Evaluation of Ropivacaine and 3-OH-Ropivacaine Pharmacokinetics Following Interpectoral Nerve Block via LC-MS/MS—A Pilot Study

Regional anesthesia techniques such as the ultrasound-guided PECS II (pectoral nerve block) block are increasingly employed to optimize perioperative analgesia while minimizing systemic anesthetic exposure. Ropivacaine is commonly used for its favorable pharmacological profile; however, clinical data on its pharmacokinetics and systemic metabolite behavior following interpectoral administration remain limited. This study aimed to characterize the plasma concentration-time profile of ropivacaine and its main active metabolite, 3-OH-ropivacaine, in patients undergoing interpectoral nerve block, using a validated LC-MS/MS (liquid chromatography coupled with mass spectrometry) method. Venous blood samples were collected from 18 patients at predefined time points (0, 1, 3, 6, and 24 h) following a PECS II block performed with a ropivacaine-lidocaine mixture. Plasma concentrations were quantified via a validated LC-MS/MS protocol in accordance with FDA (Food and Drug Administration) and EMA (European Medicines Agency) guidelines. Pharmacokinetic parameters were derived using non-compartmental analysis. Ropivacaine reached a mean peak plasma concentration (Cmax-maximum concentration) of 167.5 ± 28.3 ng/mL at 1.3 ± 0.2 h (Tmax-maximum time). The metabolite 3-OH-ropivacaine peaked at 124.1 ± 21.4 ng/mL at 2.3 ± 0.3 h. The terminal elimination half-life was 19.4 ± 2.8 h for ropivacaine and 29.2 ± 3.1 h for its metabolite. Plasma levels demonstrated prolonged systemic exposure with predictable pharmacokinetics. The PECS II block using ropivacaine results in sustained systemic levels of both the parent drug and its primary metabolite, supporting its role in prolonged perioperative analgesia. These data provide a pharmacokinetic foundation for personalized regional anesthesia protocols. This strategy facilitates the adaptation of anesthetic protocols to the individual characteristics of each patient, aligning with the principles of personalized medicine, particularly in patients with altered metabolic capacity.

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Publication Details

Journal
International Journal of Molecular Sciences
Published
2025-07-12
DOI
https://doi.org/10.3390/ijms26146696
Citations
3
Primary Topic
Anesthesia and Pain Management
Type
article
Field-Weighted Citation Impact
6.02
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article

Evaluation of Ropivacaine and 3-OH-Ropivacaine Pharmacokinetics Following Interpectoral Nerve Block via LC-MS/MS—A Pilot Study

Laurian Vlase, Camil-Eugen Vari, Mihaela Butiulca, Silvia Imre et al.
3 citations
International Journal of Molecular Sciences
Anesthesia and Pain Management
6.02
article

Evaluation of Ropivacaine and 3-OH-Ropivacaine Pharmacokinetics Following Interpectoral Nerve Block via LC-MS/MS—A Pilot Study

Laurian Vlase, Camil-Eugen Vari, Mihaela Butiulca, Silvia Imre, Lénárd Farczádi, Leonard Azamfirei, Alexandra Lazăr
article en
3 citations

Abstract

Regional anesthesia techniques such as the ultrasound-guided PECS II (pectoral nerve block) block are increasingly employed to optimize perioperative analgesia while minimizing systemic anesthetic exposure. Ropivacaine is commonly used for its favorable pharmacological profile; however, clinical data on its pharmacokinetics and systemic metabolite behavior following interpectoral administration remain limited. This study aimed to characterize the plasma concentration-time profile of ropivacaine and its main active metabolite, 3-OH-ropivacaine, in patients undergoing interpectoral nerve block, using a validated LC-MS/MS (liquid chromatography coupled with mass spectrometry) method. Venous blood samples were collected from 18 patients at predefined time points (0, 1, 3, 6, and 24 h) following a PECS II block performed with a ropivacaine-lidocaine mixture. Plasma concentrations were quantified via a validated LC-MS/MS protocol in accordance with FDA (Food and Drug Administration) and EMA (European Medicines Agency) guidelines. Pharmacokinetic parameters were derived using non-compartmental analysis. Ropivacaine reached a mean peak plasma concentration (Cmax-maximum concentration) of 167.5 ± 28.3 ng/mL at 1.3 ± 0.2 h (Tmax-maximum time). The metabolite 3-OH-ropivacaine peaked at 124.1 ± 21.4 ng/mL at 2.3 ± 0.3 h. The terminal elimination half-life was 19.4 ± 2.8 h for ropivacaine and 29.2 ± 3.1 h for its metabolite. Plasma levels demonstrated prolonged systemic exposure with predictable pharmacokinetics. The PECS II block using ropivacaine results in sustained systemic levels of both the parent drug and its primary metabolite, supporting its role in prolonged perioperative analgesia. These data provide a pharmacokinetic foundation for personalized regional anesthesia protocols. This strategy facilitates the adaptation of anesthetic protocols to the individual characteristics of each patient, aligning with the principles of personalized medicine, particularly in patients with altered metabolic capacity.

International Journal of Molecular SciencesVol. 26(14)
Iuliu Hațieganu University of Medicine and Pharmacy (RO), Universitatea de Medicină, Farmacie, Științe și Tehnologie „George Emil Palade” din Târgu Mureș (RO), Spitalul Clinic Judetean de Urgenta Târgu Mureş (RO)
Openalex Percentile: Top 4%
Anesthesia and Pain Management
6.02
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