Where is articaine metabolized

In following the European Unions report stating there was no scientific evidence of an increased risk of paresthesia from articaine, use of the drug increased. Articaine sales red line and adverse event reports blue bars in Denmark, , reference Paresthesia Following Non-Surgical Dental Treatment Surgery, especially 3rd molar extraction and placement of mandibular implants, is the primary cause of paresthesia following dental treatment.

Given that most dental treatment is non-surgical e. Table 6 shows lingual nerve involvement in four published articles. There are no reported cases of paresthesia following the non-dental use of articaine.

Is it possible for a drug to be so specifically neurotoxic that it only damages nerves with the oral cavity, specifically in the mandible and more specifically the lingual nerve? The Lingual Nerve The lingual nerve appears to be involved in reports of dentally-related paresthesia a disproportionate percentage of cases. Pogrel has studied paresthesia, with publications dating to the early s. The mechanisms are unknown and there is no known prevention or treatment.

Why is it that the lingual nerve is primarily involved in cases of paresthesia? The resulting injury is more likely than not to be a result of mechanical trauma to the lingual nerve from the metal needle. IANB is damaged, only a small portion of the sensory distribution would be affected. When a nerve with 1 to 3 fascicles e.

Fascicles within a nerve. If paresthesia involves the distribution of the IAN e. Local Anesthetics are Neurotoxins All local anesthetics are neurotoxic. If all local anesthetics were equally neurotoxic than the percentage of reported cases of paresthesia for the drug should be equal to its market share.

The resulting fraction ideally should be 1. Table 9. TABLE 9. Market share and observed incidence of paraesthesia. In a clinical study, human neuroblastoma cells were exposed to varying concentrations of articaine, lidocaine and prilocaine to determine neurotoxicity at six different drug concentrations.

In-vitro studies are accurate, sensitive and reproducible because they are conducted in a controlled environment. However, in-vitro studies do not take into account other factors such as 1 local pharmacokinetics concentration in tissues, local diffusion, absorption ; 2 potential influence of other drugs on local pharmacokinetics e.

So, What Should You Do? Doctors must always consider the benefit to be gained from use of a procedure or drug versus the risk involved in the procedure or drug. Only when, in the opinion of the treating doctor, the benefit to the patient to be gained clearly outweighs the risk should the procedure be done or the drug administered. All reports claiming an increased risk of paresthesia with articaine are anecdotal. There is no scientific evidence demonstrating an increased risk of paresthesia following the administration of articaine compared with other local anesthetics.

Stanley Malamed is a dentist anesthesiologist and emeritus professor of dentistry at the Herman Ostrow School of Dentistry of U. C, in Los Angeles, California. Editors Note : Oral Health welcomes this original article from the well-respected Dr. Stanley Malamed on articaine. In his review, Dr. Malamed discusses articaine and paraesthesias. In the interest of presenting topics in a balanced way, and acknowledging Dr.

Dan Haas and Dr. Haas and Hillerup are two of the more notable additional authors on the incidence of paraesthesias and some associated factors. Also at issue in this article is the use of articaine in pregnant women. The reason given is the shorter fetal exposure time to articaine because of its faster metabolism. What is not clear is why exposing a fetus to a potentially more harmful drug, even for a shorter time is advantageous. As always, how you choose to treat your patients is ultimately your decision.

At Oral Health, we would like these decisions to be based on the best information available. We hope that you enjoyed Dr. References : 1. The surgeons Halsted and Hall, cocaine and the discovery of dental anaesthesia by nerve blocking.

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Ein neues Lokalanasthetikum Carticain aus der Thiophenreihe [A new local anaesthetic carticaine in the thiophene series]. Prakt Anaesth 9 3 , Ultracaine en dentisterie operatoire conventionnelle. J Can Dent As soc. Dental local anesthetic market share, United States, Calendar year—, 23 April Septodont Inc.

