Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

This open one-center study included 40 patients operated on the abdomen and chest, who had moderate resting pain in the immediate postoperative hours. Paracetamol was used as a dropwise intravenous 1-g infusion for 10-15 min; the dose of the agent was 4 g. The interval of paracetamol re-infusion was not early than 4 hours. If additional analgesia was required, opioid analgesics (promedol, tramadol) were administered. As a whole, assessment of analgesia within 24 hours showed excellent and good results reported by patients in 85% of cases; and in 71% of the patients the intensity of postoperative pain was less than they had expected before surgery. The use of opioid analgesics was required in 65% of the patients and 25% did not need these agents. The remaining 10% of the patients received a combination of nonsteroidal anti-inflammatory drugs, paracetomol, and opioids. Postoperative analgesia based on the intravenous infusion of paracetamol in a single dose of 1 g (4 g/day) caused a reduction in the intensity and duration of pain. The intravenous formulation of paracetamol should be regarded as one of the essential nonopioid components of multimodality therapy for pain in patients in the early postoperative period.
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PMID:[Clinical aspects of analgesia with intravenous paracetamol in the early postoperative period]. 1728 68

Non-opioids play an ever increasing role in the treatment of postoperative pain; either on their own for mild to moderate pain or in combination with other analgesic approaches, in particular opioids, as a component of multimodal analgesia. The analgesics paracetamol (acetaminophen) and dipyrone (metamizole) as well as compounds with an additional anti-inflammatory effect (non-selective non-steroidal anti-inflammatory drugs and selective cyclo-oxygenase-2 inhibitors) are used widely in the perioperative period. Paracetamol is gaining renewed interest in this setting due to its minimal adverse effects and recent availability in a parenteral preparation, but its benefits are insufficiently studied. Dipyrone continues to be used in many countries despite the ongoing debate on the incidence and relevance of its ability to cause agranulocytosis. Among the anti-inflammatory drugs, selective cyclo-oxygenase-2 inhibitors have the most supportive data for their beneficial effects as a component of multimodal analgesia and offer benefits with regard to their adverse effect profile.
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PMID:Update on the role of non-opioids for postoperative pain treatment. 1748 17

Pain is a common occurrence for the hospitalized elderly, and may often be under recognized and inadequately managed. Insufficient pain management can lead to the sequelae of emotional distress and depression, delirium, anxiety, sleep disturbances, and physical disabilities, as well as increased health care costs. Effective pain management of the older adult begins with pain assessment using the proper tools. Morphine is the analgesic of choice for the older adult, and is appropriate for the postoperative period. It is important to maintain a therapeutic serum level of opioids to prevent inadequate management of the acute pain. Side effects of opioids include hypotension, nausea, mood disturbances, ileus, histamine production, and respiratory depression. The adage for pain treatment in the elderly is "start low and go slow". Paracetamol is commonly prescribed and may be the drug of choice for mild to moderate postoperative pain. Older adults may enjoy the benefits of Patient-Controlled Analgesia and Patient Controlled Epidural Analgesia in the postoperative period; however, thorough and ongoing teaching must occur to ensure understanding and compliance with the therapy. Treating post-procedure pain in the elderly patient requires an understanding of the normal changes associated with aging and the impact on medications, and multimodal analgesia can be the best approach.
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PMID:[Postoperative pain management in elderly patient]. 1759 59

Paracetamol analgesic mechanism of action is still poorly defined but mainly involves central inhibition of cyclooxygenases. Here we tested the peripheral antinociceptive effects of paracetamol (intraplantar injections) in a rat model of neuropathic pain. Paracetamol dose-dependently decreased mechanical allodynia and lowered nociceptive scores associated with hyperalgesia testing. These effects were inhibited by the administration of cannabinoid CB(1) (AM251) and CB(2) (AM630) receptor antagonists. The participation of the peripheral cannabinoid system in paracetamol analgesia is suggested.
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PMID:The local antinociceptive effects of paracetamol in neuropathic pain are mediated by cannabinoid receptors. 1765 22

