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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

This report describes the activity of the antiepileptic agent gabapentin (Neurontin) in animal models predictive of anxiolysis and analgesia. Gabapentin displayed anxiolytic-like action in the rat conflict test, the mouse light/dark box and the rat elevated X-maze with respective minimum effective doses (MEDs) of 3, 10 and 30 mg/kg. Furthermore, gabapentin also induced behavioural changes suggestive of anxiolysis in the marmoset human threat test with a MED of 30 mg/kg. In the rat formalin test of tonic nociception, gabapentin dose-dependently (30-300 mg/kg) and selectively blocked the late phase with a MED of 100 mg/kg. However, it failed to block carrageenan-induced paw oedema. The intracerebroventricular (ICV) administration of the glycine/NMDA receptor agonist D-Serine, dose-dependently (10-100 micrograms/animal) reversed the antinociceptive action of gabapentin (200 mg/kg, SC). D-Serine (30 micrograms/animal, ICV) also reversed the anxiolytic-like effects (in the light/dark box and the rat elevated X-maze) of gabapentin (30 mg/kg). In contrast, L-Serine (100 micrograms, ICV) failed to block the antinociceptive action of gabapentin. The antinociceptive action of (+)-HA-966 (25 mg/kg, SC), a partial agonist at the glycine/NMDA receptor, was reversed by D-Serine (100 micrograms/animal, ICV). However, D-Serine (100 micrograms/animal, ICV) failed to affect the antinociceptive action of a competitive NMDA receptor antagonist CGS 19755 (3 mg/kg, SC). Gabapentin has negligible affinity for the strychnine insensitive [3H]glycine binding site. This indicates that the interaction between gabapentin and D-Serine may not involve the NMDA receptor complex. Gabapentin may represent a novel type of anxiolytic and analgesic agent.
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PMID:The antiepileptic agent gabapentin (Neurontin) possesses anxiolytic-like and antinociceptive actions that are reversed by D-serine. 888 Sep 37

Gabapentin was administered as an "add on" therapy to 22 patients with neuropathic cancer pain only partially responsive to opioid therapy. Global pain, burning pain, shooting pain episodes, and allodynia were assessed separately. Gabapentin was given for at least a week and efficacy was assessed after 7 to 14 days of therapy. Global pain score decreased from a mean (+/- SD) of 6.4 (+/- 1.5) to 3.2 (+/- 1.3) (95% confidence interval of the baseline minus final score differences [95% CI] = 1.0-2.4). Burning pain intensity decreased from a mean (+/- SD) of 5.1 (+/- 3.6) to 2.0 (+/- 2.3) (95% CI = 1.5-3.8), and episodes of shooting pain decreased in frequency from 7.2 (+/- 3.7) to 2.2 (+/- 2.2) daily episodes (95% CI = 1.8-4.3). Allodynia was found in 9 patients and disappeared in 7 during gabapentin administration. Twenty patients judged the new drug efficacious in relieving their symptoms. The potential role of gabapentin as an adjuvant to opioid analgesia in cancer pain is discussed.
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PMID:Gabapentin as an adjuvant to opioid analgesia for neuropathic cancer pain. 1103 90

Substantial progress has been made during the last decades in our understanding of acute pain mechanisms, and this knowledge has encouraged the search for novel treatments. Of particular interest has been the observation that tissue injury initiates a number of modulations of both the peripheral and the central pain pathways, which convert the system from a 'physiological' to a 'pathological' mode of processing afferent information. Gabapentin, which binds to the alpha(2)delta subunit of the voltage-dependent calcium channel, is active in animal models of 'pathological' but not in models of 'physiological' pain. Consequently, attention has so far been focused on neuropathic pain as a target for the clinical use of gabapentin and analogues. Recently, several reports have indicated that gabapentin may have a place in the treatment of post-operative pain. This article presents a brief summary of the potential mechanisms of post-operative pain, and a systematic review of the available data of gabapentin and pregabalin for post-operative analgesia. It is concluded that the results with gabapentin and pregabalin in post-operative pain treatment published so far are promising. It is suggested that future studies should explore the effects of 'protective premedication' with combinations of various antihyperanalgesic and analgesic drugs for post-operative analgesia.
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PMID:'Protective premedication': an option with gabapentin and related drugs? A review of gabapentin and pregabalin in in the treatment of post-operative pain. 1535 59

