Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Solution, Ophthalmic, as hydrochloride:
Elestat: 0.05% (5 mL [DSC]) [contains benzalkonium chloride]
Generic: 0.05% (5 mL)
Pharmacology
Mechanism of Action
Selective H1-receptor antagonist; inhibits release of histamine from the mast cell; also has affinity for the H2, alpha1, alpha2, and the 5-HT2 receptors
Pharmacokinetics/Pharmacodynamics
Absorption
Low systemic absorption following topical application
Distribution
Does not cross blood-brain barrier
Metabolism
<10% metabolized
Excretion
IV: Urine (55%); feces (30%)
Onset of Action
3-5 minutes
Duration of Action
8 hours
Half-Life Elimination
12 hours
Protein Binding
64%
Use: Labeled Indications
Treatment of allergic conjunctivitis
Contraindications
There are no contraindications listed in the manufacturer's labeling.
Dosage and Administration
Dosing: Adult
Allergic conjunctivitis: Ophthalmic: Instill 1 drop into each eye twice daily. Continue throughout period of exposure, even in the absence of symptoms.
Dosing: Geriatric
Refer to adult dosing.
Dosing: Pediatric
Allergic conjunctivitis: Children ≥2 years and Adolescents: Ophthalmic: Instill 1 drop into each eye twice daily; continue throughout period of exposure, even in the absence of symptoms
Administration
For ophthalmic use only; avoid touching tip of applicator to eye or other surfaces. Contact lenses should be removed prior to application, may be reinserted after 10 minutes. Do not wear contact lenses if eyes are red.
Storage
Store at controlled room temperature of 15°C to 25°C (59°F to 77°F). Keep tightly closed.
Drug Interactions
There are no known significant interactions.
Adverse Reactions
Frequency not always defined.
1% to 10%:
Central nervous system: Headache (1% to 3%)
Infection: Infection (10%; defined as cold symptoms and upper respiratory tract infection)
Ophthalmic: Burning sensation of eyes, eye pruritus, follicular conjunctivitis, ocular hyperemia
Respiratory: Cough (1% to 3%), pharyngitis (1% to 3%), rhinitis (1% to 3%), sinusitis (1% to 3%)
<1%, postmarketing, and/or case reports: Increased lacrimation
Warnings/Precautions
Concerns related to adverse effects:
- Bacterial keratitis: Inadvertent contamination of multiple-dose ophthalmic solutions has caused bacterial keratitis.
Special populations:
- Contact lens wearers: Contains benzalkonium chloride which may be absorbed by contact lenses; remove contact lenses prior to use and wait 10 minutes before reinserting.
Other warnings/precautions:
- Appropriate use: For topical ophthalmic use only. Not for the treatment of contact lens irritation; do not wear contact lenses if eye is red.
Pregnancy
Pregnancy Risk Factor
C
Pregnancy Considerations
Adverse events were observed in some animal reproduction studies.
Patient Education
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience burning, common cold symptoms, or watery eyes. Have patient report immediately to prescriber vision changes, eye pain, or severe eye irritation (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
