Effects of cysteinyl leukotriene receptors on phagocytosis of mouse microglial cells / 浙江大学学报·医学版

OBJECTIVE@#: To determine the effects of cysteinyl leukotriene receptors (CysLTR and CysLTR) on phagocytosis of mouse BV2 microglial cells.@*METHODS@#: BV2 cells were stimulated with microglial activators lipopolysaccharide (LPS) or CysLT receptor agonists LTD. The phagocytosis of BV2 cells was observed by immunofluorescence analysis and flow cytometry. The intracellular distributions of CysLTR and CysLTR in BV2 cells were examined with immunofluorescence staining.@*RESULTS@#: Both LPS and LTD could significantly enhance the phagocytosis of BV2 cells, and such effect could be inhibited by CysLTR selective antagonist Montelukast and CysLTR selective antagonist HAMI 3379. The activation of BV2 cells induced by LTD or LPS resulted in changes in intracellular distributions of CysLTR and CysLTR. CysLTR and CysLTR was co-localization with a similar distribution.@*CONCLUSIONS@#: CysLTR and CysLTR regulate the phagocytosis of mouse BV2 microglial cells with a synergistic effect.

Impact of drug therapy on brachioradial pruritus

Abstract: Few studies have described therapeutic options in brachioradial pruritus. We describe a cross-sectional study of brachioradial pruritus patients treated in an outpatient unit. We reviewed medical records and interviewed brachioradial pruritus patients without indication for decompressive surgery, in order to access the perceptions of intensity of pruritus prior to treatment and response to therapy. We found that antidepressants and anticonvulsants were the most frequently prescribed drugs. Best reductions in pruritus were associated with its highest intensities prior to treatment, and with longer periods of therapy.

Prophylactic use of gabapentin to reduce postoperative nausea and vomiting in patients undergoing diagnostic gynecological laparoscopy

Introduction: Postoperative nausea and vomiting [PONV] occurs in patients during the first 24 hours of the surgery. Many drugs have been used for the prevention and treatment of PONV. In this trial, we used gabapentin to evaluate its prophylactic effect in reducing the severity and incidence of PONV in patients undergoing diagnostic laparoscopic gynecological surgery

Methodology: This, double blind randomized controlled trial, was done in operation theatre complex over a period of six months. 140 patients undergoing diagnostic gynecological laparoscopic surgery were selected. Two groups were formed and 70 patients were recruited in each group using lottery method as method of randomization. Group C [control group] was given placebo medication orally two hours before surgery and group G [gabapentin group] received 600 mg of gabapentin orally two hours before the procedure. Standard general anesthesia technique was used in all patients and incidence and severity of postoperative nausea and vomiting [PONV] was recorded in these patients till 24 hours of laparoscopy

Results: Severity of PONV was graded from mild to severe. There was no PONV in 25 patients [35.7%] in group C and 47 patients [67.1%] in group G. It was mild in severity in 8 patients [11.4%] in group C and 5 patients [7.1%] in group G, moderate in 31 patients [44.3%] in group C and 15 patients[21.4%] in group G and severe PONV was seen in 6 patients [8.6%] in group C and 3 patients [4.3%] in group G [P=0.003]. Postoperative nausea and vomiting within 24 hours after procedure was present in 45 patients [64.3%] in group C and 23 patients [32.9%] in group G. Results were significant between two groups after statistical analysis with p value of 0.001

Conclusion: Administration of 600 mg of gabapentin two hours before diagnostic gynecological laparoscopy decreases the frequency and severity of PONV

Gabapentin Differentially Modulate c-Fos Expression in Hypothalamus and Spinal Trigeminal Nucleus in Surgical Molar Extraction

Abstract The study on the efficacy of oral analgesics reported that no single class of drug is effective in post-surgical dental pain. Pain following removal of third molar is most commonly used and widely accepted acute pain model for assessing the analgesic effect of drugs in humans. Reports demonstrated that analgesic efficacy in the human dental model is highly predictive. The high incidence of false-negative findings in analgesic investigations hinders the process of molecular discovery. Molecular mechanism of post-surgical pain is not known. More importantly, the animal model for postoperative dental pain is not well established. In an attempt to discover an effective post-surgical dental pain blocker with acceptable side effects, it is essential to elucidate the molecular mechanism of post-operative dental pain. The present study investigated mandibular molars extraction in rat as an animal model for the post-operative dental pain in central nervous system. Using c-Fos immunohistochemistry, we demonstrated that pre administration of GBP (150 mg/kg. i.p) significantly (p< 0.01) neutralized the surgical molar extraction induced c-Fos expression bilaterally in rat hypothalamus. Present results indicate that pain after surgical molar extraction might follow novel neural pathways therefore difficult to treat with existing anti-nociceptive drugs.

