section name header

Introduction

ATC Class:S01GX09

VA Class:OP900

VA Class:NT400

AHFS Class:

Generic Name(s):

Chemical Name:

Molecular Formula:

Olopatadine hydrochloride is a relatively selective histamine H1-receptor antagonist;1,  2,  3,  4,  5,  6 the drug also shares many of the pharmacologic effects of mast-cell stabilizers.1,  2,  3,  4,  5,  6

Uses

Allergic Conjunctivitis

Olopatadine ophthalmic solution is used for the symptomatic management of ocular itching associated with allergic conjunctivitis.1,  2,  13,  16

Efficacy of olopatadine has been established in several clinical studies, including environmental studies and conjunctival antigen challenge studies.1,  16 In a 6-week environmental study, twice-daily administration of olopatadine 0.1% ophthalmic solution was shown to be effective in improving manifestations of allergic conjunctivitis.1 In addition, results of several conjunctival antigen challenge studies indicate that in healthy individuals who were challenged with conjunctival antigen initially and 8 hours after receiving olopatadine 0.1% ophthalmic solution or vehicle, olopatadine was more effective than vehicle in providing relief of ocular itching1,  13,  14,  15 and redness2,  13,  14,  15 associated with allergic conjunctivitis.1,  2,  13,  14,  15 In clinical studies of up to 12 weeks' duration, once-daily administration of olopatadine 0.2% ophthalmic solution was shown to be effective in improving ocular itching associated with allergic conjunctivitis.16 Ophthalmic olopatadine generally provides symptomatic relief of itching within 30 minutes following initiation of therapy.12,  13,  15 Once symptomatic improvement has been established, olopatadine therapy should be continued for as long as necessary to sustain improvement.12

Avoidance of allergen and other triggering factors (e.g., irritants) and application of cold compresses and lubricating eye drops are the initial means of managing allergic conjunctivitis.7,  8,  9,  10 Drug therapy generally is reserved for use when such avoidance is not possible or is ineffective and can include both prophylactic (e.g., mast-cell stabilizers) and symptomatic (e.g., topical and/or systemic antihistamines, topical vasoconstrictors, topical steroidal and nonsteroidal anti-inflammatory agents [NSAIAs]) therapy.7,  8,  9,  10 The specific therapy(ies) employed will depend on the characteristics and severity of the allergic conjunctivitis.7,  8,  9,  10 For patients with seasonal allergic conjunctivitis, prophylaxis with a mast-cell stabilizer often is initiated before and maintained throughout the pollen season, and symptomatic therapy with other agents (e.g., topical antihistamines, topical NSAIAs) generally is initiated as necessary to provide acute relief.7,  8,  9,  10 Topical steroids usually are reserved for short-term use in patients with moderate to severe symptoms of allergic conjunctivitis.7,  8,  9,  10

Seasonal Allergic Rhinitis

Olopatadine nasal spray is used to provide symptomatic relief of seasonal allergic rhinitis (e.g., hay fever).17

Efficacy and safety olopatadine nasal spray in the symptomatic management of seasonal allergic rhinitis have been established in 5 randomized, placebo-controlled studies of 2 weeks' duration in adults and children 6 years of age and older with seasonal allergic rhinitis.17 In 3 of the studies (which included 1598 adults and children 12 years of age and older), treatment with olopatadine 0.6 or 0.4% nasal spray (2 sprays in each nostril twice daily) was more effective than placebo in reducing nasal symptoms (i.e., nasal congestion, rhinorrhea, nasal itching, sneezing), as assessed by reduction in reflective total nasal symptom scores.17 In the other 2 studies (which included 588 children 6-11 years of age), treatment with olopatadine 0.6% nasal spray (1 spray in each nostril twice daily) was more effective than placebo in reducing nasal symptoms (i.e., nasal congestion, rhinorrhea, nasal itching, sneezing), as assessed by reduction in reflective total nasal symptom scores.17 In 3 of the 5 studies, patients receiving olopatadine nasal spray had substantially greater decreases in reflective symptom scores for itchy eyes and watery eyes (secondary end points) compared with those receiving placebo; ocular redness was not evaluated in these studies.17

