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PubMed2006

Blinded placebo crossover study of gabapentin in primary orthostatic tremor.

Primary orthostatic tremor (OT) is a rare but disabling condition characterized by leg tremor and feelings of instability during stance. Previous studies have reported a reduction in OT symptoms with gabapentin treatment. In this study, we report on the benefits of gabapentin treatment in a double-blind placebo-controlled crossover study of 6 OT patients. First, the maximally effective gabapentin dosage (600-2,700 mg/day) for each patient was determined during an initial dose-titration phase. Patients were then studied 7 days after drug withdrawal and again after two 2-week periods of treatment with either gabapentin or placebo, using force platform posturography to quantify postural sway and tremor. Other medications for OT were continued unchanged. Symptomatic response was assessed by a patient-rated severity scale and quality of life (QOL) questionnaire. All patients reported an increase in symptoms during the washout phase and symptom reduction (50%-75%) during gabapentin treatment. Tremor amplitude was reduced to 79% +/- 11% and sway area to 71% +/- 11% of the placebo state. QOL improved in all patients, no adverse drug effects were noted, and symptomatic benefit was maintained at follow-up (mean = 19 months). The findings confirm that gabapentin is an effective treatment for OT, reducing both tremor and postural instability and improving quality of life, and support its use as add-on or first-line therapy for OT.

Aged↗
PubMed1998

Double-blind controlled trial of gabapentin in essential tremor.

Gabapentin has been reported to be effective for essential tremor (ET) based on open-label trials. We studied gabapentin (1800 mg/day) and placebo in a double-blind crossover design in 20 ET patients. Eighteen patients completed the study and two patients dropped out as a result of adverse effects which resolved when the medication was discontinued. Tremor was assessed at baseline and after 2 weeks of gabapentin and placebo treatment. One patient was mildly improved and another was moderately improved with placebo. Similarly, one patient reported mild improvement and another patient had marked improvement with gabapentin. All the remaining patients either reported no change or were worse with both treatment arms. There was no significant difference for total tremor score, hand tremor score, handwriting scores, or pouring scores. Sickness Impact Profile scores were no different between placebo and gabapentin. Our results suggest that as an adjuvant therapy in ET, gabapentin has limited benefit.

Acetates↗
PubMed2006

Determination of gabapentin in human plasma using hydrophilic interaction liquid chromatography with tandem mass spectrometry.

A rapid, sensitive and selective method for the determination of gabapentin in human plasma was developed using hydrophilic interaction liquid chromatography/tandem mass spectrometry (HILIC/MS/MS). The devised method involved protein precipitation with acetonitrile followed by separation on an Atlantis HILIC silica column using an acetonitrile/ammonium formate mobile phase (100 mM, pH 3.0) (85:15, v/v). Analytes were detected using an electrospray ionization mass spectrometer in the multiple-reaction monitoring mode. The standard curve was linear (r = 1.000) over the concentration range of 50.0-10000 ng/mL. The lower limit of quantification for gabapentin was 50.0 ng/mL (ca. 20 pg gabapentin) using a 10-microL plasma sample. The coefficients of variation and relative errors for intra- and inter-assay at four QC levels (i.e., 50.0, 125, 750, and 7500 ng/mL) were 4.7 to 9.4% and -4.1 to 1.6%, respectively. Absolute and relative matrix effects for gabapentin and metformin were practically absent. Gabapentin and metformin recoveries were 98.5% and 99.0%, respectively. This method was successfully applied to a bioequivalence study of gabapentin in humans.

Amines↗
PubMed2004

Preemptive use of gabapentin significantly decreases postoperative pain and rescue analgesic requirements in laparoscopic cholecystectomy.