Resumo O estudo da eficácia relativa dos analgésicos orais relatou que nenhuma classe única de fármaco é eficaz na dor pós-cirúrgica dental. A dor após a remoção do terceiro molar é o modelo de dor aguda mais comumente usado e amplamente aceito para avaliar o efeito analgésico de drogas em seres humanos. Os relatos demonstraram que a eficácia analgésica no modelo dental humano é altamente preditiva. A alta incidência de achados falso-negativos em investigações analgésicas dificulta o processo de descoberta molecular. O mecanismo molecular da dor pós-cirúrgica não é conhecido. Mais importante ainda, o modelo animal para a dor pós-operatória não está bem estabelecido. Numa tentativa de descobrir um bloqueador de dor dental pós-cirúrgico eficaz com efeitos secundários aceitáveis, é essencial elucidar o mecanismo molecular da dor pós-operatória dental. Neste estudo investigamos a extração de molares inferiores de ratos como modelo animal para a dor pós-operatória no sistema nervoso central. Utilizando análise imunohistoquímica de c-Fos, demonstrou-se que a administração prévia de GBP (150 mg/kg i.p) significativamente (p<0,01) neutralizou a expressão c-Fos induzida por extração molar cirúrgica bilateralmente no hipotálamo de rato. Os resultados indicam que a dor após a extração molar cirúrgica pode seguir novas vias neurais, portanto, difícil tratar com as drogas anti-nociceptivas existentes.

Psychotropics in different causes of itch: systematic review with controlled studies

Abstract Among the wide range of symptoms neglected or resistant to conventional treatments in clinical practice, itch is emerging gradually as a theme to be studied. Itch complaints and the negative effects in the quality of life are observed in several medical fields. Although the partially obscure pathophysiology, some researchers decided to check and test the use of psychotropic drugs in resistant itch to conventional topical treatments and antihistamines. The objective of this study was to evaluate scientific evidence in psychotropic use in the treatment of itch of various causes. This is a systematic review of scientific literature. The following databases were used: PubMed, Web of Science, Scopus and Scielo. Randomized controlled trials that should focus on treatment with psychotropic drugs of pruritus of various causes were the inclusion criteria. All articles were analyzed by the authors, and the consensus was reached in cases of disagreement. Fifteen articles were included after analysis and selection in databases, with the majority of clinical trials focusing on psychopharmacological treatment of itch on account of chronic kidney disease. Clinical trials with psychotropic drugs mostly indicated significant improvement in the itching. In most trials of chronic kidney disease as basal disease for itch, greater effectiveness was observed with the use of psychotropic drugs compared with placebo or other antipruritic. However, the small amount of controlled trials conducted precludes the generalization that psychiatric drugs are effective for itch of various causes.

Effect of preoperative gabapentin on pain intensity and development of chronic pain after carpal tunnel syndrome surgical treatment in women: randomized, double-blind, placebo-controlled study / Efeito da gabapentina pré-operatória na intensidade da dor e desenvolvimento de dor crônica após o tratamento cirúrgico da síndrome do túnel do carpo em mulheres: estudo randomizado duplo-cego controlado com placebo

ABSTRACT CONTEXT AND OBJECTIVES: Effective postoperative analgesia is important for reducing the incidence of chronic pain. This study evaluated the effect of preoperative gabapentin on postoperative analgesia and the incidence of chronic pain among patients undergoing carpal tunnel syndrome surgical treatment. DESIGN AND SETTINGS: Randomized, double-blind controlled trial, Federal University of São Paulo Pain Clinic. METHODS: Forty patients aged 18 years or over were randomized into two groups: Gabapentin Group received 600 mg of gabapentin preoperatively, one hour prior to surgery, and Control Group received placebo. All the patients received intravenous regional anesthesia comprising 1% lidocaine. Midazolam was used for sedation if needed. Paracetamol was administered for postoperative analgesia as needed. Codeine was used additionally if the paracetamol was insufficient. The following were evaluated: postoperative pain intensity (over a six-month period), incidence of postoperative neuropathic pain (over a six-month period), need for intraoperative sedation, and use of postoperative paracetamol and codeine. The presence of neuropathic pain was established using the DN4 (Douleur Neuropathique 4) questionnaire. Complex regional pain syndrome was diagnosed using the Budapest questionnaire. RESULTS: No differences in the need for sedation, control over postoperative pain or incidence of chronic pain syndromes (neuropathic or complex regional pain syndrome) were observed. No differences in postoperative paracetamol and codeine consumption were observed. CONCLUSIONS: Preoperative gabapentin (600 mg) did not improve postoperative pain control, and did not reduce the incidence of chronic pain among patients undergoing carpal tunnel syndrome surgery.

