No Smoking Day - How much do you know about the smoking cessation drug varenicline tartrate?

In today's society, quitting smoking has become a health topic that more and more people are concerned about. However, although people are generally aware of the harm of smoking to health, quitting smoking is not easy. Smoking cessation drugs have become an important auxiliary tool because they can help smokers quit smoking in a more scientific way. Next, the editor will introduce a smoking cessation drug - varenicline tartrate.

Smoking cessation drug - Varenicline's smoking cessation mechanism

When talking about the smoking cessation mechanism of this drug, we must first introduce why smoking is addictive. Nicotine is released when smoking. After entering the brain, nicotine can activate acetylcholine nicotinic receptors, induce a large amount of dopamine release, and make people feel happy. However, due to the rapid metabolism of nicotine, as the nicotine content in the brain decreases, the amount of dopamine released will also decrease, and smokers will feel irritable and uncomfortable, and want to have another cigarette. In this way, a "reward circuit" dependent on nicotine is formed in the brain, resulting in a smoking addiction.

Varenicline, as a selective partial agonist of the a4β2 subtype of nicotinic acetylcholine receptor, has a high affinity for this receptor in nerves. Varenicline binds to the a4β2 receptor to produce an agonistic effect, activating the mesolimbic dopamine system, thereby simulating the brain reward brought by smoking, reducing the withdrawal symptoms and craving for cigarettes in smokers who quit smoking. At the same time, it blocks nicotine from binding to the receptor, reducing the pleasure brought by smoking, and thus helping smokers quit smoking.

How to use varenicline

First, patients should set a date to quit smoking and start taking varenicline 1 to 2 weeks before this date. The specific usage is as follows: Days 1 to 3: 0.5 mg each time, once a day. Days 4 to 7: 0.5 mg each time, twice a day. Day 8 to the end of treatment: 1 mg each time, twice a day. A total of 12 weeks of regular use is required, which may be extended depending on the treatment situation. It is recommended that you use it reasonably under the guidance of a doctor.

Precautions for use of varenicline

1. Can I drink alcohol while taking varenicline?

It is recommended to reduce alcohol consumption during use.

2. Do elderly people need to adjust the dosage?

No dosage adjustment is required for the elderly.

3. Can pregnant women take varenicline?

Animal studies have shown that varenicline is reproductively toxic, so as a precaution, varenicline should be avoided during pregnancy.

4. Can patients with liver or kidney damage use varenicline?

Patients with impaired liver function do not require dose adjustment, but the dose of this drug should be adjusted based on renal function as follows:

5. What are the common adverse reactions of varenicline?

Nausea is the most common adverse reaction of varenicline. Nausea symptoms are usually mild to moderate and often occur in the early stages of treatment. In addition, varenicline prevents users from feeling the pleasure of smoking, so it may also cause neuropsychiatric symptoms such as depression.

It should be noted that regardless of whether or not medication is used to quit smoking, patients may experience nicotine withdrawal symptoms, such as irritability, depression, insomnia, anxiety, increased appetite or weight gain, etc.

6. Will tolerance and dependence occur with varenicline?

The drug does not cause tolerance. Higher doses (greater than 2 mg) of varenicline are more likely to cause increased adverse reactions, such as gastrointestinal discomfort, but no clinical evidence has been found that the dose needs to be continuously increased to maintain the therapeutic effect.

Regarding dependence, studies have shown that less than 1/1000 patients experience euphoria when using varenicline. However, studies have found that if the drug is stopped suddenly, no more than 3% of patients will experience irritability and sleep disorders after abrupt discontinuation, which suggests that varenicline may cause mild physical dependence, but it has nothing to do with addiction. Therefore, it is reminded that varenicline should be taken and discontinued under the supervision of a doctor.

Finally, I would like to remind all smokers that varenicline is a prescription drug and needs to be purchased with a doctor's prescription and used reasonably under the guidance of a doctor. Before using this drug, you need to understand the product's usage, side effects, and individual differences, and quit smoking scientifically.

References:

[1] NL Benowitz, Nicotine Addiction, NEW ENGLANDJOURNAL OF MEDICINE, 362 (2010) 2295-2303.

[2] Varenicline Tartrate Tablets Instructions