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At least 973 records · Page 54Linked to original sources
PubMed1995

Non-competitive antagonism of N-methyl-D-aspartate receptor inhibits tolerance to the analgesic action of U-50,488H, a kappa-opiate receptor agonist in the rat.

1. The effect of dizocilpine (MK-801), a non-competitive inhibitor of N-methyl-D-aspartate (NMDA) receptor on the development of tolerance to the analgesic and hypothermic actions of U-50,488H, a highly selective kappa-opiate receptor agonist, was determined in the rat. 2. Male Sprague-Dawley rats were made tolerant to the pharmacological actions of U-50,488H by twice daily intraperitoneal (i.p.) injections of the drug (25 mg/kg) for 4 days. 3. Multiple injections of U-50,488H resulted in the development of tolerance to its analgesic and hypothermic actions in the rat. MK-801 injected 10 min before each injection of U-50,488H, dose-dependently inhibited the development of tolerance to the analgesic action but the tolerance to the hypothermic action of U-50,488H was unaffected. 4. Multiple injections of U-50,488H decreased the body weight gain. MK-801 dose-dependently decreased the gain in body weight further. 5. The results indicate that non-competitive antagonism of the NMDA receptor by MK-801 can selectively inhibit the tolerance to the analgesic action of U-50,488H in the rat, however, such an effect was associated with significant decreases in normal gain in body weight.

3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cycloh↗
PubMed1987

The clinical usefulness of agonist-antagonistic opioid analgesics in chronic pain.

The mixed agonist-antagonist analgesics do not have a major role in the treatment of chronic pain. Pentazocine, the first and most widely used of this group of drugs has two major limitations: by mouth it is not a strong analgesic, but is closer in efficacy to the peripherally acting drugs aspirin and paracetamol than the weak opioids; and its use is associated with psychotomimetic side effects in 10-20 percent of patients. The weak opioid analgesics codeine and dextropropoxyphene are more effective and better tolerated than pentazocine. Buprenorphine is the most useful of the agonist-antagonists in chronic pain patients. It is potent, long-acting (6-9 h) and effective when given sublingually. However, it has a limited effective dose range and produces the same side effects as morphine-like drugs, possibly more frequently at equianalgesic doses. It may be used in the treatment of cancer pain, or in patients with chronic arthritides or other forms of chronic non-cancer pain who require a potent conventional analgesic, as an alternative to the weak opioids or to morphine in low doses. Nalbuphine and butorphanol are only available for parenteral administration which means that their usefulness in the treatment of chronic pain is limited. Meptazinol is restricted by its manufacturers to 'short term' treatment and there is little information on its use in chronic pain patients.

Analgesics, Opioid↗
PubMed1995

Response of headaches to nonnarcotic analgesics resulting in missed intracranial hemorrhage.

The differential diagnosis of headache is broad, ranging from immediately life-threatening to benign etiologies. Currently, headaches can be treated successfully with various nonnarcotic analgesics. Three cases are presented in which patients with headaches were treated in an emergency department with nonnarcotic analgesics which relieved their headaches; subsequently, these patients returned to be diagnosed with intracranial hemorrhage. Some nonnarcotic analgesics may relieve symptoms of intracranial hemorrhage through their recognized mechanisms of action. Avoiding such occurrences requires that the diagnosis of headache be made with careful consideration of the patient's history. A patient presenting with a new onset of severe headache or a headache that is different from those experienced in the past deserves a thorough diagnostic work-up including a computed tomography scan followed by lumbar puncture if indicated. Diagnostic decisions regarding headache should not be based on a patient's response to any analgesic, nonnarcotic or narcotic.

Adult↗
PubMed1993

The Tromsø Study: frequency and predicting factors of analgesic drug use in a free-living population (12-56 years).

