Roche · OPRK1 · 小分子
buprenorphine 是一种小分子，由Roche研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)、Sublingual (SL)/Oral Transmucosal。
| 公司 | Roche |
| 药物类别 | 小分子 |
| 分子靶点 | OPRK1, OPRM1 |
| 给药途径 | Oral (PO), Sublingual (SL)/Oral Transmucosal |
| 状态 | Approved |
buprenorphine 作用于 2 个分子靶点：
| OPRK1 | opioid receptor kappa 1 (KOR1, OPRK) |
| OPRM1 | opioid receptor mu 1 (MOR1, LMOR) |
buprenorphine 针对 1 个适应症，涉及 1 个治疗领域。
| 治疗领域 | 疾病/病症 | 分期 |
|---|---|---|
| Gastrointestinal disorders | Abdominal pain | ✓ Approved |
Chukwudi Kelechi Nnaemeka KN, Adediji Godwin G, Lynch Meghan M, Scully Michael M et al.
Zhai Yuxiang Y, Huang Jiale J, Chen Renji R, Song Qinggao Q
Dermoid cysts are benign developmental lesions arising from ectodermal remnants formed during embryogenesis, predominantly observed in children and young adults. These cysts most frequently occur in the floor of the mouth and submental region, typically located deep within the mucosa or subcutaneous tissue, or between the muscles of the floor of the mouth. Herein, we present a case of a 39-year-old male with a 30-year history of bilateral submandibular masses. Magnetic resonance imaging revealed a sublingual cystic lesion extending into the bilateral submandibular spaces, with well-demarcated borders. After exclusion of contraindications for general anesthesia, complete resection of the lesion was performed. Postoperative histopathologic examination confirmed an epidermoid cyst. The patient achieved a favorable postoperative outcome without signs of recurrence.
Maguire Lindsay A LA, Jha Manish K MK, Murphy Nicholas N, Thomas Ynhi T YT
Oka Tatsuya T, Kobayashi Hiroyuki H
Sublingual immunotherapy (SLIT) is a safe and convenient treatment for allergic diseases, but it usually requires several years to achieve sufficient clinical benefit. Therefore, effective adjuvants are needed to enhance its efficacy and shorten the time required to achieve a therapeutic response. In this review, we summarize the rationale for using Toll-like receptor 4 (TLR4) agonists as adjuvants for SLIT and describe our recent preclinical findings with synthetic TLR4 agonist derivatives. We established a mouse model of sublingual administration using a small administration volume and a defined retention period after administration. Several TLR4 agonist derivatives enhanced allergen-specific serum IgG responses when administered with allergen. The adjuvant activity of one derivative was abolished in TLR4-knockout mice, indicating that its activity was dependent on TLR4 signaling. A selected derivative was further evaluated in combination with Japanese cedar pollen (JCP) extract. Co-administration of the derivative with JCP extract increased Cry j 1-specific IgG and IgA levels in serum and IgA levels in nasal lavage fluid. It also enhanced allergen-induced IL-10 production without substantially increasing IFN-γ or IL-4 production. Moreover, IgG from mice treated with the derivative and JCP extract more effectively inhibited allergen-induced mast cell degranulation than IgG from mice treated with JCP extract alone. These findings suggest that synthetic TLR4 agonists may enhance SLIT by promoting functional allergen-specific antibody responses. Further studies are needed to confirm their safety and clinical efficacy in humans.
Ramnarine Rishi R, McDonnell Fiona F, Korsen Jennifer J
A 31-year-old woman was referred to the Oral and Maxillofacial Surgery department with a hard swelling in the right floor of the mouth which had the clinical appearance of a salivary calculus. Plain radiography did not demonstrate a radiopacity; however, subsequent ultrasound examination supported this finding. Three months after the initial consultation, while waiting for removal of the calculus, the patient re-presented with mobility of the lower anterior teeth and progressive swelling, prompting repeat orthopantomography and an urgent computed tomography scan of the mandible. These revealed a 27 mm defect within the anterior mandible. Following extensive histopathological examination together with staging investigations and molecular analysis, a diagnosis of T4a, N1, M1 poorly differentiated salivary carcinoma NOS (not otherwise specified) of the sublingual gland was established. Metastatic disease was identified in the lungs, brain and spine, with death occurring ten months after diagnosis. This case highlights the need for careful assessment and heightened awareness of rare salivary gland pathologies particularly when symptoms progress despite initially unremarkable investigations.
Wong Aaron K AK, McManus Helen H, Vogrin Sara S, Dib Youseph Y et al.
Ongoing disruptions to opioid supply in Australia have raised ongoing concerns about their impact on cancer pain management. The withdrawal of hydromorphone slow-release (SR) tablets from the Australian market has presented challenges to advanced cancer pain management. This study aimed to determine how this affected the utilisation of alternative slow-release opioids in patients with advanced cancer. A retrospective cohort study was conducted at a quaternary cancer centre, comparing opioid prescribing patterns across two 12-month periods: before hydromorphone SR tablet discontinuation was announced and after its discontinuation. Inpatient and outpatient prescribing data were analysed for adult patients with incurable advanced or metastatic cancer who first presented to the centre during each study period. A total of 2856 patients were included (n = 1475 pre and n = 1381 post hydromorphone SR discontinuation). Following hydromorphone SR withdrawal, opioid prescribing patterns shifted. Methadone use rose modestly (adjusted odds ratio [aOR] 1.42, p = 0.07), accompanied by a doubling of median dose (45 mg vs. 22.5 mg; p = 0.005). Morphine use declined (aOR 0.69, p < 0.001), yet daily OMEDD increased by ∼20% (95% confidence interval 1.01-1.37). Tapentadol (aOR 1.40, p = 0.01) and buprenorphine (aOR 1.37, p < 0.001) were prescribed more frequently, without corresponding dose escalation. Following hydromorphone SR withdrawal, the frequency of methadone use increased and median doses doubled. Research incorporating national datasets is needed to clarify the broader impact of opioid supply interruptions. These findings indicate a potential need to reframe the place of methadone in practice, and potentially upscale the focus of clinician training on its safe and effective use.
注册免费账户还可查看另外 9996 篇文献
免费注册查看全部文献 →