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VARENICLINE (TYRVAYA®) NOSE SPRAY FOR THE TREATMENT OF DRY EYES
woman using nose spray

February 13, 2022 - When most providers think of varenicline, they think of smoking cessation, and when they think of dry eye treatment, they think of eye drops. A new product aims to change these perceptions. Tyrvaya is a nasal spray for dry eyes that contains varenicline, the active ingredient in the smoking cessation drug Chantix. Varenicline is a nicotine agonist/antagonist that binds nicotine acetylcholine receptors and stimulates a low level of nicotine activity (agonist effect) while simultaneously blocking nicotine from binding the receptor (antagonist effect). Its mechanism in treating dry eye disease is believed to occur through stimulation of nicotine acetylcholine receptors in the trigeminal nerve, which leads to increased tear production.

In trials, varenicline nasal spray was superior to placebo in improving results on the Schirmer's test. The Schirmer's test is a test for dry eye disease that involves placing a strip of filter paper inside the lower lid of the eye and measuring the amount of fluid that is absorbed. Fluid absorption is quantified by the linear movement of liquid in millimeters along the strip and is interpreted as follows: 0 - 5 mm, severe dry eyes; 5 - 10 mm, moderate dry eyes; 10 - 15 mm, mild dry eyes; more than 15 mm, normal tear function. In a 28-day study involving 512 patients with dry eyes (average baseline Schirmer’s score of 5 mm), 47% of patients treated with Tyrvaya had an increase of ≥ 10 mm on their Schirmer's score compared to 28% of placebo-treated patients (p<0.0001). Overall, patients in the Tyrvaya group had an average increase in their Schirmer’s score of 11.3 mm compared to 6.3 mm in the placebo group. [PubMed abstract] These results are more impressive than what has been seen with Restasis, another popular treatment for dry eyes. In a 6-month Restasis trial involving 1200 patients, improvement in the Schirmer's score of ≥ 10 mm was achieved in 15% of Restasis-treated patients and 5% of placebo-treated patients. It's important to note that although highly popular and frequently advertised, Restasis was never approved in many countries due to a lack of proven efficacy.

Tyrvaya is dosed as one spray in each nostril twice daily. It has no contraindications or precautions, and the main side effect is sneezing, which is seen in up to 95% of patients. In trials, sneezing usually occurred within a minute of administration and was characterized as transient and mild. Other side effects include cough (19%), throat irritation (14%), and nose irritation (8%).

Dry eyes can be challenging to treat, and the efficacy of Restasis was always questionable. Tyrvaya appears to be a viable therapy that may provide relief for a significant number of people, as long as they don't mind a little sneezing.

RELATED LINK

Tyrvaya prescribing information