Instructions for Varenicline Tartrate Tablets

Varenicline tartrate tablets (Changpei) are suitable for adults to quit smoking. Below is the instruction manual I compiled for Varenicline Tartrate Tablets. Welcome to read it. Product introduction of Varenicline Tartrate Tablets

Common name: Varenicline Tartrate Tablets

Manufacturer: Pfizer Manufacturing Deutschland GmbH (Germany)

Approval number: H20130406

Drug specification: 0.5mg*11s+1mg*14 tablets

Drug price: RMB 268 Yuan Varenicline Tartrate Tablets Instructions

Common name: Varenicline Tartrate Varenicline Tartrate Tablets

Product name Varenicline Tartrate Tablets (ChangPei) (starter pack)

English name VareniclineTartrateTablets

Pinyin full code JiuShiSuanFaNiKeLanPian (ChangPei) ( QiDongZhuang)

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 formula: C13H13N3?C4H6O6

Molecular weight: 361.36

Properties Varenicline tartrate tablets (Changpei) (starter pack) are light blue film-coated tablets , it appears white after removing the coating.

Indications/functions and indications are suitable for adults to quit smoking.

Specification model 0.5mg*11s+1mg*14s

Usage and dosage Varenicline tartrate tablets (Changpei) (starter pack) are for oral administration. First perform a 1-week dose escalation as follows, and then 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 once a day 2 times a day (light blue tablets) 4. The patient should set a quit date and start taking varenicline tartrate tablets (Changpei) (starter pack) 1-2 weeks before this date. 5. For patients who cannot tolerate the adverse reactions of Varenicline Tartrate Tablets (Changpei) (starter pack), the dose can be temporarily or long-term reduced to 0.5 mg twice a day. 6. Varenicline tartrate tablets (Changpei) (starter pack) should be swallowed whole with water, before or after meals. 7. Patients should take varenicline tartrate tablets (Changpei) (starter pack) for 12 weeks. 8. For patients who successfully quit smoking after 12 weeks of treatment, an additional 12-week course of treatment may be considered, and the dose is still 1 mg twice a day (see

Adverse reactions regardless of whether they receive smoking cessation treatment or not, quit smoking It is accompanied by a variety of symptoms, such as irritability, depression, insomnia, irritability, frustration, anger, anxiety, difficulty concentrating, restlessness, decreased heart rate, increased appetite, or weight gain. The design and results analysis of Changpei's clinical studies did not distinguish between adverse events related to drugs or nicotine withdrawal. Multiple clinical studies of Changpei involved approximately 4,000 patients, with an average treatment duration of 1 year. 84 days of administration). If adverse reactions occurred, they usually occurred during the first week of treatment and were mostly mild to moderate in severity. There were no differences in the incidence of adverse reactions by age, race, or gender after completion of the initial dose escalation. Take the recommended dose of 1 mg twice daily. The most commonly reported adverse event is nausea (28.6%), which mostly occurs in the early stages of treatment and is mild to moderate in severity and rarely leads to discontinuation of treatment. The proportion of patients who discontinued treatment was 11.4% in the treatment group and 9.7% in the placebo group. Among these patients, the treatment discontinuation rate for common adverse events was nausea (2.7% in the treatment group and 0.6% in the placebo group) and headache (0.6%). %, placebo group 1.0%), insomnia (1.3%, placebo group 1.2%), and abnormal dreams (0.2%, placebo group 0.2%).

