Alcaftadinum

Alcaftadinum Uses, Dosage, Side Effects, Food Interaction and all others data.

Alcaftadinum is an H1, H2 & H4 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. The activation of H1 receptor causes itching & H4 receptor causes itching & inflammation. Histamine binding with H1 & H2 receptor causes redness and swelling. Alcaftadinum also inhibit the release of histamine from mast cell through limit the entry of Ca++ across the membrane as a result prevent degranulation. Alcaftadinum also stabilize tight junction protein (zonula occludin) of conjuctival epithelium that normally becomes disorganized following allergen exposure so that decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.

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.

Alcaftadinum
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Alcaftadinum
Generic	Alcaftadine
Alcaftadine Other Names	Alcaftadina, Alcaftadine, Alcaftadinum
Type
Formula	C₁₉H₂₁N₃O
Weight	Average: 307.3895 Monoisotopic: 307.168462309
Protein binding	The protein binding of alcaftadine and the active metabolite are 39.2% and 62.7% respectively.
Groups	Approved
Therapeutic Class	Ophthalmic Anti-allergic preparations
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Alcaftadinum is used for the prevention of itching associated with allergic conjunctivitis.

Alcaftadinum is also used to associated treatment for these conditions: Seasonal Allergic Conjunctivitis

How Alcaftadinum works

Alcaftadinum is a H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.

Dosage

Alcaftadinum dosage

Instill one drop in each eye once daily.

Side Effects

Reported side effects are irritation, burning, eye redness, itching etc. Other side effects are headache, ocular pruritus and nasopharyngitis.

Precaution

The drug should not be instilled while wearing contact lenses. If hypersensitivity reaction occurs after instillation patients should be advised to discontinue the use of Alcaftadinum and consult with physicians.

Food Interaction

No interactions found.

Half Life

The elimination half-life of the carboxylic acid metabolite is approximately 2 hours following topical ocular administration.

Elimination Route

Based on data following oral administration of alcaftadine, the carboxylic acid metabolite is primarily eliminated unchanged in the urine.

Pregnancy & Breastfeeding use

Alcaftadinum is pregnancy Category B. Alcaftadinum has not been shown to cause birth defects or other problems during pregnancy and breastfeeding. It is not known whether Alcaftadinum is secreted in human milk or not. Caution should be exercised when Alcaftadinum is administered to a nursing mother.

Contraindication

It is contraindicated in persons with a known hypersensitivity to any component of this product.

Special Warning

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

Geriatric Use: No overall differences in safety or effectiveness were observed between elderly and younger subjects.

Acute Overdose

Ocular Adverse Reactions: The most frequent ocular adverse reactions, occurring in <4% of alcaftadine eye drops treated eyes were eye irritation, burning and/or stinging upon instillation, eye redness and eye pruritus.

Non-ocular Adverse Reactions: The most frequent non-ocular adverse reactions, occurring in <3% of subjects with alcaftadine eye drops treated eyes, were nasopharyngitis, headache and influenza. Some of these events were similar to the underlying disease being studied.