blue clip. Nasal spray: 665 mcg of olopatadine hydrochloride in each spray ( 3 ).
⛔ Contraindications ▾
4 CONTRAINDICATIONS None. None ( 4 ).
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Epistaxis, Nasal Ulceration, and Nasal Septal Perforation : Monitor patients periodically for signs of adverse effects on the nasal mucosa. Discontinue if ulcerations or perforations occur. Avoid use in patients with nasal disease other than allergic rhinitis ( 5.1 ). • Avoid engaging in hazardous occupations requiring complete mental alertness and coordination, such as driving or operating machinery when taking olopatadine hydrochloride nasal solution (nasal spray) ( 5.2 ). • Avoid concurrent use of alcohol or other central nervous system depressants with olopatadine hydrochloride nasal solution (nasal spray) ( 5.2 ).
5.1Local Nasal Effects Epistaxis and Nasal Ulceration In placebo-controlled clinical trials (vehicle nasal spray) of 2 weeks to 12 months duration, epistaxis and nasal ulcerations were reported [ see Adverse Reactions 6.1 ]. Nasal Septal Perforation Three placebo-controlled long term (12 months) safety trials (vehicle nasal spray) were conducted. In the first safety trial, patients were treated with an investigational formulation of olopatadine hydrochloride nasal solution (nasal spray) containing povidone (not the commercially marketed formulation) or a vehicle nasal spray containing povidone.
Nasal septal perforations were reported in one patient treated with the investigational formulation of olopatadine hydrochloride nasal solution (nasal spray) and 2 patients treated with the vehicle nasal spray. In the second safety trial with olopatadine hydrochloride nasal solution (nasal spray), which does not contain povidone, there were no reports of nasal septal perforation. In the third safety trial, one patient exposed to the 3.7 pH vehicle nasal spray (containing no povidone) reported a nasal septal perforation [ see Adverse Reactions ( 6.1 ) ].
Before starting olopatadine hydrochloride nasal solution (nasal spray), conduct a nasal examination to ensure that patients are free of nasal disease other than allergic rhinitis. Perform nasal examinations periodically for signs of adverse effects on the nasal mucosa and consider stopping olopatadine hydrochloride nasal solution (nasal spray) if patients develop nasal ulcerations.
5.2Somnolence and Impaired Mental Alertness In clinical trials, the occurrence of somnolence has been reported in some patients taking olopatadine hydrochloride nasal solution (nasal spray) [ see Adverse Reactions ( 6.1 ) ]. Patients should be cautioned against engaging in hazardous occupations requiring complete mental alertness and motor coordination such as driving or operating machinery after administration of olopatadine hydrochloride nasal solution (nasal spray). Concurrent use of olopatadine hydrochloride nasal solution (nasal spray) with alcohol or other central nervous system depressants should be avoided because additional reductions in alertness and additional impairment of central nervous system performance may occur.
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The most clinically significant adverse reactions described in other sections of labeling include: • Epistaxis, Nasal Ulceration, and Nasal Septal Perforation [ see Warnings and Precautions ( 5.1 ) ] • Somnolence and Impaired Mental Alertness [ see Warnings and Precautions ( 5.2 ) ] The most common (>1%) adverse reactions, included bitter taste, headache, epistaxis, pharyngolaryngeal pain, post-nasal drip, cough, and urinary tract infection in patients 12 years of age and older and epistaxis, headache, upper respiratory tract infection, bitter taste, pyrexia, and rash in patients 6 to 11 years of age ( 6.1 ).
To report SUSPECTED ADVERSE REACTIONS, contact Perrigo at 1-866-634-9120 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety data described below reflect exposure to olopatadine hydrochloride nasal solution (nasal spray) in 2770 patients with seasonal or perennial allergic rhinitis in 10 controlled clinical trials of 2 weeks to 12 months duration.
Olopatadine hydrochloride nasal solution (nasal spray) is not indicated for use in patients with perennial allergic rhinitis. The safety data from adults and adolescents are based upon 6 placebo-controlled clinical trials (3.7 pH vehicle nasal spray or 7.0 pH vehicle nasal spray) in which 1834 patients with seasonal or perennial allergic rhinitis (652 males and 1182 females) 12 years of age and older were treated with olopatadine hydrochloride nasal solution (nasal spray) two sprays per nostril twice daily. There were 1180 patients (olopatadine hydrochloride nasal solution (nasal spray), 587; vehicle nasal spray, 593) that participated in 3 efficacy and safety trials of 2 weeks duration.
