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Emadine

Generic Name: Emedastine Difumarate
Class: Antiallergic Agents
ATC Class: S03AA07
VA Class: OP900
Chemical Name: 1-(2-Ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)benzimidazole fumerate (1:2)
Molecular Formula: C17H26N4O•2C4H4O4
CAS Number: 87233-62-3

Introduction

Relatively selective histamine H1-receptor antagonist;1 2 3 14 a benzimidazole derivative.1 12

Uses for Emadine

Allergic Conjunctivitis

Symptomatic relief of allergic conjunctivitis.1

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Emadine Dosage and Administration

Administration

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

Ophthalmic Administration

Remove soft contact lenses prior to administration of each dose (since benzalkonium chloride preservative may be absorbed by the lenses); may reinsert lenses 10 minutes after administration if eyes are not red.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

Do not use if solution is discolored.1

Dosage

Available as emedastine difumarate; dosage expressed in terms of emedastine.1

Pediatric Patients

Allergic Conjunctivitis
Ophthalmic

Children ≥3 years of age: 1 drop of a 0.05% solution in the affected eye(s) up to 4 times daily.1

Adults

Allergic Conjunctivitis
Ophthalmic

1 drop of a 0.05% solution in the affected eye(s) up to 4 times daily.1

Cautions for Emadine

Contraindications

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

Warnings/Precautions

Specific Populations

Pregnancy

Category B.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

Adverse effect profile in children 3–16 years of age is similar to that in individuals ≥17 years of age.14

Geriatric Use

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

Common Adverse Effects

Headache.1

Interactions for Emadine

No formal drug interaction studies to date.12

Emadine Pharmacokinetics

Absorption

Bioavailability

Limited systemic exposure following topical application to the eye;1 plasma concentrations usually are undetectable.1 12

Onset

Rapid onset.2 14

Duration

Long duration.2 14

Elimination

Metabolism

Metabolized in the liver principally to 5- and 6-hydroxyemedastine following oral administration; metabolites appear to undergo further oxidation to form 5′-oxo analogs.1 12

Elimination Route

44% of an oral dose is recovered in urine within 24 hours.1

Half-life

3–4 hours following oral administration.1

Stability

Storage

Ophthalmic

Solution

Tightly closed bottle at 4–30°C.1

Actions

  • Inhibits the histamine-stimulated conjunctival vascular permeability response in a concentration-dependent manner.1 2

  • Potency is about 100, 357, or 5813 times that of levocabastine, pheniramine, or antazoline, respectively, on a molar basis.2 14

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 Not indicated for contact lens-related irritation.1

  • Importance of administering different topical ophthalmic preparations at least 5 minutes apart.1

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

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

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)

Preparations

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

Emedastine Difumarate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Ophthalmic

Solution

0.05% (of emedastine)

Emadine (with benzalkonium chloride)

Alcon

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. Alcon Laboratories Inc. Emadine (emedastine difumarate) ophthalmic solution 0.05% prescribing information. Forth Worth, TX; 2003 Aug.

2. Yanni JM, Stephens DJ, Parnell DW et al. Preclinical efficacy of emedastine, a potent, selective histamine H1 antagonist for topical ocular use. J Ocular Pharmacol. 1994; 10:665-75.

3. Sharif NA, Su SX, Yanni JM. Emedastine: a potent, high affinity histamine H1 receptor-selective antagonist for ocular use: receptor binding and second messenger studies. J Ocular Pharmacol. 1994; 10:653-64.

4. Fukuda T, Saito T, Yoshidomi M et al. Influence of 1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazole difumarate (KB-2413), a new antiallergic, on ciliary movement. Arzneimittelforschung. 1984; 34:816-8. [PubMed 6149756]

5. Budavari S, O’Neil MJ, Smith A et al, eds. The Merck index. 12th ed. Rahway, NJ: Merck & Co, Inc; 1996:601.

6. 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]

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

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

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

10. Friedlaender MH. Current concepts in ocular allergy. Ann Allergy. 1991; 67:5-10,13. [IDIS 312766] [PubMed 1859041]

11. Trocme SD. Medical therapy for ocular allergy. Mayo Clin Proc. 1992; 67:557-65. [IDIS 296611] [PubMed 1359206]

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

13. Reviewers’ comments (personal observations).

14. Alcon Laboratories. Emadine (emedastine difumarate) ophthalmic solution 0.05% product monograph. Fort Worth, TX: (not dated).

15. Verin P, Secchi A, Easty DL et al. Efficacy and safety of emedastine eye drops 0.05% compared to levocabastine eye drops 0.05% in allergic conjunctivitis. Invest Ophthalmol Vis Sci. 1998; 39:S549.

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