Clinical pharmacology and the use of articaine for local and regional anaesthesia
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Clinical pharmacology and the use of articaine for local and regional anaesthesia
Best Practice & Research Clinical Anaesthesiology
Volume 19, Issue 2, June 2005, Pages 293-308
Tom B. Vree PhD, Research Scientist, Chemist-pharamacologist and Senior staff member and Mathieu J.M. Gielen MD, PhD, Research and Senior anaesthesiologist and Senior staff member
Institute for Anaesthesia, University Medical Centre St Radboud, P. O. Box 9101, 6500HB Nijmegen, The Netherlands
Available online 28 April 2005.
Quicker onset and shorter elimination time favours (±) articaine as a short-acting local anaesthetic for regional anaesthesia in day-case settings, e.g. arthroscopy (shoulder, knee), hand and foot surgery, and dentistry, because patients treated with articaine will be Îdrug freeÌ more quickly than those who receive other local anaesthetics. Articaine diffuses better through soft tissue and bone than other local anaesthetics. The concentration of articaine in the alveolus of a tooth in the upper jaw after extraction was about 100 times higher than that in systemic circulation. Articaine is metabolised via hydrolysis into articainic acid, 75% of which in turn is excreted as such and 25% in the glucuronidated form by the kidneys.The half-lives of elimination (t?? and t?Ç) of articaine are 0.6 and 2.5 hours, whereas the apparent half-life of the metabolite articainic acid is 2.5 hours. Intrinsic half-lives of articainic acid are: t?? 12 minutes, and t?Ç 64 minutes (1 hour). In dentistry, articaine is the drug of choice in the vast majority of literature. In other regional aesthesia techniques (intravenous regional anaesthesia, epidural, spinal and plexus blocks) there are not enough data to prove that (±) articaine is safer and more effective than the short-acting local anaesthetics lidocaine, (±) prilocaine or (±) mepivacaine.
Keywords: articaine; articainic acid; articainic acid glucuronide; dentistry pharmacokinetics; regional anaesthesia
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