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Query: UMLS:C0030193 (pain)
 261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The effectiveness of lysine acetyl salicylate (LAS) 1.8 g, equivalent to aspirin 1 g, in relieving severe, immediate, postoperative pain has been compared with that of morphine 10 mg in comparable groups of patients. A single injection of LAS 1.8 did not give effective or consistent relief of pain, while morphine was both effective and consistent in its action. However, LAS was shown to have some analgesic activity.
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PMID:Injectable aspirin as a postoperative analgesic. 679 84

The efficacy of mild analgesics after 160 various superficial operations was studied by comparing intravenous lysine-acetylsalicylate (LAS) 1.8 g, Litalgin 4 ml (metamizole = dipyrone 2.0 g+ pitophenone 8.0 mg) or paracetamol 0.5 g to oxycodone 4 mg. At 15 min postdrug, oxycodone 4 mg had the best peak effect but this significant (P less than 0.05) difference to mild analgesics disappeared at 30 min, and thereafter all test analgesics showed an equally low effect. Two-thirds of the patients anaesthetized without peroperative analgesics needed pain relief when recovering from superficial surgery. The need for pain relief was lowest after varicose vein operations 40% of the patients as compared to about 70% after other types of superficial surgery. In 42% of the patients requiring pain relief, the test analgesics alone gave sufficient pain relief. The rest needed an additional 5 mg of oxycodone, on average, to be comfortable. The combined use of mild analgesics and oxycodone for adequate pain relief did not seem to reduce the postdrug sedation as compared to oxycodone alone. The results indicate that in traditional clinical dosages LAS, dipyrone or paracetamol can substitute about 5 mg oxycodone but offer sufficient analgesia only in about 40% of the patients recovering from superficial surgery.
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PMID:Postoperative analgesics for superficial surgery. Comparison of four analgesics. 681 Jun 42

Systemically administered lysine-8-vasopressin (LVP; 16-128 micrograms/kg) was found to induce a potent and dose-dependent antinociceptive effect, as measured by the tail-flick test in the rat. This effect could be seen in the absence of any significant change in general activity, indicating that it was not due to sedation or general motor debilitation. The antinociceptive effect of LVP does not appear to be mediated by endogenous opiates or other pituitary hormones, as evidenced by: 1) the lack of antagonism by the opiate receptor blocker naloxone, 2) the lack of cross-tolerance with morphine, and 3) its persistence after hypophysectomy. Des-glycinamide-LVP, a vasopressin analog with no appreciable pressor or antidiuretic action, showed no antinociceptive activity (128 micrograms/kg), and des-amino-arginine-vasopressin, a vasopressin analog with minimal pressor activity but greatly enhanced antidiuretic activity, was also relatively ineffective (128 micrograms/kg). These results suggest that the antinociceptive activity of vasopressin may be related to receptor types similar to those mediating its pressor effects. Nevertheless, the antinociceptive action of vasopressin does not appear to be secondary to its pressor activity, since phenylephrine failed to induce an antinociceptive effect at a dosage that mimicked the pressor response to vasopressin. These results are in concert with a growing body of evidence suggesting that vasopressin may be one of several nonopiate peptides that play a role in the modulation of pain sensitivity.
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PMID:Vasopressin-induced antinociception: an investigation into its physiological and hormonal basis. 686 6

A synthetic analogue, deamino-ethyl-oxytocin, which competitively inhibits vasopressin action on uterine activity both in vitro and in animal experiments was developed. The uterine effect of this analogue was studied during the recording of intrauterine pressure in 16 gynecologically healthy women. Increased uterine activity and dysmenorrhea-like pain was induced by infusing lysine vasopressin in a dose of 0.08 microgram/min. Deamino-ethyl-oxytocin inhibited vasopressin action, the threshold dose being approximately 200 micrograms given as a single intravenous injection for about 20 minutes. When given intranasally the drug was also shown to be effective in inhibiting vasopressin-induced uterine activity and symptoms. These results suggest that deamino-ethyl-oxytocin could be of therapeutic value in primary dysmenorrhea, a condition associated with increased vasopressin secretion.
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PMID:Inhibition of vasopressin effects on the uterus by a synthetic analogue. 687 87

Lysine acetylsalicylate (LAS) is a soluble salt of acetylsalicylic acid and can be given parenterally. LAS 12.5 mg kg-1 and 25 mg kg-1 were compared with oxycodone 0.15 mg kg-1 in the treatment of pain after operation in 60 patients undergoing varicose vein surgery. Both treatments almost completely relieved moderate to severe pain for the 3-h observation period. The time until the peak of action was longer after LAS (60-90 min) than after oxycodone (30-60 min). No significant differences were found between the smaller and larger doses of LAS, suggesting a plateau effect. Further clinical experiments with LAS using i.v. mode of administration and other pain models are warranted.
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PMID:Comparison of i.m. lysine acetylsalicylate and oxycodone in the treatment of pain after operation. 700 Jan 6

