14C-Lidocaine Disposition in Serum and Tissues of Normal and Liver Diseased Rats

Saranteas, Theodosios; Mourouzis, Constantinos; Anagnostopoulou, Sophia; Danis, Kostas; Tachmintzis, Annete; Rallis, George

doi:10.1016/j.joms.2005.11.042

« Previous Next »Journal of Oral and Maxillofacial Surgery
Volume 64, Issue 6 , Pages 892-895, June 2006

¹⁴C-Lidocaine Disposition in Serum and Tissues of Normal and Liver Diseased Rats

Theodosios Saranteas, MD, DDS, PhD
- Senior Research Fellow, Department of Pharmacology, Medical School, University of Athens, Athens, Greece; and Senior Resident, Department of Anesthesiology, General Hospital of Athens “G. Gennimatas,” Athens, Greece
- Address correspondence and reprint requests to Dr Saranteas: 19 Karatza str and Klemanso 18534 Piraeus, Athens, Greece
Constantinos Mourouzis, MD, DDS, PhD
- Oral and Maxillofacial Surgeon and Senior Research Fellow, Division of Oral Pharmacology and Therapeutics, Department of Pharmacology, Medical School, University of Athens, Athens, Greece
Sophia Anagnostopoulou, MD, DDS, PhD
- Associate Professor, Department of Human Anatomy, Medical School, University of Athens, Athens, Greece
Kostas Danis, MD, DDS, MSc
- Regional Epidemiologist, Department of Epidemiology, Health Protection Agency East Midlands, Nottingham City Hospital, Nottingham, UK
Annete Tachmintzis, MD
- Consultant, Department of Anesthesiology, General Hospital of Athens “G. Gennimatas,” Athens, Greece
George Rallis, MD, DDS, PhD
- Senior Hospital Specialist of the Department of Oral & Maxillofacial Surgery, General Hospital of Attica “KAT,” Athens, Greece

Purpose

This study was designed to investigate the disposition of ¹⁴C-lidocaine in serum and tissues in rats with liver dysfunction.

Materials and Methods

Eighteen male rats were randomly divided into 2 groups. Group A was considered as control while group B underwent liver damage by administrating CCl₄ 0.4 mg/kg twice a week for 6 weeks. Both groups received 5 doses of 2.5 mg/kg lidocaine mixture (labeled ¹⁴C-lidocaine and nonlabeled). The rats were killed 2 hours after the last dose. Total lidocaine levels (¹⁴C-lidocaine and ¹⁴C-lidocaine metabolite concentrations) as well as the percent of total lidocaine-bound fractions in tissues were measured.

Results

¹⁴C-lidocaine concentrations were significantly increased in the serum (9.4 ± 0.4 μg/mL), heart (7.8 ± 2 μg/gL), and mandible (0.97 ± 0.01μg/g) in diseased rats as compared with normal rats (serum, 5.3 ± 1.7 μg/mL; heart, 4.2 ± 0.9 μg/g; mandible, 0.68 ± 0.02 μg/g, respectively). ¹⁴C-lidocaine bound fractions in the mandible and heart did not show any significant differences between the 2 groups. Instead, ¹⁴C-lidocaine bound fractions in serum were significantly reduced in diseased animals as opposed to normal ones.

Conclusion

We concluded that liver dysfunction can modify ¹⁴C-lidocaine concentrations in the serum and tissues without altering the lidocaine binding properties in the mandible and heart.