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At least 523 records · Page 29Linked to original sources
PubMed2000

Gabapentin inhibits excitatory synaptic transmission in the hyperalgesic spinal cord.

In the present study we tested the effects of the antihyperalgesic compound gabapentin on dorsal horn neurones in adult spinal cord. Slices were taken from control and hyperalgesic animals suffering from streptozocin-induced diabetic neuropathy. At concentrations up to 100 microM, bath application failed to affect the resting membrane properties of dorsal horn neurones taken from both groups of animal. In contrast, bath application of gabapentin dramatically reduced the magnitude of the excitatory postsynaptic current (EPSC) in neurones taken from hyperalgesic animals without altering the magnitude of the EPSC in control animals. Using a paired pulse stimulation protocol, together with analysis of miniature EPSC's, it was possible to demonstrate that gabapentin mediated these effects via a pre-synaptic site of action.

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PubMed2001

Block by gabapentin of the facilitation of glutamate release from rat trigeminal nucleus following activation of protein kinase C or adenylyl cyclase.

The effect of activation of protein kinase C (PKC) or adenylyl cyclase on release of glutamate has been investigated in a perfused slice preparation from the rat caudal trigeminal nucleus. Stimulation of PKC by phorbol 12-myristate 13-acetate (PMA) produced a concentration-dependent increase in K(+)-evoked release of [(2)H]-glutamate (maximum increase 45%, EC(50) 11.8 nM), but in the presence of gabapentin (30 microM) the facilitation of release was blocked. The adenylyl cyclase activator forskolin (FSK) also induced a concentration-dependent increase in K(+)-evoked release of [(3)H]-glutamate (maximum increase 36%, EC(50) 2.4 microM), and again this facilitatory effect was blocked by gabapentin (30 microM). We suggest that these results may be of relevance to the antihyperalgesic properties of gabapentin, in conditions where concomitant release of substance P and CGRP produces activation of PKC and adenylyl cyclase respectively.

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PubMed2003

Open pilot study of gabapentin versus trazodone to treat insomnia in alcoholic outpatients.

Alcohol-dependent outpatients with persisting insomnia were treated with either gabapentin or trazodone. Patients were assessed at baseline and after 4-6 weeks on medication using the Sleep Problems Questionnaire (SPQ). Of 55 cases initially treated, 9% dropped out due to morning drowsiness. Of the remaining 50 cases, 34 were treated with gabapentin (mean dose +/- SD = 888 +/- 418 mg) at bedtime and 16 were treated with trazodone (105 +/- 57 mg) at bedtime. Both groups improved significantly on the SPQ but the gabapentin group improved significantly more than the trazodone group. Controlled studies are warranted to replicate these findings.

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PubMed2001

Gabapentin in painful HIV-related neuropathy: a report of 19 patients, preliminary observations.

The objective of this study was to assess the efficacy and safety of Gabapentin as the sole analgesic in patients with HIV-related painful neuropathy. Nineteen patients with HIV-related painful neuropathy were administered Gabapentin. Efficacy was evaluated with two 100-mm Visual Analogue Scales (VAS) (0: no symptom; 100: worst symptom), rating pain and interference of pain with sleep, performed at baseline and monthly intervals. Main Pain VAS score decreased from a baseline of 55.7 +/- 19.1 mm to a final 14.7 +/- 18.6 mm (ANOVA P = 0.0001) and mean Sleep Interference VAS score decreased from a baseline of 60.4 +/- 31.9 mm to a final 15.5 +/- 27.7 mm (ANOVA P = 0.0001). Gabapentin provided significant pain relief in our patients with HIV-associated painful sensory neuropathy.

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PubMed2000

SUNCT syndrome responsive to gabapentin (Neurontin).

A 48-year-old male suffering with SUNCT (severe unilateral neuralgiform headache with conjunctival injection and tearing, rhinorrhea and sub-clinical sweating) presented in 1996 after a 10-year history of multiple failed therapies. The symptoms included strictly left-sided ocular, as well as facial and temple pain. The pain attacks were burning, sharp, shooting and occurred 25 times daily, lasting 2 to 3 minutes with tearing and conjunctival injection. There was no associated nausea or vomiting, but there was photophobia. No other autonomic changes were reported and the pain was not triggerable. Initially Indocin (indomethacin) was tried without significant benefit. Gabapentin (Neurontin) was then started with improvement at 1800 mg per day. The patient was then lost to follow-up for 3 years, as he moved from the Los Angeles area. He returned in 1999 having stopped the gabapentin after his prescription ran out in 1996, reporting the pain returned immediately. Again gabapentin was prescribed and at 900 mg three times daily he has been pain free for 12 months.

