BACKGROUND: Venipuncture pain is an uncomfortable suffering to the patient. It creates anxiety, fear and dissatisfaction. The ketoprofen transdermal patch is a proven treatment for musculoskeletal and arthritic pain. We planned this study to evaluate the efficacy of the ketoprofen patch to reduce venipuncture pain. METHODS: Two hundred adult patients, aged 18–60 years, of either sex, ASA grade I or II, were enrolled. Presuming that therapy would decrease venipuncture pain by 30%, a power calculation with α = 0.05 and β = 0.80 required enrollment of at least 24 patients into each group. However, 100 patients in each group were recruited. Group I (Control) received a placebo patch; Group II (Ketoprofen) received a 20 mg ketoprofen patch. A selected vein on the dorsum of the patient's non-dominant hand was cannulated with 18 g intravenous cannula 1 h after the application of the respective patch. Assessment of pain was done by a 10 cm visual analogue scale (VAS) of 0–10, where 0 depicts “no pain” and 10 is “the worst imaginable pain”. The venipuncture site was assessed for the presence of skin erythema, swelling and rashes at 12 h, 24 h and at the time of decannulation. RESULTS: Incidence of pain was 100% (94/94) in the control group as compared to 93% (85/91) in the ketoprofen group. The severity of the venipuncture pain was 6 (2) and 2 (2) for control and ketoprofen groups respectively (P < 0.05). CONCLUSIONS: Application of a ketoprofen patch at the proposed site of venipuncture one hour before the attempt is effective and safe for attenuating venipuncture pain.
Adult ; Anxiety ; Catheterization ; Catheters ; Erythema ; Exanthema ; Hand ; Humans ; Incidence ; Ketoprofen ; Phlebotomy ; Skin ; Transdermal Patch ; Veins ; Visual Analog Scale

BACKGROUND: Epidural administration of dexamethasone has been suggested for pain control after minor orthopedic surgery. This study was conducted to assess its efficacy after such surgery, combined or not to IV dipyrone, IV parecoxibe or their combination. METHODS: 91 patients were randomly assigned to seven groups. Patients were submitted to spinal bupivacaine anesthesia combined to epidural administration of either 10 ml saline or 10 mg dexamethasone diluted to 10-ml volume. Patients also received 10 ml IV saline or 1 gr dipyrone and/or 40 mg parecoxibe diluted to 10 ml with saline. Control group (CG) received epidural and IV saline. Dexamethasone group (DexG) received epidural dexamethasone and IV saline. Dipyrone group (DipG) received epidural saline and IV dipyrone. Dex-Dip G received epidural dexamethasone and IV dipyrone. Parecoxibe group (ParG) received epidural saline and IV parecoxibe. Dex-ParG received epidural dexamethasone and IV parecoxibe. Finally, Dex-Dip-ParG received epidural dexamethasone and IV dipyrone plus IV parecoxibe. RESULTS: The CG expressed 4h of analgesia and sooner requested pain killer. DexG was similar to DipG or ParG or Dex-ParG (7-hours), and they requested less ketoprofen compared to the CG (P < 0.05). However, the Dex-DipG and the Dex-Dip-ParG resulted in longer time to demand pain killer (17-hours) and less ketoprofen consumption in 24-hours (P < 0.002). Adverse effects were similar among groups. CONCLUSIONS: The analgesia secondary to epidural dexamethasone was enhanced by IV dipyrone, while no effects were observed by the addition of IV parecoxibe.
Analgesia* ; Anesthesia ; Bupivacaine ; Dexamethasone* ; Dipyrone* ; Humans ; Ketoprofen ; Orthopedics* ; Pain, Postoperative

