Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0030193 (pain)
 261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Ropivacaine (Naropin) is the pure S(-)-enantiomer of propivacaine, and is a long-acting amide local anaesthetic agent, eliciting nerve block via reversible inhibition of sodium ion influx in nerve fibres. Ropivacaine is a well tolerated regional anaesthetic effective for surgical anaesthesia as well as the relief of postoperative and labour pain. The efficacy of ropivacaine is similar to that of bupivacaine and levobupivacaine for peripheral nerve blocks and, although it may be slightly less potent than bupivacaine when administered epidurally or intrathecally, equi-effective doses have been established. Clinically adequate doses of ropivacaine appear to be associated with a lower incidence or grade of motor block than bupivacaine. 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.
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PMID:Ropivacaine: a review of its use in regional anaesthesia and acute pain management. 1639 84

Ropivacaine is a relatively new amide-type local anaesthetic, mainly used for surgery and postoperative pain relief. In this study we have investigated the interaction between the CYP3A4 metabolite of ropivacaine, 2',6'-pipecoloxylidide (PPX), and premedication with, i.e., psychotropic and antianxiety agents (diazepam, midazolam), hypnotics (thiamylal), local anaesthetics (lidocaine), depolarizing muscular relaxants (vecuronium), antihypertensive (clonidine) and H(2)-receptor antagonist (cimetidine) using human liver microsomes in vitro. The effects of the interaction between PPX and premedications were examined using a human liver microsomal preparation in vitro. The concentrations of ropivacaine and PPX were determined by HPLC with UV detection. The apparent Michaelis-Menten constant (Km) and the maximal velocity of total metabolic formation (V(max)) of PPX, the main metabolite of ropivacaine in human liver microsomes, were 17.7 (microM, mean) and 711 (nmol/min./mg protein, mean), respectively. Five premedications (diazepam, lidocaine, cimetidine, vecuronium and clonidine) did not inhibit ropivacaine metabolism in human liver microsomes at concentrations within the therapeutic range. However, midazolam and thiamylal weakly inhibited ropivacaine metabolism in competitive manner (IC(50) 7.8 microM and 250 microM, respectively). The results show lack of interaction between ropivacaine and seven premedication medicines within the therapeutic range of ropivacaine using human liver microsomes in vitro.
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PMID:Effects of premedication medicines on the formation of the CYP3A4-dependent metabolite of ropivacaine, 2', 6'-Pipecoloxylidide, on human liver microsomes in vitro. 1644 92

The anesthetic, ropivacaine, has been used extensively in clinical practice, but few studies have evaluated this long-acting local anesthetic in dentistry. In this study we evaluated the effects of ropivacaine alone and ropivacaine + vasoconstrictor on the cardiovascular system when used as a dental anesthetic in volunteers. Thirty-two healthy subjects received two consecutive infiltrations of 1.8 ml of either 0.75% ropivacaine or ropivacaine + epinephrine into the pterygomandibular region. Pain sensation, numbness of the lip, arterial pressure, heart rate, and electrocardiogram changes were monitored for 2 h. The onset of anesthesia was 10 min after the injection and lasted for more than 2 h, and numbness of the lip lasted for approximately 8 h. Ropivacaine alone did not cause significant changes in the cardiovascular parameters, but ropivacaine + epinephrine caused a transient increase in arterial pressure and heart rate 2 min postinjection. We conclude that ropivacaine alone injected into the pterygomandibular region does not affect the cardiovascular system and that the addition of epinephrine has no beneficial effect. This finding may be relevant to dentists endeavoring to find an anesthetic of minimal cardiovascular risk to produce regional anesthesia for long-lasting procedures without the need of a vasoconstrictor.
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PMID:Effects of regional anesthesia with ropivacaine on arterial pressure and heart rate in healthy subjects. 1646 Mar 38

Epidural analgesia remains the "gold standard" of pain relief after total knee replacement. However, peripheral nerve block is gaining popularity because the incidence of side effects may be reduced. Our study tests this postulate. Sixty patients were prospectively randomized to receive either epidural infusion or combined continuous femoral and sciatic nerve blocks. Ropivacaine 2 mg/mL plus sufentanil 1 mug/mL was given either epidurally or through the femoral nerve catheter, and ropivacaine 0.5 mg/mL was given through the sciatic nerve catheter using elastomeric infusers (delivering 5 mL/h for 55 h). The primary outcome measure was the total incidence of side effects (urinary retention and moderate to severe degrees of dizziness, pruritus, sedation, and nausea/vomiting on the first postoperative day). Intensity of motor blockade, pain at rest and on mobilization, and rehabilitation indices were also registered for 72 h. One or more side effects were present in 87% of patients in the epidural group whereas only 35% of patients in the femoral and sciatic block groups were affected on the first postoperative day (P = 0.0002). Motor blockade was more intense in the operated limb on the day of surgery and the first postoperative day in the peripheral nerve block group (P = 0.001), whereas the non-operated limb was more blocked in the epidural group on the day of surgery (P = 0.0003). Pain on mobilization was well controlled in both groups and there were no differences in the length of hospital stay. Rehabilitation indices were similar. The results demonstrate a reduced incidence of side effects in the femoral/sciatic nerve block group than in the epidural group on the first postoperative day.
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PMID:A comparison of epidural analgesia with combined continuous femoral-sciatic nerve blocks after total knee replacement. 1757 1

