Varenicline tartrate

The main ingredient of this product 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).

Based on the properties of varenicline and current clinical experience, no clinically significant interactions have been found between this product and other drugs. No dose adjustment is required for this product and the following co-administered drugs. In vitro studies have shown that it is unlikely that varenicline will not change the pharmacokinetic parameters of compounds that are primarily metabolized by cytochrome P450; 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 (see [Pharmacokinetics]), so the dose of this product 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 eliminated through renal secretion (such as metformin - as shown below). Metformin: Varenicline does not affect the pharmacokinetic parameters of metformin. Metformin also does not affect the pharmacokinetic parameters of varenicline. Cimetidine: When varenicline and cimetidine are used simultaneously, the renal clearance of varenicline is reduced and its systemic exposure is increased by 29%. No dose adjustment is required for subjects with normal renal function or patients with mild or moderate renal impairment. For patients with severe renal impairment, the concomitant use of the two drugs should be avoided. Digoxin: Varenicline does not change the steady-state pharmacokinetic parameters of digoxin. Warfarin: Varenicline does not change the pharmacokinetic parameters of warfarin. Prothrombin time (measured in INR) is not affected by varenicline. Smoking cessation itself is unlikely to change the pharmacokinetics of warfarin (see [Precautions]). Concomitant use with other smoking cessation drugs: Bupropion: Varenicline does not change the steady-state pharmacokinetic parameters of bupropion. Nicotine replacement therapy (NRT): When varenicline was given to smokers simultaneously with transdermal NRT for 12 days, the mean systolic blood pressure measured on the last day of the study was significantly reduced (mean 2.6 mmHg), and this change was statistically significant. In this study, the incidence of nausea, headache, vomiting, dizziness, dyspepsia, and fatigue was higher in the combination treatment group than in the NRT treatment group alone. Alcohol: There is limited clinical data on the potential interaction between alcohol and varenicline. The safety and effectiveness of this product in combination with other smoking cessation therapies have not been studied.

The main ingredient of this product 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).

Based on the properties of varenicline and current clinical experience, no clinically significant interactions have been found between this product and other drugs. No dose adjustment is required for this product and the following co-administered drugs. In vitro studies have shown that it is unlikely that varenicline will not change the pharmacokinetic parameters of compounds that are primarily metabolized by cytochrome P450; 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 (see [Pharmacokinetics]), so the dose of this product 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 eliminated through renal secretion (such as metformin - as shown below). Metformin: Varenicline does not affect the pharmacokinetic parameters of metformin. Metformin also does not affect the pharmacokinetic parameters of varenicline. Cimetidine: When varenicline and cimetidine are used simultaneously, the renal clearance of varenicline is reduced and its systemic exposure is increased by 29%. No dose adjustment is required for subjects with normal renal function or patients with mild or moderate renal impairment. For patients with severe renal impairment, the concomitant use of the two drugs should be avoided. Digoxin: Varenicline does not change the steady-state pharmacokinetic parameters of digoxin. Warfarin: Varenicline does not change the pharmacokinetic parameters of warfarin. Prothrombin time (measured in INR) is not affected by varenicline. Smoking cessation itself is unlikely to change the pharmacokinetics of warfarin (see [Precautions]). Concomitant use with other smoking cessation drugs: Bupropion: Varenicline does not change the steady-state pharmacokinetic parameters of bupropion. Nicotine replacement therapy (NRT): When varenicline was given to smokers simultaneously with transdermal NRT for 12 days, the mean systolic blood pressure measured on the last day of the study was significantly reduced (mean 2.6 mmHg), and this change was statistically significant. In this study, the incidence of nausea, headache, vomiting, dizziness, dyspepsia, and fatigue was higher in the combination treatment group than in the NRT treatment group alone. Alcohol: There is limited clinical data on the potential interaction between alcohol and varenicline. The safety and effectiveness of this product in combination with other smoking cessation therapies have not been studied.