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PubMed2005

[Curative effect of gabapentin on refractory epilepsy].

OBJECTIVE: To assess the safety and efficacy of gabapentin in treatment of refractory epilepsy. METHODS: Sixty-six patients with refractory epilepsy were treated with gabapentin 200 mg/d and 72 patients with placebo, totally 138 patients in five hospitals in different cities in China. Double-blind study was performed to observe the times of seizure, and Mini-Mental State Examination (MMSE) and Activities of Daily Life (ADL) assessment were conducted every 4 weeks. RESULTS: In comparison with the control group, the seizure times at any time point in the GB group all decreased with significant differences at the 12th and 20th weeks. The significant efficacy rates, with the seizure times decreasing by more than 75%, in the gabapentin group were higher than those in the control group, with significant differences in the 4, 8, 16, and 20th weeks. Both the MMSE scores of the 2 groups were raised with a significant difference between the 2 groups at the 16 weeks. There was no significant difference in ADL between these 2 groups. No serious side effect was found in these 2 groups. CONCLUSION: Gabapentin at a dosage of 1200 mg/d is safe and effective in treatment of epilepsy.

Adolescent↗
PubMed2005

Application of Gabapentin in Thai women with menopausal syndrome.

Application of 100 mg. three times a day of Gabapentin group, 70 women to relieve menopausal syndrome with the following symptoms:Paresthesia,sweating, hot flushes in a comparative study with the amitriptyline group, 52 women 10 mg once daily. Analysis of data was done by Chi square which assumed that the Gabapentin is superior to amitripyline as accept alternative hypothesis (Ha) and other reject null hypothesis(H0) assumed both have the same action. The result of Chi square showed that the value of calculated Chi square (39.32) is higher than Table Chi square (6.63) at p < 0.01 so the authors have to accept that Ha means that Gabapentin therapy is more significantly effective than amitripyline(p < 0.01). In addition, the present study showed that the number need to treat (NNT) of Gabapentin =2.

Amines↗
PubMedDate not supplied

Treatment with gabapentin of 11 dogs with refractory idiopathic epilepsy.

Eleven dogs diagnosed with refractory idiopathic epilepsy were treated orally with gabapentin for a minimum of three months at an initial dose of 10 mg/kg every eight hours. They were all experiencing episodes of generalised tonic-clonic seizures and had been treated chronically with a combination of phenobarbital and potassium bromide at doses sufficient to reach acceptable therapeutic serum levels without causing significant side effects. In each dog, the number of seizures per week, the average duration of the seizures and the number of days on which seizures occurred were compared for the three months before and after they were treated with gabapentin. A minimum 50 per cent reduction in the number of seizures per week was interpreted as a positive response to gabapentin, and six of the dogs showed a positive response. After the addition of gabapentin, both the number of seizures per week (P= 0.005) and the number of days with any seizures in a one-week period (P=0.03) were significantly reduced. Mild side effects of ataxia and sedation were observed in five of the dogs, but they were not severe enough to warrant the treatment being discontinued during the trial.

Amines↗
PubMed1991

Intestinal absorption of gabapentin in rats.

Gabapentin (1-aminomethyl-)cyclohexaneacetic acid, Gö 3450, CI-945; CAS 60142-96-3) is a new gamma-aminobutyric acid (GABA) analogous compound that has shown an anticonvulsive effect as well as low toxicity in preclinical and clinical studies. The substance is well absorbed after oral administration and penetrates the blood-brain barrier. The aim of experiments was to study the mechanism of intestinal absorption, the relationship between the absorption rate and the applied concentration and whether the absorption rate differs between different parts of the intestine. For this purpose, isolated intestinal segments of rats (everted sac preparations) were used. Due to the fact that gabapentin is not metabolized in the intestine, its concentration in the mucosal and serosal compartments could be determined by scintillation counting of 3H-gabapentin. The results showed that gabapentin was absorbed by simple diffusion because neither indications for an uphill nor for a carrier-mediated transport could be demonstrated. The absorption rate was linearly related in the concentration range from 0.001 to 100 mmol/l. There was no significant difference between the absorption rate in the three parts of the small intestine at 1 and 10 mmol/l, while the absorption rate was significantly (p less than 0.01) lower in the colon.

Acetates↗
PubMed1996

[Clinical studies on gabapentin in Switzerland].

Gabapentin is a new antiepileptic for the combination therapy of partial seizures. It was introduced in January 1995 in Switzerland. This article describes briefly the ongoing clinical studies in Switzerland; meanwhile, these multicenter studies are conducted in different countries. An open study will evaluate the number of seizure-free patients under therapy with different dosages of gabapentin as add-on therapy. The efficacy and tolerance of gabapentin will be compared with carbamazepine as monotherapy. The last study examines the efficacy of gabapentin for the treatment of partial seizures in pediatric population.

