New small molecule analgesics

2021 ◽  
Vol 28 ◽  
Author(s):  
Sergey S. Laev ◽  
Nariman F. Salakhutdinov
Keyword(s):  
Pain Management ◽  
Small Molecule ◽  
Opioid Analgesics ◽  
Analgesic Drugs ◽  
Analgesic Effects ◽  
Design And Synthesis ◽  
Analgesic Agents ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
New Perspective

: Pain is a symptom of ninety percent of human diseases, and pain management is a very important medicinal problem. Various modulators of the pain response have been detected and analgesic effects are obtained by increasing inhibition or decreasing excitation in the nervous system. Various known analgesic drugs are commonly used to relieve the pain; however, this problem is still not fully resolved by currently available treatments. Available analgesic drugs (non-steroidal anti-inflammatory drugs, opioids, and analgesic adjuvants) are not too effective and are severely limited by adverse effects, for example, opioid addiction. Therefore, developing effective pain management is a difficult but necessary task. Thus, there is an urgent need for further development of the design and synthesis of new analgesic agents. The aim of this review is to present recent progress in search of new small molecule analgesics. The structures and effects of new perspective analgesic agents (anti-inflammatory agents, opioid analgesics, adjuvant agents for pain management and natural compounds) are presented and discussed. The review covers the literature published in 2015-2020 years and includes 173 references.

scholarly journals Nonsteroid anti-inflammatory drugs (NSAID) and risk of cardiovascular events. Literature review and clinical implications

2015 ◽  
Vol 82 (3) ◽  
Author(s):  
Pier Luigi Temporelli ◽  
Giovanni Battista Zito ◽  
Roberto Franco Pedretti ◽  
Francesco Iachini Belisarii ◽  
Giuseppe Putortì ◽  
...  
Keyword(s):  
Chronic Pain ◽  
Cardiovascular Events ◽  
Large Body ◽  
Cyclooxygenase Inhibitors ◽  
Current Status ◽  
Analgesic Drugs ◽  
Drug Agency ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Artery Disease

Non steroid anti-inflammatory drugs (NSAIDs) are largely used for treatment of acute and chronic pain, even for long periods of time (months or years). While it is known that their use is frequently associated with gastrointestinal damage, including major bleedings from peptic ulcer, the risk of cardiovascular events related to NSAID has received much less attention. However, there is a large body of evidence showing that NSAIDs (both “traditional”, such as diclofenac or indobufen, and selective cyclooxygenase inhibitors, COX-2) are associated with a significant increase of risk of cardiovascular events, both fatal and nonfatal. Consequently, several options have been proposed for the treatment of pain, including the use of analgesic drugs with different mechanisms of action, such as the opiates. Of interest, the Italian Drug Agency (AIFA) published a few years ago a warning (Nota 66) on the careful prescription of NSAIDs in patients with overt heart disease, such as coronary artery disease and heart failure. Aim of this paper is to present the current status of knowledge on the proper use of NSAIDs and other analgesic drugs in the management of acute and chronic pain.

scholarly journals Comparative analysis of different methods of anesthesia in patients with acute pancreatitis using pain scales

2016 ◽  
Vol 97 (2) ◽  
pp. 217-221
Author(s):  
V N Shilenok ◽  
E V Nikitina
Keyword(s):  
Acute Pancreatitis ◽  
Comparative Analysis ◽  
Visual Analogue Scale ◽  
Pain Intensity ◽  
Epidural Anesthesia ◽  
Analogue Scale ◽  
Pain Syndrome ◽  
Opioid Analgesics ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Aim. To conduct a comparative analysis of used anesthesia methods in patients with acute pancreatitis in intensive care units settings using pain scales.Methods. Depending on the anesthesia type, 44 patients with acute pancreatitis were divided into three groups: the first group received intramuscular injections of nonsteroidal anti-inflammatory drugs and spasmolytics, the second group - intramuscular injections of non-steroidal anti-inflammatory drugs and opioid analgesics, the third group - epidural anesthesia with local anesthetics. Comparative analysis of pain character, intensity was conducted, its dynamics in patients of all groups amid anesthesia was evaluated using a visual analogue scale, verbal rating scale, verbal descriptor scale, McGill pain questionnaire.Results. Baseline pain intensity in patients of all groups was high. Patients estimated this pain as «very strong». The time and the level of pain intensity reduction for various anesthesia types had differences. Pain syndrome was eliminated slower in patients of the second group. By the end of the 1st day, patients of this group continued to complain of «strong» pain. Pain intensity decreased only on the 2nd day - patients reported «moderate» pain. Pain syndrome was not completely eliminated in these patients for 2 days of anesthesia. 97.7% of patients reported that the visual analogue scale is the most acceptable pain assessment scale for them.Conclusion. In patients with acute pancreatitis, the most optimal anesthesia types are intramuscular nonsteroidal anti-inflammatory drugs with spasmolytics and prolonged epidural anesthesia with local anesthetics; intramuscular administration of opioid analgesics with non-steroidal anti-inflammatory drugs is less effective in relieving pain.

