Exploración de la eficacia analgésica de dos parches transdérmicos analgésicos de opioides, buprenorfina y fentanilo, según sus variaciones de dosis en el control del dolor en pacientes paliativos oncológicos / Exploration of the analgesic efficacy of two-transdermal analgesic patches of opioids, buprenorphine and fentanyl, according to their dose variations in pain control in palliative cancer patients

Objetivo: El presente trabajo de investigación tuvo como objetivo explorar la eficacia analgésica mediante la comparación de la respuesta analgésica de los parches transdérmicos (PTD) de buprenorfina y fentanilo en dolor oncológico y patrón de uso. Material y Método: Se obtuvieron los datos y variables desde los registros clínicos de pacientes ingresados a la Unidad de Cuidados Paliativos (UCP) del Instituto Nacional del Cáncer (INC) que estaban bajo tratamiento en mayo del 2017. Se incluyó en este estudio a 78 pacientes con PTD, que representan el 13% de los pacientes en control mensual. De estos, 66 estaban bajo tratamiento con buprenorfina y 8 bajo tratamiento con fentanilo. Resultados: Los resultados mostraron que el PTD de buprenorfina se utiliza más frecuentemente que el de fentanilo. El principal motivo de rotación fue dolor no controlado, seguido por imposibilidad de contar con la administración por vía oral. En pacientes con mayores intensidades de dolor somático o visceral se indicó fentanilo y en aquellos con componente neuropático se prefirió el uso de buprenorfina. PTD de fentanilo fue indicado en dosis mayores que buprenorfina, incluso al comparar sus dosis equianalgésicas, siendo la variación de dosis alta para ambos parches: aumentó en promedio 257%. Se logró una mejor respuesta analgésica con buprenorfina, con una variación de intensidad de escala numérica verbal (ENV) de 2,94 y 1,88 puntos de promedio para buprenorfina y fentanilo, respectivamente. Adicionalmente, se presentó mayor reacción local dérmica con fentanilo. Conclusiones: Se evidenció diferencias en patrón de uso y, a diferencia de lo esperado, se obtuvo una mejor eficacia analgésica con buprenorfina. Datos que deben ser corroborados en estudios con mayor número de pacientes bajo tratamiento con fentanilo.

Objective: This study aims to explore analgesic efficacy comparisons of buprenorphine and fentanyl transdermal patches (TDP) in cancer pain and it's usage pattern. Material and Method: Data and variables were collected from patient's clinical reports who were admitted in the National Cancer Institute's (NCI) Palliative Care Unit (PCU) and were under treatment with TDP in May 2017. 78 TDP patients were studied and represented 13% of the monthly control patients in the PCU. Of these, 66 were under buprenorphine treatment and 8 under fentanyl treatment. Results: The results showed that buprenorphine TDP is more frequently used than fentanyl TDP, and the main reason for exchange between them was uncontrolled pain, followed by oral administration impossibility. Fentanyl TDP was indicated in patients with higher somatic or visceral pain intensities and Buprenorphine TDP was preferred in patients with neuropathic pain. Fentanyl TDP was indicated in higher doses than buprenorphine, even when comparing its equianalgesic doses, the dose variation was high for both patches throughout the treatment: it increased on average by 257%. A better analgesic response was achieved with buprenorphine, with a variation of intensity of the Verbal Numerical Scale (VNS) of 2.94 and 1.88 average points, for buprenorphine and fentanyl respectively. Additionally, there was a higher local dermal reaction with fentanyl TDP. Conclusions: Differences in usage patterns were evidenced and, unlike what was expected, better analgesic efficacy was obtained with buprenorphine TDP. This data should be corroborated in receiving fentanyl treatment.

Transdermal buprenorphine for acute postoperative pain: a systematic review / Uso da buprenorfina transdérmica na dor aguda pós-operatória: revisão sistemática

Background and objectives: Postoperative pain is still a major concern in several surgical procedures. Multimodal analgesia is best for postoperative pain management; however, opioid therapy is still the main treatment for pain after surgical procedures. Transdermal buprenorphine is a partial µ-agonist opioid widely used for chronic pain syndromes, with limited evidence for acute postoperative pain. A systematic review of studies examining transdermal buprenorphine for acute pain management after surgery was conducted. Contents: Data from PubMed, Embase, The Cochrane Central Register of Controlled Trials (CENTRAL), CINAHL via EBSCOhost, and LILACS were reviewed, including randomized clinical trials that evaluated total postoperative pain, postoperative analgesic consumption, drug-related side effects and patient satisfaction with analgesia regimen. Data from nine studies (615 patients) were included in this review. Most studies initiated transdermal buprenorphine use 6 to 48 hours before surgery, maintaining use from 1 to 28 days after the procedure. Most studies showed lower or similar postoperative pain scores, postoperative analgesic consumption and patient satisfaction comparing buprenorphine to placebo, tramadol, celecoxib, flurbiprofen and parecoxib. The incidence of side effects varied between studies, with most showing no increase in drug-related side effects with buprenorphine use, except one study, which compared buprenorphine to oral tramadol, and one to transdermal fentanyl. However, most results were derived from evidence with an overall high or unclear risk of bias. Conclusions: Although more studies are necessary, initial results show that transdermal buprenorphine seems to be an effective and safe opioid choice for management of acute postoperative pain

