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

The role of the coxibs in the management of osteoarthritis and rheumatoid arthritis has been widely discussed, but there are other potential applications for the coxibs that have received less attention. Here we consider the use of the coxibs in acute pain syndromes such as primary dysmenorrhea and the pain associated with dental extraction, as well as considering their application in chronic low back pain and cancer pain. Another area where the coxibs may prove particularly beneficial is in the management of post-surgical pain. Traditional post-surgical analgesia has involved the use of non-selective NSAIDs and opioids, but these agents can be associated with side effects such as post-operative bleeding, gastrointestinal problems, nausea, and constipation. Because the coxibs do not inhibit COX-1 dependent platelet aggregation like traditional NSAIDs, the risk of post-surgical bleeding is reduced. The careful application of coxibs as part of a multi-modal approach to pain management in the perioperative period can reduce the requirement for opioid medications and thus reduce the risk of post-operative complications such as ileus. In the future, coxibs are likely to play an important role in multi-modal perioperative analgesic regimens with the aim of reducing post-operative periods of convalescence.
 ...
PMID:Strategies in pain management: new and potential indications for COX-2 specific inhibitors. 1260 54

Long-term administration of morphine for the treatment of chronic pain produces constipation; this requires the use of laxatives, which impair water absorption and upset the electrolyte balance. Morphine-induced constipation is mainly due to inhibition of the propulsive movement of the gastrointestinal tract combined with spastic contraction of smooth circular muscles as a result of drug binding to opioid receptors in the tract. Since papaverine lacks affinity for opioid receptors but relaxes smooth muscle, it seemed possible that oral papaverine might be capable of diminishing constipation without impairing the analgesia achieved with morphine. For this purpose, experiments were carried out on rats: constipation was checked for by measuring the intestinal transit time, and analgesia was assessed by measuring the latency of the tail-flick response to radiant heat or nociceptive activity in single neurons of the thalamus evoked by supramaximal electrical stimulation of afferent C fibres in the sural nerve. Morphine and papaverine were administered by the oral route. Control animals received saline. To measure the intestinal transit time, India ink solution was given orally. Morphine (2.5 and 5 mg/kg orally) prolonged the transit time from approx. 420 min in the controls to more than 600 min, a dose of 2.5 mg/kg producing the maximum effect. Papaverine (0.5, 1, and 2 mg/kg) administered orally together with morphine significantly reduced morphine-induced constipation (Tables 1, 2). Papaverine given alone at a dose of 2 mg/kg caused no change in transit time, while 5 mg/kg significantly increased it (Table 2). The latency of the tail-flick response was increased by oral morphine (2.5 and 5 mg/kg) at 1, 2, and 3 h after administration. Papaverine (0.5, 1 and 2 mg/kg) given in combination with morphine left the antinociceptive effect of morphine unchanged (Figs. 1-3). A study of the nociceptive activity evoked in thalamus neurons of rats under urethane anaesthesia indicated that intestinal absorption of morphine was blocked. Therefore, metoclopramide (0.15 mg/kg) was injected i. v. 10 min before oral administration of morphine or the combination of morphine plus papaverine. Subsequently, morphine produced a dose-dependent depression of evoked nociceptive activity (Fig. 4), the mean effect amounting to 60 % of the control activity and being produced by 2.5 mg/kg (Fig. 5). Since in former experiments on nociceptive activity evoked in thalamus neurones it has been found that the ED(50) of i. v. morphine is 0.05 mg/kg, it is very likely that the presystemic elimination of orally administered morphine is very high and, in addition, that the efficiency of its active metabolite, morphine-6-glucuronide, is rather poor. When morphine 2.5 mg/kg was given together with papaverine 0.5 mg/kg, and morphine 5 mg/kg was administered in combination with papaverine 2 mg/kg, there was no significant reduction in the depressant effect of morphine on nociceptive activity evoked in thalamus neurons (Figs. 6, 7). The results suggest that papaverine given by the oral route may reduce morphine-induced constipation without impairment of the analgesic action of morphine in patients suffering from pain.
 ...
PMID:[Oral papaverine prevents morphine-induced constipation without interfering with analgesia achieved with oral morphine]. 1279 74

