The FDA recently approved the first prescription-only topical eye formulation of the second-generation antihistamine cetirizine for the treatment of eye itching related to sensitive conjunctivitis.
Cetirizine ocular option 0.24% (Zerviate, Nicox Ophthalmics Inc; accredited to Eyevance Pharmaceuticals, LLC) showed robust effectiveness in 3 randomized, double-masked, placebo-controlled clinical trials using the Ora Conjunctival Irritant Challenge (CAC) design among people with sensitive conjunctivitis.
Two of the trials that reviewed start and duration showed that cetirizine ophthalmic solution resulted in statistically as well as medically considerably less ocular itching versus control group at 15 mins and 8 hrs after therapy.
The ophthalmic solution breaks the 10-year drought since the last approval for allergic conjunctivitis treatment , with the twice-daily drops hitting the marketplace in March 2020.
Cetirizine hydrochloride is recognized as the number one oral antihistamine allergy treatment recommended by specialists, with 23 years on the market and plenty of doctor and patient years of experience.
Based upon its large record of therapeutic success as well as safety in various formulations, the industry sought to develop cetirizine as an ocular option.
Allergic conjunctivitis affects at the very least 30% of Americans. Reactions range anywhere from light – making it just a self-limiting problem – to the other end of the range, when allergies come to be an incapacitating condition, causing patients to have a dramatically impaired lifestyle.
Allergens, whether tree and also grass pollens, pet hair as well as dander, or any number of various other environmental insults, show up in the familiar cascade of ocular symptoms that include itching, inflammation, chemosis, tearing, and eyelid swelling.
Many thanks to the vast work being done around ocular surface condition and also completely dry eye – along with fine-tuning of diagnostic and treatment algorithms – awareness among eye treatment experts to identify and deal with the “Pink Eye” is improving.
Allergic conjunctivitis is a constant and considerable piece of the puzzle when it involves locating the root cause of ocular surface condition.
Patients with allergies commonly have bilateral symptoms, with the most usual ocular signs being itching, burning, soreness, as well as tearing.
Allergic conjunctivitis is typically connected with swelling, a crucial area of distinction from dry eye condition. Eversion of the lower lid is extremely recommended to examine the degree of chemosis.
In reaction to an allergen, the process of conjunctivitis has an early acute phase followed by a late phase. Allergens connect with immunoglobulin E, which is bound to mast cells that in turn activate increased histamine and also subsequent degranulation.
The release of histamine as well as other proallergic mediators during the acute stage causes itching, vasodilation, and vascular leak. This is adhered to by ocular soreness, chemosis, and lid swelling.
Mast cells then synthesize, releasing cytokines, chemokines, as well as growth factors, which start a cascade of inflammatory events.
During the last late-phase reaction, eosinophils, neutrophils, as well as macrophages infiltrate conjunctival cells.
The commonly used and approved treatments for ocular allergic reactions include antihistamines and also mast cell stabilizers, or both; and these agents act to reduce the signs and symptoms of the early-phase reaction.
Ocular form of cetirizine
Cetirizine is a second-generation antihistamine (very selective H1 receptor antagonis) that binds competitively to histamine receptor sites to reduce swelling, itching, and also vasodilation. Two phase 3 efficiency studies exposed strong and similar anti-itch efficiency of cetirizine sensory service 0.24% compared with vehicle (utilizing the CAC design).
The single-center (study 1) as well as multi-center (research 2), double-masked, randomized, vehicle-controlled, parallel group CAC researches were conducted over approximately 5 weeks and 4 study visits.
Patients with modest as well as serious symptoms were enlisted in the trials, and study 2 needed patients to have more extreme allergic conjunctivitis symptoms. Subjects were screened for an irritant reaction at visit 1 as well as 2 and then randomized at visit 3.
Nearly 100 subjects were randomly assigned in each study. The key efficacy end points were ocular irritation as well as conjunctival soreness, 15 minutes and 8 hrs posttreatment, post-CAC.
Quells itching quickly
Researchers provided cetirizine 15 mins or 8 hrs prior to CAC, as well as subjects had substantially lower eye itching at all time factors post-CAC (P <.0001) compared to vehicles in both studies.
The researchers’ reading of conjunctival inflammation was substantially reduced after cetirizine therapy contrasted to vehicle at 7 mins post-CAC and at both 15 mins as well as 8 hours posttreatment in both studies (P <.05).
Many secondary end points, ocular and nasal, were also analyzed.
It needs to be noted that the most robust treatment distinctions were observed in research 2, where clients were called for to have a lot more severe symptoms in order to be included (P <.05). Investigators recognized no safety issues for cetirizine ocular remedy 0.24%.
Comfort is vital
For added comfort, cetirizine sensory solution 0.24% is developed with Hydrella, that includes glycerin as well as hydroxypropyl methylcellulose, active ingredients generally found in lubricant drops.
Patients in the FDA trials reported a mean comfort rating of less than 1 at any time points (on a scale of 1-10, with 1 being the most comfy). The solution is also developed with a neutral pH of 7.0, similar to the all-natural tear film.
Eye-care service providers currently have an option for patients with sensitive conjunctivitis experiencing disruptive ocular itching.
The drop form of cetirizine ocular solution 0.24% provides eye care providers a chance to substantially enhance patients’ quality of life with an effective and also targeted approach.
Especially, unlike some oral antihistamines, the new formula did not cause drowsiness.
Cetirizine ophthalmic solution 0.24% is a strong therapeutic with a capacity to promptly subdue eye itching for patients experiencing allergic conjunctivitis.
There are no safety concerns identified with cetirizine treatment. Drop comfort is ranked as “very comfortable.”