Justificativa e objetivos: A dor pós-operatória ainda é uma queixa importante em vários procedimentos cirúrgicos. A analgesia multimodal é a melhor conduta para a dor pós-operatória, embora a terapia com opioides ainda seja o principal tratamento para a dor após procedimentos cirúrgicos. A buprenorfina transdérmica é um opioide agonista µ amplamente prescrito nas síndromes de dor crônica, mas com limitada evidência do seu uso para dor aguda no pós-operatório. Realizamos revisão sistemática de estudos que examinaram o papel da buprenorfina transdérmica no tratamento da dor aguda pós-operatória. Conteúdo: Revisamos os dados de PubMed, Embase, Registro Central de Ensaios Controlados Cochrane (CENTRAL), CINAHL via EBSCOhost e LILACS, incluindo estudos clínicos randomizados que avaliaram a dor pós-operatória total, consumo de analgésicos pós-operatórios, efeitos colaterais relacionados a medicamentos e satisfação do paciente com esquema de analgesia. Dados de nove estudos (615 pacientes) foram incluídos nesta revisão. A maioria dos estudos iniciou o uso transdérmico de buprenorfina 6 a 48 horas antes da cirurgia, mantendo o uso de 1 a 28 dias após o procedimento. A maioria dos estudos encontrou valores semelhantes ou menores para o escore de dor pós-operatória, consumo pós-operatório de analgésicos e satisfação do paciente quando a buprenorfina foi comparada ao placebo, tramadol, celecoxibe, flurbiprofeno e parecoxibe. A incidência de efeitos colaterais oscilou nos estudos, e a maioria não mostrou aumento de efeito colateral relacionado ao uso de buprenorfina, exceto em dois estudos, um que comparou buprenorfina ao tramadol oral e outro ao fentanil transdérmico. No entanto, a maioria dos resultados foi obtida a partir de evidências com um risco geral alto ou risco de viés impreciso. Conclusões: Embora sejam necessários mais estudos, os resultados iniciais mostram que a buprenorfina transdérmica parece ser uma forma de administração segura e efetiva de opioide no tratamento da dor aguda pós-operatória

Analysis of psychiatrists' prescription of opioid, benzodiazepine, and buprenorphine in Medicare Part D in the United States

Abstract Introduction The opioid epidemic is a severe problem in the world, especially in the United States, where prescription opioid overdose accounts for a quarter of drug overdose deaths. Objective To describe psychiatrists' prescription of opioid, benzodiazepine, and buprenorphine in the United States. Methods We conducted a retrospective cross-sectional study of the 2016 Medicare Part D claims data and analyzed psychiatrists' prescriptions of: 1) opioids; 2) benzodiazepines, whose concurrent prescription with opioids can cause overdose death; 3) buprenorphine, a partial opioid agonist for treating opioid addiction; 4) and naltrexone microsphere, a once-monthly injectable opioid antagonist to prevent relapse to opioid dependence. Prescribers with 11 or more claims were included in the analysis. Results In Medicare Part D in 2016, there were a total of 1,131,550 prescribers accounting for 1,480,972,766 total prescriptions and 78,145,305 opioid prescriptions, including 25,528 psychiatrists (2.6% of all prescribers) accounting for 44,684,504 total prescriptions (3.0% of all prescriptions) and 131,115 opioid prescriptions (0.2% of all opioid prescriptions). Psychiatrists accounted for 17.3% of benzodiazepine, 16.3% of buprenorphine, and 33.4% of naltrexone microsphere prescriptions. The opioid prescription rate of psychiatrists was much lower than that of all prescribers (0.3 vs 5.3%). The buprenorphine prescription rate of psychiatrists was much higher than that of all prescribers (2.3 vs. 0.1%). There was a substantial geographical variation across the United States. Conclusions The results show that, proportionally, psychiatrists have lower rates of opioid prescription and higher rates of benzodiazepine and buprenorphine prescription.

Effect of addition of buprenorphine or dexamethasone to levobupivacaine on postoperative analgesia in ultrasound guided transversus abdominis plane block in patients undergoing unilateral inguinal hernia repair: a prospective randomized double blind controlled trial / 대한마취과학회지

