• Title/Summary/Keyword: buprenorphine

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Sucrose-Gap Apparatus를 이용한 말초신경계의 Opiate수용체 검색법

  • ;George B. Frank
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1992.05a
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    • pp.40-40
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    • 1992
  • opiate receptor들의 중추신경계에서의 분포 및 작용에 관한 실험물은 널리 알려져 있어 그 웅용 방법도 많이 있으나, 말초에 있는 opiate receptor의 존재 및 약물작용을 관찰하는 실험은 별로 알려진 것은 없다. 저자는 214mM의 sucrose 용역을 이용하여 전기적 자극에 따른 말초신경 및 말초조직(근육)에서의 opiate receptor애 대한 작용을 관찰하였다. 실험은 3분류의 약물을 이용하였다. 1) Pure agonists: morphine, meperidine, methadone, 2) Agonist-antagonist: buprenorphine 3) Pure antagonist: naloxone 위의 약물들을 이용하여 excitable cell membrane(좌골신경 및 근육)에서 일어나는 potential의 변화를 관찰하여 다음과 같은 결과를 얻었다. a. pure agonists들은 좌골신경 및 근육절편에서 action potentials을 의의있게 억제시켰으며 meperidine이 가장 강한 작용을 보였다. b. 이들의 작용은 naloxone 투여로 억제되었다. c. Agonist-antagonist인 buprenorphine은 투여용량 및 동시 투여한 pure agonist의 종류에 따라 biphasic pattern을 나타내었다. d. opiates 작용기전 및 약물작용장소를 알고자 두 종류, 즉 single 및 double technique을 사용하여 비교하였다.

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Antihypertensives affects on the drug metabolism of buprenorphine

  • Ahn, Mee-Ryung;Yoo, Tae-Moo;Sohn, Soo-Jung;Park, In-Sook;Suh, Soo-Kyung;Yang, Ji-Sun;Choi, Hong-Serck
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.81.1-81.1
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    • 2003
  • Buprenorphine(BPN) is used to treat withdrawal syndromes in narcotic addictions. When narcotics are stopped, withdrawal syndromes such as pupil dilation and blood pressure increment are appeared. And BPN is often prescribed concomitantly with antihypertensives. We researched whether combined medicines of BPN and antihypertensives affected on the metabolism of BPN. After BPN was incubated with antihypertensives such as nifedipine, verapamil, captopril and propranolol in rat or human microsomes, amounts of BPN and its metabolite, norbuprenorphine (NBPN), were measured. (omitted)

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Comparison of the Postoperative Pain Control Effects of a Buprenorphine Transdermal Patch on Total Knee Arthroplasty Surgery Patients according to Its Applied Sites: Retrospective Case-Control Study (슬관절 인공관절 전치환술 환자에서 부프레노르핀 경피 패치의 적용부위에 따른 수술 후 통증 조절 효과 비교: 후향적 환자-대조군 연구)

  • Kim, Ok-Gul;Lee, Sang-Wook;Kim, Hyun-Min
    • Journal of the Korean Orthopaedic Association
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    • v.55 no.6
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    • pp.527-533
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    • 2020
  • Purpose: This study compared the effects of a buprenorphine transdermal patch (BTDP) on the chest and knee for pain control after total knee arthroplasty (TKA). Materials and Methods: A retrospective case-control study was conducted from August 2018 to August 2019 on 231 patients who underwent TKA. Two hundred cases were selected considering age, sex, and body mass index. Before and after applying the BTDP, the Numeric Rating Scale (NRS), adverse effects and compliance were measured. All measurements in the chest application group (group A=100) and knee application group (group B=100) were compared. Results: NRS was similar in rest between the groups treated with BTDP, but at two days and three days afternoon, five, six, and seven days postoperatively in group B, the NRS was significantly lower than that of group A. The adverse effects of the central nervous system and gastrointestinal system after applying BTDP were significantly lower in group B than in group A. No significant differences in adverse effects of the cardiovascular system and skin were observed between the two groups. Regarding the maintenance of BTDP, group B was significantly higher than group A. Conclusion: The direct application of BTDP after TKA to painful knee joints showed excellent results in early postoperative pain control and can be a useful method for increasing patient compliance by reducing the frequency of adverse effects.

