Effects of smoking on the pharmacokinetics and pharmacodynamics of a nicotine patch

Abstract

The effect of smoking on the pharmacokinetics and pharmacodynamics of a nicotine transdermal delivery system, administered as a single dose or multiple doses, was examined in smokers (n=12) and nonsmokers (n=12). The study was a two-period, parallel trial. In the first period, a single dose of the Nicotinell TTS 20 patch was administered, followed by a 1-week washout period. Then, in the second period, multiple doses of the Nicotinell TTS 20 patch were administered over 4 days. Regarding the pharmacokinetics of nicotine, the AUC(36 h) and AUC(tau) of smokers were about 20% and 40% greater, respectively, than those of nonsmokers. Significant differences in heart rate were observed between smokers and nonsmokers at 10, 12, 16 and 24 h, and significant differences in systolic blood pressure were seen between smokers and nonsmokers at 12, 30 and 36 h in the single-dose study. With multiple doses, significant differences in systolic and diastolic blood pressures were detected between smokers and nonsmokers only at 72.5 and 82 h. Here, it is demonstrated for the first time that the pharmacokinetic and hemodynamic effects of a nicotine patch are significantly different between smokers and nonsmokers.

Nicotine related brain activity: The influence of smoking history and blood nicotine levels, an exploratory study

“…Higher peak nicotine levels correlated with a steeper relative decline in serum nicotine by the final nicotine measurement at 30 minutes after nicotine administration. This result is consistent with a study comparing nicotine pharmacokinetics and -pharmacodynamics resulting from nicotine patches in smokers and non-smokers (Yun et al, 2008). Benowitz and colleagues have shown that relative to nonsmokers, clearance of nicotine-d 2 , a stable isotope of nicotine, was slower in smokers (Benowitz et al, 2009; Benowitz and Jacob, 1993).…”

Pharmacokinetic Evaluation of Two Nicotine Patches in Smokers

“…Current smokers between 19 and 55 years of age with a body mass index ranging from 19 to 27 kg/m 2 were chosen as the subject population for this bioequivalence study because they are the target population for the NRT product containing the replacement PIB adhesive and because the pharmacodynamics of nicotine delivery by NTSs differ between smokers and nonsmokers . Subjects were eligible for this study if they self‐reported smoking more than 10 cigarettes per day for the 6 months preceding the study.…”

“…All forms of NRT are designed to deliver nicotine to the user to reduce the intensity of nicotine withdrawal symptoms during the quitting process and have been consistently shown to increase abstinence rates among those attempting to quit . NTSs have been shown to be effective in increasing rates of long‐term abstinence in users and have other advantages including over‐the‐counter access, an improved safety profile, sustained drug delivery, and low cost compared with other forms of NRT . Because nicotine can be readily absorbed through the skin, NTSs are designed to mimic the blood nicotine profile of a typical smoker, although at lower levels .…”

“…10 NTSs have been shown to be effective in increasing rates of long-term abstinence in users 10 and have other advantages including over-thecounter access, an improved safety profile, sustained drug delivery, and low cost compared with other forms of NRT. 11,12 Because nicotine can be readily absorbed through the skin, NTSs are designed to mimic the blood nicotine profile of a typical smoker, although at lower levels. 13 The slow release of nicotine in NTSs provides steady-state levels of nicotine without the need to redose throughout the day.…”

Modeling of Physiology Based Toxico-Kinetics and Toxico-Dynamic to Diagnose Acute Effects of Nicotine on Heart Rate

“…Ka ant fu Cven Kel ant Cant dt The parameter used are mentioned by Porchet et al in his paper [20,23,24]. Thus from the above information the modeling is done and the amount of changes in heart rate is determined, based on the value of nicotine dosage given into our body, the amount of nicotine that can be distributed can also be found out.…”