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PubMed2004

Onset of analgesia and analgesic efficacy of tramadol/acetaminophen and codeine/acetaminophen/ibuprofen in acute postoperative pain: a single-center, single-dose, randomized, active-controlled, parallel-group study in a dental surgery pain model.

BACKGROUND: The combination of tramadol and acetaminophen has demonstrated good efficacy in various clinical pain models. However, there is a need for comparisons of the onset of analgesia and other measures of analgesic efficacy with this combination and other strong combination analgesics for the management of acute pain. OBJECTIVE: The goal of this study was to compare the time to onset of analgesia and other measures of analgesic efficacy with tramadol/acetaminophen 75/650 mg (Tr/Ac) and codeine/acetaminophen/ibuprofen 20/500/400 mg (Co/Ac/Ib) in the management of acute pain after oral surgery. METHODS: This was a single-center, single-dose, randomized, active-controlled, parallel-group study in healthy subjects who had undergone surgical extraction of > or =1 impacted third molar requiring bone removal. When patients reported at least moderate pain after dental surgery (score > or =5 on a 10-point scale), they were randomized to 1 of 2 treatment groups. The time to onset of analgesia was measured using a 2-stopwatch technique. The time to the onset of perceptible and meaningful pain relief, pain intensity, pain relief, patient's overall assessment, and adverse events were recorded for 6 hours after dosing. RESULTS: One hundred twenty-eight subjects participated in the study, 64 in each treatment group. The 2 groups were similar in terms of baseline pain severity and demographic characteristics (mean age, 23.7 and 23.4 years in the Tr/Ac and Co/Ac/Ib groups, respectively; mean body weight, 58.5 and 60.3 kg). The median times to the onset of perceptible pain relief were a respective 21.0 and 24.4 minutes, and the median times to the onset of meaningful pain relief were 56.4 and 57.3 minutes. Mean total pain relief and the sum of pain intensity difference were also similar in the early period after dosing (0-4 hours). However, between 4 and 6 hours, Co/Ac/Ib was associated with significant differences in both variables compared with Tr/Ac (P < 0.05). Although similar through the 4-hour assessment, mean pain intensity difference was significantly greater with Co/Ac/Ib at 5 to 6 hours. The proportion of patients assessing their assigned treatment as good or better was significantly greater with Co/Ac/Ib compared with Tr/Ac (P < 0.05). The safety profile of Tr/Ac was comparable to that of Co/Ac/Ib. CONCLUSIONS: In this small and selected group of subjects, the onset of analgesia and analgesic efficacy of Tr/Ac was comparable to that of Co/Ac/Ib. Tr/Ac provided rapid and effective analgesia for acute postoperative dental pain in this population.

Acetaminophen↗
PubMed2001

A depressant insect toxin with a novel analgesic effect from scorpion Buthus martensii Karsch.

A new peptide named BmK dITAP3 from scorpion Buthus martensii Karsch (BmK) has been identified to possess a dual bioactivity, a depressant neurotoxicity on insects and an analgesic effect on mice. The bioassays also showed that the peptide was definitely devoid of the neurotoxicity on mammals, which indicated that the analgesic effect of BmK dITAP3 could not be ascribed to the syndromic effects of a mammalian neurotoxicity. BmK dITAP3 exhibited 43.0% inhibition efficiency of the analgesic effect on mice at a dose of 5 mg/kg and the FPU value of 0.5 microg/body (approximately 30 mg) on the fly larvae. The pI value and the molecular mass determined by MALDI-TOF MS for dITAP3 were 6.5 and 6722.7, respectively. Its first 15 N-terminal residues were determined by Edman degradation, based on which the full amino acid sequence was deduced from the cDNA sequence encoding the peptide with 3'-RACE. Circular dichroism and sequence based prediction analyses showed dITAP3 may have a similar molecular scaffold as the most scorpion toxins but with features of the more beta structures and much less of alpha helix. The details of the purification, characterization and sequencing as well as the sequence comparison with other depressant insect toxins and the correlation between the analgesic effect and the insect toxicity will be reported and discussed, respectively.

