PMID: 8600180Dec 1, 1995Paper

A pharmacokinetic and pharmacodynamic study of intravenous pilocarpine in humans

Journal of Dental Research
J M TanzerA K Willard

Abstract

Pilocarpine (P) is of potential utility in the treatment of xerostomia. Because optimal development of P dosage forms for humans requires that its pharmacokinetics and pharmacodynamics be defined, this intravenous study of its disposition and associated salivary responses was performed. In a hospital setting, two healthy female subjects were given a series of graded doses of intravenous P or placebo to stimulate salivary secretion. Plasma levels of P, heart rate, blood pressure, and respiratory rate were simultaneously monitored. Other objective and subjective physiological parameters were assessed. Plasma concentrations of P declined either mono- or bi-exponentially with time, and brisk initial salivation was followed by prolonged salivation at doses > or = 1 mg. At doses between 0.5 and 3.5 mg, dose-independent pharmacokinetic parameters included a small steady-state volume of distribution (2.4 to 3.0 L/kg), a high plasma clearance (0.026 to 0.03 L/kg/min), and a mean residence time of approximately 100 min. The cumulative volume of whole saliva secreted during the first 3 h post-dose was linearly related to the area under the plasma concentration-time curve. Plasma concentrations from 1 to 42 ng/mL were associated with signi...Continue Reading

References

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Citations

Apr 22, 1999·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·C AromdeeJ Wall
Aug 14, 2008·Pharmacogenetics and Genomics·Takuro EndoYasunori Momose
Sep 19, 2008·Expert Opinion on Drug Metabolism & Toxicology·Lawrence Berk
Apr 20, 2004·The Journal of Emergency Medicine·Robert G HendricksonMichael I Greenberg
Jan 1, 2009·The Journal of Medical Investigation : JMI·Bing QiMasataka Murakami
Dec 21, 2006·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Takuro EndoYasunori Momose

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