In clinical studies in adults and children 12 years of age and older, onset of action was evident after one day following administration of olopatadine nasal spray.17 Onset of action also was evaluated in 3 environmental exposure unit studies in which patients with seasonal allergic rhinitis were exposed to high levels of pollen in the environmental exposure unit and then received a single dose (two sprays in each nostril) of olopatadine hydrochloride or vehicle; in these studies, olopatadine 0.6% nasal spray was found to have an onset of action of 30 minutes.17

Dosage and Administration

Administration

Intranasal Administration

Olopatadine nasal spray is administered intranasally, using a spray pump.17 Caution should be exercised to avoid spraying olopatadine nasal spray into the eyes.17

Before initial use, olopatadine nasal spray should be primed by releasing 5 sprays or until a fine mist appears.17 If the nasal spray has not been used for more than 7 days, the pump should be reprimed by releasing 2 sprays.17 To actuate the pump, the bottle should be held in one hand; with the forefinger and middle finger on the shoulders of the pump and the thumb on the bottom of the bottle, the shoulders of the pump should be pressed down to produce a fine mist.18

Prior to administration, patients should clear their nasal passages.18 Patients should close one nostril; with the head tipped down (chin toward chest), patients should insert the nasal applicator ¼ to ½ inch into the other nostril, holding the bottle vertically upright, and then aim the spray tip toward the cheek side of the nose (away from the center of the nose).18 While gently breathing in through the nose, the pump should be pressed down firmly and quickly to release the spray.18 Patients should breathe out through the mouth.18 Care should be taken to avoid tipping the head back or blowing the nose immediately after administration; tipping the head back may produce a bitter taste in the mouth.18 The procedure should be repeated for the other nostril.18 Patients should be advised to alternate nostrils between each actuation.18 Following administration, the nasal applicator should be wiped with a clean tissue and the blue plastic cap replaced.18

If the nasal applicator becomes clogged, patients should be advised not to attempt to clean by inserting a sharp object.18 Instead, the nasal applicator should be removed by gently pulling it upward; once removed, the nasal applicator should be washed (while being pointed downward) by running warm tap water for about one minute.18 The applicator should be shaken to remove any water and placed back on the bottle.18 The pump should be reprimed by spraying 2 times or until a fine mist appears.18

The commercially available olopatadine nasal spray delivers about 240 metered sprays per 30.5-g bottle.17 Because the correct amount of drug released cannot be assured before the initial priming and after 240 sprays have been used, olopatadine nasal spray should be discarded after 240 sprays have been used although the bottle is not completely empty.17

Ophthalmic Administration

Olopatadine ophthalmic solution is applied topically to the eye.1 The manufacturer states that commercially available olopatadine ophthalmic solutions are not for injection or oral use.1 Care should be taken to avoid contamination of the solution container.1 (See Cautions: Precautions and Contraindications.)

Olopatadine ophthalmic solutions contain benzalkonium chloride, which may be absorbed by soft contact lenses.1 Contact lenses should be removed prior to administration of each dose of olopatadine ophthalmic solution but may be reinserted after at least 10 minutes following administration of the dose.1,  12

When more than one topical ophthalmic drug is used in a patient receiving olopatadine ophthalmic solution, the drugs should be administered at least 5 minutes apart.12

Dosage

Dosage of olopatadine hydrochloride is expressed in terms of olopatadine.1

Allergic Conjunctivitis

For the symptomatic management of allergic conjunctivitis, the recommended dosage of olopatadine 0.1% ophthalmic solution in adults and children 3 years of age or older is 1 drop in the affected eye(s) twice daily at an interval of 6-8 hours.1 The recommended dosage of olopatadine 0.2% ophthalmic solution in adults and children 2 years of age or older is 1 drop in the affected eye(s) once daily.16

Seasonal Allergic Rhinitis

After priming, each metered spray delivers 665 mcg of olopatadine hydrochloride (equivalent to 600 mcg of olopatadine).17

For the symptomatic relief of seasonal allergic rhinitis, the recommended dosage of olopatadine 0.6% nasal spray in adults and children 12 years of age or older is 2 sprays (1200 mcg) in each nostril twice daily.17 The recommended dosage in children 6-11 years of age is 1 spray (600 mcg) in each nostril twice daily.17

