Acute Porphyria Drug Database

Monograph

N01BB03 - Mepivacaine
Propably not porphyrinogenic
PNP

Rationale
Mepivacaine differs structurally from the bupivacaine only in the in the substitution of a methyl group for the N-butyl group. Sharing the structural metabolic prerequisites of the non-porphyrogenic drug bupivacaine gives theoretical grounds to classify mepivacaine as probably not porphyrinogenic. Uneventful use has been reported in 13 patients.
Chemical description
Mepivacaine hydrochloride is a local anaesthetic of the amide type. Mepivacaine differs structurally from the non-porphyrogenic drug bupivacaine only in the in the substitution of a methyl group for the N-butyl group.
Therapeutic characteristics
Local anaesthetic. Administration in combination with epinephrine (adrenaline) (not porphyrogenic) prolongs the effect of mepivacaine, and reduces hepatic exposure and the risk of systemic reactions.
Hepatic exposure
Unknown.
Metabolism and pharmacokinetics
Mepivacaine is rapidly metabolised in the liver and less than 10% of a dose is reported to be excreted unchanged in the urine. Over 50% of a dose is excreted as metabolites into the bile but these probably undergo enterohepatic circulation as only small amounts appear in the faeces. Several metabolites are also excreted via the kidneys and include glucuronide conjugates of hydroxy compounds and an N-demethylated compound, 2´,6´-pipecoloxylidide. The drug has not been found to be an inducer or irreversible inhibitor of drug metabolizing cytochrome P450 species (Rendic, 2002) and is therefore most probably devoid of capacity for ALAS1-induction. Sharing the structural metabolic prerequisites of bupivacaine, the probability is that this substance will not take part in ALAS1-induction needed for porhyrogenic action.
Personal communication
Thunell, S., study to be published: 11 patients exposed without porphyric adverse reaction reported. Andersson:
Published experience
Uneventful use reported in a case report of one 55 year old AIP woman devoid of clinical symptoms but with elevated PBG levels. Twenty ml of 1% mepivacaine was injected as postoperative pain control following a hip replacement surgery (Hiraki, T., Oishi, K. et al, 2001). Uneventful use in one 32 year old HCP woman who received routine dental local anesthesia consisting of 2% mepivacaine with 1:20,000 levonordefrin. (Moore, A.W.,& Coke,J.M., 2000).

References

# Citation details PMID
*Scientific articles
1. de Verneuil,H., Deybach,J.C. et al. Study of anaesthetic agents for their ability to elicit porphyrin biosynthesis in chick embryo liver. Biochem Pharmacol 1982; 32: 1011-18.
2. Hiraki,T., Oishi,K. et al. [Anesthetic management of a patient with a history of acute intermittent porphyria and an elevation of urinary porphobilinogen]. Masui 2001;50: 882-5.
3. Moore AW 3rd, Coke JM. Acute porphyric disorders.Oral Surg Oral Med Oral Pathol Oral Radiol Endod 2000;90(3):257-62.
4. Rendic, S. Summery of information on human CYP enzymes: human P450 metabolism. Drug metabolism reviews 2002; 34(1&2), 83-448.
5. Thunell, S., Evidence-based porphyrogenicity assessment of seven local anasthetics (2009, to be published).
*Drug reference publications
6. Sweetman SC, editor. Martindale: The complete drug reference. Mepivacaine Hydrochloride. Pharmaceutical Press 2009.
*Summary of Product Characteristics
7. Norwegian medicines agency. Summary of Product Characteristics (SPC). Carbocain Dental.

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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.
Note: The cleaning is done automatically by a proprietary algorithm, and it may produce errors. We strive to improve it continuously.
Netherlands
Imeros · Imeros 3% w/v oplossing voor injectie · MEPICART · MEPICART 30 mg/ml oplossing voor injectie · Mepivacaïne · Mepivacaïne HCl B.Braun 10 mg/ml, oplossing voor injectie · Mepivacaïne HCl B.Braun 20 mg/ml, oplossing voor injectie · Scandonest · Scandonest 3% zonder vasoconstrictor, oplossing voor injectie
Belgium
Mepicart · Mepicart 30 mg/ml sol. inj. cart. · Mepivastesin · Mepivastesin 30 mg/ml sol. inj. amp. · Scandicaine · Scandicaine 1 % sol. inj. p.dural · Scandicaine 2 % sol. inj. p.dural · Scandonest sans Vasoconstricteur · Scandonest sans Vasoconstricteur 3 % sol. inj. cart.
United Kingdom
Scandonest plain · Scandonest plain 3% solution for injection 2.2ml cartridges
Denmark
Carbocain · Mepidental · Mepivacaine · Mepivacaine "Accord" · Scandonest
Norway
Carbocain · Carbocain Dental · Carbocain sandoz · Mecain · Scandonest · Scandonest Plain
Poland
Mepidont 3% · Mepivastesin · Scandivin · Scandonest 30 mg/ml
Luxembourg
MEPICART · SCANDICAINE · SCANDONEST · SCANDONEST 3% SANS VASOCONSTRICTEUR
Iceland
Carbocain · Carbocain Dental
Finland
Mepidental · Scandonest
Latvia
Scandivin · Scandonest
 
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