Dosing & Uses
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
Adverse Effects
>10%
Sneezing (82%)
Cough (16%)
Throat irritation (13%)
1-10%
Nasal irritation (8%)
Warnings
Contraindications
None
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.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)
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
Images
Formulary
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