Products
Nicotine is commercially available in the form of chewing gum, lozenges, sublingual tablets, transdermal patch, oral spray, and inhaler (Nicorette, Nicotinell, generics). The first nicotine replacement product was approved in many countries in 1978.
Structure and properties
Nicotine (C10H14N2, Mr = 162.2 g/mol) exists as a colorless to brownish, viscous, hygroscopic, volatile liquid that is soluble in water. It is an -methylpyrrolidine and pyridine derivative and is used as a pure -enantiomer. Nicotine is a natural alkaloid found in the tobacco plant (, ) of the nightshade family. Some of the drugs contain nicotinic resinate, a complex of nicotine with a weak cation exchanger.
Effects
Nicotine (ATC N07BA01) has psychoactive, stimulant, activator, relaxant, and antianxiety properties. It promotes alertness and concentration. Its effects are due in part to binding to nicotinic acetylcholine receptors and increased release of neurotransmitters such as dopamine and serotonin in the central nervous system. Nicotine is administered as part of smoking cessation to reduce withdrawal symptoms. It increases the likelihood of quitting smoking altogether. The pharmacokinetics of nicotine replacement products are different from cigarettes. Nicotine travels much more slowly from the products through the oral mucosa or skin to the site of action in the brain. Plasma concentrations are lower and the effects last longer. When smoked, nicotine rapidly enters the circulation and central nervous system from the lungs in high concentrations.
Indications
To support smoking cessation in nicotine-dependent smokers. To reduce addictive behavior and cigarette use by decreasing withdrawal symptoms.
Dosage
According to the Smoking Guide. Dosage is based on nicotine dependence. Towards the end of treatment, the nicotine dose is progressively reduced and eventually the replacement products are discontinued altogether. Different dosage forms are available for different needs and smoker types:
| Chewing gum | Classic dosage form, easy to use as needed |
| Transdermal patches | Continuous long-term effect (24 hours), discrete and easy application |
| Oral spray | Rapid onset of action after 1 minute |
| Inhaler | Handling like a cigarette, keeps hands busy |
| Lozenges, sublingual tablets. | Discreet and easy administration |
Abuse
Nicotine replacement products can in principle be abused as stimulants and intoxicants. However, due to differences in pharmacokinetics, the potential for dependence is lower.
Contraindications
- Non-smoker
- Children under 12 years
- Pregnancy and lactation
Full precautions can be found in the drug label.
Interactions
Inhalation of cigarette smoke induces the metabolic isoenzyme CYP1A2. When smoking is discontinued, this induction ceases and plasma concentrations of CYP1A2 substrates may be increased (eg, theophylline, clozapine, ropinirole).
Adverse effects
The most common possible adverse effects include headache, hiccups, cough, irritation of the oral and pharyngeal mucosa, and gastrointestinal discomfort. Remedies must be kept out of the reach of children. Nicotine is a potent poison that can cause death even in small doses. The lethal dose for an adult is about 1 mg per kilogram of body weight. Nicotine intake with replacement products is far less harmful to health than smoking. However, there is evidence in the scientific literature that nicotine itself may also be active as a carcinogen, for example, due to the formation of corresponding metabolites (e.g., Suzuki et al., 2018; Stepanov et al., 2009; Campain, 2004). Therefore, the substitute preparations should only be used for the prescribed duration of use.
