Class: Antiallergic Agents
ATC Class: S01GX09
VA Class: OP900
Chemical Name: 11-[(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride
Molecular Formula: C21H23NO3•HCl
CAS Number: 140462-76-6
Brands: Patanol
Introduction
Relatively selective histamine H1-receptor antagonist1 2 3 4 5 6 and mast-cell stabilizer.1 2 3 4 5 6 b
Uses for Olopatadine Hydrochloride
Allergic Conjunctivitis
Temporary prevention of ocular itching associated with allergic conjunctivitis.1 2 13
Olopatadine Hydrochloride Dosage and Administration
Administration
Ophthalmic Administration
Apply topically to the eye as an ophthalmic solution.1 Not for injection or oral use.1
If more than one topical ophthalmic drug is used, administer the drugs at least 5 minutes apart.12
Avoid contamination of the solution container.1
Dosage
Available as olopatadine hydrochloride; dosage expressed in terms of olopatadine.1
Pediatric Patients
Allergic Conjunctivitis
Ophthalmic
Children ≥3 years of age: 1 or 2 drops of a 0.1% solution in the affected eye(s) twice daily (at an interval of 6–8 hours).1
Once symptomatic improvement is established, continue therapy for as long as necessary to sustain improvement.12
Adults
Allergic Conjunctivitis
Ophthalmic
1 or 2 drops of a 0.1% solution in the affected eye(s) twice daily (at an interval of 6–8 hours).1
Once symptomatic improvement is established, continue therapy for as long as necessary to sustain improvement.12
Cautions for Olopatadine Hydrochloride
Contraindications
Known hypersensitivity to olopatadine or any ingredient in the formulation.1
Warnings/Precautions
Specific Populations
Pregnancy
Category C.1
Lactation
Distributed into milk in rats following oral administration;1 not known whether distributed into human milk following topical application to the eye.1 Use with caution.1
Pediatric Use
Safety and efficacy not established in children <3 years of age.1
Appears to be well-tolerated in children 3–16 years of age.11 13
Geriatric Use
No substantial differences in safety and efficacy relative to younger adults.a
Common Adverse Effects
Headache.1 2 13
Interactions for Olopatadine Hydrochloride
No formal drug interaction studies to date.12
Olopatadine Hydrochloride Pharmacokinetics
Absorption
Bioavailability
Limited systemic exposure following topical application to the eye;1 plasma concentrations usually are undetectable.1 12 13
Onset
Rapid onset;3 13 14 15 symptomatic relief of itching generally occurs within 30 minutes.12 13 15
Duration
Long duration (≥8 hours).3 13 14 15
Distribution
Extent
Distribution into human ocular tissues and fluids not characterized.1
Elimination
Metabolism
Metabolized in the liver to monodesmethyl olopatadine and olopatadine N-oxide following topical application to the eyes.1 12
Elimination Route
Eliminated principally by renal excretion; 60–70% of systemically absorbed dose excreted in urine as parent drug.1 12
Half-life
Approximately 3 hours following topical application to the eyes.1
Stability
Storage
Ophthalmic
Solution
4–25°C.1
ActionsActions
Inhibits type I immediate hypersensitivity reactions in vitro and in vivo.1 3
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
Inhibits histamine-stimulated conjunctival vascular permeability response in a concentration-dependent manner.3
Potency is comparable to that of levocabastine and exceeds that of pheniramine or antazoline.3 13
Advice to Patients
Importance of learning and adhering to proper administration techniques to avoid contamination of the solution container.1 12
Importance of removing soft contact lenses prior to administration of each dose.1 Delay reinsertion for 10 minutes after administration if eyes are not red; do not wear contact lenses if eye(s) are red.1 12 Not indicated for contact lens-related irritation.1
Importance of administering different topical ophthalmic preparations at least 5 minutes apart.12
Importance of patients informing clinicians of exisiting or contemplated therapy, including prescription and OTC drugs.
Importance of women informing clinicians if they are or plan to become pregnant or to breast-feed.a
Importance of informing patients of other important precautionary information.a (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Ophthalmic | Solution | 0.1% (of olopatadine) | Patanol (with benzalkonium chloride) | Alcon |
Comparative Pricing
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
Pataday 0.2% Solution (ALCON VISION): 2/$119.99 or 7/$334.98
Patanol 0.1% Solution (ALCON VISION): 5/$125.99 or 15/$359.99
Disclaimer
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions May 2004. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
References
1. Alcon Laboratories. Patanol (olopatadine hydrochloride) ophthalmic solution 0.1% prescribing information. Fort Worth, TX; 1996 Dec.
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. [IDIS 360840] [PubMed 1372215]
8. Morrow GL, Abbott RL. Conjunctivitis. Am Fam Physician. 1998; 57:735-46. [IDIS 418448] [PubMed 9490996]
9. Titi MJ. A critical look at ocular allergy drugs. Am Fam Physician. 1996; 53:2637-42. [IDIS 367250] [PubMed 8644576]
10. Galindez OA, Kaufman HE. Coping with the itchy-burnies: the management of allergic conjunctivitis. Ophthalmology. 1996; 103:1335-6. [IDIS 373485] [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. [IDIS 409293] [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. [IDIS 415165] [PubMed 9759796]
a. Alcon Laboratories. Patanol (olopatadine hydrochloride) ophthalmic solution 0.1% prescribing information. Fort Worth, TX; 2003 Dec.
b. Anon. New drugs for allergic conjunctivitis. Med Lett Drugs Ther. 2000; 42:39-40. [PubMed 10825920]
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