RESUMO CONTEXTO E OBJETIVOS: Analgesia pós-operatória eficaz é importante para reduzir a incidência de dor crônica. Este estudo avaliou o efeito da gabapentina pré-operatória na analgesia pós-operatória e na incidência de dor crônica em pacientes submetidos à cirurgia para tratamento da síndrome do túnel do carpo. DESENHO E LOCAL: Randomizado, duplo cego, Universidade Federal de São Paulo. MÉTODOS: Os 40 pacientes com 18 anos ou mais de idade foram distribuídos aleatoriamente em dois grupos: o Grupo Gabapentina recebeu 600 mg de gabapentina no pré-operatório uma hora antes da cirurgia, e o Grupo Controle recebeu placebo. Todos os pacientes receberam anestesia regional intravenosa com lidocaína a 1%. Midazolam foi utilizado para sedação, se necessário. Paracetamol foi administrado para analgesia pós-operatória, conforme necessário, e codeína, se o paracetamol fosse insuficiente. Foram avaliados: a intensidade da dor pós-operatória (durante seis meses), a incidência de dor neuropática pós-operatória (durante seis meses), a necessidade de sedação intra-operatória e o uso de paracetamol e codeína no pós-operatório. A presença de dor neuropática foi estabelecida utilizando-se o questionário DN4 (dor neuropática 4). Síndrome de dor regional complexa foi diagnosticada através do questionário Budapeste. RESULTADOS: Não foram observadas diferenças na necessidade de sedação, no controle da dor pós-operatória e na incidência de síndromes dolorosas crônicas (neuropáticas ou síndrome de dor regional complexa). Não foram observadas diferenças no consumo de paracetamol e codeína. CONCLUSÕES: Gabapentina pré-operatória (600 mg) não melhorou o controle da dor pós-operatória e não reduziu a incidência de dor crônica em pacientes submetidos à cirurgia para tratamento da síndrome do túnel do carpo.

Effect of gabapentin pretreatment on myoclonus after etomidate: a randomized, double-blind, placebo-controlled study / Efeito do pré-tratamento com gabapentina sobre a mioclonia após etomidato: um estudo randômico, duplo-cego e controlado por placebo

Abstract Aim: To evaluate the effects of three different doses of gabapentin pretreatment on the incidence and severity of myoclonic movements linked to etomidate injection. Method: One hundered patients, between 18 and 60 years of age and risk category American Society of Anesthesiologists I-II, with planned elective surgery under general anesthetic were included in the study. The patients were randomly divided into four groups and 2 h before the operation were given oral capsules of placebo (Group P, n = 25), 400 mg gabapentin (Group G400, n = 25), 800 mg gabapentin (Group G800, n = 25) or 1200 mg gabapentin (Group G1200, n = 25). Side effects before the operation were recorded. After preoxygenation for anesthesia induction 0.3 mg kg−1 etomidate was administered for 10 s. A single anesthetist with no knowledge of the study medication evaluated sedation and myoclonic movements on a scale between 0 and 3. Two minutes after induction, 2 µg kg−1 fentanyl and 0.8 mg kg−1 rocuronium were administered for tracheal intubation. Results: Demographic data were similar. Incidence and severity of myoclonus in Group G1200 and Group G800 were significantly lower than in Group P; sedation incidence and level were appreciably higher compared to Group P and Group G400. While there was no difference in the incidence of myoclonus between Group P and Group G400, the severity of myoclonus in Group G400 was lower than in the placebo group. In the two-hour period before induction other than sedation none of the side effects related to gabapentin were observed in any patient. Conclusion: Pretreatment with 800 mg and 1200 mg gabapentin 2 h before the operation increased the level of sedation and reduced the incidence and severity of myoclonic movements due to etomidate.