There were 2840 patients (olopatadine hydrochloride nasal solution (nasal spray), 1247; 3.7 pH vehicle nasal spray, 1251; 7.0 pH vehicle nasal spray, 342) that participated in 3 long-term clinical trials of 1-year duration. The racial distribution of adult and adolescent patients receiving olopatadine hydrochloride nasal solution (nasal spray) was 77% white, 9% black, and 14% other. The incidence of discontinuation due to adverse reactions in these controlled clinical trials was comparable for olopatadine hydrochloride nasal solution (nasal spray) and vehicle nasal spray.
Overall, 4.7% of the 1834 adult and adolescent patients across all 6 studies treated with olopatadine hydrochloride nasal solution (nasal spray), 3.5% of the 1844 patients treated with 3.7 pH vehicle nasal spray discontinued due to adverse reactions, and 2.9% of the 342 patients treated with 7.0 pH vehicle nasal spray discontinued due to adverse reactions. The safety data from pediatric patients 6 to 11 years of age are based upon 3 clinical trials in which 870 children with seasonal allergic rhinitis (376 females and 494 males) were treated with olopatadine hydrochloride nasal solution (nasal spray) one or two sprays per nostril twice daily for 2 weeks.
The racial distribution of pediatric patients receiving olopatadine hydrochloride nasal solution (nasal spray) was 68.6% white, 16.6% black, and 14.8% other. The incidence of discontinuation due to adverse reactions in these controlled clinical trials was comparable for olopatadine hydrochloride nasal solution (nasal spray) and vehicle nasal spray. Overall, 1.4% of the 870 pediatric patients across all 3 studies treated with olopatadine hydrochloride nasal solution (nasal spray) and 1.3% of the 872 pediatric patients treated with vehicle nasal spray discontinued due to adverse reactions.
Adults and Adolescents 12 Years of Age and Older in Short-Term (2-week) Trials There were 1180 patients 12 years of age and older (olopatadine hydrochloride nasal solution (n…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Formal drug-drug interaction studies were not conducted for olopatadine hydrochloride nasal solution (nasal spray). Drug interactions with inhibitors of liver enzymes are not anticipated because olopatadine is eliminated predominantly by renal excretion. Drug interactions involving P450 inhibition and plasma protein binding are also not expected. [ See Clinical Pharmacology ( 12.3 ) ].
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Risk Summary Published data from postmarketing experience with antihistamines, with similar mechanism of action to olopatadine hydrochloride nasal solution (nasal spray), have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. However, there are no published human data specific to olopatadine hydrochloride nasal solution (nasal spray). In animal reproductive studies, oral administration of olopatadine hydrochloride to pregnant rats and rabbits caused a decrease in the number of live fetuses at maternal doses approximately 110 and 1460 times the maximum recommended human daily intranasal dose (MRHDID) on a mg/m 2 basis, respectively (see Data) .
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss or other adverse outcomes. In the U.S. general population, the background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4%, and 15% to 20%, respectively.
Data Animal Data In an oral embryo-fetal development study, pregnant rabbits were dosed throughout the period of organogenesis at doses up to 400 mg/kg/day. A decrease in the number of live fetuses was observed at 400 mg/kg/day (1460 times the MRHDID, on a mg/m 2 basis). In an oral embryo-fetal development study, pregnant rats were dosed throughout the period of organogenesis at doses up to 600 mg/kg/day.
Maternal toxicity, producing death and reduced maternal body weight gain was observed at 600 mg/kg/day (approximately 1100 times the MRHDID on a mg/m 2 basis). Olopatadine produced cleft palate at 60 mg/kg/day (approximately 110 times the MRHDID on a mg/m 2 basis) and decreased embryo-fetal viability and reduced fetal weight in rats at 600 mg/kg/day (approximately 1100 times the MRHDID on a mg/m 2 basis). In peri-/postnatal toxicity studies, pregnant rats received oral doses of olopatadine up to 600 mg/kg/day during late gestation and throughout the lactation period.
Olopatadine produced decreased neonatal survival at 60 mg/kg/day (approximately 110 times the MRHDID on a mg/m 2 basis) and reduced body weight gain in pups at 4 mg/kg/day (approximately 7 times the MRHDID on a mg/m 2 basis). These effects appeared attributable to exposure of pups via the milk as demonstrated in a cross-fostered study in which pups of untreated dams cross-fostered to dams treated with 60 mg/kg/day olopatadine orally during the lactation period exhibited decreased body weight gain.