In paediatric oncology, optimal pain control is still a challenge.A structured pain history and the regular scoring of pain intensity using age-adapted measuring tools are hallmarks of optimal pain control. Psychological measures are as important as drug therapy in prophylaxis or control of pain, especially when performing invasive procedures. Pain control is oriented on the WHO analgesic ladder. On no account the paediatric patient should have to climb up the 'analgesic ladder'- strong pain requires the primary use of strong drugs. Opioids should be given by the oral route and by the clock - short acting opioids should be used to treat break-through pain. Alternatives are IV infusion and patient-controlled analgesia. Constipation is the adverse effect most often seen with (oral) opioid therapy. Adverse effects should be anticipated, and prophylactic treatment should be given consistently. The assistance of paediatric nurses is of utmost importance in paediatric pain control. Nurses' deliver the basis for rational and effective pain control by scoring pain intensity and documenting drug administration as well as adverse effects. The nurses task is also to prepare the patient for and monitor the patient during painful procedures. It is the responsibility of both nurse and doctor to guarantee emergency intervention during sedation whenever needed. In our paper we comment on drug selection and dosage, pain measurement tools, and documentation tools for the purpose of pain control. Those tools may be easily integrated into daily routine.
 ...
PMID:[Practice of pain control in paediatric oncology--recommendations of the quality-monitoring group of the German Society for Paediatric Oncology and Haematology (GPOH)]. 1279 36

Institutions with quality management programs need to evaluate the quality of perioperative pain management as well as other aspects of the health service. With the development of anesthesia-based pain services, improvement in this field has been reported. In this prospective study performed in a university hospital, we used a Postoperative Pain Therapy Assessment Questionnaire to quantify the effectiveness of pain therapy and factors affecting the degree of satisfaction and also to pinpoint areas that need improvement. A total of 915 patients who received patient-controlled analgesia for postoperative pain were included in the study; it seems to be the largest patient population from a single hospital. Data were collected as part of the hospital's quality improvement activities. By analyzing the questionnaires, we found that patients were satisfied with the pain therapy performed under the guidance of anesthesiologists, but predictors of satisfaction such as pain intensity and side effects (nausea, vomiting, constipation and difficulty in walking) decreased patient satisfaction considerably. Patients are aware of the fact that health care givers take postoperative care seriously and they do not want any untoward effects interrupting their postoperative care. They are trying to participate in the decision making and also to learn more about pain medicine.
 ...
PMID:Evaluation of quality in patient-controlled analgesia provided by an acute pain service. 1280 98

Patients with moderate to severe pain were treated with buprenorphine patches in one of 3 concentrations: 35 micrograms/h, 52.5 micrograms/h and 70 micrograms/h (= 0.8 mg/d, 1.2 mg/d and 1.6 mg/d respectively). The aim of this review was to assess the efficacy and tolerability of this transdermal system (TDS) in patients with chronic pain. A total of 445 patients were included in 3 double-blinded studies. The dosage titration with buprenorphine patches followed pretreatment with buprenorphine sublingual tablets, higher doses of weak opioids (level 2 substances), low dose morphine (level 3) or other analgesics. Patients with chronic tumour or non-tumour pain were recruited for these studies and treated with buprenorphine patches or placebo for 6 to 15 days. All patients were offered, in addition, buprenorphine sublingual tablets to be taken as required for supplementary pain relief. Pain intensity, analgesia, consumption of buprenorphine sublingual tablets and sleep duration were all assessed. All patients in the double-blinded studies were between the ages of 22 and 88. 249 patients suffered from tumour pain and 196 patients suffered from non-tumour pain. To examine long-term efficacy and tolerability of the transdermal system, treatment was expanded, if the patients were interested in participating in an open-label-study. In all 3 studies, the number of patients with moderate, severe and very severe pain increased in the placebo-patch treated group, while the patients in the buprenorphine transdermal system treated group had a greater incidence of mild or no pain. A further benefit in the buprenorphine transdermal system treated group was evidenced by a great number of patients with a daily sleep duration of more than 6 hours compared to the placebo group--an indicator of greater well-being. The systemic side-effects were typically opioid in nature and rare and usually only mild. Of particular note was the very low incidence of constipation in only 5.3% of cases. Dermatological reactions to the patches were only rarely encountered. The dermatological reactions consisted mainly of erythema and pruritus with a mild to moderate extent. Half the cases of erythema and more than on third of the cases of pruritus were spontaneously reversible. More than half the patients (53.7%) in the double blind studies wished to continued treatment with buprenorphine transdermal system. These results demonstrate that buprenorphine patches achieved a very good analgesic effect in all 3 studies and that in particular with respect to the quality of life of the patient these patches offer an exceptional alternative to other conventional therapies.
 ...
PMID:[Transdermal buprenorphine for treatment of chronic tumor and non-tumor pain]. 1292 8

