Nicotine (Polacrilex) (nicotine polacrilex)
Smoking Deterrents - Nicotinic or Bupropion (NDRI)-Type Buccal Mini Lozenge
Last reviewed · Source: First Databank (FDB) drug data
Overview
Nicotine, a naturally occurring autonomic drug, is a ganglionic (nicotinic) cholinergic-receptor agonist.
Nicotine, a tertiary amine derived from the tobacco plant, is a ganglionic (nicotinic) cholinergic-receptor agonist. The pharmacologic actions of nicotine are complex and include a variety of effects mediated by stereospecific binding to nicotinic-cholinergic receptors in autonomic ganglia, the adrenal medulla, the neuromuscular junction, and the brain. The effects of the drug are generally dose related; large doses can produce toxic symptoms.
Chronic use of nicotine may result in psychologic and physical dependence, and tolerance to some of the pharmacologic effects may occur. As adjuncts in the cessation of cigarette smoking, nicotine replacement products provide alternative sources of nicotine that help reduce the withdrawal symptoms associated with nicotine dependence. Some evidence suggests that the behavior-reinforcing properties of nicotine may be the result of stimulant effects (e.g., increased alertness and cognitive performance) in the cerebral cortex and ''reward'' effects mediated through the mesolimbic dopaminergic system.
The stimulant effects of nicotine reportedly predominate at low doses, while high doses provide reward effects.
The cardiovascular effects of nicotine generally are dose dependent and are mediated principally via stimulation of sympathetic ganglia and the adrenal medulla and via release of catecholamines from neuronal tissue (e.g., sympathetic neurons, chromaffin cells). At low doses similar to those associated with cigarette smoking, the cardiovascular effects of nicotine appear to be mediated principally by the CNS, through activation of chemoreceptor afferent pathways or by direct effects on the brain stem. At higher doses, the drug may act directly on the peripheral nervous system, producing ganglionic stimulation and adrenal catecholamine release.
Relatively small doses of nicotine produce peripheral vasoconstriction and increase heart rate, myocardial contractile force, cardiac output, stroke volume, velocity of myocardial contraction, and blood pressure, resulting in an increase in cardiac work and oxygen consumption; however, large doses of the drug may cause hypotension. The effects of nicotine on the GI tract are mediated principally via cholinergic stimulation. Chronic use of nicotine may result in psychologic and physical dependence, and tolerance to some of the pharmacologic effects may occur.
Nicotine is readily absorbed transmucosally following intrabuccal administration via gum or lozenge and following intranasal administration; the drug is absorbed minimally from the GI tract. Nicotine is readily absorbed percutaneously following topical application of a transdermal system.
Bioavailability of the gum is approximately 53-55%, with peak concentrations achieved within 25-30 minutes. Relatively constant blood nicotine concentrations attained following repeated administration of the gum preparation are similar to those produced by smoking cigarettes. Bioavailability of the lozenge is approximately 25-27% more than with the gum at an equivalent dose.
Acidic beverages may interfere with buccal absorption. Bioavailability of the transdermal system is approximately 68-98%, with peak concentrations achieved within 2-10 hours. Plasma nicotine concentrations are generally lower and fluctuate less with transdermal nicotine systems than those produced by smoking cigarettes.
Bioavailability of the nasal spray is approximately 53%, with peak concentrations achieved within 4-15 minutes. Plasma nicotine concentrations produced by the nasal spray are similar to those produced by smoking cigarettes. The 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. Following IV administration in animals, nicotine rapidly distributes into most body tissues and fluids with highest concentrations in the cerebral cortex and adrenal medulla, and lower concentrations in the spleen, adrenal cortex, kidney, and pancreas. Plasma protein binding of nicotine is less than 5%.
Nicotine is rapidly and extensively metabolized, principally in the liver, to more than 20 primarily inactive metabolites, and excreted in urine mainly as metabolites (70-90%) and as unchanged drug (10-30%). The half-life is biphasic with a terminal half-life averaging 2 hours (range: 1-4 hours). Following removal of a transdermal system, apparent half-life averages 3-6 hours.
USES: This medication can help you quit smoking by replacing the nicotine in cigarettes. The nicotine in tobacco is an important part of cigarette addiction. When you stop smoking, your nicotine levels drop quickly.
