Alcaftadine

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# Overview
Alcaftadine is an antihistamine that is FDA approved for the prophylaxis of allergic conjunctivitis.   Common adverse reactions include eye irritation, burning and/or stinging upon instillation, eye redness and eye pruritus, nasopharyngitis, headache, eye discharge, eye swelling, erythema of eyelid, eyelid edema, hypersensitivity, and somnolence.

# Adult Indications and Dosage

## FDA-Labeled Indications and Dosage (Adult)
- LASTACAFT is an H1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis.
- Instill one drop in each eye once daily. If more than 1 topical ophthalmic medicinal product is being used, each one should be administered at least 5 minutes apart.

## Off-Label Use and Dosage (Adult)

### Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Alcaftadine in adult patients.

### NonGuideline-Supported Use
There is limited information regarding Off-Label NonGuideline-Supported Use of Alcaftadine in adult patients.

# Pediatric Indications and Dosage

## FDA-Labeled Indications and Dosage (Pediatric)
There is limited information regarding Alcaftadine FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

## Off-Label Use and Dosage (Pediatric)

### Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Alcaftadine in pediatric patients.

### NonGuideline-Supported Use
There is limited information regarding Off-Label NonGuideline-Supported Use of Alcaftadine in pediatric patients.

# Contraindications
Alcaftadine is contraindicated in patients with hypersensitivity to any component in the product.

# Warnings
- To minimize eye injury and contamination of the dropper tip and solution, care should be taken not to touch the eyelids or surrounding areas with the dropper tip of the bottle. Keep bottle tightly closed when not in use.
- Patients should be advised not to wear a contact lens if their eye is red.
- Alcaftadine should not be used to treat contact lens-related irritation.
- Alcaftadine should not be instilled while wearing contact lenses. Remove contact lenses prior to instillation of alcaftadine. The preservative in alcaftadine, benzalkonium chloride, may be absorbed by soft contact lenses. Lenses may be reinserted after 10 minutes following administration of alcaftadine.
- Alcaftadine is for topical ophthalmic use only.

# Adverse Reactions

## Clinical Trials Experience
- Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
- The most frequent ocular adverse reactions, occurring in less than 4% of eyes treated with alcaftadine, were eye irritation, burning and/or stinging upon instillation, eye redness and eye pruritus.
- The most frequent non-ocular adverse reactions, occurring in less than 3% of subjects with eyes treated with alcaftadine, were nasopharyngitis and headache. Some of these events were similar to the underlying disease being studied.

## Postmarketing Experience
- The following adverse reactions have been identified during postmarketing use of alcaftadine in clinical practice. Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made. These reactions include: eye discharge, eye swelling, erythema of eyelid, eyelid edema, hypersensitivity, and somnolence.

# Drug Interactions
There is limited information regarding Alcaftadine Drug Interactions in the drug label.

# Use in Specific Populations

### Pregnancy
Pregnancy Category (FDA): B
- Pregnancy Category B. Reproduction studies performed in rats and rabbits revealed no evidence of impaired female reproduction or harm to the fetus due to alcaftadine. Oral doses in rats and rabbits of 20 and 80 mg/kg/day, respectively, produced plasma exposure levels approximately 200 and 9000 times the plasma exposure at the recommended human ocular dose. There are however, no adequate and well controlled studies in pregnant] women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
Pregnancy Category (AUS): 
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Alcaftadine in women who are pregnant.

### Labor and Delivery
There is no FDA guidance on use of Alcaftadine during labor and delivery.

### Nursing Mothers
- It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when alcaftadine is administered to a nursing woman.

### Pediatric Use
- Safety and effectiveness in pediatric patients below the age of 2 years have not been established.

### Geriatic Use
- No overall differences in safety or effectiveness were observed between elderly and younger subjects.

### Gender
There is no FDA guidance on the use of Alcaftadine with respect to specific gender populations.

### Race
There is no FDA guidance on the use of Alcaftadine with respect to specific racial populations.

### Renal Impairment
There is no FDA guidance on the use of Alcaftadine in patients with renal impairment.

### Hepatic Impairment
There is no FDA guidance on the use of Alcaftadine in patients with hepatic impairment.

### Females of Reproductive Potential and Males
There is no FDA guidance on the use of Alcaftadine in women of reproductive potentials and males.

### Immunocompromised Patients
There is no FDA guidance one the use of Alcaftadine in patients who are immunocompromised.

