Basic opioid pharmacology: an update

Pathan, Hasan; Williams, John P.

doi:10.1177/2049463712438493

Cited by 490 publications

(342 citation statements)

References 19 publications

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“…Meperidine is a synthetic compound of morphine and has a same affinity to MU, Kappa, and Delta opioid receptors (22). In contrast to meperidine, morphine has a low efficacy in prevention of shivering.…”

Section: Discussionmentioning

confidence: 99%

Comparison of the Effects of Intrathecal Meperidine and Morphine on Incidence and Intensity of Shivering After Caesarean Sections Under Spinal Anesthesia: A Randomized Controlled Trial

Nasseri

Ghaderi

Khezripour

2017

Iran Red Crescent Med J

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Section: Discussionmentioning

confidence: 99%

Comparison of the Effects of Intrathecal Meperidine and Morphine on Incidence and Intensity of Shivering After Caesarean Sections Under Spinal Anesthesia: A Randomized Controlled Trial

Nasseri

Ghaderi

Khezripour

2017

Iran Red Crescent Med J

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“…The respective precursors to these important pain-modulating neuropeptides are pro-opiomelanocortin (POMC), pro-enkephalin, and pro-dynorphin, respectively [181]. Moreover, so-called endomorphins have also been identified; they have the highest affinity for the µ opioid receptor [129].…”

Section: Neurotransmitters and Neuropeptidesmentioning

confidence: 99%

“…However, the status of endomorphins as endogenous ligands remains controversial [149]. In addition to the classical three opioid receptors δ, κ, and µ associated with the above-mentioned endogenous opioids, a fourth opioid receptor has been described: the nociceptin receptor (also named NOP, or orphanin FQ, or OP4, or opioid-like receptor 1) [149,181]. Currently, cebranopadol, which is both a nociceptin receptor agonist and a µ receptor agonist, is being tested in several clinical trials [133].…”

Section: Neurotransmitters and Neuropeptidesmentioning

confidence: 99%

The Cerebrospinal Fluid in Severe Pain Conditions : Clinical, Pharmacological and Proteomic Aspects

Bäckryd¹

2015

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The treatment of both cancer pain and non-cancer chronic pain is still suboptimal. The overall aim of this PhD thesis was to conduct translational pain research at the interface between clinical pain medicine and the field of human proteomics, using the practice of intrathecal analgesia at our institution as a starting point. Hence, the cerebrospinal fluid (CSF) is at the centre of the present dissertation, both as a target for infusing analgesics (Papers I and II – clinical and pharmacological aspects) and as an important biofluid for human biomarker studies (Papers III and IV – proteomic aspects). In Paper I, 28 cases of intrathecal analgesia in cancer patients were prospectively followed. Movement-evoked breakthrough pain remained a major clinical problem throughout the study month despite otherwise successful intrathecal analgesia (defined as good control of spontaneous resting pain paralleled by a marked decrease of concomitant systemic opioid doses). This study therefore illustrates the importance of considering not only spontaneous resting pain but also movement-evoked breakthrough pain. In Paper II, an expert-based algorithm for trialing the intrathecal analgesic ziconotide by bolus injections was evaluated in an open-label study of 23 patients with chronic neuropathic pain. We found few responders (13%) according to the strict criteria of the algorithm, but ziconotide bolus injection trialing seems feasible. The predictive power of ziconotide bolus trialing remains unclear, and the pharmacological profile of ziconotide (with very slow tissue penetration due to high hydrophilicity) calls the rationale for ziconotide bolus trialing into question. In Paper III, we found low levels of beta-endorphin in the CSF of chronic neuropathic pain patients (n=15) compared to healthy controls (n=19). We speculate that this might indicate dysfunctional top-down control of nociception. Substance P levels in the CSF did not differ by univariate statistics. In Paper IV, the CSF proteome of 11 patients with chronic neuropathic pain and 11 healthy controls was exploratively studied, combining gel-based proteomics with multivariate data analysis. After eliminating four proteins associated with age, 32 proteins were found to highly discriminate between groups. Among these, the seven proteins having the highest discriminatory power between patients and controls were: one isoform of angiotensinogen, two isoforms of alpha-1-antitrypsin, three isoforms of haptoglobin, and one isoform of pigment epithelium-derived factor. In conclusion, this PhD thesis demonstrates the fruitfulness of studying the CSF, both as a target for infusing analgesics and as a potential mirror of the neurobiological processes involved in pathological pain conditions. The thesis points to the need for more research into the mechanisms of different pain conditions, in order to hopefully achieve the vision of mechanism-based pain diagnoses