Amino Acid Sequence↗
PubMed2003

Anti-analgesic activity of enterostatin (VPDPR) is mediated by corticosterone.

Although enterostatin (VPDPR) inhibited morphine-induced analgesia, it had no affinity for mu-opioid receptors. VPDPR administration was reported to elevate serum corticosterone levels. We found that corticosterone exhibited a similar anti-analgesic effect selective for mu-opioid. Furthermore, the anti-analgesic effect of VPDPR was inhibited by RU486, an antagonist for the glucocorticoid receptor. The anti-analgesic effect of VPDPR was not observed in adrenalectomized mice. These results suggest that the anti-analgesic activity of VPDPR is mediated by corticosterone released from the adrenal cortex.

Analgesics, Opioid↗
PubMed2000

Enhancement of cerebral cortical acetylcholine release by intraperitoneal acetic acid and its suppression by analgesics in freely moving rats.

Several lines of evidence suggest that central cholinergic neurons play a key role in the perception and control of pain. We investigated the effects of analgesics on the increase in central cholinergic activity and writhing responses elicited by i.p. injection of acetic acid. ACh efflux from the rat cerebral cortex and hippocampus was measured in the absence of a cholinesterase inhibitor using an in vivo microdialysis technique and a highly sensitive and specific radioimmunoassay. ACh efflux from the cerebral cortex was significantly increased during the first 30 min after acetic acid injection and then returned to the control levels. In contrast, acetic acid-induced writhing responses, indicative of the perception of pain, persisted for almost the entire 120 min observation period. No changes in ACh efflux were observed in the hippocampus. The centrally-acting analgesic morphine and the peripherally-acting analgesic indomethacin each completely abolished the enhanced cerebral cortical ACh efflux and the writhing, whereas diazepam, a muscle relaxant, selectively suppressed only the writhing. These results demonstrate that peripheral nociceptive stimulation transiently increases cholinergic activity in the cerebral cortex, but not in the hippocampus, and that analgesics suppress both the enhanced ACh efflux and the writhing induced by acetic acid.

Acetic Acid↗
PubMed1996

Nimodipine fails to enhance the analgesic effect of slow release morphine in the early phases of cancer pain treatment.

We assessed nimodipine's ability to increase the analgesic effect of morphine in 32 patients suffering from cancer pain in a double-blind, placebo controlled cross-over study. Morphine administration began a few days before the start of the study. The analgesic effects of two combinations were compared: morphine (M) plus placebo (P) and morphine plus 90 mg/24 h of nimodipine (N). The study lasted 8 days, including the wash-out period, and the following sequence of treatments was applied: M + P or M + N on days 1, 2 and 3; only M on days 4 and 5; and M + N or M + P on days 6, 7 and 8. Morphine dose was individualised according to the intensity of the patient's pain and the same dose was maintained throughout the study period. Analgesic response was evaluated using four 10 cm visual analogue scales of quantitative variables for pain intensity, pain relief, sleep quality and mood. A verbal rating of qualitative variables was also scored following validated descriptors of pain in the Spanish language. No significant statistical differences were found in analgesic effect between combined treatment with nimodipine or placebo, as measured on any of the scales. In order to take into account both the short duration of treatment (8 days), and nimodipine's pharmacokinetic characteristics (half-life of 6 h and steady state of 36 h), we compared treatment with nimodipine or placebo on the third day of use, at which time, likewise, there were no statistically significant differences on any of the scales. However, when the same statistical tests were used for comparison of results with pre-treatment baseline values, highly significant differences between mean scores on the scales for pain relief and pain intensity were found. Based on these negative results we conclude that nimodipine given orally at a dose of 30 mg every 8 h does not enhance analgesia when associated with morphine in the early phases of treatment for cancer pain. Our study also gives clear evidence of a placebo effect.

