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)

Complement C3a is an anti-opioid peptide, having anti-analgesic and anti-amnesic effects after intracerebroventricular administration. However, the peptide is inactive after oral administration. Orally active C3a agonist peptide was designed based on the structure of oryzatensin, a C3a agonist peptide derived from rice albumin. Tyr-Pro-Leu-Pro-Arg, a pentapeptide at the carboxyl terminus of oryzatensin is the minimally essential structure for exerting C3a activity. Due to the affinity for mu-opioid receptor, both oryzatensin and Tyr-Pro-Leu-Pro-Arg showed analgesia after intracerebroventricular administration in mice which was blocked by the opioid antagonist naloxone. Tyr-Pro-Leu-Pro-Arg lost opioid activity by substitution the amino terminus tyrosine with other hydrophobic residues. Among the newly designed peptides, Trp-Pro-Leu-Pro-Arg was found to possess the strongest C3a activity. The peptide antagonized morphine-induced analgesia at 300 mg/kg after oral administration and also improved scopolamine- and ischemia-induced amnesia in a step-through passive avoidance test.
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PMID:Designing of an orally active complement C3a agonist peptide with anti-analgesic and anti-amnesic activity. 1117 94

Within the figure of more than 200,000 surgical amputations performed in the United States each year lies another--70% of patients experience phantom limb pain after the procedure, and 50% still experience phantom pain 5 years after surgery. Patients describe burning, stabbing, twisting, cramping, or throbbing pains in the missing part. Adding to the patient's and the anesthesia professional's conundrum has been the lack of a simple model that tissue injury produces pain. The patient with a surgical amputation who experiences phantom limb pain can have several sources for discomfort including problems from the original tissue injury or from pathology, e.g., scarring or continued cellular dysfunction resulting from diabetes, ischemia, or infection. Suboptimal prosthesis fit and tissues and joints connected to the affected part can continue to generate pain long after surgical wound healing. In addition, nonaffected tissues and joints now made to carry extra loads as a result of altered gait and balance can sustain collateral stress and damage and produce nociception. In addition to this series of problems, amputee patients remain susceptible to the pain problems experienced by the general population. There is a positive correlation between a painful limb before amputation and experiencing chronic phantom limb pain. Authors have described patients with preamputation pain who benefited from effective preemptive analgesia and experienced less phantom limb pain. CRNAs can have a significant role in providing anesthesia and analgesia services to these patients and can begin to think in terms of preventing lifelong pain.
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PMID:Amputation and phantom limb pain: a pain-prevention model. 1175 64

Sedatives continue to be used on a routine basis in critically ill patients. Although many agents are available and some approach an ideal, none are perfect. Patients require continuous reassessment of their pain and need for sedation. Pathophysiologic abnormalities that cause agitation, confusion, or delirium must be identified and treated before unilateral administration of potent sedative agents that may mask potentially lethal insufficiencies. The routine use of standardized and validated sedation scales and monitors is needed. It is hoped that reliable objective monitors of patients' level of consciousness and comfort will be forthcoming. Each sedative agent discussed in this article seems to have a place in the ICU pharmacologic armamentarium to ensure the safe and comfortable delivery of care. Etomidate is an attractive agent for short-term use to provide the rapid onset and offset of sedation in critically ill patients who are at risk for hemodynamic instability but seem to need sedation or anesthesia to perform a procedure or manipulate the airway. Ketamine administered through intramuscular injection or intravenous infusion provides quick, intense analgesia and anesthesia and allows patients to tolerate limited but painful procedures. The risk/benefit ratio associated with the use of this neuroleptic agent must be weighed carefully. Ketamine is contraindicated in patients who lack normal intracranial compliance or who have significant myocardial ischemia. Barbiturates are reserved mainly to induce coma in patients at risk for severe CNS ischemia, which frequently is associated with refractory intracranial hypertension, or in patients with status epilepticus. When administered in high doses, these drugs have prolonged sedative and depressant effects. Judicious hemodynamic monitoring is required when barbiturate coma is induced. Haloperidol is indicated in the treatment of delirium. Patients should be monitored for extrapyramidal side effects and, when they require higher doses, for potential electrocardiographic prolongation of the QT interval. Dexmedetomidine may evolve into an agent with qualities comparable with midazolam and propofol, and it may even become a drug of choice in select patients. Further study is required, however. Propofol has many of the qualities of an ideal sedative agent. Benzodiazepines and narcotics often are used in concert with propofol to provide reliable amnesia and to relieve pain, respectively. Propofol frequently causes hypotension when administered as a bolus or infusion, particularly in patients with limited cardiac reserve or hypovolemia. More data must be obtained to identify potential deleterious effects of hypertriglyceridemia, and further evaluation of the potential benefits in certain patient populations, such as neurosurgical patients, is needed.
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PMID:Use of propofol and other nonbenzodiazepine sedatives in the intensive care unit. 1176 65

