N01BB10 - Levobupivacaine |
Propably not porphyrinogenic |
PNP |
Rationale
The drug has not been found to induce or irreversible inhibit drug metabolizing cytochrome P450 species (Rendic, S., 2002) and is therefore most probably devoid of capacity for ALAS1-induction. Further, levobupivacaine is the S(-)-entiomer of the non-porphyrinogenic drug bupivacaine, and this gives theoretical grounds to classify levobupivacaine as probably not porphyrinogenic. One case of uneventful use reported.
Chemical description
Levobupivacaine is a local anesthetic of the amide type, the S(-)-entiomer of bupivacaine.
Therapeutic characteristics
Local anaesthtic. Levobupivacaine is equipotent to bupivacaine.
Hepatic exposure
Volume required to obtain uM concentrations when injected intravenously: approximately 4 ml (of levobupivacaine 5 mg/ml).
Metabolism and pharmakokinetics
The pharmacokinetics of levobupivacaine are similar to those of the racemic form, bupivacaine. It is extensively metabolised and excreted as its metabolites mainly in the urine, with smaller amounts appearing in the faeces. 3-Hydroxylevobupivacaine is a major metabolite and its formation is mediated by the cytochrome P450 isoenzyme CYP1A2; the isoenzyme CYP3A4 is also involved in the metabolism of levobupivacaine. Rendic (2002) reports that levobupivacaine is a substrate of CYP3A4 and CYP1A2. Gennery et al (2000) also concludes that metabolism is primarily via cytochrome P450 isoenzymes.
Personal communication
Thunell, S., study to be published: 1 patient exposed without porphyric adverse reaction reported.
IPNet drug reports
No.
References
- Scientific articles
- Gennery, B., Mather, L.E. et al. Levobupivacaine: New Preclinical and Clinical Data. Seminars in Anesthesia, Perioperative Medicine and Pain 2000;19 (2):132-148. #2515
- 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
- Drug reference publications
- Sweetman SC, editor. Martindale: The complete drug reference. Levobupivacaine. Pharmaceutical Press 2009. #2517
- Summary of Product Characteristics
- Norwegian medicines agency. Summary of Product Characteristics (SPC). Chirocaine #2516
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