PURPOSE: To evaluate the comparative preemptive effects of gabapentin and tramadol on postoperative pain and fentanyl requirement in laparoscopic cholecystectomy. METHODS: Four hundred fifty-nine ASA I and II patients were randomly assigned to receive 300 mg gabapentin, 100 mg tramadol or placebo in a double-blind manner two hours before laparoscopic cholecystectomy under general anesthesia. Postoperatively, patients' pain scores were recorded on a visual analogue scale every two hours for the initial 12 hr and thereafter every three hours for the next 12 hr. Patients received fentanyl 2 micro g*kg(-1) intravenously on demand. The total fentanyl consumption for each patient was recorded. RESULTS: Patients in the gabapentin group had significantly lower pain scores at all time intervals (2.65 +/- 3.00, 1.99 +/- 1.48, 1.40 +/- 0.95, 0.65 +/- 0.61) in comparison to tramadol (2.97 +/- 2.35, 2.37 +/- 1.45, 1.89 +/- 1.16, 0.87 +/- 0.50) and placebo (5.53 +/- 2.22, 3.33 +/- 1.37, 2.41 +/- 1.19, 1.19 +/- 0.56). Significantly less fentanyl was consumed in the gabapentin group (221.16 +/- 52.39 micro g) than in the tramadol (269.60 +/- 44.17 micro g) and placebo groups (355.86 +/- 42.04 micro g; P < 0.05). Sedation (33.98%), nausea/retching/vomiting (24.8%) were the commonest side effects in the gabapentin group whereas respiratory depression (3.9%) was the commonest in the tramadol group and vertigo (7.8%) in the placebo group. CONCLUSION: Preemptive use of gabapentin significantly decreases postoperative pain and rescue analgesic requirement in laparoscopic cholecystectomy.

Acetates↗
PubMed2006

Preoperative gabapentin for postoperative analgesia: a meta-analysis.

PURPOSE: Gabapentin's role in the treatment of chronic neuropathic pain is well known. What is less well established is its role for managing postoperative pain. In order to clarify whether gabapentin's utility in acute pain control is more than just theoretical, we conducted a meta-analysis of all randomized trials that addressed gabapentin's role in acute postoperative pain control. We specifically addressed whether gabapentin reduces pain scores, analgesia consumption, and/or analgesia-related side effects in the first 24 hr following surgery. SOURCE: We identified eight placebo-controlled, randomized controlled trials and conducted a meta-analysis using the primary outcomes of pain scores, total analgesia consumption, and side effects over a 24-hr period. PRINCIPLE FINDINGS: Patients who received gabapentin preoperatively reported significantly lower pain scores (-11.9 at rest and -11.0 with movement on a 100-point visual analogue scale) and opioid consumption (-14.7 mg of morphine in 24 hr) with no difference in the incidence of side effects. CONCLUSION: Although gabapentin given preoperatively decreases pain scores and analgesic consumption in the first 24 hr after surgery, the clinical significance of this finding has yet to be determined. This meta-analysis could not demonstrate a significant reduction in the incidence of side effects. Due to the small numbers enrolled in the studies, larger randomized control trials are warranted.

Amines↗
PubMed2003

Acute effects of gabapentin on laboratory measures of aggressive and escape responses of adult parolees with and without a history of conduct disorder.

RATIONALE: The possible role of GABA in human aggression was evaluated by administering gabapentin to subjects with and without a history of conduct disorder and comparing the effects on laboratory measures of aggression and escape. METHODS: Eighteen male and two female subjects with a history of criminal behavior participated in experimental sessions, which measured aggressive and escape responses. Ten subjects had a history of childhood conduct disorder (CD+) and ten subjects with no history (non-CD controls). Aggression was measured using the Point Subtraction Aggression Paradigm (PSAP), which provided subjects aggressive, escape and monetary reinforced response options. RESULTS: Acute doses (200, 400 and 800 mg) of gabapentin had similar effects on aggressive responses among CD+ subjects compared to non-CD control subjects. Aggressive responses of CD+ and non-CD control subjects increased at lower gabapentin doses, and decreased at the highest 800 mg gabapentin dose. Gabapentin increased escape responses for both CD+ and non-CD controls CD- subjects at the lowest dose, but then produced dose-related decreases at the two higher doses in both groups. No changes in monetary reinforced responses were observed, indicative of no CNS stimulation or sedation. CONCLUSIONS: Gabapentin produced similar bitonic effects upon aggressive and escape responses in subjects with and without a history of childhood conduct disorder. This is in marked contrast to prior differential effects of baclofen on aggressive responses between CD+ and non-CD control subjects in a previous study.