Resumo Objetivo: Avaliar os efeitos de três doses diferentes de gabapentina como pré-tratamento sobre a incidência e a gravidade dos movimentos mioclônicos associados à injeção de etomidato. Método: Cem pacientes, entre 18-60 anos, estado físico ASA I-II, programados para cirurgia eletiva sob anestesia geral, foram incluídos no estudo. Os pacientes foram randomicamente divididos em quatro grupos e duas horas antes da operação receberam cápsulas orais de placebo (Grupo P, n = 25), 400 mg de gabapentina (Grupo G400, n = 25), 800 mg de gabapentina (Grupo G800, n = 25) e 1.200 mg de gabapentina (Grupo G1.200, n = 25). Os efeitos colaterais antes da cirurgia foram registados. Após pré-oxigenação para a indução da anestesia, etomidate (0,3 mg.kg−1) foi administrado por 10 segundos. Um único anestesista, cego para a medicação do estudo, avaliou a sedação e os movimentos mioclônicos com uma escala de 0 a 3. Dois minutos após a indução, fentanil (2 µgr.kg−1) e rocurônio (0,8 mg.kg−1) foram administrados para a intubação traqueal. Resultados: Os dados demográficos foram semelhantes. A incidência e a gravidade da mioclonia nos grupos G1.200 e G800 foram significativamente menores do que no Grupo P; a incidência e o nível de sedação foram consideravelmente maiores comparados com o Grupo P e o Grupo G400. Enquanto não houve diferença na incidência de mioclonia entre os grupos P e G400, a gravidade da mioclonia no Grupo G400 foi menor do que no grupo placebo. No período de duas horas antes da indução, nenhum dos efeitos colaterais relacionados à gabapentina, exceto sedação, foi observado em qualquer paciente. Conclusão: O pré-tratamento com 800 mg e 1.200 mg de gabapentina duas horas antes da operação aumentou o nível de sedação e reduziu a incidência e a gravidade dos movimentos mioclônicos associados ao etomidato.

Treatment of patients with painful blind eye using stellate ganglion block / Tratamento de pacientes portadores de olho cego doloroso por meio de bloqueio de gânglio estrelado

BACKGROUND AND OBJECTIVES: management of pain in painful blind eyes is still a challenge. Corticosteroids and hypotensive agents, as well as evisceration and enucleation, are some of the strategies employed so far that are not always effective and, depending on the strategy, cause a deep emotional shock to the patient. Given these issues, the aim of this case report is to demonstrate a new and viable option for the management of such pain by treating the painful blind eye with the stellate ganglion block technique, a procedure that has never been described in the literature for this purpose. CASE REPORT: six patients with painful blind eye, all caused by glaucoma, were treated; in these patients, VAS (visual analogue scale for pain assessment, in which 0 is the absence of pain and 10 is the worst pain ever experienced) ranged from 7 to 10. We opted for weekly sessions of stellate ganglion block with 4 mL of bupivacaine (0.5%) without vasoconstrictor and clonidine 1 mcg/kg. Four patients had excellent results at VAS, ranging between 0 and 3, and two remained asymptomatic (VAS = 0), without the need for additional medication. The other two used gabapentin 300 mg every 12 h. CONCLUSION: currently, there are several therapeutic options for the treatment of painful blind eye, among which stand out the retrobulbar blocks with chlorpromazine, alcohol and phenol. However, an effective strategy with low rate of serious complications, which is non-mutilating and improves the quality of life of the patient, is essential. Then, stellate ganglion block arises as a demonstrably viable and promising option to meet this demand.

JUSTIFICATIVA E OBJETIVOS: o manejo da dor em olhos cegos dolorosos ainda é um desafio. Corticosteroides e hipotensores, bem como evisceração e enucleação, são algumas das estratégias até então empregadas, nem sempre eficazes e que, a depender da estratégia, causam um profundo abalo emocional no paciente. Dadas essas questões, o objetivo deste relato de caso é demonstrar uma nova e viável opção para o manejo desse tipo de dor por meio do tratamento do olho cego doloroso com bloqueios de gânglio cervicotorácico, técnica nunca descrita na literatura para esse fim. RELATO DE CASO: foram tratados seis pacientes portadores de olho cego doloroso, todos por glaucoma, nos quais a EVA (escala visual analógica para avaliação da dor em que 0 é ausência de dor e 10 é a maior dor já experimentada) variava de 7 a 10. Optou-se por sessões semanais de bloqueio de gânglio cervicotorácico com 4 mL de bupivacaína (0,5%) sem vasoconstritor e clonidina 1 mcg/Kg. Quatro pacientes apresentaram excelente resultado EVA, com variação entre 0 e 3, e dois permaneceram assintomáticos (EVA = 0), sem necessidade de medicação suplementar. Os outros dois usaram gabapentina 300 mg de 12 em 12 horas. CONCLUSÃO: atualmente, várias são as opções terapêuticas para o tratamento do olho cego doloroso, entre as quais se destacam os bloqueios retrobulbares com clorpromazina, álcool e fenol. No entanto, uma estratégia eficaz, com pequeno índice de complicações graves, não mutilante e que melhore a qualidade de vida do paciente é imprescindível. O bloqueio do gânglio cervicotorácico surge, pois, como uma opção comprovadamente viável e promissora para atender a essa demanda.

