Ropivacaine. A review of its pharmacology and therapeutic use in regional anaesthesia

A. Markham, D. Faulds, D. R. Abernethy, I. Cederholm, H. S. Feldman, B. T. Finucane, S. P. Gatt, R. Hickey, K. Nakamura, G. T. Tucker, J. A W Wildsmith

Research output: Contribution to journalArticle

Abstract

The enantiomerically pure (S-enantiomer) amide local anaesthetic drug ropivacaine blocked nerve fibres responsible for transmission of pain (Aδ and C fibres) more completely than those that control motor function (Aβ fibres) in in vitro studies. The drug shares the biphasic vascular effects common to the amide local anaesthetic drug class. In vitro studies indicate that ropivacaine is less cardiotoxic than equimolar concentrations of bupivacaine. Apart from one trial in women undergoing hysterectomy; clinical studies that compared the efficacy of different doses of epidurally administered ropivacaine in patients undergoing various surgical procedures did not reveal any consistent dose-related differences with respect to sensory blockade. However, motor blockade did become more intense as the dose of ropivacaine increased. Overall, direct comparisons show that epidural ropivacaine is less potent than motor blockade. The greater degree of separation between motor and sensory blockade seen with ropivacaine relative to bupivacaine is more apparent at the lower end of the dosage scale. Nevertheless, higher doses of ropivacaine than bupivacaine are generally required to elicit equivalent anaesthetic effects. Ropivacaine has been shown to induce successful brachial plexus anaesthesia when given at a concentration of 5 mg/ml, but not 2.5 mg/ml, and was as effective as bupivacaine in comparative studies in this indication. Limited data indicate that continuous epidural infusion of ropivacaine postoperatively reduces postsurgical pain in a dose-related manner. Morphine consumption was also reduced. Higher doses of ropivacaine were significantly more effective than placebo. Similarly, ropivacaine controlled postsurgical pain when infiltrated directly into surgical wound sites (i.e. wound infiltration) and was as effective as bupivacaine, and more effective than placebo, in this regard. Adverse events associated with epidurally administered ropivacaine include hypotension, nausea, bradycardia, transient paraesthesia, back pain, urinary retention and fever. The drug appears to have an adverse event profile similar to that of bupivacaine. In animal studies, overdoses of ropivacaine were better tolerated than overdoses of bupivacaine but not lidocaine (lignocaine). Human volunteers tolerated a higher intravenous dosage of ropivacaine than bupivacaine before developing initial signs of toxicity. Thus, ropivacaine, according to animal data, is less cardiotoxic than bupivacaine. Based on available clinical data, ropivacaine appears to be as effective and well tolerated as bupivacaine when equianalgesic doses are compared. The greater degree of separation between motor and sensory blockade seen with ropivacaine relative to bupivacaine at lower concentrations (= 5 mg/ml) will be advantageous in certain applications.

Original languageEnglish (US)
Pages (from-to)429-449
Number of pages21
JournalDrugs
Volume52
Issue number3
StatePublished - 1996
Externally publishedYes

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Conduction Anesthesia
Therapeutic Uses
Bupivacaine
Pharmacology
Anesthetics
ropivacaine
Lidocaine
Local Anesthetics
Amides
Pain
Fibers
Animals
Placebos
Unmyelinated Nerve Fibers
Urinary Retention
Enantiomers
Paresthesia
Back Pain
Bradycardia
Hysterectomy

ASJC Scopus subject areas

  • Toxicology
  • Health, Toxicology and Mutagenesis

Cite this

Markham, A., Faulds, D., Abernethy, D. R., Cederholm, I., Feldman, H. S., Finucane, B. T., ... Wildsmith, J. A. W. (1996). Ropivacaine. A review of its pharmacology and therapeutic use in regional anaesthesia. Drugs, 52(3), 429-449.

