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Nicotine

Class: Autonomic Drugs, Miscellaneous
- Smoking Deterrents
- Deterrents, Smoking
VA Class: AD900
Chemical Name: S-3-(1-Methyl-2-pyrrolid inyl)pyridine
Molecular Formula: C10H14N2• x(C10H10•C4H6O2)x
CAS Number: 54-11-5
Brands: Commit, Nicoderm CQ, Nicorette, Nicotrol Inhaler, Nicotrol NS

Medically reviewed by Drugs.com. Last updated on June 10, 2019.

Introduction

Ganglionic (nicotinic) cholinergic-receptor agonist.

Uses for Nicotine

Smoking Cessation

Used for nicotine replacement therapy as a temporary adjunct in the cessation of cigarette smoking either unsupervised (self-medication) or in conjunction with a behavior modification program under clinician supervision.

Nicotine replacement therapy considered one of several first-line therapies by USPHS for treatment of tobacco dependence. For additional information, consult the most current USPHS clinical practice guideline available at [Web]

Nicotine replacement therapy provides alternative sources of nicotine that help reduce the withdrawal symptoms associated with nicotine dependence. Chewing the resin complex-containing gum may act as a substitute oral activity in behavior modification.

Electronic nicotine delivery systems (ENDS) such as electronic cigarettes (e-cigarettes) have been used to aid smoking cessation attempts; however, these products are not approved by FDA for this use and evidence is limited regarding their efficacy and safety. The role of ENDS relative to conventional nicotine replacement therapies for smoking cessation remains to be established.

Ulcerative Colitis

Transdermal nicotine has been used in the management of ulcerative colitis.

Nicotine Dosage and Administration

General

  • To increase smoking cessation rate, use as part of a comprehensive program of multiple treatment strategies, including behavioral modification.

  • Individualize duration of therapy based on patient response and degree of nicotine dependence.

  • Stop smoking prior to initiating nicotine replacement therapy; self-medication not recommended in patients who continue to smoke, chew tobacco, or use snuff or other nicotine-containing preparations.

  • Discontinue therapy in patients who continue to smoke 4 weeks after initiating treatment; may use nicotine replacement therapy again in subsequent attempts to quit smoking.

Administration

Administer nicotine percutaneously by topical application of a transdermal system.

Administer nicotine transmucosally by oral inhalation using a special nicotine oral inhaler or intranasally using a metered-dose spray pump.

Administer nicotine polacrilex intrabuccally (transmucosally) as a lozenge or chewing gum.

May be administered as a single nicotine preparation (i.e., intrabuccally, intranasally, percutaneously, or by oral inhalation); however, if single therapy does not enable patients to quit smoking, use of transdermal nicotine may be combined with another form of nicotine replacement (i.e., either buccal nicotine polacrilex or nicotine nasal spray).

Buccal Administration

Chewing Gum

Self-administer one piece of gum in response to the urge to smoke.

Chew gum very slowly until a distinctive peppery taste of nicotine, minty, cinnamon, or orange taste of the gum, or a slight tingling in the mouth is perceived (typically about 15 chews); stop chewing gum and park between cheek and gum; once tingling is almost gone (about 1 minute), repeat chewing procedure. Continue for about 30 minutes or until taste dissipates. Do not swallow gum.

Do not eat or drink anything other than water for 15 minutes before and during chewing of gum.

Do not chew multiple pieces of gum simultaneously; do not chew too rapidly or chew pieces in succession. May cause excessive release of nicotine and result in adverse effects (e.g., lightheadedness, nausea, vomiting, irritation of the throat and mouth, hiccups, indigestion).

Chew at least 9 pieces of gum daily to improve chances of quitting.

Do not attempt to discontinue nicotine polacrilex gum therapy until craving is satisfied by 1 or 2 pieces of the gum daily, but do not continue therapy for >6 months, unless otherwise instructed by clinician.

4-mg strength gum recommended in highly dependent smokers because of evidence of increased efficacy.

Lozenges

Suck on lozenge until dissolved; do not swallow, bite, or chew. Allow to slowly dissolve in the mouth over 20–30 minutes, periodically moving the lozenge (e.g., with the tongue) from one side of the mouth to the other; minimize swallowing. A warm or tingling sensation may be perceived.

