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Pharmacology & Therapeutics 1981
Review
Topics: Analgesics; Analgesics, Opioid; Animals; Anti-Inflammatory Agents, Non-Steroidal; Drug Interactions; Humans
PubMed: 6116240
DOI: 10.1016/0163-7258(81)90099-1 -
Phytomedicine : International Journal... Feb 2023Oxidative stress is an inevitable process that occurs during life activities, and it can participate in the development of inflammation. Although great progress has been... (Review)
Review
BACKGROUND
Oxidative stress is an inevitable process that occurs during life activities, and it can participate in the development of inflammation. Although great progress has been made according to research examining analgesic drugs and therapies, there remains a need to develop new analgesic drugs to fill certain gaps in both the experimental and clinical space.
PURPOSE
This review reports the research and preclinical progress of this class of analgesics by summarizing known nuclear factor E-2-related factor-2 (Nrf2) pathway-modulating substances.
STUDY DESIGN
We searched and reported experiments that intervene in the Nrf2 pathway and its various upstream and downstream molecules for analgesic therapy.
METHODS
The medical literature database (PubMed) was searched for experimental studies examining the reduction of pain in animals through the Nrf2 pathway, the research methods were analyzed, and the pathways were classified and reported according to the pathway of these experimental interventions.
RESULTS
Humans have identified a variety of substances that can fight pain by regulating the expression of Nrf2 and its upstream and downstream pathways.
CONCLUSION
The Nrf2 pathway exerts anti-inflammatory activity by regulating oxidative stress, thereby playing a role in the fight against pain.
Topics: Animals; Humans; NF-E2-Related Factor 2; Analgesics; Oxidative Stress; Inflammation; Pain
PubMed: 36603339
DOI: 10.1016/j.phymed.2022.154598 -
Current Drug Delivery 2017Analgesics are the drugs which bring insensibility to pain without loosing consciousness. Treatment strategy is generally based on the type of pain. Most of the... (Review)
Review
BACKGROUND
Analgesics are the drugs which bring insensibility to pain without loosing consciousness. Treatment strategy is generally based on the type of pain. Most of the analgesics are associated with serious side effects, such as NSAIDS can cause severe GI disturbance and opioids can cause addiction. There are various ways to reduce their side effects The analgesic prodrug approach is one of the several strategies used to attain the required pharmacological response with a considerable decrease in side effects. The aim of this paper is to introduce in depth the rational behind the use of the analgesic prodrug approach from past to present.
METHODS
Data is collected from online as well as from extensive literature survey which have appeared on this subject during the last decades. This review will map the origins and development of the most important of the analgesic prodrugs to date.
RESULTS
This review indicates that, designing analgesic prodrugs represent successful strategy to gain the required pharmacological activity with a considerable decrease in side effects. However thorough knowledge of diverse biological phenomena is needed which enables scientists to invent and design superior, nontoxic and better-targeted prodrugs.
CONCLUSION
The newly synthesized chemical entity or prodrugs may or may not have intrinsic pharmacological activity and also synthesizing novel molecules consume a lot of time and money than developing prodrugs of existing clinically used analgesic drugs which is surely an attractive and promising area of research now a days.
Topics: Analgesics; Humans; Prodrugs
PubMed: 27142107
DOI: 10.2174/1567201813666160504100705 -
The Veterinary Clinics of North... Jul 2000Adjuvant analgesics are drugs that have weak or nonexistent analgesic action when administered alone but can enhance analgesic actions when coadministered with known... (Review)
Review
Adjuvant analgesics are drugs that have weak or nonexistent analgesic action when administered alone but can enhance analgesic actions when coadministered with known analgesic agents. Such agents are often administered in cases of refractory pain. For some chronic pain syndromes, however, they may constitute a first-line approach. Because pain is such an individual experience, analgesic regimens may require several drugs at varying dosages to confer a comfortable state. Adjunctive therapies such as the tricyclic antidepressants, anticonvulsants, N-methyl-D-aspartic acid receptor antagonists and low-dose intravenous local anesthetics, to name a few, have proved to be efficacious in relieving certain types of pain, especially neuropathic and cancer pain. Their use in animals is increasing, with anecdotal reports of some success.