Gabapentin has antihyperalgesic and anxiolytic properties. We thus tested the hypothesis that premedication with gabapentin would decrease preoperative anxiety and improve postoperative analgesia and early postoperative knee mobilization in patients undergoing arthroscopic anterior cruciate ligament repair under general anesthesia. Forty patients were randomly assigned to receive 1200 mg oral gabapentin or placebo 1-2 h before surgery; anesthesia was standardized. Patients received morphine, 0.1 mg/kg, 30 min before the end of surgery and postoperatively via a patient-controlled pump. Pain scores and morphine consumption were recorded over 48 h. Degrees of active and passive knee flexion and extension were recorded during physiotherapy on days 1 and 2. Preoperative anxiety scores were less in the gabapentin than control group (visual analog scale scores of 28 +/- 16 mm versus 66 +/- 15 mm, respectively; P < 0.001). The gabapentin group required less morphine than the control group (29 +/- 22 mg versus 69 +/- 40 mg, respectively; P < 0.001). Visual analog scale pain scores at rest and after mobilization were significantly reduced in the gabapentin group. First and maximal passive and active knee flexions at 24 and 48 h were significantly more extensive in the gabapentin than in the control group. In conclusion, premedication with 1200 mg gabapentin improved preoperative anxiolysis, postoperative analgesia, and early knee mobilization after arthroscopic anterior cruciate ligament repair.
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PMID:Preoperative gabapentin decreases anxiety and improves early functional recovery from knee surgery. 1584 93

The saphenous partial ligation (SPL) model is a new, easily performed, rodent model of neuropathic pain that consists of a unilateral partial injury to the saphenous nerve. The present study describes behavioral, pharmacological and molecular properties of this model. Starting between 3 and 5 days after surgery, depending on the modality tested, animals developed clear behaviors indicative of neuropathic pain such as cold and mechanical allodynia, and thermal and mechanical hyperalgesia compared with naive and sham animals. These pain behaviors were still present at 1 month. Signs of allodynia also extended to the sciatic nerve territory. No evidence of autotomy or bodyweight loss was observed. Cold and mechanical allodynia but not thermal and mechanical hyperalgesia was reversed by morphine (4 mg/kg i.p.). The cannabinoid receptor agonist WIN 55,212-2 (5 mg/kg i.p.) improved signs of allodynia and hyperalgesia tested except for mechanical hyperalgesia. Gabapentin (50 mg/kg i.p.) was effective against cold and mechanical allodynia but not hyperalgesia. Finally, amitriptyline (10 mg/kg i.p.) failed to reverse allodynia and hyperalgesia and its administration even led to hyperesthesia. Neurobiological studies looking at the expression of mu opioid receptor (MOR), cannabinoid CB(1) and CB(2) receptors showed a significant increase for all three receptors in ipsilateral paw skin, L3-L4 dorsal root ganglia and spinal cord of neuropathic rats compared with naive and sham animals. These changes in MOR, CB(1) and CB(2) receptor expression are compatible with what is observed in other neuropathic pain models and may explain the analgesia produced by morphine and WIN 55,212-2 administrations. In conclusion, we have shown that the SPL is an adequate model that will provide a new tool for clarifying peripheral mechanisms of neuropathic pain in an exclusive sensory nerve.
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PMID:Behavioral, pharmacological and molecular characterization of the saphenous nerve partial ligation: a new model of neuropathic pain. 1585 13

