Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0030193 (pain)
 261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Intravenous administration of acetyl salicylate of lysine, a soluble salt of aspirin, reduced in rats the firing discharge of thalamic neurones, evoked by noxious stimuli. Concomitantly, concentrations of 5-hydroxyindole acetic acid increased, while those of met-enkephalin-like immuno-reactive derivatives were decreased in several areas of the brain. Similar electrophysiological and biochemical responses were obtained by administering tryptophan or 5-hydroxytryptophan plus carbidopa. The effect of aspirin on the evoked firing of the thalamic neurones was counteracted by pretreating the animals with metergoline. On the other hand, naloxone did not antagonize the inhibitory effect of aspirin and 5-hydroxytryptophan on pain-induced neuronal excitation. These data indicate that a serotonin-, but not a naloxone-sensitive opiate mechanism, may be relevant for aspirin-mediated antinociception.
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PMID:Effect of aspirin on serotonin and met-enkephalin in brain: correlation with the antinociceptive activity of the drug. 245 74

The effect of repeated doses of 1.8 g lysine acetyl salicylic acid (LAS) i.v. on severe pain secondary to acute renal colic (ARC) was studied in 45 consecutive patients. Clinically acceptable analgesia was obtained in 65% of the cases. No additional pain relief was achieved with the combination of pethidine 100 mg i.v. + metoclopramide 10 mg, i.m. (narcotics). Pain relief occurred within five minutes in one third of the patients while in the rest within 30 minutes. Significant reduction of systolic blood pressure (mean +/- S.D.) 23.8 +/- 19.5, pulse rate (mean +/- S.D.) 19.5 +/- 10.1 and vomiting were noted in patients who had pain relief. The incidence of nausea has increased after LAS administration. No other side effects were observed. LAS might therefore be applied as a first-hand alternative to narcotics for the treatment of ARC.
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PMID:Lysine acetyl salicylic acid in acute renal pain. 250 91

Inhibition of hemagglutinin (HA) activity in a membrane fraction of Bacteroides gingivalis was examined using various compounds. Leupeptin and anti-pain inhibited the HA activity at nM order. This potency was lost when the aldehyde group of leupeptin was converted to an alcohol moiety. Irreversible protease inhibitors, tosyl-L-lysine chloromethyl ketone (TLCK), p-chloromercuribenzoate (PCMB), and N-ethylmaleimide (NEM) were also inhibitory. From the inhibition experiments, we speculate that the HA possesses protease activity and that the same site of the molecule participates in the erythrocyte binding and the substrate binding.
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PMID:Possibility of Bacteroides gingivalis hemagglutinin possessing protease activity revealed by inhibition studies. 254 90

Free plasma tryptophan levels in patients with fibrositis syndrome were measured by Moldofsky and Warsh with the view that the pathogenesis of fibrositis syndrome might involve a functional deficiency of serotonin. The hypothesis was supported by the finding of an inverse relationship between tryptophan concentration and the severity of musculoskeletal pain. Our study examined the total serum amino acid pool in fibrositis syndrome. Twenty patients with primary fibrositis syndrome and matched normal controls were evaluated clinically. After denaturation of macromolecules, serum amino acids were quantitated by automated analysis. Patients with fibrositis syndrome exhibited significantly lower levels of total serum tryptophan (p = 0.002), as well as 6 other amino acids: alanine (p less than 0.0005), histidine (p = 0.001), lysine (p = 0.02), proline (p = 0.039), serine (p = 0.028), and threonine (p = 0.013). These findings support the serotonin deficiency hypothesis for fibrositis syndrome pathogenesis but also imply a more generalized defect in amino acid homeostasis among affected individuals.
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PMID:Serum amino acids in fibrositis/fibromyalgia syndrome. 260 10

N2-[(N-Acetylmuramoyl)-L-alanyl-D-isoglutaminyl]-N6-stearoyl-L-lysine (MDP-Lys(L18), muroctasin), a derivative of muramyl dipeptide, is known to have the activity to augment the number of white blood cells (WBC) via colony-stimulating factor. Muroctasin has been expected to be applied to leukopenia caused by anticancer chemotherapy. When WBC decreased to less than or equal to 3,000/mm3 after the 1st course of chemotherapy, 131 patients with lung cancer, who were previously classified by the combination regimens of chemotherapy, were enrolled in the study and randomized into 3 groups, 200 micrograms (H), 100 micrograms (L) and untreated control (C) groups. The patients were then subcutaneously treated once daily for 6 consecutive days. WBC and its differential count were measured on Days 4, 7 and 15 after commencement of the study. WBCs in H and L groups were recovered greater than in C group. In WBC differential count, the recovery of neutrophil was prominent in muroctasin treated groups. The portion of immature neutrophil in the bone marrow was also increased by muroctasin treatment. A restorative effect on WBC and neutrophil counts was also confirmed only in the second course of H group. On the other hand, fever and pain in the injected site as side effects were common in the H group and L group in both of courses. In this study, the usefulness of muroctasin in leukopenia was suggested when administered at dosages of 200 micrograms for 6 days.
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PMID:Restorative effect of muroctasin on leukopenia caused by anticancer chemotherapy in lung cancer. Comparative study by envelope method. 271 48