Do not eat or drink anything other than water for 15 minutes before and during sucking on the lozenge.

Use at least 9 lozenges daily for the first 6 weeks to improve chances of quitting.

Using >1 lozenge simultaneously or using one lozenge after another in uninterrupted sequence may result in adverse effects (e.g., hiccups, heartburn, nausea).

Self-administer lozenge in response to nicotine craving; decrease frequency of administration over time.

Topical Administration

Administer percutaneously by topical application of a transdermal system once daily.

Apply at the same time each day, usually after awakening.

Expose the adhesive surface of the system by peeling and discarding the protective liner just prior to application and apply system immediately to avoid loss of nicotine through volatilization.

Apply transdermal system to a clean, dry, hairless area of intact skin on the trunk or upper outer arm by firmly pressing the system with the adhesive side touching the skin. Press system firmly in place with heel of hand for about 10 seconds, ensuring good contact, particularly around the edges. Do not apply to sites that are oily, damaged, or irritated; if necessary, hair may be clipped, but do not shave area.

System may be worn for 16 or 24 hours. If cravings begin upon awakening, wear patch for 24 hours. If vivid dreams or sleep disruptions occur, wear patch for 16 hours; remove at bedtime and apply new patch upon awakening.

If system inadvertently comes off during the period of use, apply a new system; continue current application schedule or change so that the next system is applied 24 hours later.

Rotate application sites to minimize potential skin irritation; allow ≥1 week before reusing a given site. (See Dermatologic Effects under Cautions.)

Avoid unnecessary contact with transdermal systems. Avoid touching eyes after handling; wash hands with water alone as soap may enhance percutaneous absorption.

Intranasal Administration

Administer intranasally using a metered-dose spray pump.

Prime spray pump prior to initial use by spraying into a tissue until a fine spray is seen (6–8 times); discard tissue.

If spray pump is not used for 24 hours, reprime pump by spraying into a tissue 1–2 times.

Clear nasal passages prior to administration.

Tilt the head back slightly; insert tip of bottle into one nostril as far as is comfortable. Breathe through the mouth and spray once into nostril; do not sniff, swallow, or inhale through the nose while administering. Repeat this procedure for the other nostril.

If nose runs, sniff gently to keep nasal spray in nose; wait 2–3 minutes before blowing nose.

Avoid contact with skin, eyes, and mouth; if contact occurs, rinse with plain water immediately. If intranasal bottle breaks, wear protective gloves, wipe with paper towels, and wash surfaces thoroughly.

Oral Inhalation

Administer transmucosally as an inhaled vapor by oral inhalation using a special nicotine oral inhaler that mimics smoking cigarettes.

Hold the oral inhaler with two hands; separate the top and bottom pieces by pushing and turning the pieces until markings line up. Insert one nicotine cartridge and push the cartridge until it pops into place. Line up markings on the top and bottom pieces of the inhaler and push pieces together tightly; lock inhaler by turning pieces until markings do not line up.

Place the mouthpiece of the inhaler between lips and puff on the inhaler using rapid shallow sucking (“buccal mode”); alternatively, inhale slowly and deeply into back of throat (“pulmonary mode”). Nicotine is vaporized and absorbed in mouth and throat. (See Absorption under Pharmacokinetics.) Shallow puffing method generally is preferred. Deep inhalation technique requires considerable effort and does not result in substantially increased drug delivery or other benefits.

Individualize orally inhaled dosage to the level of nicotine replacement required; optimum results generally achieved by frequent continuous puffing of the inhaler over 20 minutes.

Nicotine is used up from cartridge after about four 5-minute sessions or one 20-minute session of active puffing.

When cartridge is empty, remove top of mouthpiece; discard empty cartridge away from children and pets. Store with mouthpiece in locked position and cartridges in plastic case. Clean reusable mouthpiece regularly with soap and water.

Use inhaler at temperatures >60°F; cold temperatures decrease the amount of nicotine inhaled.

Also administered transmucosally as an inhaled vapor by oral inhalation via electronic nicotine delivery systems (ENDS) such as e-cigarettes and vape pens; however, safety and efficacy in smoking cessation not evaluated by FDA.

