The effect of age on pharmacokinetics of the local anesthetic drug articaine

Institute of Clinical Pharmacology, Faculty of Medicine, Technical University, Dresden, Germany.
Regional Anesthesia and Pain Medicine (Impact Factor: 3.09). 11/1999; 24(6):524-8. DOI: 10.1016/S1098-7339(99)90043-3
Source: PubMed


With increasing age, there are physiologic changes that could affect pharmacokinetics of drugs. More elderly patients are undergoing routine dental procedures for which local anesthesia could be required. The goal of the present study was to evaluate the effect of age on pharmacokinetics of the local anesthetic agent articaine.
The submucosal infiltration anesthesia from two different dosages of 4% articaine without epinephrine was compared in healthy elderly and young volunteers. High performance liquid chromatography has been used to determine concentrations of articaine in serum. Basic pharmacokinetic parameters were calculated according to standard procedures using a two-exponent equation.
The clearance and volume of distribution (Vdss) of articaine after infiltration anesthesia were significantly lower in elderly volunteers compared with young volunteers. The area under the serum concentration-time curve and maximum drug concentration (Cmax) values did not differ significantly with age; however, both parameters tended to be higher in elderly volunteers. No changes in terminal half-life and time to reach maximum serum concentration (t(max)) were observed. The Cmax and tmax values of the metabolite articainic acid were similar in young and elderly volunteers. CONCLUSIONS The results show that the metabolism of articaine is age-independent in healthy male volunteers. The smaller Vdss in the elderly results in a trend to higher serum levels after a given dose of articaine. No change of dosage of articaine in elderly patients should be necessary.

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    • "The magnitude of the reduction of all local anesthetics should be related to the expected influence of the pharmacodynamic or pharmacokinetic change.28 In healthy elderly and young volunteers, it has been shown that the metabolism of articaine is age independent.29 "
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    ABSTRACT: Articaine is an intermediate-potency, short-acting amide local anesthetic with a fast metabolism due to an ester group in its structure. It is effective with local infiltration or peripheral nerve block in dentistry, when administered as a spinal, epidural, ocular, or regional nerve block, or when injected intravenously for regional anesthesia. In comparative trials, its clinical effects were not generally significantly different from those of other short-acting local anesthetics like lidocaine, prilocaine, and chloroprocaine, and there is no conclusive evidence demonstrating above-average neurotoxicity. Articaine proved to be suitable and safe for procedures requiring a short duration of action in which a fast onset of anesthesia is desired, eg, dental procedures and ambulatory spinal anesthesia, in normal and in special populations.
    Local and Regional Anesthesia 06/2012; 5(1):23-33. DOI:10.2147/LRA.S16682
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    • "This is in contrast to other amide local anesthetics, which is primarily metabolized in the liver, which has an capacity that decreases with age. There is an significant decrease in CL and Vdss of articaine in elderly, related to the decrease in lean body mass and increase in body fat (Oertel & al. 1999). "

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