Postoperative pain management protocols have been examined in a total of 212 patients from three Spanish hospitals. Metamizole was the analgesic drug most frequently prescribed (50%) followed by pethidine (18.4%). To a lesser degree, aspirin, pentazocine, lysine acetylsalicylate, paracetamol and buprenorphine were used. Important differences among the hospitals were found when choosing the analgesic. The dosage prescribed varied and in general, drugs were prescribed at lower doses than the daily defined dose (DDD). Intramuscular route was the most used. Only 27.6% of the patients received the prescribed doses and 43.3% received a lower one. This was basically due to a greater interval of dosing. 14.6% of the patients were painless while 25.5% showed intense and unbearable pain. From this study one may conclude that when metamizole is preferably used as an analgesic drug, it is given at a smaller dose than that recommended and in addition, nurses decrease even more the doses. An important number of patients were found with intense pain even though analgesic drugs were given.
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PMID:[Analysis of the treatment of postoperative pain at 3 hospitals]. 274 May 43

The pharmacokinetic properties of ibuprofen p.o. given either as a lysine salt or as acid to eight young, healthy male volunteers was investigated. Ibuprofen lysinate, administered after overnight fasting, produced peak plasma concentrations significantly earlier and higher than ibuprofen acid. A similar difference was observed when the drugs were given following a standardized breakfast. Under these conditions the lat-time was significantly shorter for the lysine salt than for the acid. The pharmacokinetic differences are likely to result from the faster dissolution rate of ibuprofen lysinate. They indicate that the administration of ibuprofen as lysine salt before meals may be advantageous if rapid and reliable onset of pain relief is required.
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PMID:Therapeutically relevant differences in the pharmacokinetical and pharmaceutical behavior of ibuprofen lysinate as compared to ibuprofen acid. 277 20

Pharmacological properties of LFP83, a non-steroidal analgesic and antipyretic drug, were studied in mice, rats and rabbits. LFP83 is a prodrug of flurbiprofen (FP) which is its active major metabolite in vivo. In experimental models of acetic acid writhing, the Randall and Selitto method, arthritic pain, yeast fever, LPS fever, carrageenin edema and adjuvant arthritis, LFP83 (i.v.) showed remarkable analgesic, antipyretic and antiinflammatory activities; and it was more potent than ketoprofen (i.m.) and aspirin DL-lysine (i.v.). The analgesic activity of LFP83 was equal to or more potent than that of pentazocine, and its duration was longer than those of aspirin DL-lysine and pentazocine. In addition, the analgesic potency of LFP83 was approximately the same or more potent than that of FP (p.o.), and the onset of this analgesic effect began earlier. On the other hand, the ulcerogenic activity of LFP83 on rat gastric mucosa was less than that of FP (p.o.) in both single and consecutive (7 days) administrations. The safety index (UD50/ED50) of LFP83 was three to ten-fold higher than that of FP (p.o.). As mentioned above, LFP83 is a potent analgesic, antipyretic and antiinflammatory drug; and in comparison to oral FP, it has a more potent and immediate effect, weak gastric irritation and high safety index.
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PMID:[Pharmacological studies of a non-steroidal analgesic and antipyretic drug of LFP83]. 278 48

The opioid nature of kentsin (Thr-Pro-Arg-Lys) and its ability to alter pain perception and intestinal transit were examined. Kentsin (30,000 nM) did not inhibit electrically stimulated contractions of the guinea pig ileum (GPI) or mouse vas deferens (MVD), nor did it cause a rightward displacement of the inhibitory concentration-response curves of the mu-selective opioid agonist PL017 in the GPI or the delta-selective agonist DPDPE in the MVD. Kentsin (10,000 nM) did not displace [3H] naloxone from rat brain homogenates. These results indicate that kentsin lacks opioid agonist and mu and delta opioid antagonist properties and does not bind to opioid receptors. In vivo, kentsin produced dose-dependent analgesia in both the hotplate and abdominal stretch tests when administered intracerebroventricularly (ICV) and intrathecally but not intravenously. The central analgesic effect of kentsin was partially antagonized by the opioid antagonist naloxone. Kentsin inhibited intestinal transit in a dose-dependent manner after ICV administration only. The intestinal antitransit effect of kentsin was not blocked by pretreatment with naloxone. These results suggest that kentsin acts centrally to produce both opioid and non-opioid effects. Further, the opioid-mediated analgesic effects of kentsin involve mechanisms other than direct interaction with opioid receptors.
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PMID:Kentsin: tetrapeptide from hamster embryos produces naloxone-sensitive effects without binding to opioid receptors. 281 32

A double-blind study was designed to compare the efficacy and tolerability of pirprofen and lysine soluble aspirin administered by iontophoresis to 80 patients with various painful rheumatic diseases. Treatment lasted two weeks, with five administrations a week, each lasting 20 minutes (direct current; mean intensity, 2.3 mA). After five administrations, patients showed significant improvement in pain at rest and on movement, with no significant differences between pirprofen and aspirin. Final results were excellent or good in about 75% of the patients treated and functional improvement was satisfactory in about 80%. There were no side effects.
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PMID:Iontophoretic administration of pirprofen or lysine soluble aspirin in the treatment of rheumatic diseases. 285 98


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