Topics: Analgesics; Animals; Chemotherapy, Adjuvant; Pain
PubMed: 10932826
DOI: 10.1016/s0195-5616(08)70008-1 -
Acta Pharmacologica Sinica Jul 2022Dezocine, a synthetic opioid, introduced in 1970s as an analgesic, was redeveloped for relieving moderate to severe pain by Yangtze River Pharmaceutical Group in China... (Review)
Review
Dezocine, a synthetic opioid, introduced in 1970s as an analgesic, was redeveloped for relieving moderate to severe pain by Yangtze River Pharmaceutical Group in China in 2009. To date, dezocine occupies 45% of China's opioid analgesic market. Along with dezocine being a dominated painkiller, a certain amount of research was conducted to elucidate dezocine's action. In this review we summarize the current knowledge on the receptor, preclinical and clinical pharmacology of dezocine. Briefly, preclinical data show that dezocine is effective under varying pain conditions, particularly chronic neuropathic pain and cancer pain, through activation of opioid receptors, and inhibition of norepinephrine reuptake. Clinical data establish the effectiveness of dezocine either as a primary analgesic for postoperative pain management or a supplement for balanced analgesia. The receptor profile of dezocine is different from known pure μ agonists, and allows it to be used in combination with other opioids for additivity in efficacy or lower incidence of adverse effects.
Topics: Analgesics; Analgesics, Opioid; Bridged Bicyclo Compounds, Heterocyclic; Humans; Pain; Tetrahydronaphthalenes
PubMed: 34737418
DOI: 10.1038/s41401-021-00790-6 -
Drugs Jul 2017Transdermal administration of analgesic medications offers several benefits over alternative routes of administration, including a decreased systemic drug load with... (Review)
Review
Transdermal administration of analgesic medications offers several benefits over alternative routes of administration, including a decreased systemic drug load with fewer side effects, and avoidance of drug degradation by the gastrointestinal tract. Transdermal administration also offers a convenient mode of drug administration over an extended period of time, particularly desirable in pain medicine. A transdermal administration route may also offer increased safety for drugs with a narrow therapeutic window. The primary barrier to transdermal drug absorption is the skin itself. Transdermal nanotechnology offers a novel method of achieving enhanced dermal penetration with an extended delivery profile for analgesic drugs, due to their small size and relatively large surface area. Several materials have been used to enhance drug duration and transdermal penetration. The application of nanotechnology in transdermal delivery of analgesics has raised new questions regarding safety and ethical issues. The small molecular size of nanoparticles enables drug delivery to previously inaccessible body sites. To ensure safety, the interaction of nanoparticles with the human body requires further investigation on an individual drug basis, since different formulations have unique properties and side effects.
Topics: Administration, Cutaneous; Analgesics; Animals; Drug Delivery Systems; Drug Liberation; Humans; Nanoparticles; Nanotechnology; Skin Absorption
PubMed: 28470586
DOI: 10.1007/s40265-017-0744-y -
Molecules (Basel, Switzerland) Dec 2015Pain is an unpleasant sensation associated with a wide range of injuries and diseases, and affects approximately 20% of adults in the world. The discovery of new and... (Review)
Review
Pain is an unpleasant sensation associated with a wide range of injuries and diseases, and affects approximately 20% of adults in the world. The discovery of new and more effective drugs that can relieve pain is an important research goal in both the pharmaceutical industry and academia. This review describes studies involving antinociceptive activity of essential oils from 31 plant species. Botanical aspects of aromatic plants, mechanisms of action in pain models and chemical composition profiles of the essential oils are discussed. The data obtained in these studies demonstrate the analgesic potential of this group of natural products for therapeutic purposes.
