Disease relevance of Ropivacaine

• Thus ropivacaine, with its efficacy, lower propensity for motor block and reduced potential for CNS toxicity and cardiotoxicity, appears to be an important option for regional anaesthesia and for the management of postoperative and labour pain [1].
• Adverse events associated with epidurally administered ropivacaine include hypotension, nausea, bradycardia, transient paraesthesia, back pain, urinary retention and fever [2].
• In animal studies, overdoses of ropivacaine were better tolerated than overdoses of bupivacaine but not lidocaine (lignocaine) [2].
• The studies show that ropivacaine provides postoperative pain relief in a dose-related manner with minimal or a low degree of dose-related motor blockade [3].
• Ropivacaine, a new local anesthetic, is currently being investigated for the treatment of ulcerative colitis, with promising results so far [4].

Psychiatry related information on Ropivacaine

• The present study indicates that the circadian rhythms of heart rate and locomotor activity are modified after continuous infusion of ropivacaine, which is of particular interest, given the potential cardiotoxicity of this local anesthetic agent [5].
• No significant differences in the pain threshold, onset of sensory block, or Bromage Scale were found between the lidocaine and ropivacaine groups [6].
• CASE REPORT: Two patients, after traumatic upper limb amputations and early phantom limb pain, were treated on the second and fifth day following amputation by continuous brachial plexus analgesia with ropivacaine 0.375% (30 ml for the initial block, continuous infusion rate = 5 ml/h) for 5 (Patient 1) and 9 days (Patient 2) [7].

High impact information on Ropivacaine

• Effect of rifampin and tobacco smoking on the pharmacokinetics of ropivacaine [8].
• Rifampin considerably increases the metabolism of ropivacaine to PPX and decreases the metabolism to 3-OH-ropivacaine in both nonsmokers and smokers [8].
• Rifampin decreased the AUC of ropivacaine in nonsmokers by 52% and in smokers by 38% [8].
• Ropivacaine inhibited LPA signaling in a stereoselective and noncompetitive manner, suggesting a protein interaction [9].
• CONCLUSIONS: CYP1A2 is the most important isozyme for the metabolism of ropivacaine [10].

Chemical compound and disease context of Ropivacaine

• In common with ropivacaine, levobupivacaine has been shown to have a reduced incidence of toxicity in comparison the R-(+)-enantiomer in preclinical studies, explained in part by a reduced affinity to both brain and myocardial tissue [11].
• CONCLUSIONS: The authors found that a single caudal injection of neostigmine when added to ropivacaine offers an advantage over ropivacaine alone for postoperative pain relief in children undergoing genitourinary surgery [12].
• Airway anesthesia alone does not explain attenuation of histamine-induced bronchospasm by local anesthetics: a comparison of lidocaine, ropivacaine, and dyclonine [13].
• We evaluated the safety and efficacy of a 72-h epidural infusion of ropivacaine and measured the impact of adding fentanyl 2 microg/mL to the required infusion rate, on the quality of postoperative pain relief and the incidence of side effects, after colonic surgery [14].
• The effect of epidural sufentanil in ropivacaine on urinary retention in patients undergoing gastrectomy [15].

Biological context of Ropivacaine

• CONCLUSIONS: After ambulatory orthopedic surgery, 0.2% ropivacaine delivered as a perineural infusion using a disposable elastomeric pump with patient-controlled anesthesia bolus doses optimizes functional recovery and pain relief while decreasing the consumption of rescue analgesics and ropivacaine, and the number of adverse events [16].
• Protein binding of ropivacaine in the concentration range associated with toxic manifestations was similar in sera obtained from nonpregnant and pregnant ewes [17].
• The ability of ropivacaine to produce cutaneous vasoconstriction offers several advantages over the other local anesthetics presently available for infiltration anesthesia [18].
• The lower lipid solubility of ropivacaine may be responsible for the lesser dose-dependent effects of this drug on mitochondrial bioenergetics [19].
• Action potential amplitude and maximal rate of depolarization (Vmax) were significantly decreased by all agents in the following order: bupivacaine, ropivacaine, lidocaine [20].