Acetates↗
PubMed2000

Effect of riluzole and gabapentin on cocaine- and methamphetamine-induced behavioral sensitization in mice.

RATIONALE: Recent studies have suggested the involvement of excitatory amino acid (EAA) and inhibitory gamma amino butyric acid (GABA) transmission in the effects of psychostimulants such as cocaine and amphetamines. OBJECTIVES: The present study was undertaken to investigate whether drugs that are considered to inhibit glutamate release (e.g., riluzole) or increase GABAergic transmission (e.g., gabapentin) attenuate the induction and expression of sensitization to cocaine and methamphetamine (METH) in Swiss Webster mice. METHODS: Sensitization to the psychomotor stimulating effect of cocaine and METH was rendered by five daily injections of cocaine (20 mg/kg) or METH (1.0 mg/kg). Locomotor activity was measured by infrared beam interrupts. RESULTS: Pretreatment with riluzole (2.5-20.0 mg/kg) affected neither the expression nor the induction of sensitization to cocaine. The pretreatment with riluzole (20 mg/kg) blocked the acute response to METH on day 1 and the expression of the sensitized response on day 5 but not the induction of sensitization to METH. Pretreatment with gabapentin (10 mg/kg and 30 mg/kg) affected neither the expression nor the induction of sensitization to cocaine. The pretreatment with gabapentin attenuated the acute response to METH on day 1 and the expression of the sensitized response on day 5, but it failed to block the induction of sensitization to METH. Psychostimulant-induced conditioned locomotion was affected neither by riluzole nor by gabapentin. CONCLUSIONS: Riluzole and gabapentin had no effect on the induction of sensitization to cocaine and METH; however, they attenuated the expression of sensitization to METH but not to cocaine. These findings suggest that riluzole- and gabapentin-mediated changes in EAA and GABAergic transmission, respectively, had no effect on mechanisms associated with the induction of sensitization, but they may affect the expression of the sensitized response to METH.

Acetates↗
PubMed2002

[Gabapentin in the treatment of chronic intractable pain].

INTRODUCTION: Gabapentin has been shown to reduce pain associated with diabetic neuropathia and postherpetic neuralgia. To date it is not known, whether gabapentin is generally effective in other types of pain. It was therefore the aim to study gabapentin in patients suffering from intractable pain with respect to efficacy, predictive factors and side effects. METHODS: Retrospective analysis of the data sheet of pretreated patients suffering from intractable pain and treated with gabapentin as a third line drug at a university pain clinic. Pain intensity (visual analogue scale, VAS 0 -10 cm), pain characteristics, diagnosis, pre- and co-treatment, and side effects were assessed. Response to treatment was defined as a 50% reduction in pain or a pain intensity of VAS </= 3. RESULTS: 99 patients were included. Approximately half the patients (n = 49) responded to gabapentin. Patients suffering from neuropathic pain showed a higher response rate (60%) compared to patients with muscle-sceletal pain (35%). Allodynia was twice as high in the responders (35%) compared to the non-responders (18%) before treatment. No serious side effects were reported. CONCLUSION: Gabapentin was effective in approximately 50% of pretreated patients with intractable pain. Neuropathic pain responded better than pain of other origine. Allodynia may be a predictive factor for a positive treatment effect.

Acetates↗
PubMed2006

PEPT1 enhances the uptake of gabapentin via trans-stimulation of b0,+ exchange.

