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)

Piroxicam, a NSAID with a proved analgesic and antiphlogistic efficacy, largely used in rheumatic-orthopedic pathologies, has an antalgic action also in extra-rheumatic pathologies, such as postoperative and dental pain and primary dysmenorrhea. This is probably due both to a peripheral mechanism, at the injured site level, which is particularly widespread, and goes from prostaglandin inhibition to suppression of the synthesis of different algesiogenic substances (oxygen free radicals, lytic enzymes), and to a direct non endorphin-mediated action at central level. The data base considered in this review, concerning piroxicam in extra-rheumatic analgesia, is of about 2,500 patients, in 26 clinical studies, mostly with an experimental double-blind placebo-controlled design or vs other NSAIDs. The doses ranged from 5 to 40 mg in a single administration: the doses of 20 and 40 mg showed an immediate analgesic effect, with the onset of analgesia within 30 min./1 hour from the administration. Analgesic activity was intense, comparable or superior to that of other drugs (aspirin, codeine, other NSAIDs) and more prolonged, often lasting as long as 24 hours. Tolerability of this data base was very satisfactory and comparable to that of the placebo, incidence of side effects being negligible.
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PMID:[Piroxicam in analgesia]. 182 75

Fifty patients were allocated randomly to receive placebo or piroxicam 40 mg, 2.5 h before surgical removal of lower third molars under general anaesthesia. A significantly greater number of patients in the piroxicam group did not require opioid analgesia after operation (P less than 0.05). The piroxicam group also required fewer doses of paracetamol in the first 24 h after recovery from anaesthesia (P less than 0.05), and the time from recovery to first postoperative analgesia was longer in those patients who had received piroxicam (P less than 0.05). Piroxicam did not significantly prolong the duration of recovery from anaesthesia.
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PMID:Preoperative piroxicam for postoperative analgesia in dental surgery. 224 16

The severity of postoperative dental pain can be variable depending on the type of procedure. Both centrally acting and peripherally acting analgesics, such as nonsteroidal anti-inflammatory drugs (NSAIDs), aspirin, and acetaminophen are used. NSAIDs are generally better suited to ambulatory outpatients. The most commonly used postoperative dental pain model includes patients who have undergone surgical removal of impacted third molar teeth. The analgesic efficacy of piroxicam in this pain model was studied both in the United States and in foreign centers. The foreign studies suggest that piroxicam at 20-mg doses produces analgesia in patients with postoperative dental pain. Seven single-dose, randomized, double-blind trials of 798 patients in the United States more clearly evaluated the efficacy of piroxicam. These studies used various doses of piroxicam (5, 10, 20, and 40 mg), aspirin 648 mg, and placebo. Safety results showed that a wide range of piroxicam doses were safe when administered in single doses. Although neither piroxicam 5 mg nor 10 mg produced clinically significant analgesia, 20-mg and 40-mg doses were significantly superior to placebo and both were comparable with aspirin 648 mg over the initial six hours. Piroxicam 20 mg and 40 mg, however, produced significantly longer durations of analgesia than aspirin 648 mg, and it appears that the analgesic effect of piroxicam may extend for up to 24 hours in a substantial proportion of patients.
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PMID:Analgesic efficacy of piroxicam in postoperative dental pain. 328 10

Piroxicam-beta-cyclodextrin is a complex of the established nonsteroidal antiinflammatory drug (NSAID) piroxicam and an inert cyclic macromolecule, beta-cyclodextrin. In clinical trials in patients with rheumatic diseases or pain arising from other conditions, it was as effective an analgesic as standard piroxicam, and showed a faster onset of action on the first day of treatment. In short term pharmacodynamic studies in healthy volunteers, piroxicam-beta-cyclodextrin was equivalent to or tended to show less gastrointestinal mucosal toxicity than standard piroxicam, as assessed by endoscopy and faecal blood loss. However, no data are available on its comparative gastrointestinal mucosal effects from long term clinical trials using similar measures. Preliminary findings from a clinical study suggest piroxicam-beta-cyclodextrin caused fewer gastroduodenal lesions than tenoxicam. As with other NSAIDs, the majority of adverse events associated with piroxicam-beta-cyclodextrin in clinical trials were gastrointestinal in origin, with epigastric pain, heartburn and nausea the most common. Thus, piroxicam-beta-cyclodextrin is an effective agent in patients with rheumatic diseases or other pain states. When rapid analgesia is required in the initial treatment of acute pain, the faster onset of action of piroxicam-beta-cyclodextrin may be an advantage over the parent compound; however, this is unlikely to be important during long term therapy. The results of further long term trials are awaited before firm conclusions can be reached regarding the gastrointestinal tolerability of piroxicam-beta-cyclodextrin compared with that of standard piroxicam and other NSAIDs.
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PMID:Piroxicam-beta-cyclodextrin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in rheumatic diseases and pain states. 753 98