This drop can cause withdrawal symptoms such as craving tobacco, nervousness, irritability, headache, weight gain, and difficulty concentrating. Stopping smoking is hard and your chance of success is best when you are ready and have made a commitment to quit. Nicotine replacement products are part of a total stop-smoking program that includes behavior change, counseling, and support.
Smoking causes lung disease, cancer, and heart disease. Stopping smoking is one of the most important things you can do to improve your health and live longer.
Generic name: nicotine polacrilex
Pronunciation: (NICK-oh-teen)
Drug class: Smoking Deterrents - Nicotinic or Bupropion (NDRI)-Type
Therapeutic class: Chemical Dependency, Agents to Treat
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Nicotine (Polacrilex)
Indications
The following indications are listed for Nicotine (Polacrilex):
- Smoking Cessation
Also known as: Smoking Cessation Assistance.
Dosing
The manufacturers recommend that nicotine replacement therapy (NRT) be initiated on a planned quit date for cigarette smoking. However, there is some evidence supporting the efficacy of initiating NRT in people who continue to smoke and do not plan to quit immediately. It is important to complete the full treatment regimen to increase the likelihood of successful smoking cessation.
Nicotine gum and lozenges are available as nicotine polacrilex; dosage is expressed in terms of nicotine.
Administer nicotine replacement products buccally (using a lozenge or chewing gum), transdermally (using a patch), or intranasally (using a metered-dose spray pump).
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Cigarette smoke and nicotine induce hepatic enzymes. Therefore, the effect of smoking cessation in patients receiving nicotine replacement therapy should be considered when the patient is receiving other drugs concomitantly.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity or allergy to nicotine or any component in the formulation.
- Temporomandibular joint disorder
- 30 day risk period post-myocardial infarction
- Acute myocardial infarction
- Angina
- Buerger's disease
- Life-threatening cardiac arrhythmias
- Raynaud's phenomenon
- Severe uncontrolled hypertension
- Unstable angina pectoris
- Disease of liver
- Esophagitis
- Hyperthyroidism
- Peptic ulcer
- Pharyngitis
- Pheochromocytoma
- Prinzmetal angina
- Type 1 diabetes mellitus
Adverse reactions
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.
Buccal therapy (lozenges): Nausea, dyspepsia, flatulence, headache, upper respiratory tract infections.
Transdermal therapy: Application site reactions (i.e., pruritus, burning, or erythema), dyspepsia, abdominal pain, dry mouth.
Intranasal therapy: Nasal irritation, runny nose, throat irritation, watery eyes, sneezing, cough.
Less Frequent
- Hypertension
Rare or Very Rare
- Angioedema
- Cardiac arrhythmia
- Erythema
- Hypersensitivity drug reaction
- Pruritus of skin
- Skin rash
- Tachycardia
- Urticaria
More Frequent
- Headache disorder
- Increased appetite
Rare or Very Rare
- Abdominal pain with cramps
- Anorexia
- Arthralgia
- Constipation
- Cough
- Diarrhea
- Dizziness
- Drowsy
- Dysgeusia
- Dysmenorrhea
- Flatulence
- Gastric acid hypersecretory conditions
- Heartburn
- Hiccups
- Hyperhidrosis
- Insomnia
- Irritability
- Myalgia
- Nausea
- Nervousness
- Nightmares
- Vomiting
- Xerostomia
Precautions
No enhanced messaging available.
Safety and efficacy not evaluated in the pediatric population.
Individuals <18 years of age should consult a clinician prior to use of OTC nicotine replacement therapy products.
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 the reach of children.
Animal studies indicate that nicotine may cause fetal harm when administered to pregnant women. Tobacco smoke, which contains nicotine, hydrogen cyanide, and carbon monoxide, has been shown to be harmful to the fetus; adverse effects include fetal growth retardation, increased risk of spontaneous abortion, and increased perinatal mortality. Substantial evidence indicates that decreased birthweight in neonates born to women who smoke is in part caused by a direct vasoconstrictive effect of nicotine on uterine vasculature resulting in fetal hypoxia.