The manufacturer states that dosage of olopatadine 0.6% nasal spray generally should be selected carefully in geriatric patients, reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy.17

Dosage in Renal and Hepatic Impairment

Dosage adjustment for olopatadine nasal spray is not necessary in patients with hepatic or renal impairment.17

Cautions

Olopatadine ophthalmic solution generally is well tolerated following topical application to the eye.12,  13 The most common adverse effect reported with olopatadine 0.1% ophthalmic solution is headache;1,  2,  13 the most common adverse effects reported with olopatadine 0.2% ophthalmic solution are symptoms similar to cold syndrome and pharyngitis.16

The most common adverse effects (occurring in more than 1% of patients in controlled clinical trials) reported with olopatadine nasal spray in patients 12 years of age and older include bitter taste, headache, epistaxis, pharyngolaryngeal pain, postnasal drip, cough, and urinary tract infection.17 The most common adverse effects reported in patients 6-11 years of age include epistaxis, headache, upper respiratory tract infection, bitter taste, pyrexia, and rash.17

Nasal Effects

Epistaxis, nasal ulcerations, and nasal septal perforations have been reported following use of olopatadine nasal spray.17 (See Cautions: Precautions and Contraindications.)

Ocular Effects

Blurred vision,1,  16 ocular burning or stinging,1,  16 conjunctivitis,16 dry eye,1,  16 foreign body sensation,1,  16 hyperemia,1,  16 hypersensitivity,1,  16 keratitis,1,  16 lid edema,1,  16 or ocular pain or pruritus1,  16 occurred in 5% or less of patients receiving olopatadine ophthalmic solution in clinical studies.1,  16 Some of these adverse effects were similar to the underlying disease.1,  16

Systemic Effects

Olopatadine appears to have a low potential for causing adverse systemic effects when applied topically to the eye.13 Cold syndrome (or symptoms similar to cold syndrome) and pharyngitis have been reported in less than 5% of patients receiving olopatadine 0.1% ophthalmic solution1 and in approximately 10% of those receiving olopatadine 0.2% ophthalmic solution.16 Headache has been reported in 7% of patients receiving the 0.1% solution and in 5% or less of those receiving the 0.2% solution.1,  16 Other adverse effects reported in 5% or less of patients receiving ophthalmic olopatadine in clinical studies include asthenia,1,  16 back pain,16 flu syndrome,16 cough,16 infection,16 nausea,1,  16 rhinitis,1,  16 sinusitis,1,  16 and taste perversion.1,  16 Some of these adverse effects were similar to the underlying disease.1,  16

Somnolence has been reported in some patients receiving olopatadine nasal spray.17 (See Cautions: Precautions and Contraindications.)

Precautions and Contraindications

Patients should be informed that improper handling of ocular solutions can result in contamination of the solution by common bacteria known to cause ocular infections and that they should avoid allowing the tip of the dispensing container to contact the eye, eyelids, or surrounding structures.1,  12 The dropper bottle should be tightly closed when not in use.1

Olopatadine ophthalmic solutions should not be used to treat contact lens-related irritation.1,  16 Patients who wear contact lenses should be advised not to wear contact lenses if their eyes are red.1,  16 Because olopatadine ophthalmic solutions contain the preservative benzalkonium chloride, which may be absorbed by soft contact lenses, patients who wear soft contact lenses (and whose eyes are not red) should be instructed to remove their lenses prior to administration of a dose of olopatadine12,  16 and to wait at least 10 minutes after administration of the ophthalmic solution before reinserting the lenses.1,  16

Because nasal perforations have been reported following use of olopatadine nasal spray, nasal examination should be performed prior to initiation of intranasal olopatadine therapy to ensure that no nasal diseases (other than allergic rhinitis) are present.17 Nasal examinations should be performed periodically for signs of adverse effects on the nasal mucosa.17 If nasal ulcerations occur, discontinuance of olopatadine nasal spray should be considered.17