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PubMed2001

Drug-resistant cluster headache responding to gabapentin: a pilot study.

Prompted by the results of gabaergic drugs, such as valproate and topiramate, we performed this pilot study to assess the effect of gabapentin in cluster headache. Eight patients suffering from episodic cluster headache and four suffering from chronic cluster headache were studied. All of them had failed to respond to traditional prophylactic drugs. The design of the study was an open trial. The main parameter for effectiveness was the number of daily attacks. Gabapentin was given at the daily dosage of 900 mg. All patients were pain free after a maximum of 8 days after starting therapy, with a bout duration thus reduced to 16-40% of the average previous bouts (only applies to episodic cluster patients). We hypothesize that the gabaergic action of gabapentin, perhaps combined with other mechanisms, such as calcium channel blockade, may be responsible for its remarkable effects on cluster headache.

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PubMed2001

Using gabapentin to treat failed back surgery syndrome caused by epidural fibrosis: A report of 2 cases.

Failed back surgery syndrome (FBSS) is a long-lasting, often disabling, and relatively frequent (5%-10%) complication of lumbosacral spine surgery. Epidural fibrosis is among the most common causes of FBSS, and it is often recalcitrant to treatment. Repeated surgery for fibrosis has only a 30% to 35% success rate, whereas 15% to 20% of patients report worsening of their symptoms. Long-term outcome studies focusing on pharmacologic management of chronic back pain secondary to epidural fibrosis are lacking in the literature. This report presents 2 cases of severe epidural fibrosis managed successfully with gabapentin monotherapy. In both cases, functional status improved markedly and pain was significantly diminished. Gabapentin has an established, favorable safety profile and has been shown to be effective in various animal models and human studies of chronic neuropathic pain. Clinicians should consider gabapentin as a pharmacologic treatment alternative in the management of FBSS caused by epidural fibrosis.

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PubMed2002

Gabapentin and pregabalin suppress tactile allodynia and potentiate spinal cord stimulation in a model of neuropathy.

Spinal cord stimulation (SCS) is an effective tool in alleviating neuropathic pain. However, a number of well-selected patients fail to obtain satisfactory pain relief. Previous studies have demonstrated that i.t. baclofen and/or adenosine can enhance the SCS effect, but this combined therapy has been shown to be useful in less than half of the cases and more effective substances are therefore needed. The aim of this experimental study in rats was to examine whether gabapentin or pregabalin attenuates tactile allodynia following partial sciatic nerve injury and whether subeffective doses of these drugs can potentiate the effects of SCS in rats which do not respond to SCS. Mononeuropathy was produced by a photochemically induced ischaemic lesion of the sciatic nerve. Tactile withdrawal thresholds were assessed with von Frey filaments. Effects of increasing doses of gabapentin and pregabalin (i.t. and i.v.) on the withdrawal thresholds were analysed. These drugs were found to reduce tactile allodynia in a dose-dependent manner. In SCS non-responding rats, i.e. where stimulation per se failed to suppress allodynia, a combination of SCS and subeffective doses of the drugs markedly attenuated allodynia. In subsequent acute experiments, extracellular recordings from wide dynamic range neurones in the dorsal horn showed prominent hyperexcitability. The combination of SCS and gabapentin, at the same subeffective dose, clearly enhanced suppression of this hyperexcitability. In conclusion, electrical therapy and pharmacological therapy in neuropathic pain can, when they are inefficient individually, become effective when combined.

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PubMed2006

Comparative study on the bioequivalence of two different gabapentin formulations. A randomised, two-period, two-sequence, crossover clinical trial in healthy volunteers.

The bioequivalence of two capsule formulations containing 400 mg gabapentin (CAS 60142-96-3) was assessed in 24 healthy volunteers in an open, randomised, crossover, 2 periods x 2 sequences, with a minimum washout period of 7 days, single-dose study. Plasma samples were obtained at fixed time points, over 48 h (baseline (pre-dose), +0.5 h, +1 h, +1.5, +2, +2.5, +3, +3.5, +4, +8, +5, +6, +8, +10, +12, +24, +36 and +48 h after administration) and gabapentin concentrations were determined by means of an HPLC-MS method (LLOQ 50.2 ng/mL). Pharmacokinetic parameters used for bioequivalence assessment (AUCtlast, AUCinf and Cmax) were determined from the gabapentin concentration data using non-compartmental analysis. The results showed that all 90 % confidence intervals (obtained by ANOVA) were all within the predefined ranges: 93.87-111.87 % for Cmax 94.04-108.21 % for AUCtlast and 94.23-108.29 % for AUCinf. Consequently, this bioequivalence study was well designed in order to conclude that the test formulation and reference formulation were bioequivalent in terms of rate and extent of absorption.