Synergism between gabapentin and morphine in treating incisional pain has been demonstrated in animal experiments and clinical studies. The efficacy of gabapentin for treatment of perioperative pain remains controversial. This study was designed to detect the influence of gabapentin premedication on morphine consumption in the immediate postoperative period in patients undergoing lumbar laminectomy and discectomy. Either gabapentin 800 mg (in two equally divided doses) or placebo was given preoperatively to 60 adult patients undergoing elective lumbar laminectomy or discectomy in a double-blinded, placebo-controlled, randomized study. Standard general anesthesia was given to all the patients. Morphine was administered via patient-controlled analgesia pump in the immediate postoperative period for first 8 hours. Pain at rest and on movement was assessed using a Verbal Rating Scale (VRS) every 2 hours for the first 8 postoperative hours. There were no differences in demographics or surgical duration between the two groups. The amount of fentanyl administered in the intraoperative period was similar between the two groups. In the postoperative period, the VRS score for pain at 0, 2, 4, 6, and 8 hours was not significantly different between the two groups. Highest median VRS score was recorded at 0 hours postoperatively in both groups (VRS: rest = 6, movement = 8 in placebo group; rest = 6, movement = 8 in gabapentin group). Total morphine consumption and side effects were similar in the two groups. Gabapentin does not decrease the morphine requirement or morphine side effects in the immediate postoperative period following lumbar laminectomy and discectomy.
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PMID:Effect of preemptive gabapentin on postoperative pain relief and morphine consumption following lumbar laminectomy and discectomy: a randomized, double-blinded, placebo-controlled study. 1603 39

The cyclooxygenase-2 inhibitor, rofecoxib, was a popular analgesic adjuvant for improving perioperative pain management. We designed this placebo-controlled study to test the hypothesis that gabapentin could produce similar reductions in postoperative pain and opioid analgesic usage, thereby improving the recovery process. One hundred patients undergoing abdominal hysterectomy procedures were randomly assigned to one of four treatment groups: 1) control group received placebo capsules and pills before and for 2 days after surgery, 2) rofecoxib group received 50 mg/d PO and placebo capsules before and after surgery and, 3) gabapentin group received 1.2 g/d PO and placebo pills before and after surgery, and 4) combination group received rofecoxib 50 mg/d and gabapentin 1.2 g/d PO before and after surgery. The anesthetic technique was standardized and the postoperative assessments included verbal rating scales for pain and sedation, IV morphine usage, quality of recovery assessment, recovery of bowel function, resumption of normal activities, and patient satisfaction with their pain management. Postoperative pain scores were significantly reduced in all three analgesic treatment groups (versus control group). Compared with the control group, patient-controlled analgesia morphine usage was also significantly reduced in the 3 analgesic treatment groups at 1, 8, 24, and 30 h after surgery. Total PCA morphine usage was decreased by 43%, 24%, and 50% in groups 2, 3, and 4, respectively, compared with group 1. Oral analgesic consumption was also smaller in groups 2 and 4 when compared with the control group. The opioid-sparing effects of rofecoxib and gabapentin lead to a faster recovery of bowel function. Discharge eligibility scores in groups 2 and 4 were improved at 24 h when compared with group 1, and patient satisfaction with postoperative pain management was significantly higher at 24 h in all 3 analgesic treatment groups. At the 72 h follow-up, all of the patients in group 4 were completely satisfied with their pain management compared with only 32%, 64%, and 72% in groups 1, 2, and 3, respectively. Gabapentin (1.2 g/d PO) appears to be an acceptable alternative to rofecoxib (50 mg/d PO) for short-term use as an adjuvant to opioid analgesics in patients undergoing lower abdominal surgery.
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PMID:Gabapentin: an alternative to the cyclooxygenase-2 inhibitors for perioperative pain management. 1636 26

