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)

The effect of a fractional epidural blockade on acute pancreatitis was investigated in a prospective study. PATIENTS AND METHODS. Thoracic (20 patients) or lumbar (six patients) epidural blockade was carried out in 26 patients with severe abdominal conditions comprising sub-ileus in 100%, pancreatic edema indicated by sonography/computer tomography in 57.8%, and necrosis of the pancreas in 34.6%. RESULTS. On average, 3.4 (1-6) injections with single doses of 6-20 ml 0.25% bupivacaine were injected per day. In four patients, morphine (up to 4 mg per 24 h) was added to the local anesthetic. The duration of treatment was between 1 and 15 days. After 10.5% of the injections, the systolic pressure decreased by more than 20%, and after 12.8% of the injections the blood pressure decreased by more than 30%. Hypotension of more than 30% was treated with 0.3 to 0.5 ml theodrenaline (Akrinor) and/or 0.1 to 0.2 mg dihydro-ergotamine (Dihydergot). General analgesics had to be administered in addition on 21.8% of the treatment days and intensive care treatment (artificial ventilation) on 32% of the treatment days. The duration of epidural analgesia varied between 1 and 15 days depending on the intensity of symptoms (pain, ileus). Within 4 days, the enzyme activity of the lipase fell from 8120 to 427 IU, and that of alpha amylase fell from 1401 to 143 IU. In 3 patients laparotomy (for drainage) was performed. An ERCP was carried out in 16 patients. Cardiopulmonary failure necessitated artificial ventilation over a period of 1-15 days in 6 patients; the epidural blockade was continued during the artificial ventilation. Cholecystectomy was carried out as an interval operation in 6 patients. No neurological complications were observed. All patients survived and were discharged from hospital.
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PMID:[Epidural blockade for analgesia and treatment of acute pancreatitis]. 178 Apr 89

As an approach to the development of therapeutically useful peptide pharmaceuticals that can penetrate the blood-brain barrier, we have designed and demonstrated the application of a carrier-targeting system. We have developed a prodrug design strategy that is designed to utilize membrane-bound enzymes whereby release of a bioactive peptide from a highly lipophilic triglyceride peptide-carrier is achieved in situ, thus attaining high localized concentrations of the bioactive peptide. Following localization of such a system, normal peptidase and lipase action is utilized to release the active peptide (deltorphin II) intact and in high concentration. At present, the exact mechanisms are unclear, but the observed results in which analgesia is observed following peripheral administration suggest that the active peptide is able to cross the blood-brain barrier and sustain prolonged periods of analgesia as determined by antinociception tests by release of the bioactive peptide. In vitro tests of binding and bioactivity by the peptide conjugate show essentially no potency in either target or control analogues, but potent antinociceptive effects are observed following peripheral administration.
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PMID:Peptide targeting and delivery across the blood-brain barrier utilizing synthetic triglyceride esters: design, synthesis, and bioactivity. 917 51

Mucinous peritoneal carcinomatosis from a primary gastrointestinal malignancy is a lethal condition that has few treatment options with the use of surgery, chemotherapy or radiation therapy. Recent advances in hyperthermia technology and in knowledge of the natural history of this disease has suggested the possible utility of hyperthermia in the application of aggressive local-regional therapy. Radiofrequency (RF) hyperthermia to the whole abdomen, to the hemithorax, or to an isolated mucinous tumour deposit obstructing the gastrointestinal tract was used in patients with disseminated mucinous adenocarcinoma of appendiceal origin. There were 228 hyperthermia treatments in 21 patients, with a median of 10 treatments per patient. The maximum number of treatments was 26, and minimum was one. For the first six hyperthermia treatments, escalating doses of deep hyperthermia (41-45 degrees C) was monitored with multiple sensor internal temperature probes and a single sensor subcutaneous temperature probe. After reaching a maximal hyperthermia treatment, this was maintained for all subsequent treatments. Initially, the maximal temperature allowed in tumour and subcutaneous tissue was 43 degrees C. After 50 hyperthermia treatments, this was changed to 45 degrees C. If disease stabilization or response was insufficient and maximal tolerable hyperthermia had been established, the frequency of treatment was increased from every 4 weeks to every 2 weeks, and escalating doses of mitomycin C at 8 mg/m2 were added to the regimen. Mitomycin C was infused during the hyperthermia treatment. For the first 165 treatments, patients were monitored just before and 10 days after hyperthermia with a complete blood count and a full battery of laboratory tests including amylase and lipase. Response was monitored by carcinoembryonic antigen assays on a monthly basis and CT scans on a 6 monthly basis. None of the 21 patients included in this study died, required intensive care, or required major surgical interventions as a result of hyperthermia treatments. One potentially life-endangering event was profound bradycardia and hypotension observed in a 76-year-old male receiving hyperthermia treatment to his right hemithorax. Two patients developed an enterocutaneous fistula (a frequent spontaneous event in this group of patients) while under treatment. No abnormal laboratory tests were observed in the first 165 hyperthermia treatments. Heat damage to normal tissue was limited to skin blisters in three patients and induration of the subcutaneous tissues in 10 patients. Skin pain on an analogue scale of 0-10 was scored by patients as a mean of 3.6 (range 0-8) before skin analgesia was routinely utilized. With anesthetic gel, the skin discomfort was greatly reduced. Prolonged abdominal pain for 4-20 days following treatment which required narcotic analgesia was seen in four patients. A complication rate of 62% was caused by the long-term indwelling temperature probe sheaths. Infection was observed in four patients, small bowel fistula in one, and dislodgement of the temperature probe sheath requiring repeat CT was necessary in seven patients. After maximal escalation of RF power in seven patients (33%), deep hyperthermia compatible with thermal destruction of tumour (> or = 43 degrees C for 45 min) was recorded in all subsequent treatments. In eight patients (38%), heat generation compatible with chemotherapy augmentation (41.5-43 degrees C) was consistently recorded. In six patients, non-therapeutic temperatures were recorded. There was no correlation of maximal tumour temperature, maximal subcutaneous tissue temperature and maximal RF power. With the use of skin anaesthetic there was no correlation of tumour temperature and the thickness of the subcutaneous layer of the skin. Progression was seen in 14 patients, and 11 of these patients died. No patients who showed disease stabilization have died with a minimum of 2 year follow-up. (ABSTRACT TRUNCATED)
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PMID:Radiofrequency hyperthermia in the palliative treatment of mucinous carcinomatosis of appendiceal origin: optimizing and monitoring heat delivery in western patients. 1100 76

