Assessment of the relationship between plasma nortriptyline concentration and inhibition of salivation: Single-dose study

I. J. Jang, J. G. Shin, S. G. Shin, J. J. Kim, J. I. Woo, Y. S. Lee, C. W. Park

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)

Abstract

In order to evaluate the relationship between plasma nortriptyline concentration and anticholinergic effect, a single blind cross-over study of nortriptyline was performed. Seventeen healthy male volunteers were given single doses of nortriptyline (25, 50, and 75 mg) and placebo in a cross-over manner. Plasma nortriptyline concentration was measured by high performance liquid chromatography and spontaneous salivation flow was measured. Peak plasma levels of nortriptyline were attained at about 5 hours after drug administration. The corresponding area under the plasma concentration time curve (AUC) from zero-time to 12 hours after the respective dose of 25 mg, 50 mg and 75 mg nortriptyline were 87.1 ± 32.8 ng ml-1·h (n = 7), 231.2 ± 61.3 ng ml-1·h (n = 5) and 293.0 ± 83.9 ng ml-1·h (n = 5), respectively. Saliva flow significantly decreased in all dose groups when compared with placebo. The percentage inhibitions of salivation at each indicated dose were 24.2 ± 12.1% (25 mg), 38.3 ± 13.2% (50 mg) and 51.9 ± 10.3% (75 mg). The inhibition of salivation showed highest correlation with log cumulative plasma levels of nortriptyline. The twelve hour plasma AUC which showed 50% inhibition of salivation was 338.7 ng ml-1·h.

Original languageEnglish
Pages (from-to)249-254
Number of pages6
JournalAsia Pacific Journal of Pharmacology
Volume6
Issue number3
Publication statusPublished - 1991

All Science Journal Classification (ASJC) codes

  • Pharmacology

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