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[Clinical study of postoperative sedation in pediatric patients--effects of inhalation anesthetics and postoperative analgesics].

The effects of three different inhalation anesthetics (sevoflurane, isoflurane and halothane) delivered with oxygen and nitrous oxide during surgery and of postoperative analgesics on degree %% postoperative sedation immediately following removal of the tracheal tube, in the recovery room and thereafter in the surgical ward, were studied in 74 pediatric patients under 12 years of age. They underwent elective surgical procedures including repair of inguinal hernia, orchidopexy, tonsillectomy, repair of cleft lip and certain orthopedic procedures. The degree of postoperative sedation was assessed using a nine-point behavioral scale (sedation score) designed for the rating of postoperative pain in children. There were no significant differences in sedation score or frequency of use of postoperative analgesics at any time of assessment among the three inhalation anesthetics. Thirty-eight percent of the patients received analgesics such as diclofenac and acetaminophen suppositories, and intravenous pentazocine. There were no significant differences in sedation score between the group of patients who received analgesics and the group of those who did not, and many patients had satisfactory sedation scores in the surgical ward, suggesting that appropriate administration of postoperative analgesics is possible.

Analgesics↗

Analgesic potency of mu and kappa opioids after systemic administration in amphibians.

The relative analgesic potency of 11 opioid agents was assessed by using the acetic acid test in amphibians. Systemic administration of the mu agonists, fentanyl, levorphanol, methadone, morphine, meperidine and codeine; the partial mu agonist, buprenorphine; and the kappa agonists nalorphine, bremazocine, U50488 and CI-977 was made by s.c. injection into the dorsal lymph sac of the Northern grass frog, Rana pipiens. All agents produced a dose-dependent and long-lasting analgesia which persisted for at least 4 hr. The analgesic effects of single doses of each agent were significantly blocked or reduced by pretreatment with naltrexone. Systemic opioids produced log dose-response curves which yielded ED50 values ranging from 1.4 nmol/g for fentanyl to 320.9 nmol/g for nalorphine. Comparison of ED50 values gave a rank order of analgesic potency = fentanyl > CI-977 > levorphanol > U50488 > methadone > bremazocine > morphine > buprenorphine > meperidine > codeine > nalorphine. The relative analgesic potency of mu opioids in amphibians was significantly correlated with relative analgesic potency of these same agents obtained on the mouse writhing and hot plate tests. These data suggest that the amphibian model may serve as an adjunct or alternative model for the testing of opioid agents. Furthermore, given the inactivity of kappa opioids on rodent hot plate and tail-flick tests, the acetic acid test in amphibians may be especially well-suited for the assessment of opioid analgesia after administration of kappa-selective opioids.

Analgesics↗

Concerns about reporting pain and using analgesics. A comparison of persons with and without cancer.

Cancer pain is not adequately managed, and patients' reluctance to report pain and to use analgesics contribute to this problem. The Barriers Questionnaire (BQ) assesses eight patient concerns about reporting pain and using analgesics. This study was designed to determine (a) whether such concerns differ for persons who have cancer versus those who do not, (b) whether the BQ has test-retest reliability, and (c) whether concerns are related to reticence in reporting pain and using analgesics. Two groups, 53 adults with cancer and 40 without, completed the BQ twice at a 1-week interval. The BQ has eight subscales (e.g., concerns about addiction) and a total scale score (alpha = 0.89). There were no differences between persons with and without cancer on BQ total or subscale scores. Test-retest reliability of the total scale was r = 0.90, whereas the subscales showed r = 0.60-0.81. At Time 1, 16% said they hesitated to report pain, and 12% hesitated to use analgesics; at Time 2, 15% hesitated to report pain, and 10% hesitated to use analgesics. At Time 2, those who hesitated to report pain had higher BQ total scores than those who did not hesitate to report it (p < 0.05). We discuss the results of this study with respect to patient and public education.

Adult↗

[The anodyne action of narcotic analgesics and clofelin under increased atmospheric pressure].

