N01BB08 - Articaine |
Propably not porphyrinogenic |
PNP |
Rationale
As articaine is primarily metabolized by plasma esterases, and CYP affinity has not been reported (Rendic 2002), articaine can therefore on theoretical grounds be classified as probably not porphyrinogenic. Two cases of uneventful use reported.
Chemical description
Articaine hydrochloride is a local anaesthetic of the amide type.
Therapeutic characteristics
Local anaesthetic. Often administered in combination with epinephrine (adrenaline) (not porphyrogenic) which prolongs the effect of articaine, and reduces hepatic exposure and the risk of systemic reactions.
Hepatic exposure
Unknown.
Metabolism and pharmakokinetics
Articaine, with its ester side chain, is hydrolyzed primarily by plasma esterases (Overman,P.R. 2007). Articaine hydrochloride is quickly metabolized by carboxyesterase to its primary metabolite articainic acid. In-vitro studies show that P450 isoenzymes found in the human hepatocytes microsomes metabolize approxemately 5-10 % of available artecaine, converting the drug almost quantitatively to articainic acid. CYP affinity not reported by Rendic (2002).
Personal communication
Thunell, S., study to be published: 2 AIP carriers reported uneventful use. Dentist reported uneventful use of articaine (Septocain®) in AIP patients.
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.
References
- Scientific articles
- Brown, G.J., Welbury, R.R. The management of porphyria in dental practice. British Dental Journal 2002; 193(3):145-6. PMID 12213008. #4645
- Overman, P.R. Articaine: a new alternative in dental hygiene pain control. J Dent Hyg 2007; 81: 66. PMID 17908422. #4646
- Rendic, S. Summery of information on human CYP enzymes: human P450 metabolism. Drug metabolism reviews 2002; 34(1&2), 83-448. #1025
- Thunell, Stig, Evidence-based porphyrogenicity assessment of seven local anasthetics (2009, to be published). #2510
- Drug reference publications
- Sweetman SC, editor. Martindale: The complete drug reference. Articaine Hydrochloride. Pharmaceutical Press 2009. #2509
- Summary of Product Characteristics
- Norwegian medicines agency. Summary of Product Characteristics (SPC). Septocaine. #2507
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