Because somnolence has been reported in some patients receiving olopatadine nasal spray, patients should be advised not to engage in activities requiring complete mental alertness and motor coordination (e.g., driving or operating machinery) after administration of the nasal spray.17 Concomitant use of olopatadine nasal spray with alcohol or other CNS depressants may result in additive CNS depression; therefore, such concomitant use should be avoided .17

Olopatadine ophthalmic solutions are contraindicated in patients with known hypersensitivity to the drug or any ingredient in the formulation.1 The manufacturer states there are no known contraindications to the use of olopatadine nasal spray.17

Pediatric Precautions

Safety and efficacy of olopatadine 0.1% ophthalmic solution have not been established in children younger than 3 years of age.1 Olopatadine ophthalmic solution appears to be well tolerated in children 3-16 years of age.11,  13 Treatment-related adverse effects were not observed in children 3-16 years of age receiving 1 or 2 drops of olopatadine 0.1% ophthalmic solution in each eye 3 times daily for 6 weeks.13

Safety and efficacy of olopatadine 0.2% ophthalmic solution have not been established in children younger than 2 years of age.16

Safety and efficacy of olopatadine 0.6% nasal spray have not been established in children younger than 6 years of age.17 In clinical studies, the incidence of epistaxis was higher in children 6-11 years of age (5.7%) compared with adolescents or adults (3.2%).17

Geriatric Precautions

Geriatric patients (65-80 years of age) were included in clinical studies that evaluated safety and efficacy of olopatadine ophthalmic solution.12,  14 No overall differences in safety and effectiveness have been observed between geriatric and younger patients.1,  16

Clinical studies of olopatadine nasal spray did not include sufficient numbers of patients 65 years of age and older to determine whether geriatric patients respond differently than younger patients.17 While other clinical experience has not revealed age-related differences in response, dosage of olopatadine nasal spray generally should be selected carefully in geriatric patients, reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy.17

Mutagenicity and Carcinogenicity

Olopatadine was not mutagenic in the bacterial reverse mutation (Ames) test, in an in vitro mammalian chromosome aberration assay, or in an in vivo mouse micronucleus test.1

There was no evidence of carcinogenicity in mice or rats receiving oral olopatadine dosages up to 500 or 200 mg/kg daily, respectively (i.e., 78,125 or 31,250 times the maximum recommended human ocular dosage, respectively, based on a drop size of 40 µL; approximately 420 or 340 times the maximum recommended human intranasal dosage, respectively, for adults and adolescents 12 years of age or older; and approximately 500 or 400 times the maximum recommended human intranasal dosage, respectively, for children 6-11 years of age).1,  17

Pregnancy, Fertility, and Lactation

Pregnancy

Reproduction studies in rats and rabbits receiving oral olopatadine dosages of 600 or 400 mg/kg daily, respectively (i.e., 93,750 or 62,500 times the maximum recommended human ocular dosage, respectively, based on a drop size of 40 µL, and approximately 1000 or 1400 times the maximum recommended human dose, respectively, for adults on a mg/m2 basis), have not revealed evidence of teratogenicity.1,  12,  17 However, a decrease in the number of live fetuses was observed in rabbits and rats receiving oral olopatadine dosages of 25 and 60 mg/kg (approximately 88 and 100 times the maximum recommended human dose, respectively, for adults on a mg/m2 basis) or higher.17 In rats receiving an oral olopatadine dose of 60 mg/kg (approximately 100 times the maximum recommended human dose for adults on a mg/m2 basis), viability and body weights of pups were reduced on day 4 postpartum; however, no effect on viability was observed at a dose of 20 mg/kg (approximately 35 times the maximum recommended human dose for adults on a mg/m2 basis).17 There are no adequate and well-controlled studies to date using olopatadine in pregnant women, and the drug should be used during pregnancy only if the potential benefits justify the possible risks to the embryo or fetus.1

Fertility

In reproduction studies in male and female rats receiving an oral olopatadine dosage of 400 mg/kg daily (i.e., 62,500 times the maximum recommended human ocular dosage based on a drop size of 40 µL, and approximately 680 times the maximum recommended human dose for adults on a mg/m2 basis), a slight decrease in the fertility index and reduced implantation rate were observed.1,  17 However, no effects on reproductive function (e.g., fertility) were observed in rats receiving an olopatadine dosage of 50 mg/kg daily (i.e., 7800 times the maximum recommended human ocular dosage, and approximately 85 times the maximum recommended human dose for adults on a mg/m2 basis).1,  17