# Administration and Monitoring

### Administration
- Topical

### Monitoring
There is limited information regarding Alcaftadine Monitoring in the drug label.

# IV Compatibility
There is limited information regarding the compatibility of Alcaftadine and IV administrations.

# Overdosage
There is limited information regarding Alcaftadine overdosage.  If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

# Pharmacology

## Mechanism of Action
- Alcaftadine is a sterile, topically administered H1 receptor antagonist containing alcaftadine for ophthalmic use.
- Alcaftadine is a white to yellow powder with an empirical formula of C19H21N3O and a molecular weight of 307.39.
- Active: alcaftadine 0.25% (2.5 mg/mL)
- Inactives: benzalkonium chloride 0.005% as a preservative; edetate disodium; sodium phosphate, monobasic; purified water; sodium chloride; sodium hydroxide and/or hydrochloric acid (to adjust pH)

## Structure
- Alcaftadine is a sterile, topically administered H1 receptor antagonist containing alcaftadine for ophthalmic use.
- Alcaftadine is a white to yellow powder with an empirical formula of C19H21N3O and a molecular weight of 307.39.
- Active: alcaftadine 0.25% (2.5 mg/mL)
- Inactives: benzalkonium chloride 0.005% as a preservative; edetate disodium; sodium phosphate, monobasic; purified water; sodium chloride; sodium hydroxide and/or hydrochloric acid (to adjust pH)

## Pharmacodynamics
There is limited information regarding Alcaftadine Pharmacodynamics in the drug label.

## Pharmacokinetics
- Following bilateral topical ocular administration of alcaftadine ophthalmic solution, 0.25%, the mean plasma Cmax of alcaftadine was approximately 60 pg/mL and the median Tmax occurred at 15 minutes. Plasma concentrations of alcaftadine were below the lower limit of quantification (10 pg/mL) by 3 hours after dosing. The mean Cmax of the active carboxylic acid metabolite was approximately 3 ng/mL and occurred at 1 hour after dosing. Plasma concentrations of the carboxylic acid metabolite were below the lower limit of quantification (100 pg/mL) by 12 hours after dosing. There was no indication of systemic accumulation or changes in plasma exposure of alcaftadine or the active metabolite following daily topical ocular administration.
- The protein binding of alcaftadine and the active metabolite are 39.2% and 62.7%, respectively.
- The metabolism of alcaftadine is mediated by non-CYP450 cytosolic enzymes to the active carboxylic acid metabolite.
- The elimination half-life of the carboxylic acid metabolite is approximately 2 hours following topical ocular administration. Based on data following oral administration of alcaftadine, the carboxylic acid metabolite is primarily eliminated unchanged in the urine.
- In vitro studies showed that neither alcaftadine nor the carboxylic acid metabolite substantially inhibited reactions catalyzed by major CYP450 enzymes.

## Nonclinical Toxicology
- Alcaftadine was not mutagenic or genotoxic in the Ames test, the mouse lymphoma assay or the mouse micronucleus assay.
- Alcaftadine was found to have no effect on fertility of male and female rats at oral doses up to 20 mg/kg/day (approximately 200 times the plasma exposure at the recommended human ocular dose)

# Clinical Studies
- Alcaftadine was not mutagenic or genotoxic in the Ames test, the mouse lymphoma assay or the mouse micronucleus assay.
- Alcaftadine was found to have no effect on fertility of male and female rats at oral doses up to 20 mg/kg/day (approximately 200 times the plasma exposure at the recommended human ocular dose).

# How Supplied
- Alcaftadine ophthalmic solution) 0.25% is supplied in an opaque, white low-density polyethylene bottle with a white polypropylene cap.
- 3 mL fill in 5 mL bottle        NDC 0023-4290-03

## Storage
- Store at 15-25C (59-77F).

# Images

## Drug Images

## Package and Label Display Panel

# Patient Counseling Information
- To minimize eye injury and contamination of the dropper tip and solution, patients should be advised to not touch the eyelids or surrounding areas with the dropper tip, as this may contaminate the contents.
- If more than one topical ophthalmic drug is being used, the drugs should be administered at least five minutes apart.
- Patients should be advised not to wear a contact lens if their eye is red. Patients should be advised that LASTACAFT should not be used to treat contact lens-related irritation. Patients should also be advised to remove contact lenses prior to instillation of LASTACAFT. The preservative in LASTACAFT, benzalkonium chloride, may be absorbed by soft contact lenses. Lenses may be reinserted after 10 minutes following administration of LASTACAFT.
- For topical ophthalmic administration only.

# Precautions with Alcohol
Alcohol-Alcaftadine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

# Brand Names
- LASTACAFT 

# Look-Alike Drug Names
There is limited information regarding Alcaftadine Look-Alike Drug Names in the drug label.

# Drug Shortage Status

# Price