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      Ropivacaine: A review of its pharmacology and clinical use

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          Abstract

          Ropivacaine is a long-acting amide local anaesthetic agent and first produced as a pure enantiomer. It produces effects similar to other local anaesthetics via reversible inhibition of sodium ion influx in nerve fibres. Ropivacaine is less lipophilic than bupivacaine and is less likely to penetrate large myelinated motor fibres, resulting in a relatively reduced motor blockade. Thus, ropivacaine has a greater degree of motor sensory differentiation, which could be useful when motor blockade is undesirable. The reduced lipophilicity is also associated with decreased potential for central nervous system toxicity and cardiotoxicity. The drug displays linear and dose proportional pharmacokinetics (up to 80 mg administered intravenously). It is metabolised extensively in the liver and excreted in urine. The present article details the clinical applications of ropivacaine and its current place as a local anaesthetic in the group.

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          Most cited references45

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          Central nervous and cardiovascular effects of i.v. infusions of ropivacaine, bupivacaine and placebo in volunteers.

          We have compared the incidence of CNS symptoms and changes in echocardiography and electrophysiology during i.v. infusions of ropivacaine, bupivacaine and placebo. Acute tolerance of i.v. infusion of 10 mg min-1 was studied in a crossover, randomized, double-blind study in 12 volunteers previously acquainted with the CNS effects of lignocaine. The maximum tolerated dose for CNS symptoms was higher after ropivacaine in nine of 12 subjects and higher after bupivacaine in three subjects. The 95% confidence limits for the difference in mean dose between ropivacaine and bupivacaine were -30 and 7 mg. The maximum tolerated unbound arterial plasma concentration was twice as high after ropivacaine (P < 0.001). Muscular twitching occurred more frequently after bupivacaine (P < 0.05). The time to disappearance of all symptoms was shorter after ropivacaine (P < 0.05). A threshold for CNS toxicity was apparent at a mean free plasma concentration of approximately 0.6 mg litre-1 for ropivacaine and 0.3 mg litre-1 for bupivacaine. Bupivacaine increased QRS width during sinus rhythm compared with placebo (P < 0.001) and ropivacaine (P < 0.01). Bupivacaine reduced both left ventricular systolic and diastolic function compared with placebo (P < 0.05 and P < 0.01, respectively), while ropivacaine reduced only systolic function (P < 0.01).
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            Ropivacaine: a pharmacological review.

            T Hansen (2004)
            Ropivacaine (Naropin, AstraZeneca) a new long-acting amide local anaesthetic agent, is a pure S-enantiomer, with a high pKa and relatively low-lipid solubility. Since its clinical introduction in 1996, it has been the focus of intense interest because of its increased CNS and cardiovascular safety compared with bupivacaine. This article reviews the pharmacology of ropivacaine with particular emphasis placed on toxicological issues. Compared with bupivacaine (the drug of choice for many years), ropivacaine is equally effective for subcutaneous infiltration, epidural, intrathecal and peripheral nerve block surgery, and obstetrics and postoperative analgesia. Ropivacaine is virtually identical to bupivacaine in terms of onset, quality and duration of sensory block, but seems to produce less motor block. The lesser toxicity of ropivacaine compared with bupivacaine has been confirmed in numerous animal experiments as well as human studies, including studies considering the presumed lower potency of ropivacaine. In fact, the reduced cardiovascular toxicity compared with bupivacaine may be a distinct feature of ropivacaine. So far, the increased cost of ropivacaine compared with bupivacaine has limited its wider clinical use -- in spite of the improved safety profile. During the last few years, cost differences between bupivacaine and ropivacaine have been minimized, thus making pharmacoeconomical speculations a much lesser concern when choosing a local anaesthetic drug. In conclusion, ropivacaine appears to be a safer local anaesthetic agent than bupivacaine. It seems particularly indicated for major peripheral nerve blocks and obstetrics. Ropivacaine should be considered when regional blocks are used in neonates and young infants. With the current trend in the cost development, ropivacaine will most likely be used increasingly in the future.
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              Toxicological and Local Anaesthetic Effects of Optically Active Isomers of Two Local Anaesthetic Compounds

              G Aberg (1972)
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                Author and article information

                Journal
                Indian J Anaesth
                IJA
                Indian Journal of Anaesthesia
                Medknow Publications (India )
                0019-5049
                0976-2817
                Mar-Apr 2011
                : 55
                : 2
                : 104-110
                Affiliations
                Department of Anesthesia and Critical Care, SPS Apollo Hospitals, Ludhiana, India
                [1 ]Department of Clinical Pharmacology, SPS Apollo Hospitals, Ludhiana, India
                Author notes
                Address for correspondence: Dr. Gaurav Kuthiala, Department of Anesthesia and Critical Care, SPS Apollo Hospitals, Ludhiana - 141 003, India. E-mail: chetnagaurav@ 123456yahoo.com
                Article
                IJA-55-104
                10.4103/0019-5049.79875
                3106379
                21712863
                16e0840d-dddc-45bb-b10a-a260704bc8ba
                © Indian Journal of Anaesthesia

                This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                Categories
                Review Article

                Anesthesiology & Pain management
                regional anaesthetic,anaesthesia,ropivacaine
                Anesthesiology & Pain management
                regional anaesthetic, anaesthesia, ropivacaine

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