8.2Lactation Risk Summary There are no data on the presence of olopatadine in human milk, the effects on the breastfed infant, or the effects on milk production. Although orally administered olopatadine is present in rat milk, there is no information about nasally administered olopatadine. It is not known whether topical nasal administration could result in sufficient systemic absorption to produce detectable quantities in human breast milk.
The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for olopatadine hydrochloride nasal solution (nasal spray) and any potential adverse effects on the breast fed infant from olopatadine hydrochloride nasal solution (nasal spray) or from the underlying maternal condition.
8.4Pediatric Use The safety and effectiveness of olopatadine hydrochloride nasal solution (nasal spray) for the relief of symptoms of seasonal allergic rhinitis have been established in pediatric patients aged 6 years and older. The safety and effectiveness of olopatadine hydrochloride nasal solution (nasal spray) in pediatric patients 6 to 11 years of age are supported by 3 vehicle-controlled 2-week studies in 870 patients [ see Adverse Reactions ( 6.1 ) ]. Doses studied included one and two sprays per nostril twice daily.
One of these studies evaluated the safety of olopatadine hydrochloride n…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Published data from postmarketing experience with antihistamines, with similar mechanism of action to olopatadine hydrochloride nasal solution (nasal spray), have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. However, there are no published human data specific to olopatadine hydrochloride nasal solution (nasal spray). In animal reproductive studies, oral administration of olopatadine hydrochloride to pregnant rats and rabbits caused a decrease in the number of live fetuses at maternal doses approximately 110 and 1460 times the maximum recommended human daily intranasal dose (MRHDID) on a mg/m 2 basis, respectively (see Data) .
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss or other adverse outcomes. In the U.S. general population, the background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4%, and 15% to 20%, respectively.
Data Animal Data In an oral embryo-fetal development study, pregnant rabbits were dosed throughout the period of organogenesis at doses up to 400 mg/kg/day. A decrease in the number of live fetuses was observed at 400 mg/kg/day (1460 times the MRHDID, on a mg/m 2 basis). In an oral embryo-fetal development study, pregnant rats were dosed throughout the period of organogenesis at doses up to 600 mg/kg/day.
Maternal toxicity, producing death and reduced maternal body weight gain was observed at 600 mg/kg/day (approximately 1100 times the MRHDID on a mg/m 2 basis). Olopatadine produced cleft palate at 60 mg/kg/day (approximately 110 times the MRHDID on a mg/m 2 basis) and decreased embryo-fetal viability and reduced fetal weight in rats at 600 mg/kg/day (approximately 1100 times the MRHDID on a mg/m 2 basis). In peri-/postnatal toxicity studies, pregnant rats received oral doses of olopatadine up to 600 mg/kg/day during late gestation and throughout the lactation period.
Olopatadine produced decreased neonatal survival at 60 mg/kg/day (approximately 110 times the MRHDID on a mg/m 2 basis) and reduced body weight gain in pups at 4 mg/kg/day (approximately 7 times the MRHDID on a mg/m 2 basis). These effects appeared attributable to exposure of pups via the milk as demonstrated in a cross-fostered study in which pups of untreated dams cross-fostered to dams treated with 60 mg/kg/day olopatadine orally during the lactation period exhibited decreased body weight gain.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of olopatadine hydrochloride nasal solution (nasal spray) for the relief of symptoms of seasonal allergic rhinitis have been established in pediatric patients aged 6 years and older. The safety and effectiveness of olopatadine hydrochloride nasal solution (nasal spray) in pediatric patients 6 to 11 years of age are supported by 3 vehicle-controlled 2-week studies in 870 patients [ see Adverse Reactions ( 6.1 ) ]. Doses studied included one and two sprays per nostril twice daily.
One of these studies evaluated the safety of olopatadine hydrochloride nasal solution (nasal spray) at doses of one and two sprays per nostril twice daily in 1,188 patients, of which 298 patients were exposed to olopatadine hydrochloride nasal solution (nasal spray) 1 spray and 297 patients were exposed to vehicle 1 spray. In this study, the incidence of epistaxis with olopatadine hydrochloride nasal solution (nasal spray) use was 5.7% [see Adverse Reactions ( 6.1 ), Clinical Studies ( 14 )]. The safety and effectiveness of olopatadine hydrochloride nasal solution (nasal spray) in pediatric patients aged 12 years and older are supported by 3 randomized, double blind, parallel group, multicenter, placebo-controlled clinical trials of 2 weeks duration in adult and adolescent patients [see Clinical Studies ( 14 )] .