Lancaster, PA. Aust Dent J. Clinical pharmacology and the use of articaine for local and regional anaesthesia. Best Pract Res Clin Anaesthesiol. J Amer Dent Assoc 5 , J Amer Dent Assoc, 2 , Malamed SF, Gagnon S, Leblanc D: Articaine hydrochloride in pediatric dentistry: safety and efficacy of a new amide-type local anesthetic. Pediatr Dent 22 4 , Local anesthesia: advances in agents and techniques.

Dent Clin N Amer , Rupieper N; Stocker L. Haemiglobinspiegel unter Lokalanaesthesie mit Bupivacain, Carticain und Etidocain. Ultracaine DS Forte ,, Drug package insert. Compendium 34 Spec issue 1 , The anesthetic efficacy of articaine in buccal infiltration of mandibular posterior teeth. J Am Dent Assoc , Pulpal anaesthesia for mandibular central incisor teeth: a comparison of infiltration and intraligamentary injections. Int Endod J , Articaine buccal infiltration enhances the effectiveness of lidocaine inferior alveolar nerve block.

Accessed 17 September Malamed SF. Systemic complications, in Handbook of Local Anesthesia, 6th ed. Louis, pages Hawkins JM. Local anesthetic maximum doses. Adapted from various sources, Toronto, ON, Canada. Haas DA, Lennon D : A 21 year retrospective study of reports of paresthesia following local anesthetic administration , J Can Dent Assoc — , — , — , Hillerup S, Jensen R. Nerve injury caused by mandibular block analgesia. Int J Oral Maxillofac Surg. Occurrence of paresthesia after dental local anesthetic administration in the United States.

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Oral and Dental Expert Group. Therapeutic guidelines: oral and dental , Version 2, Australian Dental Association, Melbourne, page Paresthesia definition. Available at: www. Accessed 16 September Haas DA. Articaine and paresthesia: epidemiological studies.

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Permanent nerve damage from inferior alveolar nerve blocks — an update to include articaine. J Calif Dent Assoc 36 4 , Permanent nerve damage from inferior alveolar nerve blocks: a current update.

J Calif Dent Assoc 40 10 , McDowell AJ. Effective practical steps to avoid complications in face-lifting. Review of consecutive cases. Plast Reconstr Surg. Lagarde P. Paresthesies du territoire mentonnier, secondaires a un traitement endodontique. Inf Dent. Zur Problematik von Sensibilitatsstorungen nach Leitungsanasthesie im Unterkiefer.

Dtsch Zahnarztl Z. Nickel AA Jr. A retrospective study of paresthesia of the dental alveolar nerves. Anesth Prog. Stenver DI, Case number: , Adverse effects from anaesthetics used in relation with dental care with a special focus on anaesthetics containing articaine. Pharmacovigilance Working Party of the European Union. Occurrence of paresthesia aftert dental local anesthetic administration in the United States. J Am Dent Assoc 7 , Revised 9 January Weber JCP. Epidemiology of adverse reactions to nonsteroidal antiinflammatory drugs.

Advances in Inflammation Research. New York, Raven Press, , pages Replication of the Weber effect using postmarketing adverse event reports voluntarily submitted to the United States Food and Drug Administration. Alling CC 3rd. Dysesthesia of the lingual and inferior alveolar nerves following third molar surgery. J Oral Maxillofac Surg. Ellies LG. Altered sensation following mandibular implant surgery: a retrospective study.

J Prosthet Dent. Snoeck M. Articaine: a review of its use for local and regional anesthesia. Local Regional Anesth , Pogrel MA, Thamby S. The elimination half-time of articaine is about 20 minutes. The rapid breakdown of articaine to the inactive metabolite articainic acid is related to a very low systemic toxicity and consequently to the possibility of repeated injections.

Equal analgesic efficacy along with lower systemic toxicity i. Articaine is better able to diffuse 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 times higher than that in systemic circulation. It has been concluded that an unintentional intravascular injection of articaine 80 mg does not cause toxic effects in healthy individuals.