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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 clonidine, naphazoline and xylometazoline on analgesia induced by morphine, codeine, fentanyl and pentazocine, and on cataleptic effect of morphine, codine and fentanyl was studied in rats. The biochemical assays on the influence of four analgesics on the brain concentration and turnover of noradrenaline (NA) were also performed. It was found that three drugs stimulating central NA receptors failed to affect the analgesic ED50 of all antinociceptive agents and they enhanced catalepsy induced by morphine and fentanyl. Codeine catalepsy was increased by clonidine and decreased by naphazoline and xylometazoline. The brain concentration of NA was not changed by morphine and fentanyl, but one of the doses of codeine (45 mg/kg) slightly enhanced it. Pentazocine dose-dependently decreased the brain level of NA. The rate of NA turnover was not altered by analgesics except for the higher dose of fentanyl (0.2 mg/kg) following which the disappearance of NA from the brain was diminished. The results are discussed in the light of various and non-uniform data from the literature. It is suggested that in rats the brain NA plays a less important function than the other monoamines in the behavioural activity of potent analgesics.
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PMID:Central action of narcotic analgesics. Part IV. Noradrenergic influences on the activity of analgesics in rats. 3 81

The agonist-antagonist opioid analgesics are a heterogeneous group of drugs with moderate to strong analgesic activity comparable to that of the pure agonist opioids such as codeine and morphine but with a limited effective dose range. The group includes drugs which act as an agonist or partial agonist at one receptor and an antagonist at another (pentazocine, butorphanol, nalbuphine, dezocine) and drugs acting as a partial agonist at a single receptor (buprenorphine). These drugs can be classified as nalorphine-like or morphine-like. Meptazinol does not fit into either classification and occupies a separate category. Pentazocine, butorphanol and nalbuphine are weak mu-antagonists and kappa-partial-agonists. All three drugs are strong analgesics when given by injection: pentazocine is one-sixth to one-third as potent as morphine, nalbuphine is slightly less potent than morphine, and butorphanol is 3.5 to 7 times as potent. The duration of analgesia is similar to that of morphine (3 to 4 hours). Oral pentazocine is closer in analgesic efficacy to aspirin and paracetamol (acetaminophen) than the weak opioid analgesics such as codeine. Neither nalbuphine nor butorphanol is available as an oral formulation. At usual therapeutic doses nalbuphine and butorphanol have respiratory depressant effects equivalent to that of morphine (though the duration of such effects with butorphanol may be longer). Unlike morphine there appears to be a ceiling to both the respiratory depression and the analgesic action. All of these 3 drugs have a lower abuse potential than the pure agonist opioid analgesics such as morphine. However, all have been subject to abuse and misuse, and pentazocine (but not the others) is subject to Controlled Drug restrictions. Buprenorphine is a potent partial agonist at the mu-receptor, and by intramuscular injection is 30 times as potent as morphine. A ceiling to the analgesic effect of buprenorphine has been demonstrated in animals and it is also claimed in humans. However, there are no reliable data available to define the maximal dose of buprenorphine in humans. A practical ceiling exists for sublingual use in that the only available formulation is a 2 micrograms tablet and few patients will accept more than 3 or 4 of these in a single dose. The duration of analgesia is longer than that of morphine, at 6 to 9 hours. There have been suggestions that buprenorphine causes less respiratory depression than morphine, but viewed overall it appears that in equianalgesic doses the 2 drugs have similar respiratory depressant effects.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Opioid agonist-antagonist drugs in acute and chronic pain states. 171 41

The authors report a prospective study on 944 cancer pain patients treated with one of the following opioids: codeine, oxycodone, dextropropoxyphene, buprenorphine, and pentazocine. Level of analgesia, duration of treatment, side effects, and drop out were evaluated for each drug. Twenty-four percent of the patients still benefitted from treatment at the fourth week of study, even if high drug dosages were not used. Pentazocine did not show an evident analgesic effect during the first 2 wk of treatment. The other opioids were found to be valid therapeutic instruments for chronic cancer pain control in a limited number of patients.
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PMID:A clinical study on the use of codeine, oxycodone, dextropropoxyphene, buprenorphine, and pentazocine in cancer pain. 194 Apr 86