Rat experiments have revealed that gradual increases in atmospheric pressure up to 1.1 MPa progressively alters the vocalization threshold in electrical stimulation of the tail root. Substitution of air for heliox (79.1% helium and 20.9% oxygen) leads to attenuation of the analgesic effect of hyperbarism. It is postulated that hyperbaric analgesia is due mainly to the elevated partial pressure of nitrogen. Morphine and promedol in doses of 2.5 mg/kg and clofeline in a dose of 0.1 mg failed to change analgesic effects when atmospheric pressure was increased up to 0.7 and 1.1 MPa. The analgesic effect of morphine and promedol in doses of 5 mg/kg and buprenorphine in a dose of 0.035 mg/kg under similar conditions increased during the whole period of isopression, while that of clofeline in a dose of 0.5 mg/kg increased only in the first few minutes of isopression. The analgesic action of morphoeceptine in a dose of 5 mg/kg decreased during isopression. The possible mechanisms of hyperbaric analgesia and the specific features of the analgesic action of different drugs at elevated atmospheric pressure are discussed.

Analgesics, Opioid↗

[The permissive action of glucocorticoid on the analgesic effect of kyotorphin and its analogue].

Kyotorphin (KTP) is an endogenous analgesic dipeptide which does not act on opiate receptors but may induce the release of endogenous opioid met-enkephalin. In order to investigate whether or not glucocorticoids have "permissive action" on KTP, hydrocortisone has been used to examine its action on the analgesic activities of KTP and its retro-isomer (riKTP) by employing thermal irradiation-tail flick method after intracerebroventricular injection. KTP and riKTP showed dose-dependent analgesic activity. Dose of KTP in the range of 6-24 mmol/L were effective, while the dose of riKTP at 6 mmol/L was shown to be ineffective. The analgesia of KTP was higher than that of riKTP. Hydrocortisone alone showed no significant analgesic effect. Linkers by connecting hydrocortisone with KTP or riKTP showed significantly higher analgesic effect compared with the corresponding dipeptides, not only in the duration of analgesia but also in potency. Solutions containing hydrocortisone and any one of the dipeptides exhibited the same effect as the linker. Pretreatment with sc naloxone (10 mg/kg) 15 min before icv of KTP or riKTP (24 mmol/L) could not block the analgesia. These findings implicate that: (1) Glucocorticoids have a permissive action on the analgesia of KTP and its retro-isomer. The glucocorticoids may exert its effects by acting on receptors in the membrane, and thus cause fast membrane effect. (2) KTP may also induce release of substances other than met-enkephalin to participate in the analgesia.

Analgesics↗

Effectiveness of notification and group education in modifying prescribing of regulated analgesics.

OBJECTIVE: To compare the effectiveness of group education and notification with that of notification alone in modifying prescribing of regulated analgesics. DESIGN: Randomized controlled trial conducted from Dec. 1, 1992, to Dec. 31, 1993. SETTING: Nonacademic primary care practices in British Columbia. PARTICIPANTS: Fifty-four physicians randomly selected from a group of 100 physicians who had written a number of prescriptions for regulated drugs more than than two standard deviations above the mean number of prescriptions written for such drugs in 1992. Any physician who was unable to participate was replaced from the original group of 100 before the study began. Five subjects did not complete the study and were not included in the analysis. INTERVENTIONS: Participants were randomly assigned to three groups: those in the first group received a written notification of excessive prescribing and attended a 1-day group-education activity, those in the second group received a written notification of excessive prescribing only and those in the third group were not subject to any intervention and were unaware that their prescribing had received special notice. OUTCOME MEASURE: Mean number of prescriptions for regulated analgesics issued per physician in the 6 months before and the 6 months after the interventions. RESULTS: Physicians in the group that attended the education intervention wrote, on average, 33% fewer prescriptions after the intervention, whereas physicians in the group that received only written notification wrote 25% fewer prescriptions, on average, after the intervention. No change in prescribing was shown in the control group. The differences in rates of prescribing of regulated analgesics between each intervention group and the control group were statistically significant (p < 0.01). The difference in the rate of prescribing between the two intervention groups was not significant. CONCLUSIONS: Group education and notification of prescriber status as well as notification alone significantly reduced prescribing of regulated analgesics. Hence, feedback on a physician's prescribing pattern may be a practical and less costly alternative to direct educational intervention in moderating the prescribing of regulated analgesics. The results do not, however, imply that notification is as effective as education in improving overall patient care. A follow-up study comparing the duration of the effect of the educational intervention with that of notification alone is warranted.

Analgesics↗

Research into analgesia by inhaling analgesic.

This article deals with analgesia by inhaling analgesic. According to Chinese medical theories, TCM analgesics were chosen from the literature and folk prescriptions screened and proved by analgesic tests on animals. A reasonable prescription was made up and the drug inhaled. Its analgesic effect was superior to that of dolantin injection (3 mg/kg body weight, intraperitoneal injection). Clinical trials showed its analgesic effect in 3-10 minutes and it lasted for more than 2 hours in over 70% of the cases for a total effective rate of 94.6%. The drug is absorbed quickly and acts directly on the nerve center. Its use is not addictive.