Acetates↗
PubMed2004

Retinal ganglion cell survival is enhanced by gabapentin-lactam in vitro: evidence for involvement of mitochondrial KATP channels.

BACKGROUND: Recently, gabapentin-lactam (GBP-L) was shown to be neuroprotective in vivo. It has been suggested that GBP-L may act by opening mitochondrial ATP-sensitive potassium (K(ATP)) channels. We tested this hypothesis by quantifying the effect of GBP-L on the survival of purified retinal ganglion cells (RGCs). METHODS: RGCs were purified from early postnatal rat retinae by immunopanning with antibodies against Thy1.1 and cultured in serum-free medium for 2 days. Cell survival was quantified by counting vital cells under phase-contrast optics. Results were normalized to controls. RGCs were treated with various concentrations (3.2-320 microM) of GBP-L with and without 1 microM glibenclamide, blocking both plasmalemmal and mitochondrial K(ATP) channels, or 100 microM 5-hydroxydecanoate (5-HD), antagonizing selectively mitochondrial K(ATP) channels. For comparison, additional cultures were treated with 32 microM gabapentin, the parent drug of GBP-L. A combination of the neurotrophic factors BDNF and CNTF (50 ng/ml each) served as a positive control. RESULTS. GBP-L increased RGC survival to a maximum of 145+/-5% (mean +/- SEM) in a concentration-dependent manner. The pEC(50) was 5.0, CI95 [4.7, 5.3]. Preincubation with glibenclamide changed the dose-response of GBP-L, indicating that it acted as a competitive antagonist with a pA2 value of 6.8, CI95 [5.9, 7.5]. 5-HD completely blocked the survival-promoting effect of GBP-L. Gabapentin had no effect, whereas the combination of CNTF and BDNF enhanced survival to 177+/-9%. CONCLUSIONS: GBP-L, but not gabapentin, can promote the survival of cultured central nervous system neurons, possibly by opening mitochondrial K(ATP) channels. These results suggest further testing of GBP-L as a potentially neuroprotective drug.

Adenosine Triphosphate↗
PubMed2002

Defining the role for gabapentin in the treatment of trigeminal neuralgia: a retrospective study.

The preferred treatment for trigeminal neuralgia consists of antiepileptic drugs. Among them, gabapentin has shown promise in relieving some forms of neuropathic pain. This retrospective review examined 194 consecutive cases of trigeminal neuralgia, many of whom had paroxysmal facial pain resistant to previous surgical interventions or treatment with multiple medications. Of the 92 who had received a trial of gabapentin, 43 reported reduction in facial pain. This benefit was complete in 16, nearly complete in 9, moderate in 12, and partial in 6. Onset of pain relief occurred generally within 1 to 3 weeks, depending on the rate and end point of dose titration. The effective range of stable daily dosing varied from 100 to 2400 mg divided 3 times a day, with a mean of 930 mg. Pain relief was sustained in two thirds during a mean follow-up time of 8 months. The fact that gabapentin was well-tolerated and without serious side effects is an important advantage when prescribing for elderly patients. The present study suggests that gabapentin can be effective as first or second line treatment of trigeminal neuralgia, even in cases resistant to traditional treatment modalities.

Journal Article↗
PubMed2000

Dystonia in a patient treated with propranolol and gabapentin.

We present a 68-year-old patient with essential tremor who was treated with propranolol hydrochloride (80 mg daily) and gabapentin (900 mg daily) after a history of mild success of gabapentin alone in relieving his symptoms. The patient had several daily episodes of paroxysmal dystonic movements in both hands. After reducing the propranolol dose to 40 mg daily, the dystonic movements resolved. This case suggests a synergistic effect between propranolol and gabapentin.

Acetates↗
PubMed2000

Gabapentin for essential tremor: a multiple-dose, double-blind, placebo-controlled trial.

Essential tremor (ET) is a common movement disorder that often becomes refractory to conventional pharmacologic management. Open-label studies suggest that gabapentin is efficacious for ET, but the results of controlled trials have been mixed. To determine the efficacy and tolerability of gabapentin in ET, we conducted a double-blind, placebo-controlled, cross-over trial evaluating two doses (1800 mg per day and 3600 mg per day; N = 25). Patients on other ET medications were maintained on their concurrent medications for 3 months prior to study initiation and throughout the study. Twenty patients (mean age, 69.9 +/- 6.1 yrs) completed the study. Overall, patient global assessments (p <0.05), observed tremor scores (p <0.005), water pouring scores (p <0.05), and activities of daily living scores (p <0.005) significantly improved. Accelerometry scores, spirographs, and investigator global impression scores did not improve. The results were similar for high and low doses. Statistical regression models did not demonstrate any significant predictors for response. Gabapentin may be effective in some cases of ET.

