VARENICLINE FOR SMOKING CESSATION

Generality

Varenicline is a drug with specific indications to help patients quit smoking. Varenicline represents an "alternative to" the use of other drugs used to combat smoking addiction, such as bupropion and nicotine replacement therapy.

Varenicline - Chemical Structure

Studies have even shown that varenicline may be more effective than bupropion in smoking cessation therapy and relapse prevention.
Varenicline obtained approval for entry into the European Union in 2006.

Mechanism of action

Varenicline is a partial agonist of nicotinic receptors. More specifically, varenicline interacts with the α4β2 nicotinic receptor present in the brain which is the same receptor to which nicotine deriving from tobacco smoke binds.
By binding to this receptor, varenicline is able to partially stimulate it and this causes the symptoms induced by smoking withdrawal to decrease. Furthermore, varenicline prevents nicotine from binding to the aforementioned receptor, in this way - in which case the patient resumes smoking during drug therapy - there is a decrease in pleasure and satisfaction associated with smoking.

Side effects

Smoking cessation can cause some side effects even if you are undergoing drug therapy. These effects usually consist of mood changes, insomnia, difficulty concentrating, increased appetite, weight gain. and decreased heart rate.
In addition, varenicline itself can also cause side effects, although not all patients experience them.
The most common adverse effects that can occur during varenicline therapy include:

Headache;

Inflammation of the nose and throat;

Sleep disorders;

Altered dreams

Increased or decreased appetite;

Weight gain

Drowsiness;

Dizziness

Shortness of breath or cough

Chest infections

Sinusitis;

Heartburn and abdominal pain;

He retched;

Diarrhea or constipation

Difficulty in digestion;

Skin rashes;

Joint and muscle pains.

Dosage

Varenicline is available for oral administration in the form of tablets.
Generally, a dose of 0.5 mg of varenicline per day is given for the first three days of therapy. Then, from the fourth to the seventh day of therapy, the dose of drug used is 0.5 mg to be taken twice a day. Finally, from the second week of therapy until the end of treatment, the varenicline dose is increased to 1 mg, to be taken twice a day.
Treatment usually lasts twelve weeks and smoking should be stopped within the fifth week of starting therapy.
After twelve weeks of therapy - if deemed necessary - the doctor may decide to prescribe a further twelve weeks treatment to prevent the onset of any relapses.
During therapy with varenicline it is very important to strictly follow the instructions provided by the doctor, both as regards the quantity of drug to be taken and as regards the frequency of administration and the duration of the same treatment.
Finally, it should be emphasized that in patients who are highly motivated to quit smoking there is a greater probability of success of drug therapy.

Use in pregnancy and during lactation

Varenicline should not be used in pregnant women. Furthermore, although no specific studies have been conducted in this regard, varenicline may be excreted in breast milk. Therefore, breastfeeding mothers should seek medical advice before starting any therapy with this drug.
In any case, pregnant women and breastfeeding mothers should always seek medical advice before taking medications of any kind.