Administration, Inhalation↗

Ketamine potentiates analgesic effect of morphine in postoperative epidural pain control.

BACKGROUND AND OBJECTIVES: Ketamine is currently the only N-methyl-D-aspartate receptor channel blocker in clinical use. This study evaluated the analgesic efficacy of epidurally coadministered ketamine and morphine in postoperative pain control. METHODS: The patient population consisted of ASA class I and II patients undergoing major joint replacement. Epidural lidocaine was used as the primary anesthesia for the surgery. In phase I of the study, either ketamine (10-30 mg) or morphine (0.5-2 mg) was administered via epidural catheter immediately after surgery. This was done to evaluate the dose-response effect of these drugs when used for postoperative pain relief, and the results were applied to phase II of the study, in which all patients received ketamine pretreatment (total 30 mg) with each dose of lidocaine administered before and during surgery. Forty patients were randomly divided into four groups, each of which received one of three different pain control regimens mixed with 10 ml of saline: group B received 10 mg ketamine, group C 2 mg morphine, and group D 10 mg ketamine plus 0.5 mg morphine while the control group A received 10 mL of saline with no additive. The intensity of pain expressed by patients, as well as the number of intramuscular meperidine (1 mg/kg) injections administered and any side effects that may have occurred, were recorded. RESULTS: Ketamine produced no significant pain relief. A 2-mg morphine dose did produce significant analgesia but was accompanied by a high incidence of side effects. Co-administration of subanalgesic doses of ketamine, 10 mg and morphine, 0.5 mg, however, also produced a strong analgesic effect. CONCLUSIONS: Ketamine, although not itself an epidural analgesic agent, potentiates the analgesic effect of morphine, especially when administered as a pretreatment. The resulting lowered dosage of epidural morphine needed for postoperative pain relief reduces, in turn, the incidence of side effects. Pretreatment of patients with ketamine epidurally, followed by injections of combined morphine and ketamine could be a promising new analgesic regimen.

Aged↗

[Anti-inflammatory and analgesic actions of of long-chain phenyl substituted alpha-aminoketones].

The investigated phenyl substituted alpha-amino ketones have anti-inflammatory and analgesic activities as could be shown in animal models (rats and mice). The effectiveness depends on the length of the alkyl chain. After i.p. application the most active amino ketones are ten times more effective than acetyl salicylic acid, but the activity did not reach that of indomethacin. The effective analgesic dose is ten times lower than that for anti-inflammatory action. Including the results of the toxicity the analgesic efficiency of the amino ketones could be lead to substances with high analgesic activity. After oral administration only in high doses anti-inflammatory and analgesic effectivities were found. The structural analog keto group instead of the ester or amid group leads not to the expected increase in p.o. effectivity.

Analgesics↗

[Analgesics in the postoperative period of abdominal interventions. The Study Group on Postoperative Analgesia of the Spanish Society of Clinical Pharmacology].

BACKGROUND: Analgesics can avoid postoperative pain. The aim of this study was to evaluate their prescription after abdominal surgery. PATIENTS AND METHODS: Prospective study including patients who had undergone abdominal surgery in two hospitals in Barcelona, in 1993. Prescription and administration of analgesic drugs, and pain severity during the first 48 hours of the postoperative period were evaluated. RESULTS: One hundred and sixty-four patients (83 men) were included. The most frequently prescribed drugs were metamizol (111; 68%), pethidine (83, 51%), and diclofenac (44; 27%). A high percentage of analgesic prescriptions on an "as needed" basis was recorded. Administered doses were lower than those recommended, and lower than those prescribed. Fifty-three percent of patients suffered significant pain during the first day. CONCLUSION: A too low proportion of analgesic drugs is prescribed in a predetermined schedule, in contrast to "as needed" prescription. Opiate derivatives are underused. All analgesic drugs are prescribed at inadequate dosage. This prescription pattern is associated with a high prevalence of postoperative pain.

Abdomen↗

[Possible mechanism of the analgesic effect of interleukin-2 in central nervous system].

