Pharmacological properties : תכונות פרמקולוגיות

Pharmacodynamic Properties

5.1   Pharmacodynamic properties

ATC Code: N07B A01
Pharmacotherapeutic group: Drugs used in nicotine dependence
Nicotine, the primary alkaloid in tobacco products and a naturally occurring autonomous substance, is a nicotine receptor agonist in the peripheral and central nervous systems and has pronounced CNS and cardiovascular effects. On consumption of tobacco products, nicotine has proven to be addictive, resulting in craving and other withdrawal symptoms when administration is stopped. This craving and these withdrawal symptoms include a strong urge to smoke, dysphoria, insomnia, irritability, frustration or anger, anxiety, concentration difficulties agitation and increased appetite or weight gain.
The gum replaces part of the nicotine that would have been administrated via tobacco and reduces the intensity of the withdrawal symptoms and smoking urge.

Pharmacokinetic Properties

5.2   Pharmacokinetic properties

When the gum is chewed, nicotine is steadily released into the mouth and is rapidly absorbed through the buccal mucosa. A proportion, by the swallowing of nicotine containing saliva, reaches the stomach and intestine where it is inactivated.

The nicotine peak plasma mean concentration after a single dose of the 2 mg coated gum is approximately 6.4 nanograms per ml (after 45 minutes) (average plasma concentration of nicotine when smoking a cigarette is 15-30 nanograms per ml).

The nicotine peak plasma mean concentration after a single dose of the 4 mg coated gum is approximately 9.3 nanograms per ml (after approximately 60 minutes) (average plasma concentration of nicotine when smoking a cigarette is 15-30 nanograms per ml).

Nicotine is eliminated mainly via hepatic metabolism; small amounts of nicotine are eliminated in unchanged form via the kidneys. The plasma halflife is approximately three hours. Nicotine crosses the blood-brain barrier, the placenta and is detectable in breast milk.