Dosage

Chewing gum and lozenges available as nicotine polacrilex; dosage expressed in terms of nicotine.

Nicotine oral inhaler cartridges labeled as containing 10 mg of nicotine deliver ≤4 mg total with repeated inhalation. The amount of nicotine released depends on the volume and temperature of the air passing through the inhaler. An intensive inhalation regimen (80 deep inhalations over 20 minutes) releases approximately 4 mg of nicotine.

Metered nasal spray delivers 0.5 mg of the nicotine per metered spray and about 200 sprays (i.e., 100 doses) per 100-mg container.

Adults

Smoking Cessation
Buccal (Chewing Gum)

Patients who smoke <25 cigarettes daily: Chew a 2-mg piece of gum every 2 hours during weeks 1–6; chew a 2-mg piece every 2–4 hours during weeks 7–9; and chew a 2-mg piece every 4–8 hours during weeks 10–12 of therapy. Alternatively, chew a 2-mg piece of gum whenever the urge to smoke occurs; do not exceed 2 pieces (4 mg) per hour.

Patients who smoke ≥25 cigarettes daily: Chew a 4-mg piece of gum every 2 hours during weeks 1–6; chew a 4-mg piece every 2–4 hours during weeks 7–9; and chew a 4-mg piece every 4–8 hours during weeks 10–12 of therapy. Alternatively, chew a 4-mg piece whenever the urge to smoke occurs; do not exceed 2 pieces (8 mg) per hour.

Taper dosage by chewing each piece for only 10–15 minutes and gradually reducing the number of pieces chewed, or chew each piece for longer than 30 minutes but reduce the total pieces per day, or substitute regular chewing gum for some pieces.

Buccal (Lozenges)

Patients who smoke first cigarette >30 minutes after waking: One 2-mg lozenge every 1–2 hours during weeks 1–6; then one 2-mg lozenge every 2–4 hours during weeks 7–9; and one 2-mg lozenge every 4–8 hours during weeks 10–12.

Patients who smoke first cigarette ≤30 minutes after waking: One 4-mg lozenge every 1–2 hours during weeks 1–6; then one 4-mg lozenge every 2–4 hours during weeks 7–9; and one 4-mg lozenge every 4–8 hours during weeks 10–12.

Do not exceed 5 lozenges in 6 hours or 20 lozenges daily.

Discontinue therapy if mouth problems, persistent indigestion, severe sore throat, irregular heartbeat, palpitations, or symptoms suggestive of overdosage (nausea, vomiting, dizziness, diarrhea, weakness, and rapid heartbeat) develop.

Transdermal

Patients who smoke ≤10 cigarettes daily: Initially, 14 mg daily for 6 weeks, then 7 mg daily for 2 weeks, then discontinue.

Patients who smoke >10 cigarettes daily: Initially, 21 mg daily for 4–6 weeks; then 14 mg daily for 2 weeks; then 7 mg daily for 2 weeks; then discontinue therapy.

Intranasal

Initially, 1–2 sprays (0.5–1 mg) in each nostril per hour (1–2 mg per hour total); may increase up to a maximum of 5 sprays (5 mg) in each nostril per hour (10 mg total) or a maximum total of 80 sprays (40 mg) daily.

Initially, use at least 16 sprays (8 mg total) daily to increase chance of efficacy. Then, individualize dosage based on nicotine dependence and occurrence of symptoms of nicotine excess.

Continue treatment in successfully abstinent patients for up to 8 weeks then discontinue over 4–6 weeks.

Taper dosage by using only 1 spray at a time, using the spray less frequently, keeping a tally of daily usage, trying to meet a steadily reducing usage target, skipping a dose by not medicating every hour, or setting a planned “quit date” for stopping use of the spray. Some patients may not require tapering.

Oral Inhalation

Initially, 6–16 cartridges daily for up to 12 weeks, then gradually decrease daily dosage over 6–12 weeks.

Use ≥6 cartridges daily for the first 3–6 weeks to increase chance of efficacy. Individualize dosage based on nicotine dependence and occurrence of symptoms of nicotine excess.

