- Outcome reporting in industry-sponsored trials of gabapentin for off-label use
S Swaroop Vedula
Center for Clinical Trials, Department of Epidemiology, Johns Hopkins Bloomberg School of Public Health, Baltimore, MD, USA
N Engl J Med 361:1963-71. 2009
..There is good evidence of selective outcome reporting in published reports of randomized trials...
- Gabapentin for the symptomatic treatment of painful neuropathy in patients with diabetes mellitus: a randomized controlled trial
Department of Neurology, University of Wisconsin, Madison 53792, USA
JAMA 280:1831-6. 1998
..Pain is the most disturbing symptom of diabetic peripheral neuropathy. As many as 45% of patients with diabetes mellitus develop peripheral neuropathies...
- Review of current guidelines on the care of postherpetic neuralgia
Charles E Argoff
Albany Medical College, Albany, NY 12208, USA
Postgrad Med 123:134-42. 2011
- The anti-allodynic effects of amitriptyline, gabapentin, and lidocaine in a rat model of neuropathic pain
Department of Anesthesiology and Critical Care, The Massachusetts General Hospital, Harvard Medical School, Boston 02114, USA
Anesth Analg 87:1360-6. 1998
..Finally, the site of action of LDC seems to be primarily in the periphery, and that of GBP is exclusively central, whereas that of AMI seems to have both peripheral and central components...
- Cellular and molecular action of the putative GABA-mimetic, gabapentin
Y P Maneuf
Cambridge Biotechnology Ltd, PO Box 230, Cambridge CB2 1XJ, United Kingdom
Cell Mol Life Sci 60:742-50. 2003
- Gabapentin for neuropathic cancer pain: a randomized controlled trial from the Gabapentin Cancer Pain Study Group
Rehabilitation and Palliative Care Unit, National Cancer Institute of Milan, Via Venezian 1, 20133 Milan, Italy
J Clin Oncol 22:2909-17. 2004
..To determine the analgesic effect of the addition of gabapentin to opioids in the management of neuropathic cancer pain...
- Treatment of restless legs syndrome with gabapentin: a double-blind, cross-over study
Department of Neurology, Fundacion Jimenez Diaz, Madrid, Spain
Neurology 59:1573-9. 2002
..To assess the effects of gabapentin on sensory and motor symptoms in patients with restless legs syndrome (RLS)...
- Inhibition of paclitaxel-induced A-fiber hypersensitization by gabapentin
Division of Molecular Pharmacology and Neuroscience, Nagasaki University Graduate School of Biomedical Sciences, 1 14 Bunkyo machi, Nagasaki 852 8521, Japan
J Pharmacol Exp Ther 318:735-40. 2006
- Implications and mechanism of action of gabapentin in neuropathic pain
Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, 147002, Punjab, India
Arch Pharm Res 36:237-51. 2013
..It may also act on supra-spinal region to stimulate noradrenaline mediated descending inhibition, which contributes to its anti-hypersensitivity action in neuropathic pain...
- Efficacy of gabapentin in the management of chemotherapy-induced peripheral neuropathy: a phase 3 randomized, double-blind, placebo-controlled, crossover trial (N00C3)
Ravi D Rao
Department of Medical Oncology, Mayo Clinic and Mayo Foundation, Rochester, Minnesota 55905, USA
Cancer 110:2110-8. 2007
..On the basis of these data, a multicenter, double-blind, placebo-controlled, crossover, randomized trial was conducted to evaluate the effect of gabapentin on symptoms of chemotherapy-induced peripheral neuropathy (CIPN)...
- Gabapentin in the treatment of neuropathic pain
Michael I Bennett
St Gemma s Hospice, Leeds, UK
Palliat Med 18:5-11. 2004
..In patients with neuropathic pain due to cancer, higher response rates might be observed with gabapentin when administered with opioids because of a synergistic interaction...
- Effect of systemic and intrathecal gabapentin on allodynia in a new rat model of postherpetic neuralgia
Shao Rui Chen
Department of Anesthesiology, Pennsylvania State University College of Medicine, The Milton S Hershey Medical Center, Hershey, PA 17033, USA
Brain Res 1042:108-13. 2005
..These data provide complementary new information that gabapentin administered systemically and spinally can effectively relieve tactile allodynia in this animal model of postherpetic neuralgia...
- Study of neurontin: titrate to effect, profile of safety (STEPS) trial: a narrative account of a gabapentin seeding trial
Samuel D Krumholz
Never Again Consulting LLC, Providence, Rhode Island, USA
Arch Intern Med 171:1100-7. 2011
..Seeding trials, clinical studies conducted by pharmaceutical companies for marketing purposes, have rarely been described in detail...
- Pharmacokinetics of gabapentin after a single day and at steady state following the administration of gastric-retentive- extended-release and immediate-release tablets: a randomized, open-label, multiple-dose, three-way crossover, exploratory study in hea
Depomed, Inc, 1360 O Brien Drive, Menlo Park, CA 94025, USA
Clin Ther 30:909-16. 2008
..Therefore, conventional sustained formulations would likely result in decreased bioavailability, as the dosage form would pass through the window of absorption before the drug could be completely released...