scholarly journals Peripheral Tramadol in Dentistry: A New Use for an Old Drug

2016 ◽  
Vol 18 (2) ◽  
pp. 10
Author(s):  
Daniel Chavarría DDS, MSc, PhD ◽  
Amaury Pozos DDS, MSc, PhD
Keyword(s):  
Adverse Effects ◽  
Opioid Receptors ◽  
Analgesic Effect ◽  
Health Sciences ◽  
Analgesic Drug ◽  
Orofacial Region ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
New Perspective ◽  
Inflammatory Action

Tramadol is a well known central acting analgesic drug, used in a wide variety of treatments within health sciences; including dentistry. Due to its lack of anti-inflammatory action and some adverse effects related mainly to opioid receptors agonism, it is not use as a routine alternative; keeping mainly for patients allergic to non-steroideal anti-inflammatory drugs or as an adjuvant to manage severe odontogenic pain.  Since new available evidence supports the possible analgesic effect of this drug when is applied locally in different sites, recent reports have been done to explore the same effect in the orofacial region, especially to improve the local management of odontogenic pain. This new perspective article summarize some of the current efforts develop to explore the peripheral Tramadol in dentistry; “a new use for an old drug”. 

Acute pain

2021 ◽  
pp. 1151-1180
Author(s):  
Adrian Dashfield ◽  
David Kibblewhite
Keyword(s):  
Pain Management ◽  
Epidural Analgesia ◽  
Peripheral Nerve ◽  
Acute Pain ◽  
Nerve Stimulation ◽  
Transcutaneous Electrical Nerve Stimulation ◽  
Electrical Nerve Stimulation ◽  
Analgesic Drugs ◽  
Peripheral Nerve Blockade ◽  
Inflammatory Drugs

This chapter discusses the management of acute pain. It begins with an introduction which describes the benefits of acute pain management and the measurement of pain. Analgesic drugs are then described, including paracetamol; non-steroidal anti-inflammatory drugs (NSAIDs), and opioids (including their comparative efficacy). Patient-controlled analgesia (PCA), epidural analgesia, and continuous peripheral nerve blockade are described. Transcutaneous electrical nerve stimulation (TENS) and acupuncture are discussed. The management of the patient with persistent pain and a substance misuse disorder is also discussed. The chapter concludes with a discussion of non-opioid adjuvant analgesics.

Nonsteroidal Anti-Inflammatory Drugs in Perisurgical Pain Management

Drugs ◽  
1995 ◽  
Vol 49 (1) ◽  
pp. 51-70 ◽  
Author(s):  
Jeremy Cashman ◽  
Gregory McAnulty
Keyword(s):  
Pain Management ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Synthesis of new ibuprofen hybrid conjugates as potential anti-inflammatory and analgesic agents

2020 ◽  
Vol 12 (15) ◽  
pp. 1369-1386
Author(s):  
Siva S Panda ◽  
Adel S Girgis ◽  
Hitesh H Honkanadavar ◽  
Riham F George ◽  
Aladdin M Srour
Keyword(s):  
Writhing Test ◽  
Rat Paw Edema ◽  
Analgesic Agents ◽  
Inflammatory Drugs ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Inhibition Studies

Background: A new set of hybrid conjugates derived from 2-(4-isobutylphenyl)propanoic acid (ibuprofen) is synthesized to overcome the drawbacks of the current non-steroidal anti-inflammatory drugs. Results & methodology: Synthesized conjugates were screened for their anti-inflammatory, analgesic and ulcerogenic properties. Few conjugates were found to have significant anti-inflammatory properties in the carrageenan-induced rat paw edema test, while a fair number of conjugates showed promising peripheral analgesic activity in the acetic acid-induced writhing test as well as central analgesic properties in the in vivo hot plate technique. The newly synthesized conjugates did not display any ulcerogenic liability. Conclusion: In vitro, COX-1 and COX-2 enzyme inhibition studies raveled compound 7e is more selective toward COX-2 compared with ibuprofen.

scholarly journals The use of analgesic drugs by South African veterinarians : continuing education

2001 ◽  
Vol 72 (1) ◽  
Author(s):  
K.E. Joubert
Keyword(s):  
Chronic Pain ◽  
Continuing Education ◽  
South African ◽  
Specific Drug ◽  
Analgesic Drugs ◽  
Flunixin Meglumine ◽  
Post Operative Pain ◽  
Analgesic Agents ◽  
Anti Inflammatory ◽  
Balanced Anaesthesia

According to a survey, non-steroidal anti-inflammatory agents were the most popular analgesic used in South Africa for management of peri-operative pain, acute post-operative pain and chronic pain. The most popular non-steroidal anti-inflammatory agents are flunixin meglumine and phenylbutazone. The most popular opioid type drug is buprenorphine, followed by morphine. In the peri-operative setting, analgesic agents were not actively administered to 86.3 % of cats and 80.7 % of dogs. Analgesic premedications were frequently administered, e.g. xylazine or ketamine, but no specific drug was administered for post-operative pain. Veterinarians need to critically review their anaesthetic and analgesic practices in order to achieve balanced anaesthesia.

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