Administration, Oral↗
PubMed1999

Corticotropin-releasing-hormone lacks analgesic properties: an experimental study in humans, using non-inflammatory pain.

The antinociceptive potency of corticotropin-releasing-hormone (CRH) has been established in several animal studies in which both central and peripheral sites of action were considered. However, there have not yet been any experimental trials, besides one attempt using clinical dental pain demonstrating the potential analgesic properties of CRH in humans. For this reason, we studied the effect of CRH on experimental heat pain sensitivity in 18 healthy men, using a double-blind, cross-over and placebo-controlled design. A dose of 100 microg (i.v.) was chosen because of its well-known neuroendocrine effects in humans. The pain parameters assessed were, visual analog scale (VAS) ratings for pain intensity and pain unpleasantness, pain thresholds and scores for discrimination ability. To differentiate between a direct analgesic effect of CRH and indirect effects via evoked hormonal responses in the hypothalamic-pituitary-adrenocortical (HPA) system (beta-endorphin, ACTH, cortisol), CRH was applied with and without a pre-treatment with dexamethasone. In neither of the two conditions was there any systematic change in our pain parameters. This failure to find any evidence suggesting an analgesic action of CRH or of the subsequent hormones of the HPA system was obtained despite the fact that CRH produced clear neuroendocrine responses such as increases in the plasma concentration of beta-endorphin and cortisol. It is unclear whether the lack of analgesic action of CRH is due to its non-existence in humans, due to the use of a pain model which does not assess minute changes in pain sensitivity and does not trigger substantial inflammatory responses, or due to an insufficient dose of CRH.

Adult↗
PubMed1979

Self-administered nitrous oxide: an adjunct analgesic.

In a pilot study of 26 patients, a mixture of 50% nitrous oxide and 50% oxygen (N2O-O2) appeared to be an effective and safe analgesic for the incision and drainage of closed-space infections. The analgesic effect of N2O-O2, as measured by a Mean Analgesic Index, is augmented by both amnesic and dissociative effects, ie, patients remembered experiencing significantly less pain than they complained of during the procedure (p less than .01) and reported significantly more pain than they appeared to be having, as recorded by an observer (p less than .01). The patient's recollected pain, however, correlated well (r = .68) with the observer's assessment. Forty-two percent of patients had undergone a similar or identical procedure in the past without the benefit of N2O-O2 and made uniformly favorable comparative statement concerning the analgesic effect of the gas.

Abscess↗
PubMed2003

Anti-inflammatory and analgesic activity of Bouchea fluminensis.

Dried leaves extract from Bouchea fluminensis was assessed in anti-inflammatory (mouse paw edema) and analgesic models (acetic acid-induced writhings and hot plate). Oral pretreatment of animals with a crude mixture (IG) and a purified mixture of ursolic, oleanolic and micromeric acids (IG-59) at doses ranging from 1 to 30 mg/kg, significantly inhibited carrageenin-induced edema formation. At the same doses, IG and IG-59 also exhibited peripheral and central analgesic activity. It seems that B. fluminensis triterpenes develop their analgesic effect through central opioid receptors, due to the observation that naloxone reverted analgesic activity on the hot plate model.

Acetic Acid↗
PubMed2000

Preliminary studies on the analgesic activity of latex of Calotropris procera.

In this study we have evaluated the analgesic activity of dry latex (DL) of Calotropis procera. A single oral dose of DL ranging from 165 to 830 mg/kg produced a significant dose dependent analgesic effect against acetic acid induced writhings. The effect of DL at a dose of 415 mg/kg was more pronounced as compared to a 100 mg/kg oral dose of aspirin. On the other hand DL (830 mg/kg) produced marginal analgesia in a tail-flick model which was comparable to aspirin. The analgesic effect of DL was delayed by 1 h by naloxone at a dose of 0. 5 mg/kg, i.p., which completely blocked the analgesic effect of morphine (10 mg/kg, i.p.). However, the effect of aspirin was not blocked by naloxone. The 830 mg/kg oral dose of DL did not produce toxic effects in mice and the LD(50) was found to be 3 g/kg.

