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Medical research on voltaren
J Pain. 2008 Nov 26;
Chantler I, Mitchell D, Fuller A
We assessed the efficacy of diclofenac potassium, a nonsteroidal anti-inflammatory drug, in alleviating menstrual pain and restoring exercise performance to that measured in the late-follicular phase of the menstrual cycle. Twelve healthy young women with a history of primary dysmenorrhea completed, in a random order, laboratory exercise-testing sessions when they were in the late-follicular (no menstruation, no pain) phase of the menstrual cycle and when they were experiencing dysmenorrhea and receiving, in a double-blinded fashion, either 100 mg of diclofenac potassium or placebo. We assessed the women's leg strength (1-repetition maximum test), aerobic capacity (treadmill walking test), and ability to perform a functional test (task-specific test). Compared with placebo, diclofenac potassium significantly decreased dysmenorrhea on the day of administration (Visual Analog Scale, P < .001 at all times). When receiving placebo for menstrual pain, the women's performance in the tests was decreased significantly, compared with when they were receiving diclofenac potassium for menstrual pain (P < .05) and compared with when they were in the late-follicular phase of the menstrual cycle (P < .05 for treadmill test, P < .01 for task-specific test and 1-repetition maximum test). Administration of diclofenac potassium for menstrual pain restored exercise performance to a level not different from that achieved in the late-follicular phase of the cycle. PERSPECTIVE: In women with primary dysmenorrhea, menstrual pain, if untreated, decreases laboratory-assessed exercise performance. A recommended daily dose of a readily available nonsteroidal anti-inflammatory drug, diclofenac potassium, is effective in relieving menstrual pain and restoring physical performance to levels achieved when the women were in the late-follicular (no menstruation, no pain) phase of the menstrual cycle.
Sci Total Environ. 2008 Nov 25;
Khalaf H, Salste L, Karlsson P, Ivarsson P, Jass J, Olsson PE
Pharmaceuticals are regularly released into the environment; in particular non-steroidal anti-inflammatory drugs (NSAIDs) and antibiotics. Erythromycin, naproxen, furosemide and atenolol are reported to be stable for up to 1 year in the environment, which increases the risk for accumulation. In the present study we have measured the occurrence and concentration of pharmaceuticals in river Viskan (Jössabron) downstream of a sewage treatment plant in Borås, Sweden. Pharmaceuticals and water samples were tested for potential human risk by evaluating inflammatory responses (NF-kappaB and AP-1) using human T24 bladder epithelial cells and Jurkat T-cells. NF-kappaB activity in T24 cells was significantly reduced by all NSAIDs analysed (diclofenac, ketoprofen, naproxen, ibuprophen and dextropropoxyphene), but also by trimethoprim, using environmentally relevant concentrations. NF-kappaB and AP-1 activation was further analysed in response to water samples collected from different locations in Sweden. Dose-dependent down-regulation of AP-1 activity in Jurkat cells was observed at all locations. At two locations (Jössabron and Almenäs) down-regulation of NF-kappaB was observed. In contrast, the NF-kappaB response was potentiated by exposure to water from both locations following activation of NF-kappaB by treatment with heat-killed Escherichia coli. To determine the involvement of pharmaceuticals in the responses, T24 cells were exposed to the pharmaceutical mixture, based on the determined levels at Jössabron. This resulted in reduction of the NF-kappaB response following exposure to the pharmaceutical mixture alone while no potentiation was observed when cells were co-exposed to heat killed E. coli and pharmaceuticals. The obtained results demonstrate that the identified pharmaceuticals affect the inflammatory responses and furthermore indicate the presence of unknown substance(s) with the ability to potentiate inflammatory responses.
J Chromatogr A. 2008 Nov 5;
Kosjek T, Zigon D, Kralj B, Heath E
The work presented herein discusses the potential of liquid chromatography-quadrupole-time-of-flight mass spectrometry (QqToF-MS) for the chemical structure elucidation of pharmaceutical degradation products (DPs). The model compound, the nonsteroidal anti-inflammatory drug diclofenac was subjected to microbiological transformation in a laboratory scale pilot wastewater treatment plant (WWTP) and its transformation products were detected in the outlet samples. Their chemical structures were elucidated using the principal features of the instrument, i.e. high resolution, accurate mass and MS/MS capability. A hydroxy-diclofenac, a benzoquinone imine derivative and a nitro analogue of diclofenac were successfully identified. The final structural elucidation of the fourth transformation product was not successful. Overall, the study emphasises the capabilities and potential of quadrupole-time-of-flight mass spectrometer showing it to be a powerful tool in both structure elucidation and confirming the identity of environmental contaminants.