The Effectiveness of Oral Corticosteroids for Management of Lumbar Radiating Pain: Randomized, Controlled Trial Study

BACKGROUND: Although both pregabalin and gabapentin are known to be useful for treating lumbar radiating pain and reducing the incidence of surgery, the oral corticosteroids sometimes offer a dramatic effect on severe radiating pain despite the lack of scientific evidence. METHODS: A total of 54 patients were enrolled among 703 patients who complained of lumbar radiating pain. Twenty patients who received an oral corticosteroid was classified as group A and 20 patients who received the control drugs (pregabalin or gabapentin) as group B. Oswestry Disability Index (ODI), Revised Roland Morris disability questionnaire (RMDQ), Short Form 36 (SF-36) questionnaire, lumbar radiating pain, objective patient satisfaction, and objective improvement of patients or physicians were assessed at 2, 6, and 12 weeks after medication. RESULTS: No difference in the sex ratio and age was observed between the groups (p = 0.70 and p = 0.13, respectively). Group A showed greater improvement in radiating pain after 2, 6, and 12 weeks than group B (p < 0.001, p = 0.001, and p < 0.001, respectively). No differences were observed between the groups in satisfaction at the beginning and 12 weeks after taking the medication (p = 0.062 and p = 0.061, respectively) and in objective improvement of patients and physicians (p = 0.657 and p = 0.748, respectively). Group A was less disabled and had greater physical health scores than group B (p = 0.014 and p = 0.017, respectively). CONCLUSIONS: Oral corticosteroids for the treatment of lumbar radiating pain can be more effective in pain relief than gabapentin or pregabalin. The satisfaction of patients and physicians with the drug and objective improvement status were not inferior to that with gabapentin or pregabalin.

Anthropometric indicators of obesity in the prediction of high body fat in adolescents / Indicadores antropométricos de obesidade na predição de gordura corporal elevada em adolescentes

OBJECTIVE: To determine the anthropometric indicators of obesity in the prediction of high body fat in adolescents from a Brazilian State. METHODS: The study included 1,197 adolescents (15-17 years old). The following anthropometric measurements were collected: body mass (weight and height), waist circumference and skinfolds (triceps and medial calf). The anthropometric indicators analyzed were: body mass index (BMI), waist circumference (WC), waist-to-height ratio (WHtR) and conicity index (C-Index). Body fat percentage, estimated by the Slaughter et al equation, was used as the reference method. Descriptive statistics, U Mann-Whitney test, and ROC curve were used for data analysis. RESULTS: Of the four anthropometric indicators studied, BMI, WHtR and WC had the largest areas under the ROC curve in relation to relative high body fat in both genders. The cutoffs for boys and girls, respectively, associated with high body fat were BMI 22.7 and 20.1kg/m², WHtR 0.43 and 0.41, WC 75.7 and 67.7cm and C-Index 1.12 and 1.06. CONCLUSIONS: Anthropometric indicators can be used in screening for identification of body fat in adolescents, because they are simple, have low cost and are non-invasive. .

OBJETIVO: Determinar os indicadores antropométricos de obesidade na predição da gordura corporal elevada em adolescentes de um estado brasileiro. MÉTODOS: O estudo incluiu 1.197 adolescentes (15-17 anos). As seguintes medidas antropométricas foram coletadas: massa corporal e estatura, perímetro da cintura e dobras cutâneas (tríceps e perna medial). Os indicadores antropométricos analisados foram: índice de massa corporal (IMC), perímetro da cintura (PC), razão cintura-estatura (RCE) e índice de conicidade (IC). A gordura corporal elevada, estimada pela equação de Slaughter et al., foi usada como método de referência. Estatística descritiva, teste U de Mann-Whitney e curva ROC foram usadas para a análise dos dados. RESULTADOS: Dos quatro indicadores antropométricos estudados, o IMC, a RCE e o PC tiveram as maiores áreas sob a curva ROC em relação à gordura corporal elevada relativa em ambos os sexos. Os pontos de corte para os rapazes e as moças, respectivamente, associados com gordura corporal elevada foram IMC 22,7 e 20,1 kg/m2, RCE 0,43 e 0,41, PC 75,7 e 67,7 cm e IC 1,12 e 1,06. CONCLUSÕES: Os indicadores antropométricos podem ser usados como ferramenta para identificação da gordura corporal em adolescentes, por serem um método simples, de baixo custo e não invasivo. .

