Pharmacology of Opioid Analgesic Agents — A Contemporary View

1993 ◽  
pp. 14-30
Author(s):  
L. Mather
Keyword(s):  
Opioid Analgesic ◽  
Contemporary View ◽  
Analgesic Agents

Transmodulation of Dopaminergic Signaling to Mitigate Hypodopminergia and Pharmaceutical Opioid-induced Hyperalgesia

2020 ◽  
Vol 9 (3) ◽  
pp. 164-184
Author(s):  
Raymond Brewer ◽  
Kenneth Blum ◽  
Abdalla Bowirrat ◽  
Edward J. Modestino ◽  
David Baron ◽  
...  
Keyword(s):  
Opioid Analgesic ◽  
Opioid Analgesics ◽  
Well Being ◽  
Deficiency Syndrome ◽  
Pain Tolerance ◽  
Opioid Agonist ◽  
Opioid Agonist Therapy ◽  
Analgesic Agents ◽  
Opioid Induced Hyperalgesia ◽  
Intensive Investigation

Neuroscientists and psychiatrists working in the areas of “pain and addiction” are asked in this perspective article to reconsider the current use of dopaminergic blockade (like chronic opioid agonist therapy), and instead to consider induction of dopamine homeostasis by putative pro-dopamine regulation. Pro-dopamine regulation could help pharmaceutical opioid analgesic agents to mitigate hypodopaminergia-induced hyperalgesia by inducing transmodulation of dopaminergic signaling. An optimistic view is that early predisposition to diagnosis based on genetic testing, (pharmacogenetic/pharmacogenomic monitoring), combined with appropriate urine drug screening, and treatment with pro-dopamine regulators, could conceivably reduce stress, craving, relapse, enhance well-being and attenuate unwanted hyperalgesia. These concepts require intensive investigation. However, based on the rationale provided herein, there is a good chance that combining opioid analgesics with genetically directed pro-dopamine-regulation using KB220 (supported by 43 clinical studies). This prodopamine regulator may become a front-line technology with the potential to overcome, in part, the current heightened rates of chronic opioid-induced hyperalgesia and concomitant Reward Deficiency Syndrome (RDS) behaviors. Current research does support the hypothesis that low or hypodopaminergic function in the brain may predispose individuals to low pain tolerance or hyperalgesia.

Meptazinol Overdose Producing Near Fatal Respiratory Depression

1987 ◽  
Vol 6 (4) ◽  
pp. 331-331 ◽  
Author(s):  
A.G. Davison ◽  
P.O. Collinson ◽  
A.R. Assefi ◽  
S.W. Clarke
Keyword(s):  
Respiratory Depression ◽  
Opioid Analgesic ◽  
Oral Formulation ◽  
Respiratory Arrest ◽  
Analgesic Agents ◽  
Clinically Significant

Meptazinol is one of the new powerful opioid analgesic agents, and an oral formulation has recently been marketed. Clinically significant respiratory depression is said to be absent1 and no overdoses from meptazinol have been reported in the literature. We report a patient who had a respiratory arrest following an overdose of meptazinol.

scholarly journals Designing Opioids That Deter Abuse

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Robert B. Raffa ◽  
Joseph V. Pergolizzi ◽  
Edmundo Muñiz ◽  
Robert Taylor ◽  
Jason Pergolizzi
Keyword(s):  
Current Knowledge ◽  
Opioid Analgesic ◽  
Opioid Abuse ◽  
Prescription Opioid ◽  
Opioid Agonist ◽  
Biological Targets ◽  
Actual Use ◽  
Analgesic Agents ◽  
Physical Barriers ◽  
Public Health Challenge

Prescription opioid formulations designed to resist or deter abuse are an important step in reducing opioid abuse. In creating these new formulations, the paradigm of drug development target should be introduced. Biological targets relating to the nature of addiction may pose insurmountable hurdles based on our current knowledge and technology, but products that use behavioral targets seem logical and feasible. The population of opioid abusers is large and diverse so behavioral targets are more challenging than they appear at first glance. Furthermore, we need to find ways to correlate behavioral observations of drug liking to actual use and abuse patterns. This may involve revisiting some pharmacodynamic concepts in light of drug effect rather than peak concentration. In this paper we present several new opioid analgesic agents designed to resist or deter abuse using physical barriers, the inclusion of an opioid agonist or antagonist, an aversive agent, and a prodrug formulation. Further, this paper also provides insight into the challenges facing drug discovery in this field. Designing and screening for opioids intended to resist or deter abuse is an important step to meet the public health challenge of burgeoning prescription opioid abuse.