In a cross-sectional survey carried out in Tromsø in 1986-7, 19,137 men and women aged 12-56 years from the general population were asked about their use of drugs during the preceding 14 days. Use of analgesics was very common. On average 28% of the women and 13% of the men had used analgesics. Drug use due to menstruation discomfort contributed only partly to the gender difference. Drug use was independent of age from 20 years of age. Factors having an impact on analgesic drug use were analyzed by logistic regression. The most significant predictors of analgesic use were suffering from headache (OR = 14.2(women) OR = 24.4(men)) and infections (OR = 2.0(women) OR = 2.4(men)). Drug users also tended to suffer from symptoms of depression (women) and sleeplessness (men). Lifestyle and sociodemographic factors were also significant predictors, but were of marginal importance (OR < 1.5) compared with occurrence of pain and infections.

Adolescent↗
PubMed2005

Eliminating analgesic meperidine use with a supported formulary restriction.

PURPOSE: Meperidine is a commonly used analgesic despite unique disadvantages compared with other opioid analgesics. The objective of this study was to measure the effects of a meperidine formulary restriction on the prescribing of parenteral opioid analgesics. MATERIALS AND METHODS: The study was performed at a single 750-bed tertiary care teaching hospital in Rochester, NY. The formulary restriction limited meperidine to use exclusively for rigors or procedural sedation and was supported by an educational initiative and a computerized order entry system. Independent computerized pharmacy records were used to capture all doses of parenteral morphine, meperidine, and hydromorphone administered to patients in the emergency department or on a medical or surgical inpatient floor during data-collection periods. Baseline data were collected during two 3-day periods before the formulary restriction; then comparison data were collected during three 3-day periods over 15 months after the formulary restriction. RESULTS: The number of administered doses of meperidine per day decreased from 37.5 (20.8% of parenteral opioid doses before the restriction) to 0.22 (0.1% of parenteral opioid doses, P = .001). The total number of opioid doses and morphine doses given did not change, whereas the number of hydromorphone doses increased significantly postrestriction, from 16.0 doses per day (8.9% of total) to 59.7 doses per day (29.5%) (P = .009). CONCLUSION: Meperidine formulary restriction, supported by an educational program and computerized order entry, effectively eliminated analgesic meperidine use. Hydromorphone use increased proportionately to offset the decreased use of meperidine.

Analgesics, Opioid↗
PubMed2004

Variability in emergency physician decision making about prescribing opioid analgesics.

STUDY OBJECTIVE: The purpose of this study is to determine what factors influence emergency physicians' decisions to prescribe an opioid analgesic for 3 common, painful conditions. METHODS: We developed items thought to influence the decision to prescribe an opioid analgesic through a review of the literature, expert consultation, and interviews with practicing emergency physicians. We developed a baseline vignette and items expected to influence the decision for each of the 3 conditions: migraine, back pain, and ankle fracture. We surveyed 650 physicians randomly selected from the American College of Emergency Physicians. The influence of individual items was explored through a univariate analysis of the response distribution. Patterns were assessed by analytically creating scales. RESULTS: We received responses from 398 (63%) of the 634 eligible physicians. Physicians' likelihoods of prescribing an opioid showed marked variability, with at least 10% of physicians saying they were unlikely and 10% of physicians saying they were likely to prescribe for each condition. Physician responses to individual pieces of clinical information, such as the patient requesting "something strong" for the pain, were also highly variable, with at least 10% of physicians saying they would be negatively influenced by this request and at least 10% saying they would be positively influenced by it. CONCLUSION: Even when faced with identical case scenarios, physicians' decisions to prescribe opioid analgesics are highly variable. Moreover, the same clinical information, such as a patient requesting a strong analgesic, changes the likelihood of prescribing opioids in opposite directions for different physicians.

Analgesics, Opioid↗
PubMed2005

Role of analgesic adjuncts in postoperative pain management.

Postoperative pain remains a major problem. A multi-modal analgesic approach is recommended to optimize pain management and reduce opiate-related adverse effects. Several analgesic adjuncts have been investigated, and many have proved to have a useful analgesic effect. This article reviews the literature regarding use of analgesic adjuncts in the perioperative period.