Anatomical context of Ropivacaine

• Continuous blockade of both brachial plexus with ropivacaine in phantom pain: a case report [21].
• For lumbar epidural anaesthesia for lower limb or genitourinary surgery, comparative data suggest that higher concentrations of ropivacaine (0.75 or 1.0%) may be needed to provide the same sensory and motor blockade as bupivacaine 0.5 and 0.75% [22].
• In patients about to undergo upper limb surgery, 30 to 40ml ropivacaine 0.5% produced brachial plexus anaesthesia broadly similar to that achieved with equivalent volumes of bupivacaine 0.5%, although the time to onset of sensory block tended to be faster and the duration of motor block shorter with ropivacaine [22].
• The current study was designed to compare onset time and efficacy of two different double-injection approaches for sciatic nerve block with 0.75% ropivacaine [23].
• Cardiac arrest after injection of ropivacaine for posterior lumbar plexus blockade [24].

Associations of Ropivacaine with other chemical compounds

• The ropivacaine half-life (t1/2) of 1.9 hours was almost doubled during fluvoxamine administration and the plasma concentration at the end of infusion increased slightly, whereas the corresponding parameters after ketoconazole administration remained unchanged [10].
• Levobupivacaine was found to be 1.31 (95% confidence interval, 1.04-2.01) times more potent than ropivacaine [25].
• The addition of 4 microg/ml fentanyl improves analgesia from epidural ropivacaine [26].
• RESULTS: Intravenous regional anesthesia with 0.2% ropivacaine and 0.5% lidocaine provided equivalent levels of surgical anesthesia [27].
• CONCLUSIONS: Ropivacaine 0.125% with sufentanil affords reliable analgesia with minimal motor blockade [28].

Gene context of Ropivacaine

• The main CYP isoforms involved are CYP3A4 for lidocaine and bupivacaine and CYP1A2 for ropivacaine [29].
• Ropivacaine, a new amide-type local anesthetic agent, is metabolized by cytochromes P450 1A and 3A in human liver microsomes [30].
• Sciatic nerve blockade with ropivacaine did not prevent the increase in lumbar spinal COX-2 protein levels after incision [31].
• Duration of analgesia increased with increasing concentration of ropivacaine: mean duration of analgesia was 203 and 266 min at T10 and 253 and 314 min at L5 for the 0.5 and 1% solutions, respectively [32].
• In addition, ropivacaine downregulated the expression of clusterin/ apoliporotein J, a protein with anti-apoptotic properties, in a dose-dependent manner, which well correlated with the induction of apoptosis of HaCaT cells [33].

Analytical, diagnostic and therapeutic context of Ropivacaine

• Extensive clinical data have shown that epidural ropivacaine 0.2% is effective for the initiation and maintenance of labour analgesia, and provides pain relief after abdominal or orthopaedic surgery especially when given in conjunction with opioids (coadministration with opioids may also allow for lower concentrations of ropivacaine to be used) [22].
• Lumbar epidural administration of 20 to 30ml ropivacaine 0.5% provided anaesthesia of a similar quality to that achieved with bupivacaine 0.5% in women undergoing caesarean section, but the duration of motor blockade was shorter with ropivacaine [22].
• Ropivacaine is a long-acting, enantiomerically pure (S-enantiomer) amide local anaesthetic with a high pKa and low lipid solubility which blocks nerve fibres involved in pain transmission (Adelta and C fibres) to a greater degree than those controlling motor function (Abeta fibres) [22].
• 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 [2].
• METHODS: Sixteen gynecologic patients undergoing abdominal surgery received postoperative epidural analgesia using 0.75% ropivacaine at a dose of 22.5 mg (3 ml) per hour [34].

References