BACKGROUND: The transversus abdominis plane (TAP) block is an effective technique to block the thoracolumbar nerves innervating the anterolateral abdominal wall. This study was conducted to evaluate the analgesic efficacy and opioid consumption with the use of perineural buprenorphine or dexamethasone in TAP blocks after unilateral inguinal hernioplasties. METHODS: This prospective, randomized, double-blinded, placebo-controlled study enrolled 93 patients scheduled for unilateral inguinal hernioplasty, followed by an ultrasound-guided TAP block. The participants were randomized into 3 groups (31 patients each). Group L received 20 ml 0.25% levobupivacaine + 1 ml normal saline (NS); group LB, 20 ml 0.25% levobupivacaine + 0.3 mg (1 ml) buprenorphine; and group LD, 20 ml 0.25% levobupivacaine + 4 mg (1 ml) dexamethasone. The patients were observed postoperatively for 24 h for first rescue analgesic requirement, total rescue analgesic consumption, and pain scores on the numeric rating scale (NRS). RESULTS: The time to first rescue analgesic requirement was significantly longer in Group LB than in groups LD and L (688.87 ± 36.11 min, 601.45 ± 39.85 min, and 383.06 ± 36.21 min, respectively; P < 0.001). The mean total tramadol consumption in the first 24 h was the lowest in group LB (P < 0.001, L vs. LB / LD). Groups LB and LD displayed significantly lower NRS scores than group L (P < 0.001 both). CONCLUSIONS: Levobupivacaine with perineural buprenorphine in a TAP block after unilateral open inguinal hernioplasty facilitates prolonged analgesia and reduced requirement for rescue analgesics compared to perineural dexamethasone, without significant side effects.

Buprenorphine as an adjuvant to local anesthetics in peripheral nerve blocks / 대한통증학회지

No abstract available.

Comparison of the Clinical Outcomes of a Single Injection Adductor Canal Block with the Concomitant Use of Transdermal Buprenorphine and Continuous Adductor Canal Block after Total Knee Arthroplasty / 대한정형외과학회잡지

PURPOSE: To compare the clinical outcomes of single injection adductor canal block (SACB), continuous adductor canal block (CACB), and the concomitant use of transdermal buprenorphine after total knee arthroplasty (TKA). MATERIALS AND METHODS: A total of 125 patients who underwent TKA were divided into three groups and the clinical results were retrospecitively compared. Group I was comprised of patients with pain controlled by SACB (n=41). Group II consisted of patients with pain controlled by both SACB and transdermal buprenorphine (10 µg/h) (n=44). Group III contained patients with pain controlled by CACB (n=40). The visual analogue scale (VAS) was used as the pain control indicator and the patients were measured on a VAS for resting on the bed (VAS-Rest) at 12 hours, 24 hours, and 48 hours after surgery. The VAS while doing continuous passive motion (VAS-CPM) on the first and second postoperative day was also measured. In addition, the total amount of medications used (Butopahn, Tridol, and Ketorac) for the intravenous patient controlled analgesia (PCA) was counted for 48 hours after surgery. As the indicator of the functional recovery outcome, the incidence of nausea and vomiting was observed for 48 hours after surgery. The maximum knee joint flexion range and maximum walking distance on the first and second postoperative day, and the total length of stay at the hospital were compared. RESULTS: The VAS-Rest was similar in the three groups at 12 hours after surgery, but at 24 hours and 48 hours after surgery, group II and III a lower VAS-CPM and total amount of medications used for PCA than group I (p<0.05). The three groups showed a low incidence of nausea and vomiting, maximum knee joint flexion range, and similar walking distance and total length of stay at the hospital. CONCLUSION: The combination of SACB and transdermal buprenorphine has great pain control effect initially. On the other hand, it is not associated with catheter complications and it is convenient to use and safety toward the renal function. Therefore, the concomitant use of SACB and transdermal buprenorphine can be an effective pain control method after TKA.

Successful Treatment with Transdermal Buprenorphine Patch in Opioid-Dependent Cancer Patients: Case Series / 한국호스피스완화의료학회지

Opioid aberrant behavior is an emerging problem as strong opioid is increasingly used to alleviate cancer pain in patients with cancer. Although the treatment of opioid addiction and physical dependence for non-cancer pain is well known, few studies have been conducted with cancer patients, particularly in the Korean population. Presented here are ten cases of cancer patients who were physically dependent on strong opioid and successfully treated with a partial mu-opioid receptor agonist, buprenorphine. This is the first report showing the efficacy of transdermal buprenorphine as a treatment for physical dependence on opioid medication in cancer patients.

Efectividad del cambio de tratamiento desde Metadona a Buprenorfina/Naloxona en dependientes a opiáceos, Bilbao - España / Effectiveness of treatment change from methadone to Buprenorphine / Naloxone in opiate dependents, Bilbao - Spain

