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BMC Complementary Medicine and Therapies Feb 2022Pain and inflammation are associatory events in cancer, diabetes, cardiovascular diseases, arthritis and other chronic diseases. Corticosteroids, non-steroidal...
BACKGROUND
Pain and inflammation are associatory events in cancer, diabetes, cardiovascular diseases, arthritis and other chronic diseases. Corticosteroids, non-steroidal anti-inflammatory drugs exert potential side effects on long term use. This study was aimed to investigate the acute oral toxicity, anti-inflammatory and analgesic activities of leaf and bark extracts of Albizia procera in experimental animal models.
METHODS
Ethyl acetate, ethanol, and hydroalcoholic extracts of Albizia procera (leaf and bark) were subjected for acute oral toxicity, anti-inflammatory and analgesic screening. Carrageenan and cotton pellet granuloma models were used to assess acute and chronic anti-inflammatory effects, respectively. Intraplanar formalin test was used to assess the analgesic activity.
RESULTS
All the extracts of Albizia procera were found to be well-tolerated up to 2000 mg/kg in female rats. Ethanolic leaf (ETLE) and bark (ETBE) of Albizia procera showed anti-inflammatory actions. But, only ETBE produced significant protection in chronic inflammation and analgesic activity.
CONCLUSION
In summary, Albizia procera possess significant anti-inflammatory and analgesic properties. This study adds evidence on the traditional use of Albizia procera plant for treating painful inflammatory disorders.
Topics: Albizzia; Analgesics; Animals; Anti-Inflammatory Agents; Dental Porcelain; Metal Ceramic Alloys; Plant Bark; Plant Extracts; Plant Leaves; Rats; Titanium
PubMed: 35216561
DOI: 10.1186/s12906-021-03497-7 -
Drugs Sep 2018Pain is one of the most common symptoms among patients with end-stage renal disease (ESRD), and is often under recognized and not adequately managed in hemodialysis (HD)... (Review)
Review
Pain is one of the most common symptoms among patients with end-stage renal disease (ESRD), and is often under recognized and not adequately managed in hemodialysis (HD) patients. Barriers to adequate pain management include poor awareness of the problem, insufficient medical education, fears of possible drug-related side effects, and common misconceptions about the inevitability of pain in elderly and HD patients. Caregivers working in HD should be aware of the possible consequences of inadequate pain assessment and management. Common pain syndromes in HD patients include musculoskeletal diseases and metabolic neuropathies, associated with typical intradialytic pain. Evaluating the etiology, nature, and intensity of pain is crucial for choosing the correct analgesic. A mechanism-based approach to pain management may result in a better outcome. Pharmacokinetic considerations on clearance alterations and possible toxicity in patients with ESRD should drive the right analgesic prescription. Comorbidities and polymedications may increase the risk of drug-drug interactions, therefore drug metabolism should be taken into account when selecting analgesic drugs. Automedication is common among HD patients but should be avoided to reduce the risk of hazardous drug administration. Further research is warranted to define the efficacy and safety of analgesic drugs and techniques in the context of patients with ESRD as generalizing information from studies conducted in the general population could be inappropriate and potentially dangerous. A multidisciplinary approach is recommended for the management of complex pain syndromes in frail patients, such as those suffering from ESRD.
Topics: Analgesics; Chronic Pain; Dose-Response Relationship, Drug; Drug Interactions; Humans; Kidney Failure, Chronic; Pain Management; Pain Measurement; Renal Dialysis; Treatment Outcome
PubMed: 30206801
DOI: 10.1007/s40265-018-0980-9 -
Journal of Ethnopharmacology Mar 2022"Ya gai", an important part of Dai medical theory, is traditionally recognized as an antidote. Kopsia officinalis Tsiang et P. T. Li is a "Ya gai" related medicine and...
ETHNOPHARMACOLOGICAL RELEVANCE
"Ya gai", an important part of Dai medical theory, is traditionally recognized as an antidote. Kopsia officinalis Tsiang et P. T. Li is a "Ya gai" related medicine and has been widely used by Dai people for the treatment of pain and inflammation. Previous literature on title species suggested that monoterpenoid indole alkaloids (MIAs) could be its main bioactive components. However, the specific bioactive ingredients for inflammation-related treatment are still unrevealed, which inspired us to conduct a phytochemical and pharmacological investigation related to its traditional use.
