varenicline intranasal (Rx)

Brand and Other Names:Tyrvaya
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

intranasal solution

  • 1 actuation delivers 0.03mg/0.05mL

Dry Eye Disease

Indicated for treatment of signs and symptoms of dry eye disease

0.03 mg (1 actuation) in each nostril q12hr (ie, 0.06 mg q12hr)

Safety and efficacy not established

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Adverse Effects

>10%

Sneezing (82%)

Cough (16%)

Throat irritation (13%)

1-10%

Nasal irritation (8%)

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Warnings

Contraindications

None

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Pregnancy & Lactation

Pregnancy

Data are not available regarding use in pregnant females to inform any drug-associated risks

Animal studies

  • In rat and rabbit reproduction studies, varenicline did not produce malformations at clinically relevant doses

Lactation

Data are not available on presence in human milk, effects on breastfed infants, or effects on milk production

In animal studies, varenicline was present in milk of lactating rats; however, owing to species-specific differences in lactation physiology, animal data may not reliably predict drug levels in human milk

Lack of clinical data during lactation precludes a clear determination of the risk to an infant during lactation; however, consider the developmental and health benefits of breastfeeding along with the mother’s clinical need

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

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Pharmacology

Mechanism of Action

Exact mechanism of action is unknown

It is believed that the highly selective activity at heteromeric subtypes(s) of the nicotinic acetylcholine receptor where its binding produces agonist activity and activates the trigeminal parasympathetic pathway resulting in increased production of basal tear film

The parasympathetic nervous system controls tear film homeostasis, partially via the trigeminal nerve, which is accessible within the nose

Absorption

0.12-mg dose

  • Note: Higher dose than recommended used for pharmacokinetic studies
  • Peak plasma time: 2 hr
  • Peak plasma concentration: 0.34 ng/mL
  • AUC: 7.46 h⋅ng/mL; ~7.5% of systemic exposure observed following 1 mg PO varenicline

Metabolism

Minimally metabolized

Elimination

Half-life: ~19 hr

Excretion: Urine 92% (unchanged)

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Administration

Intranasal Administration

Clear nostrils by blowing the nose

Place cap and clip on the nasal applicator after each use

Missed dose: Resume regular dosing at next scheduled dose time

Priming

  • Prime before initial use by pumping 7 actuations into the air away from face
  • If not used for >5 days, reprime with 1 spray
  • Do not shake

Storage

Store at 20-25ºC (68-77ºF)

Do not freeze

Discard 30 days after opening bottle

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Images

No images available for this drug.
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Patient Handout

A Patient Handout is not currently available for this monograph.
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Formulary

FormularyPatient Discounts

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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.