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In relation to NO-System, Stable Pentadecapeptide BPC 157 Counteracts Lidocaine-Induced Adverse Effects in Rats and
Marin Lozic1, Vasilije Stambolija1, Ivan Krezic1
1Department of Pharmacology, School of Medicine, Medical Faculty, University of Zagreb, Salata 11, P.O. Box 916, 10000 Zagreb, Croatia.
Emergency Medicine International
|June 23, 2020
Summary
Pentadecapeptide BPC 157 demonstrates significant antidote activity against lidocaine toxicity, counteracting local anesthesia side effects and central nervous system effects. This peptide offers a potential therapeutic agent for managing local anesthetic adverse events.
Area of Science:
- Pharmacology
- Neuroscience
- Toxicology
Background:
- Lidocaine is a widely used local anesthetic with potential cardiotoxicity, arrhythmias, convulsions, and cellular depolarization.
- Pentadecapeptide BPC 157 has shown promise in counteracting various toxic effects.
- The interaction between BPC 157 and the nitric oxide (NO) system in the context of local anesthetic toxicity requires investigation.
Purpose of the Study:
- To investigate the potential of pentadecapeptide BPC 157 as an antidote against lidocaine-induced toxicity.
- To explore the role of the nitric oxide system in mediating the protective effects of BPC 157.
- To evaluate BPC 157's efficacy in counteracting local anesthesia, arrhythmias, convulsions, and cellular depolarization induced by lidocaine.
Main Methods:
- Lidocaine was administered to induce local anesthesia, arrhythmias, and convulsions in animal models.
- Pentadecapeptide BPC 157 was administered via intraplantar, intraperitoneal, and intragastric routes at various time points relative to lidocaine.
- The involvement of the nitric oxide system was assessed using nitric oxide synthase (NOS) blocker L-NAME and NOS substrate L-arginine.
Main Results:
- BPC 157 administration significantly ameliorated lidocaine-induced plantar effects and limb function failure.
- BPC 157 counteracted lidocaine-induced bradycardia and eliminated tonic-clonic convulsions.
- BPC 157 also antagonized lidocaine-induced depolarization of HEK293 cells, with its effects modulated by L-NAME and L-arginine.
Conclusions:
- Pentadecapeptide BPC 157 exhibits significant intrinsic antidote activity against lidocaine and general local anesthetic toxicity.
- The study suggests a complex interaction between BPC 157, the nitric oxide system, and lidocaine's toxic effects.
- BPC 157 represents a promising therapeutic candidate for managing adverse events associated with local anesthetics.
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