This study compared the efficacy and adverse effects of three low doses of morphine (10, 15 and 30 microg x kg(-1)) for caudal epidural analgesia in children undergoing circumcision. A total of 135 boys undergoing out-patient circumcision were randomly assigned to receive 10, 15 or 30 microg x kg(-1) of caudal morphine. Anaesthesia was induced and maintained with propofol. After induction, the morphine was added to 0.5 ml.kg(-1) 1% lignocaine solution with adrenaline 5 microg.ml(-1) and injected caudally. Anaesthesia quality, postoperative pain and adverse events in a 24-hour period were evaluated. Paracetamol (20 mg.kg(-1) orally) was used as rescue analgesia as required. No patient required paracetamol in the first eight hours after the caudal injections. In the first 24 hours postoperatively no further analgesia was required in 66.7%, 77.8% and 91.1% of the patients in the 10, 15 and 30 microg.kg(-1) groups, respectively (P=0.01 for 10 vs. 30 groups). All patients had excellent analgesia. No respiratory complications were observed. Nausea-vomiting occurred in 13.3%, 20% and 46.7% of the patients in the 10, 15 and 30 gg.kg(-1) groups (P=0.002 for 10 vs. 30 and 0.044 for 15 vs. 30). Pruritus occurred in 8.9%, 11% and 15.6% in the 10, 15 and 30 microg.kg(-1) groups but was localised and did not require treatment. This study was not powered to assess concerns that low dose epidural morphine may rarely be associated with delayed apnoea and is therefore considered unsuitable for outpatient use in many centres. Increases in caudal morphine dose above 10 microg.kg1 produce some 'paracetamol sparing' but no improvement in analgesia, some pruritus and a significant increase in nausea and vomiting.
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PMID:Effects of reduction of the caudal morphine dose in paediatric circumcision on quality of postoperative analgesia and morphine-related side-effects. 1793 62

Oral opioids are the treatment of choice for chronic cancer pain. Morphine is the strong opioid of choice for the treatment of moderate to severe cancer pain according to guidelines from the World Health Organization (WHO). This recommendation by the WHO was derived from availability, familiarity to clinicians, established effectiveness, simplicity of administration, and relative inexpensive cost. It was not based on proven therapeutic superiority over other options. Patients who experience inadequate pain relief or intolerable side effects with one opioid may often be successfully treated with another agent or with the same agent administered by a different route. Opioid rotation, or switching to an alternative opioid, helps some patients achieve better pain control with fewer associated adverse effects. Oxycodone is a mu-opioid receptor specific ligand, with clear agonist properties. It is an active potent opioid, which is in part a kappa-receptor agonist. Like morphine and other pure agonists, there is no known ceiling to the analgesic effects of oxycodone. The active metabolites of oxycodone (eg, oxymorphone) could be important in oxycodone-mediated analgesia. The main pharmacokinetic difference between oxycodone and morphine is in oral bioavailability. The bioavailability of oxycodone is >60% and the bioavailability of morphine is 20%. Controlled-release oxycodone is absorbed in a bi-exponential fashion. There is a rapid phase with a mean half-life of 37 min, accounting for 38% of the dose, and a slow phase with a half-life of 6.2 h, which accounts for the residual 62%. Oxycodone elimination is impaired by renal failure because there are both an increased volume of distribution and reduced clearance. A lot of studies prove that the efficacy of controlled-release oxycodone in cancer-pain control is at least the same as morphine, immediate-release oxycodone and hydromorphone. Its toxicity profile seems better than that of morphine. There are actually several illustrations of a lower incidence of side-effects in the central nervous system. It is therefore possible to conclude that oxycodone represents a valid alternative to morphine in the management of moderate to severe cancer pain, also as first-line treatment.
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PMID:Oxycodone controlled release in cancer pain management. 1836 May 98

Analgesia from most opioids is mediated by mu receptors located mainly in the central nervous system. Previous studies have shown a different pharmacological profile of oxycodone in respect to visceral analgesia. This study investigated if morphine and oxycodone have different pharmacokinetic/pharmacodynamic profiles, in particular with respect to delay between opioid blood concentration and analgesia. Twenty-four healthy subjects had oral morphine (30 mg), oxycodone (15 mg), or placebo. Mechanical, thermal, and electrical pain tests were performed in the skin and viscera. Blood samples and pain measurements were taken at baseline and after 15, 30, 60, 90, and 120 minutes. Pharmacokinetic/pharmacodynamic profiles were modeled using a 2-stage, nonlinear, mixed-effects approach with an effect compartment to represent the concentration-analgesia delay. Morphine kinetics was best described by a 2-compartment model, whereas oxycodone kinetics was best described with a 1-compartment model. Generally the analgesic effects of morphine were best related to plasma concentration by introducing a delay via an effect compartment. However, for oxycodone, this was only the case for analgesia in the somatic pain measures, whereas the plasma concentration correlated better to the course of the analgesia with no delay in the visceral pain measures. Oxycodone and morphine showed different pharmacodynamic/pharmacokinetic relationships for the visceral analgesia, whereas relationships were alike for somatic analgesia.
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PMID:Pharmacokinetic-pharmacodynamic modeling of morphine and oxycodone concentrations and analgesic effect in a multimodal experimental pain model. 1844 Sep 21