Taper dosage by using less frequently, keeping a tally of daily usage, trying to meet a steadily reducing usage target, or setting a planned “quit date” for stopping use of the inhaler. Some patients may not require tapering.

Prescribing Limits

Adults

Smoking Cessation
Buccal (Chewing Gum)

Maximum 2 pieces of 2-mg gum per hour (i.e., maximum 24 pieces [48 mg nicotine] daily). Maximum 12 weeks of therapy.

Maximum 2 pieces of 4-mg gum per hour (i.e., maximum 24 pieces [96 mg nicotine] daily). Maximum 12 weeks of therapy.

Clinician supervised: Maximum 30 pieces of 2-mg gum daily (i.e., 60 mg nicotine) or 24 pieces of 4-mg gum daily (i.e., 96 mg nicotine).

Buccal (Lozenges)

Maximum 5 lozenges in 6 hours or 20 lozenges daily. Maximum 12 weeks of therapy.

Transdermal

Patients who smoke ≤10 cigarettes daily: Maximum 8 weeks of therapy.

Patients who smoke >10 cigarettes daily: Maximum 10 weeks of therapy.

Continued therapy for periods longer than usually recommended may be appropriate for certain patients to promote extended abstinence. Continuation of therapy >12 weeks not recommended by manufacturer.

Intranasal

Maximum 5 sprays (5 mg) in each nostril per hour (maximum 10 mg total) or a maximum total of 80 sprays (40 mg) daily.

Manufacturer states that continuing therapy >12 weeks does not improve outcome. Safety of continuing therapy >6 months not established.

Oral Inhalation

Maximum 16 cartridges daily for up to 12 weeks.

Manufacturer states that safety of continuing therapy >6 months not established.

Special Populations

No special population dosage recommendations at this time.

Cautions for Nicotine

Contraindications

  • Known hypersensitivity to nicotine, menthol (oral inhaler), or any ingredient in the formulation.

  • Nicotine polacrilex gum in patients with temporomandibular joint disease. (See Oral and Dental Effects under Cautions.)

Warnings/Precautions

Warnings

Nicotine Toxicity

Risk of nicotine toxicity (e.g., nausea, hypersalivation, abdominal pain, vomiting, diarrhea, perspiration, headache, dizziness, hearing and visual disturbances, mental confusion, weakness) and addiction. Sustained use of nicotine preparations is not recommended. Weigh risk of nicotine replacement against hazard of continued smoking concurrent with nicotine replacement therapy and likelihood of smoking cessation without nicotine replacement.

Discontinue nicotine polacrilex lozenges if symptoms suggestive of overdosage (nausea, vomiting, dizziness, diarrhea, weakness, and rapid heartbeat) occur.

Fetal/Neonatal Morbidity

Animal studies indicate fetal harm; pregnant women should attempt smoking cessation with educational and behavioral interventions before considering nicotine therapy.

Use during pregnancy only if the increased likelihood of smoking cessation justifies potential risk to the fetus and patient of nicotine replacement and possible continued smoking. If used during pregnancy or if patient becomes pregnant, apprise of potential fetal hazard.

General Precautions

Respiratory Effects

Possible exacerbation of bronchospasm. Use oral inhaler with caution in patients with bronchospastic disease; other dosage forms may be preferable.

Intranasal nicotine is not recommended in patients with severe reactive airway disease.

Nasopharyngeal Effects

Nicotine nasal spray may irritate nasal mucosa; use of nasal spray not recommended in patients with a history of chronic nasal disorders (e.g., allergy, rhinitis, polyps, sinusitis).

Discontinue nicotine polacrilex lozenges if severe sore throat occurs.

Cardiovascular Effects

Possible increased risk of adverse cardiovascular effects; however, causal relationship between nicotine replacement therapy and cardiac complications not established.

Discontinue therapy if irregular heartbeat or palpitations occur.

Use with caution and only after careful evaluation in patients with coronary heart disease (i.e., history of MI, angina pectoris), serious cardiac arrhythmias, or vasospastic diseases (e.g., Buerger's disease, Prinzmetal's variant angina, Raynaud's phenomena). Benefit of nicotine replacement therapy must outweigh risks of continued cigarette smoking.

