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Elestat

Generic Name: Epinastine Hydrochloride
Class: Antiallergic Agents
Chemical Name: 3-Amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine
Molecular Formula: C16H15N3
CAS Number: 80012-43-7

Introduction

Relatively selective histamine H1-receptor antagonist1 with mast-cell stabilizing properties.2

Uses for Elestat

Allergic Conjunctivitis

Prevention of ocular itching associated with allergic conjunctivitis.1

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Elestat Dosage and Administration

Administration

Ophthalmic Administration

Apply topically to the eye as an ophthalmic solution.1 Not for injection or oral use.1

Dosage

Available as epinastine hydrochloride; dosage expressed in terms of the salt.1

Pediatric Patients

Allergic Conjunctivitis
Ophthalmic

Children ≥3 years of age: 1 drop of a 0.05% solution in each eye twice daily for up to 8 weeks.1

Continue therapy throughout period of exposure (i.e., until pollen season is over or until exposure to offending allergen is terminated), even in absence of symptoms.1

Adults

Allergic Conjunctivitis
Ophthalmic

1 drop of a 0.05% solution in each eye twice daily for up to 8 weeks.1

Continue therapy throughout period of exposure (i.e., until pollen season is over or until exposure to offending allergen is terminated), even in absence of symptoms.1

Cautions for Elestat

Contraindications

  • Known hypersensitivity to epinastine or any ingredient in the formulation.1

Warnings/Precautions

Specific Populations

Pregnancy

Category C.1

Lactation

Distributed into milk in rats; not known whether distributed into human milk.1 Use with caution.1

Pediatric Use

Safety and efficacy not established in children <3 years of age.1

Geriatric Use

No overall differences in safety and efficacy relative to younger adults.1 11

Common Adverse Effects

Ocular discomfort (e.g., burning, folliculosis, hyperemia, pruritus), infection (e.g., cold symptoms, upper respiratory infections).1

Interactions for Elestat

No formal drug interaction studies to date.11

Elestat Pharmacokinetics

Absorption

Bioavailability

Limited systemic exposure following topical application to the eye.1 No increase in systemic absorption following multiple dosing.1

Peak plasma concentrations attained approximately 2 hours after ophthalmic administration.1

Onset

Rapid onset (within 3–5 minutes).1

Duration

8 hours.1

Distribution

Extent

Does not penetrate blood-brain barrier.1

Distributed into milk in rats; not known whether distributed into human milk.1

Plasma Protein Binding

64%.1

Elimination

Metabolism

Less than 10% is metabolized.1

Elimination Route

55 or 30% of IV dose excreted unchanged in urine or feces, respectively.1

Half-life

Approximately 12 hours.1

Stability

Storage

Ophthalmic

Solution

Tightly closed bottle at 15–25°C.1

Actions

  • Inhibits the release of mediators (e.g., histamine) from cells involved in hypersensitivity reactions (e.g., mast cells).1 2

  • Exhibits mast-cell stabilizing properties.2

  • Exhibits some affinity for histamine H2, α1- and α2-adrenergic, and 5-HT2 receptors.1

Advice to Patients

  • Importance of learning and adhering to proper administration techniques to avoid contamination of the solution with common bacteria that can cause ocular infections.1 9 Serious damage to the eye and subsequent loss of vision may result from using contaminated ophthalmic solutions.1 9

  • Importance of delaying insertion of contact lenses for at least 10 minutes after epinastine instillation, since benzalkonium chloride preservative may be absorbed by soft lenses; importance of not wearing contact lenses in the presence of ocular redness.1 9

  • Not indicated for contact lens-related ocular irritation.1 9

  • Importance of reporting any worsening of symptoms or new-onset ocular pain/discomfort.9

  • Importance of women informing clinician if they are or plan to become pregnant or plan to breast-feed.9

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

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

Epinastine Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.05% (of epinastine hydrochloride)

Elestat (with benzalkonium chloride)

Allergan

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Elestat 0.05% Solution (ALLERGAN): 5/$124.99 or 15/$349.96

Epinastine HCl 0.05% Solution (CYPRESS PHARMACEUTICAL): 5/$105.99 or 15/$285.98

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions July 1, 2005. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

1. Allergan. Elestat (epinastine hydrochloride) ophthalmic solution 0.05% prescribing information. Irvine, CA; 2003 Oct. 2

2. Food and Drug Administration Center for Drug Evaluation and Research. Clinical Pharmacology and Biopharmaceutics review: epinastine. Executive Summary. December 19, 2002.

3. Abelson MB, Gomes P, Crampton HJ et al. Efficacy and tolerability of ophthalmic epinastine assessed using the conjunctival antigen challenge model in patients with a history of allergic conjunctivitis. Clin Ther. 2004; 26:35-47. [IDIS 511841] [PubMed 14996516]

4. Whitcup SM, Bradford R, Lue J et al. Efficacy and tolerability of ophthalmic epinastine: a randomized, double-masked, parallel-group, active- and vehicle-controlled environmental trial in patients with seasonal allergic conjunctivitis. Clin Ther. 2004; 26:29-34. [IDIS 511840] [PubMed 14996515]

5. 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]

6. Morrow GL, Abbott RL. Conjunctivitis. Am Fam Physician. 1998; 57:735-46. [IDIS 418448] [PubMed 9490996]

7. Titi MJ. A critical look at ocular allergy drugs. Am Fam Physician. 1996; 53:2637-42. [IDIS 367250] [PubMed 8644576]

8. Galindez OA, Kaufman HE. Coping with the itchy-burnies: the management of allergic conjunctivitis. Ophthalmology. 1996; 103:1335-6. [IDIS 373485] [PubMed 8841290]

9. Food and Drug Administration. Elestat consumer information. 2003 Dec 04. From FDA website.

10. Tasaka K. Epinastine: An update of its pharmacology, metabolism, clinical efficacy and tolerability in the treatment of allergic diseases. Drugs Today. 2000; 36:735-57. [PubMed 12845334]

11. Allergan. Irvine, CA: Personal communication.

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