• The Korean Journal of Pain
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• 제30권3호
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• pp.183-191
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• 2017

Background: Current therapy for the treatment of neuropathic pain is often unsatisfactory. Considerable variation in treatment pattern still exists in spite of availability of sufficient literature from various guidelines. Recent Indian market data suggested that the utilization (sale) of drugs such as amitriptyline, pregabalin, and gabapentin was more for low-dose unit packs than that of the high-dose unit packs, raising the belief that these drugs are prescribed at a lower dose than is actually recommended in the guidelines. To test this hypothesis, a survey was conducted across speciality throughout the country to observe the prescription pattern of these drugs amongst the health care providers in India. Methods: Three hundred fifty survey forms were distributed of which 281 forms were included for analysis. Results: It was observed that the commonly used initiation and maintenance dose for amitriptyline, pregabalin, and gabapentin was 5-10 mg/day, 50-75 mg/day, and 100-300 mg/day, respectively. The reason to select the lower dosages was to have a balancing effect to achieve good efficacy with minimum side effects. Care-givers reported no side effects/not many side effects as a reason in 22.2%, 16.88%, and 23.86% patients with amitriptyline, pregabalin, and gabapentin, respectively. Sedation and giddiness were commonly reported with all three drugs. Conclusions: Commonly prescribed drugs for management of neuropathic pain, such as amitriptyline, pregabalin, and gabapentin are preferred at lower doses in Indian clinical settings. Acceptable efficacy and low tolerance to the standard dosage is believed to be the reason behind the prescribed dose.

• Journal of Oral Medicine and Pain
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• 제39권3호
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• pp.96-99
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• 2014

Purpose: The objective of this retrospective pilot study was to evaluate the effectiveness of Gabapentin in patients with primary burning mouth syndrome (BMS). Methods: Ten subjects were diagnosed with primary BMS (8 women and 2 men). The mean age was 60.1 years. They had clinical examination to exclude local factors such as the presence of Candida species, xerostomia, lichen planus, etc. They also underwent hematological examination to exclude secondary BMS due to systemic disorders. Pain was assessed by patients on an 11-point numerical rating score system (0 to 10). Gabapentin was administered at a starting dose of 300 mg/day, slowly titrated up to maximum of 1,800 mg/day. All patients were treated for 4 weeks. Results: One half of the patients (n=5) obtained reduction in pain over the treatment period. Four patients reported no reduction in pain symptoms. One patient reported that symptoms were worsening. The average pain score before the treatment was 6.3 and after the treatment was 5.25. No significant relationship was detected between pretreatment and posttreatment pain score. Only one patient noted mild side effect (dizziness). Conclusions: This retrospective pilot study provides no preliminary evidence that Gabapentin has effect in the management of BMS. However, further research (well-designed, randomized, and controlled trial with large sample) would be needed to investigate the efficacy of Gabapentin in treatment of BMS.

• 약학회지
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• 제52권4호
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• pp.299-305
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• 2008

Gabapentin, 1-(aminomethyl) cyclohexaneacetic acid, is a amino acid derivative, and is clinically effective in the treatment of neuropathic pain and partial seizures of epilepsy as a complementary therapy. The purpose of the present study was to evaluate the bioequivalence of two gabapentin tablets, $Neurontin^{R}$ tablet 800 mg (Pfizer Pharmaceuticals Co., Ltd.) and Gabapenin tablet 800 mg (Hanmi Pharm. 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 0.06 M HCI dissolution media. Twenty six healthy male subjects, $23.85{\pm}2.24$ years in age and $69.40{\pm}11.11$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ crossover study was employed. After a single tablet containing 800 mg as gabapentin was orally administered, blood samples were 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 in the tested dissolution media. 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, $Neurontin^{R}$, were 1.28%, 0.63% and 0.62% 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., $log0.9097{\sim}log1.1598$ and $log0.8919{\sim}log1.1262$ for $AUC_{t}$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Gabapenin tablet 800 mg was bioequivalent to $Neurontin^{R}$ tablet 800 mg.