Two hundred ninety-eight patients with post-operative pain after the surgical removal of an impacted third molar were randomly assigned, on a double-blind basis, to receive a single oral dose of piroxicam 20 mg, or piroxicam-beta-cyclodextrin equivalent to 20 mg piroxicam, or paracetamol 500 mg, or placebo. Using a semi-quantitative self-rating scale, patients rated their pain and its relief at 30-min intervals for the first 2 h, and then hourly for 4 h after treatment administration. All active medications were reported to be significantly superior to placebo. The three active drugs were comparable for the degree of analgesia up to the third hour, after which the effect of paracetamol decreased significantly as compared to piroxicam-beta-cyclodextrin and piroxicam. Piroxicam-beta-cyclodextrin and paracetamol were more rapid than piroxicam in inducing analgesia. The tolerability for the active drugs was comparable to that for placebo.
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PMID:Evaluation of piroxicam-beta-cyclodextrin, piroxicam, paracetamol and placebo in post-operative oral surgery pain. 767 75

An open comparative study was carried out to evaluate the efficacy and safety of piroxicam FDDF, for sublingual administration, versus naproxen in the treatment of osteoarthritis. Sixty-one patients with acute-phase osteoarthritis involving various joints are reported. They were treated with 20 mg/day piroxicam FDDF or with 1000 mg/day naproxen for a total of 4 weeks. Drug efficacy was evaluated on the base of the variation of spontaneous pain, pain on motion, functional limitation and capacity to perform a specific activity. The intensity of spontaneous pain on the first day showed a statistically significant improvement with both drugs, but the onset of analgesia was only after 15 minutes with piroxicam and after 1 hour with naproxen. The improvement in pain intensity increased on the first day and until the 7th day with both drugs, but the comparative analysis between the analgesic efficacy of the two treatments proved to be favourable to piroxicam. On the 7th day, pain on motion and the capacity to perform a specific activity showed a statistically significant improvement with both drugs, but the comparative analysis between the two treatments proved to be favourable to piroxicam. The two drugs showed the same efficacy in functional restriction. The local and systemic tolerability of piroxicam was good. Only 5 patients experienced 6 systemic side-effects, and 1 patients showed local side-effects, but 11 patients of the naproxen group showed 12 systemic side-effects. Thus piroxicam showed a better analgesic and anti-inflammatory efficacy than naproxen. Piroxicam proved to have a better systemic tolerability than naproxen. The local tolerability of piroxicam FDDF was good.
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PMID:[Fast-dissolving sublingual tablets of piroxicam versus naproxen in the treatment of recurrent acute osteoarthrosis. Multicenter clinical trial]. 819 49

In a double-blind, placebo-controlled study, the non-steroidal anti-inflammatory drug, piroxicam, in combination with alfentanil given in a patient-controlled analgesia system, was compared with alfentanil alone given by the same route for analgesic effect, side effects and acute phase reaction over a 4-day period following anterior cruciate ligament reconstruction of the knee. The patients receiving piroxicam had lower pain scores and consumed less alfentanil. There were no differences with regard to side effects between the two treatment groups, apart from significantly more sedation at 08.00 h on the first postoperative day in the non-piroxicam group. Piroxicam did not influence either the levels of interleukin-6 or the acute phase response to surgery.
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PMID:Systemic piroxicam as an adjunct to patient-controlled analgesia with alfentanil for postoperative pain relief. 875 59

