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)

Concern with the suboptimal management of pain in hospitalized patients has led to the development of a patient-controlled analgesia system. In this system, a preset amount of narcotic is delivered intravenously when the patient activates the demand button. We tested the safety and efficacy of this mode of treatment in eight patients with cancer suffering from severe pain. Respiratory rates, mental status, and pain relief were recorded at baseline and during the study period. Morphine sulfate doses ranged from 1 to 5 mg, and lockout intervals from 15 to 90 minutes. Patients had a higher analgesic demand, ie, self-administered more doses, during the first four hours than during the remaining time of treatment. Respiratory rates decreased during the first four hours of treatment, but no cases of significant respiratory depression were encountered during this period or thereafter in the study. Significant pain relief was produced in all patients without causing undue sedation. Patient acceptance of this mode of therapy was excellent, and the majority of patients preferred this type of analgesia to other forms of pain treatment. In conclusion, patient-controlled analgesic is effective and safe therapy for cancer pain.
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PMID:Patient-controlled analgesia for severe cancer pain. 242 59

D-Phenylalanine, along with morphine, acetylsalicylic acid and zomepirac sodium were evaluated for their antinociceptive actions in monkeys (M. fascicularis) trained to autoregulate nociceptive stimulation using a discrete-trials, aversive-threshold paradigm. Morphine sulfate produced dose-related increases in aversive threshold which were reversible after administration of naloxone (12.5 or 25 micrograms/kg i.m.). D-Phenylalanine (500 mg/kg p.o.) produced a small increase in aversive threshold which was not statistically significant and not naloxone reversible. Acetylsalicylic acid (200 mg/kg p.o.) but not zomepirac sodium (200 mg/kg p.o.) in combination with D-phenylalanine (500 mg/kg) produced a small statistically significant increase in aversive threshold. Our results argue against the hypothesis that D-phenylalanine is responsible for increasing aversive thresholds via opiate receptor mechanisms involving increased activity of enkephalins at synaptic loci. Previous studies by others in rats and mice showed that D-phenylalanine and acetylsalicylic acid produced increases in nociceptive thresholds which were naloxone reversible. Our failure to find opiate receptor mediated analgesia in a primate model with demonstrated opiate receptor selectivity and sensitivity is discussed in terms of previous basic and clinical research indicating an analgesic role for D-phenylalanine. Possible species difference in drug action is discussed in terms of inhibition by D-phenylalanine of carboxy-peptidase-like enkephalin processing enzymes as well as inhibition of carboxypeptidase-like enkephalin degrading enzymes.
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PMID:D-phenylalanine: a putative enkephalinase inhibitor studied in a primate acute pain model. 351 91

Morphine sulfate Contin (MSC) is an investigational matrix delivery system for oral morphine sulfate that allows for prolonged blood levels of morphine. Twenty-six patients with inadequately controlled cancer-related pain were examined in an open but controlled study using MSC. Initially, all patients were converted from the prestudy analgesic regimen to an equianalgesic amount of immediate-release morphine sulfate (IRMS) on a q4h dose schedule that was in turn titrated to the level of adequate pain relief. Patients then were switched to MSC q8h and eventually to q12h, starting at doses representing the same total daily amount of morphine that was in the final IRMS dose. Of the 18 patients who completed the study, all achieved satisfactory levels of analgesia on MSC, seven at q8h and 11 at q12h dosing intervals. All patients reported better analgesia while taking MSC compared with their previous regimen. Side effects associated with MSC included sedation and constipation but not nausea or respiratory difficulty. Significant drug tolerance did not develop during a mean follow-up period of four weeks (range, 1-18 weeks). MSC is an effective oral opioid analgesic that allows an increased dose interval without increased side effects or decreased potency. It can improve the quality of life of cancer patients by allowing them to be maintained without frequent dosing or parenteral medication.
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PMID:Management of cancer pain with oral controlled-release morphine sulfate. 368 May 67

