N01BB54 - Prilocaine, Combinations |
Propably not porphyrinogenic |
PNP |
Rationale
Limitations: This safety classification applies only to preparations containing a combination of the two drugs prilocaine and felypressin. The same ATC-code (N01BB54) can in some countries be used for different combinations of prilocaine 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or has been classified as porphyrinogenic (PSP, PRP or P), the safety classification of such a combination as PNP is no longer valid.
Prilocaine: Used uneventfully in 105 patients with latent or active acute porphyria. By clinical criteria the local anaesthetic prilocaine is not porphyrinogenic.
Felypressin: Not metabolised by CYP. Pharmacodynamic or side-effect porphyrogenicity not probable. Felypressin is probably not porphyrinogenic.
Chemical description
Prilocaine hydrochloride is a local anaesthetic of the amide type. Felypressin is a synthetic nonapeptide. It is freely soluble in water.
Therapeutic characteristics
Prilocain is a local anaesthetic. Felypressin is a synthetic vasopressin analogue used as vasoconstrictor. It is added to prolong the effect of prilocaine and to reduce the hepatic exposure and the risk of systemic reactions.
Metabolism and pharmakokinetics
Prilocaine hydrochloride is metabolized principally in the liver. Some metabolism of prilocaine may also occur in the kidneys. Prilocaine is excreted in urine as various metabolites and less than 1% as unchanged drug. Not been found to be an inducer or irreversible inhibitor of drug metabolizing cytochrome P450 species (Rendic, 2002). Felypressin is not metabolised by CYP.
Personal communication
Thunell, S., study to be published: 105 patients exposed without porphyric adverse reaction reported. Andersson: Reports to have frequently used it in infiltrations without ill effects.
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria. Also prilocaine (N01BB04) has been used uneventfully by 6 patients with acute porphyria.
References
- Scientific articles
- 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. #1192
- Parikh, RK, Moore, MR. Effect of certain anaesthetic agents on the activity of rat hepatic delta-aminolaevulinate synthase. Br J Anaesth 1978; 50:1099-1103. PMID 718778. #4376
- Rendic, S. Summery of information on human CYP enzymes: human P450 metabolism. Drug metabolism reviews 2002; 34(1&2), 83-448. #1025
- Thunell, S. Evidence-based porphyrogenicity assessment of seven local anasthetics (2009, to be published). #2497
- Böhrer H, Schmidt H. Regional anesthesia as anesthetic technique of choice in acute hepatic porphyria. J Clin Anesth 1992;4(3):259. PMID 1610588. #2503
- Drug reference publications
- McEvoy GK, editor. Prilocaine Hydrochloride. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (March 2009). #2504
- Sweetman SC, editor. Martindale: The complete drug reference. Felypressin. Pharmaceutical Press 2009. #2520
- Sweetman SC, editor. Martindale: The complete drug reference. Prilocaine Hydrochloride. Pharmaceutical Press 2009. #2505
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