The adverse reactions that occur more frequently in the treatment group than in the placebo group are listed in the table below, arranged according to system organ type and frequency of occurrence: very common (?1/10), common (?1/100 to <1/10) , rare (?1/1000 to <1/100), rare (?1/10000 to <1/1000)). Adverse reactions with similar frequency of occurrence are listed in order from severe to mild. Infection: Rarely bronchitis, nasopharyngitis, sinusitis, fungal infection, viral infection. Metabolic and nutritional abnormalities: Common are increased appetite; rare are anorexia, loss of appetite, and polydipsia. Mental abnormalities: Abnormal dreams and insomnia are very common; panic, slow thinking, abnormal thinking, and emotional instability are rare. Nervous system abnormalities: Headache is very common; drowsiness, dizziness, and dysgeusia are common; tremor, ataxia, dysarthria, hypertonia, restlessness, dysthymia, hypoesthesia, hypogeusia, narcolepsy, and increased sexual desire are rare. Decreased libido. Heart abnormalities: Atrial fibrillation and palpitations are rare. Eye abnormalities: rare dark spots, scleral depigmentation, eye pain, mydriasis, photophobia, myopia, and excessive tearing. Ear and labyrinth abnormalities: Tinnitus is rare. Respiratory system, chest and mediastinal abnormalities: Rarely, dyspnea, cough, hoarseness, sore throat, throat irritation, respiratory congestion, sinus congestion, postnasal drip, rhinorrhea, and snoring. Gastrointestinal abnormalities: nausea is very common; vomiting, constipation, diarrhea, bloating, stomach discomfort, indigestion, flatulence, dry mouth are common; hematemesis, hematochezia, gastritis, gastroesophageal reflux disease, abdominal pain, and bowel habits are rare Changes, abnormal stool, belching, ulcerative stomatitis, gum pain, thick and greasy tongue coating. Skin and subcutaneous tissue abnormalities: rare systemic rash, erythema, pruritus, acne, hyperhidrosis, and night sweats. Musculoskeletal and connective tissue abnormalities: Rarely, joint stiffness, muscle spasm, chest wall pain, and costochondritis. Renal and urinary abnormalities: rare glycosuria, nocturia, and polyuria. Reproductive system and breast abnormalities: rare menorrhagia, vaginal discharge, and sexual dysfunction. Systemic abnormalities and abnormalities at the administration site: fatigue is common; chest discomfort, chest pain, fever, chills, weakness, circadian rhythm sleep disorder, general discomfort, and cysts are rare. Objective examination: Rarely, elevated blood pressure, electrocardiogram ST segment depression, electrocardiogram T wave amplitude reduction, accelerated heart rate, abnormal liver function tests, decreased platelet count, weight gain, abnormal semen, increased C-reactive protein, and decreased blood calcium.

People who are allergic to Changpei’s active ingredients or any excipients are contraindicated.

Notes on the effects of smoking cessation: Regardless of whether you receive Changpei treatment or not, the physiological changes caused by smoking cessation itself can change the pharmacokinetics or pharmacodynamics of some drugs, so the dosage of these drugs may need to be adjusted ( Such as aminophylline, warfarin and insulin). Smoking induces CYP1A2 activity, so quitting smoking may result in increased plasma levels of CYP1A2 substrates. Smoking cessation itself, whether treated with medication or not, is associated with worsening of underlying mental illness, such as depression. Patients with a history of mental illness should be treated with caution and given appropriate advice. There is no clinical experience using Changpei in patients with epilepsy. At the end of treatment, up to 3% of patients experienced an increase in symptoms such as irritability, craving for cigarettes, depression and/or insomnia, which were associated with discontinuation of the drug. Therefore, the prescriber should inform the patient of the relevant information and consider or discuss with the patient whether the dosage needs to be tapered gradually. Effects on Ability to Drive and Use Machinery: Changpei may have mild to moderate effects on the ability to drive and use machinery. Changpei may cause dizziness and drowsiness, which may affect your ability to drive and operate machinery. It is recommended that patients first determine whether Changpei will affect their driving, operating complex machinery, or engaging in other potentially risky activities before engaging in such activities. Substance Abuse and Dependence: Less than 1/1000 patients reported feelings of euphoria in clinical studies. Higher doses (greater than 2 mg) are more likely to cause gastrointestinal discomfort, such as nausea and vomiting. No evidence was found in clinical studies that the dose needs to be continuously increased to maintain the therapeutic effect, which suggests that tolerance to Changpei will not occur. If the drug is stopped suddenly, no more than 3% of patients will develop irritability and sleep disorders. This suggests that varenicline may produce mild physical dependence in some patients but is not associated with addiction. In a laboratory human abuse potential study, a single oral dose of 1 mg of Trimax did not produce significant positive or negative subjective reactions in smokers. In non-smokers, 1 mg of Trimax was associated with an increase in some positive subjective responses, but was accompanied by negative adverse effects, particularly an increase in nausea.

A single oral dose of 3 mg of Changpei will cause unpleasant subjective reactions in both smokers and non-smokers.

Pediatric Medication Due to the limited safety and effectiveness data of Changpei in children or adolescents under 18 years of age, it is not recommended to use Changpei in this population (see Pharmacokinetics).

Elderly patients do not need to adjust the dosage (see Pharmacokinetics). Because elderly patients are more likely to develop decreased renal function, prescribers should consider the renal function status of elderly patients.

Pregnant and lactating women have limited data on the use of Changpei in pregnant women. Animal studies have shown that Changpei is reproductively toxic (see Changpei Pharmacology and Toxicology). The potential risk for human use is unknown. Changpei should not be used during pregnancy. It is unknown whether varenicline is excreted in human milk. Animal studies suggest that varenicline may be excreted in breast milk. The benefits of breast-feeding to the infant and the benefits of TROPET treatment to the breastfeeding woman should be weighed to make a decision to continue/terminate breastfeeding or to continue/terminate TRAMP treatment.