The purpose of the present study was to determine the value of circular hemorrhoidectomy (procedure for prolapse and hemorrhoids [PPH]) on the basis of data collected prospectively during the initial experience of a group of Latin American surgeons. Between 2000 and 2001, PPH was performed using a circular stapler in 177 patients who had third- and fourth-degree hemorrhoidal disease. The average age of the patients was 47.7 years (range 26 to 85 years). Anal bleeding was the most common preoperative complaint (93.2%) followed by anal pain (60.2%), anal itching (43%), and constipation (41%). Hemorrhoids were classified as third degree in 132 patients (74%) and fourth degree in 45 patients (25.4%). Skin tags were detected in 86 patients (48.8%) and rectocele in 14 patients (7.9%). Data collected included patient demographics, type of anesthesia, and specific details of the surgery such as duration of the operation, distance from the staple line to the dentate line, need for complementary hemostasis, and any unexpected occurrences. Postoperative data collected included the degree of pain, which was evaluated on the basis of the type and dosage of analgesics required, laxative consumption, and the presence of bleeding, fever, urinary retention, or hematomas. Each patient completed a written questionnaire addressing these events. Patients returned for follow-up visits on days 7, 15, 30, and 90. Responses to pain, bleeding, fever, anal continence, recurrence of hemorrhoids, and level of satisfaction were compiled. The duration of the procedure ranged from 6 minutes to 2 hours (average 23 minutes), and most operations lasted no more than 20 minutes, with the exception of one that lasted 2 hours because of intraoperative bleeding. Intraoperative problems were minor. An additional one or a few sutures were required in 58.7% of patients to achieve perfect hemostasis. In 128 patients (72.3%) the hospital stay was less than 24 hours. Same-day surgery was chosen for 37 patients (20.9%). Pain was controlled with analgesia only using one to six doses of oral dipirona in 126 patients. Five patients were readmitted to the hospital: four for control of bleeding and one for conventional hemorrhoidectomy due to an acute episode of external hemorrhoidal thrombosis. At day 30, patients rated the efficacy of the procedure in alleviating preoperative symptoms as follows: 77.5% excellent; 16% good; 5.3% average, and 1.2% poor. At 3 months postoperatively no patient had had a recurrence of hemorrhoidal prolapse, and there were no instances of stenosis or anal incontinence. Surgeons also rated the efficacy of the procedure as excellent in 75%, good in 19.8%, average in 4.7%, and poor in 0.6%. With proper selection of patients and adequate stapling technique, stapled hemorrhoidectomy may be considered safe; it is easily learned, has a satisfactory degree of pain, and is well accepted by both patients and surgeons.
 ...
PMID:Stapled hemorrhoidectomy: initial experience of a Latin American group. 1312 62

Opioid abuse has been postulated as a cofactor in the immunopathogenesis of human immunodeficiency virus (HIV) infection and AIDS. We and others have recently demonstrated that opioid enhances HIV infection of human macrophages through modulation of beta-chemokines and the CCR5 receptor and that this effect is reversed by naltrexone, a tertiary opioid antagonist. Tertiary opioid antagonists cannot be used in opioid-dependent patients because they precipitate withdrawal or reversal of analgesia. We determined whether the quaternary opioid antagonist methylnaltrexone (MNTX), now in phase III clinical trials for opioid-induced constipation, reverses the opioid-mediated enhancement of HIV infection of macrophages at clinically relevant doses. MNTX completely abrogated morphine-induced HIV Bal strain infection of macrophages. MNTX also inhibited the R5 strain (ADA) envelope-pseudotyped HIV replication induced by morphine. Furthermore, MNTX abolished morphine-mediated up-regulation of CCR5 receptor expression. The ability of MNTX to block opioid-induced CCR5 expression and HIV replication at clinically relevant doses may have additional benefit for opioid abusers with HIV infection, or patients with AIDS pain receiving opioids.
 ...
PMID:Methylnaltrexone antagonizes opioid-mediated enhancement of HIV infection of human blood mononuclear phagocytes. 1456 41