Adolescent↗
PubMedDate not supplied

A randomized, open-label, controlled trial of gabapentin and phenobarbital in the treatment of alcohol withdrawal.

Gabapentin was compared with phenobarbital for the treatment of alcohol withdrawal in a randomized, open-label, controlled trial in 27 inpatients. There were no significant differences in the proportion of treatment completers between treatment groups or the proportion of patients in each group requiring rescue medication for breakthrough signs and symptoms of alcohol withdrawal. There were no significant treatment differences in withdrawal symptoms or psychological distress, nor were there serious adverse events. These findings suggest that gabapentin may be as effective as phenobarbital in the treatment of alcohol withdrawal. Given gabapentin's favorable pharmacokinetic profile, further study of its effectiveness in treating alcohol withdrawal is warranted.

Adolescent↗
PubMed2002

Gabapentin withdrawal presenting as status epilepticus.

A 34-year-old male with lumbar disc disease and surgery was placed on gabapentin daily for chronic back pain. He remained on a steady dose of 8000 mg/day for 9 months, almost doubled what is considered therapeutic. He ran out of medication, was unable to refill his prescription for 2 days and presented to the emergency department in status epilepticus. There was no previous history of seizure disorder and he was on no other medications. A medical evaluation for an alternative etiology of his seizures was negative. Although gabapentin withdrawal has been previously reported and usually consists of anxiety, diaphoresis, and palpitations, this is the first reported patient with generalized seizures and status epilepticus secondary to gabapentin withdrawal.

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PubMed1996

Determination of gabapentin in serum using solid-phase extraction and gas-liquid chromatography.

A gas-liquid chromatographic method for the determination of gabapentin (Neurontin) is described. The method involves extracting 0.5 mL of acidified sample by C18 solid-phase column, derivatization with MTBSTFA plus 1% tBDMCS, and analysis on an HP-1 column with a flame-ionization detector. Quantitation was performed with peak-height ratios of gabapentin to a gabapentin analogue [(1-aminomethyl-1-cycloheptyl) acetic acid] as the internal standard. The assay had a limit of detection of 0.2 mg/L and a linear range from 0.5 to 30.0 mg/L. Several compounds were analyzed for potential interference, and none interfered with the assay.

Acetamides↗
PubMed1998

Gabapentin reverses the allodynia produced by the administration of anti-GD2 ganglioside, an immunotherapeutic drug.

UNLABELLED: Systemically administered, the anti-GD2 antibody produces allodynia demonstrated by decreased mechanical withdrawal threshold. Electrophysiologic recordings indicate a probable neuropathic origin, as small-diameter sensory fibers develop continuous high-frequency discharge after antibody administration. Gabapentin (GBP) is a gamma-aminobutyric acid analog originally synthesized for its anticonvulsant actions. Several open-label clinical studies, as well as a wealth of anecdotal evidence, suggest that GBP may be beneficial for the treatment of neuropathic pain. This study examined the effects of GBP given as a posttreatment after induction of an anti-GD2-associated allodynia. Anti-GD2 (1 mg/kg intravenously [i.v.]) administered to Sprague-Dawley rats reduced the mean withdrawal threshold from 14.71 to 4.95 g (P < 0.001), as measured by using von Frey hairs. This was reversed by GBP in a dose-dependent fashion; the minimal effective dose was between 3 and 30 mg/kg i.v. The maximal percent analgesic effect of GBP was 76% and 93% at doses of 30 and 100 mg/kg, respectively (P < 0.001). With these doses, side effects were minimal and were manifested as slightly decreased spontaneous movement and startle response. No changes were seen in reflex responses to corneal or pinna stimulation, and no motor deficits were observed. These data support the use of GBP as an effective therapy for neuropathic pain. IMPLICATIONS: After the administration of anti-GD2 antibody, rats display an escape reaction to light touch, increased blood pressure, and aberrant firing in nerve fibers associated with pain transmission. Systemic gabapentin reduced or eliminated the escape response and reversed the hypertension with minimal side effects. This suggests that gabapentin blocked the antibody-associated (neuropathic) pain.

