• 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.

• The Korean Journal of Pain
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• 제12권2호
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• pp.188-190
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• 1999

Background: The goal of this study was to evaluate the effects of gabapentin on postherpetic neuralgia. Gabapentin is a known anti-seizure medication, whose cellular mechanism of action is not well understood. Unlike other anticonvulsant, gabapentin has the advantage of a low toxicity and favorable side effect profile. If has been recently recommended for use in treatment of neuropathic pain. Methods: Twelve patients with a diagnosis of postherpetic neuralgia were prescribed gabapentin after failure of routine therapeutic regimens. The dose of gabapentin ranged 300~1800 mg per day, in three divided doses. If initial dose was ineffective and no side effects were noted, the dosages was increased by 300 mg a day in divided doses, to the maximum level for 2 weeks. Patients were evaluated for analgesia using visual analogue scale (VAS) pain score (0; no pain, 10; worst possible pain) and possible side effects. Results: A significant decrease in pain scores with gabapentin were noted. There were several mild side effects such as dizziness, somnolence, dry mouth, constipation and facial edema, without need of special treatment. Conclusions: Gabapentin may be a useful adjunct for treating intractable postherpetic neuralgia with a minimal side effects.

• The Korean Journal of Pain
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• 제12권2호
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• pp.242-245
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• 1999

Gabapentin is an oral antiepileptic agent with an unknown mechanism of action. There have been many proposed uses for gabapentin, including neuropathic pain, reflex sympathetic dystrophy, postherpetic neuralgia, midscapular pain secondary to radiation myelopathy and migraine prophylaxis. This report presents patients who were treated with gabapentin when other pharmacologic interventions failed to relieve neuropathic pain 3 patients with neuropathic pain were included among these cases. All patients were started on 200 mg gabapentin. The maximum dose required for pain relief was between 800 mg and 2400 mg. Gabapentin may be a useful adjunct for treating neuropathic pain with minimum of side effects.

• 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.

• 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.

• The Korean Journal of Pain
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• 제34권1호
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• pp.4-18
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• 2021

Except for carbamazepine for trigeminal neuralgia, gabapentinoid anticonvulsants have been the standard for the treatment of neuropathic pain. Pregabalin, which followed gabapentin, was developed with the benefit of rapid peak blood concentration and better bioavailability. Mirogabalin besylate (DS-5565, Tarlige®) shows greater sustained analgesia due to a high affinity to, and slow dissociation from, the α2δ-1 subunits in the dorsal root ganglion (DRG). Additionally, it produces a lower level of central nervous system-specific adverse drug reactions (ADRs), due to a low affinity to, and rapid dissociation from, the α2δ-2 subunits in the cerebellum. Maximum plasma concentration is achieved in less than 1 hour, compared to 1 hour for pregabalin and 3 hours for gabapentin. The plasma protein binding is relatively low, at less than 25%. As with all gabapentinoids, it is also largely excreted via the kidneys in an unchanged form, and so the administration dose should also be adjusted according to renal function. The equianalgesic daily dose for 30 mg of mirogabalin is 600 mg of pregabalin and over 1,200 mg of gabapentin. The initial adult dose starts at 5 mg, given orally twice a day, and is gradually increased by 5 mg at an interval of at least a week, to 15 mg. In conclusion, mirogabalin is anticipated to be a novel, safe gabapentinoid anticonvulsant with a greater therapeutic effect for neuropathic pain in the DRG and lower ADRs in the cerebellum.

• 수면정신생리
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• 제25권1호
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• pp.5-8
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• 2018

Restless legs syndrome (RLS) is a sleep disorder characterized by an urge to move the legs or arms and uncomfortable paresthesia in the legs. Treatment of RLS can be various depending on the causes, severity, and frequency of the symptoms. In the case of secondary RLS, it is important to identify and manage the cause of RLS. Dopamine agonists have been used as firstline treatments for primary RLS treatment. However, due to augmentation, which is a common side effect of dopamine agonists, recent treatment guidelines are changing to prefer to anticonvulsants such as pregabalin and gabapentin. Iron, opioid, or benzodiazepine may be used when anticonvulsants or dopamine agonists are not adequately treated. Because RLS is a chronic disease, it is essential to establish a long-term treatment plan considering both efficacy and side effects.