Population pharmacokinetics of oral diclofenac for acute pain in children.
Br J Clin Pharmacol. 2008 Dec; 66(6): 846-53
Standing JF, Howard RF, Johnson A, Savage I, Wong IC
WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT * Diclofenac is an effective oral analgesic for acute postoperative pain. In adults 25 mg is half as effective as 50 mg, but 50 mg and 100 mg are similarly effective (ceiling effect). Diclofenac has linear pharmacokinetics in this range. * Diclofenac is frequently used 'off-label' in children for acute pain but optimum dosing is unclear (dosing of diclofenac in clinical paediatric studies ranges from 0.5-2.5 mg kg(-1)). There is currently no licensed oral paediatric formulation of diclofenac. WHAT THIS STUDY ADDS * Using a new diclofenac oral suspension, a dose of 1 mg kg(-1) in children aged 1 to 12 years gives a similar exposure to 50 mg in adults; paediatric patients are unlikely to benefit from higher doses. AIMS To develop a population pharmacokinetic model for a new diclofenac suspension (50 mg 5 ml(-1)) in adult volunteers and paediatric patients, and recommend a dose for acute pain in children. METHODS Blood samples were drawn at the start and end of surgery, and on removal of the venous cannula from 70 children (aged 1 to 12 years, weight 9 to 37 kg) who received a preoperative oral 1 mg kg(-1) dose; these were pooled with rich (14 post-dose samples) data from 30 adult volunteers. Population pharmacokinetic modelling was undertaken with NONMEM. The optimum adult dose of diclofenac for acute pain is 50 mg. Simulation from the final model was performed to predict a paediatric dose to achieve a similar AUC to 50 mg in adults. RESULTS A total of 558 serum diclofenac concentrations from 100 subjects was used in the pooled analysis. A single disposition compartment model with first order elimination and dual absorption compartments was used. The estimates of CL/F and V(D)/F were 53.98 l h(-1) 70 kg(-1) and 4.84 l 70 kg(-1) respectively. Allometric size models appeared to predict adequately changes in CL and V(D) with age. Of the simulated doses investigated, 1 mg kg(-1) gave paediatric AUC((0,12 h)) to adult 50 mg AUC((0,12 h)) ratios of 1.00, 1.08 and 1.18 for ages 1-3, 4-6 and 7-12 years respectively. CONCLUSIONS This study has shown 1 mg kg(-1) diclofenac to produce similar exposure in children aged 1 to 12 years as 50 mg in adults, and is acceptable for clinical practice; patients are unlikely to obtain further benefit from higher doses.
Int Urol Nephrol. 2008 Nov 25;
Besen A, Kose F, Paydas S, Gonlusen G, Inal T, Dogan A, Kibar M, Balal M
INTRODUCTION: Renal physiology is a partially cyclooxygenase (COX)-dependent system. Kidneys express both COX-1 and COX-2 enzymes. In this study, we tried to investigate the effects of diclofenac sodium (D), with or without furosemide (F), on plasma renin activity (PRA), serum and urine electrolytes, creatinine clearance, and COX-1 and COX-2 expression in the renal cortex. METHOD: Forty-two Wistar-albino rats were divided into four groups (G). G1, G2, G3, and G4 were treated with placebo, F (20 mg/kg), F (20 mg/kg) plus D (2.5 mg/kg), and D (2.5 mg/kg), respectively, and followed for seven days. Urinary osmolality and volume, and levels of serum and urinary creatinine, sodium, and potassium were measured. Renal COX-1 and COX-2 expression were examined by the immunohistochemical method. RESULTS: Compared with G1, body weights were significantly reduced in G3 and G4 (P < 0.05 for all). Serum sodium in G2 decreased significantly compared with G1, G3, and G4. Serum potassium in G2 decreased significantly compared with G1 and G3. Urine volume in G2 increased significantly compared with G1, G3, and G4. Urine osmolality in G2 and G4 decreased significantly compared with G1 and G3. Urine Na in G2 increased significantly compared with G4. Although urine K was lowest in G4, there were no statistically significant differences between the groups. Creatinine clearance decreased in G4 compared with the other groups. PRA was similar in all groups. Renal cortical COX-2 expression was lowest in G1. COX-1 expression in cortical collecting tubules was significantly reduced in G3 and G4 compared with G1 and G2 (P < 0.05 for all). Although creatinine clearance in G4 was significantly lower than in G3, COX-1 and COX-2 expression were no different in G3 and G4. DISCUSSION: Acute renal failure was caused by D. F prevented development of renal failure in rats treated with a combination of D and F. The diuretic effect of F was neutralized by D. Whereas COX-1 expression was reduced by D and by the combination of D and F in G3 and G4, renal COX-2 immunoreactivity was increased by F and D and the combination of both. Although creatinine clearance was lower in rats that were given D alone compared with the combination of F and D, COX-1 and COX-2 expression were similar in these groups.