A nivel mundial la dependencia a opiáceos es un problema vigente, y los pacientes afectados por esta condición requieren programas de tratamiento sustitutivo farmacológico, que utilizan tradicionalmente Metadona. Actualmente, existe debate sobre el hecho de que la Buprenorfina/Naloxona podria ser utilizada como un reemplazo adecuado del fármaco tradicional. Las investigaciones aún no son totalmente concluyentes, faltando estudios que prueben los resultados en la práctica clínica. Objetivos: Determinar la efectividad del tratamiento con Buprenorfina/Naloxona como reemplazo de la metadona en pacientes dependientes de opiáceos tratados en un Módulo de Asistencia Psicosocial en la ciudad de Bilbao, España. Métodos: Se realizó un estudio cuasiexperimental, cuantitativo, longitudinal, prospectivo, con 21 pacientes dependientes de opiáceos que formaban parte del Programa de mantenimiento con Metadona con dosis inferiores o iguales a 40 mg/día, en quienes se sustituyó ese tratamiento por el de Buprenorfina/Naloxona (8mg/2mg) siguiendo para esto los criterios de la Guía para el tratamiento de la adicción a opiáceos con Buprenorfina/Naloxona de la Sociedad Científica Española de estudios sobre alcohol, el alcoholismo y otras toxicomanías del 2010. Resultados: Después de tres meses de cambio de terapéutica a Buprenorfina/Naloxona se evidencio una reducción estadísticamente significativa en el consumo de opiáceos ilegales, medido a través de los controles de substancias en orina desde un promedio de 2,67 controles positivos con metadona, a 2,24 controles con Buprenorfina/Naloxona. La adherencia, se mantuvo similar a la previa, presentando además una retención del 100% de los pacientes. La calidad de vida, medida con el Test TECVASP, presento una mejora estadísticamente significativa, desde una puntuación de 76,76 cuando recibían Metadona (DE 6,41) hasta 90,33 (DE 5,77 ) con la nueva terapéutica. Conclusiones: Cambiar la terapia de mantenimiento con Metadona, en pacientes dependientes de opioides, por buprenorfina/naloxona es una buena opción, ya que tiene una efectividad similar en términos de adherencia y retención, y produce una mayor reducción en el uso de opiáceos ilegales, al tiempo que mejora la calidad de vida del paciente.

At the global level, opioid dependence is an ongoing problem, and patients with this condition require pharmacological substitution treatment programs, which traditionally use methadone. Currently there is debate over whether Buprenorphine / Naloxone could be used as a suitable replacement for the traditional drug. The investigations are not yet totally conclusive, lacking studies that prove the results in the clinical practice. Objectives: To determine the effectiveness of treatment with Buprenorphine / Naloxone as a replacement for Methadone in opioid dependent patients treated in a Psychosocial Assistance Module in the city of Bilbao, Spain. Methods: A quasi-experimental, quantitative, longitudinal, prospective study was conducted with 21 opioid-dependent patients that were part of the maintenance program with Methadone at doses lower than or equal to 40 mg / day, in which treatment was replaced by that of Buprenorphine / Naloxone (8 mg/2 mg) following for this the criteria of the Guide for the treatment of the addiction to opiates with Buprenorphine / Naloxone of the Spanish Scientific Society of studies on alcohol, alcoholism and other drug addictions of 2010. Results: After a three-month change in therapy to Buprenorphine / Naloxone, a statistically significant reduction in illegal opioid use was observed, measured through urine substance controls from an average of 2.67 methadone-positive controls 2.24 controls with Buprenorphine / Naloxone. The Adherence remained similar to the previous one, presenting a retention of 100% of the patients. Quality of life, measured with the TECVASP test, showed a statistically significant improvement, from a score of 76.76 when receiving Methadone (DE 6.41) to 90.33 (DE 5.77) with the new therapy. Conclusions: Changing maintenance therapy with methadone, in opioid-dependent patients, by buprenorphine/naloxone is a good option, because it has a similar effectiveness in terms of adherence and retention, and produces a greater reduction in the use of illegal opiates, and the same time improves the quality of life of the patient.

Development and Cross-cultural Validation of the Korean Version of SMArtphone’s uSability Heuristics (SMASH) / 대한의료정보학회지

OBJECTIVES: The purpose of this study was to develop and cross-culturally validate the Korean version of SMArtphone's uSability Heuristics (K-SMASH). METHODS: In the study, it was used the adaptation process consisted of five stages, namely, translation, synthesis, back translation, expert committee review, and pretesting. In the pretesting stage, a mobile application, using the prefinal K-SMASH, was evaluated for the severity of usability problems by three experts in computer science and informatics. Each participant completed the evaluation and was interviewed about their understanding, interpretation, and opinion of the cultural relevance of the prefinal K-SMASH. Next, we reviewed the differences in the experts’ opinions and the questionnaire results. RESULTS: Twelve SMASH items, words and sentences, were translated, back translated, and revised, considering the conceptual meaning in the context of the Korean culture, by experts in various fields, including a Korean linguist and a bilingual translator, through the first stage to the fourth stage. In the pretesting stage, the results showed no major differences among the severity ratings of participants. Furthermore, all participants answered that there were no critical discrepancies or inconsistencies with the cultural relevance of the prefinal K-SMASH. CONCLUSIONS: The results of the study provide preliminary evidence that the modified K-SMASH can be used for heuristic evaluation, one of the usability tests, when developing applications in Korea.