According to a previous study, an excellent level of analgesia can be expected when using epidural anaesthesia in patients with acute pancreatitis. In the present investigation, the effectiveness and safety of epidural anaesthesia is demonstrated in a large group of patients with severe acute pancreatitis, who were admitted to an intensive care unit. Epidural anaesthesia alone produced excellent analgesia on 1,083 of 1,496 observation days (72%) without the systemic use of other analgesic substances. Even in patients with marginal cardiovascular stability, epidural injection of local anaesthetic solution was tolerated well. Only 8% of all local anaesthetic injections were associated with a haemodynamic reaction that required pharmacological intervention. There was no case of a septic or neurological complication of epidural anaesthesia. Initially elevated serum amylase and lipase were normalized after 17.4 days (minimum one day, maximum 19 days). Surgical intervention was necessary for 36 patients, with a total of 64 surgeries having to be performed, including cholecystectomy. Sixteen patients required artificial ventilation for an average time of 12.3 days (minimum two days, maximum 48 days). Lethality was 2.5% (three patients), with all three patients suffering from an acute stage III pancreatitis. The average duration of ICU treatment was 12.4 days (minimum two days, maximum 101 days).
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PMID:[Using epidural anesthesia in patients with acute pancreatitis--prospective study of 121 patients]. 1190 96

Hyperlipemic pancreatitis and pseudocyst formation late in pregnancy is a rare event. We report a case of hyperlipemic pancreatitis occurring in a G1P0 oriental woman at 32 weeks gestation. The initial serum lipase level was 1070 U/L, serum cholesterol level was 38.50 mmol/L and triglyceride level was > 57 mmol/L. She was treated conservatively with fasting, narcotic analgesia, and fluid resuscitation. Her symptoms resolved rapidly and lipase returned to normal within 2 days. During the first week in hospital she developed peripancreatic fluid collections and became symptomatic from a collection that extended down into the right pelvis. One week after admission she developed pre-term labor and delivered a healthy infant vaginally. There was an excellent outcome for both mother and infant. Serum lipid levels returned to near normal by 6 weeks post delivery.
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PMID:Hyperlipemic pancreatitis and pseudocyst formation in late pregnancy. 1282 7

Baclofen is chemically (RS)-beta-(aminomethyl)-4-chlorobenzene propanoic acid. It is used in therapy of pain and as a muscle relaxant. Baclofen produces analgesia by increasing the concentration of gamma amino butyric acid (GABA), the major rapid inhibitory transmitter. Both the isomers of baclofen have different therapeutic activity with respect to their interaction to the receptors at the site of action. Lipase from Candida cylindracea has been used as a catalyst for resolving racemic mixtures of numerous drug molecules. The present investigation deals with the racemic resolution of RS-baclofen using lipase from Candida cylindracea and a study of the factors affecting resolution.
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PMID:Racemic resolution of RS-baclofen using lipase from Candida cylindracea. 1595 92

