Class: Antiallergic Agents
Chemical Name: 6,11-dihydro-11-(1-methyl-4-piperidinylidene)-5H-imidazo[2,1-b]  benzazepine-3-carboxaldehyde
Molecular Formula: C19H21N3O
CAS Number: 147084-10-4
Uses for Alcaftadine
Alcaftadine Dosage and Administration
Remove contact lenses prior to each dose (since benzalkonium chloride preservative may be absorbed by soft lenses); may reinsert lenses after 10 minutes following administration if eyes are not red.1
Avoid contamination of the solution container.1
Children ≥2 years of age: 1 drop of a 0.25% solution in each eye once daily.1
1 drop of a 0.25% solution in each eye once daily.1
No special population recommendations at this time.1
Cautions for Alcaftadine
Manufacturer states none known.1
Safety and efficacy not established in children <2 years of age.1 Safety evaluated in children ≥3 years of age;3 9 efficacy in children 2–9 years of age extrapolated from demonstrated efficacy in adults and children ≥10 years of age.9
No overall differences in safety and efficacy relative to younger patients.1
Common Adverse Effects
Interactions for Alcaftadine
No formal drug interaction studies to date.3
Not metabolized by CYP enzymes; does not substantially inhibit major CYP enzymes in vitro.1
Appears rapidly in systemic circulation following topical application to eye.1 3 Peak plasma concentrations of alcaftadine and its active metabolite occur at a median of 15 minutes and at 1 hour, respectively, after administration.1
Not known whether distributed into milk.1
Plasma Protein Binding
Alcaftadine: About 39%.1
Carboxylic acid metabolite: About 63%.1
Metabolized by cytosolic, non-CYP enzymes to an active carboxylic acid metabolite.1
Carboxylic acid metabolite is eliminated mainly in urine (based on data for oral alcaftadine).1
Carboxylic acid metabolite: About 2 hours.1
Plasma concentrations of alcaftadine and carboxylic acid metabolite are below limit of quantitation by 3 and 12 hours, respectively, after administration of alcaftadine ophthalmic solution.1
Advice to Patients
Importance of delaying insertion of contact lenses for ≥10 minutes after alcaftadine instillation to prevent absorption of benzalkonium chloride by soft lenses; do not wear contact lenses if eyes are red.1
Not indicated for contact lens-related ocular irritation.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 concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1
Importance of informing patients of other important precautionary information.1 (See Cautions.)
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.
AHFS DI Essentials. © Copyright, 2004-2016, Selected Revisions May 6, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
1. Allergan. Lastacaft (alcaftadine) ophthalmic solution 0.25% prescribing information. Irvine, CA; 2010 Sep.
2. del Cuvillo A, Sastre J, Montoro J et al. Allergic conjunctivitis and H1 antihistamines. J Investig Allergol Clin Immunol. 2009; 19 Suppl 1:11-8. [PubMed 19476049]
3. Food and Drug Administration. Center for Drug Evaluation and Research: Application number 22-134 (alcaftadine ophthalmic solution): Clinical review. From FDA website.
4. Torkildsen G, Shedden A. The safety and efficacy of alcaftadine 0.25% ophthalmic solution for the prevention of itching associated with allergic conjunctivitis. Curr Med Res Opin. 2011; 27:623-31. [PubMed 21250860]
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. Center for Drug Evaluation and Research: Application number 22-134 (alcaftadine ophthalmic solution): Office director memo. From FDA website.
More about alcaftadine ophthalmic
- Other brands: Lastacaft