Digestive disorders caused by sudden changes in diet or inappropriate diet are among the most common disorders of the digestive system. Cecal or intestinal tympany, one consequence of inappropriate diet, is characterized by the accumulation of gases, marked distension of the cecum and colon and the induction of inflammatory processes. To know the effects of intestinal tympany on the enteric plexuses, we developed a method of experimental tympanic colic (TC) in the Chinchilla lanigera. This species was used in view of its susceptibility to TC. TC was induced with a diet rich in alfalfa associated with grain overload for two weeks. Physical and clinical examination including the von Frey test confirmed the diagnosis. The chinchillas with acute abdomen were treated with 1% ketoprofen and resumption of a balanced diet. Necropsy and histopathological analysis showed tympany-induced alterations mainly in the cecum and colon. After treatment, the control conditions were restored. The TC protocol is proposed as an experimental approach designed to aid the study of the effects of acute intestinal inflammation and obstruction caused by an inappropriate diet.
Abdomen, Acute ; Cecum ; Edible Grain ; Chinchilla* ; Colic* ; Colon ; Diagnosis ; Diet ; Digestive System ; Gases ; Inflammation ; Ketoprofen ; Medicago sativa ; Models, Theoretical*

BACKGROUND: Epidural administration of dexamethasone has been suggested for pain control after minor orthopedic surgery. This study was conducted to assess its efficacy after such surgery, combined or not to IV dipyrone, IV parecoxibe or their combination. METHODS: 91 patients were randomly assigned to seven groups. Patients were submitted to spinal bupivacaine anesthesia combined to epidural administration of either 10 ml saline or 10 mg dexamethasone diluted to 10-ml volume. Patients also received 10 ml IV saline or 1 gr dipyrone and/or 40 mg parecoxibe diluted to 10 ml with saline. Control group (CG) received epidural and IV saline. Dexamethasone group (DexG) received epidural dexamethasone and IV saline. Dipyrone group (DipG) received epidural saline and IV dipyrone. Dex-Dip G received epidural dexamethasone and IV dipyrone. Parecoxibe group (ParG) received epidural saline and IV parecoxibe. Dex-ParG received epidural dexamethasone and IV parecoxibe. Finally, Dex-Dip-ParG received epidural dexamethasone and IV dipyrone plus IV parecoxibe. RESULTS: The CG expressed 4h of analgesia and sooner requested pain killer. DexG was similar to DipG or ParG or Dex-ParG (7-hours), and they requested less ketoprofen compared to the CG (P < 0.05). However, the Dex-DipG and the Dex-Dip-ParG resulted in longer time to demand pain killer (17-hours) and less ketoprofen consumption in 24-hours (P < 0.002). Adverse effects were similar among groups. CONCLUSIONS: The analgesia secondary to epidural dexamethasone was enhanced by IV dipyrone, while no effects were observed by the addition of IV parecoxibe.
Analgesia ; Anesthesia ; Bupivacaine ; Dexamethasone ; Dipyrone ; Humans ; Ketoprofen ; Orthopedics ; Pain, Postoperative

Nicolau syndrome is a rare complication of intramuscular injection consisting of ischemic necrosis of skin, soft tissue, and muscular tissue that arises locoregionally. The characteristic pattern is pain around the injection site, developing into erythema, a livedoid dermatitis patch, and necrosis of the skin, subcutaneous fat, and muscle tissue. Three patients were injected with drugs (diclofenac sodium, ketoprofen, meperidine) for pain relief. Three patients complained of pain, and a skin lesion was observed, after which necrosis developed on their buttocks. Each patient underwent debridement and coverage. The wound healed uneventfully. We report three cases of Nicolau syndrome in the buttocks following diclofenac intramuscular injection.
Buttocks ; Debridement ; Dermatitis ; Diclofenac ; Erythema ; Humans ; Injections, Intramuscular ; Ketoprofen ; Muscles ; Necrosis ; Skin ; Sodium ; Subcutaneous Fat