Vasopressin (VP) neurons project to extrahypothalamic sites involved in pain perception, including the substantia gelatinosa of the spinal cord as well as the trigeminal and vagus nerves. Previous studies have reported antinociceptive activity following intracerebroventricular (ICV) or subcutaneous (SC) VP injections (16-100 microgram) on the tail-flick test while hyperalgesia has been observed in rats either genetically deficient in VP or treated with antisera to VP. The present study investigated whether nanogram (ng) doses of lysine-vasopressin (LVP) and a VP analogue with prolonged activity increased tail-flick latencies and flinch-jump thresholds following ICV or SC injections. LVP (150 and 500 ng, ICV) significantly increased tail-flick latencies while the analogue 1-deamino-(8-Lys-N epsilon-(Gly-Gly-Gly))-VP (500 ng, ICV) produced more powerful and prolonged analgesia. In contrast, latencies were not increased by SC injections of LVP (150-1500 ng). Further, flinch-jump thresholds were affected minimally by either ICV or SC LVP injections. These data suggest a role for VP in pain modulation and a central site of this action.
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PMID:Central antinociceptive effects of lysine-vasopressin and an analogue. 713 29

Electrical stimulation pain thresholds and EMG activity were studied, using the vastus medialis muscle of healthy control subjects and of patients with osteoarthritis of the knee. Various categories of sensation elicited by progressive increases of the level of electrical stimulation (including one defined as pain threshold) were defined for control subjects. For patients, muscular pain thresholds differed significantly for the two sides of the body; they were usually lower in the more affected side. Involuntary activity of certain motor units and delayed relaxation following voluntary contraction were consistently observed in patients. The involuntary activity was affected by limb position and by mechanical stimulation of tender areas of the muscle or joint. Differences in pain threshold between the two sides were significantly reduced and the EMG pattern became normal following treatment with injections of local anaesthetic into tender periarticular areas and systemic administration of lysine acetylsalicylate. In standing patients, abnormal EMG activity (which was characteristically sensitive to body load and its variations) was found. Injection of a local anaesthetic into the joint cavity was able to induce a rapid subjective improvement and a consistent reduction of EMG activity.
Pain 1981 Feb
PMID:Pain thresholds and electromyographic features of periarticular muscles in patients with osteoarthritis of the knee. 723 12

1 In 17 gynaecological patients with postoperative pain the analgesic efficacy of intravenous lysine salicylate 1.8 g (corresponding to acetylsalicylic acid (ASA) 1.0 g) and dipyrone 1.0 g were compared in a double-blind randomized study. 2 In the ASA group, mean pain relief and pain intensity difference scores reached a maximum 30 min after drug administration and remained at this level for the next 90 minutes. 3 In the dipyrone group, these scores reached their peak 60 min after drug administration and seemed to fall off during the next hour. 4 The mean pain relief and intensity difference scores were greater following aspirin than dipyrone. However, firm conclusions cannot be drawn from the results of this small study.
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PMID:Comparison of intravenous acetylsalicylic acid and dipyrone in postoperative pain: an interim report. 743 74

The anti-inflammatory and analgesic profile of a new topical foam formulation of ketoprofen lysine salt (CAS 57469-78-0, Artrosilene Schiuma, KLS-foam) was characterized in comparison with marketed gel formulations containing KLS (KLS-gel) or diclofenac diethylammonium salt (DCF-gel). KLS-foam dose-dependently inhibited oedema formation and hyperalgesia induced by subplantar injection of carrageenan or substance P, being more potent than KLS-gel. At equieffective anti-inflammatory doses, KLS-foam provided a more pronounced analgesic effect than DCF-gel. KLS-foam also markedly inhibited exudate formation and prostaglandin production induced by subcutaneous implantation of carrageenan soaked sponges. In carrageenan induced paw inflammation, KLS-foam provided the same anti-inflammatory effect as orally administered KLS, but induced significantly less gastric damages. Oral administration of KLS resulted in sustained systemic absorption of ketoprofen, whereas after topical application of KLS-foam no appreciable ketoprofen plasma levels were detected. These data support the anti-inflammatory and particularly the analgesic effectiveness of the new foam formulation of KLS, a finding that, together with the high gastric tolerability, further emphasizes the usefulness of KLS-foam in the treatment of localized flogistic diseases and associated pain.
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PMID:Effects of a new foam formulation of ketoprofen lysine salt in experimental models of inflammation and hyperalgesia. 754 96

The release of prostanoids from rat brain, gastric mucosa, lungs and kidneys incubated ex vivo has been investigated for up to 5 h after oral administration of 10 mg/kg lysine clonixinate or 1 mg/kg ketorolac tromethamine. Additionally, 60 min after drug administration, a time point of near-maximal inhibition of prostanoid release, the effects of 2.5, 10 and 30 mg/kg lysine clonixinate and of 0.0225, 0.15 and 1 mg/kg ketorolac tromethamine were compared. In all organs investigated both drugs inhibited fatty acid cyclooxygenase (COX) in a dose-dependent manner, but ketorolac tromethamine was more potent and had a longer-lasting effect than lysine clonixinate. While the ID50 values for lysine clonixinate were in the same order of magnitude for all 4 organs investigated, ketorolac tromethamine exhibited some organ selectivity with a particularly high activity in the kidneys. This effect might be related to the renal toxicity of ketorolac tromethamine. On the other hand, the difference in potency was smallest in brain suggesting that inhibition of central prostanoid biosynthesis could contribute to the rapid and effective inhibition of pain by both drugs. IC50 values for inhibition of purified COX-1 and COX-2 in vitro were slightly lower for lysine clonixinate (2.4 and 24.6 micrograms/ml, respectively) than for ketorolac tromethamine (3.7 and 25.6 micrograms/ml, respectively).
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PMID:Effects of lysine clonixinate and ketorolac tromethamine on prostanoid release from various rat organs incubated ex vivo. 760 99


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