Opioid Analgesic Agents and Cancer Cell Biology

2015 ◽  
Vol 5 (3) ◽  
pp. 278-284 ◽  
Author(s):  
Nan Xie ◽  
Marie-Odile Parat
Keyword(s):  
Cancer Cell ◽  
Cell Biology ◽  
Opioid Analgesic ◽  
Analgesic Agents

Centrally-acting non-opioid analgesic agents

Pain ◽  
1987 ◽  
Vol 30 ◽  
pp. S219
Author(s):  
Ilmar Jurna
Keyword(s):  
Opioid Analgesic ◽  
Analgesic Agents

Recovery after a lumbar disc herniation is dependent on a gender and OPRM1 Asn40Asp genotype interaction

2012 ◽  
Vol 3 (3) ◽  
pp. 182
Author(s):  
M.B. Olsen ◽  
L.M. Jacobsen ◽  
E.I. Schistad ◽  
L.M. Pedersen ◽  
L.J. Rygh ◽  
...  
Keyword(s):  
Pain Intensity ◽  
Lumbar Disc Herniation ◽  
Disc Herniation ◽  
Lumbar Disc ◽  
Opioid Analgesic ◽  
University Hospital ◽  
Endogenous Opioid ◽  
Discogenic Low Back Pain ◽  
Analgesic Agents ◽  
Exon 1

AbstractBackground/aimsThe μ-opioid receptor (OPRM1) is the major target of endogenous opioid peptides and opioid analgesic agents. An important single nucleotide polymorphism (SNP) in this gene is the functional SNP, rs1799971, leading to a substitution of asparagine (Asn) to aspartic acid (Asp) at codon 40 in exon 1. Previous studies have suggested that this SNP may give different phenotypes in males and females. In the present study we therefore investigated whether the OPRM1 Asn40Asp SNP, grouped by gender, could predict clinical outcome regarding progression of pain intensity and disability in patients with discogenic low back pain and sciatica.MethodsPatients (n = 252) with lumbar disc herniation and sciatic pain, all European-caucasian, were recruited from Oslo University Hospital Ullevål and Haukeland University Hospital. Blood samples were drawn, genomic DNA isolated and the OPRM1 Asn40Asp SNP was detected by TaqMan methodology. Pain intensity and functional consequences were rated on a visual analogue scale (VAS), by McGill Sensory and by Oswestry Disability Index (ODI) over a 12 months period (inclusion, 6 weeks, 6 months and 12 months).ResultsThe genotype */Asp was associated with more pain in women, but seemed to protect the men from pain after lumbar disc herniation. Wildtype Asn/Asn women and men reported similar pain ratings. Analysis of the recovery for the four groups; women Asn/Asn, women */Asp, men Asn/Asn and men */Asp, showed that the */Asp women had a significantly slower recovery, i.e., pain intensity over time than the */Asp men (VAS activity score p = 0.002, McGill sense score p = 0.021, ODI p = 0.205, rmANOVA including covariates smoke, treatment and age with p ≤ 0.1).ConclusionThe present data suggest that the OPRM1 Asp variant increases the pain intensity in women, but have the opposite effect on men the first year after a disc herniation.

Exogenous gaseous superoxide potentiates the antinociceptive effect of opioid analgesic agents

1996 ◽  
Vol 45 (9) ◽  
pp. 473-478 ◽  
Author(s):  
N. Goldstein ◽  
T. Lewin ◽  
A. Kamensky ◽  
V. Dubinin ◽  
S. Baumann ◽  
...  
Keyword(s):  
Opioid Analgesic ◽  
Antinociceptive Effect ◽  
Analgesic Agents

N-substituted aminohydroxypyridines as potential non-opioid analgesic agents

1995 ◽  
Vol 3 (7) ◽  
pp. 929-937 ◽  
Author(s):  
M.C. Viaud ◽  
P. Jamoneau ◽  
J.G. Bizot-Espiard ◽  
B. Pfeiffer ◽  
P. Renard ◽  
...  
Keyword(s):  
Opioid Analgesic ◽  
Analgesic Agents

Analgesics in anaesthetic practice

2017 ◽  
Author(s):  
John Williams ◽  
Francis Bonnet
Keyword(s):  
Postoperative Pain ◽  
Opioid Analgesic ◽  
Postoperative Outcome ◽  
Perioperative Period ◽  
Well Being ◽  
Number Needed To Treat ◽  
Analgesic Agents ◽  
The Central Nervous System ◽  
Sensory Consequence ◽  
History Of Use

Each year, approximately 230 million major surgical procedures are undertaken worldwide, with over three-quarters of the patients complaining of pain postoperatively and 10% complaining of severe pain. Pain is not, however, just an unpleasant sensory consequence of surgery, but can also have significant physiological implications impacting negatively on well-being and postoperative outcome. Postoperative pain may also result in changes within the central nervous system, leading to the development of chronic pain states lasting in excess of 3–6 months. Adequate analgesia has proven to be effective when employed in the perioperative period at combating many of these adverse effects. An understanding of the basic physiological and pharmacological mechanisms responsible for producing, transmitting, and sustaining pain has allowed for a variety of effective analgesic agents to be fashioned and used clinically to treat pain. Morphine, the archetypal opioid analgesic, is the most familiar of these agents with a long history of use and evidence of effectiveness; morphine possesses a number-needed-to-treat (NNT) to reduce pain by 50% of around 3 when given in doses of between 10 and 15 mg. Non-steroidal agents and paracetamol are similarly effective in the immediate postoperative period with NNTs of between 2 and 4. More recently, a number of analgesic adjuncts such as gabapentin, pregabalin, ketamine, clonidine, and nefopam have found favour for the treatment of acute postoperative pain. None of these agents, however, are without side-effects, ensuring that the search for effective analgesic agents continues to be a vibrant area of research with new analgesic agents continuing to be developed.

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