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)

Diclofenac (CAS 15307-86-5) is a non-steroidal anti-inflammatory drug largely used, mainly to relief pain of various origin. Diclofenac is present on the market as free acid, as sodium salt (CAS 15307-79-6) and as potassium salt (CAS 15307-81-0). The last salification form has shown a prompter absorption rate and a faster onset of analgesic activity than the acid form and sodium salt. This paper extensively reviews three trials carried out on healthy volunteers, where potassium salt of diclofenac present in three fast-acting formulations, namely sachets (Trial 1), tablets (Trial 2) and oral drops (Trial 3), were compared to reference tablet formulations from the market. A very fast absorption rate was encountered with the three test formulations, with the peak reached in one case 5 min and in most cases within 10-15 min after dosing. The quick absorption rate of test formulations was attributed to the special combination of the salt of diclofenac with a dynamic buffering agent, namely bicarbonate, present in the test formulations and covered by an international patent. The prompt absorption of diclofenac from the new fast-acting formulations was accompanied by the presence of only one peak, whereas the reference formulations produced in most cases two peaks, as widely described in literature. This finding suggested the hypothesis that the absorption of test formulations should occur in a shorter tract of the gut. The faster absorption of diclofenac from the three fast-acting formulations is expected to produce a faster onset of analgesic action, which highlights these new formulations as particularly indicated to relief pain of any origin.
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PMID:Increased absorption rate of diclofenac from fast acting formulations containing its potassium salt. 1176 89

The purpose of this project was to evaluate the analgesic efficacy of misoprostol when combined with ibuprofen or diclofenac Na. Animal experiments using the inflamed rat paw formalin model suggested that misoprostol potentiates the analgesic effect of some NSAIDs (nonsteroidal anti-inflammatory drugs) including diclofenac Na but not propionic acid derivatives or opiates. The dental pain model was used to evaluate the clinical relevance of this interaction. Patients received a single oral dose of study medication following surgical removal of impacted teeth. Patients were medicated for moderate to severe postsurgical pain and then filled in an analgesic diary for a 6-h observation period. Several blood samples were taken over the observation period. In addition, microdialysis samples were taken directly from the extraction socket and were analyzed for immunoreactive prostaglandin E(2) levels. The studies were single-dose, parallel group and double-blind assays. In the first study, 70 patients received an oral dose of either placebo (n = 13), misoprostol 200 &mgr;g (n = 18), ibuprofen 200 mg (n = 19), or the combination of misoprostol + ibuprofen (n = 20). Misoprostol alone demonstrated a small analgesic effect compared to placebo. Both the ibuprofen and combination groups were substantially more effective than placebo but not different from each other. The combination group had higher ibuprofen blood levels during the first 45 min but had a lower C(max) and longer time to T(max). The second study evaluated oral doses of placebo (n = 11), misoprostol 200 &mgr;g (n = 21), diclofenac Na 50 mg (n = 18), and the combination of misoprostol + diclofenac Na (n = 20). Relative to placebo, misoprostol performance was similar to the first study. When the results of the two studies were combined, there was a small, but statistically significant, analgesic effect for misoprostol. Diclofenac Na was superior to both placebo and to misoprostol alone. The combination was the most effective treatment, and for hours 4--6 it was significantly better than diclofenac Na alone. Analysis of the blood samples showed an earlier and higher peak effect for the diclofenac Na group compared to the combination, and the combination again had a lower C(max). The microdialysis probe assays demonstrated that misoprostol depressed PGE(2) levels at the peripheral site of trauma over the first 2 h after surgery. These pilot studies used small samples, and the results only suggest trend effects. Both studies demonstrated that misoprostol 200 &mgr;g, a prostaglandin analog, does have an analgesic effect. When combined with ibuprofen, there was no potentiation of analgesia. In contrast, the combination of misoprostol + diclofenac Na demonstrated an enhanced peak effect, total effect for pain intensity difference and pain relief (sum pain intensity difference [SPID] and total pain relief [TOTPAR]), and
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PMID:The Analgesic Interaction of Misoprostol with Nonsteroidal Anti-Inflammatory Drugs. 1186 59