In these studies, the incidence of epistaxis with olopatadine hydrochloride nasal solution (nasal spray) use in 587 patients was 3.2% [see Adverse Reactions ( 6.1 )] . The safety and effectiveness of olopatadine hydrochloride nasal solution (nasal spray) have not been established in pediatric patients under 6 years of age. The safety of olopatadine hydrochloride nasal solution (nasal spray) at a dose of one spray per nostril twice daily was evaluated in one 2-week vehicle-controlled study in 132 pediatric patients 2 to 5 years of age with allergic rhinitis.
In this trial, 66 patients were exposed to olopatadine hydrochloride nasal solution (nasal spray). The most common (greater than 1.0%) adverse reactions reported were diarrhea (9.1%), epistaxis (6.1%), rhinorrhea (4.5%), bitter taste (3.0%) and wheezing (3.0%). Diarrhea was reported more frequently (9.1%) in patients 2 to 5 years of age than 6 to 11 year old age group (< 1%).
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical studies of olopatadine hydrochloride nasal solution (nasal spray) did not include sufficient numbers of patients aged 65 years and older to determine whether they respond differently from younger patients. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy.
🆘 Overdosage ▾
10 OVERDOSAGE Symptoms of antihistamine overdose may include drowsiness in both adults and children. Agitation and restlessness followed by drowsiness may also occur in children. There is no known specific antidote to olopatadine hydrochloride nasal solution (nasal spray).
Should overdose occur, symptomatic or supportive treatment is recommended, taking into account any concomitantly ingested medications. For additional information about overdose treatment, call a poison control center (1-800-222-1222).
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Olopatadine is a histamine H 1 receptor antagonist. The antihistaminic activity of olopatadine has been documented in isolated tissues, animal models, and humans.
12.2Pharmacodynamics Cardiac Electrophysiology In a placebo-controlled cardiovascular safety study, 32 healthy volunteers received 20 mg oral solution of olopatadine twice daily for 14 days (8-fold greater daily dose than the recommended daily nasal dose). The mean QTcF (QT corrected by Fridericia’s correction method for heart rate) change from baseline was -2.7 msec and -3.8 msec for olopatadine, and placebo, respectively. In this study, 8 subjects treated with olopatadine had a QTcF change from baseline of 30-60 msec, 1 subject had a QTcF change from baseline greater than 60 msec, and no subjects had QTcF values greater than 500 msec.
Eight subjects treated with placebo had a QTcF change from baseline of 30-60 msec, no subjects had a QTcF change from baseline greater than 60 msec, and no subjects had QTcF values greater than 500 msec. In a 12-month study in 429 perennial allergic rhinitis patients treated with olopatadine hydrochloride nasal solution (nasal spray) two sprays per nostril twice daily, no evidence of any effect of olopatadine hydrochloride on QT prolongation was observed.
12.3Pharmacokinetics The pharmacokinetic properties of olopatadine were studied after administration by the nasal, oral, intravenous, and topical ocular routes. Olopatadine exhibited linear pharmacokinetics across the routes studied over a large dose range. Absorption Healthy Subjects: Olopatadine was absorbed with individual peak plasma concentrations observed between 30 minutes and 1 hour after twice daily intranasal administration of olopatadine hydrochloride nasal solution (nasal spray).
The mean ( ± SD) steady-state peak plasma concentration (C max ) of olopatadine was 16.0 ± 8.99 ng/mL. Systemic exposure as indexed by area under the curve (AUC 0-12 ) averaged 66.0 ± 26.8 ng·h/mL. The average absolute bioavailability of intranasal olopatadine is 57%.
The mean accumulation ratio following multiple intranasal administration of olopatadine hydrochloride nasal solution (nasal spray) was about 1.3. Seasonal Allergic Rhinitis Patients: Systemic exposure of olopatadine in seasonal allergic rhinitis SAR patients after twice daily intranasal administration of olopatadine hydrochloride nasal solution (nasal spray) was comparable to that observed in healthy subjects. Olopatadine was absorbed with peak plasma concentrations observed between 15 minutes and 2 hours.
The mean steady-state C max was 23.3 ± 6.2 ng/mL and AUC 0-12 averaged 78.0 ± 13.9 ng·h/mL. Distribution The protein binding of olopatadine was moderate at approximately 55% in human serum, and independent of drug concentration over the range of 0.1 to 1000 ng/mL. Olopatadine was bound predominately to human serum albumin.
Elimination The plasma elimination half-life of olopatadine is 8 to 12 hours. Olopatadine is mainly eliminated through urinary excretion. Approximately 70% of a [ 14 C] olopatadine hydrochloride oral dose was recovered in urine with 17% in the feces.