The monoclonal antibody against IL-2R (Tac) could not block the analgesic effect of IL-2, and IL-2 mutant that could not bind to beta subunit of IL-2 receptor still had capability of increasing the pain threshold of rats. All these facts suggest that the analgesic effect of IL-2 in CNS is not mediated through the IL-2 receptor, and that the immune and analgesic effects of IL-2 are mediated through different receptor mechanisms. It is suggested that there are common antigenic determinants and similar structure between IL-2 and endogenous opioid peptides (EOP). This implies that the analgesic effect of IL-2 might be mediated by interaction between IL-2 and opioid receptors in CNS. Using radioimmunoassay the contents of EOP of different nuclei were measured at different times after injecting IL-2 into the lateral ventricle of rats. The results suggested that the analgesic effect of IL-2 may be related to beta-EP and LEK in arcuate hypothalamic nucleus, paraventricular hypothalamic nucleus and locus ceruleus.

Analgesics, Non-Narcotic↗

[Response to treatment of chronic daily headache with analgesic abuse].

The overuse of analgesics in patients with chronic daily headache (CDH) perpetuates and worsens the headache. The aim of this study was to evaluate the clinical response to withdrawal of analgesics and to preventive treatment in a group of patients with CDH. Eighty-four patients who were taking daily symptomatic medications, and suffering from CDH were studied. Treatment consisted of withdrawal of daily symptomatic medications and prophylactic therapy. Improvement was considered when intensity and frequency of the headache were reduced more than 50%. After a 2-15 months follow-up, 57 of the 76 patients that continued in the study had improved. From these, 98% had reduced the consumption of analgesics below the figures considered as abuse and a 94% took the prophylactic medications correctly. After giving up the preventive treatment, 26% of the patient presented CDH and the 60% overuse again of analgesics. These results show that withdrawal of analgesics is necessary for improvement in patients with CDH, but the possibility of relapses is elevated. We think that there are other factors implicated in the development of CDH. We therefore believe that in order to avoid the relapses this group of patients need follow-up and preventive treatments during long periods of time.

Analgesics↗

Analgesic effect of interscalene block using low-dose bupivacaine for outpatient arthroscopic shoulder surgery.

BACKGROUND AND OBJECTIVES: Although interscalene brachial plexus block (ISBPB) is often used to provide anesthesia for arthroscopic shoulder surgery, its selective analgesic effect, provided by low-dose local anesthetic, has not been studied. We hypothesized that ISBPB using a low volume and low concentration of bupivacaine can provide effective postoperative analgesia for shoulder surgery without producing significant sensory or motor block elsewhere. METHODS: In this double-blind study, 30 outpatients scheduled to undergo shoulder arthroscopy were randomly assigned to receive either an ISBPB with 10 mL 0.125% bupivacaine with epinephrine 1:400,000 (n = 15) or 10 mL of normal saline (n = 15). The block was performed preoperative, prior to a standardized general anesthetic. Postoperative pain scores, imorphine and oral analgesic consumption, recovery profile, and patient satisfaction were recorded. RESULTS: In the ISBPB group, verbal analog pain scores within 120 minutes after surgery were lower, morphine consumption in the postanesthesia care unit was significantly lower (2.7+/-2.6 mg vs 9.5+/-5.2 mg), the time to postoperative administration of the first systemic or oral analgesic was significantly longer (141+/-182 minutes vs 13+/-10 minutes), the degree of motor and sensory block 120 minutes after surgery was minimal, time to reach hospital discharge criteria was earlier, and patient satisfaction with postoperative analgesia at 24-hour follow-up was greater. Thirty-three percent of the patients receiving ISBPB did not require any analgesic prior to hospital discharge. CONCLUSIONS: Interscalene brachial plexus block with low-dose bupivacaine is a useful and selective analgesic technique for outpatient shoulder arthroscopic surgery.

Adult↗

[Analgesic agents: comparative evaluation, mechanisms of action, prospects].

A classification of analgesics based on the localization and mechanisms of their action is proposed. Opioid analgesics are compared: opioid receptor agonists, agonists-antagonists, and partial agonists. Central-action nonopioid analgesics are listed: alpha 2-adrenomimetics, Na- and K-channel blockers, reverse monoamine neuronal capture inhibitors, stimulating amino acid antagonists, etc. Peripheral-action analgesics (cycloxygenase inhibitors) are described.

Analgesics↗

Analgesic use for headache treatment by schoolchildren of southern Brazil.