Morphine sulfate (5 mg/kg s.c.) given 30 min prior to administration of methadone prolonged methadone analgesia and increased the brain level of methadone measured 60, 120 and 180 min after administration of methadone. Rats rendered tolerant to morphine analgesia by subcutaneous implantation of two pellets, each containing 75 mg of morphine base, for 1-3 days showed cross-tolerance to methadone analgesia regardless of the presence or absence of morphine pellets. Decreases in the brain concentrations of methadone measured at 60 and 120 min time points accompanied the decreased analgesia. Neither acute nor chronic morphine pretreatment affects the biotransformation of methadone. The results suggest that the cross-tolerance to methadone analgesia seen in chronic morphine-implanted rats was partly associated with a decrease in the brain concentration of methadone occurring by a mechanism not directly related to a change in the biotransformation of methadone. In view of the known inhibitory effect of chronic morphine pretreatment on drug metabolism, our findings might demonstrate a unique phenomenon between morphine and methadone.
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PMID:Effects of acute and chronic morphine treatment on methadone analgesia and metabolism. 399 68

Antinociception following central opioid microinjection in rats was assessed weekly via a tail-flick procedure during chronic tricyclic antidepressant (TCA) treatment. (1) Daily TCA: Subcutaneous injections of desipramine (DMI), 30 mg/kg, chlorimipramine (CMI), 10 mg/kg, or saline, 1 ml/kg, were given daily for 22 days. Morphine sulfate (M), 5 micrograms, was microinjected into the ventrolateral periaqueductal gray (VLPAG) at 7 day intervals. On day 1, DMI or CMI enhanced M analgesia whereas saline did not. Augmentation of M disappeared by days 8 and 15 for CMI and DMI, respectively, and was replaced by attenuation which was still observed on day 22 for both TCAs. L-Tryptophan (LT), 100 mg/kg, i.p., on days 15 and 22 temporarily restored TCA enhancement of M. Fourteen days after cessation of all daily TCA treatments, enhancement of M by CMI was similar to that observed on day 1, whereas recovery of DMI-induced facilitation was incomplete. (2) Weekly TCA: Weekly treatment with DMI, CMI, or saline in the same doses as above had similar effects. M analgesia was enhanced by the TCAs but not saline on day 1; this facilitation was absent by day 15. Attenuation of M by DMI or CMI was evident on day 22; 2 weeks after cessation of all weekly TCA treatments, complete recovery of TCA-induced augmentation was observed. Loss of M facilitation during chronic daily or weekly TCA administration may be related to reduction of central opioid and/or 5-HT2 receptors.
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PMID:Contrasting effects of acute vs. chronic tricyclic antidepressant treatment on central morphine analgesia. 609 58

Morphine sulfate is a weak analgesic in the frog Rana pipiens pipiens, causing a slight increase in nociceptive threshold at a dose of 10 mg/kg and a pronounced increase at 100 mg/kg. Morphine-induced analgesia persists for at least 165 min and is significantly attenuated by naloxone. The analgesic doses of morphine are well below the lethal dose and are without noticeable effect on the behavior of the frogs or their responses to non-painful stimuli. Higher doses of morphine (320 and 640 mg/kg) induced a state of hyper-responsiveness to sensory stimuli similar to the explosive motor behavior induced in rats by microinjection of morphine into the periaqueductal gray.
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PMID:Morphine-induced analgesia and explosive motor behavior in an amphibian. 660 62

Morphine sulfate and methadone hydrochloride exhibit very different half-lives but are described as having an analgesic potency of one. The use of a drug like methadone may provide prolonged and constant analgesia in the perioperative setting. This double-blinded investigation used methadone and morphine intraoperatively and measured pain scores and narcotic requirements in the first 24 hours postoperatively. Thirty American Society of Anesthesiology (ASA) patients, physical status I through III, between the ages of 18 to 65 years were scheduled for orthopedic surgery and randomly assigned to receive morphine or methadone at 0.30 mg/kg. Fifteen patients received morphine and fifteen patients received methadone. There was no significant difference between the two groups in terms of age, height, weight, and ASA status. No statistically significant difference was observed among the two groups between the amount of analgesic requirements postoperatively or in the visual analogue scale pain score.
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PMID:A comparison of intraoperative morphine sulfate and methadone hydrochloride on postoperative visual analogue scale pain scores and narcotic requirements. 759 43

