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

Clonidine ((2-[2,6-dichlorophenyl]amino)-2-imidazoline) preferentially stimulates central alpha(2)-adrenoceptors, which leads to inhibition of sympathetic tone, resulting in a lowering of arterial pressure and of heart rate. Additionally, many other desirable and undesirable effects are described, including analgesia, sedation and withdrawal reactions, which consist of a sudden rise in arterial pressure, nervousness, agitation and increased heart rate. The present study has the goal to develop a simple and effective method for the analysis of trace amounts of clonidine in human blood serum. Special emphasis is necessary to make application of electron impact ionization and separation of the analyte fragments in a quadruple mass analyzer suitable. The procedure comprises solid phase extraction followed by formation of the pentafluorobenzyl derivative. Further purification is achieved by phase transfer extraction into an acidic aqueous solution succeeded by re-extraction into dichloromethane. After solvent exchange, an aliquot is injected into the gas chromatograph equipped with a DB5 MS capillary column and a mass spectrometric detector. Chromatograms are recorded in single ion monitoring mode. Quantification is accomplished by internal standardization with moxonidine [4-chloro-5-(2-imidazolin-2-yl-amino)-6-methoxy-2-methylpyridine].
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PMID:Determination and quantification of clonidine in human blood serum. 1240 95

Preclinical studies suggest that visceral afferents constitutively express kappa-opioid receptors (KORs) and that noxious visceral stimuli can be inhibited at a peripheral site by KOR activation. To test the relevance of these observations to humans, we infused, in a randomized, double blind manner, a peripherally selective KOR agonist (ADL 10-0101) or placebo into six patients with chronic pancreatitis and ongoing abdominal pain despite mu-opioid agonist therapy. Pain was assessed using a pain magnitude estimate, an open ended scale of each patient's choosing and compared to their rating of pain from a 1.6 cm(2) thermode applied to the skin and heated to 49 degrees C for 5s. Normalizing pain scores to this rating as 100, pain prior to study drug treatment was 4070, and was unaffected by placebo infusion in the two individuals receiving this therapy. In contrast, ADL 10-0101 infusion reduced pain score from 63+/-7.6 (mean+/-SE) prior to infusion to 23+/-15 4h after infusion (P<0.05 vs. baseline). One patient receiving placebo and one receiving ADL 10-0101 experienced a mild headache during the study. One patient receiving ADL 10-0101 experienced restlessness and another had assymptomatic transient dysrhythmia upon standing after the 4h study. Neither of the treatments affected blood pressure, heart rate, respiratory rate, or oxyhemoglobin saturation, and no patient experienced nausea during the study. These limited data support the hypothesis that human visceral afferents express KOR and that peripherally restricted KOR agonists produce analgesia in patients with chronic visceral pain.
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PMID:Analgesia from a peripherally active kappa-opioid receptor agonist in patients with chronic pancreatitis. 1250 3

Since venous cannulation in children has become easier and extensive experience has been gained with total intravenous anaesthesia (TIVA) in adults, the interest in TIVA for children has recently increased. An intensified sensitivity of the operating room atmosphere to contamination with volatile anaesthetic agents is another important reason to choose intravenous techniques for paediatric anaesthesia. One of the most interesting agents for TIVA in paediatric anaesthesia is propofol. The pharmacokinetic and pharmacodynamic data for modern intravenous drugs is poor. Because the interpatient variability is relatively large, pharmacokinetic data can only provide guidelines for the dosage of propofol. Propofol has a rapid and smooth onset of action and is as easy to titrate in children as in adults. Propofol can be excellently controlled. Severe haemodynamic side-effects are missing in healthy children and plasma is cleared rapidly of propofol by redistribution and metabolism. There is no evidence of significant accumulation, not even after prolonged infusion times. Because propofol has no analgetic properties it must be combined with analgetics or a regional block for all painful procedures. The combination with the ultra-short acting remifentanil is a major advantage, but requires effective analgetic concepts for painful procedures. In comparison the combination of propofol with long acting opioids abolishes some of the favourable properties of propofol. Further studies of the kinetics and dynamics of propofol and other intravenous agents are needed in paediatrics which should focus on age, maturity and severity of illness. The whole importance of the propofol-infusion syndrome has to be cleared up urgently. TIVA has an important significance in paediatric anaesthesia for diagnostic and therapeutic procedures, especially where these have to be repeated. In day-case anaesthesia TIVA has advantages for all short procedures and for ENT and ophthalmic surgery: even after prolonged infusion children have an short recovery time. There is no evidence of agitation or other behavioural disorders after TIVA with propofol in paediatric anaesthesia. Propofol has anti-emetic properties. TIVA with propofol can be combined with regional anaesthesia advantageously to provide long-lasting analgesia after surgery. TIVA with propofol has been used successfully for sedation of spontaneously breathing children for MRI and CT and other procedures with open airways like bronchoscopy or endoscopy. Propofol facilitates endotracheal intubation without the use of muscle relaxants. Of course, in malignant hyperthermia TIVA will continue to be the technique of choice. Nothing is known about awareness under TIVA in paediatric patients. TIVA must be considered by comparison with the volatile agents. The use of ultra-short acting agents may cause problems such as awareness, vagal response, involuntary movements and in some cases slow recovery after prolonged infusion of propofol. But it is not known exactly how often this happens during paediatric anaesthesia. With TIVA an effective postoperative analgesia must be provided. Newer administration techniques such as the target-controlled infusions or closed-loop control systems are under development and will help to minimise the potential risk of overdosage with TIVA in paediatrics. At the present TIVA is an interesting and practicable alternative to volatile anaesthesia for pre-school and school children. TIVA with propofol in infants younger than 1 year old requires extensive experience with TIVA in older children and with the handling of this special age group and should be undertaken with maximum precautionary measures.
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PMID:[Total intravenous anesthesia. On the way to standard practice in pediatrics]. 1450 2