Ropivacaine. A review of its pharmacology and therapeutic use in regional anaesthesia. / Markham, A.; Faulds, D.; Abernethy, D. R.; Cederholm, I.; Feldman, H. S.; Finucane, B. T.; Gatt, S. P.; Hickey, R.; Nakamura, K.; Tucker, G. T.; Wildsmith, J. A W.

In: Drugs, Vol. 52, No. 3, 1996, p. 429-449.

Research output: Contribution to journalArticle

Markham, A, Faulds, D, Abernethy, DR, Cederholm, I, Feldman, HS, Finucane, BT, Gatt, SP, Hickey, R, Nakamura, K, Tucker, GT & Wildsmith, JAW 1996, 'Ropivacaine. A review of its pharmacology and therapeutic use in regional anaesthesia', Drugs, vol. 52, no. 3, pp. 429-449.
Markham A, Faulds D, Abernethy DR, Cederholm I, Feldman HS, Finucane BT et al. Ropivacaine. A review of its pharmacology and therapeutic use in regional anaesthesia. Drugs. 1996;52(3):429-449.
Markham, A. ; Faulds, D. ; Abernethy, D. R. ; Cederholm, I. ; Feldman, H. S. ; Finucane, B. T. ; Gatt, S. P. ; Hickey, R. ; Nakamura, K. ; Tucker, G. T. ; Wildsmith, J. A W. / Ropivacaine. A review of its pharmacology and therapeutic use in regional anaesthesia. In: Drugs. 1996 ; Vol. 52, No. 3. pp. 429-449.
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N2 - The enantiomerically pure (S-enantiomer) amide local anaesthetic drug ropivacaine blocked nerve fibres responsible for transmission of pain (Aδ and C fibres) more completely than those that control motor function (Aβ fibres) in in vitro studies. The drug shares the biphasic vascular effects common to the amide local anaesthetic drug class. In vitro studies indicate that ropivacaine is less cardiotoxic than equimolar concentrations of bupivacaine. Apart from one trial in women undergoing hysterectomy; clinical studies that compared the efficacy of different doses of epidurally administered ropivacaine in patients undergoing various surgical procedures did not reveal any consistent dose-related differences with respect to sensory blockade. However, motor blockade did become more intense as the dose of ropivacaine increased. Overall, direct comparisons show that epidural ropivacaine is less potent than motor blockade. The greater degree of separation between motor and sensory blockade seen with ropivacaine relative to bupivacaine is more apparent at the lower end of the dosage scale. Nevertheless, higher doses of ropivacaine than bupivacaine are generally required to elicit equivalent anaesthetic effects. Ropivacaine has been shown to induce successful brachial plexus anaesthesia when given at a concentration of 5 mg/ml, but not 2.5 mg/ml, and was as effective as bupivacaine in comparative studies in this indication. Limited data indicate that continuous epidural infusion of ropivacaine postoperatively reduces postsurgical pain in a dose-related manner. Morphine consumption was also reduced. Higher doses of ropivacaine were significantly more effective than placebo. Similarly, ropivacaine controlled postsurgical pain when infiltrated directly into surgical wound sites (i.e. wound infiltration) and was as effective as bupivacaine, and more effective than placebo, in this regard. Adverse events associated with epidurally administered ropivacaine include hypotension, nausea, bradycardia, transient paraesthesia, back pain, urinary retention and fever. The drug appears to have an adverse event profile similar to that of bupivacaine. In animal studies, overdoses of ropivacaine were better tolerated than overdoses of bupivacaine but not lidocaine (lignocaine). Human volunteers tolerated a higher intravenous dosage of ropivacaine than bupivacaine before developing initial signs of toxicity. Thus, ropivacaine, according to animal data, is less cardiotoxic than bupivacaine. Based on available clinical data, ropivacaine appears to be as effective and well tolerated as bupivacaine when equianalgesic doses are compared. The greater degree of separation between motor and sensory blockade seen with ropivacaine relative to bupivacaine at lower concentrations (= 5 mg/ml) will be advantageous in certain applications.

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