Pharmacokinetic profile of epidurally injected bupivacaine in awake patients

R H Taverne1, T I Ionescu, A V Dijk

  • 1Department of Anaesthesiology, Hospital GOOI-NOORD, Blaricum, The Netherlands.

In order to investigate the influence of general anaesthesia on the pharmacokinetics of bupivacaine 0.5% after a single, epidurally injected dose of 20ml (= 100mg), 5 patients, scheduled for surgical procedures appropriate for epidural anaesthesia without the need for combination with general anaesthesia, were studied. In all patients an arterial, central venous and intrathecal catheter were inserted for sampling of, respectively, arterial and central venous blood and cerebrospinal fluid (CSF), at regular intervals up to 12 hours after administration. Bupivacaine was analysed by gas chromatography. The drug appeared after 2 minutes in the plasma and CSF samples, and was still detectable after 12 hours. There were no significant differences between the bupivacaine concentrations in the arterial and central venous plasma samples at all times. The same applied for the calculated plasma pharmacokinetic parameters at all intervals. The bupivacaine concentrations in the CSF were many dozen times higher than in the plasma samples at all times. There was no clear evidence of a pulmonary retention of bupivacaine in this study. From a pharmacokinetic point of view the epidural anaesthesia was largely spinal anaesthesia.

Related Concept Videos

Local Anesthetics: Clinical Application as Epidural Anesthesia01:29

Local Anesthetics: Clinical Application as Epidural Anesthesia

Epidural anesthetics are administered in the fat-filled epidural space, the outermost part of the spinal canal. This technique is commonly employed for pain management and anesthesia during lower abdomen and pelvis surgeries or labor and delivery.
Since epidural anesthetics can be infused through an epidural catheter, all types of drugs, including short-acting ones, can be administered. Chloroprocaine and lidocaine are examples of short and long-duration anesthetics, respectively. Bupivacaine...
Local Anesthetics: Clinical Application as Spinal Anesthesia01:11

Local Anesthetics: Clinical Application as Spinal Anesthesia

Spinal anesthetics are given during lower abdomen and limb surgeries to block sensory and motor neurons. They are administered in the mid to low lumbar regions, primarily acting on the cauda equina's nerve roots. The blockade level depends on the local anesthetic (LA) concentration. Usually, low LA concentrations are sufficient to block sensory fibers, while only high LA concentrations block motor fibers. Other factors like injection volume and speed, the patient's posture, and the drug...
Local Anesthetics: Pharmacokinetics01:13

Local Anesthetics: Pharmacokinetics

The potency and duration of action of local anesthetics (LAs) are determined by their pharmacokinetics. Pharmacokinetics describes how LAs are absorbed, distributed, metabolized, and eliminated from the body. When administered to the vascular tissues, LAs are quickly absorbed and enter the systemic circulation, reducing their localized effects. Adding vasoconstrictors such as epinephrine to LAs reduces their absorption into the systemic circulation, making them clinically effective. The...
Parenteral Anesthetics: Overview01:24

Parenteral Anesthetics: Overview

Intravenous anesthetics are drugs administered parenterally to induce anesthesia or sedation. Propofol is a widely used agent formulated as a 1% emulsion in soybean oil, glycerol, and egg phosphatide. It induces rapid anesthesia primarily due to its rapid distribution from the bloodstream to target tissues and is metabolized in the liver. However, it can cause significant pain on injection and hypertriglyceridemia. Fospropofol, a water-based prodrug of propofol, lacks these adverse effects.
Depolarizing Blockers: Pharmocokinetics01:19

Depolarizing Blockers: Pharmocokinetics

Depolarizing blockers are administered through intravenous injection. Succinylcholine is the most common choice of depolarizing blockers in emergency clinical practices. Although they have a rapid onset, they readily diffuse away from the motor end plate into the extracellular fluid. They are metabolized by enzymes such as liver butyrylcholinesterase and plasma pseudocholinesterases. This produces a short duration of action, typically 5-10 minutes long, unlike nondepolarizing blockers, which...
Local Anesthetics: Clinical Application as Intravenous Regional Anesthesia01:16

Local Anesthetics: Clinical Application as Intravenous Regional Anesthesia

Intravenous regional anesthesia or the Bier block technique is used to anesthetize a specific limb or extremity. It uses exsanguinated or blood-drained vessels to transport local anesthetics or LAs to the peripheral nerve trunks. Lidocaine without vasoconstrictors like epinephrine is most commonly used for this technique. Other drugs used are prilocaine, ropivacaine, and chloroprocaine. Bupivacaine is not recommended for this technique due to its high cardiac toxicity.
One of the advantages of...