Acetic Acid↗
PubMed2001

Antiulcerogenic and analgesic effects of Maytenus aquifolium, Sorocea bomplandii and Zolernia ilicifolia.

Maytenus aquifolium (Celastraceae), Sorocea bomplandii (Moraceae) and Zolernia ilicifolia (Fabaceae) are native plants from the Tropical Atlantic Forest (Mata Atlântica, Brazil) known as "espinheira-santa". These plants are traditionally used as analgesic and antiulcerogenic medicine, with the same traditional uses of the true "espinheira-santa" (Maytenus ilicifolia, Celastraceae), an efficient antiulcerogenic agent. Pharmacological and toxicological studies with these plants have not been carried out. The purpose in this study was to evaluate the efficacy (analgesic and antiulcerogenic activities), safety (acute toxicity) and quality (phytochemical profile) of these three plants. The analgesic effect was analyzed by writhing and tail flick tests, while antiulcerogenic effect was performed through ulcer induction by ethanol and indomethacin/bethanecol assays. LD(50) and acute toxic effects, as well as phytochemical profiles of all plants also were carried. Surprisingly, the three plants showed analgesic and antiulcerogenic effects at dose of 1000 mg/kg, v.o. Maytenus aquifolium lowering all ulcerogenic parameters (ethanol test), but increased the ulcerogenic effects in the indomethacin/bethanecol test. Sorocea bomplandii produced antiulcerogenic effects in both experimental models used, while Zolernia ilicifolia showed significant effects only in indomethacin/bethanecol-induced gastric lesions. Pre-treatment with Zolernia ilicifolia induced someone toxic effects. A phytochemical profile for each plant species was determined and its main chemical classes of compounds were described.

Administration, Oral↗
PubMed1998

Analgesic effects of intra-articular morphine during and after knee arthroscopy: a comparison of two methods.

The objective of this study was to compare the analgesic effects of intra-articularly administered bupivacaine with bupivacaine/morphine during and after therapeutic knee arthroscopy. In a prospective, randomized study, 50 patients with clinical signs of medial meniscal injury were allocated to two groups, A and B. The patients in group A received 40 mL of 0.25% bupivacaine while the same dose of bupivacaine combined with 1 mg of morphine sulphate was administered in group B. Pain was estimated using the visual analogue scale (VAS) during surgery and at 2, 4, 6, and 24 hours after the operation was completed. Supplementary analgesic requirements were also registered, as well as the patients' overall rating of the entire procedure. The pain scores were significantly lower in Group B throughout the whole postoperative observation period. However, no significant differences were found between the two groups in terms of intraoperative pain scores, supplementary analgesic requirements, or the overall rating of the procedure. This study provides evidence that arthroscopic surgery can be performed in a safe manner after intra-articularly administered bupivacaine with or without low-dose morphine. The combination of low-dose morphine and bupivacaine did, however, produce a superior postoperative analgesic effect during the 24 hours following knee arthroscopy compared with bupivacaine alone.

Adult↗
PubMed2000

Physicians' knowledge and attitudes toward the use of analgesics for cancer pain management: a survey of two medical centers in Taiwan.

