Dosing & Uses
Dosage Forms & Strengths
intranasal spray
- 0.5mg/actuation
Smoking Cessation
Nicotine replacement therapy to reduce withdrawal symptoms during smoking cessation
1 spray/nostril (ie, 2 sprays to provide 1 mg/dose); typically 10-12 sprays/day in each nostril PRN
Initiate with 1-2 doses/hr; for greatest success, instruct patient to use at least 8 doses/day initially
Depending on individual addiction; may increase up to maximum dose of 40 mg (80 sprays/day)
Administration
Tilt head back when administering
Do not sniff, swallow, or inhale through the nose as the spray is being administered
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (1)
- cabotegravir
nicotine intranasal will decrease the level or effect of cabotegravir by increasing metabolism. Contraindicated. Cabotegravir is metabolized by UGT1A1 and UGT1A9. Strong UGT1A1 or UGT1A9 inducers decrease cabotegravir systemic exposure, thereby increasing potential for loss of virologic response.
Serious - Use Alternative (0)
Monitor Closely (11)
- adenosine
nicotine intranasal increases effects of adenosine by unknown mechanism. Use Caution/Monitor. Adenosine associated tachycardia and chest pain.
- cimetidine
cimetidine increases levels of nicotine intranasal by decreasing metabolism. Use Caution/Monitor.
cimetidine increases levels of nicotine intranasal by decreasing renal clearance. Use Caution/Monitor. - esketamine intranasal
esketamine intranasal, nicotine intranasal. Either increases toxicity of the other by sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor. Closely monitor blood pressure with concomitant use of esketamine nasal with stimulants. .
- green tea
green tea, nicotine intranasal. Other (see comment). Use Caution/Monitor. Comment: Green tea may include caffeine. Caffeine is a CNS-stimulant and additive effects may be seen when coadministered with other CNS stimulants. Caffeine should be avoided or used cautiously.
- naphazoline
naphazoline decreases levels of nicotine intranasal by Other (see comment). Use Caution/Monitor. Comment: Nasal vasoconstrictors prolong the time to peak concentrations by ~40% and decreases peak concentration by ~20%.
- oxymetholone
oxymetholone decreases levels of nicotine intranasal by Other (see comment). Use Caution/Monitor. Comment: Nasal vasoconstrictors prolong the time to peak concentrations by ~40% and decreases peak concentration by ~20%.
- phenylephrine nasal
phenylephrine nasal decreases levels of nicotine intranasal by Other (see comment). Use Caution/Monitor. Comment: Nasal vasoconstrictors prolong the time to peak concentrations by ~40% and decreases peak concentration by ~20%.
- propylhexedrine
propylhexedrine decreases levels of nicotine intranasal by Other (see comment). Use Caution/Monitor. Comment: Nasal vasoconstrictors prolong the time to peak concentrations by ~40% and decreases peak concentration by ~20%.
- solriamfetol
nicotine intranasal and solriamfetol both increase sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Use Caution/Monitor.
- varenicline
varenicline increases toxicity of nicotine intranasal by Other (see comment). Use Caution/Monitor. Comment: Varenicline is a partial agonist at the nicotinic Ach receptor; concomitant use with nicotine replacement therapy may increase adverse effects.
- xylometazoline
xylometazoline decreases levels of nicotine intranasal by Other (see comment). Use Caution/Monitor. Comment: Nasal vasoconstrictors prolong the time to peak concentrations by ~40% and decreases peak concentration by ~20%.
Minor (5)
- bupropion
bupropion, nicotine intranasal. Either increases effects of the other by pharmacodynamic synergism. Minor/Significance Unknown. Risk of hypertension.
- dihydroergotamine
dihydroergotamine, nicotine intranasal. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Additive vasospasm.
- dihydroergotamine intranasal
dihydroergotamine intranasal, nicotine intranasal. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Additive vasospasm.
- niacin
nicotine intranasal increases effects of niacin by pharmacodynamic synergism. Minor/Significance Unknown.
- rose hips
nicotine intranasal decreases levels of rose hips by increasing elimination. Minor/Significance Unknown.
Adverse Effects
>10%
Local irritation (94%)
1-10%
Anxiety
Irritability
Restlessness
Cravings
Dizziness
Impaired concentration
Weight increase
Emotional lability
Somnolence and fatigue
Increased sweating
Insomnia
Confusion
Depression
Apathy
Tremor
Increased appetite
Incoordination
Increased dreaming
Warnings
Contraindications
Hypersensitivity
Cautions
Irritating to nasal mucosa
Not studied in reactive airway disease; may cause bronchospasm
Caution with hypertension, cardiovascular, or peripheral vascular disease
Caution with hyperthyroidism, pheochromocytoma, or insulin-dependent diabetes, since nicotine causes the release of catecholamines by the adrenal medulla
Delays healing of peptic ulcer disease
Pregnancy & Lactation
Pregnancy Category: D
Lactation: Distributed in breast milk; milk to plasma ratio is 2.9
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
Agonist at nicotinic receptors
Absorption
Bioavailability: 53%
Peak plasma time: 4-15 minutes
Peak plasma concentration: 2-12 ng/mL
Absorption half-life: 3 minutes
Distribution
Protein bound: <5%
Vd: 2-3 L/kg
Metabolism
Metabolized primarily in the liver; some metabolism also takes place in kidney and lungs
More than 20 metabolites of nicotine identified, all are less active than the parent compound
The primary urinary metabolite is cotinine (15% of the dose)
Elimination
Half-life: 1-2 hr (nicotine); 15-20 hr (cotinine)
Plasma clearance: 1.2 L/min
Excretion: Urine (10-30% unchanged)
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Formulary
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