Pharmacokinetics and pharmacodynamic effects of nicotine nasal spray devices on cardiovascular and pulmonary function

J Investig Med. 2000 Nov;48(6):435-40.

Abstract

Background: A nasal spray form of nicotine replacement therapy (Nicotrol NS, McNeil Consumer Products Co, Fort Washington, Pa) has been approved and, because of its rapid absorption across the nasal mucosa, may be more effective than nicotine gum or transdermal patches. We tested the hypothesis that the nicotine absorbed into the nasal mucosa would produce significant changes in hemodynamics and pulmonary function in 20 healthy, nonsmoking men and women.

Methods: In this double-blind, randomized study of Nicotrol NS versus placebo, we measured serum nicotine concentrations, blood pressure, heart rate, and indices of pulmonary function at timed intervals before and after nasal spray administration of 3 mg of nicotine.

Results: A peak serum nicotine concentration of 4.71 +/- 3.16 ng/mL occurred 10 minutes after drug administration. The maximum change in systolic blood pressure occurred 5 minutes after dosing and was significantly related to nicotine administration (7.1 +/- 9.4% for the nicotine group vs -1.6 +/- 7.3% for the placebo; P = 0.03). In contrast, neither diastolic blood pressure (P = 0.8) nor heart rate (P = 0.07) changed significantly after nicotine administration, when compared with placebo. Pulmonary function was not altered acutely by a single inhalation of nicotine. Pharmacokinetic modeling revealed a classic one-compartment model in which nicotine is absorbed into the systemic circulation by a zero-order process and eliminated by a first-order process.

Conclusions: In this population of nonsmokers, hemodynamic effects of the nicotine nasal spray were observed shortly after administration and before the peak serum nicotine concentration.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Administration, Intranasal
  • Adult
  • Blood Pressure / drug effects*
  • Double-Blind Method
  • Female
  • Heart Rate / drug effects*
  • Humans
  • Lung / drug effects*
  • Lung / physiology
  • Male
  • Nicotine / administration & dosage*
  • Nicotine / pharmacokinetics
  • Nicotine / pharmacology

Substances

  • Nicotine