- Selective phosphodiesterase-4 inhibitors in chronic obstructive lung disease
Francisco J Soto
Division of Pulmonary and Critical Care Medicine, Medical College of Wisconsin, Milwaukee, Wisconsin 53226, USA
Curr Opin Pulm Med 11:129-34. 2005
..Novel anti-inflammatory therapies such as selective phosphodiesterase 4 (PDE4) inhibitors are in clinical development. Their potential role in the management of COPD is described in this review...
- Gabapentin in neuropathic pain syndromes: a randomised, double-blind, placebo-controlled trial
M G Serpell
University Department of Anaesthesia and Pain Management, Gartnavel General Hospital, 30 Shelly Court, G12 0YN, Scotland, Glasgow, UK
Pain 99:557-66. 2002
..This study shows that gabapentin reduces pain and improves some quality-of-life measures in patients with a wide range of neuropathic pain syndromes...
- Chemotherapy-evoked painful peripheral neuropathy: analgesic effects of gabapentin and effects on expression of the alpha-2-delta type-1 calcium channel subunit
Department of Anesthesia, Anesthesia Research Unit, McGill University, Montreal, Quebec, Canada
Neuroscience 144:714-20. 2007
- Spinal gabapentin and antinociception: mechanisms of action
Myung Ha Yoon
Department of Anesthesiology and Pain Medicine, Chonnam National University, Medical School, Gwangju, Korea
J Korean Med Sci 18:255-61. 2003
- Mechanisms of the antinociceptive action of gabapentin
Jen Kun Cheng
Institute of Pharmacology, College of Medicine, National Taiwan University, Taipei
J Pharmacol Sci 100:471-86. 2006
- Multiple-steering QM-MM calculation of the free energy profile in chorismate mutase
Departamento de Quimica Inorganica, Analítica y Química Física and INQUIMAE CONICET, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria Pab II, C1428EHA, Buenos Aires, Argentina
J Am Chem Soc 127:6940-1. 2005
..The conversion reaction of chorismate to prephenate catalyzed by the Bacillus subtilis enzyme chorismate mutase has been chosen as an illustrative example...
- Gabapentin dosing for neuropathic pain: evidence from randomized, placebo-controlled clinical trials
Department of Neurology, Anesthesiology, and Rehabilitation Medicine, University of Wisconsin Hospital and Clinics, Madison, Wisconsin 53792, USA
Clin Ther 25:81-104. 2003
..Tricyclic antidepressants are considered first-line agents for neuropathic pain, but their use is limited by unwanted side effects and a risk of cardiovascular mortality...
- Antihyperalgesic effect of systemic dexmedetomidine and gabapentin in a rat model of monoarthritis
Wei Shi Zhang
Department of Anesthesiology, Changhai Hospital, The Second Military Medical University, Shanghai, China
Brain Res 1264:57-66. 2009
..These results provide the first identification that co-application of dexmedetomidine and gabapentin may synergistically antagonize inflammatory pain, and this might prove to be beneficial in the treatment of arthritic pain...
- Gabapentin for the treatment of pain in guillain-barré syndrome: a double-blinded, placebo-controlled, crossover study
Chandra K Pandey
Department of Anaesthesiology and Critical Care Medicine, Sanjay Gandhi Postgraduate Institute of Medical Sciences, Lucknow, India
Anesth Analg 95:1719-23, table of contents. 2002
..11 +/- 21.39 to 65.53 +/- 16.17 [ micro g]) in comparison to the placebo therapy period (319.44 +/- 25.08 to 316.67 +/- 24.25 [ micro g]) (P < 0.001)...
- Anxiety-like behaviour in rats with mononeuropathy is reduced by the analgesic drugs morphine and gabapentin
Department of CNS Research, Boehringer Ingelheim Pharma GmbH and Co KG, Birkendorfer Strasse 65, Biberach an der Riss, Germany
Pain 139:349-57. 2008
..Morphine and gabapentin had no anxiolytic-like effect in sham treated animals, thus their effect on anxiety-like behaviour in the neuropathic pain model is likely indirect via their anti-nociceptive properties...
- Molecular cloning and characterization of the human voltage-gated calcium channel alpha(2)delta-4 subunit
Johnson and Johnson Pharmaceutical Research and Development, Spring House, Pennsylvania 19477 0776, USA
Mol Pharmacol 62:485-96. 2002
..Whether the alpha(2)delta-4 subunit plays a distinct physiological role in select endocrine tissues remains to be demonstrated...