Lactation

Olopatadine is distributed into milk in rats following oral administration.1 It is not known whether topical ophthalmic administration of olopatadine could result in sufficient systemic absorption to produce detectable quantities in milk; therefore, olopatadine ophthalmic solutions should be used with caution in nursing women.1,  16 Olopatadine nasal spray should be used in nursing women only if the potential benefits to the woman outweigh the potential risks to the infant.17

Drug Interactions

Specific drug interaction studies involving olopatadine ophthalmic solution or nasal spray and other drugs have not been conducted to date.12,  17

Olopatadine does not inhibit the in vitro metabolism of substrates of cytochrome P-450 (CYP) isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1, or 3A4.17

Drugs Affecting or Metabolized by Hepatic Enzymes

Interactions with drugs that inhibit hepatic enzymes (e.g., CYP microsomal enzymes) are unlikely because olopatadine is eliminated predominantly by renal excretion.17

The potential for olopatadine and its metabolites to act as inducers of CYP isoenzymes has not been evaluated.17

Protein-bound Drugs

Interactions with protein-bound drugs (e.g., possible displacement of other protein-bound drugs) are unlikely because olopatadine is modestly protein bound.17

CNS Depressants

Concomitant use of olopatadine nasal spray with CNS depressants (e.g., alcohol) may result in additive CNS depression; therefore, such concomitant use should be avoided.17

Other Information

Acute Toxicity

The manufacturer states that overdosage following oral ingestion of the commercially available ophthalmic solution is unlikely given the limited amount (1 mg/mL) of olopatadine present in the solution and volume (5 mL) per container.13 Single oral olopatadine doses up to 360 mg have been well tolerated in humans.13

There have been no reported overdosages with olopatadine nasal spray.17 The manufacturer states that acute overdosage with olopatadine nasal spray is unlikely due to the configuration of the primary container closure system.17 However, symptoms of antihistamine overdosage may include drowsiness in adults and, initially, agitation and restlessness, followed by drowsiness, in children.17 There is no known specific antidote to olopatadine nasal spray.17 If overdosage occurs, symptomatic or supportive treatment is recommended, taking into account any concomitantly ingested medications.17

The oral median LD50 of olopatadine for mice or rats is 1490 or 3870 mg/kg, respectively.13,  17

Pharmacology

Olopatadine is a relatively selective histamine H1-receptor antagonist.1,  2,  3,  4,  5,  6 In addition, olopatadine shares many of the pharmacologic effects of mast-cell stabilizers (e.g., cromolyn sodium, lodoxamide tromethamine, nedocromil sodium).1,  2,  3,  4,  5,  6 Olopatadine inhibits type I immediate hypersensitivity reactions in vitro and in vivo.1,  3

In vitro studies indicate that olopatadine has a high binding affinity for H1 receptors (KI of 31.6-41.1 nmol/L) and considerably weaker affinity for H2 (KI of 43,437-100,000 nmol/L) and H3 receptors (KI of 79,400-171,666 nmol/L).4,  5 Olopatadine suppresses the release of inflammatory mediators (e.g., histamine, prostaglandin D2, tryptase) in response to antigenic stimulation of human conjunctival mast cells in a dose-dependent manner.5,  13 In vitro studies have demonstrated that olopatadine possesses virtually no affinity for α-adrenergic, dopaminergic (D1 and D2), muscarinic (M1 and M2), or serotonergic receptors.1,  5,  13

Decreased chemotaxis and inhibition of eosinophil activation has been observed with olopatadine.16

Ocular Effects

In one animal study, ophthalmic administration of olopatadine (0.0001-1%) 5 minutes to 24 hours prior to subconjunctival injection of histamine inhibited the conjunctival vascular permeability response in a concentration-dependent manner.3 In addition, the effect of topical olopatadine on vascular permeability appears to be receptor-specific because ophthalmic solutions of olopatadine 0.01% failed to substantially attenuate changes in conjunctival vascular permeability induced by serotonin or platelet-activating factor (PAF).3 In animals, topically applied olopatadine inhibits histamine-induced conjunctivitis to a greater extent than antigen-induced conjunctivitis.6 Olopatadine has been shown to inhibit histamine-induced effects on human conjunctival epithelial cells.1 Olopatadine does not appear to have local anesthetic activity12 or to affect pupillary size.13