[Evaluation of the therapeutic effect of oral gabapentin on the severity of acute low back pain]

Acute low back pain is one of the most common complaints of the patients seeking medical advice. Nowadays various drugs are recommended for the treatment of this problem. Selection of appropriate medications with high efficacy and minimal side effects has always been a challenging issue in medical treatments. The present study was conducted to investigate the effect of oral gabapantin on pain intensity in patients with acute low back pain. This double-blind clinical trial study included 100 patients with acute low back pain who had referred to the treatment centers affiliated with Shahrekord University of Medical Sciences in 2011-2012.Using convenient sampling method the patients were randomly assigned to intervention [n50] and control [n=50] groups. Intervention group received two 500 mg naproxen tablets and two 100 mg gabapantin tablets/ day and control group, received two 500 mg naproxen tablets and two placebo tablets/ day. The patients were examined for pain intensity based on visual analogue scale and the rate of complications on the days of 0, 8, 15, and 30.Using SPSS software, data analysis was performed by descriptive and inferential statistics. In this study, mean pain score was significantly lower in the intervention group compared to the control group [p<0.05]. Also, the women in the intervention group had a lower mean pain score on all 3 examinations-compared to the women in the control group. But no statistically significant difference was observed in pain intensity between the men in the intervention and control groups. In this study, pain significantly relieved in the patients in the intervention group compared to those in the control group. It seems that use of gabapantin in addition to nonsteroidal anti-inflammatory drugs [NSAIDs] is more effective than NSAIDs alone in reducing the pain intensity

Effect of carbamazepine and gabapentin on excitability in the trigeminal subnucleus caudalis of neonatal rats using a voltage-sensitive dye imaging technique

BACKGROUND: The antiepileptic drugs carbamazepine and gabapentin are effective in treating neuropathic pain and trigeminal neuralgia. In the present study, to analyze the effects of carbamazepine and gabapentin on neuronal excitation in the spinal trigeminal subnucleus caudalis (Sp5c) in the medulla oblongata, we recorded temporal changes in nociceptive afferent activity in the Sp5c of trigeminal nerve-attached brainstem slices of neonatal rats using a voltage-sensitive dye imaging technique. RESULTS: Electrical stimulation of the trigeminal nerve rootlet evoked changes in the fluorescence intensity of dye in the Sp5c. The optical signals were composed of two phases, a fast component with a sharp peak followed by a long-lasting component with a period of more than 500 ms. This evoked excitation was not influenced by administration of carbamazepine (10, 100 and 1,000 µM) or gabapentin (1 and 10 µM), but was increased by administration of 100 µM gabapentin. This evoked excitation was increased further in low Mg²+ (0.8 mM) conditions, and this effect of low Mg²+ concentration was antagonized by 30 µM DL-2-amino-5-phosphonopentanoic acid (AP5), a N-methyl-D-as-partate (NMDA) receptor blocker. The increased excitation in low Mg²+ conditions was also antagonized by carbamazepine (1,000 µM) and gabapentin (100 µM). CONCLUSION: Carbamazepine and gabapentin did not decrease electrically evoked excitation in the Sp5c in control conditions. Further excitation in low Mg²+ conditions was antagonized by the NMDA receptor blocker AP5. Carbamazepine and gabapentin had similar effects to AP5 on evoked excitation in the Sp5c in low Mg²+ conditions. Thus, we concluded that carbamazepine and gabapentin may act by blocking NMDA receptors in the Sp5c, which contributes to its anti-hypersensitivity in neuropathic pain.

efficacy of gabapentin in patients with central post-stroke pain

Thalamic pain syndrome, a type of central post-stroke pain [CPSP], may develops after a hemorrhagic or ischemic stroke and results in impairment of the thalamus. There is limited experience about gabapentin in treatment of central pains like CPSP. In a prospective observational study, the intensity of pain was recorded using the Numeric Rating Scale [NRS] at the entrance to the study. Patients eligible for treating with gabapentin, received gabapentin 300 mg twice-daily. The pain intensity was measured at entrance to the study and after one month using NRS. Decrease of 3 points from the initial NRS considered being clinically significant. From a total of 180 primarily screened patients, 84 [44 men and 40 women] were recruited. There was a significant difference between pre-treatment and post-treatment NRS [5.9 +/- 2.51 vs. 4.7 +/- 3.01; 95% CI: 0.442-1.962, p = 0.002]. Fisher›s exact test showed no statistically significant effect of clinical and demographic characteristics of patients on their therapeutic response to gabapentin. Given the safety, efficacy, well tolerability and lack of interaction with other drugs we suggest gabapentin to be more considered as a first line therapy or as add-on therapy for reducing the pain severity in patients with thalamic syndrome

Clinical effects of gabapentin on the treatment of pruritus of scar resulting from deep partial-thickness burn / 中华烧伤杂志