• 한국임상약학회지
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• 제16권1호
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• pp.63-68
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• 2006

Gabapentin, 1-(aminomethyl-1-cyclohexyl)acetic acid, is anew antiepileptic drug related to ${\gamma}-aminobutyric$ acid(GABA) currently being introduced in therapy worldwide. The bioavailability and pharmacokinetics of gabapentin capsules were examined in 22 volunteers who received a single oral dose in the fasting state by randomized balanced $2{\times}2$ crossover design. After dosing, blood samples were collected for a period of 24 hours and analyzed by liquid chromatography-tandem mass spectrometry (LC/MS/MS). Time course of plasma gabapentin concentration was analyzed with non-compartmental and compartmental approaches. $WinNonlin^{(R)}$, the kinetic computer program, was used for compartmental analysis. One compartment model with first-order input, first-order output with no lag time and weighting by $1/(predieted\;y)^2$ was chosen as the most appropriate pharmacokinetic model for the volunteers. The major pharmacokinetic parameters $(AUC_{0-24hr},\;AUC_{inf},\;C_{max}\;and\;T_{max})$ and other parameters $(K_a,\;K_{el},\;V_d/F\;and\;Cl/F)$ of $Gapentin^{TM}$ (test drug) and $Neurontin^{TM}$ (reference drug) were estimated by non-compartmental analysis and compartmental analysis. The 90% confidence intervals of mean difference of logarithmic transformed $AUC_{0-24hr}\;and\;C_{max}$ were $log(0.9106){\sim}log(1.l254)\;and\;log(0.8521){\sim}log(1.0505)$, respectively. It shows that the bioavailability of the test drug is equivalent with that of the reference drug. There was no statistically significant difference between the two drugs in all pharmacokinetic parameters.

• 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.

• Journal of Photoscience
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• 제12권3호
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• pp.113-117
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• 2005

Spectroscopic investigations on the interaction of gabapentin (GBP) with bovine serum albumin (BSA) were reported. The association constant of GBP-BSA system was determined at different temperatures (298, 302, 306 and 311 K) based on the fluorescence quenching results. The GBP was found to quench the fluorescence of BSA through static mechanism. Thermodynamic parameters, the standard enthalpy change, $({\Delta}H^o)$ and the standard entropy change $({\Delta}S^o)$ were observed to be $-9.61{\pm}0.008\;kJ\;mol^{-1}$ and $3.58{\pm}0.011\;Jmol^{-1}K{-1}$ respectively. These indicated that the hydrophobic and electrostatic forces played a role in the interaction of GBP with BSA. The negative value of ${\Delta}G^o$ revealed that the binding reaction is spontaneous. The circular dichroism studies indicated the conformational changes in BSA upon interaction with GBP. The effect of some metal ions on the binding constant was also investigated.

• Journal of Korean Neurosurgical Society
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• 제43권5호
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• pp.237-238
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• 2008

Myoclonus is a rare side effect of gabapentin (GBP) and has been reported in patients with preexisting myoclonus, mental retardation, chronic static encephalopathy, diffuse brain damage, impaired renal function, or end stage renal disease. We report a case of myoclonus in a patient with normal renal function and no previous disorders. A 69-year-old female underwent diskectomy and foraminotomy at the left L4-L5 level. Post-operatively, she complained of paresthesia in her left leg, which was thought to be due to root manipulation during surgery. To relieve the paresthesia, she was given tramadol, an oral opioid agonist, and GBP. One week after GBP was increased to 900 mg per day, myoclonus developed, which severely impaired her normal activity. Her symptoms resolved 2 days after discontinuation of GBP. The coadministration of tramadol and GBP may mutually enhance the myoclonic potential of each drug. The causal relationship between GBP and myoclonus was suggested by cessation of myoclonus after GBP discontinuation despite continued therapy with tramadol.