A novel excisional wound pain model for evaluation of analgesics in rats

  • Parra, Sergio;Thanawala, Vaidehi J.;Rege, Ajay;Giles, Heather
    • The Korean Journal of Pain
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    • v.34 no.2
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    • pp.165-175
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    • 2021
  • Background: Management of pain from open wounds is a growing unmet healthcare need. However, the models available to study pain from wounds or to develop analgesics for the patients suffering from them have primarily relied on incisional models. Here, we present the first characterized and validated model of open wound pain. Methods: Unilateral full-skin excisional punch biopsy wounds on rat hind paws were evaluated for evoked pain using withdrawal responses to mechanical and thermal stimulation, and spontaneous pain was measured using hind paw weight distribution and guarding behavior. Evaluations were done before wounding (baseline) and 2-96 hours post-wounding. The model was validated by testing the effects of buprenorphine and carprofen. Results: Pain responses to all tests increased within 2 hours post-wounding and were sustained for at least 4 days. Buprenorphine caused a reversal of all four pain responses at 1 and 4 hours post-treatment compared to 0.9% saline (P < 0.001). Carprofen decreased the pain response to thermal stimulation at 1 (P ≤ 0.049) and 4 hours (P < 0.011) post-treatment compared to 0.9% saline, but not to mechanical stimulation. Conclusions: This is the first well-characterized and validated model of pain from open wounds and will allow study of the pathophysiology of pain in open wounds and the development of wound-specific analgesics.

Molecular Modeling Study on Morphine Derivatives Using Density Functional Methods and Molecular Descriptors (범밀도 함수법과 Molecular Descriptor를 이용한 모르핀 유도체에 대한 분자 모델링 연구)

  • Cotua, Jose;Cotes, Sandra;Castro, Pedro;Castro, Fernando;Mora, Liadys
    • Journal of the Korean Chemical Society
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    • v.54 no.4
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    • pp.363-373
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    • 2010
  • Computational studies were carried out on the opiates morphine, heroin, codeine, pentazocine, and buprenorphine, under the density functional theory. The geometric parameters of the pharmacophore and substituents were evaluated at the B3LYP/6-31+G(d) level of theory. The electronic structure calculations were performed using the same hybrid functional at the B3LYP/6-311++G (d,p) level of theory. The atomic charges were obtained by Mulliken population analysis. Given the reported biological activity, calculated partition coefficients, and electronic and geometric analysis, pentazocine and buprenorphine were chosen as models for proposed analogues. These analogues were then studied and compared with the model molecules. The study reveals that the geometry and electronic structure of the pharmacophore remains consistent in the presence of different substituents. Because the proposed analogues preserve the studied properties of the model molecules, it is likely that these analogues display biological activity.

Prevention, diagnosis, and treatment of opioid use disorder under the supervision of opioid stewardship programs: it's time to act now

  • Kim, Eun-Ji;Hwang, Eun-Jung;Yoo, Yeong-Min;Kim, Kyung-Hoon
    • The Korean Journal of Pain
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    • v.35 no.4
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    • pp.361-382
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    • 2022
  • The third opium war may have already started, not only due to illicit opioid trafficking from the Golden Crescent and Golden Triangle on the international front but also through indiscriminate opioid prescription and opioid diversion at home. Opioid use disorder (OUD), among unintentional injuries, has become one of the top 4 causes of death in the United States (U.S.). An OUD is defined as a problematic pattern of opioid use resulting in clinically significant impairment or distress, consisting of 2 or more of 11 problems within 1 year, as described by the Diagnostic and Statistical Manual for Mental Disorders, Fifth Edition. Observation of aberrant behaviors of OUD is also helpful for overworked clinicians. For the prevention of OUD, the Opioid Risk Tool and the Current Opioid Misuse Measure are appropriate screening tests before and during opioid administration, respectively. Treatment of OUD consists of 3 opioid-based U.S. Food and Drug Administration-approved medications, including methadone, buprenorphine, and naltrexone, and non-opioid-based symptomatic medications for reducing opioid withdrawal syndromes, such as α2 agonists, β-blockers, antidiarrheals, antiemetics, non-steroidal anti-inflammatory drugs, and benzodiazepines. There are at least 6 recommendable guidelines and essential terms related to OUD. Opioid stewardship programs are now critical to promoting appropriate use of opioid medications, improving patient outcomes, and reducing misuse of opioids, influenced by the successful implementation of antimicrobial stewardship programs. Despite the lack of previous motivation, now is the critical time for trying to reduce the risk of OUD.

Efficacy of medications in adult patients with trigeminal neuralgia compared to placebo intervention: a systematic review with meta-analyses

