Levobupivacaine: A Review of its Pharmacology and Use as a Local Anaesthetic

Foster, R.H.; Markham, A.
March 2000
Drugs;Mar2000, Vol. 59 Issue 3, p551
Academic Journal
Based on findings that the cardiotoxicity infrequently observed with racemic bupivacaine shows enantioselectivity, i.e. it is more pronounced with the R(+)-enantiomer, the S(-)-enantiomer (levobupivacaine) has been developed for clinical use as a long acting local anaesthetic. The majority of in vitro, in vivo and human pharmacodynamic studies of nerve block indicate that levobupivacaine has similar potency to bupivacaine. However, levobupivacaine had a lower risk of cardiovascular and CNS toxicity than bupivacaine in animal studies. In human volunteers, levobupivacaine had less of a negative inotropic effect and, at intravenous doses >75mg, produced less prolongation of the QT interval than bupivacaine. Fewer changes indicative of CNS depression on EEG were evident with levobupivacaine. Levobupivacaine is long acting with a dose-dependent duration of anaesthesia. The onset of action is ≤15 minutes with various anaesthetic techniques. In studies of surgical anaesthesia in adults, levobupivacaine provided sensory block for up to 9 hours after epidural administration of ≤202.5mg, 6.5 hours after intrathecal 15mg, and 17 hours after brachial plexus block with 2 mg/kg. Randomised, double-blind clinical studies established that the anaesthetic and/or analgesic effects of levobupivacaine were largely similar to those of bupivacaine at the same dose. Sensory block tended to be longer with levobupivacaine than bupivacaine, amounting to a difference of 23 to 45 minutes with epidural administration and approximately 2 hours with peripheral nerve block. With epidural administration, levobupivacaine produced less prolonged motor block than sensory block. This differential was not seen with peripheral nerve block. Conditions satisfactory for surgery and good pain management were achieved by use of local infiltration or peribulbar administration of levobupivacaine. Levobupivacaine was generally as effective as bupivacaine for pain management during labour, and was effective for the management of postoperative pain, especially when combined with clonidine, morphine or fentanyl. The tolerability profiles of levobupivacaine and bupivacaine were very similar in clinical trials. No clinically significant ECG abnormalities or serious CNS events occurred with the doses used. The most common adverse event associated with levobupivacaine treatment was hypotension (31%). Conclusions: Levobupivacaine is a long acting local anaesthetic with a clinical profile closely resembling that of bupivacaine. However, current preclinical safety and toxicity data show an advantage for levobupivacaine over bupivacaine. Clinical data comparing levobupivacaine with ropivacaine are needed before the role of the drug can be fully established. Excluding pharmacoeconomic considerations, levobupivacaine is an appropriate choice for use in place of bupivacaine.


Related Articles

  • phenazopyridine.  // Davis's Drug Guide for Nurses, 10th edition;2007, p944 

    The article presents information on the drug phenazopyridine for nurses. Forms of this drug include Azo-Standard, Baridium and Geridium. Phenazopyridine provides relief from the following urinary tract symptoms. It acts locally on the urinary tract mucosa to produce analgesic or local anesthetic...

  • Relationships Between the Structure of Dexoxadrol and Etoxadrol Analogues and their NMDA Receptor Affinity. Sax, Michael; Wunsch, Bernhard // Current Topics in Medicinal Chemistry;Apr2006, Vol. 6 Issue 7, p723 

    In the mid 1960s the (dioxolan-4-yl)piperidine derivatives dexoxadrol ((S,S)-1a) and etoxadrol ((S,S,S)-2a) were synthesized. Their pharmacological potential as analgesics, anesthetics and local anesthetics was evaluated in animal models and later on in clinical trials with patients. However,...

  • counter-irritant (Major drug group).  // Royal Society of Medicine: Medicines;2002, p175 

    This article presents information on the counter-irritant preparations called rubefacient. The drug causes a feeling of warmth and offset the pain from underlying muscle and joints or viscera when rubbed in topically to the skin. Some are rubbed onto the gums where they have a local anaesthetic...

  • Central Nervous System Drugs.  // Pharm Phlash! Pharmacology Phlash Cards;2009, p100 

    The article offers information on several central nervous system drugs including analgesics, opioid reversal agents and anesthetics and sleep inducers. They include acetaminophen, naloxone and propofol. The drugs' pharmacologic class, therapeutic indications and actions and adverse reactions are...

  • Recent Advances in the Pharmacological Management of Pain. Guindon, Josée; Walczak, Jean-Sébastien; Beaulieu, Pierre // Drugs;2007, Vol. 67 Issue 15, p2121 

    Pain is an unpleasant sensation that originates from ongoing or impending tissue damage. Management of different types of pain (acute, postoperative, inflammatory, neuropathic or cancer) is the most frequent issue encountered by clinicians and pharmacological therapy is the first line of...

  • Minimizing the pain of venipuncture. Scholz, Mary J. // RN;May96, Vol. 59 Issue 5, p78 

    Presents information on the pain killer Alidocaine and prilocaine anesthetic cream (EMLA) used when having an injection. Details on the dosage; How to use the cream.

  • Correction.  // American Journal of Health-System Pharmacy;2/15/2002, Vol. 59 Issue 4, p383 

    Presents a correct version of the article, titled 'Clinical practice guidelines for the sustained use of sedatives and analgesics in the critically ill adult,' published in the January 15, 2002 issue of the 'American Journal of Health-System Pharmacy'.

  • Pharmacological management of acute dental pain. Canavan, Dermont // Journal of the Irish Dental Association;Autumn2007, Vol. 53 Issue 3, p141 

    The recent withdrawal of a popular analgesic medication by the Irish Medicines Board has raised a number of important questions regarding the use of analgesics for acute dental pain. This short article reviews some of the principles of analgesic usage and outlines the scope of available...

  • Erratum.  // Clinical Pediatrics;Feb1963, Vol. 2 Issue 2, p60 

    Presents a correction to the article "Clinical Use of Analgesics: Some Basic Pharmacologic Principles," that was previously published in the January 1963 issue.


Read the Article


Sorry, but this item is not currently available from your library.

Try another library?
Sign out of this library

Other Topics