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)

1. The effect of administration of thyroxine or thyroidectomy on the pharmacological action of (+)-amphetamine, caffeine, hexobarbitone and morphine was determined in rats or mice.2. Locomotor activity induced by (+)-amphetamine or caffeine was increased by hyperthyroidism and decreased by hypothyroidism.3. The LD50s of (+)-amphetamine and caffeine in hyperthyroid rats were 1/30 and 2/5 that of control rats. With each drug, the LD50 regression lines in hyperthyroid and control rats were not parallel, suggesting that hyperthyroidism modifies the mechanism of the toxic effects. Hypothyroidism reduced toxicity to (+)-amphetamine.4. Hexobarbitone sleeping time was prolonged in hyperthyroid male rats, but was shortened in hyperthyroid female rats. In control rats, sleeping time was approximately four times as long in females as it was in males. Ethinyloestradiol treatment and castration also prolonged sleeping time in male rats. No further prolongation was produced by combined administration of thyroxine and ethinyloestradiol, but thyroxine further prolonged the sleeping time of castrated rats indicating that its mode of action in producing these changes is not mediated via sex hormones.5. In contrast to rats, a sex difference in the duration of action of hexobarbitone was not found in mice. Thyroxine prolonged sleeping time equally in each sex.6. Analgesia induced by morphine in mice was unaffected by hyperthyroidism. No increase in sedative or ;Straub tail' activity could be detected, but toxicity was increased when higher doses of morphine were used.7. The mechanism by which thyroid hormones produce these changes in sensitivity to centrally acting drugs is discussed. It is suggested that the effects of thyroxine vary according to whether the mode of action of the drug or its metabolism is modified.
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PMID:The effect of thyroid hormones on the action of some centrally acting drugs. 553 41

In C57BL/6 mice caffeine antagonized morphine-induced hyperactivity. This effect was most evident when caffeine was used in doses that slightly increased locomotor activity. Given at the same dose caffeine did not affect morphine-induced analgesia. Two possibilities of explanation of this effect are discussed: action of caffeine on dopaminergic mechanisms responsible for morphine-induced running fit through its effect on cyclic AMP level, and a direct action of caffeine on delta opiate receptors involved in the stimulatory effect of morphine.
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PMID:Caffeine interferes with morphine-induced hyperactivity but not analgesia. 667 94

Our objective was to determine the value of caffeine in combination with acetaminophen in the relief of pain from uterine cramping, episiotomy, and third molar extraction. In the dental study, 173 patients received two or four tablets of 500 mg acetaminophen or the combination of 500 mg acetaminophen and 65 mg caffeine. In the three postpartum studies, 1345 patients received one, two, or three tablets of acetaminophen, the combination, or a placebo. The mean scores for the summary variable percent sum of the pain intensity differences (% SPID) were higher in all for the combination than for acetaminophen alone, and in two studies the null hypothesis of no differences was rejected. The relative potency estimates for % SPID were 1.9, 1.8, and 1.3 for the three studies in which bioassays could be performed and the pooled relative potency was 1.7 with a 95% confidence interval of 1.1 to 3.1. The results were essentially the same among pain models and among patient groups with similar habitual caffeine consumption. Onset of analgesia was also faster with the combination. We conclude that caffeine enhances the analgesic efficacy of acetaminophen.
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PMID:Effect of caffeine on acetaminophen analgesia. 683 29

The analgesic efficacy of a hydrocodone-acetaminophen combination, a codeine-acetaminophen combination, a codeine-APC (aspirin, phenacetin, and caffeine) combination, and a placebo was evaluated in outpatients who had moderate or severe pain after the surgical removal of impacted third molars. Each of the active medications had a significant effect on essentially all measures of total and peak analgesia; they did not differ significantly on any measure of analgesia. Adverse effects were transitory and, in general, appear to have been related to the centrally acting component of each combination analgesic.
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PMID:An evaluation of the analgesic efficacy of three opioid-analgesic combinations in postoperative oral surgery pain. 693 24

A double-blind randomized clinical trial was conducted in eighty-seven patients with mild, moderate or severe dental surgery pain to evaluate the analgesic activity of a single dose of the following compounds: (i) ibuprofen 400 mg, (ii) ACC-30 (a compound containing ASA 375 mg; codeine phosphate 30 mg; caffeine citrate 30 mg), (iii) placebo. Ibuprofen was significantly better than ACC-30 and placebo on almost all pain intensity, degree of relief and duration of analgesia parameters. ACC-30 was not significantly different from placebo on any analgesic measurement. No serious side-effects were reported with any of the study medications.
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PMID:A double-blind comparison of ibuprofen, ASA-codeine-caffeine compound and placebo in the treatment of dental surgery pain. 702 Dec 62