Acetaminophen is the most used analgesic/antipyretic drug. Its unclear mechanism of action could rely on cyclooxygenase inhibition, NO synthesis blockade or reinforcement of the serotonergic system. Here we show that in thermal, mechanical and chemical pain tests, AM-251, a specific CB(1) receptor antagonist, abolished the analgesic action of acetaminophen, which was also lost in CB(1) receptor knockout mice. Moreover, acetaminophen was shown unable to bind to CB(1) receptors demonstrating an indirect involvement of these receptors in the analgesic effect of this compound. Accordingly with these results, we also demonstrated that the inhibition of FAAH, an enzyme involved in the cerebral metabolism of acetaminophen into AM404, known to reinforce the activity of the endocannabinoid system, suppressed the antinociceptive effect of acetaminophen. In addition, similarly to the interaction of acetaminophen with bulbospinal serotonergic pathways and spinal serotonin receptors, we observed that the antinociceptive activity of ACEA, a CB(1) receptor agonist, was inhibited by lesion of bulbospinal serotonergic pathways and antagonists of spinal 5-HT receptors. We therefore propose that acetaminophen-induced analgesia could involve the following sequence: (1) FAAH-dependent metabolism of acetaminophen into AM404; (2) indirect involvement of CB(1) receptors by this metabolite; (3) endocannabinoid-dependent reinforcement of the serotonergic bulbospinal pathways, and (4) involvement of spinal pain-suppressing serotonergic receptors.
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PMID:Endocannabinoid and serotonergic systems are needed for acetaminophen-induced analgesia. 1848 96

Paracetamol, a centrally acting inhibitor of cyclooxygenase, has less gastrointestinal and platelet-inhibiting side effects and is clinically better tolerated than nonsteroidal anti-inflammatory drugs. Therefore, it will be ideally suited for postoperative pain relief. In this prospective, double-blind, randomized, placebo-controlled study, we evaluated the analgesic efficacy, opioid-sparing effect and effects on opioid-related adverse effects of intravenous (IV) paracetamol in combination with IV morphine after lumbar laminectomy and discectomy. Forty patients were divided into 2 groups (n=20 each) to receive either paracetamol 1 g (group 1) or 0.9% NaCl 100 ml (group 2) at the end of the operation and at 6-hour intervals over 24 hours. IV patient-controlled analgesia with morphine was used as a rescue analgesic in both groups. Pain was evaluated at rest and on movement at the 1st, 2nd, 4th, 6th, 12th, 18th, and 24th hours using a visual analog scale. Hemodynamic parameters, morphine usage, patient satisfaction, and probable side effects were also evaluated. Pain scores at rest and on movement at the 12th, 18th, and 24th hours were significantly lower in group 1 (P<0.001). Morphine consumption was not statistically significantly different between the groups (P>0.05). Vomiting in group 2 was significantly higher (P=0.027). Significantly more patients in the paracetamol group rated their pain management as excellent (45% vs. 5%). Although repeated IV paracetamol usage after lumbar laminectomy and discectomy did not demonstrate a significant opioid-sparing effect, it did decrease visual analog scale scores at certain evaluation times and incidence of vomiting and increase patient satisfaction.
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PMID:Intravenous paracetamol improves the quality of postoperative analgesia but does not decrease narcotic requirements. 1858 Mar 46

We reviewed commonly used analgesics and determined their safety and efficacy in surgical neonates in a retrospective study on surgical neonates who had analgesics at the University of Benin Teaching Hospital between January 1998 and December 2007. A total of 2590 pediatric operations were performed on 2563 children; 368 (14.2%) on neonates, 256 boys and 112 girls with male:female ratio 2.3:1, aged 12 hours to 28 days (mean, 8 +/- 5.1 days), and weighing 1.8 to 4.9 kg (mean, 2.7 +/- 0.5 kg). Paracetamol, pentazocine, pethidine, fentanyl, tramadol, and breast milk/glucose drinks were common analgesics and pacifiers used, and morphine, meperidine, alfentanil, and ketorolac were rarely used during the period. Opioids, especially pentazocine, produced satisfactory analgesia but were associated with life-threatening morbidities and mortalities, chiefly due to respiratory depression compounded by nonavailability of pediatric ventilator ( P < 0.0001). Excessive sedation, apnea, and mucous/vomiting were other complications. Nonsteroidal anti-inflammatory agents, particularly tramadol, had excellent analgesia with no significant complication. Overall, 18 (4.9%) deaths were recorded, 15 (83.3%) of them following pentazocine use. Many analgesics relieved pain but most were unsafe; cautious selection is important where there may be no adequate facilities.
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PMID:Safety profile and efficacy of commonly used analgesics in surgical neonates in Benin City, Nigeria. 1884 87


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