Nicotine

Nicotine is used in the treatment of:

• Colitis, Ulcerative
• Tobacco Use Disorder

Nicotine is used in the prevention of:

• Substance Withdrawal Syndrome

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Smoking Cessation

Used for nicotine replacement therapy as a temporary adjunct in the cessation of cigarette smoking either unsupervised (self-medication)188 189 190 246 257 or in conjunction with a behavior modification program under clinician supervision.1 2 5 6 7 8 9 10 11 29 30 31 96 97 191 192 193 194 195 196 244 245 257 258 263

Nicotine replacement therapy considered one of several first-line therapies by USPHS for treatment of tobacco dependence.257 For additional information, consult the most current USPHS clinical practice guideline available at

Provides alternative sources of nicotine that help reduce the withdrawal symptoms associated with nicotine dependence.1 2 50 78 79 80 97 101 102 103 104 Chewing the resin complex-containing gum may act as a substitute oral activity in behavior modification.5

Ulcerative Colitis

Transdermal nicotine has been used in the management of ulcerative colitis†.125 204 205 206 207 208 209 210

General

• To increase smoking cessation rate,101 144 194 195 196 use as part of a comprehensive program of multiple treatment strategies, including behavioral modification.43 44 101 102 103 104 115 116 119 126 131 144 148 149 167 193 194 195 196 258 a

• Individualize duration of therapy based on patient response and degree of nicotine dependence.1 190 257 263 264 a

• Stop smoking prior to initiating nicotine replacement therapy;1 190 263 264 self-medication not recommended in patients who continue to smoke, chew tobacco, or use snuff or other nicotine-containing preparations.188 189 190

• Discontinue therapy in patients who continue to smoke 4 weeks after initiating treatment;101 102 103 104 may use nicotine replacement therapy again in subsequent attempts to quit smoking.101 102 103 104 121

Administration

Administer nicotine percutaneously by topical application of a transdermal system.b i

Administer nicotine transmucosally by oral inhalation using a special nicotine oral inhaler or intranasally using a metered-dose spray pump. d 265 g

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

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).257

Buccal Administration

Self-administer one piece of gum in response to the urge to smoke.1

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);1 stop chewing gum and park between cheek and gum; once tingling is almost gone (about 1 minute), repeat chewing procedure.1 Continue for about 30 minutes or until taste dissipates.1 Do not swallow gum.1

Do not eat or drink anything other than water for 15 minutes before and during chewing of gum.1 190

Do not chew multiple pieces of gum simultaneously; do not chew too rapidly or chew pieces in succession.1 May cause excessive release of nicotine and result in adverse effects (e.g., lightheadedness, nausea, vomiting, irritation of the throat and mouth, hiccups, indigestion).1

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

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,1 unless otherwise instructed by clinician.9 43 65

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

Suck on lozenge until dissolved; do not swallow, bite, or chew.260 263 264 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.263 264 A warm or tingling sensation may be perceived.h

Do not eat or drink anything other than water for 15 minutes before and during sucking on the lozenge.257 263 264

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

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

Self-administer lozenge in response to nicotine craving; decrease frequency of administration over time.263 264

Topical Administration

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

Apply at the same time each day, usually after awakening.101 102 103 104 129 167 188 189

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.101 102 103 104 129

Apply transdermal system to a clean, dry, hairless area of intact skin43 101 129 on the trunk or upper outer arm101 102 103 104 129 167 188 189 by firmly pressing the system with the adhesive side touching the skin.101 129 167 Press system firmly in place with heel of hand for about 10 seconds, ensuring good contact, particularly around the edges.101 129 167 a Do not apply to sites that are oily, damaged, or irritated;43 101 129 if necessary, hair may be clipped, but do not shave area.167

System may be worn for 16 or 24 hours.b i If cravings begin upon awakening, wear patch for 24 hours.189 b If vivid dreams or sleep disruptions occur, wear patch for 16 hours; remove at bedtime and apply new patch upon awakening.189 257 b i

If system inadvertently comes off during the period of use, apply a new system; 101 102 103 104 167 a continue current application schedule or change so that the next system is applied 24 hours later.129

Rotate application sites to minimize potential skin irritation; allow ≥1 week before reusing a given site.101 102 103 129 (See Dermatologic Effects under Cautions.)

Avoid unnecessary contact with transdermal systems.101 102 103 104 Avoid touching eyes after handling; wash hands with water alone as soap may enhance percutaneous absorption.101 102 103 104 167

Intranasal Administration

Administer intranasally using a metered-dose spray pump.191

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

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

Clear nasal passages prior to administration.d

Tilt the head back slightly;191 d insert tip of bottle into one nostril as far as is comfortable.d Breathe through the mouth and spray once into nostril; do not sniff, swallow or inhale through the nose while administering.191 Repeat this procedure for the other nostril.d

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

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

Oral Inhalation

Administer transmucosally as an inhaled vapor by oral inhalation using a special nicotine oral inhaler that mimics smoking cigarettes.244 245 246 247 248

Hold the oral inhaler with two hands; separate the top and bottom pieces by pushing and turning the pieces until markings line up.g Insert one nicotine cartridge and push the cartridge until it pops into place.g 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.g

