-
Drugs Jul 2021We conducted a narrative review of the literature to compare the pharmacological, efficacy and safety profiles of tapentadol and tramadol, and to assess the clinical...
We conducted a narrative review of the literature to compare the pharmacological, efficacy and safety profiles of tapentadol and tramadol, and to assess the clinical interest of tapentadol in adult patients. Tapentadol and tramadol share a mixed mechanism of action, including both mu-agonist and monoaminergic properties. Tapentadol is approximately two to three times more potent than tramadol and two to three times less potent than morphine. It has no identified analgesically active metabolite and is not significantly metabolised by cytochrome P450 enzymes, thus overcoming some limitations of tramadol, including the potential for pharmacokinetic drug-drug interactions and interindividual variability due to genetic polymorphisms of cytochrome P450 enzymes. The toxicity profiles of tramadol and tapentadol are similar; however tapentadol is likely to result in less exposure to serotoninergic adverse effects (nausea, vomiting, hypoglycaemia) but cause more opioid adverse effects (constipation, respiratory depression, abuse) than tramadol. The safety of tapentadol in real-world conditions remains poorly documented, particularly in at-risk patient subgroups and also in the ability to assess the risk associated with its residual serotonergic activity (serotonin syndrome, seizures). Because of an earlier market introduction, more real-world safety data are available for tramadol, including data from at-risk patient subgroups. The level of evidence on the efficacy of both tramadol and tapentadol for the treatment of chronic pain is globally low. The trials published to date show overall that tapentadol does not provide a clinically significant analgesic improvement compared to existing treatments, for which the safety profile is much better known. In conclusion, tapentadol is not a first-line opioid but represents an additional analgesic in the therapeutic choices, which some patients may benefit from after careful examination of their clinical situation, co-morbidities and co-medications.
Topics: Analgesics, Opioid; Cytochrome P-450 CYP2D6; Dose-Response Relationship, Drug; Humans; Liver Failure; Pain; Renal Insufficiency; Tapentadol; Tramadol
PubMed: 34196947
DOI: 10.1007/s40265-021-01515-z -
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 -
Journal of Pain and Symptom Management May 2005Hydromorphone is a semi-synthetic opioid that has been used widely for acute pain, chronic cancer pain and to a lesser extent, in chronic nonmalignant pain. Its... (Review)
Review
Hydromorphone is a semi-synthetic opioid that has been used widely for acute pain, chronic cancer pain and to a lesser extent, in chronic nonmalignant pain. Its pharmacokinetics and pharmacodynamics have been well studied, including immediate release oral preparations, a variety of slow release oral preparations, as well as administration through intravenous, subcutaneous, epidural, intrathecal and other routes. It is known to be metabolized to analgesically inactive metabolites that have been associated with neuroexcitatory states and other toxicity. There is no evidence that hydromorphone has any greater abuse liability than other opioids. Further research is needed to address remaining areas of uncertainty: equianalgesic ratios; relative risk of toxicity compared with other opioids, its use in nonmalignant pain, and the role of specific hydromorophone metabolites in the development of toxicity, particularly in association with organ failure.
Topics: Analgesics, Opioid; History, 20th Century; Humans; Hydromorphone; Neoplasms; Pain; Pharmaceutical Preparations; Substance-Related Disorders
PubMed: 15907647
DOI: 10.1016/j.jpainsymman.2005.01.007 -
Toxins Feb 2019Chronic pain is a major medical issue which reduces the quality of life of millions and inflicts a significant burden on health authorities worldwide. Currently,... (Review)
Review
Chronic pain is a major medical issue which reduces the quality of life of millions and inflicts a significant burden on health authorities worldwide. Currently, management of chronic pain includes first-line pharmacological therapies that are inadequately effective, as in just a portion of patients pain relief is obtained. Furthermore, most analgesics in use produce severe or intolerable adverse effects that impose dose restrictions and reduce compliance. As the majority of analgesic agents act on the central nervous system (CNS), it is possible that blocking pain at its source by targeting nociceptors would prove more efficient with minimal CNS-related side effects. The development of such analgesics requires the identification of appropriate molecular targets and thorough understanding of their structural and functional features. To this end, plant and animal toxins can be employed as they affect ion channels with high potency and selectivity. Moreover, elucidation of the toxin-bound ion channel structure could generate pharmacophores for rational drug design while favorable safety and analgesic profiles could highlight toxins as leads or even as valuable therapeutic compounds themselves. Here, we discuss the use of plant and animal toxins in the characterization of peripherally expressed ion channels which are implicated in pain.
Topics: Analgesics; Animals; Humans; Ion Channels; Toxins, Biological
PubMed: 30813430
DOI: 10.3390/toxins11020131 -
Alcoholism, Clinical and Experimental... Aug 2022Although recent literature provides promising support for the analgesic properties of alcohol, potential differences in alcohol analgesia as a function of chronic pain... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
Although recent literature provides promising support for the analgesic properties of alcohol, potential differences in alcohol analgesia as a function of chronic pain status are not well understood. Thus, this study examined chronic pain status as a potential moderator of alcohol analgesia and distinguished between multiple aspects of pain experience and sensitivity: pain threshold, pain intensity, pain unpleasantness, and perceived relief.