PURPOSE: The aims of this study were (1) to determine whether amino acid and dipeptide loading can improve the effective permeability of gabapentin and (2) to characterize the underlying mechanism that is responsible for this interaction. MATERIALS AND METHODS: An in situ single-pass rat intestinal perfusion model was used to assess the effective permeability of gabapentin in rat, in the absence and presence of cellular loading by amino acid and dipeptide mixtures. RESULTS: Compared to gabapentin alone, cellular loading with amino acid and dipeptide mixtures significantly improved the effective permeability of gabapentin by 46-79% in jejunum and by 67-72% in ileum (p < or = 0.01). However, coperfusion of glycylsarcosine (i.e., PEPT1 substrate), methionine sulfoximine (i.e., glutamine synthase inhibitor), or lysine and arginine (i.e., b(0,+) substrates) with the amino acid and dipeptide mixtures compromised the intestinal uptake of gabapentin. CONCLUSIONS: These findings demonstrate, for the first time, a direct relationship between the PEPT1-mediated uptake of a dipeptide and the trans-stimulated uptake of gabapentin (an amino acid-like drug) through the transport system b(0,+).

Amines↗
PubMed1991

Gabapentin increases aminooxyacetic acid-induced GABA accumulation in several regions of rat brain.

Gabapentin exerts anticonvulsant effects in different animal models of seizure states and in epileptic patients with different seizure types, but the mechanism of action of these effects is unknown. In the present study, the gamma-aminobutyric acid (GABA) accumulation induced by aminooxyacetic acid (AOAA) was used as a method to study the effects of gabapentin on regional turnover of GABA in the rat brain. Gabapentin was administered at a dose of 23 mg/kg i.p. (the ED95 against tonic electroconvulsions in rats) 1, 2 and 8 h prior to injection of AOAA, 100 mg/kg, i.p. Gabapentin significantly increased the AOAA-induced GABA accumulation in most of the 12 brain regions examined, but the time course of the increases in GABA accumulation differed from region to region. Regions in which the time course of the increase in GABA accumulation was similar to the anticonvulsant time course of gabapentin included substantia nigra, amygdala and thalamus. The data suggest that an effect of gabapentin on GABA synthesis might be involved in its mechanism of anticonvulsant action.

Acetates↗
PubMed2006

Simple and sensitive liquid chromatographic method with fluorimetric detection for the analysis of gabapentin in human plasma.

A simple and sensitive liquid chromatographic method is described for the quantitative analysis of gabapentin in human plasma. Gabapentin (GBP) is an anticonvulsant and widely used in the treatment of epilepsy. No peculiar chromophore is available on gabapentin moiety for direct analysis by absorption spectrophotometry. In human plasma after deproteinisation with acetonitrile, gabapentin was derivatized with a fluorescent reagent, (2-naphthoxy)acetyl chloride (NAC) in borate buffer (pH 10.0). The resulting naphthoxy derivative of gabapentin was separated on a phenyl-hexyl column with a mobile phase consisting of a mixture of sodium acetate buffer (100 mM; pH 5.0)-methanol (32:68, v/v) used in isocratic mode. Using fluorimetric detection (excitation at 225 nm and emission at 360 nm), a low detection limit of about 0.04 microM (S/N = 3, 10 microl injected) was reached. The relative standard deviations (RSD) of the method for intra- and inter- day analyses (n = 5) are between 2.7 and 4.0%, respectively. The method was successfully applied to the analysis of gabapentin in plasma from dosed patients for therapeutic drug monitoring.

Adult↗
PubMed2004

Gabapentin maintenance decreases smoked cocaine-related subjective effects, but not self-administration by humans.

Data from research with laboratory animals indicate that cocaine self-administration can be reduced by lambda-aminobutyric acid (GABA) agonists. Yet, the effectiveness of GABA agonists to decrease human cocaine self-administration has not been investigated under controlled laboratory conditions. The purpose of this study was to assess the effects of gabapentin, a GABA agonist, on cocaine-related behaviors, including self-administration, in human research participants under controlled laboratory conditions. During this 48-day double-blind, crossover design study, the effects of gabapentin (0, 600, and 1200 mg/d) maintenance on response to cocaine (0, 12, 25, and 50 mg) were investigated in seven cocaine abusers. Active cocaine significantly increased choice to self-administer cocaine, subjective-effect ratings (e.g., "Good Drug Effect"), blood pressure and heart rate (HR). Gabapentin did not reduce cocaine choice or cardiovascular measures, but it did decrease some subjective effects of cocaine (e.g., "Good Drug Effect" and "Anxious"). These data suggest that the cocaine-gabapentin combination was well-tolerated, and because some cocaine-related subjective effects were reduced by maintenance on relatively low gabapentin doses, future studies should test higher gabapentin doses.