Place the mouthpiece of the inhaler between lips and puff on the inhaler using rapid shallow sucking (“buccal mode”);244 248 alternatively, inhale slowly and deeply into back of throat (“pulmonary mode”).248 g Nicotine is vaporized and absorbed in mouth and throat.g (See Absorption under Pharmacokinetics.) Shallow puffing method generally is preferred.244 248 250 Deep inhalation technique requires considerable effort and does not result in substantially increased drug delivery or other benefits.248

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.244

Nicotine is used up from cartridge after about four 5-minute sessions or one 20-minute session of active puffing.250

When cartridge is empty, remove top of mouthpiece; discard empty cartridge away from children and pets.g Store with mouthpiece in locked position and cartridges in plastic case.g Clean reusable mouthpiece regularly with soap and water.244

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

Dosage

Chewing gum and lozenge available as nicotine polacrilex; dosage expressed in terms of nicotine.1 264

Nicotine oral inhaler cartridges labeled as containing 10 mg of nicotine deliver ≤4 mg total with repeated inhalation.244 247 250 The amount of nicotine released depends on the volume and temperature of the air passing through the inhaler.244 245 246 247 248 An intensive inhalation regimen (80 deep inhalations over 20 minutes) releases approximately 4 mg of nicotine.265

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.191

Adults

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.c Alternatively, chew a 2-mg piece of gum whenever the urge to smoke occurs; do not exceed 2 pieces (4 mg) per hour.1

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.c Alternatively, chew a 4-mg piece whenever the urge to smoke occurs; do not exceed 2 pieces (8 mg) per hour.1

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.c

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 once 2-mg lozenge every 4–8 hours during weeks 10–12.263 264 h

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 10–12.263 264 h

Do not exceed 5 lozenges in 6 hours or 20 lozenges daily.263 264

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) develops.264

Patients who smoke ≤10 cigarettes daily: Initially, 14 mg daily for 6 weeks, then 7 mg daily for 2 weeks, then discontinue.189 b i

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.189 b i

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.191 e

Initially, use at least 16 sprays (8 mg total) daily to increase chance of efficacy.191 Then, individualize dosage based on nicotine dependence and occurrence of symptoms of nicotine excess.191

Continue treatment in successfully abstinent patients for up to 8 weeks then discontinue over 4–6 weeks.191

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.191 Some patients may not require tapering.191

Initially, 6–16 cartridges daily for up to 12 weeks, then gradually decrease daily dosage over 6–12 weeks.244 245 246

Use ≥6 cartridges daily for the first 3–6 weeks to increase chance of efficacy.244 Individualize dosage based on nicotine dependence and occurrence of symptoms of nicotine excess.244

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.265 Some patients may not require tapering.265

Prescribing Limits

Adults

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

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

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).1 190 195

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

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

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

Continued therapy for periods longer than usually recommended may be appropriate for certain patients to promote extended abstinence.257 Continuation of therapy >12 weeks not recommended by manufacturer.101 102 103 104

Maximum 5 sprays (5 mg) in each nostril per hour (maximum 10 mg total) or a maximum total of 80 sprays (40 mg) daily.191 257 e

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

Maximum 16 cartridges daily for up to 12 weeks.265

Manufacturer states that safety of continuing therapy >6 months not established.265

Special Populations

No special population dosage recommendations at this time.a b

Storage

Oral

<30°C; protect from light.1

20–25°C; protect from light.264

Transdermal

20–25°C in unopened, protective pouch.b

Intranasal

<30°C.191

Oral Inhalation

<30°C; protect cartridges from light.244 250

• Nicoderm CQ [OTC]
• Nicorelief [OTC]
• Nicorette Mini [OTC]
• Nicorette Starter Kit [OTC]
• Nicorette [OTC]
• Nicotine Step 1 [OTC]
• Nicotine Step 2 [OTC]
• Nicotine Step 3 [OTC]
• Nicotrol
• Nicotrol NS
• Thrive [OTC]

Hypersensitivity to nicotine or any component of the formulation.

OTC labeling: Nicorette lozenge: When used for self-medication, do not use if you are allergic to soya.

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); because total system clearance of nicotine is dependent on hepatic blood flow, anticipate reduced clearance.

Some products may contain phenylalanine and/or sodium.

Signs and symptoms of nicotine toxicity (eg, severe headache, dizziness, mental confusion, disturbed hearing and vision, abdominal pain; rapid, weak and irregular pulse; salivation, nausea, vomiting, diarrhea, cold sweat, weakness)

Nicotine crosses the placenta (HHS 2014). Maternal smoking is associated with birth defects (HHS 2014; Hachshaw 2011); the incidence of birth defects following nicotine replacement therapy may be similar (limited data) (Dhalwani 2015). Nicotine exposure via cigarette smoke may cause increased ectopic pregnancy, low birth weight, increased risk of spontaneous abortion, increased perinatal mortality; increased aortic blood flow, increased heart rate, decreased uterine blood flow, and decreased breathing have been reported in the fetus. Smoking during pregnancy is associated with sudden infant death syndrome (SIDS), an increased risk of asthma, infantile colic, and childhood obesity (ACOG 2010; HHS 2014). Women who are pregnant should be encouraged not to smoke. The use of nicotine replacement products to aid in smoking cessation has not been adequately studied in pregnant women (amount of nicotine exposure is varied). Nonpharmacologic treatments are recommended. If the benefits of nicotine replacement therapy outweigh the unknown risks, it should be done under close supervision (ACOG 2010).