We screened a strain NK13 for a certain extent asymmetric hydrolysis the rac-ketoprofen Chloroethyl ester to (S)-Ketoprofen. As identified, NK13 was Bacillus megaterium. Digested NK13 genomic DNA with Sau3AI partially and recovered the fragment from 2 kb to 6 kb, cleaved the plasmid of pUC18 with BamH I, ligated the 2-6 kb fragment of NK13 genomic DNA into pUC18 plasmid, and then transformed an Escherichia coli strain DH5alpha. We created the gene library of NK13 and obtained a positive clone, pUC-NK1 in the library from the tributyrin flat. The result of sequencing showed that there was a whole open read frame (ORF) of 633 bp lipase gene in the plasmid of pUC-NK1. To compare with the genes of GenBank, this lipase gene was reported firstly (GenBank Accession No. EU381317). The lipase gene was amplified by PCR, using pUC-NK1 plasmid as template, and subcloned into the high expression vector pET21b(+) under the control of T7 promoter. The recombinant plasmid, pET-NKest1, was then transformed into an Escherichia coli strain BL21 (DE3) for the production of recombinant lipase protein. After 3 hours of induction by isopropyl-beta-D-thiogalactoside (IPTG), lipase was expressed. SDS-PAGE analysis showed that the relative molecular mass of the lipase protein was about 20 kDa. The result of high performance liquid chromatography (HPLC) showed that the conversion rate of the recombinant strain was fifty times than the wild strain NK13's. The (S)-Ketoprofen enantiomeric excess of the recombinant strain was 75.28%, which indicated that the lipase could hydrolyze (S)-Ketoprofen Chloroethyl ester firstly. If we research the conditions of the hydrolysis rac-ketoprofen Chloroethyl ester of this lipase further, maybe it could offer a foundation to product (S)-Ketoprofen industrially.
Amino Acid Sequence ; Bacillus megaterium ; genetics ; isolation & purification ; metabolism ; Base Sequence ; Cloning, Molecular ; Escherichia coli ; genetics ; metabolism ; Ketoprofen ; analogs & derivatives ; chemistry ; isolation & purification ; Lipase ; biosynthesis ; genetics ; Molecular Sequence Data ; Open Reading Frames ; genetics ; Recombinant Proteins ; biosynthesis ; genetics ; Stereoisomerism

OBJECTIVETo study the stability and degradation kinetics of Ketoprofen-Paeonol conjugate (Ket-Pae).

METHODRP-HPLC method was used to determine the solubility and partition coefficient of Ket-Pae. Stability test was carried out to investigate the factors affecting Ket-Pae. The kinetic studies of Ket-Pae degradation were conducted in different pH buffer solutions and 80% rat plasma at 37 degrees C.

RESULTKet-Pae showed significant degradation phenomenon at high temperature. The solubility of Ket-Pae was decreased about 200 to 300 times compared with parent drugs in water while the lnP increased about 4 times. The degradation curve displayed a V-shape, and kept maximum stability at week acidic (pH 5.0, t(1/2) = 11.4 d). Ket-Pae degraded quickly with very short half life of 1.3 min in plasma, therefore easily released ketoprofen and paeonol.

CONCLUSIONThe lipophilicity of Ket-Pae is increased, its stability is affected by temperature and pH value.

Acetophenones ; chemistry ; Drug Stability ; Drugs, Chinese Herbal ; chemistry ; Hydrogen-Ion Concentration ; Ketoprofen ; chemistry ; Kinetics ; Solubility

OBJECTIVETo evaluate the clinical efficacy and safety of dexketoprofen trometamol in the treatment of patients with chronic prostatitis/chronic pelvic pain syndrome (CP/CPPS).

METHODSA total of 115 patients with CP/CPPS were divided into a dexketoprofen trometamol group (n = 40), treated with dexketoprofen trometamol (25 mg, tid) and terazosin (2 mg, qn), an indometacin group (n = 40) given indometacin (25 mg, tid) and terazosin (2 mg, qn), and a terazosin group (n = 35) administered terazosin (2 mg, qn) only, all treated for 4 weeks. Scores on the NIH-chronic prostatitis symptom index (NIH-CPSI) were obtained before and after the treatment, and the efficacy and adverse events were observed and compared.