The teratogenic potential of cigarette smoking or nicotine in humans has not been clearly established. Cigarette smoking is known to increase fetal aortic blood flow and heart rate and decrease uterine blood flow and fetal breathing movements. In a limited study of pregnant (e.g., between 24-36 weeks of gestation) women who continued to smoke at least 10 cigarettes daily for 5 days or who discontinued smoking and began taking nicotine polacrilex gum for 5 days at a dosage of at least 6 pieces of 2-mg gum (up to 30 pieces) daily chewed at a rate not to exceed 2 pieces hourly, there were no differences between the groups in changes in maternal or fetal hemodynamic measurements (e.g., maternal heart rate and mean arterial pressure, fetal heart rate, uterine resistance index, umbilical resistance index). The maternal serum cotinine concentration after 5 days was decreased with nicotine polacrilex gum but did not change with continuance of smoking. Peak and trough maternal serum nicotine concentrations after 5 days were lower with nicotine polacrilex gum than with continuance of smoking.
Individuals who are pregnant should consult a healthcare provider prior to the use of OTC nicotine replacement therapy products. Although these products are believed to be safer than smoking, the fetal/neonatal risks are not fully known. The USPHS guideline states that behavioral counseling interventions are effective in improving smoking cessation during pregnancy, but additional research is needed on pharmacotherapy options.
Nicotine is distributed into human milk in a milk to plasma ratio averaging 2.9. Proper use of nicotine polacrilex preparations or transdermal or intranasal nicotine would be expected to produce lower nicotine concentrations in milk than would cigarette smoking because of lower maternal plasma nicotine concentrations with nicotine replacement therapy. Although some clearance of orally absorbed nicotine in infants will occur through first-pass metabolism in the liver, the efficiency of nicotine removal is probably lowest at birth. Nicotine replacement therapy should be used with caution in breastfeeding individuals. The safety of nicotine replacement therapy in infants who are breastfeeding has not been evaluated. Whether to use nicotine replacement therapy in a nursing woman should be based on comparison of the risks associated with exposure to tobacco smoke from continued smoking by the mother, and those associated with use of nicotine replacement therapy alone or in combination with continued smoking. Individuals who are breastfeeding should consult a healthcare provider prior to the use of any nicotine replacement therapy product.
Nicotine nasal spray: Select dosage with caution.
Nicotine nasal spray: 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.
Pharmacokinetics of nicotine in geriatric patients have not been studied.
ICD codes
| Code | Type | Description |
|---|---|---|
| Smoking cessation | ||
| F17 | ICD10CM | Nicotine dependence |
| F17.2 | ICD10CM | Nicotine dependence |
| F17.20 | ICD10CM | Nicotine dependence, unspecified |
| F17.200 | ICD10CM | Nicotine dependence, unspecified, uncomplicated |
| F17.201 | ICD10CM | Nicotine dependence, unspecified, in remission |
| F17.203 | ICD10CM | Nicotine dependence unspecified, with withdrawal |
| F17.208 | ICD10CM | Nicotine dependence, unspecified, with other nicotine-induced disorders |
| F17.209 | ICD10CM | Nicotine dependence, unspecified, with unspecified nicotine-induced disorders |
| F17.21 | ICD10CM | Nicotine dependence, cigarettes |
| F17.210 | ICD10CM | Nicotine dependence, cigarettes, uncomplicated |
| F17.211 | ICD10CM | Nicotine dependence, cigarettes, in remission |
| F17.213 | ICD10CM | Nicotine dependence, cigarettes, with withdrawal |
| F17.218 | ICD10CM | Nicotine dependence, cigarettes, with other nicotine-induced disorders |
| F17.219 | ICD10CM | Nicotine dependence, cigarettes, with unspecified nicotine-induced disorders |
| O99.33 | ICD10CM | Tobacco use disorder complicating pregnancy, childbirth, and the puerperium |
| O99.330 | ICD10CM | Smoking (tobacco) complicating pregnancy, unspecified trimester |
| O99.331 | ICD10CM | Smoking (tobacco) complicating pregnancy, first trimester |
| O99.332 | ICD10CM | Smoking (tobacco) complicating pregnancy, second trimester |
| O99.333 | ICD10CM | Smoking (tobacco) complicating pregnancy, third trimester |
| O99.334 | ICD10CM | Smoking (tobacco) complicating childbirth |
| O99.335 | ICD10CM | Smoking (tobacco) complicating the puerperium |
| Z87.891 | ICD10CM | Personal history of nicotine dependence |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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