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)

An efficient narco-analgesia is given by the association of two drugs: -- diazepam (Valium): a benzodiazepine with an anxiolytic and myoresolutive effect, inducing sleep and giving amnesia; -- lysine acetylsalicylate (Aspegic) giving an analgesia inferior to that of morphinomimetic drugs but not inducing respiratory depression. These two drugs are given in an intravenous catheter. Their effects last about 20 minutes - vomiting is rare. The authors report their experience of 50 cases and think that this technique is recommended in remote medical units for moderately painful and short duration operations.
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PMID:[Valium-aspegic association. Its value in a remote medical unit (author's transl)]. 678 84

We have compared the analgesic properties in post-operative pain using Morphine (3 mg) injected in the extradural space and I.V. Lysine acetil salicilate (ASL) (1.8 g). Extradural morphine is much more effective in eliminating pain and in prolonging the analgesia. Insignificant the side effect for both treatments. The authors underline the possibility of dependence with extradural morphine especially in those cases when morphine is repeated more than 2-3 times.
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PMID:[Comparison between extradural morphine and lysine acetylsalicylate in the treatment of postoperative pain]. 679 27

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

The amino acid sequence of a newly isolated pentapeptide, neo-kyotorphin from bovine brain was synthetically verified to be Thr-Ser-Lys-Tyr-Arg corresponding to the C-terminal portion of hemoglobin alpha-chain. The synthetic neo-kyotorphin showed the dose-dependent analgesia in mice which was approximately equal to that of Leu-enkephalin.
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PMID:Neo-kyotorphin (Thr-Ser-Lys-Tyr-Arg), a new analgesic peptide. 685 39

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

1. The analgesic effect of clonixinate of L-lysine (Clx) in the nociceptive C-fiber reflex in rat and in the writhing test in mice is reported. 2. Clx was administered by three routes, i.v., i.t. and i.c.v., inducing a dose-dependent antinociception. 3. The antinociceptive effect of Clx was 40-45% with respect to the control integration values in the nociceptive C-fiber reflex method. 4. The writhing test yielded ED50 values (mg/kg) of 12.0 +/- 1.3 (i.p.), 1.8 +/- 0.2 (i.t.) and 0.9 +/- 0.1 (i.c.v.) for Clx administration. 5. Ondansetron was not able to antagonize the antinociception response of Clx in the algesiometric tests used. 6. Chlorophenilbiguanide did not produce any significative change in the analgesic effect of Clx in the nociceptive C-fiber reflex method. 7. It is suggested that the mechanism of action of the central analgesia of Clx is not mediated by 5-HT3 subtype receptors.
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PMID:The analgesic effect of clonixine is not mediated by 5-HT3 subtype receptors. 759 Jan 33

In two multicentric randomized, double-blind, parallel design trials the more appropriate dose of ketoprofen lysine salt suppositories, by considering benefit-risk ratio, was determined in children affected by acute inflammatory disease of respiratory or urinary tract with fever and pain. Fifty-three children ranging 6-36 months (infants) randomly assigned to 20, 30, 40 mg dose levels, and 54 children ranging 3-13 years (children) randomly assigned to 40, 60, 80 mg dose levels were included in the studies. Efficacy variables considered were hyperthermia and pain; body temperature was measured rectally, at fixed intervals and pain was evaluated by Maunuskela scale at the same interval times. Standard laboratory test were obtained at the beginning and end of treatment, and blood arterial pressure and heart rate were recorded regularly. Systemic and local tolerability were also determined. In infants all doses were associated with analgesia and temperature reduction; antipyretic effect was statistically significant starting from the first hour (p = 0.007). The dose of 30 mg resulted different from 20 mg dose from third hour (p < 0.05). The appropriate dose that better relate antipyretic and analgesic efficacy with a good tolerability was 30 mg. In children the analgesic and antipyretic efficacy was well established at all doses tested, however the effects were more marked and prolonged at 60 and 80 mg doses, with a better tolerability for 60 mg dose. The tolerability of all doses studied was good. Doses of 30 mg in infants and 60 mg in children correspond to a range of 2.0-3.5 mg of ketoprofen lysine salt for kg body weight, for each administration.
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PMID:[Effects of various dosage of ketoprofen salt suppositories in acute inflammatory disease in infants (3-36 month old) and children (3-13 year old)]. 764 21

