KINETICS OF DISTRIBUTION OF RADIOACTIVE LABELLED MUSCLE RELAXANTS

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Abstract
The urinary elimination and the kinetics of distribution of gallamine were investigated in dogs by intravenous administration of a single trace dose of radioactive (14C) labelled gallamine. Although some aspects of the distribution of gallamine remain to be studied, the data of the present study suggest certain general conclusions of practical interest. Gallamine is eliminated in the urine at a higher rate than other muscle relaxants. The molecule of gallamine is eliminated intact. The duration of the muscle-paralyzing effect of gallamine coincides with a rapid distribution and with a limited urinaryelimination. The role of urinary elimination becomes important during the phase following the muscular paralysis when the drug slowly disappears from plasma and from the extravascular compartment. Gallamine does not cross the blood-cerebrospinal fluid barrier. However, once injected into the subarachnoid space, it can easily diffuse into blood. Arterial hypotension, shock, hypoxia and hypercapnia decrease urinary elimination of gallamine. Diuresis—as per Ringer-lactate infusion —seems to correct the decreased urinary elimination during generalized arterial hypotension. Renal insufficiency, though probably not affecting the clinical response to a single dose of gallamine, might cause prolonged recovery from subsequent maintenance doses.

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