Adrenal Cortex Hormones↗
PubMed2003

A fusion protein of conotoxin MVIIA and thioredoxin expressed in Escherichia coli has significant analgesic activity.

omega-Conotoxin MVIIA (CTX MVIIA) is a potent and selective blocker of the N-type voltage-sensitive calcium channel in neurons. Its analgesic and neuroprotective effects may prove useful in treatment of severe pains and ischemia. In this paper, we report that a fusion form of CTX MVIIA with thioredoxin (Trx) has analgesic function. The DNA fragments were chemically synthesized and ligated to form the DNA sequence encoding CTX MVIIA. The synthetic gene was then cloned into the expression vector pET-32a(+) and the fusion protein Trx-CTX MVIIA containing 6x His-tag was purified by one-step metal chelated affinity chromatography (MCAC). The purity of final product was over 95% determined by HPLC and the yield of the fusion protein was approximately 40 mg/L. The analgesic function was detected by using mouse hot-plate assay. After intracranially administering fusion protein with the dose of 0.6 mg/kg, marked analgesia was observed. The analgesic effects (elevated pain thresholds) were dose-dependent and the biological half-life of the fusion toxin was approximately 1.6 h.

Analgesics↗
PubMed2006

Preparation of 5-aryl-3-alkylthio-l,2,4-triazoles and corresponding sulfones with antiinflammatory-analgesic activity.

In this study, a series of 5-aryl-3-alkylthio-1,2,4-triazoles and corresponding sulfones were prepared with the objective of developing better analgesic-antiinflammatory compounds with minimum ulcerogenic risk. The structures of the compounds were elucidated by spectral and elemental analysis. The compounds were assayed per os in mice for their antiinflammatory and analgesic activity as well as the ulcerogenic risk and acute toxicity. Several of these compounds showed significant activity. Alkylsulfone derivatives were found to be much more potent analgesic-antiinflammatory agents than the corresponding alkylthio analogs. Compounds 9 and 11 were the most active of the series in both analgesic and antiinflammatory activity tests. In contrast to reference compound acetyl salicylic acid, these compounds did not induce gastric lesions in the stomach of experimental animals at the doses that exhibited analgesic/antiinflammatory activity.

Analgesics↗
PubMed2005

Interaction of mu-opioid receptor agonists and antagonists with the analgesic effect of buprenorphine in mice.

Buprenorphine is a potent opioid analgesic with partial agonistic properties at mu-opioid receptors. This study investigated the interaction potential with several full mu-agonists in the tail-flick test in mice. We further examined the reversibility of buprenorphine antinociception by different mu-opioid receptor antagonists. Combination of buprenorphine with morphine, oxycodone, hydromorphone and fentanyl in the analgesic dose range resulted in additive or synergistic effects. When given after the decline of the acute buprenorphine effect, both morphine and fentanyl also showed full efficacy. A moderate antagonistic effect according to the partial mu-agonistic properties of buprenorphine was only seen when high doses exceeding the therapeutic dose ranges were combined. Under these conditions antinociception of morphine was reduced to the effect of buprenorphine alone. Prophylactic administration of naloxone (10 mg/kg i.v.), naltrexone (1 mg/kg i.v.) and clocinnamox (5 mg/kg s.c.) fully and persistently blocked the antinociception of a high dose of buprenorphine. An established effect of buprenorphine was less sensitive, although repeated administration of naloxone induced complete antagonism, as did the irreversible antagonist clocinnamox under prophylactic and curative treatment conditions. Our results suggest that the antinociceptive effect of buprenorphine is mainly, if not exclusively, mediated by activation of mu-opioid receptors. They confirm clinical experience that in the analgesic dose range a switch between buprenorphine and full mu-agonists is possible without loss of analgesic efficacy and without a refractory period between the termination of buprenorphine analgesia and the onset of action of the new mu-opioid treatment. Antinociception of buprenorphine is sensitive towards mu-opioid receptor antagonists and incomplete inhibition can be improved by increasing the dose or repetitive dosing.