In animals, the potency of olopatadine (as measured by inhibition of histamine-induced increases in conjunctival vascular permeability) was comparable to that of levocabastine and exceeded that of pheniramine or antazoline.3,  13

Systemic Effects

The likelihood of systemic effects appears to be minimal following ophthalmic or intranasal administration of olopatadine.1,  2,  3,  4,  5,  6 (See Cautions: Systemic Effects.)

Pharmacokinetics

Absorption

The extent of systemic absorption of olopatadine following topical application to the eye in humans has not been fully elucidated;16 however, only limited concentrations appear to be achieved systemically following such application.1 Following topical application to both eyes of 2 drops (60 µL) of a 0.15% solution of olopatadine every 12 hours for 2 weeks in a limited number of healthy adults, plasma concentrations usually were undetectable (detection limit of 0.5 mcg/mL) at various sampling times.1,  12,  13 However, within 2 hours of drug administration, detectable plasma concentrations of 0.5-1.3 mcg/mL occurred in approximately 67% of individuals.1,  12 Results of histamine challenge studies indicate that olopatadine has a rapid onset and long duration of action (8 hours or longer for 0.1% ophthalmic solution) following ocular administration of the drug.3,  13,  14,  15

Following twice-daily intranasal administration in patients with seasonal allergic rhinitis, peak plasma concentrations were observed between 15 minutes and 2 hours.17 The average absolute bioavailability of intranasal olopatadine in healthy individuals is 57%.17 In clinical studies, onset of action occurs within one day following intranasal administration of olopatadine nasal spray.17 (See Uses: Seasonal Allergic Rhinitis.)

Distribution

Distribution of olopatadine into human ocular tissues and fluids has not been characterized.12 Olopatadine is approximately 55% bound to plasma proteins (mainly albumin).17

Elimination

Following topical application of olopatadine hydrochloride to the eyes, the plasma elimination half-life of the drug is about 3 hours.1

Olopatadine is not extensively metabolized.17 Following oral administration, unchanged olopatadine accounts for 77% of peak plasma total radioactivity, while metabolites (e.g., olopatadine N -oxide, N -desmethyl olopatadine) account for less than 6%.17 The plasma elimination half-life of olopatadine following oral administration is 8-12 hours.16,  17

Olopatadine is eliminated principally by renal excretion; about 60-70% of a systemically absorbed dose of olopatadine is excreted in the urine (86% as unchanged olopatadine), and about 17% is excreted in feces.1,  12,  17

Chemistry and Stability

Chemistry

Olopatadine is a propylidenebenzoxepin derivative and differs structurally from other currently available antiallergic agents, including antihistamines and mast-cell stabilizers.1,  2,  3,  4,  5,  6,  12,  13 Olopatadine is a relatively selective histamine H1-receptor antagonist.1,  2,  3,  4,  5,  6 In addition, olopatadine shares many of the pharmacologic effects of mast-cell stabilizers.1,  2,  3,  4,  5,  6

Olopatadine occurs as a white crystalline powder and has solubilities of 16 mg/mL in water and 6.9 mg/mL in alcohol at 25°C.1,  12 The drug has pKas of 4.18 and 9.79.12

Olopatadine ophthalmic solutions are sterile solutions of the drug in purified water.1 The commercially available ophthalmic solutions contain benzalkonium chloride as a preservative; the solutions have a pH of approximately 7 and an osmolality of approximately 300 mOsm/kg.1,  16

Olopatadine nasal spray contains 0.6% w/v olopatadine in a nonsterile aqueous solution with a pH of approximately 3.7.17 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 (equivalent to 600 mcg of olopatadine).17 Olopatadine nasal spray contains benzalkonium chloride (0.01%).17