The purposes of this study were to examine the attitudes of physicians regarding the optimal use of analgesics for cancer pain management (CPM), to evaluate their knowledge and attitudes toward opioid prescribing, and to comprehend their perceptions of the barriers to optimal CPM. A survey was conducted on 356 physicians with cancer patient care responsibilities practicing in two medical centers in Taiwan. A total of 204 (57%) physicians responded, including internists (28%), surgeons (27%), oncologists (11%), anesthesiologists (10%), and other specialties (24%). The majority of physicians displayed significantly inadequate knowledge and negative attitudes toward the optimal use of analgesics and opioid prescribing. Multivariate analyses showed that the following six categories of physicians would be inclined to have inadequate knowledge of opioid prescribing: 1) those with perception of good medical school training in CPM, 2) those with perception of poor residency or fellowship training in CPM, 3) those with a medical specialty in surgery, medicine, or oncology (vs. anesthesiology), 4) those with limited clinical experience in cancer patient care (number of patients less than 30), 5) those with a limited aim of pain relief, and 6) those with an underestimation of analgesic effect. Additionally, physicians with inadequate knowledge of opioid prescribing and with hesitation to intervene earlier with maximal dose of analgesia would be inclined to have reluctant attitudes toward opioid prescribing. The most important barriers to optimal CPM identified by physicians themselves were physician-related problems, such as inadequate guidance from a pain specialist, inadequate knowledge of CPM, and inadequate pain assessment. The results of this study suggest that active analgesic education programs are urgently needed in Taiwan.

Adult↗
PubMed2003

Unique spirocyclopiperazinium salt I: synthesis and structure-activity relationship of spirocyclopiperazinium salts as analgesics.

Based on the structure of compound 3, two series of spirocyclopiperazinium derivatives 7a-n and 10a-h were synthesized and evaluated for their in vivo analgesic and sedative activities. Compounds 7f and 10c were discovered to exhibit excellent analgesic activity. Structure-activity relationships revealed that anion of the quaternary salt affected the analgesic and sedative activity significantly; the allyl group is a most effective group among the compounds 7a-n; the electron-released substitute on the aromatic ring is favorable to increase the analgesic activity.

Alkenes↗
PubMed2003

Unique spirocyclopiperazinium salt. Part 2: synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics.

Three series of spirocyclopiperazinium derivatives 5a-d, 6a-f and 17a-d were synthesized and evaluated for their in vivo analgesic activities. Compounds 5a, 17a and 17b exhibited excellent analgesic activity. Two important structure-activity relationships were observed from this study: (1) the quaternary ammonium functionality is a critical pharmacophore for analgesic activity; (2) it is important to adjust the lipophilic property of compounds to improve analgesic activity.

Analgesics↗
PubMed2001

N-(3-Acyloxy-2-benzylpropyl)-N'-(4-hydroxy-3-methoxybenzyl) thiourea derivatives as potent vanilloid receptor agonists and analgesics.

A series of N-(3-acyloxy-2-benzylpropyl)-N'-(4-hydroxy-3-methoxybenzyl) thiourea derivatives were investigated as vanilloid receptor ligands in an effort to discover a novel class of analgesics. The proposed pharmacophore model of resiniferatoxin. which includes the C20 homovanillic moiety, the C3-carbonyl and the orthoester phenyl ring as key pharmacophoric groups, was utilized as a guide for drug design. The compounds were synthesized after several steps from diethylmalonate and evaluated in vitro in a receptor binding assay and in a capsaicin-activated channel assay. Additional evaluation of analgesic activity, anti-inflammatory activity and pungency was conducted in animal models by the writhing test, the ear edema assay, and the eye-wiping test, respectively. Among the new compounds, 23 and 28 were found to be the most potent receptor agonists of the series with Ki values of 19 nM and 11 nM, respectively. Their strong in vitro potencies were also reflected by an excellent analgesic profile in animal tests with ED50 values of 0.5 microg kg for 23 and 1.0 microg/kg for 28. Relative to capsaicin these compounds appear to be ca. 600 and 300 times more potent. Both 23 and 28 were found to be less pungent than capsaicin based on the eye-wiping test. However, the compounds did not show significant anti-inflammatory activity. A molecular modeling study comparing the energy-minimized structures of resiniferatoxin and 35 demonstrated a good correlation in the spatial disposition of the corresponding key pharmacophores. The thioureas described in this investigation, which were designed as simplified resiniferatoxin surrogates, represent a novel class of potent vanilloid receptor agonists endowed with potent analgesic activity and reduced pungency.