Acetates↗
PubMed2005

The acute effects of gabapentin in combination with alcohol in heavy drinkers.

BACKGROUND: Alcohol effects in humans involve gamma-amino butyric acid (GABA) neurotransmission. It has been proposed that GABAergic medications may be effective in the treatment of alcohol dependence. This study evaluated the acute effects of gabapentin, an anticonvulsant that increases extracellular GABA, on the subjective, physiological, and performance effects of alcohol in heavy (mean 34 drinks per week) alcohol drinkers. METHODS: Seventeen volunteers without alcohol dependence were tested using a double-blind design with three 3-day long inpatient phases, each separated by at least a 1-week wash-out period. Each phase, gabapentin (0, 1000, or 2000mg) was administered 4h before alcohol (0.75g/kg), which was given in four divided doses every 20min. RESULTS: Gabapentin impaired the ability to balance without producing changes in subjective, physiological or other performance measures. Pretreatment with gabapentin did not significantly alter subjective and performance effects of alcohol and did not alter alcohol craving. Gabapentin, dose-dependently enhanced alcohol-induced tachycardia. CONCLUSIONS: Acute gabapentin administration was well tolerated in combination with alcohol, but did not alter the effects of alcohol.

Adult↗
PubMed2006

Inhibition of the rat brain sodium channel Nav1.2 after prolonged exposure to gabapentin.

Prolonged exposure of neurons to gabapentin inhibits repetitive firing of Na(+)-dependent action potentials. Here, we studied the effect of such prolonged exposure to gabapentin on a rat sodium channel, Nav1.2. After 3 days of continuous incubation with gabapentin (10-1000 microM), Nav1.2 current density was decreased dose-dependently relative to untreated cells. The reduction was 57% at 30 microM gabapentin, while higher concentrations (100-1000 microM) did not result in greater effects. Prolonged treatment with gabapentin also caused the channel to inactivate at more hyperpolarized potentials. These effects provide a mechanistic basis for the inhibition of Na(+)-dependent repetitive firing upon prolonged exposure to gabapentin and may contribute to its anticonvulsant activity.

Action Potentials↗
PubMed2006

Examination of the interaction between peripheral diclofenac and gabapentin on the 5% formalin test in rats.

It has been shown that the association of diclofenac with other analgesic agents can increase its antinociceptive activity, allowing the use of lower doses and thus limiting side effects. Therefore, the aim of the present study was to examine the possible pharmacological interaction between diclofenac and gabapentin at the peripheral level in the rat using the 5% formalin test and isobolographic analysis. Diclofenac, gabapentin or a fixed-dose ratio diclofenac-gabapentin combination were administrated locally in the formalin-injured paw and the antinociceptive effect was evaluated using the 5% formalin test. All treatments produced a dose-dependent antinociceptive effect. ED30 values were estimated for the individual drugs and an isobologram was constructed. The derived theoretical ED30 for the diclofenac-gabapentin combination was 597.5+/-87.5 microg/paw, being significantly higher than the actually observed experimental value, 170.9+/-26.07 microg/paw. These results correspond to a synergistic interaction between diclofenac and gabapentin at the peripheral level, potency being about three times higher with regard to that expected from the addition of the effects of the individual drugs. Data suggest that low doses of the diclofenac-gabapentin combination can interact synergistically at the peripheral level and therefore this drug association may represent a therapeutic advantage for the clinical treatment of inflammatory pain.

Amines↗
PubMed2006

Possible activation of the NO-cyclic GMP-protein kinase G-K+ channels pathway by gabapentin on the formalin test.