Summary Gabapentin is an antiepileptic drug indicated for the treatment of partial seizures in children. Many studies have proved its analgesic action in the treatment of neuropathic pain in adults and we have noticed an analgesic action of gabapentin in neuropathic pain in children. Five patients treated in the Children's Hospital Pain Control Service for intractable neuropathic pain were included in gabapentin treatment. Four were cancer patients and one suffered from neuropathic pain in the neck (C3). The visual analog scale (VAS) scores of pain were compared before and during treatment with gabapentin. We noticed a rapid improvement, in 1 week, of our patients' VAS scores (from 9 or 10 to 4 or 3) with minimal adverse effects. In the follow-up period of 6 months we gradually reduced the dose of gabapentin. Our findings are that gabapentin should be included earlier in the treatment of neuropathic pain in adolescents, because it rapidly improves analgesia and has minimal side effects.
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PMID:Experience with gabapentin for neuropathic pain in adolescents: report of five cases. 1649 Jan

Chemotherapeutics in the taxane and vinca-alkaloid classes sometimes produce a painful peripheral neuropathy for which there is no validated treatment. Experiments with rat models of paclitaxel- and vincristine-evoked pain suggest that these conditions may not respond to all of the analgesics that have efficacy in other models of painful peripheral neuropathy. We tested gabapentin as a potential analgesic for paclitaxel- and vincristine-evoked pain. We used a repeated dosing paradigm because there are precedents showing that repeated drug exposure may be necessary to demonstrate analgesia in neuropathic pain models. Gabapentin is believed to work via binding to voltage-gated calcium channels that contain the alpha-2-delta type-1 (alpha(2)delta-1) subunit, and the expression of this subunit is known to be increased in some painful peripheral neuropathy models. Thus we also examined whether the paclitaxel-evoked pain syndrome was accompanied by an alpha(2)delta-1 increase, and whether gabapentin had any effect on subunit expression. We found that the paclitaxel- and vincristine-evoked mechano-allodynia and mechano-hyperalgesia were significantly reduced by gabapentin, but only with repeated dosing. Paclitaxel-evoked painful peripheral neuropathy was associated with an increased expression of the alpha(2)delta-1 subunit in the spinal dorsal horn, but not in the dorsal root ganglia. The spinal cord increase was normalized by repeated gabapentin injections. Together, these findings suggest that repeated dosing with gabapentin may be beneficial in patients with chemotherapy-evoked painful peripheral neuropathy and that gabapentin's mechanisms of action may include normalization of the nerve injury-evoked increase in calcium channel alpha(2)delta-1 subunit expression.
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PMID:Chemotherapy-evoked painful peripheral neuropathy: analgesic effects of gabapentin and effects on expression of the alpha-2-delta type-1 calcium channel subunit. 1708 35

Neuropathic pain is defined as pain caused by a lesion in the nervous system and is common in clinical practice. Diagnosis can be difficult. Recommendations for first-line pharmacologic treatments are based on positive results from multiple, randomized, controlled trials, and recommendations for second-line pharmacologic treatments are based on the positive result of a single, randomized, controlled trial or inconsistent results of multiple, randomized, controlled trials. The results of published trials and clinical experience provide the foundation for specific recommendations for first-line treatments, which include gabapentin, 5% lidocaine patch, opioid analgesics, tramadol hydrochloride, and tricyclic antidepressants (TCAs). Gabapentin (up to 3,600 mg/day) significantly reduced pain compared with placebo; improvements in sleep, mood, and quality of life were also demonstrated. Adverse effects of gabapentin include somnolence and dizziness, and, less commonly, gastrointestinal symptoms and mild peripheral edema. Thus, monitoring and dosage adjustment are required, without discontinuation of the drug. Gabapentin combined with morphine achieved better analgesia at lower doses of each drug than each drug alone, with only mild adverse effects. The first medication that proved effective for neuropathic pain in placebo-controlled trials was TCAs. Treatment decisions for patients with neuropathic pain can be difficult. Interest in the mechanisms and treatment of chronic neuropathic pain has increased during the past years, resulting in significant treatment advances in the future. In this article all recent knowledge on therapeutic management of chronic neuropathic pain is presented.
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PMID:Therapeutic management of chronic neuropathic pain: an examination of pharmacologic treatment. 1719 64


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