<p><b>OBJECTIVE</b>To study the clinical effects of gabapentin on the treatment of pruritus of scar resulting from deep partial-thickness burn.</p><p><b>METHODS</b>A total of fifty-eight patients suffering from pruritus of scar after deep partial-thickness burn were hospitalized from January 2013 to January 2014. Patients were divided into placebo group (n =18, treated with oral vitamin C in the dose of 100 mg for 4 weeks, twice per day) , cetirizine group (n = 20, treated with oral cetirizine in the dose of 10 mg for 4 weeks, twice per day) , and gabapentin group (n = 20, treated with oral gabapentin in the dose of 300 mg for 4 weeks, twice per day) . Before treatment and on post treatment day (PTD) 3 and 28, the Visual Analog Scale (VAS) was used to assess the itching degree, and the mean scores were recorded. The remission rates of pruritus on PTD 3 and 28 were calculated. The adverse effects were observed during treatment. Data were processed with analysis of variance, q test, and chi-square test.</p><p><b>RESULTS</b>Compared with that before treatment, the itching degree of patients with light, moderate, and severe itching in placebo group was not relieved after treatment; the itching degree of patients with moderate or severe itching in cetirizine group was alleviated after treatment, but not in patients with light itching; itching degree of all patients in gabapentin group was significantly relieved after treatment. There were no obvious differences in VAS scores among the 3 groups before treatment (F = 2.78, P > 0.05). On PTD 3 and 28, the VAS scores of patients in both gabapentin group [(2.3 ± 0.8) and (0.6 ± 0.3) points] and cetirizine group [(4.2 ± 1.7) and (2.8 ± 1.2) points] were lower than those in placebo group [(5.7 ± 2.0) and (5.7 ± 1.9) points, with q values from 6.70 to 7.75, P values below 0.05]. The VAS scores of patients in gabapentin group on PTD 3 and 28 were lower than those in cetirizine group (with q values respectively 6.30 and 6.90, P values below 0.05). The remission rates of pruritus of patients in gabapentin group on PTD 3 and 28 were respectively (66 ± 20)% and (91 ± 17)%, and they were higher than those in cetirizine group [(33 ± 8)% and (56 ± 14)%, with q values respectively 4.70 and 3.82, P values below 0.05]. The remission rate of pruritus of patients in placebo group on PTD 3 and 28 was 0, which was lower than that of the other 2 groups each (with q values from 3.94 to 6.76, P values below 0.05). During the course of treatment, 5 patients in gabapentin group suffered from adverse effects including mild-to-moderate drowsiness and dizziness, but they disappeared one week later. No adverse effects were observed in patients of the other two groups.</p><p><b>CONCLUSIONS</b>For patients with deep partial-thickness burn, gabapentin can effectively alleviate scar itching after wound healing with safety.</p>

Metabotropic glutamate receptor 8 activation promotes the apoptosis of lung carcinoma A549 cells in vitro / 生理学报

This study aims to detect the expression of metabotropic glutamate receptors (mGluRs) in lung carcinoma A549 cells, and to investigate the effects of mGluR8 and mGluR4 activation on the growth of A549 cells in vitro. The mRNA expression levels of the 8 subtypes of mGluRs in A549 cells were determined by real-time PCR. Immunohistochemistry was used to analyze the protein expression of mGluR4 and mGluR8 in A549 cells and lung tissue sections obtained from lung adenocarcinoma patients. To observe the effects of mGluR8 and mGluR4 activation on the growth of A549 cells, the cultured cells were treated with (S)-3,4-DCPG (an agonist of mGluR8) and VU0155041 (an agonist of mGluR4), respectively, and then the cell viability was analyzed by CCK-8 kit, the percentage of DNA synthesis was detected by EdU incorporation, and the apoptosis of the cells was measured by hoechst 33258 staining and flow cytometry. The results showed that there were low expressions of mGluR1, mGluR5, mGluR6, mGluR7 mRNA, no expression of mGluR2 and mGluR3 mRNA, and high expressions of mGluR8 and mGluR4 mRNA in A549 cells. Accordingly, there were also mGluR4 and mGluR8 protein expressions in the A549 cells and the lung adenocarcinoma tissue sections. VU0155041 had no effect on the growth of A549 cells, but (S)-3,4-DCPG significantly decreased the cells' growth in a dose-dependent manner and increased the apoptosis of the cells. The results revealed a role of mGluR8 in the growth and apoptosis of A549 cells and suggested a potential target for clinical treatment of lung cancer.

