PHARMACOKINETICS OF I.M. GLYCOPYRRONIUM

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Abstract
A sensitive radioreceptor assay was used to determine the pharmacokinetics of glyco-pyrronium following a single i.m. injection of 8 ug kg−1 in nine surgical patients. Rapid absorption was found, with a mean peak plasma concentration after 16.1 min and mean elimination half-life of 75.4 min. Almost half (49.3%) of the drug was excreted in pharmacologically active form in the urine within 3 h. A significant increase in heart rate (P < 0.05) occurred in 15 min, lasting up to 60 min, and an antisialagogue effect in 10 min, lasting up to 8 h (P < 0.05). There was no measurable glycopyrronium in lumbar cerebrospinal fluid samples (n = 9) taken 40 min after administration of drug.