Eficacia y seguridad del uso de buprenorfina parche transdérmico de 35 mcg/h - 20mg en pacientes con dolor crónico oncológico moderado a severo que no toleran otro tratamiento analgésico por vía oral, vía endovenosa o vía subcutánea / Efficacy and safety of the use of buprenorphine transdermal patch of 35 mcg / h - 20mg in patients with moderate to severe chronic oncologic pain who do not tolerate another analgesic treatment by oral, intravenous or subcutaneous route

INTRODUCCIÓN: Antecedentes: El presente dictamen expone la evaluación de tecnología de la eficacia y seguridad del uso buprenorfina parche transdérmico 35mcg/h- 20mg en pacientes con dolor crónico oncológico, moderado a severo, que no toleran otro tratamiento analgésico opioide previo por vía oral, vía endovenosa o vía subcutánea. Aspectos Generales: El dolor es un síntoma frecuente en los pacientes con cáncer. De acuerdo a una revisión sistemática que incluye información de estudios realizados en los últimos 50 años, la prevalencia del dolor oncológico es de 55% en los pacientes en tratamiento antineoplásico, 66.4% en pacientes con enfermedad avanzada (i.e. metastásica o terminal) y 33% en pacientes después de tratamiento curativo. Tecnologia Sanitaria de Interés: La buprenorfina es un opioide con propiedades mixtas agonistas y antogonistas. Su actividad agonista parcial se da en los receptores opioides p y ORL-1, mientras que las propiedades antagonistas se dan en los receptores kappa y delta. METODOLOGIA: Estrategia de Búsqueda: Se realizó una estrategia de búsqueda sistemática de la evidencia científica con respecto a la eficacia y seguridad de eficacia y seguridad de buprenorfina parche transdérmico para dolor oncológico, moderado a severo. Esta búsqueda se realizó utilizando los meta-buscadores: Translating Research into Practice (TRIPDATABASE), National Library of Medicine (Pubmed-Medline) y Health Systems Evidence. Adicionalmente, se amplió la búsqueda revisando la evidencia generada por grupos internacionales que realizan revisiones sistemáticas (RS), evaluación de tecnologías sanitarias (ETS) y guías de práctica clínica (GPC), como la Cochrane Group, The National Institute for Health and Care Excellence (NICE), the Agency for Health cave Research and Quality (AHRQ), y The Scottish Medicines 1Consortium (SMC). RESULTADOS: Sinopsis de la Evidencia: Se realizó búsqueda bibliográfica y de evidencia científica para el sustento del uso de buprenorfina para dolor crónico oncológico que no tolera tratamiento previo Se presenta la evidencia disponible según el tipo de publicación priorizada en los criterios de inclusión. CONCLUSIONES: La presente evaluación de tecnología sanitaria tuvo por objetivo la evaluación de la eficacia y seguridad del uso de burprenorfina parche transdérmico de 35 mcg/h - 20mg en pacientes con dolor crónico oncológico moderado a severo que no toleran otro tratamiento analgésico por vía oral, vía endovenosa o vía subcutánea. Fueron incluidos un total de 24 publicaciones científicas (5 guías de práctica clínica, 8 revisiones sistemáticas y 11 estudios primarios). Para el tratamiento del dolor crónico oncológico moderado a severo dolor, la morfina sigue siendo la terapia de primera línea. No se encontró evidencia suficiente para considerar a la buprenorfina transdérmica como una opción válida de medicamento de primera línea, comparada con las opciones terapéuticas tradicionales. Sin embargo, su vía de administración transdérmica hace que su uso pueda ser una buena opción para pacientes que no puedan ingerir medicamentos por vía oral. Si se decide el uso de buprenorfina transdérmica, ésta debe ser usada en pacientes con dolor estable. La conversión de opioides orales a buprenorfina transdérmica debe ser calculada para cada caso y con ayuda de un especialista. El uso de opioides debe tener una previa evaluación cuidadosa del paciente, valorando los factores de riesgo de cada paciente. El seguimiento debe ser realizado con frecuencia, para evaluar efectos adversos y adicción. Por lo expuesto, el Instituto de Evaluación de Tecnologías en Salud e Investigación- IETSI, aprueba el uso de buprenorfina transdérmica en pacientes con dolor oncológico moderado a severo, que no toleran la vía oral, endovenosa o subcutánea o en los que el tratamiento analgésico opioide previo ya no es una alternativa por presentar eventos adversos o toxicidad por acumulación de metabolitos, según lo establecido en el anexol. El presente dictamen tiene vigencia de 1 año a partir de la fecha de publicación.

A randomized, double-blind, controlled study: Ji-Tai tablet for the treatment of acute withdrawl syndrome of mild heroin dependence / 中南大学学报(医学版)

OBJECTIVE@#To investigate the efficacy and safety of Ji-Tai tablet and Ji-Tai tablet combined with buprenorphine in the treatment of patients with acute withdrawal syndrome of mild heroin dependence.@*METHODS@#A total of 150 patients with mild heroin dependence were recruited, and were randomly assigned to a Ji-Tai tablet group (n=50), a Ji-Tai tablet combined with buprenorphine group (n=50) and a control group (n=50) during a 10-day clinical trial. Opiate withdrawal scale (OWS) was used to measure the severity of withdrawal symptoms. Anxiety symptoms assessments were made at 0 day (baseline), the day 5 (middle), and the day 10 (end) by the Hamilton anxiety scale (HAMA). Symptoms were assessed before and 1 h or 2 h after medication each day. The total withdrawal symptoms scores and the daily reduction rate were used to measure the effect of Ji-Tai tablet vs Ji- Tai tablet plus buprenorphine. Safety evaluation was carried out by the following measures: baseline of treatment, drug side effects after the treatment, vital signs (blood pressure, heart rate, and respiration rate), laboratory examination (routine blood and urine tests and the liver and kidney function tests), and electrocardiograms.@*RESULTS@#A total of 142 mild heroin dependence patients performed the experiments (including 48 in the Ji-Tai tablet group, 48 in the Ji-Tai tablet with buprenorphine group and 46 in the control group). The scores of baseline withdrawal symptoms were 43.520±19.786, 42.640±17.648 and 47.100±24.450, respectively, with no significant differences among the 3 groups (all P>0.05 ). During the 10-day treatment, the reduction rate of acute withdrawal symptoms scores increased daily, the acute withdrawal syndrome scores and the anxiety symptoms scores declined from day 0 to day 10, there was also no significant difference among the 3 groups (all P>0.05). Ji-Tai tablet did not affect vital signs such as blood pressure, heart rate, and respiration rate.@*CONCLUSION@#Ji-Tai tablet or Ji-Tai tablet combined with buprenorphine had no effect on acute withdrawal symptoms of mild heroin dependence.