Fever is a common symptom in cancer patients. The most frequent causes of fever are infections, malignancy itself, various medications, transfusions, and allergy. Although it is necessary to treat the cause of fever, if possible, symptomatic fever management is also important. Surprisingly, little attention is paid to this topic in the medical literature, despite the fact that it is a very frequent problem. In order to support symptomatic fever therapy, we wanted to study the patients' discomfort accompanying fever and the beneficial effects of the symptomatic fever management. To the best of our knowledge, there is an absence of studies in this area, despite the fever discomfort can be an important reason for the antipyretic treatment, mainly in cancer patients. In this non-randomized open label pilot study, three intravenous antipyretics were tested in five groups of patients: diclofenac (75 mg, brief intravenous [IV] infusion) vs. metamizol (2500 mg or 1000 mg, brief IV infusion) vs. propacetamol (2000 mg or 1000 mg, slow IV injection or brief IV infusion). The study included 254 febrile episodes mainly in hemato-oncological patients with axillary temperature at least 38 degrees C. The main study endpoints were: changes in axillary temperature, improvement in patient comfort, and number and nature of adverse events. To support justification for symptomatic fever management in febrile patients, we asked the first 45 study subjects to fill in a questionnaire concerning their opinions about fever, fever-associated discomfort, and relief upon antipyretic therapy. All study medications had a significant antipyretic effect. However, metamizol at the dose 2500 mg was considered as the most effective, while propacetamol at the dose 1000 mg showed the lowest antipyretic efficacy. Concerning tolerability and adverse events, there were significant differences among the treatment groups. Diclofenac and metamizol (both 2500 mg and 1000 mg) were tolerated at best. All tested antipyretics significantly improved comfort in febrile patients. Overall, 87% of patients declared improvement in their comfort after administration of antipyretics. Based on the results of the present study, the choice of the antipyretic drug should depend on the clinical status of patient, contraindications, and potential adverse events and risks of the selected agent. It is advisable to use proparacetamol at the higher dosage and to administer it as a brief IV infusion in order to avoid injection-related adverse events. The symptomatic antipyretic treatment in febrile cancer patients is supported by patients themselves and has a significant role in the complex supportive care. Discomfort of patients during fever episodes may be greater than previously thought.
J Pain Symptom Manage 2002 Dec
PMID:Symptomatic intravenous antipyretic therapy: efficacy of metamizol, diclofenac, and propacetamol. 1255 12

The article compares efficacy and safety of ketonal used in a dose 300 mg/day and diclofenac in a dose 150 mg/day in patients with primary spinal pain. The treatment of 60 patients aged 35 to 70 years (mean age 42.7 +/- 12.4 years) showed high efficacy of ketonal in spinal pain and low rate of side effects induced by this drug. Diclofenac was also effective.
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PMID:[Effectiveness of ketonal and diclofenac in spondylarthrosis complicated with spinal pain]. 1497 Nov 61

The purpose of the case-study was to evaluate the efficiency of non-steroid antiinflammatory drugs (NAD) for postoperative analgesia in children after small-scope surgical interventions. Diclofenac, 1 mg/kg per day administered as rectal suppositories or intramuscular injections after initial narcosis, was used for postoperative analgesia in children of the main group; postoperative analgesia made by analgin and promedol in the control group was compared with the former. Forty-seven children and 10 children with identical diseases like groin hernia, varicocele and dropsy of testicular membranes, were respectively in the main and control groups. Clinical examinations and registration of functional parameters were made in patients during certain time periods, i.e. before surgery (in the standing and lying postures) and after surgery (in 20 minutes, as well as in 1, 2, and 3 hours after surgical interventions). The efficiency of postoperative analgesia was evaluated by means of cardiointervalography according to Bayevsky method as well as by a state of central hemodynamics and by clinical examinations, including the visual-analogue 10-point scale and the 0-4 point verbal pain assessment scale. The postoperatively obtained data revealed a pronounced misbalance between the main and control groups, which is indicative of that the application of NAD for preventive and postoperative analgesia in children improves essentially the postoperative course and contributes to a fast rehabilitation of patients. A comparative analysis of the efficiency of postoperative analgesia by the discussed drugs showed that diclofenac possesses a sufficient analgetic activity and is free of any side-effects inherent in narcotic analgetics.
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PMID:[Postoperative analgesia with nonsteroid anti-inflammatory drugs in children]. 1520 15

