Ocular Anti-Allergics, Antihistamines
For topical administration to the eyes only.
Wash hands prior to and after use. Tilt the head back slightly and pull the lower eyelid down with the index finger. Squeeze one drop into the conjunctival sac of each eye and gently close eyes for 1—2 minutes. Do not blink.
Take care to avoid contamination. Do not touch the tip of the dropper to the eye, fingertips, or other surface.
Instruct patients to remove contact lenses prior to instilling the ophthalmic solution; contact lenses may be reinserted 10 minutes after administration of the ophthalmic solution.
If more than 1 topical ophthalmic medication is being used, separate administration by at least 5 minutes.
Do not share ophthalmic drops between patients.
angioedema / Rapid / Incidence not known
ocular inflammation / Early / Incidence not known
blurred vision / Early / Incidence not known
ocular irritation / Rapid / 0-4.0
ocular pain / Early / 0-4.0
ocular pruritus / Rapid / 0-4.0
pharyngitis / Delayed / 0-3.0
headache / Early / 0-3.0
lacrimation / Early / Incidence not known
ocular discharge / Delayed / Incidence not known
drowsiness / Early / Incidence not known
Common Brand Names
Topical ophthalmic H1-antagonist
Used for the prevention of ocular pruritus associated with allergic conjunctivitis
Once daily administration
Dosage And Indications
1 drop in the affected eye(s) once daily.
1 drop in the affected eye(s) once daily.
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.Renal Impairment
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
There are no drug interactions associated with Alcaftadine products.
LASTACAFT Ophthalmic Sol: 0.25%
1 drop/day ophthalmic solution in each eye.Geriatric
1 drop/day ophthalmic solution in each eye.Adolescents
1 drop/day ophthalmic solution in each eye.Children
>= 2 years: 1 drop/day ophthalmic solution in each eye.
< 2 years: Safety and efficacy have not been established.
Safety and efficacy have not been established.Neonates
Safety and efficacy have not been established.
Mechanism Of Action
Alcaftadine is a topically active, H1-receptor antagonist and an inhibitor of histamine release from mast cells. After topical ocular administration, alcaftadine inhibits histamine-stimulated vascular permeability in the conjunctiva, thereby preventing the formation of ocular edema and wheal. Alcaftadine has also been shown to decrease chemotaxis and activation of eosinophils. As a result of these pharmacologic actions, alcaftadine relieves ocular pruritus associated with allergic conjunctivitis.
Alcaftadine is administered topically to the eyes. Once absorbed, alcaftadine is metabolized by non-CYP450 enzymes to an active metabolite, carboxylic acid. The protein binding of alcaftadine and carboxylic acid are 39.2% and 62.7%, respectively. Carboxylic acid has a half-life of approximately 2 hours and is primarily eliminated unchanged in the urine.Other Route(s)
Systemic absorption is limited after ophthalmic administration of alcaftadine. Instilling alcaftadine into both eyes results in a mean peak plasma concentrations (Cmax) of approximately 60 pg/mL. The median time to reach peak plasma concentration (Tmax) is 15 minutes, and the plasma concentrations fall below the limits of quantification (10 pg/mL) by 3 hours post-dose. The Cmax for carboxylic acid is approximately 3 ng/mL and occurs about 1 hour after dosing. The plasma concentrations of carboxylic acid are detectable for up to 12 hours after dosing. According to the manufacturer, there appears to be no systemic accumulation of alcaftadine or the active metabolite after daily topical ocular administration.
Pregnancy And Lactation
No adequate and well-controlled studies have been conducted to evaluate the use of alcaftadine during human pregnancy. In animal studies involving rats (20 mg/kg/day oral alcaftadine) and rabbits (80 mg/kg/day oral alcaftadine), no fetal or maternal toxicities were observed following exposure during the period of organogenesis. The plasma exposures in the pregnant rats and rabbits were 230- and 8,819-times higher, respectively, than the plasma exposure after a recommended human ocular dose. Lower pup weights were observed with 20 and 30 mg/kg/day doses of oral alcaftadine that were administered to rats from day 6 of pregnancy until day 20 postpartum; no adverse effects observed with the 5 mg/kg/day dose. Because animal reproductive studies are not always predictive of human response, only administer alcaftadine during pregnancy if the benefit justifies the potential risk to the fetus.
There are no data regarding the excretion of alcaftadine into human milk, the effects on a breast-fed infant, or the effects on milk production. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally administered drug, health care providers are encouraged to report the adverse effect to the FDA.