Self-medication not recommended in patients in the immediate post-MI period, with serious arrhythmias, or with severe or worsening angina.

Endocrine Effects

Possible hyperinsulinemia and insulin resistance with prolonged nicotine replacement therapy. Use with caution in hyperthyroidism, pheochromocytoma, or insulin-dependent diabetes.

GI Effects

Possible delayed healing of peptic ulcer disease; use with caution.

Discontinue nicotine polacrilex lozenges if persistent indigestion develops.

Use nicotine polacrilex gum with caution in patients with a history of esophagitis.

Hypertension

Possible increased risk of malignant hypertension in patients with accelerated hypertension; use with caution in such patients.

Possible perpetuation of hypertension; use with caution in patients with systemic hypertension.

Nicotine Dependence

Transference of dependence on nicotine may occur; potential for abuse and dependence on nicotine nasal spray appears to be greater than that for other formulations of nicotine (i.e., nicotine polacrilex gum, transdermal nicotine systems) but less than that of cigarettes.

To minimize withdrawal symptoms and the risk of dependence on nicotine, withdraw gradually or discontinue use of nicotine polacrilex gum or transdermal or intranasal nicotine after 2–3 months of therapy.

Concern exists regarding possible risk of nicotine dependence transference from use of electronic nicotine delivery systems (ENDS) such as e-cigarettes and vape pens in individuals, particularly adolescents, not previously dependent on nicotine but who subsequently transition to actual cigarette use.

Phenylketonuria

Commit nicotine polacrilex lozenges contain aspartame (NutraSweet), which is metabolized in the GI tract to provide 3.4 mg of phenylalanine per lozenge.

Oral and Dental Effects

Risk of occlusal stress when nicotine polacrilex gum is chewed for long periods of time; may result in displaced dental restorations or loosening of dental inlays or fillings. Gum may stick to dentures, dental caps, or partial bridges; if excessive sticking or damage to dental work occurs, discontinue gum and consult clinician.

Use nicotine polacrilex gum with caution in patients with a history of oral or pharyngeal inflammation, or dental conditions exacerbated by chewing gum.

Discontinue nicotine polacrilex lozenges if mouth problems develop.

Dermatologic Effects

Possible skin reactions (e.g., urticaria, hives, rash) with transdermal systems. Increased risk of such reactions in patients with some dermatologic conditions (e.g., psoriasis, atopic or eczematous dermatitis).

If skin reaction occurs, discontinue transdermal system and contact clinician; topical corticosteroids and/or oral antihistamines recommended.

Risk of contact sensitization with transdermal systems; serious reaction may occur with re-exposure to smoking or other nicotine products.

Nervous System Effects

Potential adverse nervous system effects (e.g., insomnia, headache, dizziness, lightheadedness).

Specific Populations

Pregnancy

Category D. (See Fetal/Neonatal Morbidity under Cautions.)

Lactation

Distributed into milk. Use caution.

Weigh risk of exposure to nicotine in drug versus risk of nicotine and other components of tobacco smoke from cigarettes.

Pediatric Use

Safety and efficacy not established.

Use or ingestion of used or unused nicotine replacement systems by children may cause poisoning or be fatal; keep used and unused containers out of reach of children.

Risk of choking if nicotine oral inhalers are swallowed; keep out of reach of children.

Geriatric Use

Insufficient experience in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults; select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and potential for concomitant disease.

Hepatic Impairment

Not studied in patients with hepatic impairment; use with caution.

Renal Impairment

Not studied in patients with renal impairment; clearance may be decreased in patients with severe renal impairment.

Common Adverse Effects

Buccal therapy (gum): Indigestion; nausea; hiccups; traumatic injury to oral mucosa and/or teeth; irritation and/or tingling of the tongue, mouth, and throat; oral mucosal ulceration; jaw-muscle ache; eructation; gum sticking to teeth; unpleasant taste; dizziness; lightheadedness; headache; insomnia.

Buccal therapy (lozenges): Nausea, dyspepsia, flatulence, headache, upper respiratory tract infections.

Transdermal therapy: Application site reactions (i.e., pruritus, burning, or erythema), diarrhea, dyspepsia, abdominal pain, dry mouth.

