The Effect of Age on Pharmacokinetics of the Local Anesthetic Drug Articaine

Oertel, Reinhard; Ebert, Ulrike; Rahn, R; Kirch, Wilhelm

doi:10.1097/00115550-199924060-00009

Cited by 29 publications

(11 citation statements)

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“…Age has been demonstrated to be a significant covariate on the clearance and volume of distribution of articaine, another anesthetic used in dental procedures. Subjects aged 59 to 68 years experienced decreased clearance and volume with a resulting increase in systemic articaine exposure compared to those subjects between the ages of 20 and 37 years. Age was not shown to be a significant influence on oxymetazoline or PBBA disposition in our study populations.…”

Section: Discussionmentioning

confidence: 91%

Population Pharmacokinetics of an Intranasally Administered Combination of Oxymetazoline and Tetracaine in Healthy Volunteers

Cacek

Gobburu

Gopalakrishnan

2016

The Journal of Clinical Pharmacology

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The primary objective of the current investigation was to establish the pharmacokinetic characteristics of oxymetazoline and tetracaine's primary metabolite, para-butylaminobenzoic acid (PBBA), after the intranasal administration of oxymetazoline/tetracaine. Thirty-six subjects contributing a total of 1791 plasma concentration results from 2 open-label trials were utilized. Model development was achieved using data from the second trial (N = 24) in which 0.3 mg oxymetazoline/18 mg tetracaine was administered. External model validation utilized data from the first trial (N = 12), which included doses of 0.3 mg oxymetazoline/18 mg tetracaine and 0.6 mg oxymetazoline/36 mg tetracaine. Oxymetazoline and PBBA dispositions were described by a 2-compartment model with first-order absorption. An allometric model for body weight was included on volumes and clearances to describe unexplained between-subject variability. The final oxymetazoline parameter estimates were k 4.41 h ; peripheral volume 418 L; clearance 66.4 L/h; central volume 6.97 L; and intercompartmental clearance 419 L/h for a 70-kg subject. The final PBBA parameter estimates were k 8.51 h ; peripheral volume 32.0 L; clearance 16.7 L/h; central volume 29.8 L; and intercompartmental clearance 2.43 L/h for a 70-kg subject. Between-subject variability ranged from 14% to 39% for oxymetazoline and from 10% to 94% for PBBA.

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Section: Discussionmentioning

confidence: 91%

Population Pharmacokinetics of an Intranasally Administered Combination of Oxymetazoline and Tetracaine in Healthy Volunteers

Cacek

Gobburu

Gopalakrishnan

2016

The Journal of Clinical Pharmacology

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“…Due to ester group, articaine is rapidly hydrolyzed by the action of pseudocholinesterase in blood, unlike amide type anesthetics that are mainly metabolized by the liver microsomes. Therefore, plasma elimination half-life of articaine is about 20 minutes, whereas elimination half-life of other amide-type local anesthetic is about 100 minutes 2 . Because its main metabolite (articainic acid) is inactive, articaine has low central nervous system toxicity 2 .…”

Section: Articainementioning

confidence: 99%

“…Therefore, plasma elimination half-life of articaine is about 20 minutes, whereas elimination half-life of other amide-type local anesthetic is about 100 minutes 2 . Because its main metabolite (articainic acid) is inactive, articaine has low central nervous system toxicity 2 . In dentistry, a 4% articaine solution with 1:200000 epinephrine is widely used for infiltration and conduction anesthesia.…”

Section: Articainementioning

confidence: 99%

“…These methods include liquidliquid extraction (LLE) of the sample with t-butyl-ethyl ether 8 , diethyl ether 9 , cyclohexane 14 , and solid-phase extraction (SPE) with polystyrenedivinylbenzene copolymer (SDB-RPS) 1 , SDB-XC 10 and extrelut 6 . In most of the works, the sample was directly introduced in LC column after the precipitation with perchloric acid 2,3,15 . The blocking of pseudocholinesterase activity was achieved with neostigmine 6 or echothiophate 15,16 , while in some works this activity was not blocked [9][10][11][12][13] .…”

Section: Articainementioning

confidence: 99%

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Determination of Articaine in Human Blood by Gas and Liquid Chromatography and its Application in a Preliminary Pharmacokinetic Study

Manda

Popescu

Baniceru

2015

IJDDT

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Two simple, sensitive and specific gas and liquid chromatographic methods are developed and validated for quantification of articaine in human whole blood. Liquid-liquid extraction with n-hexane-isoamyl alcohol 90:10 (v/v) is used for sample preparation in both methods. GC-FID (gas chromatographic-flame ionization detection) analysis is performed with a gas chromatograph equipped with a split-splitless injector, flame-ionization detector and HP INNOwax capillary column. Reverse phase LC-PDA (liquid chromatographic-photo diode array detection) analysis is carried out using a C18 Hypersil GOLD column with two mobile phases: acetonitrile-water 10 mM ammonium acetate 50:50 (v/v), pH 7, and acetonitrile-buffer solution sodium acetate 10 mM and acetic acid 10 mM 50:50 (v/v), pH 4.7, respectively. A comparison between GC-FID and LC-PDA is performed, as well as between internal and external standard as quantification methods in LC. The best results in terms of accuracy (as recovery) and precision (as relative standard deviation) are obtained in GC (95-98% and 5.5-8.2%, respectively) with lidocaine internal standard and in LC (96-102% and 4.2-6.1%, respectively) with external standard and mobile phase pH 4.7. This method is applied in a preliminary pharmacokinetic study to three healthy volunteers to whom anesthesia with articaine is performed.

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“…Classificada como uma amida, sua cadeia intermediária tem um nitrogênio que forma ligação com um ácido carboxílico e apresenta um derivado tiofeno lhe conferindo propriedades como uma anestesia mais profunda com início de ação mais rápido e com uma duração de ação mais longa com maior potência anestésica e menor potencial alergênico (WINTHER; PATIRUPANUSARA, 1974;OERTEL;KIRCH, 1997;LEUSCHNER;LEBLANC, 1999;ISEN, 2000;HAWKINS;MOORE, 2002;MALAMED, GAGNON, LEBLANC, 2001;YAGIELA, 2004;VREE;GIELEN, 2005). O anel tiofênico garante à molécula maior solubilidade em lipídeos e, portanto, maior facilidade para cruzar barreiras lipídicas como, por exemplo, a membrana neuronal (OGLE; MAHJOUBI, 2011).…”

Section: Revisão De Literaturaunclassified

Análise comparativa entre articaína 2% e articaína 4%, ambas com adrenalina 1:200.000: avaliação da eficácia anestésica, sangramento intraoperatório e parâmetros hemodinâmicos em exodontias de terceiros molares inferiores

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The Effect of Age on Pharmacokinetics of the Local Anesthetic Drug Articaine

Cited by 29 publications

References 0 publications

Population Pharmacokinetics of an Intranasally Administered Combination of Oxymetazoline and Tetracaine in Healthy Volunteers

Population Pharmacokinetics of an Intranasally Administered Combination of Oxymetazoline and Tetracaine in Healthy Volunteers

Determination of Articaine in Human Blood by Gas and Liquid Chromatography and its Application in a Preliminary Pharmacokinetic Study

Análise comparativa entre articaína 2% e articaína 4%, ambas com adrenalina 1:200.000: avaliação da eficácia anestésica, sangramento intraoperatório e parâmetros hemodinâmicos em exodontias de terceiros molares inferiores

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