AIM OF THE STUDY
To support the traditional use of K. officinalis by assessing the anti-inflammatory and analgesic effects of its purified MIAs.
MATERIAL AND METHODS
Compounds were isolated and purified from the barks and leaves of K. officinalis using diverse chromatographic methods. The structures were established by means of extensive spectroscopic analyses and quantum computational technique. The anti-inflammatory activities of the purified MIAs were evaluated in vitro based on the suppression of lipopolysaccharide-activated inflammatory mediators (COX-2, IL-1β, and TNF-α) in RAW 264.7 macrophage cells. Anti-inflammatory and analgesic activities in vivo were assessed with carrageenan-induced paw edema and acetic acid-stimulated writhing in mice models.
RESULTS
23 MIAs including four new compounds were obtained and structurally established. Most of isolates showed significant anti-inflammatory effects in vitro by inhibiting inflammatory mediators (COX-2, IL-1β, and TNF-α). Further pharmacological evaluation in vivo revealed that 12-hydroxy-19(R)-hydroxy-ibophyllidine (1) and 11,12-methylenedioxykopsinaline N-oxide (5) remarkably decreased the number of writhing, while kopsinic acid (8), (-)-kopsinilam (12), and normavacurine-21-one (20) significantly relieved paw edema, respectively, even better than the positive control aspirin.
CONCLUSIONS
The in vitro and in vivo findings supported the traditional use of K. officinalis with respect to its anti-inflammatory and analgesic effect, as well as provided potent bioactive MIAs for further chemical modification and pharmacological investigation.
Topics: Analgesics; Animals; Anti-Inflammatory Agents; Apocynaceae; Male; Mice; Mice, Inbred ICR; Models, Molecular; Molecular Structure; Phytotherapy; Secologanin Tryptamine Alkaloids
PubMed: 34798159
DOI: 10.1016/j.jep.2021.114848 -
Journal of Clinical Pharmacy and... Aug 2018Current analgesic pharmacotherapy-opioids, non-steroidal anti-inflammatory drugs (NSAIDs), acetaminophen (paracetamol) and related drugs-is effective for acute pain, but... (Review)
Review
WHAT IS KNOWN AND OBJECTIVE
Current analgesic pharmacotherapy-opioids, non-steroidal anti-inflammatory drugs (NSAIDs), acetaminophen (paracetamol) and related drugs-is effective for acute pain, but their use is limited by adverse effects on the renal, hepatic, cardiovascular or gastrointestinal systems, or they have potential for abuse. Therefore, alternative options are desired. Compounds used in traditional medicine might offer such alternatives, but the evidence must be based on pharmacologic properties and on clinical trial data. This review summarizes the evidence for one of these: the analgesic properties of turmeric and other curcumins.
METHODS
The PubMed database and other sources were searched using keywords related to turmeric, curcumin, antinociception and analgesia. Primary sources and reviews of preclinical and clinical studies were identified, assessed and summarized. Bibliographies within these sources provided additional information.
RESULTS
Turmeric has consistently been demonstrated to produce analgesic and anti-inflammatory effects in animal models and in clinical trials, and appears to have less serious adverse effects than many current analgesics.
WHAT IS NEW AND CONCLUSIONS
Turmeric (curcumin) appears to be a possible candidate for consideration for use as a stand-alone analgesic, or in analgesic combinations as part of opioid-, NSAID- or paracetamol (acetaminophen)-sparing strategies.