The importance of the use of analgesic medication for the symptomatic relief of pain has been underestimated in medical practice. The objective of this study was to determine the prevalence of tension-type and migraine-type headaches and the associated analgesic consumption for its treatment within elementary school students from Porto Alegre (Brazil). A systematic random sample of 538 students from 5th to 8th grades was produced to complete the cross-sectional delineation. Subjects were individually submitted to a structured interview on headache and to general physical and neurological examination. Lifetime prevalence for headaches was 93.3%, 82.9% of the students recalled having headaches during the last year and 31.4% reported headaches in the last week. The prevalence for headaches in the previous 24 h was 8.9%. There was a significant prevalence of headache in females. The prevalence of analgesic consumption was 84.1% throughout life, 85.7% in the last year, and 54% in the last 3 months. A significantly higher prevalence of headache medication consumption was also depicted for females. However, the small age differences within the sample did not appear to be an important factor in influencing analgesic use for headaches. Different agents composed the individual treatment of headaches, with predominant use of over-the-counter preparations. Acetylsalicylic acid, consumed by 58.3% of the children, was the drug most frequently used for both tension-type and migraine-type headache treatments. In spite of the verification that headache was very frequently experienced by the children composing this sample accompanied by a consequent use of analgesics, no medication abuse was diagnosed.

Journal Article↗

Synthesis and analgesic and anti-inflammatory activity of some new (6-acyl-2-benzoxazolinone and 6-acyl-2-benzothiazolinone derivatives with acetic acid and propanoic acid residues.

In this study for developing potent analgesic and anti-inflammatory compounds, we synthesized 6-acyl-2-benzoxazolinone and 6-acyl-2-benzothiazolinone derivatives with acetic acid and propanoic acid side chain, and performed preliminary screening of their in vivo analgesic and anti-inflammatory activities at a single dose of 100 mg/kg inmice by a p-benzoquinone-induced writhing test and a Carrageenaninduced hind paw edema model, respectively. We also determined their gastric ulceration effects in the tested animals. Propanoic acid derivatives were generally found to have higher analgesic and anti-inflammatory activities, and among them, 3-(6-benzoyl-2-benzothiazolinon-3-yl)propanoic acid (Compound 4 a) exhibited the highest analgesic and anti-inflammatory activity. However, all compounds showed lower anti-inflammatory effects than we observed for indomethacin at 10 mg/kg dose. Consequently, 6-acyl-2-benzoxazolinone/2-benzothiazolinones having propanoic acid side chain might lead to further studies for developing better candidates with potent analgesic and anti-inflammatory effects while acetic acid derivatives do not exhibit comparable satisfactory features.

Animals↗

Analgesic abuse in urological practice.

Thirty-three patients seen in a urological department had taken large doses of analgesic for prolonged periods of time. In 9 cases a diagnosis of pyramidal necrosis was established, while 4 other had pyelographic evidence of pyelonephritis, and analgesic abuse was probably an important aetiological factor in their renal condition. Analgesic nephropathy is easily overlooked unless patients are questioned routinely regarding their intake of analgesic. It is important to identify the group of patients without evidence of serious renal disease who are taking excessive quantities of analgesic and to urge them to abandon the practice.

Acute Kidney Injury↗

Tolerance to the analgesic, but not discriminative stimulus effects of morphine after brief social defeat in rats.

One of the most prominent consequences of defeat in a social confrontation is a long-lasting tolerance-like insensitivity to the analgesic effects of opiates, even when only small short-lived changes in nociception are detectable during the acute social stress. The present experiments examined (1) which kinds of social experiences lead to morphine tolerance, (2) whether or not the morphine tolerance in defeat-experienced rats extends from the analgesic effects to the discriminative stimulus and rate-decreasing effects of morphine, and (3) how long morphine tolerance lasts after a defeat experience. After five brief social confrontations including attack and threat by a resident rat leading to submission or defeat of the intruder, the latter exhibits marked tolerance to the analgesic effects of morphine, but not to the discriminative stimulus or behaviorally suppressive effects. Changes in social housing did not alter morphine's behavioral effects. Tolerance to the analgesic morphine effects was detected for 2 months after the defeat experience, whereas the discriminative stimulus and rate-decreasing effects were closely similar to those before defeat. This pattern was seen in animals for whom discriminative stimulus training with morphine was suspended after defeat as well as in those for whom it continued. In additional defeated and non-defeated animals, morphine's effects on the acoustic startle reflex was assessed. In contrast to the tail flick reflex to a noxious heat stimulus, the acoustic startle response remained unaffected by defeat experience or by morphine (up to 30 mg/kg). The long-lasting and large degree of tolerance after brief social defeat experiences appears to be limited to the analgesic effects of morphine.(ABSTRACT TRUNCATED AT 250 WORDS)

Acoustic Stimulation↗