OBJECTIVES: To present research data about the adverse effects of pain and agitation in the emergency room with the best therapeutic options.METHODS: Review of the literature, covering some of the most important studies about analgesia and sedation in the emergency room, and pharmacokinetics and pharmacodynamics of the most important drugs.RESULTS: The metabolic responses, scales of evaluation of pain and anxiety and the different clinical situations in the emergency room are presented, inluding also the main drugs to be used.CONCLUSIONS: In the situations of stress in the emergency room we should not underestimate the clinical situations that cause pain and anxiety.
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PMID:[Sedation and analgesia at the emergency room] 1468 76

OBJECTIVES: To update information about available neonatal pain assessment and pain relief methods.METHOD: Medical literature review of the past 10 years, including textbooks, general reviews, systematic reviews, prospective, randomized controlled studies, retrospective works and case studies. Literature was reviewed based on the author clinical and scientific experience regarding pain evaluation and treatment.RESULTS: Lack of verbal expression of pain is one of the major impediments to adequate pain relief in the neonatal period. Nowadays, several valid pain assessment tools are available, including the analysis of the neonate facial features and multidimensional tools, as NIPS, CRIES, and PIPP. Non-pharmacological pain relief can be achieved by non-nutritive suction and suction of dextrose water. Neonatal analgesia, in general, includes de the use of paracetamol, opioids and local anesthetics. Opioids remain the main resource for acute pain treatment in the neonatal intensive care unit. Sedatives are important agents to decrease patient activity and restlessness, but they do not relieve pain.CONCLUSION: Based on medical, ethical, and humanitarian grounds, neonatal pain should be considered and treated.
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PMID:[Assessing and treating pain in the newborn] 1468 35

The brain-derived interleukin-1beta (IL-1beta) has been involved in the modulation of nociceptive processing. The direction of the effects, however, analgesia or hyperalgesia, is controversial. Here, we report the role of IL-1beta injected intracisternally in orofacial pain transmission. Experiments were carried out on 90 male SD rats and surgical procedures were performed under pentobarbital sodium. Intracisternal injection of 0.3 or 0.6 microg of N-methyl-d-aspartic acid (NMDA) produced intense scratching behavioral responses including vocalization, agitation and a desire to escape in a dose-related manner. The intracisternal injection of 1 or 10 ng IL-1beta significantly decreased the NMDA-evoked scratching behavioral responses. Pretreatment with an IL-1 receptor antagonist or naloxone, an opioid receptor antagonist, blocked the IL-1beta-induced antinociceptive response. These results suggest that cytokine injected intracisternally seems to produce antinociceptive effects in the NMDA-evoked pain model of the orofacial area and the antinociceptive effect seems to be mediated by an opioid pathway.
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PMID:Interleukin-1 beta injected intracisternally inhibited NMDA-evoked behavioral response in the orofacial area of freely moving rats. 1508 73