Cardiac surgery elicits a cascade of stress responses mediated by the release of various cytokines and stress hormones [Roth-Isigkeit 1998]. Apart from the stress induced by the surgical process, cardiopulmonary bypass (CPB) has been documented to play a major role in the perioperative stress response seen following cardiac surgery [Butler 1993, McBride 1995, Hall 1997]. The imbalance in pro- and anti-inflammatory responses may affect outcome in cardiac surgery patients [Casey 1993, McBride 1995, Menasch 1995]. Contact of blood with the CPB circuit, along with hypoperfusion of various organs prior to and during CPB, may aggravate this stress response and contribute to adverse outcomes in the perioperative period [Casey 1993, Menasch 1995, Tonnesen 1996]. Splanchnic hypoperfusion that occurs in cardiac surgery patients [Landow 1991] can result in increased permeability of the gut mucosal barrier, resulting in endotoxemia and release of proinflammatory cytokines. Lungs and kidneys play a role in sequestrating the proinflammatory cytokines and, in the presence of hypoperfusion, may be damaged by these cytokines [Gilliland 1999, Liebold 1999, Gormley 2000]. Avoiding CPB may reduce this stress response. Anesthetic techniques such as thoracic epidural analgesia (TEA) that improve splanchnic perfusion [Moore 1995, Kapral 1999, Ai 2001] may have a role in improving patient outcome. It is further known that ischemic myocardium can be a major source of proinflammatory cytokines [Wan 1999a]. The cardiac sympathetic block resulting from TEA has been shown to reduce ischemia reperfusion injury [Blomberg 1989, Blomberg 1990, Liem 1992a, Liem 1992b, Liem 1992c, Kirno 1994, Stenseth 1994]. Beating heart surgery done without the aid of CPB significantly attenuates cytokine and stress response [Brasil 1998, Fransen 1998, Gu 1998, Wan 1999b, Ganapathy 1999a, Ganapathy 2000a]. There is reduced renal dysfunction following beating heart surgery [Ascione 1999], which may be related to reduced proinflammatory cytokine surge. Thoracic epidural analgesia inhibits intraoperative cortisol as well as catecholamine surge but does not add further to the reduction in cytokine response [Ganapathy 1999b].
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PMID:Stress and inflammatory response after beating heart surgery versus conventional bypass surgery: the role of thoracic epidural anesthesia. 1182 61

Conscious sedation and analgesia are integral components of successful uterine fibroid embolization (UFE), both in providing comfort to the anxious patient undergoing an elective procedure and for providing relief of the severe pelvic pain, cramps, and nausea that may result from acute uterine ischemia and the postembolization syndrome that may follow. The agents used are typically those with which interventional radiologists already have extensive experience in the performance of a variety of invasive procedures. Immediate postprocedure care benefits greatly from the use of narcotic delivered via PCA (patient-controlled analgesia) pump. Nonsteroidal anti-inflammatory drugs (NSAIDs) are also particularly useful for treating the pain and cramping caused by UFE and help reduce the amount of narcotic necessary for pain relief during the recovery period. Detailed instructions for the first week of convalescence are necessary to insure comfort and avoid complications.
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PMID:III. Uterine fibroid embolization: pain management. 1209 6

A case of chest pain in a 31-year-old woman after vaginal delivery with epidural analgesia during sulprostone administration is described. Chest pain occurred shortly after sulprostone was started and disappeared when sulprostone was stopped. Ischaemia related data were negative. Angiographically coronary arteries were normal. Coronary artery spasm aetiology was retained. Sulprostone pharmacology is summarized. Coronary artery effects are compared with literature reports. Recommendations before sulprostone use are underlined.
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PMID:[Chest pain and sulprostone during postpartum hemorrhage]. 1247 87

