Monograph
N01BB58 - Articaine, Combinations |
Propably not porphyrinogenic |
PNP |
Rationale
Limitations: This safety classification applies only to preparations containing a combination of the two drugs articaine and adrenaline (epinephrine). The same ATC-code (N01BB58) can in some countries be used for different combinations of articaine and other drugs which in theory may be porphyrinogenic. Please refer to the classification and monograph of each individual substance. If the combination contains a substance which is not classified (NC) or has been classified as porphyrinogenic (PSP, PRP or P), the safety classification of such a combination as PNP is no longer valid.
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.
Adrenalin (epinephrine): Endogenous catecholamine. Metabolism is Not CYP-dependent . No data pointing to CYP-interaction.
Epinephrine is classified NP.
Chemical description
Articaine hydrochloride is a local anaesthetic of the amide type. Adrenaline is a catecholamine added for longer duration of local anaesthesia.
Therapeutic characteristics
Local anaesthetic. Administration in combination with adrenaline (epinephrine) (not porphyrinogenic) prolongs the effect of articaine, and reduces hepatic exposure and the risk of systemic reactions.
Metabolism and pharmacokinetics
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 approximately 5-10 % of available artecaine, converting the drug almost quantitatively to articainic acid. CYP affinity not reported by Rendic (2002).
Adrenalin (epinephrine) is an endogenous compound. It is very rapidly inactivated by processes which include uptake into adrenergic neurones, diffusion, and enzymatic degradation in the liver and body tissues. Metabolism involves monoamine oxidase (MAO) and catechol-O-methyl transferase (COMT).
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 2 patients with acute porphyria. Also articaine (N01BB08) has been used uneventfully by one patient.
References
# | Citation details | PMID |
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* | Scientific articles | |
1. | Brown, G.J., Welbury, R.R. The management of porphyria in dental practice. British Dental Journal 2002; 193(3):145-6.
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12213008 |
2. | Overman, P.R. Articaine: a new alternative in dental hygiene pain control. J Dent Hyg 2007; 81: 66.
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17908422 |
3. | Rendic, S. Summery of information on human CYP enzymes: human P450 metabolism. Drug metabolism reviews 2002; 34(1&2), 83-448.
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4. | Thunell, Stig, Evidence-based porphyrogenicity assessment of seven local anasthetics (2009, to be published).
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* | Drug reference publications | |
5. | Sweetman SC, editor. Martindale: The complete drug reference. Adrenaline. Pharmaceutical Press 2009.
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6. | Sweetman SC, editor. Martindale: The complete drug reference. Articaine Hydrochloride. Pharmaceutical Press 2009.
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* | Summary of Product Characteristics | |
7. | Norwegian medicines agency. Summary of Product Characteristics (SPC). Septocaine.
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Similar drugs
Tradenames and packages
From some sources, we get a list of packages (United Kingdom, Ireland, Estonia).
Other sources contain more or less "clean" versions of the trade name (Denmark, Finland, Iceland, Lithuania, Norway).
What you see here is the raw data we get from each country, so there will appear to be duplicates. The bold names
are the searchable terms. The gray names that follow are all mapped to the bolded term.
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Netherlands
CITOCARTIN · CITOCARTIN 40/0,005 mg/ml, oplossing voor injectie · CITOCARTIN 40/0,01 mg/ml, oplossing voor injectie · LONCARTI · LONCARTI 40/0,005 mg/ml oplossing voor injectie, oplossing voor injectie · LONCARTI 40/0,01 mg/ml oplossing voor injectie, oplossing voor injectie · Septanest · Septanest SP 40 mg/ml + 10 microgram/ml oplossing voor injectie · Septanest SP 40 mg/ml + 10 microgram/ml, oplossing voor injectie · Septanest N · Septanest N 40 mg/ml + 5 microgram/ml, oplossing voor injectie · Topicainol · Topicainol 40 mg/ml + 5 microgram/ml oplossing voor injectie · Topicainol Forte · Topicainol Forte 40 mg/ml + 10 microgram/ml oplossing voor injectie · Ubistesin · Ubistesin 4% articaine met 1/100 000 adrenaline, oplossing voor injectie · Ubistesin 4% articaine met 1/200 000 adrenaline, oplossing voor injectie · Ultracain · Ultracain D-S forte, injectievloeistof · Ultracain D-S, injectievloeistofBelgium
LONCARTI · LONCARTI 40 mg/ml - 0.005 mg/ml sol. inj. cart. · LONCARTI 40 mg/ml - 0.01 mg/ml sol. inj. cart. · Septanest · Septanest Special 40 mg/ml - 10 µg/ml sol. inj. cart. · Septanest Normal · Septanest Normal 40 mg/ml - 5 µg/ml sol. inj. cart. · Ubistesin Adrenaline · Ubistesin Adrenaline 1-100000 40 mg/ml - 10 µg/ml sol. inj. cart. · Ubistesin Adrenaline 1-200000 40 mg/ml - 5 µg/ml sol. inj. cart.United Kingdom
Anestadent 4% and 1:100,000 · Anestadent 4% and 1:100,000 solution for injection 2.2ml cartridges · Septanest · Septanest 1 in 100,000 solution for injection 2.2ml cartridges · Septanest 1 in 200,000 solution for injection 2.2ml cartridgesDenmark
Dentocaine · Septanest · Septocaine · Sopira CitocartinNorway
Septocaine · Septocaine FortePoland
Citocartin 100 · Citocartin 200 · Dentocaine · Orabloc · Septanest z adrenalina 1:100 000 · Septanest z adrenalina 1:200 000 · Ubistesin · Ubistesin ForteLuxembourg
Loncarti · Septanest · Septanest Special · Septanest Normal · Ubistesin Adrenaline · Ubistesin Adrenaline 1/100000 · Ubistesin Adrenaline 1/200000Finland
Dentocaine · Septocaine · Septocaine Forte · Ubistesin · Ubistesin Forte · Ubistesin MildLatvia
Dentocaine · Septanest · Septanest Forte · Ubistesin · Ubistesin forteSerbia
ARTINIBSA · ARTINIBSA 4% · ORABLOC · ORABLOC® · Septanest adrenaline · Septanest adrenaline 1/100 000
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