Recently, most studies reported magnesium as a N-methyl-D-aspartate receptor antagonist and its analgesic and perioperative anaesthetic effects have been discussed with central desensitization pathway. We investigated the effects of caudal ropivacaine plus magnesium and compared with ropivacaine alone on postoperative analgesia requirements. After hospital ethic committee's consent, 60 patients (ASA I-II, 2-10 years old) who had lower abdominal or penoscrotal surgery were enrolled in the study. After general anaesthesia induction, caudal blockage was applied. Patients were randomly assigned in two groups. Ropivacaine 0.25% was administered to Group R (n=37), ropivacaine 0.25% plus 50 mg magnesium to Group RM (n=23) in 0.5 ml kg-1 volume. Postoperative analgesia level was recorded at 15 min and 1, 2, 3, 4, 6 h by using Paediatric Objective Pain Scale (POPS) and The Children's Hospital of Eastern Ontoria Pain Scale (CHEOPS). Postoperative motor blocks were evaluated with Modified Bromage Motor Block Scale. According to demographic characteristics, there were no significant differences between the two groups (P>0.05). POPS, CHEOPS, Bromage Motor Scales, analgesia duration and adverse effects were similar in Group R and Group RM. It has been shown that addition of magnesium as an adjuvant agent to local anaesthetics for caudal analgesia has no effect on postoperative pain and analgesic need.
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PMID:Could adding magnesium as adjuvant to ropivacaine in caudal anaesthesia improve postoperative pain control? 1702 40

The rostral ventromedial medulla (RVM) is involved in facilitation of spinal nociceptive processing and generation of hyperalgesia in inflammatory and neuropathic pain models. We hypothesized that the bilateral hyperalgesia that develops after repeated intramuscular injections of acidic saline is initiated and maintained by activation of descending facilitatory pathways from the RVM. Male Sprague-Dawley rats were implanted with intracerebral guide cannulae into the nucleus raphe magnus (NRM) or the nucleus gigantocellularis (Gi). Two injections of acidic saline into one gastrocnemius muscle 5 days apart lead to robust hyperalgesia after the second injection. Either ropivacaine (local anesthetic) or vehicle (control) was microinjected into the RVM prior to the first intramuscular acid injection, prior to the second injection, or 24h after the second injection. Mechanical withdrawal thresholds of the paw (von Frey filaments) and the muscle (tweezer) were measured before and 24h after induction of hyperalgesia. The withdrawal thresholds for both the paw (cutaneous secondary hyperalgesia) and muscle (primary hyperalgesia) were decreased 24h after the second intramuscular acid injection in the vehicle control groups. Administration of ropivacaine prior to the first intramuscular acid injection had no effect on development of either cutaneous or muscle hyperalgesia that develops after the second injection. However, neither cutaneous nor muscle hyperalgesia developed in the group treated with ropivacaine prior to the second intramuscular injection. Ropivacaine also significantly reversed the hyperalgesia in the group treated 24h after the second intramuscular acid injection. Thus, the RVM is critical for both the development and maintenance of hyperalgesia after muscle insult.
Pain 2008 Jun
PMID:Descending facilitatory pathways from the RVM initiate and maintain bilateral hyperalgesia after muscle insult. 1776 41

Ropivacaine blood and drain levels were measured in 20 hip and 15 total knee arthroplasties after intraoperative wound infiltration with 150 to 200 mL (360-400 mg) of ropivacaine, followed by a 48-hour intra-articular pain pump infusion of 1000 mg (knees) and 300 mg (hips) commencing 12 hours postoperatively. Concentrations were below 2 microg/mL over the first 12 hours before the pain pump increased levels. Peak total ropivacaine concentration ranged from 0.65 to 4.36 microg/mL with the pain pump. The high infiltration doses produced levels below or within the safe threshold of 1 to 3 microg/mL. Pain pump infusion produced some C(max) levels above 3.0 microg/mL, but there was no clinical evidence of toxicity. Wound drain amounts (0.53-26.69 mg) indicate reinfusion should be safe, although further study is needed to confirm this.
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PMID:Serum and wound drain ropivacaine concentrations after wound infiltration in joint arthroplasty. 1782 81

