• The Korean Journal of Pain
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• 제14권1호
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• pp.98-103
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• 2001

Neuropathic pain originating from multiple condition of nerve cell injury is common, but is difficult to treat. Even though many drugs such as anti-convulsants, anti-depressants, NSAIDs, opioids have been used, their clinical analgesic action were not satisfactory due to occur severe side effects. Gabapentin was introduced in 1994 as a novel antiepileptic drug and has been used to treat partial seizure. After 1995 gabapentin treatment for reflex sympathetic dystrophy (RSD) started, 45% of the reports about the analgesic efficacy of gabapentin were restricted to the treatments of non-epileptic pain syndrome. This drug is preferred to treat neuropathic pain because of a lower incidence of its side effects than those of other anti-convulsants and anti-depressants. For evaluating it's analgesic efficacy, the changes in the patients' subjective pain intensity was measured by the score on the visual analogue scale (VAS) and patient's objective pain intensity by measuring the skin temperature via infrared thermography were investigated respectively. Side effects of gabapentin were look into. We observed successful relief of neuropathic pain in the three patients which included post-herpetic neuraligia, complex regional pain syndrome (CRPS) and diabetic neuropathic pain, and the side effects of gabapentin were at acceptable levels.

• The Korean Journal of Pain
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• 제13권1호
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• pp.101-104
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• 2000

Since conventional analgesics have showed limited therapertic value in the treatment of painful neuropathy, the new anticonvulsant gabapentin, has been tried and turned out to be effective and safe in the treatment for various forms of neuropathic pain. The basic pathophysiology of neuropathic pains is abnormal neuronal hyperactivity similar to epileptic seizures. Therefore, we could expect that neuropathic pain would be suppressed by anticonvulsants which inhibit abnormal excessive neuronal output and nerve conduction. This report include effective pain relief in four cases of neuropathic pain with gabapentin without any significant complications.

• Carbon letters
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• 제27권
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• pp.50-63
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• 2018

An imprinted potentiometric sensor was developed for direct and selective determination of gabapentin. Sensor is based on carbon paste electrode adapted by graphene oxide that is decorated with silver nanoparticles and mixed with molecularly imprinted polymers nanoparticles using gabapentin as a template molecule. The synthesized nanoparticles were characterized by Fourier transmission infrared spectroscopy, transmission electron microscopy and X-ray diffraction. Under optimal experimental conditions, the studied sensor exhibited high selectivity and sensitivity with LOD of $4.8{\times}10^{-11}mol\;L^{-1}$. It provided a wide linearity range from $1{\times}10^{-10}$ to $1{\times}10^{-3}mol\;L^{-1}$ and high stability for more than 3 mo. The sensor was effectively used for the determination of gabapentin in pharmaceutical tablets and spiked plasma samples.

• Tuberculosis and Respiratory Diseases
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• 제81권3호
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• pp.167-174
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• 2018

Despite recent clinical guidelines, the optimal therapeutic strategy for the management of refractory chronic cough is still a challenge. The present systematic review was designed to assess the evidence for efficacy and safety of gabapentin in the treatment of chronic cough. A systematic search of PubMed, Embase, Cochrane Library databases, and publications cited in bibliographies was performed. Articles were searched by two reviewers with a priori criteria for study selection. Seven relevant articles were identified, including two randomized controlled trials, one prospective case-series designed with consecutive patients, one retrospective case series of consecutive patients, one retrospective case series with unknown consecutive status, and two case reports comprising six and two patients, respectively. Improvements were detected in cough-specific quality of life (Leicester Cough Questionnaire score) and cough severity (visual analogue scale score) following gabapentin treatment in randomized controlled trials. The results of prospective case-series showed that the rate of overall improvement of cough and sensory neuropathy with gabapentin was 68%. Gabapentin treatment of patients with chronic cough showed superior efficacy and a good safety record compared with placebo or standard medications. Additional randomized and controlled trials are needed.

• Journal of Pharmaceutical Investigation
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• 제39권4호
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• pp.269-273
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• 2009

The objective of this investigation was to develop a gastro-retentive(GR) dosage form of gabapentin and was to evaluate of its dissolution characteristics. GR tablet consists of expandable core tablet matrix and semi-permeable membrane coating. Poloxamer 407 and sodium bicarbonate were used to prepare the core matrix. Polyvinly acetate dispersion (Kollicoat $SR30D^{(R)}$) and polyvinyl alcohol-polyethylene glycol copolymer ((Kollicoat $IR^{(R)}$)) were employed to form the semi-permeable membrane. The GR tablets significantly expanded up to fivefold in simulated gastrointestinal fluids with no apparent damage of the coating membrane over 12 hours. Also, the swelling rate was controllable with the amount of sodium bicarbonate. The drug release was observed to be substantially sustained based on coating level. The release rate of gabapentin from the GR tablet was gradually slowed down as the coasting amount was increased. The gabapentin GR tablet with 8% coating level showed a pseudo-zero order release kinetics over 12 hours. These results suggest that this swellable GR tablet system having semi-permeable membrane coating can be applicable for hydrophilic drug substances like gabapentin.