Intranasal therapy: Runny nose, throat irritation, watery eyes, sneezing, cough.

Oral inhalation therapy: Dyspepsia, oropharyngeal irritation (e.g., coughing, mouth and throat irritation), rhinitis, headache.

Interactions for Nicotine

Cigarette smoke and nicotine induce hepatic enzymes.

Smoking Cessation

Cessation of smoking may alter the response to concomitant administration of various drugs in patients who previously smoked.

Potential pharmacokinetic interaction (decreased metabolism and increased blood concentrations of certain drugs) with cessation of smoking.

Consider the effect of smoking cessation in patients receiving nicotine replacement therapy when patient is receiving other drugs concomitantly.

Sympathomimetic and Sympatholytic Drugs

Potential pharmacodynamic interaction (increased circulating plasma concentrations of cortisol and catecholamines); may require dosage adjustment of sympathomimetic (adrenergic) or sympatholytic (adrenergic blocking) drugs.

Possible altered absorption of transdermal nicotine from drugs producing cutaneous vasoconstriction (e.g., sympathomimetic agents) or vasodilation (e.g., antihypertensive agents).

Foods Affecting Salivary Acidity

Transient decrease of salivary pH may inhibit buccal absorption of nicotine from gum, lozenge, or oral inhaler.

Specific Drugs and Foods

Drug or Food

Interaction

Comments

Acetaminophen

Smoking cessation may decrease metabolism and increase blood concentrations of acetaminophen

Decrease dosage of acetaminophen as required

Acidic beverages (e.g., coffee, juices, carbonated soft drinks)

May inhibit buccal absorption of nicotine from gum, lozenge, or orally inhaled drug

Do not eat or drink for 15 minutes before and during gum or lozenge therapy

Adrenergic agonists (e.g., isoproterenol, phenylephrine)

Smoking cessation may decrease circulating plasma concentrations of catecholamines

Increase dosage of adrenergic agonists as required

Adrenergic antagonists (e.g., prazosin, labetalol)

Smoking cessation may decrease circulating plasma concentrations of catecholamines

Decrease dosage of adrenergic antagonists as required

β-Adrenergic blocking agents (e.g., propranolol)

Smoking cessation may decrease metabolism and increase blood concentrations of β-adrenergic blocking agents

Smoking cessation may restore the decreased cardiac output and hypotensive effect induced by propranolol

Decrease dosage of β-adrenergic blocking agent as required

Bupropion

Possible increased risk of hypertension

May be used concomitantly with transdermal nicotine therapy

Caffeine

Smoking cessation may decrease metabolism and increase blood concentrations of caffeine

Decrease dosage of caffeine as required

Furosemide

Smoking cessation may increase diuretic effects of furosemide

Glutethimide

Smoking cessation may decrease absorption of glutethimide

Insulin

Smoking cessation increases absorption of subcutaneous insulin

Monitor blood glucose closely; adjust insulin dosage as needed

Nasal vasoconstrictors (e.g., xylometazoline)

Delays time to peak plasma concentration of nicotine nasal spray

Oxazepam

Smoking cessation may decrease metabolism and increase blood concentrations of oxazepam

Decrease dosage of oxazepam as required

Pentazocine

Smoking cessation may decrease metabolism and increase blood concentrations of pentazocine

Decrease dosage of pentazocine as required

Propoxyphene

Smoking cessation may decrease metabolism of propoxyphene

Decrease dosage of propoxyphene as required

Theophylline

Smoking cessation may decrease metabolism and increase blood concentrations of theophylline

Monitor plasma concentrations and adjust dosage of theophylline as required

Tricyclic antidepressants (e.g., imipramine)

Smoking cessation may decrease metabolism and increase blood concentrations of tricyclic antidepressants

Adjust dosage of tricyclic antidepressant as required

Nicotine Pharmacokinetics

Absorption

Bioavailability

Readily absorbed transmucosally following intrabuccal administration via chewing gum or sucking a lozenge, and following oral inhalation and intranasal administration; absorbed minimally from the GI tract.

Readily absorbed percutaneously following topical application of a transdermal system.