Transdermal fentanyl is effective and well tolerated for the treatment of chronic pain caused by malignancy and non-malignant conditions when administered according to the manufacturer's recommendations. Compared with oral opioids, the advantages of transdermal fentanyl include a lower incidence and impact of adverse effects (constipation, nausea and vomiting, and daytime drowsiness), a higher degree of patient satisfaction, improved quality of life, improved convenience and compliance resulting from administration every 72 hours, and decreased use of rescue medication. Transdermal fentanyl is a useful analgesic for cancer patients who are unable to swallow or have gastrointestinal problems. Transdermal fentanyl forms a depot within the upper skin layers before entering the microcirculation. Therapeutic blood levels are attained 12-16 hours after patch application and decrease slowly with a half-life of 16-22 hours following removal. Patients with chronic pain should be titrated to adequate relief with short-acting oral or parenteral opioids prior to the initiation of transdermal fentanyl in order to prevent exacerbations of pain or opioid-related adverse effects. Transdermal fentanyl can then be initiated based on the 24-hour opioid requirement once adequate analgesia has been achieved. The prolonged elimination of transdermal fentanyl can become problematic if patients develop opioid-related adverse effects, especially hypoventilation. Adverse effects do not improve immediately after patch removal and may take many hours to resolve. Patients who experience opioid-related toxicity associated with respiratory depression should be treated immediately with an opioid antagonist such as naloxone and closely monitored for at least 24 hours. Because of the short half-life of naloxone, sequential doses or a continuous infusion of the opioid antagonist may be necessary. Transdermal fentanyl should be administered cautiously to patients with pre-existing conditions such as emphysema that may predispose them to the development of hypoventilation. Transdermal fentanyl is indicated only for patients who require continuous opioid administration for the treatment of chronic pain that cannot be managed with other medications. It is contraindicated in the management of acute and postoperative pain, as pain may decrease more rapidly in these circumstances than fentanyl blood levels can be adjusted, leading to the development of life-threatening hypoventilation. Cognitive and physical impairments such as confusion and abnormal co-ordination can occur with transdermal fentanyl. Therefore, patients should be instructed to refrain from driving or operating machinery immediately following the initiation of transdermal fentanyl, or after any dosage increase. Patients may resume such activities once the absence of these potential adverse effects is documented.
 ...
PMID:Benefit-risk assessment of transdermal fentanyl for the treatment of chronic pain. 1458 70

The inhibitory effect of repetitiously administered loperamide, a peripheral mu-opioid receptor agonist and well-recognized antidiarrheal agent, on mouse gastrointestinal transit was compared with that of morphine in order to examine the development of tolerance to mu-opioid receptor agonist-induced constipation (antitransit effect). When administered subcutaneously 15 min before the oral injection of charcoal meal, loperamide (0.1-30 mg/kg) and morphine (1-8 mg/kg) dose-dependently and significantly inhibited gastrointestinal transit of charcoal with the ID(50) values of 1.6 (0.3-7.1) mg/kg and 3.6 (1.5-8.5) mg/kg, respectively. When loperamide (30 mg/kg) was administered twice daily for 2 days, the antitransit effect was significantly reduced. On the other hand, morphine did not develop tolerance in even more severe conditions than those of loperamide. It is known that P-glycoprotein, an ATP-dependent drug efflux pump, is involved in the development of tolerance to morphine analgesia. The tolerance observed with loperamide was significantly prevented by cyclosporin (30 mg/kg, i.p.), a P-glycoprotein inhibitor, thus the ID(50) value in loperamide-tolerant mice was markedly reduced from >1000 mg/kg to 40 (2.7-603.0) mg/kg by cyclosporin. These results indicate that loperamide, different from morphine, readily develops tolerance to the inhibitory effect on mouse gastrointestinal transit, and the P-glycoprotein may be involved in the development of tolerance to the antitransit effect of loperamide.
 ...
PMID:Development of tolerance to the inhibitory effect of loperamide on gastrointestinal transit in mice. 1459 2

Some recent literature relevant to analgesia in palliative care is reviewed. Reports on clinical use of bisphosphonates for bone pain in cancer, controlled release opioids, selection of laxatives for opioid-induced constipation and the calcium channel blocker nifedipine as an analgesic are described.
 ...
PMID:Analgesia issues in palliative care: bone pain, controlled release opioids, managing opioid-induced constipation and nifedipine as an analgesic. 1465 Apr 52


<< Previous 1 2 3 4 5 6 7 8 9 10 Next >>