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Features of pharmacokinetics of sustained drug preparation of Theopes and Euphylong in elderly with COPD

Abstract

By means of the open randomized study design features of pharmacokinetics and pharmacodynamics of two sustained drug preparations of theophylline (TP) named as Theopec (T) (for double medication per day in 8°° and 20°° p.m.) and Euphylong (E) (for single medication in 20° p. m.) were investigated in 59 elderly patients with COPD (bronchial asthma, chronic obstructive bronchitis). After 9—10 days of treatment, the daily monithoring of TP concentration in blood serum revealed that the TP concentration at the background of both drugs administration was restricted by limits of the therapy during the whole period of medication. In the period from 2°° to 8°° p.m. the TP concentration was significantly greater in the E group than the one in the T group (p<C0.01). The parameter analysis of pharmacokinetics during the steady-state stage revealed that minimal TP concentrations were 6,75±0,46 mkg/ml in the E group and 6,88+0,4 mkg/ml in the T group, and maximal ones were 13,55+0,67 mkg/ml and 12,5+0,79 mkg/ml respectively. The time of the reachment of the maximal concentration 4,13+0,41 hours for the E group and 13,6+0,66 hours for the T one. During the night time, the TP concentration in blood serum after T medication was smaller, on average, on 14,7 % in comparison with the day time.

The parameters revealing the absorbtional velocity and intencity in the night (the average TP concentration in the time interval from 2°° to 6°° p. m. named as C2°° — 6°°, the square under the concentration curve in that time period, and the parameter (Cav) revealing the percent of C2°°—6°° exeed over the averaged daily concentration) were significantly greater in the E group (p<0.01). The T group demonstrated the smaller range of TP concentration fluctuation in blood serum in comparison with the averaged TP concentration. The revealed features of pharmacokinetics are illustrated by dynamics of parameters of the respiratory function in the morning and evening time. The subjects medicated with E performed significantly greater values of the peak expiratory flow in 8°° p.m. in comparison with T. That featuers of E in single dosage makes it more preferable for patients with “sleep” asthma.

About the Authors

V. V. Salikova

Russian Federation


V. E. Nonikov

Russian Federation


Y. B. Belousov

Russian Federation


References

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Review

For citations:


Salikova V.V., Nonikov V.E., Belousov Y.B. Features of pharmacokinetics of sustained drug preparation of Theopes and Euphylong in elderly with COPD. PULMONOLOGIYA. 1993;(1):57-61. (In Russ.)

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ISSN 0869-0189 (Print)
ISSN 2541-9617 (Online)