Stability

Olopatadine ophthalmic solutions should be stored at 2-25°C.1,  16 When stored as directed, the commercially available ophthalmic solutions have an expiration date of 24 months following the date of manufacture.12

Olopatadine nasal spray should be stored at 4-25°C.17

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Olopatadine Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Nasal

Solution

0.6% (600 mcg [of olopatadine]/metered spray)*

Olopatadine Hydrochloride Nasal Spray

Patanase®

Alcon

Ophthalmic

Solution

0.1% (of olopatadine)

Patanol®

Alcon

0.2% (of olopatadine)

Pataday®

Alcon

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Copyright

AHFS® Drug Information. © Copyright, 1959-2025, Selected Revisions March 28, 2013. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.

References

1. Alcon Laboratories, Inc. Patanol® (olopatadine hydrochloride) ophthalmic solution 0.1% prescribing information. Fort Worth, TX; 2007 Jan.

2. Anon. Olopatadine for allergic conjunctivitis. Med Lett Drugs Ther . 1997; 39:108-9. [PubMed 9398823]

3. Yanni JM, Stephens DJ, Miller ST et al. The in vitro and in vivo ocular pharmacology of olopatadine (AL-4943A), an effective anti-allergic/antihistaminic agent. J Ocul Pharmacol Ther . 1996; 12:389-400. [PubMed 8951675]

4. Sharif NA, Xu SX, Yanni JM. Olopatadine (AL-4943A): ligand binding and functional studies on a novel, long acting H1-selective histamine antagonist and anti-allergic agent for use in allergic conjunctivitis. J Ocul Pharmacol Ther . 1996; 12:401-7. [PubMed 8951676]

5. Sharif NA, Xu SX, Miller ST et al. Characterization of the ocular antiallergic and antihistaminic effects of olopatadine (AL-4943A), a novel drug for treating ocular allergic diseases. J Pharmacol Exp Ther . 1996; 278:1252-61. [PubMed 8819509]

6. Kamei C, Sugimoto Y, Nakamura S et al. Effect of (Z)-11-[3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride on experimental allergic conjunctivitis and rhinitis in rats and guinea pigs. Arzneimittelforschung . 1995; 45:1005-8. [PubMed 7488300]

7. Ciprandi G, Buscaglia S, Cerqueti PM et al. Drug treatment of allergic conjunctivitis: a review of the evidence. Drugs . 1992; 43:154-76. [PubMed 1372215]

8. Morrow GL, Abbott RL. Conjunctivitis. Am Fam Physician . 1998; 57:735-46. [PubMed 9490996]

9. Titi MJ. A critical look at ocular allergy drugs. Am Fam Physician . 1996; 53:2637-42. [PubMed 8644576]

10. Galindez OA, Kaufman HE. Coping with the itchy-burnies: the management of allergic conjunctivitis. Ophthalmology . 1996; 103:1335-6. [PubMed 8841290]

11. Reviewers' comments (personal observations).

12. Alcon Laboratories; Fort Worth, TX: Personal communication.

13. Alcon Laboratories. Patanol® (olopatadine hydrochloride) ophthalmic solution 0.1% product monograph. Fort Worth, TX: (not dated).

14. Abelson MB, Spitalny L. Combined analysis of two studies using the conjunctival allergen challenge model to evaluate olopatadine hydrochloride, a new ophthalmic antiallergic agent with dual activity. Am J Ophthalmol . 1998; 125:797-804. [PubMed 9645717]

15. Abelson MB. Evaluation of olopatadine, a new ophthalmic antiallergic agent with dual activity, using the conjunctival allergen challenge model. Ann Allergy Asthma Immunol . 1998; 81:211-8. [PubMed 9759796]

16. Alcon Laboratories, Inc. Patanol® (olopatadine hydrochloride) ophthalmic solution 0.2% prescribing information. Fort Worth, TX; 2010 Aug.

17. Alcon Laboratories, Inc. Patanase® (olopatadine hydrochloride) nasal spray prescribing information. Fort Worth, TX; 2012 Feb.

18. Alcon Laboratories, Inc. Patanase® (olopatadine hydrochloride) nasal spray patient information. Fort Worth, TX. 2009 Dec. From DailyMed website. [Web]