吗啡:胺混合物在老鼠中的抗感和不良影响
Conor D Strumberger1, Evangeline J D'Epagnier, Kevin H Nguyen
1Department of Psychological Science, Creighton University, Omaha, Nebraska, USA.
Behavioural pharmacology
|March 7, 2024
概括
结合吗啡和胺来缓解疼痛,在较低剂量下显示出协同效应. 这种组合可能会降低阿片类药物的剂量,但需要进一步的研究来了解依赖和呼吸系统抑郁等风险.
科学领域:
- 药理学 药理学 是一个学科.
- 疼痛管理 疼痛管理
- 神经科学是一个神经科学.
背景情况:
- 阿片类药物对中度至严重的疼痛是有效的,但存在滥用和致命过量服用的风险.
- 将阿片类药物与非阿片类止痛药结合使用可能会减少所需的阿片类药物剂量并减轻副作用.
- 胺,一种N-甲基-D-酸盐受体对手,具有镇痛特性,但临床使用有限.
研究的目的:
- 描述单独或混合的吗啡和胺的抗受体,行为抑制剂和胃肠道作用.
- 在临床前模型中确定吗啡和胺之间的相互作用.
主要方法:
- 成年雄性斯普拉格-道利大鼠被用来评估吗啡和胺的作用.
- 药物单独和在各种吗啡:胺混合物中被使用.
- 测量了抗受体,寻找食物的行为,以及胃肠道过渡.
主要成果:
- 无论是吗啡还是胺,都会产生抗,减少寻找食物,单独服用时会引起便秘.
- 吗啡:胺混合物通常显示添加效应.
- 在较低剂量的1:1混合物中观察到协同作用的抗受体作用,在较高剂量的混合物中观察到附加性.
- 吗啡的便秘效应并没有被胺增强.
结论:
- 吗啡和胺呈现复杂的相互作用,在特定的比率下具有协同作用的疼痛缓解的潜力.
- 进一步的研究至关重要,以了解完整的治疗窗口和组合使用的潜在不良影响.
- 确定最佳比率可以提高阿片类药物在疼痛管理中的安全性.
相关概念视频
Opioid Analgesics: Synthetic and Semisynthetic Opioids
295
Synthetic and semisynthetic opioids are pivotal in pain management and tackling opioid addiction. Semisynthetic opioids, including morphinans (morphine derivatives), oxycodone, oxymorphone, hydrocodone, and hydromorphone, have improved pharmacokinetic profiles compared to morphine. Additionally, heroin and 6-MAM (6-Monoacetylmorphine) show better CNS penetration than morphine due to heightened lipid solubility. Hydromorphone, a potent opioid, undergoes hepatic metabolism to form the active...
295
Parenteral Anesthetics: Overview
122
Intravenous anesthetics are drugs administered parenterally to induce anesthesia or sedation. Propofol is a widely used agent formulated as a 1% emulsion in soybean oil, glycerol, and egg phosphatide. It induces rapid anesthesia primarily due to its rapid distribution from the bloodstream to target tissues and is metabolized in the liver. However, it can cause significant pain on injection and hypertriglyceridemia. Fospropofol, a water-based prodrug of propofol, lacks these adverse effects.
122
Analgesia and Pain Management
618
Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
618
Opioid Analgesics: Morphine and Other Natural Cogeners
249
Opioids are a class of drugs that mimic endogenous opioid peptides and act on opioid receptors, and help in pain relief. These compounds are classified as natural, synthetic, or semi-synthetic. Natural opioids, like morphine, codeine, and thebaine, are derived from the opium poppy plant (Papaver somniferum or Papaver album) and are termed opiates. Synthetic opioids are artificial, while semi-synthetic opioids combine natural and synthetic compounds. Morphine, a prototypical opioid, possesses a...
249
Local Anesthetics: Adverse Effects
414
While local anesthetics are generally safe and well-tolerated, they can occasionally cause adverse effects that vary in severity. Local anesthetics can induce toxicity at two distinct levels. They can either produce local effects through direct contact with the neural elements or be absorbed into the bloodstream from the injection site, leading to systemic effects.
Once absorbed into the systemic circulation, local anesthetics can affect the organs that depend on the functioning of sodium...
Once absorbed into the systemic circulation, local anesthetics can affect the organs that depend on the functioning of sodium...
414
Sedatives and Hypnotics Drugs: Miscellaneous Agents
172
Sedatives and hypnotics encompass a wide range of substances, each with its unique mechanism of action, uses, and potential adverse effects.
Melatonin congeners like ramelteon (Rozerem) and tasimelteon (Hetlioz) selectively bind to melatonin receptors (MT1 and MT2) and thus mimic the actions of melatonin, a hormone that regulates sleep-wake cycles. Tasimelteon is primarily used for non-24-hour sleep-wake disorder, common in blind patients. They are also used to treat conditions like insomnia...
Melatonin congeners like ramelteon (Rozerem) and tasimelteon (Hetlioz) selectively bind to melatonin receptors (MT1 and MT2) and thus mimic the actions of melatonin, a hormone that regulates sleep-wake cycles. Tasimelteon is primarily used for non-24-hour sleep-wake disorder, common in blind patients. They are also used to treat conditions like insomnia...
172


