Alcaftadine, sold under the brand name Lastacaft, is an

antihistamine Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provide ...

used to help prevent itching of the eyes. It is an H1 histamine receptor antagonist. It is given as an

drops Drop, DROP, drops or DROPS may refer to: * Drop (liquid) or droplet, a small volume of liquid ** Eye drops, saline (sometimes mydriatic) drops used as medication for the eyes * Drop (unit), a unit of measure of volume * Falling (physics), allowin ...

in the

eye Eyes are organs of the visual system. They provide living organisms with vision, the ability to receive and process visual detail, as well as enabling several photo response functions that are independent of vision. Eyes detect light and conv ...

. It was approved for medical use in the United States in July 2010. It is available as a

generic medication A generic drug is a pharmaceutical drug that contains the same chemical substance as a drug that was originally protected by chemical patents. Generic drugs are allowed for sale after the patents on the original drugs expire. Because the active c ...

and as an

over-the-counter medication Over-the-counter (OTC) drugs are medicines sold directly to a consumer without a requirement for a prescription from a healthcare professional, as opposed to prescription drugs, which may be supplied only to consumers possessing a valid prescr ...

Medical uses

Alcaftadine is

indicated In medicine, an indication is a valid reason to use a certain test, medication, procedure, or surgery. There can be multiple indications to use a procedure or medication. An indication can commonly be confused with the term diagnosis. A diagnosis ...

for the prevention of itching associated with allergic conjunctivitis.

Pharmacology

Alcaftadine is an antagonist of histamine receptor 1. By blocking the receptor, alcaftadine has been shown to reduce itching and redness of the eyes, and to reduce recruitment of

eosinophils Eosinophils, sometimes called eosinophiles or, less commonly, acidophils, are a variety of white blood cells (WBCs) and one of the immune system components responsible for combating multicellular parasites and certain infections in vertebrates. A ...

after exposure to an allergen. Alcaftadine reduces the number of eosinophils compared to olopatadine 0.1%, and in animal models, alcaftadine 0.25% decreased the expression of the epithelial protein E-cadhedrin-1 compared to placebo. Reducing E-cadherin decreases junctions that lead to the progression of allergic conjunctivitis.

Adverse effects

In studies comparing the effectiveness of olopatadine to alcaftadine, there was not a dose-response increase of adverse effects as alcaftadine doses increases for 0.05% to 0.1% to 0.25%. The most common seen side effect of alcaftadine administration was irritation or a stinging sensation at the administration site.

Pharmacokinetics

Because alcaftadine is administered at low concentrations and at a local site (the eye), it appears to have minimal systemic effects, and the low absorption of alcaftadine results in minimal systemic accumulation.

History

When alcaftadine was tested against placebo and olopatadine, only alcaftadine 0.25% showed a clinically significant reduction in conjunctival redness scores 7 and 15 minutes after administration. Alcaftadine 0.05%, 0.1%, and 0.25% all reduced lid swelling, conjunctival redness, and ocular itching/tearing compared to placebo.

Society and culture

Economics

Allergan, Inc. Allergan, Inc. was an American global pharmaceutical company focused on eye care, neurosciences, medical dermatology, medical aesthetics, breast enhancement, obesity intervention and urologics. Allergan, Inc. was formed in 1948, incorporated in ...

began selling alcaftadine under the trade name Lastacaft after it was approved by the US

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food ...

in July 2010. By March 2012, 139,000 prescriptions had been written for 104,000 unique patients, and alcaftadine exceeded the sales of epinastine (Elestat).

Legal status

Alcaftadine was approved for medical use in the United States in July 2010.

References

{{Authority control H1 receptor antagonists Mast cell stabilizers Drugs developed by AbbVie Ophthalmology drugs