In June 1988, the new type of the lithotripter MPL 9000 (Dornier), which was the first interdisciplinary lithotripter for treatment of urinary and biliary calculi, was installed at the Shakai Hoken Chukyo Hospital. MPL 9000 has some features which enable one to treat with low range of shock wave energy and without anesthesia due to the enlarged aperture of the ellipsoid (210 mm), and locate the stone by computerized two ultrasound probes (coaxial, lateral). Unlike HM-3, the water bath is not used: shock wave is shot through the water cushion. From June to November 1988, 35 patients suffering from 64 urinary calculi were treated. The majority represented caliceal (75%) and pelvic (17%) stones, whereas 5 calculi were treated in the upper and lower ureter. Twenty-four patients were treated in one session and 11 patients needed additional sessions. The given number of shock waves was between 1337 and 3050 per one session and averaged 2403 with low generator voltage (15-18 kv). Twenty sessions (42%) were given without any medication and other 28 sessions (58%) were under analgesia (Pentazocine, i.v.) for the pain complained during the treatment. The rate of successful disintegration (less than 5 mm) was 88%. After the 1-month followup, 47.1% were free of stone, and 62.1% were free after the 3-month. Four patients had arrhythmia and one patient was with a subcapsular renal hematoma. We have concluded that this lithotripter is useful to treat upper and lower urinary tract calculi, in particular radiolucent ones in high risk patients because it is applicable without anesthesia.
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PMID:[Clinical experience with ESWL with new Dornier lithotripter MPL 9000]. 232 21

The opioid agonist-antagonists are a heterogeneous group of compounds capable of providing analgesia sufficient to treat moderate to severe acute pain. Pentazocine, butorphanol and nalbuphine produce subjective effects which are quite different from those of morphine. Lack of mood elevation and occasional dysphoria may contribute to a lower level of patient acceptance, but all of these analgesics are significantly safer than the pure agonists. Doses in the therapeutic range are unlikely to produce dangerous levels of respiratory depression in most patients. Other opioid side-effects such as nausea, constipation and biliary spasm appear to be less frequent as well. The mu partial agonist buprenorphine shares many of the safety advantages of the older drugs, and its subjective effects appear more morphine-like. It is not clear whether mu partial agonists have real clinical advantages over kappa-type analgesics. All of these drugs are opioid antagonists and are able to precipitate abstinence in individuals with significant prior exposure to opiates. Neither absolute potency nor the ratio of agonist to antagonist effect are predictors of therapeutic usefulness. There is now an enormous amount of clinical experience with the agonist-antagonists. In many, but not all, clinical situations they are acceptable alternatives to the morphine-like drugs.
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PMID:The clinical usefulness of agonist-antagonist analgesics in acute pain. 289 87

The analgesic activity of Viminol R2 was compared to that of Pentazocine and placebo in a double-blind, "between subjects" study involving 42 patients with postoperative pain randomly assigned to 3 groups of 14 patients each and treated with a single intravenous dose of Viminol R2 10 mg, Pentazocine 30 mg or placebo. Pain relief scores were recorded over a 2 h period after treatment. The analgesic activity of Viminol R2 and Pentazocine was significantly greater than that of placebo both in terms of time-course of action and frequency of classes of satisfactory analgesia. No statistically significant differences were found between Viminol R2 and Pentazocine. No side effects were observed in any patients treated with Viminol R2.
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PMID:Viminol R2 analgesic activity in patients with postoperative pain: comparison with pentazocine. 352 23

Published clinical studies and extensive experience has shown that pentazocine, the first of the practical agonist/antagonist analgesics, is a potent analgesic with wide application in clinical medicine. It has been shown to have a spectrum of pharmacological activity which has qualitative differences from pure opiate agonists and these have important implications in clinical medicine. Pentazocine can provide analgesia as great as the opiates including morphine and meperidine, but does not have the same effect on mood. It is, therefore, less effective than the opiates in those situations where an anxiolytic effect is desired. Conversely, it produces less CNS depression in particular with regard to respiratory depression and nausea and vomiting. It also does not have the same potential for producing hypotension. The parenteral administration of pentazocine produces rapid strong analgesia which is of less duration than with morphine or meperidine. The oral administration of pentazocine is less predictable with regard to response but in appropriate patients it is capable of providing a similar degree of analgesia to that achieved with parenteral pentazocine. The dependence liability of pentazocine is substantially less than that with the opiates, and where abuse of parenteral pentazocine alone has taken place, it has usually been in medical and paramedical personnel seeking a support for inadequate personalities. Though physical and psychic dependence to parenteral pentazocine is undoubtedly possible, its incidence is extremely low with regard to the extent of the therapeutic use of pentazocine.
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PMID:Pentazocine. 388 78