- Long-term regulation of voltage-gated Ca(2+) channels by gabapentin
Myoung Goo Kang
Howard Hughes Medical Institute, Department of Physiology and Biophysics, The University of Iowa College of Medicine, 400 Eckstein Medical Research Building, Iowa City 52242, USA
FEBS Lett 528:177-82. 2002
- Down-regulation of N-type voltage-activated Ca2+ channels by gabapentin
Department of Physiology, Biophysics and Neuroscience, CINVESTAV IPN, Mexico City, Mexico
Cell Mol Neurobiol 22:185-90. 2002
..3. Consistent with this, radioligand binding experiments showed a comparable reduction in the total number of membrane HVA N-type channels after GBP treatment...
- Gabapentin in postamputation phantom limb pain: a randomized, double-blind, placebo-controlled, cross-over study
Departments of Anaesthesia and Pain Management, University Hospitals of Leicester NHS Trust, Leicester General Hosptial, Leicester, UK
Reg Anesth Pain Med 27:481-6. 2002
..Gabapentin is effective in several syndromes of neuropathic pain. Therefore, we evaluated its analgesic efficacy in phantom limb pain...
- The effects of remifentanil and gabapentin on hyperalgesia in a new extended inflammatory skin pain model in healthy volunteers
Department of Anesthesia and General Intensive Care Medicine B, University of Vienna, Vienna, Austria
Anesth Analg 98:401-7, table of contents. 2004
..With the exception of a small increase of HPTT in the sunburn (P = 0.02) gabapentin had no noticeable effect on either hyperalgesia. In conclusion, opioid analgesia was reliably demonstrated in this new extended pain model...
- Gabapentin augmentation therapy in bipolar depression
Po W Wang
Department of Psychiatry and Behavioral Sciences, Stanford University School of Medicine, Stanford, CA 94305 5723, USA
Bipolar Disord 4:296-301. 2002
..Gabapentin (GBP) may be useful in bipolar disorders, including as adjunctive therapy for bipolar depression, although controlled studies suggest inefficacy as primary treatment for mania or treatment-resistant rapid cycling...
- Presynaptic NMDA autoreceptors facilitate axon excitability: a new molecular target for the anticonvulsant gabapentin
Luz M Suárez
Servicio de Neurobiologia, Dpto de Investigación, Hospital Ramon y Cajal, Ctra de Colmenar Km 9, Madrid 28034, Spain
Eur J Neurosci 21:197-209. 2005
..These findings suggest that sodium entry through presynaptic NMDA-R channels facilitates axon excitability. The interaction of gabapentin with this newly described mechanism might contribute to its therapeutic benefits...
- Abnormal gait, due to inflammation but not nerve injury, reflects enhanced nociception in preclinical pain models
Michael J Piesla
Wyeth Research, Neuroscience Discovery Research, CN 8000, Princeton, NJ 08543, USA
Brain Res 1295:89-98. 2009
..Gait may therefore constitute an alternative and potentially clinically relevant measure of pain due to inflammation...
- Chorismic acid, a key metabolite in modification of tRNA
T G Hagervall
Department of Microbiology, Umea University, Sweden
J Bacteriol 172:252-9. 1990
..This metabolic link between intermediary metabolism and translation also exists for another member of the family Enterobacteriaceae, Salmonella typhimurium, as well as for the distantly related gram-positive organism Bacillus subtilis...
- Gastroretentive gabapentin (G-GR) formulation reduces intensity of pain associated with postherpetic neuralgia (PHN)
Christine N Sang
Translational Pain Research, Brigham and Women s Hospital, Harvard Medical School, Boston, MA 02115, USA
Clin J Pain 29:281-8. 2013
..To evaluate the safety and efficacy of a once-daily gastroretentive formulation of gabapentin (G-GR; 1800 mg)...
- Clinical development of a once-daily gastroretentive formulation of gabapentin for treatment of postherpetic neuralgia: an overview
Charles E Argoff
Albany Medical College Neurology Group, 47 New Scotland Avenue, MC 70, Physicians Pavilion, 1st Floor, Albany, NY 12208, USA
Expert Opin Drug Deliv 9:1147-60. 2012
..G-GR slowly releases the drug from the tablet to the upper small intestine, where gabapentin is best absorbed, over approximately 10 h...
- A comparison of the pharmacokinetics and pharmacodynamics of pregabalin and gabapentin
Howard N Bockbrader
Pfizer Global Research and Development, Ann Arbor, Michigan 48105, USA
Clin Pharmacokinet 49:661-9. 2010
..In conclusion, pregabalin appears to have some distinct pharmacokinetic advantages over gabapentin that may translate into an improved pharmacodynamic effect...
- The intestinal absorption mechanism of gabapentin makes it appropriate for gastroretentive delivery
Depomed Inc, 1360 O Brien Drive, Menlo Park, CA 94025, USA
Curr Clin Pharmacol 8:67-72. 2013
..The net result is a once-daily formulation of gabapentin that is well tolerated and efficacious for the treatment of PHN...
- Once-daily gastroretentive gabapentin for postherpetic neuralgia: integrated efficacy, time to onset of pain relief and safety analyses of data from two phase 3, multicenter, randomized, double-blind, placebo-controlled studies
Richard L Rauck
Center for Clinical Research, Winston Salem, North Carolina, USA
J Pain Symptom Manage 46:219-28. 2013
..Treatment options for postherpetic neuralgia (PHN), a complication of herpes zoster, are commonly unsatisfactory and associated with adverse events...
