nicotine intranasal (Rx)

Brand and Other Names:Nicotrol NS
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Dosing & Uses

AdultPediatric

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

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Interactions

Interaction Checker

and nicotine intranasal

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            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.

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              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

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              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

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              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.

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              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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              Images

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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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              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
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              Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the 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.