Sickle cell disease (SCD) is one of the most common inherited diseases worldwide. The disease is characterized by chronic hemolytic anemia, as well as acute and chronic complications. One of the most intractable problems encountered by children with SCD is the painful episode that results from tissue ischemia due to vaso-occlusion. Pain related to SCD is unique among pain syndromes due to the unpredictable, recurrent, and often persistent nature of the disease, as well as the recurring and essential need for the use of opioids. Painful vaso-occlusive episodes (VOE) are a principal cause of morbidity and account for a significant number of emergency department and hospital admissions. When untreated or inadequately managed, the pain of VOE may cause both short- and long-term consequences. Despite the fact that pain is an almost universal feature of the disease, children with SCD may form one of the most undertreated and understudied populations. One of the factors contributing to poor pain management is conflicting perceptions between patients, their families, and healthcare professionals about pain that is reported and analgesia that is required. Pain management guidelines have recently been published in an effort to overcome barriers in the assessment and management of pain related to SCD. Although there is considerable variability in the way SCD pain is managed, the standard treatment protocol for painful episodes has been rest, rehydration, and analgesia. However, pain control for children with SCD is often a difficult and complex process, and one that requires frequent systematic pain assessments and continuous adjustment of comfort measures, especially analgesics. There are a variety of analgesic agents to choose from, such as acetaminophen (paracetamol), oral or parenteral nonsteroidal anti-inflammatory drugs, and oral or parenteral opioids. Each of these options has advantages and disadvantages to their use. Continuous infusions of analgesics and patient controlled analgesia have been shown to be effective and widely used in hospital settings to manage severe pain. However, the opioid dose required to achieve pain relief varies considerably within each painful episode, from one episode to another, and between individual patients. Although not yet curable in humans, pain related to SCD can be effectively managed in most patients by using a comprehensive approach that incorporates pharmacologic, psychologic, behavioral, and physical pain management strategies.
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PMID:Pain management in children with sickle cell disease. 1266 19

Superior mesenteric venous thrombosis (SMVT) is an uncommon but potentially life-threatening disorder. We describe a cirrhotic patient with hepatocellular carcinoma who had partial SMVT for at least 28 months. Our experience may help in the management of such patients. The partial SMVT was not treated at the time of discovery because there was no evidence of bowel infarction. Moreover, the patient had a tendency to bleed severely and was in a poor condition. SMVT was followed using regular ultrasonography and the pattern of SMVT did not change significantly during the follow-up period. A symptom that may have been related to SMVT was abdominal colic pain after meals, which was sometimes followed by diarrhea and / or nausea and vomiting. There was no evidence of bowel ischemia or infarction during follow-up. Abdominal discomfort can be successfully treated using anticholinergic drugs with or without analgesia.
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PMID:Long-term follow-up of partial thrombosis of the superior mesenteric vein in a cirrhotic patient with hepatocellular carcinoma: a case report. 1282 80

The selective kappa-opioid receptor agonist spiradoline mesylate (U62,066E), an arylacetamide, was synthesized with the intention of creating an analgesic that, while still retaining its analgesic properties, would be devoid of the, mainly mu receptor mediated, side effects such as physical dependence and respiratory depression associated with morphine. Spiradoline is highly selective for the kappa receptor with K(i) of 8.6 nM in guinea pig. Examination of the enantiomers of spiradoline, showed the (-)enantiomer to be responsible for the kappa agonist properties. Spiradoline easily penetrates the blood brain barrier, and does not seem to have any significant active metabolites. In preclinical studies, spiradoline has a short duration of action with a peak at around 30 min after administration. The analgesic properties of spiradoline are well documented in mice and rats. Antitussive properties have also been reported in rats. Furthermore, spiradoline was reported to display effects suggestive of neuroprotective properties in animal models of ischemia. In humans, spiradoline is a potent diuretic. It also produces significant sedation presumably due to its antihistamine properties. Preclinical studies have shown that spiradoline reduces blood pressure and heart rate, and has possible antiarrhythmic properties. Clinical studies did not confirm these findings. kappa Receptors inhibit dopaminergic neurotransmission. Spiradoline, given systematically to rats, produces a significant and long lasting decrease in dopamine release, and in locomotor activity. It has also antipsychotic-like effect in animal behavioral tests. At low doses spiradoline was reported to decrease tics in patients with Tourette's syndrome. Although spiradoline had promising effects in animal tests of analgesia, and a reasonably good safety profile in preliminary studies, it did not replace morphine as an analgesic. The available clinical data suggest that spiradoline produces disturbing adverse effects such as diuresis, sedation, and dysphoria at doses lower than those needed for analgesic effects. Thus, future development of spiradoline-like analgesic compounds should preferably focus on reduction of unwanted effects on the central nervous system. Spiradoline, which currently is commercially available for preclinical research, might prove useful in some psychiatric conditions and possibly as a neuroprotective agent.
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PMID:A review of the properties of spiradoline: a potent and selective kappa-opioid receptor agonist. 1284 58

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.
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PMID:A fusion protein of conotoxin MVIIA and thioredoxin expressed in Escherichia coli has significant analgesic activity. 1459 43


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