- Olefin isomerization regiochemistries during tandem action of BacA and BacB on prephenate in bacilysin biosynthesis
Jared B Parker
Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02115, United States
Biochemistry 51:3241-51. 2012
..On the other hand, acceleration of the allylic isomerization by BacB gives a mixture of the E- and Z-geometric isomers of the 7R- product, indicating some rerouting of the flux, likely through dienolate geometric isomers...
- Antinociceptive effects of gabapentin & its mechanism of action in experimental animal studies
Fatma Sultan Kilic
Department of Pharmacology, Eskisehir Osmangazi University, Medical School, Eskisehir, Turkey
Indian J Med Res 135:630-5. 2012
..Thus, clinical studies have been carried out especially for neuropathic syndroms. This study was undertaken to investigate experimentally whether gabapentin has analgesic effects in mice and rats...
- Gabapentin extended-release tablets for the treatment of patients with postherpetic neuralgia: a randomized, double-blind, placebo-controlled, multicentre study
Mark S Wallace
Center for Pain Medicine, University of California, San Diego School of Medicine, La Jolla, California 92037 765092093, USA
Clin Drug Investig 30:765-76. 2010
..Postherpetic neuralgia (PHN) is a neuropathic pain syndrome that may develop subsequent to healing of herpes zoster rash...
- Real-world treatment of post-herpetic neuralgia with gabapentin or pregabalin
Health Economics and Outcomes Research, OptumInsight, 12125 Technology Drive MN002 0258, Eden Prairie, MN 55344, USA
Clin Drug Investig 33:35-44. 2013
..This study examines dosing patterns, therapy outcomes, healthcare utilization and costs of patients with PHN who initiate treatment with gabapentin or pregabalin...
- The alpha2delta ligand gabapentin inhibits the Rab11-dependent recycling of the calcium channel subunit alpha2delta-2
Department of Neuroscience, Physiology and Pharmacology, University College London, London WC1E 6BT, United Kingdom
J Neurosci 30:12856-67. 2010
..In contrast, the internalization of α2δ-2 was unaffected by GBP. We conclude that GBP acts by preventing the recycling of α2δ-2 from Rab11-positive recycling endosomes to the plasma membrane...
- Pharmacokinetics, efficacy, and tolerability of a once-daily gastroretentive dosage form of gabapentin for the treatment of postherpetic neuralgia
Depomed Inc, Newark, California 94560, USA
J Pharm Sci 102:1155-64. 2013
..The effect of GR formulation on efficacy and the incidence of adverse events that are commonly associated with G-IR treatment in PHN patients are also discussed...
- α,β-Unsaturated monoterpene acid glucose esters: structural diversity, bioactivities and functional roles
Jason Q D Goodger
School of Botany, The University of Melbourne, Melbourne, Victoria 3010, Australia
Phytochemistry 72:2259-66. 2011
..Finally we discuss how the use of a recently developed protocol to isolate secretory cavities in a functional state could be used in conjunction with systems biology approaches to help characterize their biosynthesis and roles in plants...
- The next generation of PDE4 inhibitors
Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire, Dorval, Quebec, H9R 4P8, Canada
Curr Opin Chem Biol 5:432-8. 2001
..The recent developments in understanding PDE4 catalysis, inhibitor binding and their emetic response should facilitate the design of the next generation of PDE4 inhibitors...
- Hemodynamic effects of gabapentin in rats
Myung Ha Yoon
Department of Anesthesiology and Pain Medicine, Chonnam National University, Medical School, Gwangju, Korea
J Korean Med Sci 18:478-82. 2003
..Intracerebroventricular gabapentin increased systolic and diastolic blood pressure, but there is no statistically difference in blood pressure change according to the dose...
- Implementation of a publication strategy in the context of reporting biases. A case study based on new documents from Neurontin litigation
S Swaroop Vedula
Department of Epidemiology, Center for Clinical Trials, Johns Hopkins Bloomberg School of Public Health, 615 N, Wolfe Street, Mailroom W5010, Baltimore, MD 21205, USA
Trials 13:136. 2012
..migraine prophylaxis, treatment of bipolar disorders, neuropathic pain, and nociceptive pain...
- Synthesis of the monoterpenoid esters cypellocarpin C and cuniloside B and evidence for their widespread occurrence in Eucalyptus
Bio21 Molecular Science and Biotechnology Institute and School of Chemistry, The University of Melbourne, Victoria 3010, Australia
Carbohydr Res 345:2079-84. 2010
..The widespread occurrence of these carbohydrate monoterpenoid esters supports their roles in essential oil biosynthesis or mobilization from sites of synthesis to secretory cavity lumena...