Environ Int. 2008 Nov 21;
Letzel M, Metzner G, Letzel T
Although various single-concentration measurements of the pharmaceutical diclofenac are available in literature, detailed information on the mass flux in the aquatic environment is often missing. Therefore, the overall load of diclofenac was obtained by recording each concentration in nine effluents of sewage treatment plants (STP) and at three river sites located in the area of the river Main (Germany) over a time period of six weeks. In STP effluents, concentrations of up to 2200 ng/L were obtained. In combination with flow rates and connected population an average specific load per capita and day of 0.28 mg (+/-0.11 mg) diclofenac reaches the receiving water course. This average specific load per capita is an expressive parameter to assess main diclofenac exposure to the aquatic environment avoiding uncertainties of estimated data commonly used in exposure assessment. Accordingly, predicted environmental concentrations (PEC) of 140 ng/L for a realistic worst case scenario and 2 to 52 ng/L based on water quality modeling were derived. Since concentrations of up to 140 ng/L were observed in surface water, the obtained PEC is in perfect agreement with measured concentrations. Hence, comparing the PEC with published predicted no effect concentrations (PNEC), chronic adverse effects in fish populations may occur.
Uterine relaxant effects of Curcuma aeruginosa Roxb. rhizome extracts.
J Ethnopharmacol. 2008 Nov 5;
Thaina P, Tungcharoen P, Wongnawa M, Reanmongkol W, Subhadhirasakul S
The effects and plausible mechanism of action of Curcuma aeruginosa Roxb. (Zingiberaceae) rhizome chloroform and methanol extracts on the uterine contraction were investigated using isolated uterus strips from estrogen primed rats. The contractile responses were recorded isometrically with a Grass FT03 force transducer connected to a MacLab system. The experiments were carried out on both nonstimulated, agonist- and KCl-stimulated uteri. In the nonstimulated uterus, the two extracts (10-400mug/ml) had no significant effect. In contrast, in the stimulated uterus, the chloroform and methanol extracts exerted concentration-dependent inhibition of the contractions induced by oxytocin (1mU/ml), prostaglandin F(2alpha) (PGF(2alpha), 0.5mug/ml), ACh (3x10(-6)M) and KCl (40mM) with the IC(50) (inhibition of force) of 31.4, 58.59, 56.21 and 29.28mug/ml; and 57.79, 69.3, 223.8 and 69.19mug/ml, respectively. Verapamil, the reference L-type calcium channel blocker, exhibited a similar pattern of inhibition with the IC(50) of 0.03, 0.25, 0.35 and 0.04mug/ml. The IC(50) of diclofenac against a PGF(2alpha)-induced contraction was 31.36mug/ml. It is known that the contraction induced by agonists and KCl is mainly due to calcium influx through the voltage-gated L-type calcium channels opened indirectly or directly by agonist-receptor activation and KCl. Thus, it is speculated that the two plant extracts might inhibit uterine contraction by interrupting the influx of Ca(2+) probably through voltage-gated L-type calcium channels. This possibility was further substantiated by the ability of the extracts to shift the CaCl(2)-contraction curves to the right. As the methanol extract also reduced the contraction of oxytocin in Ca(2+)-free EDTA solution; thus, it is suggested that part of its action may be involved with an intracellular mechanism. The effect of the two extracts did not involve the activation of beta(2)-adrenoceptors since their effects were unaffected by propranolol. Based on the inhibitory effect of the extracts on the oxytocin-induced contraction, it is concluded that the extracts might be useful as tocolytic agents for the prevention of preterm labor. Their effects on the inhibition of PGF(2alpha)-induced contractions also seem useful for the treatment of dysmenorrhea. There are reports by others that the plant rhizome contains beta-pinene and sesquiterpenes. In addition, there is evidence that these compounds possess spasmolytic effects in the rat intestine and uterus. Therefore, the uterine relaxant effect of the plant extracts could be due to beta-pinene and some sesquiterpene lactones contents. The methanol extract is less potent than the chloroform extract, and this might be due to the lower amount of terpene compounds or different compounds may involve in this action.
