Drug information of Nicotine

Nicotine


Nicotine is the primary ingredient in tobacco products.
Nicotine gum and lozenges are medical products used to aid in smoking cessation in adults.
Using a controlled amount of nicotine helps reduce withrawal symptoms when you quit smoking.

Mechanism of effect

Nicotine, a naturally occurring alkaloid, binds stereo-selectively to nicotinic-cholinergic receptors at the autonomic ganglia, in the adrenal medulla, at neuromuscular junctions, and in the brain. Two types of CNS effects are believed to be the basis of nicotine's positively reinforcing properties; a stimulating effect is exerted mainly in the cortex via the locus ceruleus and a reward effect is exerted in the limbic system. At low doses the stimulant effects predominate while at high doses the reward effects predominate.

Pharmacodynamic

Ganglionic (nicotinic) cholinergic-receptor agonist

Pharmacokinetics

Absorption
Buccal mucosa, transdermal: Slow; Intranasal: ~53%; Inhaler: <5% reaches the lower respiratory tract
Distribution
2 to 3 L/kg (Svensson 1987)
Metabolism
Hepatic (major), kidney, and lung; >20 metabolites (primarily metabolites are to cotinine (1/5 as active) and trans-3-hydroxycotinine)
Excretion
Urine (~10% as unchanged)
Onset of Action
Intranasal: More closely approximate the time course of plasma nicotine levels observed after cigarette smoking than other dosage forms (Svensson 1987)
Time to Peak
Serum: Transdermal: ~2 to 8 hours (Bannon 1989; DeVeaugh-Geiss 2010); Intranasal: 10 to 20 minutes; Oral inhalation: ≤15 minutes; Gum: ~30 minutes (Svensson 1987)
Half-Life Elimination
Transdermal: ~4 hours (Bannon 1989); Nasal spray: 1 to 2 hours; Inhaler: 1 to 2 hours
Protein Binding
5% to 20% (Svensson 1987)

Drug indications

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.257 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.5
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†

Dosage

GUM:
Recommended dose:
-First cigarette within 30 minutes of waking up: 4 mg
-First cigarette more than 30 minutes after waking up: 2 mg
Recommended regimen:
-Weeks 1 to 6: 1 piece of gum orally every 1 to 2 hours
-Weeks 7 to 9: 1 piece of gum orally every 2 to 4 hours
-Weeks 10 to 12: 1 piece of gum orally every 4 to 8 hours
-Maximum dose: 24 pieces/day

INHALER:
Initial Treatment:
-Recommended dose: At least 6 cartridges inhaled once a day for the first 3 to 6 weeks
-Maximum dose: 16 cartridges/day
-Duration of therapy: Up to 12 weeks

Gradual Dose Reduction:
-Duration of therapy: Up to 12 weeks

NASAL SPRAY:
Initial Treatment:
-Recommended dose: 1 to 2 sprays in each nostril every hour for up to 3 months
-Maximum dose: 40 mg/day

PATCH:
STEP 1: 21 mg patch transdermally once a day
STEP 2: 14 mg patch transdermally once a day
STEP 3: 7 mg patch transdermally once a day

More than 10 cigarettes/day:
-Step 1 for 4 weeks, then step 2 for 2 weeks, and finally step 3 for 2 weeks

10 cigarettes/day or less:
-Step 2 for 6 weeks, then step 3 for 2 weeks

Drug contraindications

Known hypersensitivity to nicotine, menthol (oral inhaler), or any ingredient in the formulation.
Nicotine polacrilex gum in patients with temporomandibular joint disease.

Side effects

Check with your doctor immediately if any of the following side effects occur while taking nicotine:
Less common
Blurred vision
dizziness
headache
nervousness
pounding in the ears
Rare
Fast or irregular heartbeat
hives, itching, rash, redness, or swelling of the skin
Get emergency help immediately if any of the following symptoms of overdose occur while taking nicotine:
Symptoms of overdose
Dizziness
fast heartbeat
nausea or vomiting
weakness

Alerts

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.

Points of recommendation

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).

Pregnancy level

Category D

Breast feeding warning

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

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