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PubMedDate not supplied

[Effect of acetylsalicylic and mefenamic acids on cytoarchitectonic of skin in rats with acute local cryogenic trauma].

The effect of acetylsalicylic (250 mg/kg) and mephenamic (50 mg/kg) acids on the process of skin cytoarchitectonics restoration was studied in rats with acute local cryogenic traumas induced by acting with a stream of ethyl chloride upon epilated back skin area (1.5 cm2). The animals were killed under narcosis on the 12th day of post-treatment observation. Both acetylsalicylic and mephenamic acids were administered per os twice per day over various periods after cryogenic damage. The effect depended on the treatment duration. The normal skin cytoarchitectonics was restored by acetylsalicylic acid in half, and by mephenamic acid, in one-third of cases (for a "combined" administration scheme).

Administration, Oral↗
PubMed2003

[Pain management after third molar extraction. Observations of the use of mefenamic acid and rofecoxib in the treatment of postoperative pain in the dental office].

Pain monitoring is often inadequate in the ambulant field to assure therapy results. Today NSAID take the centre in acute pain and inflammation control in dental interventions. Compared to conventional non-selective NSAID modern selective Cyclooxygenase-2 inhibitors (COX-2) provide the potential for improved compatibility and simplified medication with heightened effectiveness in acute postoperative toothaches. The aim of this study was to compare the effect of selective COX-2 inhibitors with NSAID after operative wisdom tooth extraction in 30 ambulant patients. The pain curve under mefenamine acid showed a significant increase during the first 48 hours after extraction. With rofecoxib a continuous pain decrease with the lowest stand 48 hours after intervention was registered. One week after extraction the patient's satisfaction was in favour of rofecoxib, which showed a clearly prolonged analgetic effect over 24 hours. Additionally rofecoxib as a COX-2 selective inhibitor doesn't bear the risk for severe non-anticipatable gastrointestinal side effects or prolonged bleeding after surgical intervention.

Adult↗
PubMed2000

Mycophenolic acid glucuronidation and its inhibition by non-steroidal anti-inflammatory drugs in human liver and kidney.

OBJECTIVE: The aims of this investigation were to study the glucuronidation of mycophenolic acid (MPA) in human liver and kidney and to search for a compound that inhibits MPA glucuronidation among the non-steroidal anti-inflammatory drugs (NSAIDs). METHODS: A sensitive and reproducible radiometric assay was developed to measure the rate of MPA glucuronidation in human liver and kidney microsomes. The assay employed uridine 5'-diphosphate-[U-14C]-glucuronic acid (UDPGA) and MPA-glucuronide was isolated by TLC. The final concentrations of UDPGA and MPA necessary were 1 mM (liver), and MPA concentration was 0.5 mM (kidney). The inhibition of MPA glucuronidation was studied with 18 NSAIDs and tacrolimus. RESULTS: Glucuronosyl transferase activity followed Michaelis-Menten kinetics and the Km (mean +/- SD; mM) was 0.31+/-0.06 (liver; n = 5) and 0.28+/-0.07 (kidney; n = 5; P = 0.555); the Vmax (mean SD; nmol/mg per minute) was 5.2+/-1.4 (liver; n = 5) and 10.5+/-1.2 (kidney; n = 5; P = 0.0005). The MPA glucuronidation rates (mean +/- SD; nmol/min/mg) were 3.3+/-0.9 (liver; n = 10) and 7.8+/-1.5 (kidney; n = 10; P = 0.0002). The rate of MPA glucuronidation ranged between 2.0 and 5.1 nmol/ mg per minute with a 2.5-fold variation (liver) and between 5.7 and 9.8 nmol/mg per minute with a 1.7-fold variation (kidney). The inhibition study was performed in liver and revealed that the percentage of control ranged from 8%+/-3% (niflumic acid) to 119%+/-16% (Ketoralac). The inhibition curves for MPA glucuronidation rate were determined with the four most effective inhibitors: niflumic acid, flufenamic acid, mefenamic acid and diflunisal. Their IC50 estimates (microM) were 8+/-1, 19+/-9, 63+/-8 and 109+/-15, respectively (liver), and 8+/-2, 13+/-2, 49+/-4 and 122+/-18, respectively (kidney). The IC50 estimate for niflumic acid was eightfold lower than the peak plasma levels after a single oral dose of 250 mg of this drug. CONCLUSION: The human liver and kidney are important sites of MPA glucuronidation. MPA glucuronidation was inhibited to various extents by different NSAIDs and the four most effective inhibitors were niflumic acid, flufenamic acid, mefenamic acid and diflunisal. These drugs have similar molecular structures consisting of two aromatic rings bearing a carboxylic group.

Aged↗
PubMed1992

Separation of non-steroidal anti-inflammatory agents using supercritical fluid chromatography.

Supercritical fluid chromatography (SFC) was investigated for the separation of non-steroidal anti-inflammatory agents (NSAIs). Three different stationary phases (SB-methyl-100, SB-biphenyl-30, and SB-cyanopropyl-50) were compared for the separation of the compounds. Baseline separation of a flufenamic acid, mefenamic acid, fenbufen and indomethacin mixture was achieved on the SB-biphenyl-30 column using a pressure gradient. A mixture containing flufenamic acid, mefenamic acid, acetylsalicylic acid, ketoprofen and fenbufen and another mixture containing ibuprofen, fenoprofen, naproxen, ketoprofen and tolmetin were well separated on the SB-cyanopropyl-50 column using pressure gradients. Typical analysis time for a mixture of NSAIs on the biphenyl or cyanopropyl column was approximately 20-25 min. Application of the method using the biphenyl column to the determination of NSAIs present in selected commercial dosage forms was demonstrated.

Anti-Inflammatory Agents, Non-Steroidal↗