Pharmacoepidemiol Drug Saf. 2000 May; 9(3): 207-14
Gauld NJ, Shaw JP, Emmerton LM, Pethica BD
PURPOSE: Postmarketing surveillance of prescription medicines is a routine practice, yet similar evaluation of non-prescription medicines, including those recently switched from prescription status, is uncommon. This study presents the methodologic issues and limitations of the use of pharmacies in the 'post-reclassification' surveillance of oral diclofenac potassium 25 mg which had been recently switched from physician prescription to non-prescription sale. METHODS: Consenting user-purchasers were recruited from 175 New Zealand pharmacies over 4 months. Purchasers were mailed a questionnaire for completion 7 days post-purchase. Those purchasers who met criteria for being potentially 'at risk' of adverse events were re-surveyed 30 days post-purchase. A descriptive analysis was carried out using t-test and chi-square as appropriate. These results were compared to those from other types of studies in this area. RESULTS: The 1240 recruited purchasers returned 990 valid questionnaires (80% response). Of these 557 (56%) met 'at risk' criteria and received the second questionnaire with 480 valid returns (86.2% response). CONCLUSIONS: Useful data was gathered on the 'real-life' usage of a medicine recently reclassified from prescription to non-prescription sale. The use of community pharmacies as recruiting centres was found to be effective. Copyright (c) 2000 John Wiley & Sons, Ltd.
Pharmacoepidemiol Drug Saf. 2000 Mar; 9(2): 113-7
Lanes SF, Rodrígeuz LA, Hwangg E
Meloxicam (Mobic((R))) was introduced in the UK in 1996 as a nonsteroidal anti-inflammatory drug (NSAID). To help evaluate the postmarketing experience with meloxicam in the UK, we used the General Practitioners Research Database (GPRD) to characterize the baseline risk of an upper gastrointestinal (GI) event among new users of meloxicam, ibuprofen, diclofenac, naproxen and indomethacin. We selected for analysis a random sample of 5000 meloxicam users, and 5000 users of each of the comparator NSAIDS except indomethacin, for which we selected 2500 subjects. Comparators were matched to meloxicam subjects on age and sex. We examined for each subject history of certain GI diagnoses and recent use of anti-inflammatory drugs and acid-suppressing drugs. We found that patients receiving meloxicam were at least twice as likely as patients receiving other NSAIDs to have a recent history of GI diagnoses or treatment. We conclude that in the UK meloxicam was used more often than other popular NSAIDs among patients who were at increased baseline risk of GI events. The occurrence of GI events among users of meloxicam, even at a relatively high frequency, therefore, would be expected based solely on this increased baseline risk. Copyright (c) 2000 John Wiley & Sons, Ltd.
Arzneimittelforschung. 2008; 58(10): 515-20
Bolakatti GS, Maddi VS, Mamledesai SN, Ronad PM, Palkar MB, Swamy S
A novel series of coumarinyl Mannich bases (3a-1) have been synthesized by reacting 3-acetyl coumarin (1) with various substituted secondary amines (2a-1) in presence of paraformaldehyde. The structures of the newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR and HRMS (high resolution mass spectral) data. Title compounds were screened for in vivo acute anti-inflammatory activity using the carrageenan-induced rat paw edema assay model. Among the compounds tested, 3-[3-(diethylamino)propanoyl]-2H-chromen-2-one (3a)and 3-[3-(piperidine-1-yl) propanoyl]-2H-chromen-2-one (3c) showed 63.1 and 66.7% inhibition, respectively, as compared to the standard drug diclofenac (CAS 15307-86-5, 68.8%). These potent compounds showed encouraging analgesic andantipyretic activities.