Acetates↗
PubMed2005

Gas chromatography-tandem mass spectrometry analysis of gabapentin in serum.

A new highly sensitive analytical method for determining gabapentin [1-(aminomethyl) cyclohexaneacetic acid; Neurontin] in serum using gas chromatography/tandem mass spectrometry (GC-MS/MS) was developed. GC-MS/MS was applied to determine the levels of gabapentin in serum samples of mice at 1 and 6 h after oral or intraperitoneal treatment (300 mg/kg). At 1 h, the concentrations of the drug were 4.02 +/- 0.42 and 4.32 +/- 0.28 microg/mL in mice treated orally and intraperitoneally, respectively. At 6 h, drug levels decreased by about 66% in both groups. The method, coupling two stages of mass analysis, could be very useful in identifying the drug in complex mixtures such as blood and urine. Moreover, it is easy and rapid to perform, and sensitive enough to allow the presence of the drug to be determined at very low detection limits. It is a very reliable method for both clinical and experimental monitoring of gabapentin.

Amines↗
PubMed1998

Isolation of the [3H]gabapentin-binding protein/alpha 2 delta Ca2+ channel subunit from porcine brain: development of a radioligand binding assay for alpha 2 delta subunits using [3H]leucine.

The novel antiepileptic agent gabapentin (Neurontin) binds with high affinity to the alpha 2 delta subunit of a voltage-dependent Ca2+ channel. We report here a simple purification scheme for detergent-solubilized alpha 2 delta subunits from porcine brain. This involves sequential chromatography on Q-Sepharose, Cu(2+)-charged iminodiacetic acid-Sepharose, wheat germ lectin-agarose, and Mono Q. The purified protein was essentially homogeneous by SDS-polyacrylamide gel electrophoresis with a subunit Mr of 145,000. Using [3H] gabapentin as the radiolabeled tracer and (S)-3-isobutyl gamma-aminobutyric acid to define nonspecific binding, the overall purification factor was 2760-fold and the apparent yield 26.6%. We also developed and validated a novel binding assay for alpha 2 delta Ca2+ channel subunits using the ligand pair L-[3H]leucine/L-isoleucine. Even in binding assays of crude brain membrane fractions, [3H]leucine proved to be remarkably stable and specific for the alpha 2 delta Ca2+ channel subunit. [3H]Leucine offers several advantages over custom-labeled [3H]gabapentin: it has a higher specific activity, is relatively inexpensive, and is available from commercial sources.

Acetates↗
PubMed2005

A case of recurrent and migratory complex regional pain syndrome type I: Prevention by gabapentin.

Complex regional pain syndrome type I (CRPS I) or reflex sympathetic dystrophy (RSD) is a painful and disabling neuropathic pain syndrome. We report a case of a patient who has experienced CRPS I four times with an unidentified cause for all recurrences. The patient responded well to a combination of physiotherapy and intravenous regional sympathetic block in the first two attacks, but not in the fourth one. Gabapentin was effective in the last two attacks. Gabapentin was gradually discontinued 12 months after the last attack and no other recurrence was observed for a follow-up period of 9 months. This case suggests that gabapentin might be considered in the treatment and prevention of CRPS I.

Amines↗
PubMed1996

Antimyoclonic effect of gabapentin in a posthypoxic animal model of myoclonus.

The antimyoclonic property of the novel antiepileptic drug, gabapentin (1-(aminomethyl) cyclohexane acetic acid), was tested in cardiac arrest-and p,p'-DDT(1,1,1-trichloro-2,2-bis (p-chlorophenyl)ethane)-induced animal models of myoclonus. Gabapentin dose-dependently attenuated myoclonus in posthypoxic rats for more than 3 h. The drug was also found to be effective in controlling the early stages of seizures following the anoxic insult. In contrast, the drug was ineffective in controlling either myoclonus or seizures in p,p'-DDT-treated animals. These results suggest that gabapentin can be used used as an effective therapeutic agent in an acute hypoxia/ischemia-induced neurological disorder. The data further indicate that distinct neurological mechanisms may be operating in the expression of myoclonus among posthypoxic and p,p'-DDT-induced animal models.