Right upper-quadrant pain in a patient with drug abuse, secondary syphilis and occult hepatitis B virus

To describe the etiology of hepatitis and identify occult hepatitis B virus [HBV] infection. Clinical Presentation and Intervention: A 40-year-old man presented with severe abdominal pain and jaundice, a history of acute HBV infection that had cleared as well as the use of acetaminophen, methamphetamine, buprenorphine and marijuana. He admitted to having had unprotected sex with multiple partners of both genders. A thorough skin examination revealed papulosquamous lesions on his penis, scrotum, upper and lower extremities and feet. Transaminases and bilirubin were elevated. His rapid plasma reagin was reactive, and hepatitis serologies showed occult HBV. Liver biopsy showed severe hepatitis, but the stains for hepatitis B surface antigen and hepatitis B core antigen were negative. The pathological findings were highly indicative of drug-induced hepatitis without evidence of chronic hepatitis, reactivation of HBV or syphilitic hepatitis. With supportive management and abstinence from drugs, his condition improved. This case describes a patient with multiple potential causes for hepatitis and highlights the importance of obtaining a detailed social history. Further, one should consider the presence of occult HBV and recognize the serologic pattern

Study on the distribution of buprenorphione in the bodies of the rabbits / 中南大学学报(医学版)

OBJECTIVE@#To investigate the distribution of buprenorphione in the bodies of rabbits.@*METHODS@#Buprenorphione was administrated to rabbits orally or by intravenous injection (0.04 mg/kg buprenorphione). Two hours after administration, rabbits were killed and their blood, urine, liver, kidney, lung, stomach, brain, heart, stomach content and feces were collected. The concentrations of buprenorphione in these body fluids and tissues were determined by liquid chromatography-mass spectrometry (LC-MS).@*RESULTS@#The results show the distribution of buprenorphione in rabbit's body: urine>stomach content>brain >heart >stomach>lung> kidney > liver > blood> feces.@*CONCLUSION@#The method developed can be used for the detection of buprenorphione in biological fluids and tissues in forensic practice. Urine is the preferred sample for screening for buprenorphione abuse.

quantitative and qualitative study of rat testis following administration of methadone and buprenorphine

Opiate abuse is a matter of serious concern in adolescent men. The primary drugs used in the treatment of opiate addiction are methadone and buprenorphine. This study was undertaken to determine the quantitative and qualitative changes in rat testes after methadone and buprenorphine administration. In this experimental study, 15 male Wistar rats, each weighing 250 +/- 15 g, were selected and randomly divided into 3 groups [n = 5]. The first group received an intraperitoneal dose of 0.5 mg/kg/day methadone and the second group received an intraperitoneal dose of 30 mg/kg/day buprenorphine for 15 days each. The third group [control] received normal saline injections. After the last injection dose, the rats were sacrificed and their testes were removed, weighed, and fixed in modified Lillie's solution, and embedded in 3.5% agar, after which 1-mm slices perpendicular to the long axis of the testes were prepared using a tissue slicer. Then, on the basis of Cavaleri's principle, the testis volume was calculated by point-counting method. For histological analysis, systematic random samples of each testis were selected, processed, and stained by hematoxylin and eosin [H and E] and periodic acid schiff [PAS] methods. The results obtained for the 3 groups were compared using nonparametric Kruskal-Wallis test. P < 0.05 was considered as the level of significance. Stereological analysis of rat testes showed no significant effect of methadone and buprenorphine administration on the testis volume [P > 0.05]. However, microscopic studies of rat tissues in the methadone-administered group showed atrophic seminiferous tubules, reduction of sperm stem cells, destruction of Sertoli cells, irregularities in the basement membrane of seminiferous tubules, cellular degeneration of spermatogonia and primary spermatocytes, and significantly fewer spermatozoids than in the control group. Furthermore, in the methadone-administered group, the germinal cells of seminiferous tubules were damaged and extensively detached from the basement membrane and the vessels of the interstitial tissue were congested. Microscopic studies of the buprenorphine-administered group showed no significant changes in the basement membrane, seminiferous tubules, Sertoli cells, interstitial tissue, and sperms. Buprenorphine is more suitable for treating opiate addiction in males since it does not affect normal testicular structure and function