Analgesics, Opioid↗
PubMed2005

Synergistic affective analgesic interaction between delta-9-tetrahydrocannabinol and morphine.

Evidence for an analgesic interaction between delta-9-tetrahydrocannabinol (Delta(9)-THC) and morphine was sought using an experimental pain model applied to normal volunteers. The study incorporated a double blinded, four treatment, four period, four sequence, crossover design. Subjects received Delta(9)-THC 5 mg orally or placebo and 90 min later morphine 0.02 mg/kg intravenously or placebo. Fifteen minutes later subjects rated the pain associated with the application of thermal stimuli to skin using two visual analog scales, one for the sensory and one for the affective aspects of pain. Among sensory responses, neither morphine nor Delta(9)-THC had a significant effect at the doses used, and there was no significant interaction between the two. Among affective responses, although neither morphine nor Delta(9)-THC had a significant effect, there was a positive analgesic interaction between the two (p = 0.012), indicating that the combination had a synergistic affective analgesic effect. The surprisingly limited reported experimental experience in humans does not support a role for Delta(9)-THC as an analgesic or as an adjunct to cannabinoid analgesia, except for our finding of synergy limited to the affective component of pain. Comparison of our results with those of others suggests that extrapolation from experimental pain models to the clinic is not likely to be a straight-forward process. Future studies of Delta(9)-THC or other cannabinoids in combination with opiates should focus upon clinical rather than experimental pain.

Adolescent↗
PubMed2006

Specific down-regulation of spinal mu-opioid receptor and reduced analgesic effects of morphine in mice with postherpetic pain.

The analgesic effects of opioid agonists and the expression of mu- and kappa-opioid receptors were compared between mice with herpetic pain and those with postherpetic pain induced by herpetic virus inoculation. Morphine inhibited herpetic pain more effectively than postherpetic pain. Intrathecal injection reduced the analgesic effects of morphine on postherpetic pain, but intracerebroventricular injection did not. The kappa-opioid receptor agonist nalfurafine suppressed herpetic and postherpetic pain to similar degrees. mu-Opioid receptor-like immunoreactivities in the lumbar dorsal horn were markedly decreased at the postherpetic, but not herpetic, stage of pain. In the dorsal root ganglia, the expression of mu-opioid receptor mRNA was significantly decreased in mice with postherpetic pain, whereas the kappa-opioid receptor mRNA level was not altered. These results suggest that specific down-regulation of the mu-opioid receptor in the primary sensory neurons is responsible for the reduced analgesic action of morphine on postherpetic pain. The kappa-opioid receptor may be a useful target for the analgesic treatment of postherpetic neuralgia.

Analgesics, Opioid↗
PubMed2006

Local analgesic efficacy of tramadol following intraplantar injection.

Several studies have suggested that systemic tramadol, an opioid, can represent a valuable treatment in severe pain conditions because of their effects on central pain pathways. However, there are not enough studies supporting that tramadol is efficacious when administered locally. Therefore, we studied the potential local analgesic effects of tramadol in peripheral nociception. In addition, we tested the antinociceptive effects of tramadol-CaCl(2) or naloxone combinations after subcutaneous intraplantar injection in a validated rat model of acute thermal nociception. Local analgesic effects of tramadol were compared with those of lidocaine. The effects of tramadol on thermal paw withdrawal latencies were monitored using the plantar test. The antinociceptive potency of tramadol is higher and long-lasting than that of lidocaine. Naloxone was unable to inhibit the increased antinociceptive response produced by tramadol. Ca(2+) modified the effect of tramadol. When Ca(2+) dose was increased in the solution, thermal antinociceptive potency of tramadol, but not lidocaine was prolonged. Thermal nociceptive responses were not affected in the non-injected paws, indicating a lack of systemic effects with doses of tramadol and lidocaine that elicited local analgesia. These results suggest that intraplantar tramadol administration can produce local analgesic effect with a different action mechanism than that of lidocaine. In addition, extracellular Ca(2+) may play an important role in the local analgesic action of tramadol.