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PubMed1996

Gabapentin for the treatment of hemifacial spasm.

Pharmacologic therapy for hemifacial spasm is often limited by the paucity of effective medications and problems with side effects. Gabapentin is a novel antiepileptic drug that is generally well tolerated. Its anticonvulsant effect is independent of gamma-aminobenzoic acid (GABA) receptor mechanisms. We report a patient with hemifacial spasm who responded well to gabapentin therapy. Gabapentin may be a useful alternative medical therapy to currently used drugs.

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PubMed2000

Anorgasmia in a patient with bipolar disorder type 1 treated with gabapentin.

Gabapentin is a relatively new anticonvulsant indicated for adjunctive therapy in the treatment of partial seizures, with and without secondary generalization, in adults with epilepsy. Overall, it has a minimal side effect profile compared with other anticonvulsant agents. Postmarketing surveillance is needed to further delineate the spectrum of adverse events that may be experienced by patients treated with this medication. This is a case report of a 25-year-old man with a 10-year history of mood swings that progressively worsened and resulted in a suicide attempt 8 months before his first appointment. A diagnosis of bipolar disorder was established, and a clinical interview ruled out other mental disorders. The patient was administered gabapentin 300 mg/day, and the dose was titrated upward to 900 mg/day. A follow-up appointment revealed improved control of his bipolar symptoms. However, the patient reported that he could not have an orgasm during sexual intercourse. The medication was changed to valproic acid 250 mg three times daily. His bipolar symptoms remained under control and the anorgasmia resolved. This was maintained at the next follow-up appointment. The side effect profile and therapeutic monitoring requirements of gabapentin are favorable when compared with those of other anticonvulsant agents. However, because this agent is relatively new, especially for use in the treatment of bipolar disorder, a more thorough development of its side effect profile is needed. Observing, recording, and reporting atypical adverse events and side effects are critical to postmarketing surveillance and enhance the clinician's ability to make rational therapeutic decisions.

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PubMed2005

Monotherapy treatment of paruresis with gabapentin.

Paruresis, the difficulty or inability to urinate in the presence of others, is a highly prevalent (7-32%) social anxiety subtype that is both chronic and pervasive. Paruresis negatively impacts quality of life. Treatment strategies have focused on psychological interventions. To date, standard social anxiety pharmacotherapies utilized in the treatment of paruresis have shown minimal efficacy. A PUBMED search revealed no references to paruresis treatment with selective serotonin reuptake inhibitors or gabapentin. This case report presents the first instance of successful monotherapy treatment of paruresis with gabapentin. The patient's relative medicine noncompliance resulted in an on-off-on treatment design with a dose-dependent response. Efficacy persisted throughout a 7-month treatment course. Gabapentin should be studied further for its potential use in the treatment of paruresis.

Amines↗
PubMed2005

Gabapentin in the treatment of antipsychotic-induced akathisia in schizophrenia.

Antipsychotic-induced akathisia is characterized by subjective and objective motor restlessness, which is observed as a common extrapyramidal side-effect of antipsychotic agents. A patient is described who had antipsychotic-induced akathisia unresponsive to conventional therapy, and who began gabapentin therapy for insomnia. Significant improvement in his akathisia occurred when the gabapentin dose was increased, and his other treatment for akathisia was decreased and discontinued. Gabapentin may be effective by mechanisms similar to its action in restless legs syndrome and Parkinsonism, and/or via the GABA neurotransmitter system.

Adult↗
PubMed1998

Gabapentin for treatment of pain and tremor: a large case series.

BACKGROUND: Several anticonvulsant agents, including carbamazepine, phenytoin, and valproate, are effective in some patients for the treatment of pain and tremor. This study reports on a trial of the newly introduced anticonvulsant, gabapentin, for pain and tremor control. METHODS: A large case series of patients with centrally mediated pain, peripherally mediated pain, migraine, and tremor were treated in an open-label study with gabapentin (maximum of 2,700 mg/day). RESULTS: Thirty-nine patients (65%) had moderate-to-excellent improvement in symptoms, with the best responses occurring in patients with peripherally mediated neuropathic pain. The other conditions treated that showed some improvement were benign essential/familial tremor, restless legs syndrome, centrally mediated pain, and periodic nighttime leg movements. CONCLUSIONS: Gabapentin offers an effective, safe alternative therapy or co-therapy for the listed painful conditions and tremor; it does not affect the metabolism of other medications and is well tolerated.

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