Drug Interactions Based on the characteristics of Changpei and current clinical experience, no clinically significant interactions have been found between Changpei and other drugs. There is no need to adjust the dosage of Changpei and the following concomitant medications. In vitro studies show that for compounds that are mainly metabolized by cytochrome P450, it is unlikely that Changpei will not change its pharmacokinetic parameters; since less than 10% of varenicline is eliminated by metabolism, it is known to affect the cytochrome P450 system. As an active substance, Changpei has little effect on its pharmacokinetic parameters, so the dosage of Changpei does not need to be adjusted. In vitro studies have shown that therapeutic concentrations of varenicline have no inhibitory effect on human renal transporters. Therefore varenicline is unlikely to affect active substances that are cleared by renal secretion (such as metformin - shown below). Metformin: Changpei does not affect the pharmacokinetic parameters of metformin. Metformin also does not affect the pharmacokinetic parameters of Changpei. Cimetidine: When using Changpei and cimetidine at the same time, the renal clearance rate of Changpei is reduced, and its systemic exposure is increased by 29%. Subjects with normal renal function or patients with mild or moderate renal impairment do not need to adjust the dose when taking both drugs simultaneously. For patients with severe renal impairment, simultaneous use of the two drugs should be avoided. Digoxin: Changpei does not change the steady-state pharmacokinetic parameters of digoxin. Warfarin: Changpei does not change the pharmacokinetic parameters of warfarin. Prothrombin time (measured as INR) is not affected by varenicline. Smoking cessation itself may alter the pharmacokinetic parameters of warfarin. Concomitant use with other smoking cessation treatments: Bupropion-varenicline does not alter the steady-state pharmacokinetic parameters of bupropion. Nicotine replacement therapy (NRT) - When varenicline and transdermal NRT were given to smokers simultaneously for 12 days, the mean systolic blood pressure measured 1 day after the study was significantly reduced (mean 2.6mmHg), and this change was statistically significant. In this study, the incidence of nausea, headache, vomiting, dizziness, indigestion and fatigue in the combined treatment group was higher than that in the NRT treatment group alone. Alcohol: There are limited clinical data on the potential interaction between alcohol and Changpai. The safety and effectiveness of Changpei in combination with other smoking cessation treatments have not been studied. FDA pregnancy classification: Class C: Animal studies have proven that the drug is harmful to the fetus (teratogenic or embryonic death, etc.), or there are no controlled studies on pregnant women, or no studies on pregnant women and animals have been conducted. This type of drug can only be used after weighing the benefits to the pregnant woman outweighing the harm to the fetus.

In the event of drug overdose, standard supportive care should be provided as required. Studies have shown that varenicline can be eliminated by dialysis when given to patients with end-stage renal disease (see Changpei Pharmacokinetics), but there is no experience with dialysis in the treatment of drug overdose.

Pharmacology and Toxicology Varenicline is a selective partial agonist of nicotinic acetylcholine receptor ?4?2 subtype and has high affinity for this receptor in nerves. Varenicline binds to the ?4?2 receptor to produce an agonistic effect, and at the same time blocks the binding of nicotine to the receptor. This is the mechanism by which varenicline exerts its smoking cessation effect. In vitro electrophysiological studies and in vivo neurochemical studies have shown that Changpei binds to neural 4-2 nicotinic acetylcholine receptors and stimulates receptor-mediated activities, but this effect is significantly weaker than that of nicotine. Changpei can block the agonistic effect of nicotine on ?4?2 receptors and the mesolimbic dopamine system, which is the underlying neural mechanism of the reinforcing and rewarding effects of smoking.

Varenicline is highly selective for ?4?2 receptors, and its binding ability to this receptor subtype is stronger than that of other common nicotinic receptors (?3?4>500 times, ?7>3500 times,? 1>20000 times), non-nicotinic receptors and transporters (>2000 times). In addition, varenicline has a moderate affinity for 5-HT3 receptors (Ki=350nM).