Topics: Analgesia; Analgesics; Animals; Anti-Inflammatory Agents; Curcuma; Curcumin; Humans; Pain
PubMed: 29722036
DOI: 10.1111/jcpt.12703 -
Bioorganic Chemistry Dec 2023The opioids have been used for more than a thousand years and are not only the most widely prescribed drugs for moderate to severe pain and acute pain, but also the... (Review)
Review
The opioids have been used for more than a thousand years and are not only the most widely prescribed drugs for moderate to severe pain and acute pain, but also the preferred drugs. However, their non-analgesic effects, especially respiratory depression and potential addiction, are important factors that plague the safety of clinical use and are an urgent problem for pharmacological researchers to address. Current research on analgesic drugs has evolved into different directions: de-opioidization; application of pharmacogenomics to individualize the use of opioids; development of new opioids with less adverse effects. The development of new opioid drugs remains a hot research topic, and with the in-depth study of opioid receptors and intracellular signal transduction mechanisms, new research ideas have been provided for the development of new opioid analgesics with less side effects and stronger analgesic effects. The development of novel opioid drugs in turn includes selective opioid receptor ligands, biased opioid receptor ligands, and multi-target opioid receptor ligands and positive allosteric modulators (PAMs) or antagonists and the single compound as multi-targeted agnoists/antagonists for different receptors. PAMs strategies are also getting newer and are the current research hotspots, including the BMS series of compounds and others, which are extensive and beyond the scope of this review. This review mainly focuses on the selective/biased/multi-targeted MOR/DOR/KOR (mu opioid receptor/delta opioid receptor/kappa opioid receptor) small molecule ligands and involves some cryo-electron microscopy (cryoEM) and structure-based approaches as well as the single compound as multi-targeted agnoists/antagonists for different receptors from 2019 to 2022, including discovery history, activities in vitro and vivo, and clinical studies, in an attempt to provide ideas for the development of novel opioid analgesics with fewer side effects.
Topics: Analgesics, Opioid; Receptors, Opioid, kappa; Receptors, Opioid, mu; Cryoelectron Microscopy; Analgesics; Ligands
PubMed: 37797454
DOI: 10.1016/j.bioorg.2023.106869 -
Phytotherapy Research : PTR Nov 2023Pain can become a chronic and deliberating experience with a significant burden. In preclinical and clinical studies, Saffron (Crocus sativus L.) has shown analgesic... (Review)
Review
Pain can become a chronic and deliberating experience with a significant burden. In preclinical and clinical studies, Saffron (Crocus sativus L.) has shown analgesic activities. Considering the unsatisfactory results of current therapeutic management for chronic pain conditions, we aimed to review saffron's analgesic activity and underlying mechanisms. Saffron showed antinociceptive activities in formalin-, carrageenan-, and capsaicin-induced experimental pain models. Saffron analgesic activities affected several targets, including ion channels of nociceptors; the adrenergic system and central histaminic system; inhibition of inflammatory pathways, apoptotic pathways, and oxidative stress; regulation of NO pathway, and the endocannabinoid system. Clinical studies showed analgesia of Saffron in rheumatoid arthritis, after-pain following childbirth, dysmenorrhea, and fibromyalgia. Our literature review showed that saffron can be beneficial as an adjunct therapy to commonly used analgesics in practice, particularly in chronic pain conditions.
Topics: Crocus; Chronic Pain; Capsaicin; Arthritis, Rheumatoid; Biological Products; Analgesics; Plant Extracts
PubMed: 37528638
DOI: 10.1002/ptr.7968 -
European Journal of Pharmaceutical... Jan 2022The development of new COX-2 inhibitors with analgesic and anti-inflammatory efficacy as well as minimal gastrointestinal, renal and cardiovascular toxicity, is of vital...
The development of new COX-2 inhibitors with analgesic and anti-inflammatory efficacy as well as minimal gastrointestinal, renal and cardiovascular toxicity, is of vital importance to patients suffering from chronic course pain and inflammatory conditions. This study aims at evaluating the therapeutic activity and adverse drug reactions associated with the use of the newly synthesized pyrazole derivative, compound AD732, E-4-[3-(4-methylphenyl)-5-hydroxyliminomethyl-1H-pyrazol-1-yl]benzenesulfonamide, as compared to indomethacin and celecoxib as standard agents. Anti-inflammatory activity was assessed using carrageenan-induced rat paw edema and cotton pellet granuloma tests; formalin-induced hyperalgesia and hot plate tests were done to study analgesic activity. In vitro tests to determine COX-1/COX-2 selectivity and assessment of renal and gastric toxicity upon acute exposure to AD732 were also conducted. Compound AD732 exhibited promising results; higher anti-inflammatory and analgesic effects compared to standard agents, coupled with the absence of ulcerogenic effects and minimal detrimental effects on renal function. Additionally, compound AD732 was a less potent inhibitor of COX-2 in vitro than celecoxib, which may indicate lower potential cardiovascular toxicity. It may be concluded that compound AD732 appears to be a safer and more effective molecule with promising potential for the management of pain and inflammation.