The effect of modulators of the nitric oxide-cyclic GMP-protein kinase G-K+ channels pathway on the local peripheral antinociceptive action induced by gabapentin was assessed in the rat 1% formalin test. Local peripheral administration of gabapentin produced a dose-dependent antinociception in the second phase of the test. Gabapentin-induced antinociception was due to a local action as its administration in the contralateral paw was ineffective. Local peripheral pretreatment of the paws with NG-L-nitro-arginine methyl ester (L-NAME, a nitric oxide synthesis inhibitor), 1H-(1,2,4)-oxadiazolo(4,2-a)quinoxalin-1-one (ODQ, a soluble guanylyl cyclase inhibitor) and KT-5823 (a protein kinase G inhibitor) dose-dependently reduced gabapentin-induced antinociception. Likewise, glibenclamide or tolbutamide (ATP-sensitive K+ channel inhibitors), 4-aminopyridine or tetraethylammonium (non-selective inward rectifier K+ channel inhibitors) or charybdotoxin (large-conductance Ca2+-activated-K+ channel blocker), but not apamin (small-conductance Ca2+-activated-K+ channel blocker) or naloxone (opioid receptor antagonist), reduced the antinociception induced by gabapentin. Our data suggest that gabapentin could activate the nitric oxide-cyclic GMP-protein kinase G-K+ channels pathway in order to produce its peripheral antinociceptive effect in the rat 1% formalin test.

4-Aminopyridine↗
PubMed2006

Gabapentin enhances the analgesic response to morphine in acute model of pain in male rats.

Whenever opioids as drug of choice result in inadequate analgesia, the combinational therapy would be the solution. In this study the co-administration of gabapentin with morphine is evaluated in acute model of pain. Therefore the antinociceptive effect of gabapentin (30 or 90 mg/kg, s.c.) and morphine (0.5, 1 or 3 mg/kg, s.c.) alone or in combination were measured by tail-flick test in intact adult male rats. Control rats received normal saline. Tail-flick latency time and Area Under Curve (AUC), as antinociception index were calculated for each groups. There was not any significant difference between the antinociceptive response of 0.5 mg/kg morphine and 30 mg/kg gabapentin as compared to controls, but co-administration of these subanalgesic doses increased significantly AUC as compared to morphine alone. The co-administration of gabapentin with analgesic doses of 1 and 3 mg/kg morphine had also increased significantly AUC. Therefore gabapentin enhanced the antinociceptive effect of both analgesic and subanalgesic doses of morphine in a dose dependent manner. In conclusion co-administration of gabapentin with low doses of morphine produced therapeutic analgesia which could have important clinical application.

Amines↗
PubMedDate not supplied

The analgesic effects of perioperative gabapentin on postoperative pain: a meta-analysis.

BACKGROUND AND OBJECTIVES: Gabapentin is an anticonvulsant that has been shown to be effective in the treatment of neuropathic and inflammatory pain in animal and human studies. The analgesic effect of its perioperative use has not been fully elucidated. METHODS: This systematic review (meta-analysis) included 12 randomized controlled trials of 896 patients undergoing a variety of surgical procedures that investigated the impact of perioperative administration of gabapentin on postoperative outcome. RESULTS: The pooled visual analog scores for pain at 4 hours and 24 hours were significantly less in those patients who received gabapentin (weighted mean difference [WMD] = -1.57; 95% confidence interval [CI], -2.14 to -0.99 and WMD = -0.74; CI, -1.03 to -0.45, respectively). A concomitant decrease in opioid usage by those patients who received gabapentin was also noted (odds ratio [OR] = -17.84; CI, -23.50 to -12.18). Gabapentin administration was associated with sedation and anxiolysis (OR = 3.28; CI, 1.21-8.87) but not associated with a difference in lightheadedness, dizziness, nausea, or vomiting. CONCLUSIONS: Based on this systematic review, perioperative oral gabapentin is a useful adjunct for the management of postoperative pain that provides analgesia through a different mechanism than opioids and other analgesic agents and would make a reasonable addition to a multimodal analgesic treatment plan.

Amines↗