Zomepirac is an analgesic which is closely related chemically to the nonsteroidal anti-inflammatory agent, tolmetin. In short term studies mainly involving patients with acute pain of moderately severity, zomepirac was at least as effective as usual therapeutic doses of aspirin, codeine alone or with aspirin, phenacetin and caffeine, dextropropoxyphene with paracetamol, or orally administered pentazocine. Additionally, zomepirac may provide analgesia comparable to that with standard doses of intramuscular morphine in patients with acute pain of moderate intensity, but in severe pain states strong analgesics may be more appropriate. Zomepirac has also been studied in patients with chronic orthopaedic pain or osteoarthritic pain for up to several months, without the need for increased doses. It appears to be at least as effective as usual doses of aspirin when used in this way, with a lower incidence of some side effects such as gastrointestinal disturbances and hearing disorders. Preliminary studies suggest that zomepirac may also be effective in patients with chronic cancer pain who have not been previously maintained on strong analgesics, but further experience is needed to clarify its usefulness in this difficult treatment area.
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PMID:Zomepirac: a review of its pharmacological properties and analgesic efficacy. 704 54

In this work we show that the pain-induced functional impairment model (PIFIR) can be used with cannulated rats as a useful procedure for pharmacokinetic/pharmacodynamic modelling. This model evaluates analgesia by measuring motor impairment of the right limb after intra-articular administration of uric acid. Time of contact with a rotating cylinder is referred to the control limb. We studied the pharmacokinetic and pharmacodynamics of naproxen after six peroral doses to Wistar rats, and we examined the adjuvant action of caffeine with naproxen. Surgery and blood sampling did not produce any difference on functional impairment either in rats without uric acid or in the dysfunction produced by uric acid. The relation between naproxen plasma concentration and the analgesic effect was obtained with few rats. Caffeine alone did not produce any significant modification in functional impairment but the co-administration significantly increased the effect of naproxen. Plasma levels of naproxen did not change when caffeine was co-administered. The PIFIR model with blood sampling is a suitable method for pharmacokinetic/pharmacodynamic relationship studies and is specially useful to characterize drug-drug interactions.
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PMID:Usefulness of the pain-induced functional impairment model to relate plasma levels of analgesics to their efficacy in rats. 767 28

Opioids, particularly morphine sulfate and fentanyl, continue to be the most commonly used agents for analgesia. Morphine provides greater sedation, and there is less of a problem with rigidity of the chest wall than with fentanyl. Morphine also has a higher level of tolerance than does fentanyl. Table 2 provides considerations for administration of morphine and fentanyl. Sedation for the relief of pain without analgesia is not acceptable. Sedation and analgesia together may be in the baby's best interest. Before any plan of care is implemented, the baby should be evaluated for need based on the amount of current respiratory support versus spontaneous respiration. There is evidence in the research literature that narcotic administration can be safely carried out in the preterm when using intravenous caffeine simultaneously to offset the risk of apnea. Others state that there really is no safe therapeutic window for narcotic administration in the preterm infant, yet the benefits outweigh the respiratory depressant effect. The complication of respiratory depression can be readily dealt with through the administration of neonatal Narcan via the intramuscular, intratracheal, or intravenous routes.
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PMID:Research utilization: pharmacologic management of neonatal pain. 778 25

In the present investigation the intensity of stimulated electro-acupuncture (EA) was measured by electrophysiological collision technique. In the behavioral experiments, by applying the weak electro-acupuncture pulses (50 Hz, 1-1.5mA), not enough to activated A delta afferent fibers, to Yanglingquan and Xuanzhong points, the latency of nociceptive hind limb withdrawal reflex, but not tail-flick latency was prolonged. Administered intraperitoneally, both theophylline and caffeine, P1-purinergic (adenosine) receptor antagonists, could block the electroacupuncture-induced elevation of the nociceptive thresholds in a dose-effect related manner, whereas dipyridamole, an inhibitor of adenosine release, could shorten the after of electro-acupuncture in a dose dependent way. These results suggest that weak electro-acupuncture may induce analgesia and purines appear to be involved in this process.
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PMID:[Involvement of purines in analgesia produced by weak electro-acupuncture]. 783 56

The ability of caffeine to potentiate the analgesic effect of aspirin was studied in the pain-induced functional impairment model in the rat. Female Wistar rats received an intra-articular injection of 30% uric acid in the right hind limb, inducing its dysfunction. Once the dysfunction was complete, animals received aspirin oral doses of 0, 0.55, 0.98, and 1.74 mmol/kg with and without 0.17 mmol/kg of caffeine, and the recovery of functionality over time was considered as an expression of analgesia. Blood samples were drawn simultaneously with hind limb functionality determinations, and plasma concentrations of aspirin, salicylic acid, and gentisic acid were measured by high-performance liquid chromatography. Aspirin induced a dose-dependent analgesic effect. Caffeine alone was ineffective. However, caffeine significantly increased the analgesic effect of aspirin at all doses, without modifying aspirin, salicylic acid, or gentisic acid plasma levels. It is concluded that caffeine potentiates the analgesic effect of aspirin by a pharmacodynamic, but not by a pharmacokinetic mechanism.
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PMID:Potentiation by caffeine of the analgesic effect of aspirin in the pain-induced functional impairment model in the rat. 788 76


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