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Varenicline (nasal): Drug information

Varenicline (nasal): Drug information
(For additional information see "Varenicline (nasal): Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Brand Names: US
  • Tyrvaya
Pharmacologic Category
  • Cholinergic Agonist
Dosing: Adult
Dry eye disease

Dry eye disease: One spray in each nostril twice daily (~12 hours apart).

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Nasal, as tartrate:

Tyrvaya: 0.03 mg/actuation (4.2 mL)

Generic Equivalent Available: US


Administration: Adult

Intranasal: For use in nostrils only; do not spray in eyes or mouth. Do not shake bottle. Prime pump (press 7 times into air away from face) prior to first use. If spray unused for >5 days, reprime with 1 spray into the air. Blow nose if needed to clear nostrils. Tilt head back slightly without lying down. Insert applicator into nostril, pointing the tip toward the top of the ear, leaving space between tip of the applicator and wall of nose. Place tongue on roof of mouth and breathe gently while pressing pump to release spray. Do not spray directly at the septum. Wipe applicator with a clean tissue after each use. A 1-month supply consists of 2 bottles; finish the first bottle before opening the second bottle.

Use: Labeled Indications

Dry eye disease: Treatment of the signs and symptoms of dry eye disease.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Reported adverse reactions are for adults.


Respiratory: Cough (16%), sneezing (82%), throat irritation (13%)

1% to 10%:

Local: Application site irritation (8%)


There are no contraindications listed in the manufacturer's labeling.

Metabolism/Transport Effects

None known.

Drug Interactions

There are no known significant interactions.

Pregnancy Considerations

Adverse events were not observed in animal reproduction studies following administration of oral varenicline at clinically relevant doses.

Varenicline is absorbed systemically following nasal administration; concentrations are ~7.5% of an oral 1 mg dose.

Breastfeeding Considerations

It is not known if varenicline is present in breast milk.

According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother.

Mechanism of Action

Partial α4 β2, α4 α6 β2, α3 β4, α3 α5 β4, and full α7 neuronal nicotinic acetylcholine receptor agonist with binding at the heteromeric sub-type(s) of the nicotinic acetylcholine receptor–producing agonist activity and activation of the trigeminal parasympathetic pathway resulting in increased production of basal tear film.


Metabolism: Minimal.

Half-life elimination: ~19 ± 10 hours.

Time to peak: ≤2 hours.

Excretion: Urine (92% as unchanged drug).

Pricing: US

Solution (Tyrvaya Nasal)

0.03 mg/ACT (per mL): $84.61

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

  1. Tyrvaya (varenicline) [prescribing information]. Princeton, NJ: Oyster Point Pharma; October 2021.
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