Of the drug-related material recovered within the first 24 hours in the urine, 86% was unchanged olopatadine with the balance comprised of olopatadine N-oxide and N-desmethyl olopatadine. Metabolism Olopatadine is not extensively metabolized. Based on plasma metabolite profiles following oral administration of [ 14 C] olopatadine, at least six minor metabolites circulate in human plasma.
Olopatadine accounts for 77% of peak plasma total radioactivity and all metabolites amounted to <6% combined. Two of these have been identified as the olopatadine N-oxide and N-desmethyl olopatadine. In in vitro studies with cDNA-expressed human cytochrome P450 isoenzymes (CYP) and flavin-containing monooxygenases (FMO), N-desmethyl olopatadine (Ml) formation was catalyzed mainly by CYP3A4, while olopatadine N-oxide (M3) was primar…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Olopatadine is a histamine H 1 receptor antagonist. The antihistaminic activity of olopatadine has been documented in isolated tissues, animal models, and humans.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied Olopatadine Hydrochloride Nasal Solution (Nasal Spray), 665 mcg is supplied in a white plastic bottle with a metered-dose manual spray pump, a white nasal applicator, a blue overcap and a blue clip in a box of 1 (NDC 63629-8434-1). Each trade size bottle contains 30.5 g of clear, colorless liquid and will provide 240 metered sprays. After priming [ see Dosage and Administration (2.3) ], each spray delivers a fine mist containing 665 mcg of olopatadine hydrochloride in 100 µL of formulation through the nozzle.
Net content 30.5 g, 240 sprays: NDC 63629-8434-1 (trade size) Storage Store olopatadine hydrochloride nasal solution (nasal spray) at room temperature between 4°C to 25°C (39°F to 77°F). Repackaged/Relabeled by: Bryant Ranch Prepack, Inc. Burbank, CA 91504
📋 Description ▾
11 DESCRIPTION Olopatadine hydrochloride nasal solution (nasal spray), 665 mcg is a metered-spray solution for nasal administration. Olopatadine hydrochloride, the active component of olopatadine hydrochloride nasal solution (nasal spray), is a white, water-soluble crystalline powder. The chemical name for olopatadine hydrochloride is (Z)-11-[3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride.
It has a molecular weight of 373.88 g/mol, and its molecular formula is C 21 H 23 NO 3 • HCl with the following chemical structure: Olopatadine hydrochloride nasal solution (nasal spray) contains 0.6% w/v olopatadine (base) in a nonsterile aqueous solution with pH of approximately 3.7. After initial priming (5 sprays), each metered spray from the nasal applicator delivers 100 µL of the aqueous solution containing 665 mcg of olopatadine hydrochloride, which is equivalent to 600 mcg of olopatadine (base) [ see Dosage Forms and Strengths ( 3 ) ] .
Olopatadine hydrochloride nasal solution (nasal spray) also contains benzalkonium chloride (0.01%), dibasic sodium phosphate, edetate disodium, hydrochloric acid and/or sodium hydroxide (to adjust pH), purified water and sodium chloride.
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information and Instructions for Use). Local Nasal Effects and Other Common Adverse Reactions Inform patients that treatment with olopatadine hydrochloride nasal solution (nasal spray) may lead to adverse reactions, which include epistaxis and nasal ulcerations [ see Warnings and Precautions ( 5.1 ) ]. Other common adverse reactions reported with use of olopatadine hydrochloride nasal solution (nasal spray) include bitter taste, headache, and pharyngolaryngeal pain [ see Adverse Reactions ( 6 ) ].
Somnolence and Impaired Mental Alertness Somnolence has been reported in some patients taking olopatadine hydrochloride nasal solution (nasal spray). Caution patients against engaging in hazardous occupations requiring complete mental alertness and motor coordination, such as driving or operating machinery after administration of olopatadine hydrochloride nasal solution (nasal spray) [ see Warnings and Precautions ( 5.2 ) ]. Concurrent Use of Alcohol and Other Central Nervous System Depressants Advise patients that concurrent use of olopatadine hydrochloride nasal solution (nasal spray) with alcohol or other central nervous system depressants should be avoided because additional reductions in alertness and additional impairment of central nervous system performance may occur [ see Warnings and Precautions ( 5.2 ) ].
Keep Spray Out of Eyes Inform patients to avoid spraying olopatadine hydrochloride nasal solution (nasal spray) in their eyes [ see Dosage and Administration ( 2.3 ) ]. Made in Israel Manufactured by Perrigo Yeruham, Israel Distributed By Perrigo Allegan, MI 49010 ● www.perrigorx.com Rev 06-21 4S000 RC J3