Monograph
N01BB04 - Prilocaine |
Not porphyrinogenic |
NP |
Rationale
Used uneventfully in 105 patients with latent or active acute porphyria. By clinical criteria the local anaesthetic prilocaine is not porphyrinogenic.
Chemical description
Prilocaine hydrochloride is a local anaesthetic of the amide type.
Therapeutic characteristics
Local anaesthetic.
Hepatic exposure
Volume required to reach uM concentrations when injected intravenously: approximately 2 ml (of prilocaine 30 mg/ml).
Metabolism and pharmacokinetics
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).
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 illeffects.
IPNet drug reports
Uneventful use reported in 6 patients with acute porphyria.
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.
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| 2. | 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.
|
718778 |
| 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, S. Evidence-based porphyrogenicity assessment of seven local anasthetics (2009, to be published).
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| 5. | Regional anesthesia as anesthetic technique of choice in acute hepatic porphyria. J Clin Anesth 1992;4(3):259.
Böhrer H, Schmidt H. |
1610588 |
| * | Drug reference publications | |
| 6. | McEvoy GK, editor. Prilocaine Hydrochloride. The AHFS Drug Information 2008. Bethesda, MD: American Society of Health-System Pharmacists; 2009. Electronic version (March 2009).
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| 7. | Sweetman SC, editor. Martindale: The complete drug reference. Prilocaine Hydrochloride. Pharmaceutical Press 2009.
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