- Tissue-specific expression and gabapentin-binding properties of calcium channel alpha2delta subunit subtypes
H C Gong
Department of Molecular Sciences, Pfizer Global Research and Development, Ann Arbor, MI 48105, USA
J Membr Biol 184:35-43. 2001
..72 +/- 9 nm). Inhibition of gabapentin binding to alpha2delta-2 by selected amino acids and gabapentin analogs produced a binding profile similar, but not identical to that of alpha2delta-1...
- The role of gabapentin in treating diseases with cutaneous manifestations and pain
Department of Dermatology, St Luke s Roosevelt Hospital Center, New York, NY 10025, USA
Int J Dermatol 42:491-5. 2003
..It appears to be a promising agent in the treatment of pain, alterations of sensation and pruritus associated with dermatological disease, but no review of these uses exists...
- The interaction of gabapentin and N6-(2-phenylisopropyl)-adenosine R-(-)isomer (R-PIA) on mechanical allodynia in rats with a spinal nerve ligation
Jong Yeon Park
Department of Anesthesiology and Pain Medicine, University of Ulsan, College of Medicine, Seoul Asan Medical Center, Songpa Gu, Seoul, Korea
J Korean Med Sci 23:678-84. 2008
..These results suggest that activation of adenosine A1 receptors at the spinal level is required for the synergistic interaction on the mechanical allodynia...
- Eucalmaidins A-E, (+)-oleuropeic acid derivatives from the fresh leaves of Eucalyptus maideni
Li Wen Tian
State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, People s Republic of China
J Nat Prod 72:1608-11. 2009
..Of the tested compounds, only quercetin showed slight anti-herpes simplex virus 1 (HSV-1) activity in vitro...
- The use of gabapentin for the treatment of postherpetic neuralgia
Pharmacy Practice, Nova Southeastern University College of Pharmacy Davie Campus, Fort Lauderdale, Florida 33328 2018, USA
Clin Ther 25:852-89. 2003
..Varicella-zoster virus causes chickenpox and can reemerge later in life to cause herpes zoster or shingles. One of the most common and disabling complications of herpes zoster is postherpetic neuralgia (PHN)...
- Efficacy and tolerability of gastric-retentive gabapentin for the treatment of postherpetic neuralgia: results of a double-blind, randomized, placebo-controlled clinical trial
Swedish Pain and Headache Center, Seattle, WA 98104, USA
Clin J Pain 25:185-92. 2009
..To determine the efficacy and safety of a gastric-retentive, extended-release gabapentin (gabapentin ER) taken once or twice daily for treatment of postherpetic neuralgia...
- False Claims Act prosecution did not deter off-label drug use in the case of neurontin
Aaron S Kesselheim
Division of Pharmacoepidemiology and Pharmacoeconomics, Department of Medicine, Brigham and Women s Hospital, Boston, Massachusetts, USA
Health Aff (Millwood) 30:2318-27. 2011
- Gabapentin inhibits calcium currents in isolated rat brain neurons
IRCCS Ospedale S Lucia, Rome, Italy
Neuropharmacology 37:83-91. 1998
- Antiallodynic effect of intrathecal gabapentin and its interaction with clonidine in a rat model of postoperative pain
J K Cheng
Department of Anesthesiology, Wake Forest University School of Medicine, Winston Salem, North Carolina, USA
Anesthesiology 92:1126-31. 2000
- Treatment of neuropathic pain: an overview of recent guidelines
Alec B O'Connor
Department of Medicine, University of Rochester School of Medicine and Dentistry, Rochester, New York 14642, USA
Am J Med 122:S22-32. 2009
..For all treatments for neuropathic pain, long-term studies, head-to-head comparisons, and studies of treatment combinations are a priority for future research...
- Gabapentin for neuropathic pain: systematic review of controlled and uncontrolled literature
M A Mellegers
University of Maastricht, The Netherlands
Clin J Pain 17:284-95. 2001
..Well-designed controlled trials may provide insight into differential symptom sensitivity to the drug...
- Gabapentin inhibits high-threshold calcium channel currents in cultured rat dorsal root ganglion neurones
K G Sutton
Department of Biology, Pfizer Global R and D, Cambridge Laboratories, Cambridge, CB2 2QB
Br J Pharmacol 135:257-65. 2002
..8. The present study is the first to demonstrate that gabapentin directly mediates inhibition of voltage-gated Ca(2+) influx in DRG neurones, providing a potential means for gabapentin to effectively mediate spinal anti-nociception...
- Pharmacological disruption of calcium channel trafficking by the alpha2delta ligand gabapentin
Laboratory for Cellular and Molecular Neuroscience, Department of Pharmacology, University College London, London WC1E 6BT, United Kingdom
Proc Natl Acad Sci U S A 105:3628-33. 2008
- Narrative review: the promotion of gabapentin: an analysis of internal industry documents
Michael A Steinman
San Francisco Veterans Affairs Medical Center and University of California, San Francisco, San Francisco, California 94143, USA
Ann Intern Med 145:284-93. 2006
..Such documents have become available through litigation concerning the promotion of gabapentin (Neurontin, Pfizer, Inc., New York, New York) for off-label uses...