Efficacy of gabapentin in the improvement of pruritus and quality of life of patients with notalgia paresthetica

BACKGROUND: notalgia paresthetica is a subdiagnosed sensory neuropathy presenting as a condition of intense itching and hyperchromic macule on the back that interferes with daily habits. OBJECTIVES: To determine the efficacy of treatment of notalgia paresthetica using oral gabapentin, assessing the degree of improvement in itching and influence on quality of life. Moreover, to evaluate the signs and symptoms associated with notalgia paresthetica. METHODS: We conducted an experimental, non-randomized, parallel, non-blinded study including 20 patients with clinical and histopathological diagnosis of notalgia paresthetica. After application of the visual analogue scale of pain adapted for pruritus and of the questionnaire of dermatology life quality index (DLQI), ten patients with visual analogue scale > 5 were given treatment with gabapentin at the dose of 300 mg/day for four weeks. The other ten were treated with topical capsaicin 0.025% daily for four weeks. After the treatment period, patients answered again the scale of itching. RESULTS: The use of gabapentin was responsible for a significant improvement in pruritus (p=0.0020). Besides itching and hyperchromic stain on the back, patients reported paresthesia and back pain. It was observed that the main factor in the worsening of the rash is heat. CONCLUSION: Gabapentin is a good option for the treatment of severe itching caused by nostalgia paresthetica. .

Activity of mediterranean fruit fly, cemtitis capitata wied [diptera: tephritidae], in response to some weather factors at Assuit governorate

A field study was carried out on the population dynamics of the Mediterranean fruit fly [MFF] Cemtitis capitata Wied. males in Assuit governorates [upper Egypt] during 2011/2012 and 2012/2013 seasons in mixed orchards by using Jakson trap. The obtained data revealed that the occurrence of MFF was relatively ail over the two seasons with some exceptions, The abundance of the pest was higher in the second season than that in the first one. The higher appearance of the pest was recorded on September-November in both first and second seasons. Temperature had significant negative correlation [r=0.105] in the first season and insignificant negative correlation [r=0.076] in the first and second seasons, respectively. However, R.H.% had high significant positive [r=0.451] and insignificant positive [r=0.203] in the first and second seasons, respectively. Results obtained could be exploited in management of this insect pest especially, in the control programs

Oral clonidine versus gabapentin as premedicant for obtunding hemodynamic response to laryngoscopy and tracheal intubation

We compared the effects of oral clonidine and gabapentin as premedicant in obtunding hemodynamic response to laryngoscopy and intubation in normotensive patients undergoing elective surgery. A total of 100 patients of either sex enrolled in the study were randomly divided into two groups of 50 each. Group A patients received oral clonidine 200 microg and Group B patients received oral gabapentin 900 mg, 90 min prior to induction of anesthesia. Both groups were matched for age, sex weight and intubation time. Anxiety score and sedation scores before induction were significantly better in Group A as compared with Group B. Heart rate rise was obtunded in Group A except at 1 min, as compared with Group B in which tachycardia persisted even at 3 and 5 min following intubation. Mean arterial pressure was maintained below baseline at all times in Group A as compared with Group B in which significant rise [+7.55%, P < 0.001] was seen at 1 min after intubation. Oral clonidine provided good attenuation of hemodynamic response to laryngoscopy and intubation as compared with oral gabapentin.

effect of pre-operative administration of gabapentin on post-operative pain relief after herniorrhaphy

Gabapentin, an anticonvulsant, recently has been suggested as an effective post-operative "analgesic" agent. The objective of the present study was to examine the analgesic effectiveness and opioid-sparing effects associated with the use of a single dose of gabapentin as a prophylactic analgesic. In a randomized double-blinded clinical trial, 50 American Society of Anesthesiologists I and II patients with an age range of 40-60 years who were the candidate for inguinal herniorrhaphy under spinal anesthesia were randomly assigned to receive 400 mg gabapentin or placebo 2 h prior to surgery. Post-operatively, the pain was assessed on a visual analog scale [VAS] at 2, 4, 12 and 24 h at rest. Morphine 0.05 mg/kg intravenously was used to treat post-operative pain on patient's demand. Total morphine consumption in the first 24 h after surgery was also recorded. Patients in the gabapentin group had significantly lower VAS scores at the all-time intervals of study than those in the placebo group [P < 0.05]. The total morphine consumption in the first 24 h after surgery was also significantly lower in gabapentin group than in the placebo group [0.9 +/- 1.23 vs. 1.8 +/- 1.5; P = 0.003]. There was no significant difference between the first time of analgesic request among the two groups. In conclusion, prophylactic administration of gabapentin decreases pain scores and analgesic consumption in the first 24 h after repair of inguinal hernia.