Analgesics, Opioid↗
PubMed2005

Analgesic potential of marrubiin derivatives, a bioactive diterpene present in Marrubium vulgare (Lamiaceae).

Marrubiin, a furane labdane diterpene, is the main analgesic compound present in Marrubium vulgare, a medicinal plant used in Brazil and other countries to treat several ailments. Considering its important pharmacological action, as well as its high yield, some structural modifications were performed in order to obtain more active compounds. Success was obtained in reducing the lactonic function, in the formation of marrubiinic acid and two esterified derivatives, which exhibited significant analgesic effect against the writhing test in mice. Marrubiinic acid showed better activity and excellent yield, and its analgesic effect was confirmed in other experimental models of pain in mice, suggesting its possible use as a model to obtain new and potent analgesic agents.

Analgesics↗
PubMed2005

Diagnosis of chronic pain caused by osteoarthritis and prescription of analgesics in patients with cognitive impairment.

OBJECTIVE: Evaluation of the ability to detect symptoms of osteoarthritis and prescription of analgesics in older adults with different degrees of cognitive impairment. SETTING AND PATIENTS: Patients consecutively admitted to a Geriatric Evaluation and Rehabilitation Unit (GERU) for disability due to orthopedic, neurological, or cardiopulmonary diseases, after a surgical intervention, or for behavioral disturbances of dementia. Subjects with a recent orthopedic intervention were excluded. Eight hundred eighty-eight patients were analyzed (mean age 78.4 +/- 7.2 years, 69.5% female) and divided into 4 groups according to cognitive impairment: severe (Mini-Mental State Examination, MMSE 0-12), moderate (MMSE 13-18), mild (MMSE 19-24), or absent (MMSE 25-30). METHODS: Patients underwent a geriatric multidimensional assessment; the diagnosis of musculoskeletal pain was based on patients' direct report, objective signs (inflammatory signs around the joints), and "pain behaviors" (reductions in activity, social withdrawal, self-protective maneuvers, increased alterations in facial expressions or body postures, observable displays of distress). Analgesic drugs were registered on discharge in subjects with symptomatic osteoarthritis. RESULTS: Of the patients admitted to GERU, 16.8% (n = 149) had osteoarthritis; this percentage is different according to cognitive impairment (MMSE 0-12: 1%, MMSE 13-18: 8%, MMSE 19-24: 17.4%, MMSE 24-30: 34.1%, P < .001). If patients admitted for osteoarthritis are excluded, the new diagnoses of pain due to osteoarthritis are 306 (41.4%), without differences between cognitive status groups. On discharge, analgesic drugs are prescribed to 28.8% of patients with symptomatic arthritis (n = 131); the percentage is lower in patients with severe cognitive impairment in comparison with subjects with better cognitive functions. CONCLUSION: There is a poor attention to chronic pain due to osteoarthritis in community-dwelling elders with cognitive impairment. In a rehabilitative setting, an accurate evaluation of objective signs allows the diagnosis of symptomatic osteoarthritis. However, the link between the diagnosis and the treatment is not direct, since the prescription of analgesics is lower in patients with a more severe cognitive impairment.

Activities of Daily Living↗
PubMed2005

The combination of epidural clonidine and S(+)-ketamine did not enhance analgesic efficacy beyond that for each individual drug in adult orthopedic surgery.