Pharmacokinetic absorption: Varenicline generally reaches peak plasma concentration 3-4 hours after oral administration. After multiple oral administrations to healthy volunteers, the plasma concentration can reach a steady state within 4 days. It is completely absorbed after oral administration and has high systemic bioavailability. The oral bioavailability of varenicline is not affected by food and time of administration. Distribution: Changpei is distributed in various tissues including brain tissue. Steady-state apparent volume of distribution averaged 415 liters (%CV=50). The plasma protein binding rate of varenicline is low (?20%) and has nothing to do with age and renal function. In rodents, varenicline crosses the placenta and is excreted in breast milk. Biotransformation: The metabolism of varenicline is very low, 92% is excreted in the urine as unchanged drug, and no less than 10% is excreted as metabolites. Minor metabolites found in urine include varenicline-N-carbamoylglucuronide and hydroxyvarenicline. 91% of the substances related to varenicline in the systemic circulation are unchanged drugs. Minor metabolites in the systemic circulation include varenicline-N-carbamoylglucuronide and N-transglucosylvarenicline. Excretion: The excretion half-life of varenicline is approximately 24 hours. Its renal excretion is mainly through glomerular filtration and active secretion by the renal tubules with the help of the organic cation transporter OCT2. Linear/Nonlinear: Varenicline has linear kinetics when administered as a single dose (0.1-3 mg) or as a repeated dose (1-3 mg/day). Pharmacokinetics in Special Populations: Specific pharmacokinetic studies and population pharmacokinetic analyzes have shown that the pharmacokinetic parameters of varenicline do not differ based on age, race, gender, smoking status, or concomitant medications. There are clinically significant changes. Patients with hepatic impairment: Since Changpei is basically not metabolized by the liver, its pharmacokinetic parameters will not be affected when patients with hepatic impairment use this drug. Patients with Renal Impairment: There are no changes in varenicline pharmacokinetic parameters in subjects with mild renal impairment (estimated creatinine clearance >50 mL/min and ~80 mL/min). Systemic exposure to varenicline in patients with moderate renal impairment (estimated creatinine clearance ?30mL/min and ?50mL/min) compared with subjects with normal renal function (estimated creatinine clearance >80mL/min) Volume increased by 1.5 times. Systemic exposure to varenicline was increased 2.1-fold in subjects with severe renal impairment (expected creatinine clearance <30 mL/min). In subjects with end-stage renal disease (ESRD), varenicline is effectively eliminated by hemodialysis. Elderly patients: In elderly patients (65-75 years) with normal renal function, the pharmacokinetic parameters of varenicline are similar to those in younger adult subjects (see Elderly patients with reduced renal function. Adolescent patients: 22 12 -Adolescents aged 17 years old (including 12 and 17 years old) take a single dose of 0.5 mg and 1 mg of varenicline. The pharmacokinetic parameters of varenicline between the two doses are basically proportional to the dose (AUC0). -?) Evaluate the systemic exposure and renal clearance of varenicline and the results are comparable to those in adults. Compared with adults, it can be seen that the Cmax of adolescents is increased by 30% and the elimination half-life is shortened (10.9 hours). Does not inhibit cytochrome P450 (IC50>6400ng/mL). P450 enzymes tested by inhibition experiments include: 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1 and 3A4/5. Hepatocyte varenicline does not induce the activity of cytochrome P4501A2 and 3A4. Therefore, for compounds that are primarily metabolized by cytochrome P450 enzymes, varenicline is unlikely to alter the pharmacokinetic parameters.

Packing: 0.5mg*11 tablets + 1mg*14 tablets/box.

Validity period: 12 months

Implementation standard JX20070067

Approval number H20130406

Manufacturer PfizerManufacturingDeutschlandGmbH (Germany)

Efficacy and functions of Varenicline Tartrate Tablets (Changpei) Varenicline Tartrate Tablets (Changpei) are suitable for adults to quit smoking. Frequently Asked Questions about Taking Varenicline Tartrate Tablets

What is the price of Varenicline Tartrate Tablets (Changpei)? Smoking has certain harmful effects on health, especially the lungs, which are the main organs affected. Varenicline tartrate tablets are suitable for adults to quit smoking. So, what is the price of Varenicline Tartrate Tablets (Changpei)?

Varenicline Tartrate Tablets are suitable for adults to quit smoking. Varenicline tartrate tablets are white to off-white film-coated tablets (0.5 mg specification) or light blue film-coated tablets (1.0 mg specification). They appear white after the coating is removed. The common name of Varenicline Tartrate Tablets is Varenicline Tartrate Tablets.

According to the accounts of many smokers who quit smoking with the help of varenicline tartrate tablets, it is known that personal dependence on nicotine and psychological factors will affect the length of time to quit smoking, which can be as short as ten years. It may last twenty days or even several years. It is difficult to define the efficacy of varenicline tartrate tablets with a precise number. But we cannot deny varenicline tartrate tablets for this reason. Currently, the world's clinical medicine for smoking cessation recommends that the first-line drug for smoking cessation is varenicline tartrate tablets. It can help you reduce the discomfort when quitting smoking, and can also help you gradually eliminate your dependence on tobacco.

The mechanism of action of varenicline tartrate tablets is: by partially stimulating and antagonizing nicotine acetylcholine receptors, it has a dual regulatory effect on the human body, helping to relieve the craving for tobacco, dizziness and irritability after stopping smoking. and various withdrawal symptoms; its antagonistic effect can prevent the binding of nicotine to receptors and reduce the pleasure of smoking.