The effects of duration of sucrose consumption on morphine-induced analgesia (MIA) were examined in 20 adult male Long-Evans rats. Ten rats were tested for MIA on a tail-flick apparatus following acute (5 h), chronic (3 weeks) intake, and subsequent removal of a 32% sucrose solution. Ten rats that never received the sucrose solution served as controls. Morphine sulfate was administered according to a cumulative dosing procedure beginning with 2.5 mg/kg morphine. The same dose was administered every 30 min until a total dose of 15 mg/kg was achieved. Tail-flick latencies were measured immediately prior to injections, and 30 min following each injection. After acute intake of sucrose, there was a trend for animals drinking the sugar solution to show suppressed MIA relative to animals drinking water. In contrast, after drinking the sucrose for 3 weeks, rats showed an enhanced MIA relative to rats drinking water. Three weeks after sucrose removal, there were no differences in MIA as a function of prior dietary conditions. The results support the hypothesis that length of exposure to sucrose influences morphine-induced analgesia and suggest that any change in physiology resulting from sucrose exposure may be reversible.
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PMID:Duration of sucrose availability differentially alters morphine-induced analgesia in rats. 885 91

The effects of saccharin, sucrose, or Polycose intake on morphine-induced analgesia (MIA) were examined in 40 adult male Long-Evans rats. Rats were tested for MIA on a tail-flick apparatus following acute (5-h) and chronic (3-wk) intake of a 0.15% saccharin solution, a 32% sucrose solution, a 33.68% Polycose solution, or water. During the chronic phase, all rats were given a choice between the test solution and water. Morphine sulfate was administered according to a cumulative dosing procedure beginning with 2.5 mg/kg morphine. The same dose was administered every 30 min. Tail-flick latencies were measured immediately prior to injections and 30 min following each injection. After acute intake of flavored solutions or water, there were no differences in MIA as a function of diet. However, after drinking the flavored solutions or water for three weeks rats drinking Polycose or sucrose showed significantly enhanced MIA relative to rats drinking saccharin. Rats drinking Polycose also showed enhanced MIA relative to rats drinking water. Comparison between the acute and chronic phases of the study demonstrated that tolerance to morphine's analgesic effects did not develop in rats drinking Polycose or sucrose, but did develop in rats drinking saccharin or water. The results support the hypothesis that, in addition to palatability, the nutritive value of flavored solutions influences MIA.
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PMID:Beyond sweet taste: saccharin, sucrose, and polycose differ in their effects upon morphine-induced analgesia. 907 67

Kadian/Kapanol (K) is a capsule formulation of morphine designed for 12- or 24-hourly dosing. This double-blind study compared the efficacy and safety of K every 24 hr to K every 12 hr and MS Contin tablets (MSC) every 12 hr. One hundred fifty-two patients with cancer pain were titrated to adequate analgesia with immediate-release morphine (IRM) solution. Stabilized patients were randonized to one of the three treatments for 7 +/- 1 days. Rescue medication was IRM tablets. Efficacy and safety were assessed by time to first remedication and total dose of rescue medication, pain scores, global assessments, and incidence of morphine-related side effects. Fifty-four patients were treated with K every 24 hr. 45 with K every 12 hr. and 53 with MSC every 12 hr. Mean age was 61 years and mean total daily dose of morphine was 138 mg. Forty-six percent of the K every 24 hr patients, 51% of the K every 12 hr patients, and 55% of the MSC every 12 hr patients required rescue medication on the final day. Time to remedication was 16.0 hr for K every 24 hr, 9.1 hr for K every 12 hr and 8.7 hr for MSC every 12 hr (P = 0.0010). Patient global assessment significantly favored K every 24 hr over MSC every 12 hr (P = 0.018). There were no statistically significant differences among the treatments for any morphine-related side effects when adjusted for baseline. K had efficacy and safety profiles similar to MSC every 12 hr but had the advantage of 12- or 24-hourly administration.
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PMID:Comparison of a once-a-day sustained-release morphine formulation with standard oral morphine treatment for cancer pain. 926 35


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