Topics: Analgesics; Animals; Anti-Inflammatory Agents; Anti-Inflammatory Agents, Non-Steroidal; Carrageenan; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Edema; Pyrazoles; Rats; Rats, Wistar
PubMed: 34818572
DOI: 10.1016/j.ejps.2021.106080 -
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 -
Current Clinical Pharmacology 2015Orthotopic liver transplantation (OLT) recipients have been reported to have decreased perioperative opioid and intraoperative inhalational anesthetic requirements when... (Review)
Review
Orthotopic liver transplantation (OLT) recipients have been reported to have decreased perioperative opioid and intraoperative inhalational anesthetic requirements when compared to patients without liver disease undergoing other types of major abdominal surgeries. The severity of the liver disease and the process of the transplantation itself may alter the pharmacokinetic and pharmacodynamic effects of different pain medications. Chemical injury of the liver and the high degree of surgical stress may also increase the levels of neuropeptides involved in pain modulation. Per the U.S. Department of Health and Human Services Organ Procurement and Transplantation Network, more than 5,000 OLT cases are being done per year since 2000. With better understanding of the pathophysiology of liver disease and the development of perioperative anesthesia management, the recent concept of improving patient outcome following OLT includes a fast-track approach in selected patients, which may shorten or completely bypass intensive care unit stay and reduce costs. With this development, the understanding of the analgesic pharmacology in the care of the OLT patients is even more important. Proper dosage of medications can achieve adequate intraoperative anesthetic depth and postoperative pain control, while avoiding over-sedation which increases risk of prolonged postoperative mechanical ventilation. The purpose of this review is to summarize the pharmacokinetics and pharmacodynamics of the analgesic medications commonly administered to this patient population.
Topics: Analgesics; Analgesics, Opioid; Anesthetics; Animals; Dose-Response Relationship, Drug; Humans; Liver Diseases; Liver Transplantation; Patient Selection; Severity of Illness Index
PubMed: 24521192
DOI: 10.2174/1574884709666140212101228 -
Current Medicinal Chemistry 2021Despite significant research progress on the pathogenesis, molecular biology, diagnosis, treatment, and prevention of cancer, its morbidity and mortality are still high... (Review)
Review
Despite significant research progress on the pathogenesis, molecular biology, diagnosis, treatment, and prevention of cancer, its morbidity and mortality are still high around the world. The emerging resistance of cancer cells to anticancer drugs remains still a significant problem in oncology today. Furthermore, an important challenge is the inability of anticancer drugs to selectively target tumor cells thus sparing healthy cells. One of the new potential options for efficient and safe therapy can be provided by opioid growth factor (OGF), chemically termed Met-enkephalin. It is an endogenous pentapeptide (Tyr-Gly-Gly-Phe-Met) with antitumor, analgesic, and immune-boosting properties. Clinical trials have demonstrated that OGF therapy alone, as well as in combination with standard chemotherapies, is a safe, non-toxic anticancer agent that reduces tumor size. In this paper, we review the structure-activity relationship of OGF and its analogues. We highlight also OGF derivatives with analgesic, immunomodulatory activity and the ability to penetrate the blood-brain barrier and may be used as safe agents enhancing chemotherapy efficacy and improving quality of life in cancer patients. The reviewed papers indicate that Met-enkephalin and its analogues are interesting candidates for the development of novel, non-toxic, and endowed with an analgesic activity anticancer drugs. More preclinical and clinical studies are needed to explore these opportunities.
Topics: Analgesics; Analgesics, Opioid; Antineoplastic Agents; Enkephalin, Methionine; Humans; Intercellular Signaling Peptides and Proteins; Quality of Life
PubMed: 32129162
DOI: 10.2174/0929867327666200304122406