Tyrvaya®
Varenicline 0.06% · nasal spray
Dry Eye/OSD
Approved uses
Dry eye disease
1 spray in each nostril BID, approximately 12 hours apart; prime with 7 actuations before first use and re-prime with 1 actuation after more than 5 days unused
Tear production rises by week 4 and holds at 12 weeks; dryness symptoms did not improve.
OFF-LABELNot in the FDA label for this product
Perioperative dry eye with LASIK, PRK, or corneal collagen crosslinking, started before surgery
1 spray in each nostril BID beginning 28 days before surgery, continued 84 days after LASIK or PRK and 28 days after crosslinking
3 RCTs · n=101 · all negative
Three small vehicle-controlled trials from one investigator group, randomized per the published reports (LASIK n=40, PRK n=41, crosslinking n=20): no primary endpoint reached statistical significance in any of the three, leaving only directional trends in corneal staining, tear osmolarity, and epithelial closure. The LASIK report concluded that a larger trial is needed.
Contraindications
None.
Available FormsCarton of 2 nasal spray bottles, 4.2 mL each, 60 sprays per bottle (30-day supply), 0.03 mg varenicline per 0.05 mL spray, 0.6 mg/mL solution
Mechanism of ActionNicotinic acetylcholine receptor agonist delivered intranasally; binding activates the trigeminal parasympathetic pathway and increases basal tear film production. Partial agonist at α4β2, α4α6β2, α3β4 and α3α5β4 receptors and full agonist at α7; the label states the exact mechanism is unknown.
Warnings & Precautions
- Contraindications: Allergic reactions to varenicline or other ingredients in the formulation.
- Warnings/Precautions: Patients should inform their healthcare provider if they are pregnant, planning a pregnancy, or breastfeeding. The medication is for nasal use only.
- Common Side Effects: Sneezing, cough, throat irritation, nose irritation. Most side effects are mild, and less than 2% of patients in clinical trials discontinued treatment due to side effects.
Common Side Effects
- Nasal: Sneezing 82%, instillation-site (nose) irritation 8% (n=349 across three dry eye trials).
- Respiratory: Cough 16%, throat irritation 13%.
- Ocular: None reported.
- Severity and tolerability: Sneezing and cough transient and predominantly mild; 93.5% of varenicline-treated subjects across three trials completed the treatment period.
Pregnancy & LactationPregnancy: No human data. Animal reproduction studies produced no fetal structural abnormalities; maternal toxicity with reduced fetal weights occurred in rabbits at 4864 times the MRHD, and offspring of rats dosed at 1216 times the MRHD showed decreased fertility and increased auditory startle response.
Lactation: No human data on presence in milk, effects on the infant, or milk production; varenicline is present in the milk of lactating rats.
Pediatric UseSafety and efficacy not established in pediatric patients.