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Clinical Effects in Relation to Plasma Concentration

Torbjörn Tomson, MD; Gunnel Tybring, Engr; Leif Bertilsson, PhD; Karl Ekbom, MD; Anders Rane, MD

Arch Neurol. 1980;37(11):699-703.

Abstract
• Seven patients with trigeminal neuralgia were treated with carbamazepine at three dose levels, each period lasting for six days. A single-blind technique was used, the patients being unaware of the dose changes. During the last three days of each dose treatment, the pain score was determined by the patients and the plasma concentrations of carbamazepine and its epoxide metabolite were measured. There was a correlation between the dose and plasma level of carbamazepine (r =.56; P <.01). At the carbamazepine doses studied (200 to 1,400 mg/day), no indication of saturation kinetics was seen. As the ratio between the plasma levels of the epoxide and carbamazepine was relatively low and constant, it was not possible to evaluate the potency of the epoxide. In six of the patients studied a plasma level-effect relationship was found. The best effect was seen at carbamazepine levels between 24 and 43 µmole/L (5.7 and 10.1 µg/mL). In one patient who was studied twice, the plasma level-response curve was different on the two occasions. Side effects were recorded in two patients, both with carbamazepine plasma levels above 33 µmole/L (7.9 µg/mL).

Author Affiliations
From the Department of Neurology, Södersjukhuset, Stockholm (Drs Tomson and Ekbom); and the Department of Clinical Pharmacology, Huddinge (Sweden) Hospital (Mr Tybring and Drs Bertilsson and Rane).

Footnotes
Accepted for publication Feb 2, 1980.

Read in part before the annual meeting of the Scandinavian Migraine Society, Uppsala, Sweden, Sept 22, 1979.

Reprint requests to Department of Neurology, Södersjukhuset, S-100 64 Stockholm 38, Sweden (Dr Tomson).

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