Capsaicin (Cap) and its analogs (CAPanalogs) have diverse effects in sensory neurons including analgesia, implying they modulate other cellular targets besides the TRPV1 Cap receptor. Since Cap and CAPanalogs are not largely available and their chemical synthesis is cumbersome, they have been obtained through a direct lipase-catalyzed reaction. Capsiate, the ester CAPanalog, was synthesized using a novel enzymatic transacylation one-pot strategy. Five different CAPanalogs were synthesized by amidation in 2-methyl-2-butanol with higher yields than previously reported. Voltage-dependent Ca(2+) channels (Ca(v)s) are among the main Ca(2+) entry paths into cells. They are classified as high-voltage-activated Ca(2+) channels (HVA) and low-voltage-activated Ca(2+) channels (LVA) constituted only by T-type channels. Though HVA Ca(v)s are Cap sensitive, it is not known if capsaicinoids inhibit LVA Ca(v)s which participate in the primary sensory neuron pain pathway. Here we first report that Cap, dihydrocapsaicin, N-VAMC(8), N-VAMC(9), and N-VAMC(10) can directly and partially reversibly inhibit T-type Ca(v)s, whereas olvanil, capsiate, and vanillylamine cannot. The Cap inhibition of T-type Ca(v)s was independent of TRPV1 activation.
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PMID:Enzymatic synthesis of capsaicin analogs and their effect on the T-type Ca2+ channels. 1736 79

Acute pancreatitis is a potentially life-threatening illness, with a short time frame for diagnosis and treatment. A number of recent experimental and clinical multicentre trials as well as meta-analyses have provided more far-reaching recommendations compared to previous guidelines. To answer 12 key questions, we performed a review of recent literature and current guidelines. Diagnosis can be made on the basis of history, physical examination and serum lipase alone. Cholestatic parameters and upper abdominal ultrasound enable verification of biliary etiology. Poor prognostic indicators include elevated blood sugar, BUN and hematocrit. The latter suggests early, adequate volume replacement, which should be tailored to the clinical picture, echocardiography and/or modern hemodynamic parameters. In addition to opiate analgesia, meta-analyses support the use of endoscopic retrograde cholangiography in pancreatitis of biliary origin, antibiotics in necrotizing pancreatitis and early enteral feeding. Even where necrosis is present, conservative management (radiologically or endoscopically placed drains) is appropriate.
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PMID:[Diagnosis and treatment of acute pancreatitis. Current recommendations]. 2167 47

Mushroom toxicosis is rarely diagnosed in dogs and is poorly reported in the veterinary literature. This report suggests that mushroom toxicosis is a potentially under-diagnosed condition in first opinion practice in the UK. Nine dogs with clinical signs consistent with mushroom toxicosis were identified from the records of an out-of-hours emergency service between August 2010 and January 2011. Four dogs were later excluded because of clinical inconsistencies. Clinical signs included acute profuse ptyalism (5/5), diarrhoea (5/5), vomiting (4/5), hypovolaemia (4/5), stuporous (3/5) or obtunded mentation (1/5), miosis (2/5) and hypothermia (2/5). Serum lipase activity was elevated in 4/4 dogs; canine-specific pancreatic lipase was elevated in the remaining dog. Four dogs recovered with aggressive intravenous fluid therapy, analgesia and supportive care; the remaining dog was euthanased due to severe clinical signs and financial constraints. Mushroom toxicosis is an important differential diagnosis for acute gastroenteritis and one possible cause of some cases of "Seasonal Canine Illness". Affected dogs may demonstrate elevated pancreatic enzymes and mushroom toxicosis should be considered in cases of elevated lipase or abnormal semi-quantitative canine-specific pancreatic lipase activities.
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PMID:Mushroom toxicosis in dogs in general practice causing gastroenteritis, ptyalism and elevated serum lipase activity. 2390 18

Bladder-related pain is one of the most common forms of visceral pain, and visceral pain is among the most common complaints for which patients seek physician consultation. Despite extensive studies of visceral innervation and treatment of visceral pain, opioids remain a mainstay for management of bladder pain. Side effects associated with opioid therapy can profoundly diminish quality of life, and improved options for treatment of bladder pain remain a high priority. Endocannabinoids, primarily anandamide (AEA) and 2-arachidonoylglycerol (2-AG), are endogenously-produced fatty acid ethanolamides with that induce analgesia. Animal experiments have demonstrated that inhibition of enzymes that degrade AEA or 2-AG have the potential to prevent development of visceral and somatic pain. Although experimental results in animal models have been promising, clinical application of this approach has proven difficult. In addition to fatty acid amide hydrolase (FAAH; degrades AEA) and monacylglycerol lipase (MAGL; degrades 2-AG), cyclooxygenase (COX) acts to metabolize endocannabinoids. Another potential limitation of this strategy is that AEA activates pro-nociceptive transient receptor potential vanilloid 1 (TRPV1) channels. Dual inhibitors of FAAH and TRPV1 or FAAH and COX have been synthesized and are currently undergoing preclinical testing for efficacy in providing analgesia. Local inhibition of FAAH or MAGL within the bladder may be viable options to reduce pain associated with cystitis with fewer systemic side effects, but this has not been explored. Further investigation is required before manipulation of the endocannabinoid system can be proven as an efficacious alternative for management of bladder pain.
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PMID:Potential of Endocannabinoids to Control Bladder Pain. 2986 82


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