• 대한암한의학회지
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• 제28권1호
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• pp.33-44
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• 2023

목적: 항암유발말초신경병증은 암 환자가 겪는 흔한 항암 부작용이나 현재까지 효과적으로 알려진 치료법은 없다. 본 연구의 목적은 항암유발말초신경병증에 대한 침 치료와 가바펜틴의 병용 요법의 효과와 안전성을 평가하는 것이다. 방법: 항암유발말초신경병증을 겪고 있는 24명의 암 환자를 침 치료 단독군 (AG, acupuncture group)과 침과 가바펜틴의 병용요법군 (CG, combined acupuncture and gabapentin group)으로 무작위 배정하였다. 두 그룹 모두 침 치료는 주 3회, 4주간 수행하였다. 병용 요법군은 침 치료와 더불어 1일 900mg의 가바펜틴을 복용하도록 하였다. 치료 효과는 Neuropathic Pain Symptom Inventory (NPSI), visual analogue scale (VAS), European Organization for Research and Treatment of Cancer Quality of Life Questionnaire-Chemotherapy-Induced Peripheral Neuropathy 20 items (EORTC-CIPN20)를 이용하여 측정하였다. 치료로 인한 부작용은 대상자가 방문할 때마다 조사하였다. 결과: 총 23명의 대상자(AG, n=12; CG, n=11)의 평가지표를 분석한 결과, 치료 4 주 후 침 치료 단독군은 NPSI 점수가 44.33±25.04에서 30.58±21.55으로 감소하였고, 병용 요법군은 30.55±25.59에서 18.64±19.42로 감소하였으며, 두 군 모두 통계적으로 유의미하게 감소하였다(p<0.001). VAS점수는 침 치료 단독군에서는 4.79±2.17 에서 3.42±2.49으로 감소하였고, 병용 요법군에서는 3.55±2.07에서 2.73±2.49 로 감소하였다(p<0.05). 치료 효과는 치료 완료 2주후까지 지속되었으며, 두 군간의 유의미한 차이는 없었다. EORTC-CIPN20은 침 치료 단독군은 30.27±18.87에서 20.84±16.35으로 감소하여(p<0.01), 두 군 모두에서 삶의 질이 향상되었다. 결론: 본 연구로 침 치료와 가바펜틴의 병용 요법이 항암유발말초신경병증 환자의 증상 및 삶의 질 개선에 효과적이며 안전한 치료법임을 확인하였다. 그러나 침 치료와 가바펜틴의 시너지 효과에 대해서는 확인 할 수 없었으며, 이를 확인하기 위해 추가적인 연구가 필요할 것으로 사료된다.

• 대한약학회:학술대회논문집
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• 대한약학회 2001년도 Proceedings of International Convention of the Pharmaceutical Society of Korea
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• pp.163.1-163.1
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• 2001

• The Korean Journal of Physiology and Pharmacology
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• 제21권6호
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• pp.657-666
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• 2017

Paclitaxel, a chemotherapeutic drug, induces severe peripheral neuropathy. Gabapentin (GBT) is a first line agent used to treat neuropathic pain, and its effect is mediated by spinal noradrenergic and muscarinic cholinergic receptors. Electro-acupuncture (EA) is used for treating various types of pain via its action through spinal opioidergic and noradrenergic receptors. Here, we investigated whether combined treatment of these two agents could exert a synergistic effect on paclitaxel-induced cold and mechanical allodynia, which were assessed by the acetone drop test and von Frey filament assay, respectively. Significant signs of allodynia were observed after four paclitaxel injections (a cumulative dose of 8 mg/kg, i.p.). GBT (3, 30, and 100 mg/kg, i.p.) or EA (ST36, Zusanli) alone produced dose-dependent anti-allodynic effects. The medium and highest doses of GBT (30 and 100 mg/kg) provided a strong analgesic effect, but they induced motor dysfunction in Rota-rod tests. On the contrary, the lowest dose of GBT (3 mg/kg) did not induce motor weakness, but it provided a brief analgesic effect. The combination of the lowest dose of GBT and EA resulted in a greater and longer effect, without inducing motor dysfunction. This effect on mechanical allodynia was blocked by spinal opioidergic (naloxone, $20{\mu}g$), or noradrenergic (idazoxan, $10{\mu}g$) receptor antagonist, whereas on cold allodynia, only opioidergic receptor antagonist blocked the effect. In conclusion, the combination of the lowest dose of GBT and EA has a robust and enduring analgesic action against paclitaxel-induced neuropathic pain, and it should be considered as an alternative treatment method.