• 약학회지
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• 제52권3호
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• pp.195-200
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• 2008

Gabapentin, [1-(aminomethyl) cyclohexaneacetic acid], a structural analog of $\gamma$-aminobutyric acid (GABA), is being developed for the treatment of epilepsy. Unlike GABA, gabapentin crosses the blood-brain barrier after systemic administration. Gabapentin is an effective antiepileptic drug in patients with partial and secondarily generalized seizures who are uncontrolled with use of existing anticonvulsant drug therapy. The purpose of the present study was to evaluate the bioequivalence of two gabapentin 400 mg capsules, $Neurontin^{(R)}$ capsule 400 mg (Pfizer Inc.) and Gabatin capsule 400 mg (Korean Drug Co. Ltd), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of gabapentin from the two gabapentin formulations in vitro was tested using KP VIII Apparatus II method with various dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty six healthy male subjects, 23.58$\pm$1.50 years in age and 66.74$\pm$8.31 kg in body weight, were divided into two groups and a randomized 2$\times$2 cross-over study was employed. After one capsule containing 400 mg as gabapentin were orally administered, blood was taken at predetermined time intervals and the concentrations of gabapentin in serum were determined using HPLC with fluorescence detector. The dissolution profiles of two formulations were similar at all dissolution media. In addition, the pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, $Neurontin^{(R)}$ capsule 400 mg, were 2.04, -3.68 and 16.79% for $AUC_t$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., log 0.91$\sim$log 1.16 and log 0.87$\sim$log 1.11 for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Gabatin capsule 400 mg was bioequivalent to $Neurontin^{(R)}$ capsule 400 mg.

• Journal of Dental Anesthesia and Pain Medicine
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• 제22권5호
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• pp.377-385
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• 2022

Background: Postoperative endodontic pain is an enigma for the dentist. This study aimed to evaluate the analgesic effect of 300 mg gabapentin or 75 mg pregabalin in reducing postoperative endodontic pain compared with a placebo. Methods: Ninety patients who needed root canal treatment with an initial numerical rating scale (NRS) pain score of > 4 (T0) were randomly divided into three groups (n=30). Patients were then administered either 300 mg gabapentin (group A), 75 mg pregabalin (group B), or a placebo (group C) 30 min prior to the start of endodontic treatment. A single operator performed single-visit endodontics, and pain was evaluated immediately after endodontic treatment (T1) and at 4 h (T2), 8 h (T3), 12 h (T4), 24 h (T5), 48 h (T6), and 72 h (T7) using the NRS. Ibuprofen/paracetamol (400 mg/325 mg) was administered as a rescue dose if needed. Results: Pregabalin performed significantly better when compared with gabapentin at all time points except at 72 h after treatment (P=0.170). The placebo group showed significantly higher pain scores than the other two groups. The percentage of pain relief was maximum for pregabalin (92.1%), followed by gabapentin (87.6%) and placebo (69.1%) at 72 h after treatment completion. Conclusion: This study showed that pretreatment with a single dose of pregabalin and gabapentin both had greater analgesic effects than a placebo. They can be effectively used to reduce postoperative endodontic pain.

• Biomolecules & Therapeutics
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• 제21권2호
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• pp.126-131
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• 2013

Neuropathic pain is a chronic pain disorder caused by nervous system lesions as a direct consequence of a lesion or by disease of the portions of the nervous system that normally signal pain. The spinal nerve ligation (SNL) model in rats that reflect some components of clinical pain have played a crucial role in the understanding of neuropathic pain. To investigate the direct effects of gabapentin on differential gene expression in cultured dorsal root ganglion (DRG) cells of SNL model rats, we performed a differential display reverse transcription-polymerase chain reaction analysis with random priming approach using annealing control primer. Genes encoding metallothionein 1a, transforming growth factor-${\beta}1$ and palmitoyl-protein thioesterase-2 were up-regulated in gabapentin-treated DRG cells of SNL model rats. The functional roles of these differentially expressed genes were previously suggested as neuroprotective genes. Further study of these genes is expected to reveal potential targets of gabapentin.

• The Korean Journal of Pain
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• 제18권2호
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• pp.222-225
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• 2005

Hiccups are due to an intermittent clonic spasm of the diaphragm. In most cases, hiccups are self-limiting disease, but persistent hiccups may be related to the presence of serious underlying systemic disease. Two patients who had persistent hiccups that were not controled by conventional methods and medications were referred to the pain clinic. We administered a single oral medication of gabapentin, and then the hiccups disappeared in both cases. We concluded that gabapentin should be considered as an alternative therapy to control persistent or intractable hiccup. It could be particularly useful for those patients with solid malignancies, either alone or as an "add-on therapy" with other oral agents.

• 대한족부족관절학회지
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• 제8권1호
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• pp.58-63
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• 2004

Purpose: The purpose of this study is to evaluate the effectiveness of low-dose gabapentin for interdigital neuroma. Metrials and Methods: Between April 2000 and June 2003, 32 patients (39 feet) with interdigital neuroma were treated with using low-dose gabapentin. Two of the 32 patients were male, and thirty were female, and the average age was 47.4 years. The follow-up was 6 to 44months (mean 15.1 months). All cases were diagnosed by physical examination and ultrasonography or MRI. Low-dose gabapentin (300-600 mg) was prescribed and shoe modification was recommended. The patients were evaluated through questionnaire. Results: Neuroma was found in twenty one cases at the third intermetatarsal space, and thirteen at the second intermetatarsal space. The sensitivity of ultrasonography was 96% and that of MRI was 79%. Overall satisfaction was rated as excellent or good by 18 cases (57%). Average pain relief ratio was 50.3%, and in 14 cases, more than 80% of pain relief was noted. Nine (28%) of 32 patients showed they had no activity restrictions, such as daily activities or work, whereas 8 (25%) had mild restrictions and 15 (47%) had major restrictions. Twelve of 15 patient with major restrictions had been treated operatively (neurectomy; 10 cases, decompression; 2 cases). One case had gastrointestinal problem. Conclusion: Low-dose gabapentin for interdigital neuroma was one of the effective conservative treatments. The operation may be preserved for patient with the persist symptoms, nevertheless the conservative treatments and use of low-dose gabapentin.