Gum: Averages 53–55%, with peak concentrations achieved within 25–30 minutes.

Lozenge: Approximately 25–27% more of an equivalent dose absorbed with lozenge than with gum.

Transdermal: Approximately 68–98%, with peak concentrations achieved within 2–10 hours.

Intranasal: Approximately 53%, with peak concentrations achieved within 4–15 minutes.

Oral inhalation: Approximately 60%, mostly absorbed in the mouth, with peak concentrations achieved within 15–30 minutes.

Food

Acidic beverages may interfere with buccal absorption. (See Specific Drugs and Foods under Interactions.)

Plasma Concentrations

Gum: Relatively constant blood nicotine concentrations attained following repeated administration are similar to those produced by smoking cigarettes.

Transdermal: Plasma nicotine concentrations generally lower and fluctuate less than those produced by smoking cigarettes.

Intranasal: Plasma nicotine concentrations similar to those produced by smoking cigarettes.

Oral inhalation: Lower plasma nicotine concentrations compared with nasal spray.

Special Populations

Common cold or rhinitis may decrease extent of absorption and peak plasma concentrations of intranasal nicotine.

Obesity decreases peak plasma concentration and AUC of transdermal systems.

Distribution

Extent

Following IV administration in animals, rapidly distributes into most body tissues and fluids with highest concentrations in the cerebral cortex and adrenal medulla, and lower concentrations in spleen, adrenal cortex, kidney, and pancreas.

Nicotine crosses the placenta and is distributed into milk.

Plasma Protein Binding

<5%.

Elimination

Metabolism

Rapidly and extensively metabolized, principally in the liver, to >20 primarily inactive metabolites.

Elimination Route

Excreted in urine mainly as metabolites (70–90%) and as unchanged drug (10–30%).

Half-life

Biphasic; terminal half-life averages 2 hours (range: 1–4 hours).

Following removal of a transdermal system, apparent half-life averages 3–6 hours.

Special Populations

Hepatic impairment may reduce clearance.

Severe renal failure may reduce clearance.

Stability

Storage

Oral

Gum

<30°C; protect from light.

Lozenge

20–25°C; protect from light.

Transdermal

20–25°C in unopened, protective pouch.

Intranasal

Solution

<30°C.

Oral Inhalation

<30°C; protect cartridges from light.

Actions

  • A ganglionic (nicotinic) cholinergic-receptor agonist; exhibits stereospecific binding to receptors in autonomic ganglia, the adrenal medulla, the neuromuscular junction, and the brain.

  • Exhibits both stimulant (e.g., marked CNS and respiratory stimulation) and depressant effects in the CNS and peripheral nervous system.

  • Behavior-reinforcing properties of nicotine result from dose-related effects on the CNS.

  • Low doses produce stimulant effects (e.g., increased alertness and cognitive performance) in the cerebral cortex by stimulating autonomic ganglia and facilitating neurotransmission.

  • High doses produce reward effects mediated through the mesolimbic dopaminergic system, with initial ganglionic stimulation, which is quickly followed by inhibition of neurotransmission.

  • Activates neurohormonal pathways, releasing acetylcholine, norepinephrine, dopamine, serotonin, vasopressin, beta-endorphin, growth hormone, and ACTH.

  • Cardiovascular effects mediated principally via stimulation of sympathetic ganglia and the adrenal medulla and via release of catecholamines from neuronal tissue. Low doses produce peripheral vasoconstriction and increase heart rate, myocardial contractile force, cardiac output, stroke volume, velocity of myocardial contraction, and BP, resulting in an increase in cardiac work and oxygen consumption; however, large doses may cause hypotension.

  • GI effects mediated principally via cholinergic stimulation; results in increased tone and motor activity of GI smooth muscle. Systemic absorption may cause nausea, vomiting, and diarrhea.

  • Chronic use may result in psychologic and physical dependence; tolerance to some of the pharmacologic effects may occur.

Advice to Patients

  • Importance of not smoking or using other tobacco products during nicotine replacement therapy.

  • Advise patient of improved smoking cessation success with a comprehensive treatment approach (e.g., support groups, counseling, or specific behavior change techniques).