Acetates↗
PubMed1995

Absence of Ki-ras mutations in exocrine pancreatic tumors from male rats chronically exposed to gabapentin.

Human pancreatic malignancies originating from duct cells most frequently demonstrate activation of Ki-ras gene by G-to-A transition at codons 12 and 13. Rat pancreatic exocrine tumors more frequently and almost exclusively derive from acinar cells and thus differ morphologically from human pancreatic neoplasms. Male Wistar rats fed with 2% gabapentin (1-(aminomethyl)cyclohexane acetic acid) in diet for 2 years developed pancreatic exocrine adenomas and adenocarcinomas. To study the mutations in Ki-ras gene, rat pancreatic proliferative lesions induced by gabapentin were retrospectively analyzed by PCR amplification of DNA isolated from paraffin sections of formalin-fixed rat pancreatic adenomas and adenocarcinomas, using specific primers for regions encoding exon 1 (codon 12/13) and exon 2 (codon 61). The amplified 110-bp fragments of exon 1 and exon 2 were analyzed for mutations at codon 12/13 and 61. The results showed Ki-ras mutations at codon 12 in human pancreatic carcinomas. Novel mutations GGT-to-TGT and GGT-to-CGT were detected at codon 12 in 1/5 and 2/5 human pancreatic tumors. Rat adenomas or carcinomas induced by gabapentin expressed wild type sequences at codons 12, 13 and 61. These findings were confirmed by allele-specific oligonucleotide hybridization, single-strand confirmation polymorphism of exon 1 and direct sequencing of exon 1 and exon 2. The absence of mutations in these rat pancreatic tumors suggests that these tumors do not correspond to the human tumors, and that the pathogenesis of this rodent tumor formation may follow different molecular mechanisms.

Acetates↗
PubMed1995

Determination of gabapentin in serum by capillary electrophoresis.

A rapid capillary electrophoresis method for the quantification of gabapentin, a new anticonvulsant drug, in serum was developed. The assay involves derivatization of gabapentin with fluorescamine to provide a chromophore for UV-fluorescence detection. The migration time is about 11 min. The assay was linear between 0 and 20 mg/l. No other therapeutic drugs or amino acids interfered with the gabapentin peak. The relative standard deviation is 2.4% at a mean of 11 mg/l (n = 17). The mean serum level for 52 patients on this drug was 5.2 mg/l with a range of 0-12 mg/l.

Acetates↗
PubMed1992

Long-term treatment with gabapentin for partial epilepsy.

Gabapentin was studied as an open-label 'add-on' antiepileptic drug in 35 patients with partial seizures. Follow-up at 6 months, 12 months, 18 months, and 24 months is reported. There was a trend toward improvement in simple (SPS) and complex partial seizures with it reaching significance for SPS at 12 and 24 months and for the weighted combination of seizures at 3 months. Five of nine patients were subsequently successfully converted to gabapentin monotherapy. Of those five, one is now seizure free and three are significantly improved since baseline. One remains with unchanged seizure frequency compared to baseline, but is experiencing less toxicity than at that time. This long-term observation suggests that the short-term effect demonstrated in blinded studies continues and that indeed some patients with refractory epilepsy can be maintained on gabapentin alone. Based on these findings, double-blind monotherapy trials of this drug are presently being conducted.

Acetates↗
PubMed1993

Potent and stereospecific anticonvulsant activity of 3-isobutyl GABA relates to in vitro binding at a novel site labeled by tritiated gabapentin.

3-Isobutyl GABA is a derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) and is also structurally related to the novel anticonvulsant gabapentin. The S(+) enantiomer of 3-isobutyl GABA blocks maximal electroshock seizures in mice and also potently displaces tritiated gabapentin from a novel high-affinity binding site in rat brain membrane fractions. The R(-) enantiomer is much less active in both assays, suggesting that the gabapentin binding site is involved in the anticonvulsant activity of 3-isobutyl GABA.

Acetates↗
PubMed2004

Effect of gabapentin derivates on mechanical allodynia-like behaviour in a rat model of chronic sciatic constriction injury.

A series of mutual prodrugs derived from gabapentin, pregabalin, memantine, venlafaxine were synthesized and their pharmacological properties to treat neuropathic pain were investigated in a rat model of chronic sciatic nerve constriction injury (CCI). In vivo evaluation demonstrated that the mutual prodrugs 2002413A, 2002823A composed of two gabapentins, 2002414 composed of gabapentin and pregabalin were effective in reversal tactile allodynia in CCI rats. The prodrugs 2002413A, 2002414 had no significant influence on the rotarod activity. The result suggest that the prodrugs may be possible candidates for further development.

Amines↗