We investigated the efficacy and safety of gabapentin in rhinoplasty or endoscopic sinus surgery patients. Patients received either oral placebo or gabapentin 1200 mg 1 h before surgery. After standard premedication, 25 patients in each group received propofol, fentanyl, and local anesthesia at the operative site. Sedation was maintained by a continuous infusion of propofol adjusted according to the Ramsay scale. Sedation and pain scores were obtained at 5, 15, 30, 45, and 60 min during surgery and 30 min and 2, 4, 6, 8, 12, 16, 20, and 24 h after the procedure. Diclofenac 75 mg IM was administered as a rescue analgesic. Postoperative pain scores and intraoperative pain scores at 45 and 60 min were significantly lower in the gabapentin group. Fentanyl (122 +/- 40 microg versus 148 +/- 42 microg; P < 0.05) and diclofenac (33 +/- 53 mg versus 111 +/- 92 mg; P < 0.001) consumption was smaller and the time to first analgesic request (18 +/- 9 h versus 9 +/- 7 h; P < 0.001) was longer in the gabapentin group. A more frequent incidence of dizziness was found in the gabapentin (versus placebo) group (24% versus 4%, respectively). We conclude that gabapentin provided a significant analgesic benefit for intraoperative and postoperative pain relief in patients undergoing ambulatory rhinoplasty or endoscopic sinus surgery; however, dizziness may be a handicap for ambulatory use.
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PMID:The analgesic effects of gabapentin in monitored anesthesia care for ear-nose-throat surgery. 1527 9

Although the use of non-steroidal anti-inflammatory drugs (NSAIDs) is well established in the postoperative setting, their use after caesarean sections is still controversial. In a randomised, double-blinded, placebo controlled study we have estimated the opioid-sparing effect of diclofenac suppositories after elective caesarean sections in spinal anaesthesia. Eighty-two women ASA class I or II scheduled for caesarean section were randomised to receive either diclofenac suppositories 100 mg or placebo every 12 h after the operation. The diclofenac group (n = 40) consumed significantly less morphine in the postoperative period (14.0 +/- 1.5 mg in 32 h) compared with the placebo group (21.5 +/- 1.6 mg in 32 h, P < 0.05). The average level of postoperative pain as estimated by a visual analogue scale (VAS) and a verbal scale tended to be lower in the diclofenac group, but this was not significant. There were no differences in demographic data, perioperative bleeding, side-effects or discharge time between the groups. Diclofenac suppositories 100 mg given twice daily after caesarean section are opioid sparing.
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PMID:High-dose diclofenac for postoperative analgesia after elective caesarean section in regional anaesthesia. 1532 59

We report a case of an acute allergic reaction to rectal diclofenac following elective caesarean section in a patient taking ibuprofen. The reaction presented as severe angio-oedema affecting the face and tongue. Serial blood samples failed to show the rise in tryptase levels characteristic of an anaphylactic or anaphylactoid reaction. Diclofenac is widely used for postoperative pain relief in women undergoing caesarean section. To our knowledge this is the first time that an adverse reaction to diclofenac given via this route has been reported in an obstetric patient.
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PMID:Angio-oedema following rectal diclofenac after caesarean section. 1532 29

Previous studies on the pharmacology of South African medicinal plants in our laboratories and elsewhere have shown that some plants possess therapeutic attributes. One such ethnomedically useful plant is Sutherlandia frutescens R. BR. (family: Fabaceae). S. frutescens is widely used in South African traditional medicine for the management and/or control of a plethora of human ailments. In order to scientifically appraise some of the ethnomedical uses of S. frutescens, the present study was undertaken to investigate the analgesic, antiinflammatory and antidiabetic properties of the plant's shoot aqueous extract in experimental animal models. The analgesic effect of the herb's shoot extract was evaluated using the hot-plate and acetic acid test models of pain in mice, while the antiinflammatory and hypoglycemic effects of the plant's shoot aqueous extract were investigated in rats, using fresh egg albumin-induced pedal (paw) edema, and streptozotocin (STZ)-induced diabetes mellitus. Diclofenac (100 mg/kg) and chlorpropamide (250 mg/kg) were used, respectively, as reference drugs for comparison. S. frutescens shoot aqueous extract (50-800 mg/kg i.p.) produced significant (p < 0.05-0.001) analgesic effects against thermally- and chemically-induced nociceptive pain stimuli in mice. The plant extract (50-800 mg/kg p.o. or i.p.) also significantly (p < 0.05-0.001) inhibited fresh egg albumin-induced acute inflammation and caused significant (p < 0.05-0.001) hypoglycemia in rats. The various chemical constituents and secondary metabolites of the herb are speculated to account for the observed analgesic, antiinflammatory and hypoglycemic effects of the plant. The results of this experimental animal study suggest that S. frutescens shoot aqueous extract possesses analgesic, antiinflammatory, and hypoglycemic properties, and thus lend pharmacological credence to the suggested folkloric uses of the herb in the management and/or control of painful, arthritic and other inflammatory conditions, as well as for adult-onset, type-2 diabetes mellitus in some communities of South Africa.
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PMID:Analgesic, antiinflammatory and hypoglycemic effects of Sutherlandia frutescens R. BR. (variety Incana E. MEY.) [Fabaceae] shoot aqueous extract. 1534 36

