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Pharmacokinetics of tacrine hydrochloride in Alzheimer's disease

Pharmacokinetics of tacrine hydrochloride in Alzheimer's disease The clinical pharmacokinetics of tacrine hydrochloride have been characterized in patients who have Alzheimer's disease. Serum concentrations of the drug and of its probable metabolite were monitored in eight patients after a 25 mg oral dose, in six patients after a 50 mg oral dose, in four patients after repeated administration of 50 mg, and in two patients after a small intravenous dose. Urinary excretion of drug and metabolite for 24 hours was measured in one of the patients who received a small intravenous dose. The serum half‐life was 1.59 ± 0.15 hours (mean ± SEM) after the 25 mg dose, 2.14 ± 0.24 hours after the 50 mg dose, and 2.91 ± 0.39 hours after continuous treatment. After intravenous administration, clearance was above 600 ml/min in both patients, and oral bioavailability was calculated at below 5%. Urine recovery was less than 3% of the dose. The low bioavailability of tacrine hydrochloride is partly explained by presystemic metabolism. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Clinical Pharmacology & Therapeutics Wiley

Pharmacokinetics of tacrine hydrochloride in Alzheimer's disease

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References (25)

Publisher
Wiley
Copyright
© 1989 American Society for Clinical Pharmacology and Therapeutics
ISSN
0009-9236
eISSN
1532-6535
DOI
10.1038/clpt.1989.199
Publisher site
See Article on Publisher Site

Abstract

The clinical pharmacokinetics of tacrine hydrochloride have been characterized in patients who have Alzheimer's disease. Serum concentrations of the drug and of its probable metabolite were monitored in eight patients after a 25 mg oral dose, in six patients after a 50 mg oral dose, in four patients after repeated administration of 50 mg, and in two patients after a small intravenous dose. Urinary excretion of drug and metabolite for 24 hours was measured in one of the patients who received a small intravenous dose. The serum half‐life was 1.59 ± 0.15 hours (mean ± SEM) after the 25 mg dose, 2.14 ± 0.24 hours after the 50 mg dose, and 2.91 ± 0.39 hours after continuous treatment. After intravenous administration, clearance was above 600 ml/min in both patients, and oral bioavailability was calculated at below 5%. Urine recovery was less than 3% of the dose. The low bioavailability of tacrine hydrochloride is partly explained by presystemic metabolism.

Journal

Clinical Pharmacology & Therapeutics – Wiley

Published: Dec 1, 1989

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