- Stimulus-dependent modulation of [(3)H]norepinephrine release from rat neocortical slices by gabapentin and pregabalin
D J Dooley
Department of Neuroscience Therapeutics, Pfizer Global Research and Development, Ann Arbor, Michigan 48105, USA
J Pharmacol Exp Ther 295:1086-93. 2000
..This type of modulation of neurotransmitter release may be integral to the clinical pharmacology of these drugs...
- A comparison of the glutamate release inhibition and anti-allodynic effects of gabapentin, lamotrigine, and riluzole in a model of neuropathic pain
T J Coderre
Department of Anesthesia, McGill University, Montreal, Canada
J Neurochem 100:1289-99. 2007
..Riluzole's pronounced suppressive effects on spinal EAA levels is attributed to its established role as a glutamate release inhibitor and an enhancer of glutamate transporter activity...
- alpha2delta and the mechanism of action of gabapentin in the treatment of pain
Y P Maneuf
Cambridge Biotechnology Ltd, Biovitrum AB, Babraham Research Campus, Cambridge CB2 4AT, UK
Semin Cell Dev Biol 17:565-70. 2006
- Block by gabapentin of the facilitation of glutamate release from rat trigeminal nucleus following activation of protein kinase C or adenylyl cyclase
Y P Maneuf
Pfizer Global R and D, Cambridge Laboratories, University of Cambridge Forvie Site, Robinson Way, Cambridge CB2 2QB
Br J Pharmacol 134:237-40. 2001
..We suggest that these results may be of relevance to the antihyperalgesic properties of gabapentin, in conditions where concomitant release of substance P and CGRP produces activation of PKC and adenylyl cyclase respectively...
- Gabapentin in postherpetic neuralgia: a randomised, double blind, placebo controlled study
A S Rice
Pain Research Group, Department of Anaesthetics, Imperial College School of Medicine, Chelsea and Westminster Hospital Campus, 369 Fulham Road, London SW10 9NH, UK
Pain 94:215-24. 2001
..The most common adverse events were dizziness and somnolence, particularly during the titration phase. Thus, this study confirms the role of gabapentin as an efficacious and well-tolerated treatment for postherpetic neuralgia...
- New onset geriatric epilepsy: a randomized study of gabapentin, lamotrigine, and carbamazepine
A J Rowan
VA Medical Center, Bronx, NY 10468, USA
Neurology 64:1868-73. 2005
..To determine the relative tolerability and efficacy of two newer antiepileptic drugs, lamotrigine (LTG) and gabapentin (GBP), as compared to carbamazepine (CBZ) in older patients with epilepsy...
- Varicella zoster virus induces neuropathic changes in rat dorsal root ganglia and behavioral reflex sensitisation that is attenuated by gabapentin or sodium channel blocking drugs
Emer M Garry
Division of Veterinary Biomedical Sciences, Centre for Neuroscience Research, University of Edinburgh, Summerhall, Edinburgh EH9 1QH, UK
Pain 118:97-111. 2005
- Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease
Brian J Lipworth
Department of Medicine and Therapeutics, Asthma and Allergy Research Group, University of Dundee, Ninewells Hospital and Medical School, Dundee DD1 9SY, UK
Lancet 365:167-75. 2005
..Ultimately, clinicians will want to know whether PDE4 inhibitors are anything more than expensive "designer" theophylline, the archetypal non-selective phosphodiesterase inhibitor...
- Gabapentin for the prevention of postoperative pain after vaginal hysterectomy
Michael G F Rorarius
Department of Anaesthesiology and Intensive Care, Tampere University Hospital, P O Box 2000, 33521 Tampere, Finland
Pain 110:175-81. 2004
..No preoperative differences between the two groups were encountered with respect to the side effects of the premedication. However, 15 mg oxazepam was more effective in relieving preoperative anxiety than 1200 mg gabapentin...
- Gabapentin reverses microglial activation in the spinal cord of streptozotocin-induced diabetic rats
Neurorestoration Group, Wolfson Centre for Age Related Diseases, King s College London, London SE1 1UL, UK
Eur J Pain 13:807-11. 2009
..Consequently, spinal microglial activation is a key mechanism underlying diabetic neuropathy. Furthermore, we suggest that Gabapentin may exert its anti-allodynic actions partially through alterations of microglial cell function...
- Gabapentin selectively reduces persistent sodium current in injured type-A dorsal root ganglion neurons
Rui Hua Yang
epartment of Occupational and Environmental Health, The Fourth Military Medical University, Xi an 710032, PR China
Pain 143:48-55. 2009
..The results suggest that GBP decreased the amplitude of resonance and abolished the SMPO of A-type DRG neurons through the inhibition of I(NaP), and thus inhibited the SMPO dependent repetitive and bursting firings...
