February 01, 2010
3 min read
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Drop relieves early- and late-stage allergic mediators

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An oral medication that has been formulated into an eye drop for treating allergic conjunctivitis has also been found to alleviate the symptoms of nasal rhinitis.

Bepreve (bepotastine besilate ophthalmic solution 1.5%, Ista Pharmaceuticals) is a mast-cell stabilizer with a highly selective affinity for the histamine1 (H1) receptor.

Allergist Warner W. Carr, MD, FAAAAI, FACAAI, states that one of the unique benefits of Bepreve is its ability to work against both early- and late-stage allergic reactions.

“Bepreve works by stabilizing the mast cell so it doesn’t release histamine, but it also blocks the histamine once it’s been released. It’s dual-acting and has a fast onset of action,” Dr. Carr told Primary Care Optometry News.

“By instilling this product into the eye, some of it is getting into the nose, and about 20% of patients can actually taste it,” he continued. “By doing this, the same reaction is taking place in the nose as in the eye.”

Bepreve also works by inhibiting IL-5 and the production and migration of eosinophils to prevent tissue damage, according to the manufacturer. In addition, Bepreve reduces other secondary mediators including LTB-4 to further repress the allergy cascade.

According to PCON Editorial Board member Paul M. Karpecki, OD, FAAO, Bepreve works quickly and is comfortable for patients to use twice a day.

“It has a fast onset, which is valuable,” he said in an interview. “You always want to see a response right away when the patient is in your office.”

Works against late-stage mediators

Jill C. Autry, RPh, OD, also a PCON Editorial Board member, has found that her patients with nasal symptomatology in addition to their ocular complaints feel relief while using Bepreve for their allergic conjunctivitis.

“One secondary endpoint that was discovered during clinical trials was nasal congestion,” she told PCON. “Many patients who have eye itching also have associated nasal allergic symptoms. So I’ve been trying to specifically select those patients and ask them for feedback, and I’d say that every patient I had with symptomatology of both nasal and ocular irritation from allergies does very well on the product.”

According to Dr. Carr, patients with nasal symptoms find relief from this eye drop due to the molecule bepotastine.

“When the allergic reaction occurs, there’s an immediate response where the allergy cells release histamine and other chemicals,” he said. “Some of those chemicals attract allergy cells and other immune cells into the area where the reaction took place. Once those cells come in, you have a late-phase inflammatory response. In the nose, the late-phase symptom manifested is nasal congestion, which is when cells line the nasal and sinus cavities, causing an ongoing inflammatory response.”

Impending nasal formulation

Currently, bepotastine is approved in Japan for use as an oral medication for the treatment of nasal rhinitis under the brand name Talion. In the United States in 2007, Ista licensed executive North American rights to nasal dosage forms of bepotastine, and future rights for oral dosage.

Though Ista did not release a timeline for the development and implementation of a nasal form of bepotastine for nasal rhinitis, Dr. Carr is certain it will be an effective treatment for patients’ nasal complaints.

“Today, the cornerstone of treating allergic rhinitis, otherwise known as hay fever, is a nasal steroid that takes time to work and has the risk of side effects. If [bepotastine] was formulated into a nasal spray, I would expect it to have good efficacy,” Dr. Carr said.

For more information:

  • Warner W. Carr, MD, FAAAAI, FACAAI, is the associate medical director of Southern California Research and can be reached at the Allergy and Asthma Associates of Southern California, 27800 Medical Center Road, Suite #244, Mission Viejo, Ca 92691; (949) 364-2900; fax: (949) 364-0134; e-mail: warnercarr@hotmail.com. Dr. Carr has nodirect financial interest in the products mentioned in this article. He is a paid consultants for Ista.
  • Paul M. Karpecki, OD, FAAO, is clinical director of Corneal Services and Ocular Surface Research for Koffler Vision Group and a member of the Editorial Board of Primary Care Optometry News. He can be reached at 120 N. Eagle Creek Drive, Ste 431, Lexington, KY 40509; (859) 227-7781; fax: (859) 263-5694; e-mail: paul@karpecki.com. Dr. Karpecki has no direct financial interest in the products mentioned in this article. He is a paid consultants for Ista.
  • Jill C. Autry, RPh, OD, is a member of the PCON Editorial Board and can be reached at the Eye Center of Texas, 6565 West Loop South, Ste. 650, Bellaire, TX 77401; (713) 797-1010; fax: (713) 797-6200; e-mail: jillautry@gmail.com. Dr. Autry has no direct financial interest in the products mentioned in this article, nor is she a paid consultant for any companies mentioned.