Analgesics↗
PubMed2002

Analgesic effects of calcitonin.

The analgesic activity of salmon calcitonin (subcutaneous or intranasal) has been demonstrated in several prospective clinical trials, in patients suffering different painful skeletal conditions, including recent nontraumatic osteoporotic vertebral fractures. The mechanism of the analgesic effect of calcitonin is not clear. It is possible that specific binding sites for salmon calcitonin exist in the brain. Another explanation is that changes in descending serotonergic modification on the sensory transmission mediated by C afferents contribute to the analgesic effects of calcitonin on pain in osteoporotic patients. From the clinical point of use, the analgesic effect of calcitonin is beneficial throughout the whole period of medical treatment of osteoporotic patients. Salmon calcitonin in a daily dose of 100 IU subcutaneously or 200 IU intranasally reduces dramatically the back pain (p < 0.0005) after a recent osteoporotic vertebral fracture, and promotes the early mobility of patients. The finding that injectable or intranasally administered salmon calcitonin effectively controls severe pain in osteoporotic patients with a recent vertebral fracture, allowing them earlier mobility in combination with a reduction of the urinary hydroxyproline excretion, and a limitation of the considerable bone loss that may occur during prolonged bed rest, make this therapeutic scheme attractive.

Analgesics↗
PubMed2005

Post-craniotomy analgesia: current practices in British neurosurgical centres--a survey of post-craniotomy analgesic practices.

BACKGROUND AND OBJECTIVE: An evaluation of post-craniotomy analgesia within the University Hospital of Wales Neurosurgical Unit, Cardiff, found that many patients were experiencing moderate to severe pain post-craniotomy. It was therefore decided to undertake a nationwide survey of analgesic practices in order to establish best practice guidelines and benchmark with other units. METHOD: A postal questionnaire was sent to the senior nurse of every Neurosurgical Directorate within the UK inquiring about the current, standard analgesic practices for post-craniotomy patients in their unit. RESULTS: Completed replies were received from 23 of the 33 centres (70%). Intramuscular (i.m.) codeine phosphate was found to be the principal first-line analgesic used post-craniotomy. Only three centres used morphine as the first-line analgesic and only one centre used patient controlled analgesia routinely. The majority of centres (82%) used balanced analgesia. Pain assessments were only carried out in 57% of centres and no centre used a validated pain assessment tool specifically for dysphasic patients. CONCLUSIONS: Codeine phosphate continues to be the mainstay of post-craniotomy analgesia, however, it is proposed that patient controlled analgesia with morphine is an efficacious and safe alternative.

Analgesia↗
PubMed2005

Comparisons of analgesic effects of different doses of morphine and morphine plus methylprednisolone after knee surgery.

BACKGROUND: In this double-blind randomized study, the analgesic effects of morphine alone and with methylprednisolone were examined in 72 patients undergoing arthroscopic knee surgery. METHODS: At the end of arthroscopy, patients were allocated randomly to one of four groups to receive intra-articular administrations of saline, morphine 1 mg, morphine 5 mg or morphine 1 mg with methylprednisolone 40 mg. Preoperative and postoperative pain levels at rest and during movement (active flexion of the knee) were measured by a visual analogue scale (VAS). Postoperative analgesic requirements to alleviate pain were evaluated. RESULTS: Pain scores were significantly lower for the patients who received 5 mg morphine and 1 mg morphine with 40 mg methylprednisolone than for those who received saline or 1 mg morphine. This was accompanied by a decrease in the postoperative consumption of analgesics and prolongation of the duration of pain relief. CONCLUSIONS: This study confirms that the analgesic effect of morphine given intra-articularly is dose dependent and that combination of methylprednisolone with morphine has an additive effect on analgesia.

Adult↗