STUDY OBJECTIVES: To evaluate the benefit of epidural clonidine and S(+)-ketamine combination through the epidural route in adult orthopedic surgery. DESIGN: Randomized double-blinded study. SETTING: Teaching hospital. PATIENTS: Scheduled to undergo knee surgery, 56 American Society of Anesthesiologists physical status 1 and 2 adult patients. INTERVENTIONS: Patients were randomized to 1 of 4 groups to receive the combined epidural-intrathecal technique. A 10-mL epidural injection of either study drug or normal saline was first administered to all patients. Intrathecal anesthesia was performed with 15 mg of bupivacaine. The control group (CG) received epidural saline. The 0.1-mg/kg S(+)-ketamine epidural group received 0.1 mg/kg epidural S(+)-ketamine. The 0.5-microg/kg clonidine epidural group received 0.5 microg/kg epidural clonidine. The S(+)-ketamine/clonidine group received 0.1 mg/kg epidural S(+)-ketamine plus 0.5 microg/kg epidural clonidine. MEASUREMENTS AND MAIN RESULTS: Pain and adverse effects were evaluated by visual analog scale. Rescue analgesics were available to patients. The groups were demographically similar. Sensory level to pinprick, surgical and anesthetic time, and visual analog scale scores for pain at first rescue medication were similar among the groups. The time to first rescue analgesic (minute) was lowest in CG (P < .005). The CG required more rescue analgesics in 24 hours than any of the other groups (P < .0005). Patients who received either epidural clonidine, S(+)-ketamine, or both displayed similar analgesia. The frequency of adverse effects was similar among groups (P > .05). CONCLUSIONS: The association of epidural clonidine or S(+)-ketamine did not result in a greater analgesic effect in the model of acute postoperative pain studied, although the interaction of epidural clonidine and S(+)-ketamine is not attributable to sharing of a common second messenger system.

Adult↗
PubMed2003

Analgesic and anti-inflammatory effects of essential oils of Eucalyptus.

Many species of the genus Eucalyptus from the Myrtaceae family are used in Brazilian folk medicine for the treatment of various medical conditions such as cold, flue, fever, and bronchial infections. In the current investigation, we evaluated the analgesic and anti-inflammatory effects of essential oil extracts from three species of Eucalyptus employing various standard experimental test models. Using acetic acid-induced writhes in mice and hot plate thermal stimulation in rats, it was shown that the essential oils of Eucalyptus citriodora (EC), Eucalyptus tereticornis (ET), and Eucalyptus globulus (EG) induced analgesic effects in both models, suggesting peripheral and central actions. In addition, essential oil extracts from the three Eucalyptus species produced anti-inflammatory effects, as demonstrated by inhibition of rat paw edema induced by carrageenan and dextran, neutrophil migration into rat peritoneal cavities induced by carrageenan, and vascular permeability induced by carrageenan and histamine. However, no consistent results were observed for some of the parameters evaluated, both in terms of activities and dose-response relationships, reflecting the complex nature of the oil extracts and/or the assay systems used. Taken together, the data suggest that essential oil extracts of EC, ET, and EG possess central and peripheral analgesic effects as well as neutrophil-dependent and independent anti-inflammatory activities. These initial observations provide support for the reported use of the eucalyptus plant in Brazilian folk medicine. Further investigation is warranted for possible development of new classes of analgesic and anti-inflammatory drugs from components of the essential oils of the Eucalyptus species.

Analgesics↗
PubMed2006

Anti-inflammatory and analgesic activity of the topical preparation of Verbena officinalis L.

Verbena officinalis has traditionally been used in herbal medicine in Navarra, Spain, in the treatment of topical inflammation. Due to the anti-inflammatory activity of Verbena officinalis 50% methanolic extract in i.p. and topical administration, the effects of several formulations were prepared and studied using carrageenan-induced edema and formalin testing. Piroxicam gel and methyl salicylate ointment were studied as positive control for anti-inflammatory and analgesic activity, respectively. The edema inhibition of the preparations containing extract at the doses of 1-3% w/w were significantly different from the control group. The anti-inflammatory effect of VO-3% was similar to the effect of piroxicam gel 3 h after carrageenan injection. The analgesic activity of topical preparation with more than 2.5% w/w was observed in the early phase. This activity was observed in concentrations of more than 2% w/w in the late phase. The topical analgesic activity of the extract was less than the analgesic activity of methyl salicylate ointment.

Administration, Topical↗