Tramal as a monotheraphy; pain buprenorphine with control - a comparison

To achieve reduction in postoperative pain and improved quality of analgesia accompanied by reduction in side effects. This study was carried out by the anaesthesia department and intensive care unit, Nishtar Hospital, Multan from June 2009 to May 2010. A total of 200 patients were observed, which were undergoing for thyroidectomy and were divided into two groups. The duration of analgesia in the two groups was almost similar. Rescue analgesia was given to 10 patients out of 100 patients in Buprenorphine and 24 patients out of 100 patients in tramadol. Pain scores were more in group-I than group-II, although nausea/vomiting were more in group-I than in group-II. This analgesia regimen of intramuscular buprenorphine was found to be an improved, balanced and safe analgesic technique for postoperative pain relief

Avances en la comprensión de las adicciones: niveles, modelos, farmacoterapia / Progress in the understanding of addictins: Levels, models, pharmacotherapy

La comprensión de los mecanismos subyacentes en las diversas adicciones avanza continuamente. Las diferentes líneas de investigación, ya sea tanto en el plano molecular, o de los circuitos y áreas involucradas, como así también de los abordajes psicosociales, profundizan su búsqueda con el objetivo de mejorar la eficacia de los tratamientos. Un interesante artículo de Koob y colaboradores (2009), que lleva por subtítulo El abordaje de la piedra de Rosetta, revisa detalladamente los distintos niveles en juego en esta compleja problemática. El objetivo del mencionado artículo es aportar elementos en el sentido de favorecer el desarrollo de fármacos adecuados para el tratamiento de estas condiciones patológicas, que incluyen tanto el uso de drogas ilícitas, como del alcohol y el tabaco. Las actuales farmacoterapias utilizadas para el tratamiento de la adicción pueden ser empleadas para validar y mejorar los modelos de laboratorios en animales y humanos, para así identificar nuevos candidatos viables para tratamientos. Esta aproximación tiene la capacidad de promover la investigación traslacional y puede proveer un marco heurístico para desarrollar farmacoterapias eficientes y efectivas para la adicción

The comprehension of the mechanisms underlying the different addictions is in constant progess. The different lines of research, both in the molecular field or the circuits and areas involved, as well as in psychosocial approaches emphasize their investigations with the purpose of enhancing the efficacy of the treatments. An interesting article by Koob et al (2009), which is subtitled "The Rosetta Stone Approach", provides a detailed review of the different levels involved in this complex issue. The purpose of the mentioned article is to provide elements that promote the development of pharmacological drugs suitable for the treatment of these pathological conditions, which include both the use of illegal drugs, as well as acohol and tobacco. The current pharmacological therapies used for the treatment of addiction can be used to validate and improve labortory models in animals and humans, in order to identify new potential candidates for treatments. This approach is able to promote a translational research and can offer a heuristic framework to develop efficient and effective pharmacotherapies for addiction

Buprenorfina transdérmica en el manejo del dolor crónico nociceptivo y neuropático no oncológico en ortopedia / Buprenorfine transdermal matrix patch in the treatment of chronic nociceptive non malignant pain and neurophatic pain in the orthopaedic patology

Objetivo: siendo el año del dolor musculoesquelético, es importante evitar el subtratamiento, dado la prevalencia de dolor crónico, los costos, limitación funcional y disminución de la calidad de vida en el paciente ortopédico, requiriéndose de vías menos invasivas, como la administración transdérmica, a través de sistema matricial de buprenorfina, en base a su liposolubilidad, y biodisponibilidad, sin riesgo de hiperalgesia ni afectación del sistema inmune, considerando su efecto techo en depresión respiratoria, y su empleo en comorbilidad renal y hepática. Material y métodos: estudio longitudinal, prospectivo, aleatorizado, de septiembre de 2008 a febrero de 2010, en el servicio de algología de orthocaz, unidad de ortopedia. N=108 de ambos sexos bajo consentimiento informado. Resultados: prevalencia de dolor en consulta externa de ortopedia r= 60-80 por ciento, x = 70, el crónico nociceptivo mayor de 30 por ciento y neuropático 1, 5 por ciento con predominio en el sexo femenino de 53,8 por ciento y, etiológicamente, el síndrome de columna fallida ocupa 40,7 por ciento, osteoartrosis 44, 4 por ciento, edad X= 66,59 años r= 20-85, dolor neuropático crónico secundario a metástasis en columna lumbar 3,7. La causa más común fue cáncer prostático, síndrome complejo regional 3,7 por ciento, el tamaño del efecto (EZ) fue de 1,2 el NNT= 4, a la 3ra semana se incrementó el dolor incidental e irruptivo, a partir del 10º día disminuyeron los efectos secundarios, como la somnolencia y nausea. Discusión y conclusiones: la osteoartritis, el síndrome de columna fallida, conducto lumbar estrecho mixto, síndrome complejo regional, secuelas de fracturas, prótesis fallidas, secuelas de displasia del desarrollo de la cadera, síndrome doloroso lumbar crónico, son padecimientos musculoesqueléticos en el que se aceptan el manejo de opiodes clase 3 de la OMS, de libración prolongada, como la buprenorfina...