METHODS
Social drinkers with (N = 19) and without (N = 29) chronic jaw pain completed two testing sessions in a counterbalanced order: alcohol (target BrAC = 0.08 g/dl) and placebo. In each, pressure algometry was performed at the insertion of the masseter. Alcohol analgesia was assessed by examining the main and interactive effects of beverage condition, pressure level (4, 5, or 6 pound-feet [lbf]), and chronic jaw pain status (chronic pain vs. pain-free control) on quantitative sensory testing measures and pain relief ratings following noxious stimuli.
RESULTS
Analyses indicated significant increases in pain threshold and pain relief and reductions in pain unpleasantness and pain intensity, under the alcohol condition. Chronic pain participants demonstrated lower pain thresholds and greater pain intensity and pain unpleasantness ratings than controls. There were no interactive effects of alcohol and pain conditions on any pain measure.
CONCLUSIONS
Findings provide experimental evidence of alcohol's analgesic and pain-relieving effects and suggest that these effects do not significantly differ by chronic pain status. Individuals, who self-medicate pain via alcohol consumption, irrespective of pain status, may be at increased risk to engage in hazardous drinking patterns and thus experience adverse alcohol-related consequences.
Topics: Adult; Alcohol Drinking; Analgesics; Chronic Pain; Ethanol; Humans; Pain Measurement; Pain Threshold
PubMed: 35989585
DOI: 10.1111/acer.14883 -
Molecules (Basel, Switzerland) Dec 2021extract (YHS) has been used for centuries across Asia for pain relief. The extract is made up of more than 160 compounds and has been identified as alkaloids, organic... (Review)
Review
extract (YHS) has been used for centuries across Asia for pain relief. The extract is made up of more than 160 compounds and has been identified as alkaloids, organic acids, volatile oils, amino acids, alcohols, and sugars. However, the most crucial biological active constituents of YHS are alkaloids; more than 80 have been isolated and identified. This review paper aims to provide a comprehensive review of the phytochemical and pharmacological effects of these alkaloids that have significant ties to analgesia.
Topics: Alkaloids; Analgesics; Corydalis; Drugs, Chinese Herbal; Humans; Molecular Structure; Pain; Plant Extracts
PubMed: 34946576
DOI: 10.3390/molecules26247498 -
Molecules (Basel, Switzerland) Sep 2021Adequate pain management, particularly chronic pain, remains a major challenge associated with modern-day medicine. Current pharmacotherapy offers unsatisfactory... (Review)
Review
Adequate pain management, particularly chronic pain, remains a major challenge associated with modern-day medicine. Current pharmacotherapy offers unsatisfactory long-term solutions due to serious side effects related to the chronic administration of analgesic drugs. Morphine and structurally related derivatives (e.g., oxycodone, oxymorphone, buprenorphine) are highly effective opioid analgesics, mediating their effects via the activation of opioid receptors, with the mu-opioid receptor subtype as the primary molecular target. However, they also cause addiction and overdose deaths, which has led to a global opioid crisis in the last decades. Therefore, research efforts are needed to overcome the limitations of present pain therapies with the aim to improve treatment efficacy and to reduce complications. This review presents recent chemical and pharmacological advances on 14-oxygenated--methylmorphinan-6-ones, in the search of safer pain therapeutics. We focus on drug design strategies and structure-activity relationships on specific modifications in positions 5, 6, 14 and 17 on the morphinan skeleton, with the goal of aiding the discovery of opioid analgesics with more favorable pharmacological properties, potent analgesia and fewer undesirable effects. Targeted molecular modifications on the morphinan scaffold can afford novel opioids as bi- or multifunctional ligands targeting multiple opioid receptors, as attractive alternatives to mu-opioid receptor selective analgesics.
Topics: Analgesics; Analgesics, Opioid; Animals; Morphinans; Receptors, Opioid, mu; Signal Transduction
PubMed: 34577147
DOI: 10.3390/molecules26185677 -
Journal of Opioid Management 2009Historically and anecdotally cannabinoids have been used as analgesic agents. In recent years, there has been an escalating interest in developing cannabis-derived... (Review)
Review
Historically and anecdotally cannabinoids have been used as analgesic agents. In recent years, there has been an escalating interest in developing cannabis-derived medications to treat severe pain. This review provides an overview of the history of cannabis use in medicine, cannabinoid signaling pathways, and current data from preclinical as well as clinical studies on using cannabinoids as potential analgesic agents. Clinical and experimental studies show that cannabis-derived compounds act as antiemetic, appetite modulating, and analgesic agents. However, the efficacy of individual products is variable and dependent upon the route of administration. As opioids are the only therapy for severe pain, analgesic ability of cannabinoids may provide a much-needed alternative to opioids. Moreover, cannabinoids act synergistically with opioids and act as opioid sparing agents, allowing lower doses and fewer side effects from chronic opioid therapy. Thus, rational use of cannabis-based medications deserves serious consideration to alleviate the suffering of patients due to severe pain.
Topics: Analgesics; Analgesics, Opioid; Animals; Antiemetics; Appetite Stimulants; Cannabinoids; Chronic Disease; Drug Therapy, Combination; Humans; Pain; Pain Measurement; Receptors, Cannabinoid; Severity of Illness Index; Signal Transduction; Treatment Outcome
PubMed: 20073408
DOI: No ID Found -
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 -
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