  • Importance of providing patient a copy of the manufacturer's patient information. When used for self-medication, importance of reading patient instructions provided by the manufacturer.

  • Importance of patient understanding the proper use (see Administration under Dosage and Administration) and disposal of nicotine preparations.

  • Importance of avoiding unnecessary contact with transdermal systems. Advise patients to discard transdermal system carefully; fold so adhesive side sticks to itself, place in empty protective pouch, and dispose of immediately. Importance of washing hands with water alone; importance of not touching eyes prior to handwashing.

  • Importance of keeping used and unused transdermal systems, intranasal containers, oral inhaler cartridges, gum, and lozenges out of the reach of children and pets. Importance of contacting clinician or poison control immediately if a child or pet chews or swallows a nicotine product.

  • Importance of calling clinician or poison control center if symptoms of nicotine overdose occur (e.g., bad headaches, dizziness, upset stomach, drooling, vomiting, diarrhea, cold sweat, blurred vision, hearing difficulties, mental confusion, weakness, fainting).

  • Advise patients of symptoms of nicotine withdrawal (e.g., craving, nervousness, restlessness, irritability, mood lability, anxiety, drowsiness, sleep disturbances, impaired concentration, increased appetite, minor somatic complaints [headache, myalgia, constipation, fatigue], weight gain).

  • For transdermal therapy, importance of consulting clinician before initiating therapy if patient has a dermatologic condition or is allergic to adhesive tape. (See Dermatologic Effects under Cautions.) Importance of discontinuing use and contacting clinician if severe or persistent skin reaction occurs at transdermal site (e.g., severe erythema, pruritus, edema).

  • Advise patients receiving nicotine polacrilex gum that chewing gum too rapidly may result in lightheadedness, nausea, vomiting, irritation of throat and mouth, hiccups, and indigestion.

  • Advise patients receiving intranasal therapy of likelihood of nasal irritation; may become less bothersome with continued use.

  • Advise patients receiving nicotine for oral inhalation of likelihood of mild irritation of the mouth or throat and cough; may become tolerant of these effects.

  • Importance of patients taking lozenges to stop use and contact clinician if mouth problems, persistent indigestion, severe sore throat, irregular heartbeat or palpitations occur. Patients receiving nicotine polacrilex gum should stop use and contact clinician if mouth, teeth, or jaw problems, or irregular heartbeat or palpitations occur.

  • Importance of informing patients with phenylketonuria that Commit nicotine polacrilex lozenges contain aspartame.

  • Importance of consulting clinician if patient feels the need for continued nicotine replacement therapy at the end of regimen.

  • Risk of dependence to nicotine in oral inhaler and nasal spray; importance of using inhaler and nasal spray only as long as directed by clinician.

  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.

  • Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as any concomitant illnesses (e.g., chronic nasal problems, heart problems, high blood pressure, stomach ulcers, wheezing or asthma, overactive thyroid, diabetes requiring insulin, kidney or liver disease).

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Nicotine

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Nasal

Solution

0.5 mg/metered spray

Nicotrol NS

Pfizer

Oral Inhalation

Inhalant

4 mg/metered spray

Nicotrol Inhaler

Pfizer

Topical

Transdermal System

7 mg/24 hours*

NicoDerm CQ Step 3

GlaxoSmithKline

Nicotine Transdermal System

14 mg/24 hours*

NicoDerm CQ Step 2

GlaxoSmithKline

Nicotine Transdermal System

21 mg/24 hours*

NicoDerm CQ Step 1

GlaxoSmithKline

Nicotine Transdermal System

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Nicotine Polacrilex

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Buccal (Transmucosal)

Lozenges

2 mg (of nicotine)*

Commit

GlaxoSmithKline

Nicotine Polacrilex Lozenge

4 mg (of nicotine)*

Commit

GlaxoSmithKline

Nicotine Polacrilex Lozenge

Pieces, chewing gum

2 mg (of nicotine)*

Nicorette

GlaxoSmithKline

Nicotine Polacrilex Gum

4 mg (of nicotine)*

Nicorette DS

GlaxoSmithKline

Nicotine Polacrilex Gum

AHFS DI Essentials™. © Copyright 2021, Selected Revisions June 10, 2019. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

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