Objetive: being the international year of the pain skeletal muscle, it is important to avoid the sub treatment, dice the prevalence of chronic pain, with the costs, functional limitation and diminution of the quality of life in the orthopedic patient requiring itself of less invasive routes as it is it the transdermal administration through matrix system of buprenorfina, on the basis of his high lip solubility without risk of hiperalgesia nor affectation of inmune system, considering his effect ceiling in respiratory depression, and its use in renal and hepatic comorbidity. Material and methodology: longitudinal, prospective study, randomized, of September of the 2008 to February 2010, in the service of algology of Orthocaz unit of N= orthopedics 108 both sexes, under informed consent. Results: Prevalence of pain in external consultation of orthopedics r= 60-80 per cent, x =70, the chronic greater nociceptive of 30 percent and neurophatic 1,5 percent with predominance in 53,8 percent feminine sex etiology the syndrome of insolvent column occupies 40,7 percent, osteoartrosis 44,4 percent, X= age 66,59 years, r= 20-85, secondary chronic neuropathic pain to metastasis in 3,7 lumbar column the cause most common prostate cancer, regional complex syndrome 3,7 percent the size of effect (EZ) the EU of 1,2 NNT= 4, to third week increase the incidental and irruptive pain, from the 10 day diminished the indirect effect, as drowsiness and feels nauseous. Discussion and and conclusions osteoarthritis, syndrome of insolvent column, lumbar conduit narrow compound, regional complex syndrome, sequels of fractures, prosthesis insolvent, sequels of dysplasia of the developement of the hip, chronic lumbar painful syndrome, are sufferings skeletal muscle in wich the handing of opiods is accepted class III, of the WHO of liberation prolonged as it is it buprenorfina transdermal, wih progressive degree, and to allow tolerability.

In vitro comparison of thienorphine metabolism in liver microsomes of human, Beagle dog and rat / 药学学报

The inter-species differences of thienorphine metabolism were investigated in human, Beagle dog and rat liver microsomes, by comparing enzyme kinetics of the parent drug and the formation of its major metabolites. The incubation systems of thienorphine with liver microsomes of the three species were optimized in terms of thienorphine concentration, microsomal protein content and incubation time. The concentrations of thienorphine and its metabolites in incubates were measured by a LC-MS/MS method. The biotransformation of thienorphine by human liver microsomes was the lowest among the three species. The K(m), V(max), CL(int) and T1/2 of thienorphine obtained from human liver microsomes were (4.00 +/- 0.59) micromol x L(-1), (0.21 +/- 0.06) micromol x L(-1) x min(-1), (117 +/- 3.19) mL x min(-1) x kg(-1) and (223 +/- 6.10) min, respectively. The corresponding kinetic parameters for dog and rat liver microsomes were (3.57 +/- 0.69) and (3.28 +/- 0.50) micromol x L(-1), (0.18 +/- 0.04) and (0.14 +/- 0.04) micromol x L(-1) x min(-1), (213 +/- 1.06) and (527 +/- 7.79) mL x min(-1) x kg(-1), (244 +/- 1.21) and (70.7 +/- 1.05) min, respectively. A total of six phase I metabolites were observed in liver microsomes, including one N-dealkylated metabolite, three oxidative metabolites and two N-dealkylated oxidation metabolites. All these six metabolites were detected in the liver microsomes of the three species. However, the relative amounts of the metabolites generated were different in three species. The results indicated that the major phase I metabolic pathway of thienorphine was similar in the liver microsomes from all three species. However, the inter-species differences observed were relative amounts of the metabolites as well as the metabolic characteristics of thienorphine in liver microsomal incubates.

Buprenorfina en el manejo de dolor por cáncer / The Use of Buprenorphine to Control Cancer Pain

Actualmente los opioides son el soporte del manejo farmacológico, en particular del dolor moderado a severo. En este sentido, es importante disponer de distintas formulaciones y vías de administración, aún más en el contexto del paciente oncológico. La buprenorfina tiene un bajo peso molecular, de alta potencia y liposolubilidad combinada a una favorable tolerabilidad y un bajo potencial de abuso. Por dichas razones la buprenorfina es ideal para aplicación transdérmica. La evidencia clínica disponible demuestra eficacia y seguridad en el empleo de la buprenorfina transdérmica en el tratamiento de dolor de moderado a severo en el paciente oncológico. Sin embargo, la buprenorfina no ha sido extensamente estudiada en ciertas poblaciones como otros opioides y se requieren nuevas investigaciones para definir el rol de esta en circunstancias clínicas específicas.

Opiods are the current pharmalogical remedies of choice for the control of moderate to severe pain. Subsequently, it is important to rely on a number of prescriptions and applications for these drugs, particularly in the case of oncological patients. Low molecular weight, high potency and liposolubility of buprenorphine combine with its favorable tolerance and low abuse probability. Clinical evidence reveals that the use of transdermal buprenorphine in the treatment of moderate to severe pain in oncological patients is effective and safe. However, buprenorphine has not been widely studied among certain populations, as have other opiods, thus making further research necessary in order to define its role under specific clinical circumstances.