RESULTSThe NIH-CPSI scores were significantly improved after the treatment in all the three groups. The clinical efficacy was significantly better in the dexketoprofen trometamol and indometacin groups than in the terazosin group (P < 0.05), but with no significant difference between the former two (P > 0.05). The rates of adverse events were 10.00%, 18.57% and 27.50% in the dexketoprofen trometamol, terazosin and indometacin groups, significantly lower in the former two than in the latter one (P < 0.05).

CONCLUSIONThe combination of dexketoprofen trometamol with terazosin could effectively improve the clinical symptoms of CP/CPPS, better than terazosin in therapeutic efficacy and than indometacin in drug tolerance.

Adult ; Chronic Disease ; Humans ; Indomethacin ; administration & dosage ; therapeutic use ; Ketoprofen ; administration & dosage ; analogs & derivatives ; therapeutic use ; Male ; Pelvic Pain ; drug therapy ; Prazosin ; administration & dosage ; analogs & derivatives ; therapeutic use ; Prostatitis ; drug therapy ; Tromethamine ; administration & dosage ; analogs & derivatives ; therapeutic use

OBJECTIVETo compare therapeutic effects, safety and tolerance of TCM, western medicine and integrated Chinese and western medicine for treatment of acute lumbosacral pain induced by prolapse of lumbar intervertebral disc.

METHODSNinety cases were randomly divided into 3 groups, 30 cases in each group. They were treated respectively with western medicine, TCM and combined TCM and western medicine, and the pain intensity, activity, muscular tension, and other indexes were monitored after 7 days and 30 days of treatment.

RESULTSAfter treatment of 7 days, the combined treatment group in improvement of VAS scores of lumbosacral pain and radiating pain of the lower limbs was superior to the TCM group with no significant difference between the two groups, and in improvement of VAS scores of lumbosacral pain and radiating pain of the lower limbs, Lasegue's sign, activity of spinal column (Schober test and distance from finger tip to floor), etc. were superior to the western medicine group (P < 0.05). After treatment of 30 days, there was no significant differences in the therapeutic effect among the 3 groups. The patients in the 3 groups had good tolerance with no severe adverse reaction.

CONCLUSIONCombined TCM and western medicine treatment has rapid effects and definite therapeutic effect in alleviating pain, improving activity for acute lumbosacral pain induced by prolapse of lumbar intervertebral disc.

Benzodiazepines ; therapeutic use ; Humans ; Intervertebral Disc Displacement ; therapy ; Ketoprofen ; therapeutic use ; Lumbar Vertebrae ; Medicine, East Asian Traditional

AIMTo investigate the in vitro recovery and influencing factors of ketoprofen in microdialysis probe, and study the pharmacokinetic of unbound ketoprofen in rat after iv administration.

METHODSThe recovery of ketoprofen was detected by a concentration difference method. After microdialysis probe was inserted into the jugular vein of male Wistar rats, the probe was infused with various concentrations perfusate. The in vivo recovery and the pharmacokinetics of unbound ketoprofen in rat were investigated. Dialysate samples were determined by HPLC.

RESULTSThe recovery detected by gain was as the same as that by loss; the recovery was independent of the drug concentration surrounding the probe. The in vitro recovery was 28.75% by concentration difference method and the in vivo recovery was (40.3 +/- 2.7) % by retrodialysis method. After i.v. administration of ketoprofen in rat, T 1/2, AUC and CL of unbound ketoprofen were (181 +/- 16) min, (112 +/- 27) microg x min x mL(-1) and (0.22 +/- 0.05) L x min(-1), respectively.

CONCLUSIONMicrodialysis sampling can be used for the pharmacokinetic study of unbound ketoprofen in rat.

Animals ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; pharmacokinetics ; Area Under Curve ; Chromatography, High Pressure Liquid ; Injections, Intravenous ; Ketoprofen ; administration & dosage ; pharmacokinetics ; Male ; Microdialysis ; methods ; Rats ; Rats, Wistar