Pentazocine or pethidine was administered to healthy parturients up to the time of delivery using a self-demand (self-administration on demand) intravenous apparatus, the Cardiff Palliator. Good analgesia was obtained with both drugs. The patients receiving pethidine exhibited side-effects (nausea, vomiting and drowsiness), whereas there were no side-effects among those receiving pentazocine. Apgar and neurobehavioural scores of the babies of mothers in both groups were the same and did not differ from those of a third group of babies, the mothers of whom had received 4-hourly intramuscular pethidine on demand according to the usual hospital routine. The self-administration technique proved a safe and effective means of providing analgesia during labour and delivery, with pentazocine having a decided advantage over pethidine because of its lack of side-effects.
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PMID:Self-administered intravenous analgesia during labour. A comparison between pentazocine and pethidine. 399 3

Patient-controlled analgesia (PCA, intravenous self-application of narcotics) was studied during the early postoperative period. Subjects were 40 ASA I-III patients recovering from elective major and minor surgery (each 20 having undergone abdominal or orthopaedic operations). Pentazocine bolusses of each 8 mg were available via a hand-button whenever the patients felt pain relief necessary, and delivered by a microprocessor-controlled injection pump (On-Demand Analgesia Computer, ODAC). Hourly maximum dose was set to 60 mg with a pump refractory time of 1 min between valid demands. A continuous low-dose pentazocine infusion (1 mg/h) was additionally administered in order to prevent catheter obstruction. Duration of the PCA period was 20.3 +/- 5.9 h (mean, standard deviation). During this time, 20.0 +/- 12.7 demands per patient were recorded resulting in mean pentazocine consumption of 135.6 +/- 81.4 micrograms/kg/h. Self-administration was characterized by considerable intra- and interindividual variability. There were no statistically significant differences with regard of pentazocine consumption or pain relief between abdominal and orthopaedic patients, nor could any be demonstrated between the sexes. Similarly, no clear differences were found after various anaesthetic techniques (neuroleptanalgesia, halothane or spinal anaesthesia). Over-all efficacy and patient acceptance proved to be excellent. Effectiveness of PCA was judged superior by about 68% of patients when compared with previously experienced conventional postoperative analgesia. Side effects (nausea, emesis, sweating) occurred in about 10-18% but were usually of minor intensity. Circulatory or respiratory problems were not observed during the PCA period. Patient-controlled analgesia is discussed as a promising concept for the treatment of acute pain and clinical pain research.
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PMID:[Postoperative on-demand analgesia with pentazocine (Fortral)]. 409 11

Interactions between buprenorphine, narcotic analgesic, and centrally acting drugs were studied in prolongation of halothane-induced sleeping and analgesia using the D'Amour-Smith method in mice, and the effect of buprenorphine on monoamine metabolism was studied in rat brain. Diazepam and chlorpromazine prolonged the halothane-induced sleeping time dose-dependently. Buprenorphine (0.01, 0.1, and 1 mg/kg s.c.) inhibited the effect of diazepam, but not that of chlorpromazine. Pentazocine and naloxone also inhibited the effect of diazepam, but morphine did not. It is suggested that the inhibitory effect of buprenorphine on prolongation of halothane-induced sleeping time by diazepam is due to its opiate antagonistic property. Since narcotic antagonists inhibited the effect of diazepam, the endogenous opiate system seems to be involved in this effect. Diazepam or droperidol had no effect on the analgesia of buprenorphine, morphine, and pentazocine. Buprenorphine analgesia was inhibited by reserpine and p-chlorophenylalanine, potentiated by 5-hydroxytryptophan, and not affected by alpha-methyl-p-tyrosine or 3,4-dihydroxyphenylalanine. These results suggest that the serotonergic system plays a modulating role in buprenorphine analgesia. Imipramine and nialamide inhibited buprenorphine analgesia in the test at low stimulus intensity, but potentiated at high stimulus intensity. Buprenorphine (0.1, 1 and 10 mg/kg s.c.) increased the dopamine metabolites, 3,4-dihydroxyphenylacetic acid and homovanillic acid, in various brain areas and the serotonin metabolite, 5-hydroxyindoleacetic acid, in midbrain.
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PMID:[Interactions between buprenorphine, narcotic analgesic, and centrally acting drugs in prolongation of halothane-induced sleeping and analgesia (author's transl)]. 612 74


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