In critically ill patients, adequate analgesia and sedation increase comfort, reduce stress response and facilitate diagnostic and therapeutic procedures. Analgesia and sedation may also have a beneficial impact on morbidity, particularly by reducing pulmonary complications such as atelectasis and pneumonia, and delirium or agitation with subsequent accidental extubation. The method and depth of analgesia and sedation should be adapted to the needs of the individual patient. While evaluation of analgesia and sedation is important, technical tools for assessment are generally unreliable. Accordingly, management of these patients is best guided by simple clinical scores, though there is no consensus on how frequently pain and sedation should be evaluated. While there is some degree of consensus on what constitutes an acceptable level of pain relief, the same is not true of sedation, with the attendant risk of over-sedation. Analgesia and sedation are performed chiefly by pharmacological means. The first step includes adequate analgesia, usually with opioids. There is no evidence of a difference in efficacy between opioids as far as clinically relevant outcomes are concerned. However, there is some evidence that more sophisticated methods of opioid administration, such as patient-controlled analgesia, may improve pulmonary outcomes. In Europe, midazolam and propofol are most frequently used for sedation of the critically ill. Regular evaluation of the effect of these drugs and subsequent adaptation of dosage are more important than the choice of specific analgesics and hypnotics. Implementation of guidelines for rational analgesia and sedation would help to reduce patients' length of stay in the intensive care unit.
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PMID:Analgesia and sedation in critically ill patients. 1531 83

Sedation and analgesia are central elements in the care of critically ill, mechanically-ventilated patients. The goal of analgesic therapy is to provide relief from pain and physical discomfort which may lead to poor sleep, agitation, or a stress response. Opioids, such as morphine, fentanyl, and hydromorphone, are considered first-line agents for treating pain. All of these agents are equally effective at equipotent doses and the choice of an agent depends on both drug and patient characteristics. Sedatives with amnestic properties are desirable to prevent or relieve anxiety and agitation. The benzodiazepines and propofol are the primary sedative agents used in the intensive care unit (ICU). Agents such as clonidine and haloperidol may have a role in the ICU when used concomitantly with sedatives and analgesics. An understanding of the pharmacotherapy of sedation and analgesia in the ICU will help support appropriate usage of these agents and improve patient care.
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PMID:Analgesic and sedative pharmacology in the intensive care unit. 1546 May 18

The paper deals with the comparison of inhalational anesthesia using a fluoroethane-monooxide-oxygen mixture in apparatus-mask and endotracheal fashions in children during adenotomy. Children aged 4 to 15 years, who had undergone apparatus-mask (n = 51) and endotracheal (n = 57) anesthesia, were examined. The patients were divided into two age groups: 4-8 years and 8-15 years. The parameters of central hemodynamics, the data of cardiointervalograms, respiration rate, and SatO2 were studied. The studies were repeated 5 times for each patient at the stages of anesthesia and surgery. The use of inhalational fluroethane-monoxide-oxygen anesthesia in apparatus-mask and endotracheal fashions was found to be inadequate in children during adenotomy without addition of analgesics. In 4-8-year-old children, apparatus-mask fluoroethane-monooxide-oxygen anesthesia during surgery is ineffective, as shown by the data of central hemodynamics and cardiointervalography. The pain syndrome was observed in the postoperative period. Endotracheal fluoroethane-monooxide-oxygen anesthesia fails to ensure adequate analgesia during intubation and surgery. The pain syndrome and sympathicotony were seen in the postoperative period. In 8-15-year-old children, apparatus-mask fluoroethane-monooxide-oxygen anesthesia is characterized by prehypoxia and inadequate anesthesiological defense at the traumatic stage of an operation. In endotracheal fluoroethane-monooxide-oxygen anesthesia, the stability of cardiac output is maintained by the tension of more mature compensatory mechanisms responsible for regulation of central hemodynamics. A marked sympathicotony is noted at the traumatic stage of a surgery, as evidenced by cardiointervalography. There is motor agitation in the postoperative period.
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PMID:[Inhalational anesthesia during adenoidectomy in children]. 1583 14

The bispectral index (BIS) is processed electroencephalographic technology used in concert with clinical evaluations to objectively evaluate a patient's level of consciousness and probability of recall. Although the BIS has been extensively studied in the operating room setting, differences in patient populations, goals of treatment, and the environments themselves necessitate the development of BIS data specific to the intensive care unit. Data have evolved over the last several years, but for many reasons, the results and conclusions have varied. Yet within the data are important consistencies that help define the usefulness of BIS in patients who cannot be evaluated with subjective assessment tools such as the Sedation-Agitation Scale or the Richmond Agitation-Sedation Scale. Some of these patients cannot be evaluated with such tools because they lack motor responsiveness due to therapeutic paralysis or because they are receiving deep sedation. Bispectral index scores that are higher than expected in clinically sedated patients can often be traced to electromyographic activity or to the possibility of inadequate sedation and analgesia. The BIS must not be regarded as the sole indicator of level of consciousness, but should be used as part of an integrated approach to the evaluation of carefully selected patients with critical illness.
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PMID:Bispectral index monitoring in the intensive care unit provides more signal than noise. 1589 45


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