The pharmacokinetics of ropivacaine in hepatic and renal insufficiency

Flip-flop Pharmacokinetics – Delivering a Reversal of Disposition: Challenges and Opportunities During Drug Development

“…It has been observed that some local anesthetics exhibit flip-flop pharmacokinetics following epidural administration, such as ropivacaine [130–132]. For instance, ropivacaine 0.2% was continuously infused (5 ml/h) epidurally for 48 h postoperation in patients scheduled for major abdominal or urologic surgery [130].…”

Liquid chromatography–electrospray mass spectrometry determination of free and total concentrations of ropivacaine in human plasma

“…After EP administration a constant increase in drug concentration occurred during the 48-h infusion period. The absorption rate constant from the site of administration could be lower than the elimination rate constant (0.35 h −1 ) [6]; indicating that absorption is the rate-limiting step in elimination of ropivacaine after EP administration [6]. After a CPCB, plasma concentrations of ropivacaine decreased from 1.5 to 6 h then increased until 48 h (end of infusion) (Fig.…”

“…Other metabolites include 2-hydroxymethyl-ropivacaine and 4-hydroxyropivacaine. After intra-venous administration, an elimination half-life of about 2 h was reported [6]. Ropivacaine is extensively bound to plasma proteins (mainly to ␣ 1 -acid glycoprotein) with a free fraction around 6% [7].…”

Erector spinae plane block for urgent pleuroscopy: a possible change in anesthetic approach for high-risk patients

“…Ropivacaine as a single shot local anesthetic can be considered safe in patients with liver and kidney disease. 8 In patients with chronic end-stage liver disease, peak plasma concentrations of ropivacaine after a single intravenous ropivacaine dose are similar to those in healthy subjects. 8 , 9 Additionally, uremic patients have significantly higher alpha-1-acid glycoprotein plasma concentrations than non-uremic patients, so the peak plasma concentrations of free ropivacaine (related to toxicity) are similar in both groups.…”