In a single-dose, double-blind, parallel-group, single-site study, ibuprofen lysine 200 mg (IBL 200) was compared with acetylsalicylic acid 500 mg (ASA 500) and placebo in 183 patients with moderate-to-severe postoperative dental pain. The relative onset of analgesic response, duration and degree of analgesia, and safety were assessed over a 6-hour postdose period. Analgesic efficacy was assessed by patient self-rating of pain intensity, pain relief, time to meaningful pain relief, global evaluation, and requirement for additional analgesic medication; both IBL 200 and ASA 500 were significantly more effective than placebo. IBL 200 also had a significantly faster onset of action, greater peak and overall analgesic effect, and longer duration of analgesia than ASA 500. All treatments were generally well tolerated.
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PMID:Comparison of single-dose ibuprofen lysine, acetylsalicylic acid, and placebo for moderate-to-severe postoperative dental pain. 792 12

Delivery through the blood-brain barrier of opioid peptide-based therapeutic agents may be achieved with the use of conjugation of avidin and blood-brain barrier transport vectors. However, this drug delivery strategy requires that 1) the peptide is monobiotinylated and 2) the peptide is biologically active after cleavage of a disulfide linker and peptide release from the avidin-vector conjugate. Whether these criteria may be successfully fulfilled was examined in the present studies. The highly mu receptor-specific dermorphin analog, Tyr-D-Arg-Phe-Lys-NH2 (DALDA), was selectively monobiotinylated at the epsilon-NH2 group of Lys4 with the cleavable biotin linker, sulfosuccinimidyl-2-(biotinamidoethyl) 1,3'-dithioproprionate to obtain biotinylated DALDA (bio-DALDA). The N-terminal alpha-NH2 group of the peptide was protected during biotinylation with the N-9-fluorenylmethoxycarbonyl group. Cleavage of the disulfide bridge yielded the desbiotinylated derivative, desbio-DALDA. The identity of these peptides was verified by secondary ion mass spectrometry. In receptor binding assays with 3H-Tyr-D-Ala-Gly-Phe-(N-Me)-Gly-ol, the Kis of DALDA, bio-DALDA and desbio-DALDA for mu opioid receptors were determined to be 2.3 +/- 0.4, 6.5 +/- 1.1 and 4.0 +/- 0.9 nM, respectively. Binding of bio-DALDA to avidin resulted in a Ki of 14.5 +/- 2.4 nM. The i.c.v. administration of DALDA and desbio-DALDA induced potent and long-lasting analgesia in the rat tail-flick assay. It was found that 1 microgram of DALDA was equipotent to 3 micrograms of desbio-DALDA and 20 micrograms of morphine. The analgesic effect could be blocked by naloxone pretreatment. In conclusion, these studies 1) described methods for the preparation of a biologically active monobiotinylated mu opioid receptor-specific ligand and 2) demonstrated the advantages of using cleavable biotinylation of opioid peptides because the affinity of desbio-DALDA for the receptor approximated the affinity of DALDA and had a 3- to 4-fold higher affinity than did the bio-DALDA-avidin complex.
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PMID:Synthesis and bioactivity of monobiotinylated DALDA: a mu-specific opioid peptide designed for targeted brain delivery. 811 91

1. A cross-over single blind study examined the possible central effects of non-opioid analgesic drugs on the trigeminal reflexes. 2. The corneal reflex and blink reflex (R1, R2) were recorded electromyographically and response areas measured in healthy volunteers before and after intramuscular injection of piroxicam (40 mg); and after intravenous injection of lysine acetylsalicylate (500 mg). After the last drug recording the subjects received intravenous naloxone (2 mg) followed 5 minutes later by further reflex testing. Saline was used as a placebo in control experiments. 3. Both analgesics reduced the corneal reflex: piroxicam induced a 27% and lysine acetylsalicylate a 21% a reduction that naloxone did not reverse. Neither drug reduced the early or the late component of the blink reflex. 4. The marked inhibitory changes that the two non-narcotic analgesics produced on the corneal reflex--a nociceptive response--indicate a centrally-mediated action. 5. Naloxone's failure to reverse the induced analgesia argues against opiate receptor mediation.
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PMID:Analgesic-antiinflammatory drugs inhibit orbicularis oculi reflexes in humans via a central mode of action. 811 66


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