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.
Abdominal Wall ; Analgesia ; Analgesics ; Buprenorphine ; Dexamethasone ; Hernia, Inguinal ; Herniorrhaphy ; Humans ; Prospective Studies ; Tramadol ; Ultrasonography

No abstract available.
Anesthetics, Local ; Buprenorphine ; Peripheral Nerves

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.
Analgesia, Patient-Controlled ; Arthroplasty, Replacement, Knee ; Buprenorphine ; Catheters ; Hand ; Humans ; Incidence ; Knee Joint ; Length of Stay ; Methods ; Nausea ; Pain, Postoperative ; Passive Cutaneous Anaphylaxis ; Vomiting ; Walking

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.
Analgesics, Opioid ; Buprenorphine* ; Humans ; Opioid-Related Disorders

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.
Buprenorphine ; Evaluation Studies as Topic ; Heuristics* ; Informatics ; Korea ; Mobile Applications ; Smartphone

Introduction: Opioid dependence is recorded as the most common drug of abuse in Malaysia. Currently, the preferred substitution therapy for most Government treatment centres is methadone used as substitution therapy for opioid dependence. There are, however patients who may benefit from being on the combined buprenorphine-naloxone formulation as substitution therapy instead. We discuss six cases of opioid dependence of varied backgrounds that were treated with buprenorphinenaloxone therapy and their outcomes. Discussion: All of the reported patients improved after the induction of buprenorphine- naloxone. Two of the cases highlighted the transfer of patients on methadone to buprenorphine-naloxone due to the adverse effect and interactions of methadone with other medications. During the transfer there were no major adverse reactions noted, and patients were safely able to continue with the maintenance therapy of buprenorphine- naloxone. Conclusion: Buprenorphine-naloxone is a safe and effective drug substitution therapy for opioid dependence. It has fewer interactions with other medications, and has similar efficacy to methadone. Being a partial agonist, it has a less sedating effect making patients more functional.
Buprenorphine, Naloxone Drug Combination

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.
Anxiety ; Buprenorphine ; therapeutic use ; Double-Blind Method ; Drugs, Chinese Herbal ; therapeutic use ; Heroin Dependence ; drug therapy ; Humans ; Substance Withdrawal Syndrome ; drug therapy ; Tablets

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.
Analgesics, Opioid ; pharmacokinetics ; Animals ; Buprenorphine ; pharmacokinetics ; urine ; Female ; Male ; Rabbits ; Tissue Distribution

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.
Animals ; Biotransformation ; Buprenorphine ; analogs & derivatives ; metabolism ; pharmacokinetics ; Chromatography, High Pressure Liquid ; methods ; Dogs ; Humans ; Male ; Microsomes, Liver ; metabolism ; Rats ; Rats, Sprague-Dawley ; Species Specificity ; Tandem Mass Spectrometry ; methods

Thienorphine is a chemically-new opioid developed in Beijing Institute of Pharmacology and Toxicology. To elucidate the chemical basis for the unique pharmacological effects of thienorphine, 15 derivatives were synthesized according to combinatorial chemistry and the structure-activity relationships of these compounds were studied. It is demonstrated that thienorphine is a potent long-acting partial agonist. N-Cyclopropylmethyl is responsible for the antagonist effect of thienorphine. More importantly, thiophene at the end of side chain is most likely the pharmacophore accounts for the long-lasting effect of thienorphine. Change of the connection of thiophene and the side chain does not result in changes in the antinociceptive activity.
Animals ; Buprenorphine ; analogs & derivatives ; pharmacokinetics ; pharmacology ; Combinatorial Chemistry Techniques ; Dose-Response Relationship, Drug ; Female ; Male ; Mice ; Mice, Inbred Strains ; Morphine ; pharmacology ; Rats ; Rats, Wistar ; Receptors, Opioid ; agonists ; Structure-Activity Relationship