Varenicline tartrate tablets

Varenicline selectively binds to the a4p2 nicotinic acetylcholine receptor and has a high affinity for the receptor. Varenicline binds to the a4p2 nicotinic acetylcholine receptor subtype to produce an agonist effect, while blocking nicotine from binding to the receptor, which is the mechanism by which varenicline exerts its smoking cessation effect. In vitro electrophysiological studies and in vivo neurochemical studies have shown that varenicline binds to the neural α4β2 nicotinic acetylcholine receptor and stimulates receptor-mediated activity, but this effect is significantly weaker than nicotine. Varenicline can block nicotine from binding to the α4β2 nicotinic acetylcholine receptor, thereby activating the mesolimbic dopamine system, which is the underlying neural mechanism of the reinforcement-reward effect of smoking. Varenicline is highly selective for the α4β2 nicotinic acetylcholine receptor, and its binding to this receptor subtype is stronger than that to other common nicotine receptors (α3β4500 times, α73500 times, α1βγδ20000 times), non-nicotine receptors and transporters (2000 times). In addition, varenicline has a moderate affinity for 5-hydroxytryptamine (5-HT3) receptors (Ki=350nM).

The main ingredient is varenicline tartrate. Chemical name: 7,8,9,10-tetrahydro-6,10-methylene-6H-pyrazinamide [2,3-h]-[3]benzazepine-(2R,3R)-2,3-dihydroxysuccinate (1:1) Molecular weight: C13H13N3middot; C4H6O6

This product is a light blue film-coated tablet, which appears white after removing the coating.

Suitable for adults to quit smoking.

This product is for oral administration. First, perform a 1-week dose increase as follows, after which the recommended dose is 1 mg twice a day. 1. Days 1-3: 0.5 mg, once a day (white tablets) 2. Days 4-7: 0.5 mg, twice a day (white tablets) 3. Day 8 - end of treatment: 1 mg, twice a day (light blue tablets) 4. Patients should set a date to quit smoking and start taking this product 1-2 weeks before this date. 5. For patients who cannot tolerate the adverse reactions of this product, the dose can be temporarily or permanently reduced to 0.5 mg twice a day. 6. This product should be swallowed whole with water and can be taken before or after meals. 7. Patients should take this product for 12 weeks of treatment. 8. For patients who successfully quit smoking after 12 weeks of treatment, consider adding another 12-week course of treatment, and the dose is still daily

1. Regardless of whether or not you receive smoking cessation treatment, quitting smoking itself is accompanied by a variety of symptoms. For example, it has been reported that patients who try to quit smoking experience restlessness, depression, insomnia, irritability, frustration, anger, anxiety, inability to concentrate, restlessness, decreased heart rate, increased appetite or weight gain. The design and result analysis of the clinical study of this product did not distinguish between the adverse events that occurred and the relevance of drug or nicotine withdrawal. 2. Multiple clinical studies of this product involved approximately 4,000 patients, with the longest treatment time being 1 year (average administration of 84 days). If adverse reactions occur, they usually occur in the first week of treatment, and the severity is mostly mild to moderate. There is no difference in the incidence of adverse reactions among different ages, races or genders. 3. After completing the initial dose escalation, patients take the recommended dose twice a day, 1 mg each time. The most reported adverse event is nausea (28.6%). Nausea mostly occurs in the early stages of treatment, with a severity of mild to moderate, and rarely leads to treatment interruption. 4. The proportion of patients who interrupted treatment due to adverse events was 11.4% in the treatment group and 9.7% in the placebo group. Among these patients, the treatment discontinuation rates for common adverse events in the treatment group were: nausea (2.7%, placebo group 0.6%), headache (0.6%, placebo group 1.0%), insomnia (1.3%, placebo group 1.2%), and abnormal dreams (0.2%, placebo group 0.2%). 5. The following table lists the adverse reactions with a higher incidence in the treatment group than in the placebo group, all according to system organ type.

1. Patients who are highly sensitive to tramadol hydrochloride sustained-release tablets and patients with acute poisoning by alcohol, hypnotics, analgesics or other psychotropic drugs. 2. Tramadol hydrochloride sustained-release tablets should be used with caution in opioid-dependent patients with unclear causes of disordered consciousness, respiratory center and respiratory function disorders, increased intracranial pressure without artificial respiration equipment, and infants under 18 years old.

Precautions for children: Due to limited safety and efficacy data for this product in children or adolescents under 18 years of age, this product is not recommended for use in this population. Precautions for pregnancy and lactation: There is limited data on the use of Changpei in pregnant women. Animal studies have shown that Changpei is reproductively toxic. The potential risks for human use are unknown. Changpei should not be used during pregnancy. It is not clear whether Changpei is excreted in human milk. Animal studies suggest that Changpei can be excreted into breast milk. The benefits of breastfeeding for the infant and the benefits of Changpei treatment for breastfeeding women should be weighed to make a decision to continue/terminate breastfeeding or continue/terminate Changpei treatment. Precautions for the elderly: Because elderly patients are more susceptible to renal impairment, prescribing physicians should consider the renal function status of elderly patients.

1. Based on the characteristics of varenicline and current clinical experience, no clinically significant interactions have been found between this product and other drugs. There is no need to adjust the dose of this product and the following combined medications. 2. In vitro studies have shown that for compounds that are mainly metabolized by cytochrome P450, it is unlikely that varenicline will not change their pharmacokinetic parameters; since less than 10% of varenicline is eliminated by metabolism, varenicline has little effect on the pharmacokinetic parameters of active substances known to affect the cytochrome P450 system.

Seal and store at 30℃.

1.0mg*56s

24 months