  • Peterson-Houle, Georgia M.;AbdelFattah, Magda R.;Padilla, Mariela;Enciso, Reyes
    • Journal of Dental Anesthesia and Pain Medicine
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    • v.21 no.5
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    • pp.379-396
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    • 2021
  • Background: Trigeminal neuralgia (TN) is characterized by brief, unilateral, sharp, stabbing, and shooting pain of the fifth cranial nerve. The objective of this systematic review with meta-analysis was to determine the effect of medications compared to placebo in adult patients with TN. Methods: Review authors identified randomized placebo-controlled trials (RCTs) from PubMed, Web of Science, Cochrane, and EMBASE up to February 2021. We assessed the inclusion and exclusion criteria as well as the risk of bias of the studies based on the Cochrane Handbook. A total of 324 unduplicated references were scanned independently and reduced to eight relevant RCTs, with 89 patients included. Medications investigated included oral carbamazepine, subcutaneous sumatriptan, lidocaine (intranasal, 8% spray on the oral mucosa or intravenous), buprenorphine (ganglionic local opioid analgesia), and oral Nav1.7, a selective sodium channel blocker. Results: Meta-analyses showed that overall patients receiving lidocaine reported a significantly lower post-treatment intensity of pain -3.8 points on a 0-10 scale (95% Cl = -4.653 to -2.873; P < 0.001). Patients who received lidocaine were 8.62 times more likely to have pain improvement than patients on placebo (P < 0.001). In one RCT, patients receiving oral carbamazepine showed a significant improvement in pain intensity of -32% compared to the placebo (P < 0.001). In one trial, patients receiving 3 mg subcutaneous sumatriptan had a significantly lower intensity of pain on average -6.1 points on a scale of 0-10 compared to placebo (P < 0.001) and a significant improvement in pain intensity of -75% compared to the improvement in the placebo group (P < 0.001). Patients who received subcutaneous sumatriptan were 10 times more likely to have pain improvement than those who received placebo (P = 0.001) in one study. Due to the unclear/high risk of bias and small sample size, the quality of the evidence for lidocaine in the treatment of TN was low. Conclusion: Further studies are needed for carbamazepine, sumatriptan, buprenorphine, and oral Nav1.7 sodium channel blockers, as only one study reported outcomes.

Comparison of Quality of Pain Using Patient-Controlled Analgesia (PCA) after Total Abdominal Hysterectomy (TAH) (전자궁적출술후 통증자가조절장치 사용에 따른 통증점수 비교)

  • Lee, Jung-Koo;Park, Seok;Chung, Jung-Kil
    • The Korean Journal of Pain
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    • v.11 no.2
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    • pp.253-257
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    • 1998
  • Background: The purpose of this study was to examine the extent and evaluation of pain after total abdominal hysterectomy (TAH) and to establish correlation between three types of pain; pain at rest, pain with movement and pain with coughing (maximum pain). Methods: The present study compared quality of pain during pain management in 48 patients undergoing TAH. Patients received i.v. meperidine as loading dose in the recovery room and PCA with nalbuphine 90 mg, ketorolac 180 mg, buprenorphine 0.9 mg, droperidol 5 mg, plasma solution A 28 ml for 3 days. The PCA device used was the Baxter infusor$^{(R)}$ (PCA module PC-19-55, 0.5 ml/hr basal rate, 15 minute lockout interval). Patients were then interviewed on Operative Day (OPD), Postoperative Day 1, 2, and 3 (POD 1, 2 and 3) to assess their pain on a visual analogue scale (VAS) of 0 (none) to 10 (worst imaginable). Results: The mean pain score at rest was 2.0 on OPD and decreased to 0.7 on POD 3. The mean pain score with movement was 3.2 on OPD and decreased to 1.6 on POD 3. The mean pain score with coughing was 4.2 on OPD and decreased to 2.2 on POD 3. Conclusions: Patients' experience of three types of postoperative pain emphasizes the need for more effective pain management.

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Auricular acupuncture for sleep quality in participants with mental and behavioral disorders due to prior multiple drug use: a retrospective consecutive case series

  • Yuri Gimelfarb;Eran Goldstien
    • Journal of Yeungnam Medical Science
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    • v.40 no.1
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    • pp.78-85
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    • 2023
  • Background: Poor sleep quality is associated with psychoactive substance abuse/addiction/withdrawal. Auricular acupuncture (AA) is a nonpharmacological method used for the treatment of sleep disturbances. This study aimed to examine the quality of sleep before and after AA in participants with mental and behavioral disorders due to prior multiple drug use in the therapeutic community. Methods: This was a consecutive case series of 27 participants (25 male [92.6%]). The median age was 35.0 years (interquartile range [IQR], 29.0-37.2 years), methadone/buprenorphine were not used, and the participants were treated with AA (median number of treatments, 15.0 [IQR, 12.0-18.0]) during a median period of 51.0 days (IQR, 49.0-51.0 days) according to the National Acupuncture Detoxification Association (NADA)-Acudetox protocol. Sleep quality was determined using the Pittsburgh Sleep Quality Index (PSQI), a self-rated questionnaire that assesses sleep quality and disturbances over a 1-month interval. Results: The global PSQI score dropped (indicating better sleep quality) by a median of 3.0 points (IQR, 0.0-8.0 points) after treatment. In the multivariate logistic regression analysis, with an increase in global PSQI score during AA by 1 point, there was a 0.73-fold reduction in the risk of poor sleep quality post-AA (adjusted odds ratio, 0.73; 95% confidence interval, 0.52-1.01; p<0.055; Nagelkerke's R2 =0.66). Conclusion: The results revealed a positive effect of AA (by the NADA-Acudetox protocol) on sleep quality (as measured by PSQI) among participants in a treatment center with mental and behavioral disorders due to multiple drug use.