A randomised, double-blind placebo-controlled trial was conducted to compare the analgesic efficacy of piroxicam as Feldene "Melt' with diclofenac suppositories following day case wisdom tooth extraction. Piroxicam was found to be equivalent to diclofenac in speed of onset and efficacy when given 1 h prior to surgery with no significant adverse effects. It is therefore possible to confer the benefits of postoperative analgesia from a non-steroidal anti-inflammatory drug whilst avoiding the inconvenience of the rectal route of administration.
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PMID:Postoperative analgesia in dental day case surgery. A comparison between Feldene "Melt' (piroxicam) and diclofenac suppositories. 879 27

Piroxicam (Feldene) is indicated for osteoarthritis and rheumatoid arthritis but not analgesia due to its delayed onset of pain relief. Piroxicam-beta-cyclodextrin (PBCD) was developed for pain indication by virtue of the increased absorption rate of piroxicam. Forty-eight patients received a single dose of PBCD or Feldene (10, 20, and 40 mg) in a randomized study, and piroxicam plasma concentration and pain relief were measured. The purpose of the study was to investigate the PK-PD relationship of piroxicam, determine the optimal dose, and evaluate the effect of increased absorption rate on analgesic effect of piroxicam for the pain model studied. The pharmacokinetic data were best described by a two-compartment model with first-order absorption. The absorption rate of PBCD (5/h) was faster than Feldene (1.41/h). Pain relief was found to be increasing with drug concentration in a hypothetical effect compartment (Emax model). The estimated half-life of the equilibration between plasma and effect site was about 2.34 hours. Monte Carlo simulation showed that the time when at least 50% of the patients have a 75% probability of achieving meaningful pain relief (pain intensity difference (PID > or = 1) for PBCD and Feldene at a dose of 20 mg was about 0.5 and 1.5 hours, respectively. PBCD demonstrated an advantage with an onset of pain relief 1 hour earlier than Feldene.
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PMID:Comparative population pharmacokinetic-pharmacodynamic analysis for piroxicam-beta-cyclodextrin and piroxicam. 1107 11

Piroxicam is a non-steroidal anti-inflammatory drug that is characterized by low solubility and high permeability. The purpose of the study was to investigate the in vitro and in vivo performance of the semi-solid dispersion prepared with Gelucire 44/14 and Labrasol into hard gelatin capsules (GL) for enhancing the dissolution rate of the drug. The results were evaluated by comparing with pure piroxicam filled into hard gelatin capsules (PP) and a commercially available tablet dosage form containing a piroxicam:beta-cyclodextrin complex (CD). The in vitro dissolution testing of the dosage forms was performed in different media (simulated gastric fluid, pH 1.2; phosphate buffers, pH 4.5 and 6.8; and water). Amongst the dosage forms, GL provided at least 85% piroxicam dissolution within 30 min in each of the media, behaving like a fast-dissolving immediate release drug product. Oral bioavailability of 20 mg piroxicam in GL, CD, and PP was compared after administration of a single dose to eight healthy volunteers. Three treatments were administered in crossover fashion, separated by a washout period of 2 weeks. Piroxicam was monitored in plasma by high-performance liquid chromatography. The apparent rate of absorption of piroxicam from GL (Cmax=2.64 micrograms/ml, tmax=82.5 min) was significantly higher than that of the PP (Cmax=0.999 micrograms/ml, tmax=144 min) (P<0.05) and similar to that of CD (Cmax=2.44 micrograms/ml, tmax=120 min) (P>0.05). The relative bioavailability values as the ratios of mean total AUC for GL relative to PP and CD, were 221 and 98.6%. Piroxicam is characterized by a slow and gradual absorption via the oral route and this causes a delayed onset of therapeutic effect. Thus, plain piroxicam preparations are not indicated for analgesia. The results of the in vivo study revealed that the GL dosage form would be advantageous with regards to rapid onset of action, especially in various painful conditions where an acute analgesic effect is desired.
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PMID:Enhanced bioavailability of piroxicam using Gelucire 44/14 and labrasol: in vitro and in vivo evaluation. 1460 90


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