Topics: Analgesics; Animals; Biological Products; Disease Models, Animal; Mice; Oils, Volatile; Pain; Rats
PubMed: 26703556
DOI: 10.3390/molecules21010020 -
Fundamental & Clinical Pharmacology Feb 2024Cannabis, more commonly known as marijuana or hemp, has been used for centuries to treat various conditions. Cannabis contains two main components cannabidiol (CBD) and... (Review)
Review
BACKGROUND
Cannabis, more commonly known as marijuana or hemp, has been used for centuries to treat various conditions. Cannabis contains two main components cannabidiol (CBD) and tetrahydrocannabinol (THC). CBD, unlike THC, is devoid of psychoactive effects and is well tolerated by the human body but has no direct effect on the receptors of the endocannabid system, despite the lack of action on the receptors of the endocannabid system.
OBJECTIVES AND METHODS
We have prepared a literature review based on the latest available literature regarding the analgesic effects of CBD. CBD has a wide range of effects on the human body. In this study, we will present the potential mechanisms responsible for the analgesic effect of CBD. To the best of our knowledge, this is the first review to explore the analgesic mechanisms of CBD.
RESULTS AND CONCLUSION
The analgesic effect of CBD is complex and still being researched. CBD models the perception of pain by acting on G protein-coupled receptors. Another group of receptors that CBD acts on are serotonergic receptors. The effect of CBD on an enzyme of potential importance in the production of inflammatory factors such as cyclooxygenases and lipoxygenases has also been confirmed. The presented potential mechanisms of CBD's analgesic effect are currently being extensively studied.
Topics: Humans; Cannabidiol; Cannabis; Analgesics; Pain
PubMed: 37584368
DOI: 10.1111/fcp.12947 -
Molecules (Basel, Switzerland) Mar 2024Pain affects one-third of the global population and is a significant public health issue. The use of opioid drugs, which are the strongest painkillers, is associated... (Review)
Review
Pain affects one-third of the global population and is a significant public health issue. The use of opioid drugs, which are the strongest painkillers, is associated with several side effects, such as tolerance, addiction, overdose, and even death. An increasing demand for novel, safer analgesic agents is a driving force for exploring natural sources of bioactive peptides with antinociceptive activity. Since the G protein-coupled receptors (GPCRs) play a crucial role in pain modulation, the discovery of new peptide ligands for GPCRs is a significant challenge for novel drug development. The aim of this review is to present peptides of human and animal origin with antinociceptive potential and to show the possibilities of their modification, as well as the design of novel structures. The study presents the current knowledge on structure-activity relationship in the design of peptide-based biomimetic compounds, the modification strategies directed at increasing the antinociceptive activity, and improvement of metabolic stability and pharmacodynamic profile. The procedures employed in prolonged drug delivery of emerging compounds are also discussed. The work summarizes the conditions leading to the development of potential morphine replacements.
Topics: Animals; Humans; Analgesics; Peptides; Morphine; Pain; Analgesics, Opioid
PubMed: 38611824
DOI: 10.3390/molecules29071544 -
Drug Research Feb 2021Piperazine, a nitrogen-containing heterocyclic has acquired an inimitable position in medicinal chemistry because of its versatile structure, which has fascinated... (Review)
Review
Piperazine, a nitrogen-containing heterocyclic has acquired an inimitable position in medicinal chemistry because of its versatile structure, which has fascinated researchers to design novel piperazine based molecules having various biological actions. The subsistence of various compounds possessing diverse pharmacological activities in the literature further confirms this fact. Currently available analgesics and anti-inflammatory drugs are associated with side effects that limit their use. Moreover, the literature reveals the incredible anti-inflammatory and analgesic potential of piperazine derivatives along with their method of synthesis, therefore; the present review has been designed to collate the development made in this area that will surely be advantageous in designing novel piperazine based candidates with enhanced efficacy and less toxicity. An extensive literature survey was carried by scrutinizing peer reviewed articles from worldwide scientific databases available on GOOGLE, SCOPUS, PUBMED, and only relevant studies published in English were considered.
Topics: Analgesics; Animals; Anti-Inflammatory Agents; Humans; Piperazine
PubMed: 33336346
DOI: 10.1055/a-1323-2813