In order to appraise some of the ethnomedical uses of Sclerocarya birrea (A. Rich.) Hochst., subspecies caffra (Sond.) Kokwaro [family: Anacardiaceae], the present study was undertaken to investigate the analgesic, anti-inflammatory and anti-diabetic properties of the plant's stem-bark aqueous extract in experimental models of pain, inflammation and diabetes mellitus. The analgesic effect of Sclerocarya birrea stem-bark aqueous extract was evaluated in mice, while its anti-inflammatory and anti-diabetic effects were investigated in rats. Diclofenac (DIC, 100 mg/kg p. o.) and chlorpropamide (250 mg/kg p. o.) were used respectively as reference analgesic, anti-inflammatory and anti-diabetic agents for comparison. Like diclofenac (DIC, 100 mg/kg p. o.), Sclerocarya birrea stem-bark aqueous extract (SBE, 100-800 mg/kg p. o.) produced dose-dependent, significant protection (p < 0.05-0.001) against electrical heat-induced pain. The plant extract (SBE, 25-800 mg/kg p. o.) also produced dose- and time-related, sustained and significant reductions (p < 0.05-0.001) in the fresh egg albumin-induced acute inflammation of the rat hind paw oedema. However, the analgesic and anti-inflammatory effects of the plant's extract were found to be approximately 10-15 times less than that of diclofenac. In one set of experiments involving hypoglycaemic/antidiabetic evaluation of the plant's extract, graded doses of Sclerocarya birrea stem-bark aqueous extract (SBE, 25-800 mg/kg p. o.) were separately administered to groups of fasted normal and fasted diabetic rats. In another set of experiments, a single dose of the plant's aqueous extract (SBE, 800 mg/kg p. o.) was used. The hypoglycaemic effect of this single dose of Sclerocarya birrea stem-bark aqueous extract (SBE, 800 mg/kg p. o.) was compared with that of chlorpropamide (250 mg/kg p. o.) in both fasted normal and fasted streptozotocin (STZ)-treated diabetic rats. Following acute treatment, relatively moderate to high doses of Sclerocarya birrea stem-bark aqueous extract (SBE, 25-800 mg/kg p. o.) produced dose-dependent, significant reductions (p < 0.05-0.001) in the blood glucose concentrations of both fasted normal and fasted diabetic rats. Chlorpropamide (250 mg/kg p. o.) also produced significant reductions (p < 0.05-0.001) in the blood glucose concentrations of the fasted normal and fasted diabetic rats. Administration of the single dose of Sclerocarya birrea stem-bark aqueous extract (SBE, 800 mg/kg p. o.) significantly reduced (p < 0.01-0.001) the blood glucose levels of both fasted normal (normoglycaemic) and fasted STZ-treated, diabetic rats. The results of this experimental animal study indicate that Sclerocarya birrea stem-bark aqueous extract possesses analgesic, anti-inflammatory and hypoglycaemic properties. These experimental findings lend pharmacological support to the suggested folkloric uses of the plant's stem-bark in the management and/or control of pain, inflammatory conditions, and adult-onset, type-2 diabetes mellitus in some communities of South Africa.
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PMID:Evaluation of the analgesic, anti-inflammatory and anti-diabetic properties of Sclerocarya birrea (A. Rich.) Hochst. stem-bark aqueous extract in mice and rats. 1547 10


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