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“…It is a potent hydrophilic, selective for µ opioid agonist, with slow onset of action, longer duration of action, less pulmonary first pass effect, less unionized form, and less plasma proteins bound. [7,8] Fentanyl is a potent lipophilic opioid agonist, but 100 times more potent than morphine, with rapid onset of action, shorter duration of action, undergoes significant pulmonary first pass effect, highly bound to plasma protein, larger volume of distribution, longer elimination halftime, longer context sensitivity halftime, and effect site-equilibrium time. It produces less histamine than morphine.…”

Section: Introductionmentioning

confidence: 99%

A randomized clinical study comparing the analgesic efficacy of intra venous patient- controlled analgesia of morphine with fentanyl in post-operative pain management of major surgery patients

Kumar¹,

Ramakrishnappa²,

Bekal³

2018

Natl J Physiol Pharm Pharmacol

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Background: Post-operative pain is a protective but an unwanted effect which is to be treated for the better outcome of surgery. Aims and Objectives: The aim of this study is to compare the safety and analgesic efficacy of intravenous patient-controlled analgesia (IV PCA) using morphine and fentanyl for post-operative pain management in major surgery patients. Materials and Methods: The randomized clinical study initiated after the ethics committee approval and informed consenting. A total of 60 patients belonging to the American Society of Anesthesiology Grade -I, II, and III physical status, scheduled for major abdominal, oncological surgeries under general anesthesia were randomly allocated to two groups. Group M received IV PCA with morphine (basal continuous infusion 0.02 mg/kg/h, bolus dose of 0.02 mg/kg, and lockout period of 20 min), and the Group F received IV PCA with fentanyl (basal continuous infusion 0.5 µg/kg/h, bolus dose of 0.5 µg/kg, and lockout period of 20 min). Fentanyl dosage was converted into morphine equivalents. The outcomes such as visual analog scale (VAS), sedation score, hemodynamic parameters, and adverse effects were compared between groups and analyzed statistically. Results: Morphine provides better analgesia than fentanyl as indicated by lower VAS scores (score = 3) at the end of 24-72 h. Mean cumulative analgesic consumption was higher in fentanyl group (436.3 ± 330.2 mg) compared with morphine group (123.9 ± 28.2 mg) by 72 h. Regarding the hourly consumption, Group M consumed less drug than fentanyl group was statistically significant (P = 0.05). Conclusion: Morphine provides more effective post-operative analgesia than fentanyl administered through IV PCA. The PCA allows patients to balance between administration of analgesics and adverse events by self-adjusting the dose of analgesic used.

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Basic opioid pharmacology: an update

Cited by 490 publications

References 19 publications

Comparison of the Effects of Intrathecal Meperidine and Morphine on Incidence and Intensity of Shivering After Caesarean Sections Under Spinal Anesthesia: A Randomized Controlled Trial

Comparison of the Effects of Intrathecal Meperidine and Morphine on Incidence and Intensity of Shivering After Caesarean Sections Under Spinal Anesthesia: A Randomized Controlled Trial

The Cerebrospinal Fluid in Severe Pain Conditions : Clinical, Pharmacological and Proteomic Aspects

A randomized clinical study comparing the analgesic efficacy of intra venous patient- controlled analgesia of morphine with fentanyl in post-operative pain management of major surgery patients

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