- Alternative splicing of the Ca2+ channel beta4 subunit confers specificity for gabapentin inhibition of Cav2.1 trafficking
Patrice M Mich
Department of Clinical Sciences, College of Veterinary Medicine, Cornell University, Ithaca, NY 14850, USA
Mol Pharmacol 74:904-12. 2008
..This mechanism may help to explain why gabapentin is both effective and selective in the treatment of neuropathic pain states that involve up-regulation of alpha2delta subunits...
- Differential analgesic effects of morphine and gabapentin on behavioural measures of pain and disability in a model of osteoarthritis pain in rats
Jean Laurent Vonsy
University College London, Neuroscience, Physiology and Pharmacology, London WC1E 6BT, UK
Eur J Pain 13:786-93. 2009
..In terms of translational research, the effects of morphine and gabapentin validate the model and suggest trials of these therapeutic approaches in OA patients...
- Gabapentin in traumatic nerve injury pain: a randomized, double-blind, placebo-controlled, cross-over, multi-center study
Torsten E Gordh
Multidisciplinary Pain Center, Uppsala University Hospital, S 751 85 Uppsala, Sweden
Pain 138:255-66. 2008
..023) and Clinician (p=0.037) Global Impression of Change indicated a better response with gabapentin compared with placebo. Gabapentin was well tolerated. The most common adverse effects were dizziness and tiredness...
- The effect of the palmitoylethanolamide analogue, palmitoylallylamide (L-29) on pain behaviour in rodent models of neuropathy
V C J Wallace
Pain Research Group, Department of Anaesthetics, Pain Medicine and Intensive Care, Faculty of Medicine, Imperial College London, Chelsea and Westminster Hospital Campus, 369 Fulham Road, London, UK
Br J Pharmacol 151:1117-28. 2007
- Nummular headache: another case treated with gabapentin
J Headache Pain 8:137-8. 2007
- The effects of intrathecal gabapentin on spinal morphine tolerance in the rat tail-flick and paw pressure tests
Department of Pharmacology and Toxicology, Kingston General Hospital, Queen s University, Ontario, Canada
Anesth Analg 99:1180-4, table of contents. 2004
..Future studies are required to examine the respective roles of supraspinal and peripheral sites of GBP-morphine interaction and to investigate the mechanisms underlying the action of GBP on opioid tolerance...
- Effectiveness of gabapentin for the treatment of behavioral disorders in dementia
Division of Geriatric Psychiatry, University of Toronto, Ontario, Canada
J Clin Psychopharmacol 20:90-3. 2000
..Gabapentin may have a role in treating a subgroup of dementia patients with severe behavioral disorders who have not responded to neuroleptics...
- Neurotransmitter mechanisms in gabapentin antinociception
R K Dixit
Department of Pharmacology, PGIMER, Chandigarh, India
Pharmacology 65:198-203. 2002
..c.) antinociception except for L-arginine which increased the pain score from 1.68 +/- 0.29 (gabapentin) to 2.29 +/- 0.41. Results suggest the involvement of L-arginine nitric oxide pathways in gabapentin antinociception...
- The effects of GABA(B) agonists and gabapentin on mechanical hyperalgesia in models of neuropathic and inflammatory pain in the rat
Novartis Institute for Medical Sciences, 5 Gower Place, London WC1E 6BN, UK
Pain 90:217-26. 2001
..These data indicate that CGP35024 and L-baclofen modulate nociceptive transmission in the spinal cord to inhibit neuropathic hyperalgesia, and that CGP35024 has a therapeutic window for antihyperalgesia over spasmolysis...
- Gabapentin and pregabalin can interact synergistically with naproxen to produce antihyperalgesia
Robert W Hurley
Department of Anesthesia and Critical Care, and Committee on Neurobiology, University of Chicago, Illinois, USA
Anesthesiology 97:1263-73. 2002
..This study characterized the manner in which gabapentin or pregabalin interacts with naproxen to suppress thermal hyperalgesia and inflammation in the carrageenan model of peripheral inflammation...
- Gabapentin-induced paradoxical exacerbation of psychosis in a patient with schizophrenia
Can J Psychiatry 47:975-6. 2002
- Gabapentin enhances the analgesic effect of morphine in healthy volunteers
Dr Margarete Fischer Bosch Institut fuer Klinische Pharmakologie, Stuttgart, Germany
Anesth Analg 91:185-91. 2000
..These results and the good tolerability of GBP should favor clinical trials investigating the clinical relevance of the combination of morphine and GBP for treating severe pain...
- The use of gabapentin in chronic cluster headache patients refractory to first-line therapy
Department of Neurology, Charite Universitatsmedizin Berlin, Berlin
Eur J Neurol 14:694-6. 2007
..We conclude that gabapentin may be offered as treatment trial in patients refractory to first-line treatment. However, patients may fail to respond to treatment and drug tolerance may occur with time...
- Gabapentin suppresses spasticity in the spinal cord-injured rat
P H Kitzman
Department of Rehabilitation Science, The University of Kentucky, 210D Charles T Wethington Building, 900 South Limestone Avenue, Lexington, KY 40536 0200, USA
Neuroscience 149:813-21. 2007
..The present study examined the efficacy of gabapentin, an agent that has been shown to reduce glutamate release, in managing spasticity within the tail musculature...