Transverse rectus abdominis musculocutaneous (TRAM) flap surgery is a complex procedure characterised by an extensive wound site. We present a pilot study with 17 patients receiving continuous wound instillation with ropivacaine or isotonic saline. Patients undergoing TRAM flap surgery were included in the study and randomised to the ropi group or the control group. Two catheters were placed subcutaneously before wound site closure. At the end of surgery patients received a single shot dose of 20 ml ropivacaine 0.2% or isotonic saline. After surgery the continuous instillation of ropivacaine or isotonic saline was commenced at an infusion rate of 10 ml/h per catheter. The perfusion of the TRAM flap was measured intraoperatively and postoperatively over 48 h. Pain scores, patient satisfaction, and the quality of recovery score were also assessed postoperatively over 48 h. Ropivacaine plasma levels were quantified 24 and 48 h after start of infusion. Pain scores at rest and on coughing were lower for the ropi group and reached significance in the first 8h at rest (P=0.007). Patient satisfaction, quality of recovery score, and adverse events were also comparable between the groups. Patients of the ropi group had bowel movement earlier than the control group (P=0.003). No differences were seen in the flap perfusion. Ropivacaine plasma levels were within therapeutic range. Our data show a trend that continuous wound instillation of ropivacaine 0.2% increases pain relief after TRAM flap surgery with earlier bowel movement than intravenous opioid patient controlled analgesia (IV-PCA) alone. A does of 960 mg of ropivacaine daily did not result in toxic plasma concentrations. Ropivacaine 0.2% did not show a vasoconstrictor effect.
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PMID:Postoperative analgesia and flap perfusion after pedicled TRAM flap reconstruction - continuous wound instillation with ropivacaine 0.2%. A pilot study. 1838 65

The use of lidocaine in spinal anaesthesia is associated with transient neurological syndrome (TNS). Bupivacaine has a lower incidence of TNS as an alternative but it may have a prolonged action. This study systematically reviews the literature about the recovery profile of patients undergoing spinal anaesthesia, using bupivacaine for arthroscopic knee surgery. We identified 17 eligible randomized clinical trials (RCTs) (1268 patients). All the articles in this review, except one, used hyperbaric bupivacaine. Five trials compared different doses of bupivacaine (range 3-15 mg). Large doses of bupivacaine (10 and 15 mg) were associated with delayed recovery, and supine positioning was associated with a high incidence of failure. With unilateral positioning, a dose as low as 4-5 mg seems to be sufficient. Five trials comparing bupivacaine or levobupivacaine with ropivacaine showed no significant difference in the time to home discharge. When bupivacaine was combined with fentanyl in two trials, marginal delay in recovery was found [time to discharge (min); weighted mean difference (WMD) 14.1, 95% CI 11.9-40.1] and increased nausea and pruritus but had reduced postoperative pain. Unilateral and bilateral spinal anaesthesia were assessed in two trials, and the latter group was associated with early recovery and discharge [time to discharge (min); WMD -41.6, 95% CI -63.6 to -19.6). The results of our systematic review suggest that 4-5 mg of hyperbaric bupivacaine can effectively produce spinal anaesthesia for knee arthroscopy with unilateral positioning. Ropivacaine or the addition of adjuvants did not improve the recovery time. There is a need for tighter RCTs with more consistent endpoints.
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PMID:Systematic review of spinal anaesthesia using bupivacaine for ambulatory knee arthroscopy. 1919 51

Local anesthetics are able to induce pain relief by binding to the sodium channels of excitable membranes, blocking the influx of sodium ions and the propagation of the nervous impulse. Ropivacaine (RVC) is an amino amide, enantiomerically pure, local anesthetic largely used in surgical procedures, which present physico-chemical and therapeutic properties similar to those of bupivacaine but decreased toxicity and motor blockade. The present work focuses on the preparation and characterization of nanospheres containing RVC; 0.25% and 0.50% RVC were incorporated in poly(d,l-lactide-co-glycolide (PLGA) 50:50) nanospheres (PLGA-NS), prepared by the nanoprecipitation method. Characterization of the nanospheres was conducted through the measurement of pH, particle size, and zeta potential. The pH of the nanoparticle system with RVC was 6.58. The average diameters of the RVC-containing nanospheres was 162.7 +/- 1.5 nm, and their zeta potentials were negative, with values of about -10.81 +/- 1.16 mV, which promoted good stabilization of the particles in solution. The cytotoxicity experiments show that RVC-loaded PLGA-NS generate a less toxic formulation as compared with plain RVC. Since this polymer drug-delivery system can effectively generate an even less toxic RVC formulation, this study is fundamental due to its characterization of a potentially novel pharmaceutical form for the treatment of pain with RVC.
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PMID:Initial development and characterization of PLGA nanospheres containing ropivacaine. 1966 31


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