Epidural and spinal analgesia
Pamela E Macintyre, Suellen M Walker, David J Rowbotham in Clinical Pain Management, 2008
Almost every LA agent can be administered neuraxially. The first LA drugs to be used on a larger scale in the 1980s were of the ester type, such as procaine and tetracaine. These were then replaced by amino-amides (for example, lidocaine, bupivacaine) with an improved safety profile. When it was found that bupivacaine was associated with cardiac arrest and life-threatening arrhythmias, levobupivacaine and ropivacaine were introduced. These are S-enantiomers with similar anesthetic efficacy and reduced toxicity when compared to the racemic mixture.9 While levobupivacaine is less cardiotoxic, ropivacaine also appears to cause less motor blockade. A meta-analysis of neuraxial ropivacaine in obstetric analgesia suggests clinical advantages, notably a differential block with improved motor function, 10 but the clinical relevance of this aspect continues to be debated.
Local Anesthetics
Sahab Uddin, Rashid Mamunur in Advances in Neuropharmacology, 2020
Ropivacaine is marketed as an injectable solution for perineural and epidural administration for the treatment of acute pain and for anesthesia in surgery (i.e., peripheral nerve and ocular block; epidural administration for abdominal surgery, cesarean section and lower limb surgery, and intrathecal administration for orthopedics and urological surgeries). Ropivacaine has pharmacokinetic properties very similar to those of levobupivacaine: high binding to plasma proteins, hepatic drug metabolism with CYP1A2 and CYP3A4 isoenzymes involvement giving rise to the metabolites 3′-hydroxy-ropivacaine and 2′,6′-pipecoloxylidide, and primary renal excretion in form of these metabolites (Leone et al., 2008; Li et al., 2014; Sisk, 1992).
Intrathecal Pumps
Mark V. Boswell, B. Eliot Cole in Weiner's Pain Management, 2005
Local anesthetics are often added to opioids in patients experiencing burning or lancinating pain. The drug with the most experience in clinical use is bupivacaine. Clinical experience shows the drug is safe and shows efficacy when compared with opioid alone. The drug is most commonly used at doses of 1 to 20 mg per day (Deer et al., 2002).20 Work in the laboratory shows that bupivacaine is stable, compatible, and safe when administered via an implantable delivery system.21 Tetracaine has shown signs of neurotoxicity and has been discouraged for clinical use. Ropivacaine has now been used clinically, but data on this drug are limited and its use should be approached cautiously.22
The role of DRP1 in ropivacaine-induced mitochondrial dysfunction and neurotoxicity
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2019
Yan Chen, Lili Yan, Yan Zhang, Xianhui Yang
Although they are widely used and benefit the majority of patients, LAs have been reported to cause neurotoxicity and cardiac toxicity [5,6]. These studies demonstrate that commonly used LAs including bupivacaine and ropivacaine could induce apoptosis in neuronal cells and have similar cytotoxicity in clinically used concentrations [7,8]. Both bupivacaine and ropivacaine are long-acting amide LAs. Administration of bupivacaine has been shown to induce neurological damage in a preclinical experimental rodent study [9,10]. Ropivacaine was developed after bupivacaine was noted to be associated with cardiac toxicity [11]. Ropivacaine, a drug that can penetrate the blood–brain barrier is used routinely and effectively [12]. However, many such drugs are known to activate neurotoxic pathways.
Comparative study of analgesic effect of epidural ketamine vs. epidural tramadol in patients undergoing mastectomy under thoracic epidural anesthesia
Published in Egyptian Journal of Anaesthesia, 2022
Mohammed A Raheem, Fawzy Abbas Badawy, Hitham MA. Elsayed
Baraka et al. [3] found that administration of 100 mg of ET resulted in a more decrease in VAS score in all times of scoring than our results. The difference can be due to the use of a larger dose of tramadol in their study compared with our study (1 mg/kg) and due to the different times of injection, as they gave ET at skin closure. In contrast, we gave epidural tramadol before the start of surgery. In other studies, Siddik et al. [32] compared two doses of tramadol dose (100 and 200 mg) with the control group who received no tramadol. They found that prolonged duration of analgesia was dose-dependent with tramadol but with a higher incidence of side effects especially vomiting. Also, a study done by Singh et al. [33], who compared two doses of thoracic ET, 1 and 2 mg/kg, added to ropivacaine 0.2% for providing analgesia after upper abdominal surgeries under general anesthesia found that lowering the VAS score and prolonged analgesia duration with the dose 2 mg/kg but associated with more side effects (nausea and vomiting).
Safety of epidural drugs: a narrative review
Published in Expert Opinion on Drug Safety, 2019
ML van Zuylen, W ten Hoope, EME Bos, J Hermanides, MF Stevens, MW Hollmann
At equipotent dosing, all LA have similar toxic properties, however systemic LA toxicity after epidural injection is rare [16]. It has been suggested that ropivacaine has a superior safety profile compared to racemic bupivacaine. When given systemically to healthy volunteers, the tolerated maximum dosage of ropivacaine before start of neurotoxic and cardiovascular effects was twice as high as that of racemic bupivacaine [17,18]. Ropivacaine has a lower potency than both levo- and racemic bupivacaine and is approximately 10 times less lipophilic. At equipotent dose [19], it is uncertain whether there is really clinically relevant lower toxicity. Several cases in which intended epidural doses of ropivacaine were accidentally administered either intrathecally or intravenously resulted in severe complications [20,21]. Thus, whether ropivacaine actually has a safer clinical profile is questionable.
Related Knowledge Centers
- Adverse Drug Reaction
- Amide
- Amine
- Cardiac Arrest
- Cardiotoxicity
- Enantiomer
- Racemic Mixture
- Bupivacaine
- Local Anesthetic
- Intravenous Regional Anesthesia