- Effects of systemic carbamazepine and gabapentin on spinal neuronal responses in spinal nerve ligated rats
Department of Pharmacology, University College London, UK
Pain 75:261-72. 1998
..Further studies at the spinal level may shed light on the physiology and pharmacology of the aberrant processes associated with neuropathic pain...
- Reduction of postherpetic neuralgia in herpes zoster
M Vander Straten
Department of Dermatology, University of Texas Medical Branch, UTMB Center for Clinical Studies, 2060 Space Park Drive, Galveston, TX 77058, USA
J Cutan Med Surg 5:409-16. 2001
..Widespread use of the varicella vaccine may lead to secondary reductions in PHN in the distant future...
- Antiinflammatory effects of the phosphodiesterase-4 inhibitor cilomilast (Ariflo) in chronic obstructive pulmonary disease
Department of Pulmonology, Leiden University Medical Centre, Leiden, The Netherlands
Am J Respir Crit Care Med 168:976-82. 2003
..Phosphodiesterase-4 inhibitors represent a promising new class of substances for use in antiinflammatory treatment of this disease...
- Persistent primary thunderclap headache responsive to gabapentin
Department of Neurology, Mayo Clinic, 200 First Street SW, Rochester, MN 55905, USA
J Headache Pain 7:419-21. 2006
..Whether gabapentin may help other primary thunderclap headache sufferers or not remains unclear. Further research is needed...
- An East-West approach to the management of central post-stroke pain
Hwee Ling Yen
Department of Rehabilitation Medicine, Tan Tock Seng Hospital, Singapore, Singapore
Cerebrovasc Dis 16:27-30. 2003
..To the best of our knowledge, the use of acupuncture for the treatment of CPSP has not been previously reported...
- The effects of gabapentin on different ligand- and voltage-gated currents in isolated cortical neurons
Istituto di Ricovero e Cura a Carattere Scientifico IRCCS, Ospedale Santa Lucia, Via Ardeatina 306, 00179, Rome, Italy
Epilepsy Res 43:239-48. 2001
..These unconventional effects might underlie its efficacy in a variety of diseases which involve periodic discharge patterns as neuropathic pain or essential tremor...
- Calcium channel alpha(2)delta subunits-structure and Gabapentin binding
, , Germany
Mol Pharmacol 59:1243-8. 2001
..alpha(2)delta-1 and alpha(2)delta-2, but not alpha(2)delta-3, were found to bind gabapentin. The K(d) value of gabapentin binding to alpha(2)delta-2 was 153 nM compared with the higher affinity binding to alpha(2)delta-1 (K(d) = 59 nM)...
- A placebo-controlled trial of gabapentin for painful HIV-associated sensory neuropathies
Department of Neurology, Charite Campus Mitte, Schumannstr 20 21, D 10117 Berlin, Germany
J Neurol 251:1260-6. 2004
..The pathogenesis is unknown and the treatment very limited. Gabapentin (GBP) is effective in painful diabetic neuropathy and postherpetic neuralgia and its effectiveness on painful HIV-SN has been reported anecdotally...
- Modulation of K+-evoked [3H]-noradrenaline release from rat and human brain slices by gabapentin: involvement of KATP channels
T M Freiman
, Neurozentrum, Freiburg, Germany
Naunyn Schmiedebergs Arch Pharmacol 363:537-42. 2001
- Gabapentin: an alternative to the cyclooxygenase-2 inhibitors for perioperative pain management
Department of Anaesthesiology, Trakya University, Edirne, Turkey
Anesth Analg 102:175-81. 2006
..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...
- Inhibitory mechanisms of gabapentin, an antiseizure drug, on platelet aggregation
Chi Feng Pan
Graduate Institute of Medical Sciences and Topnotch Stroke Research Center, Taipei Medical University, Taipei, Taiwan
J Pharm Pharmacol 59:1255-61. 2007
..Thus, it is possible that gabapentin treatment, alone or in combination with other antiplatelet drugs, may induce or potentiate inhibition of platelet aggregation, which may affect haemostasis in-vivo...
- Gabapentin affects glutamatergic excitatory neurotransmission in the rat dorsal horn
Department of Physiology, Chiba University School of Medicine, 1 8 1 Inohana, Chuo Ku, Chiba shi, Japan
Pain 85:405-14. 2000
..The antinociceptive effects of GBP may involve the inhibition of the release of excitatory amino acids from presynaptic terminals...
- Role of spinal voltage-dependent calcium channel alpha 2 delta-1 subunit in the expression of a neuropathic pain-like state in mice
Department of Toxicology, Hoshi University School of Pharmacy and Pharmaceutical Sciences, 2 4 41 Ebara, Shinagawa ku, Tokyo, 142 8501, Japan
Life Sci 80:2015-24. 2007
..Furthermore, the present data provide evidence that the neuropathic pain may be effectively controlled by repeated treatment with GBP at the early stage...