Reference

Dexketoprofen trometamol in postoperative pain management

Some chemicals with cas registry numbers like 156604-79-4 are also used. Dexketoprofen trometamol in postoperative pain management. Burke, Daniel; Bannister, Jonathan (Department of Anaesthesia, St. John's Hospital at Howden, Livingston EH54 6PP, UK). Acute Pain, 5(2), 57-62 (English) 2003 Elsevier Science Ltd. CODEN: ACPAFS. ISSN: 1366-0071. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) A review. Dexketoprofen trometamol is the dextrorotatory enantiomer of ketoprofen formulated as the tromethamine salt. Producing a single isomer formulation of ketoprofen simplifies the pharmacokinetics of the drug and allows a 50% redn. in dosage. This may reduce adverse effects by reducing metabolic and renal load. Formulation as the tromethamine salt results in faster absorption from the gut and therefore quicker onset of analgesia. This paper reviews studies of the use of dexketoprofen in acute postoperative pain, and concludes that it produces rapid and reliable onset of analgesia. .

Preclinical and clinical development of dexketoprofen

Preclinical and clinical development of dexketoprofen. Mauleon, David; Artigas, Remei; Garcia, M. Luisa; Carganico, Germano (Laboratorios Menarini SA, Research and Development Department, Barcelona, Spain). Drugs, 52(Suppl. 5), 24-46 (English) 1996 Adis. CODEN: DRUGAY. ISSN: 0012-6667. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) A review, with 163 refs. Dexketoprofen trometamol is a water-sol. salt of the dextro-rotatory enantiomer of the nonsteroidal anti-inflammatory drug (NSAID) ketoprofen. Racemic ketoprofen is used as an analgesic and an anti-inflammatory agent, and is one of the most potent in vitro inhibitors of prostaglandin synthesis. This effect is due to the S(+)-enantiomer (dexketoprofen), while the R(-)-enantiomer is devoid of such activity. The pharmacokinetic profile of ketoprofen and its enantiomers was assessed in several animal species and in human volunteers. In humans, the relative bioavailability of oral dexketoprofen trometamol (12.5 and 25mg, resp.) is similar to that of oral racemic ketoprofen (25 and 50mg, resp.), as measured in all cases by the area under the concn.-time curve values for S(+)-ketoprofen. Dexketoprofen trometamol, given as a tablet, is rapidly absorbed, with a time to max. plasma concn. (tmax) of between 0.25 and 0.75 h, whereas the tmax for the S-enantiomer after the racemic drug, administered as tablets or capsules prepd. with the free acid, is between 0.5 and 3 h. 156604-79-4 and 22071-15-4 which are cas registry numbers are also used here. Peak plasma concns. of 1.4 and 3.1 mg/L are reached after administration of dexketoprofen trometamol 12.5 and 25mg, resp. From 70 to 80% of the administered dose is recovered in the urine during the first 12 h, mainly as the acyl-glucuronoconjugated parent drug. No R(-)-ketoprofen is found in the urine after administration of dexketoprofen [S(+)-ketoprofen], confirming the absence of bioinversion of the S(+)-enantiomer in humans. In animal studies, the anti-inflammatory potency of dexketoprofen was always equiv. to that demonstrated by twice the dose of ketoprofen. Similarly, animal studies showed a high analgesic potency for dexketoprofen trometamol. The R(-)-enantiomer demonstrated a much lower potency, its analgesic action being apparent only in conditions where the metabolic bioinversion to the S(+)-enantiomer was significant. The gastric ulcerogenic effects of dexketoprofen at various oral doses (1.5 to 6 mg/kg) in the rat do not differ from those of the corresponding double doses (3 to 12 mg/kg) of racemic ketoprofen. Repeated (5-day) oral administration of dexketoprofen as the trometamol salt causes less gastric ulceration than was obsd. after the acid form of both dexketoprofen and the racemate. In addn., single dose dexketoprofen as the free acid at 10 or 20 mg/kg does not show a significant intestinal ulcerogenic effect in rats, while racemic ketoprofen 20 or 40 mg/kg is clearly ulcerogenic to the small intestine. The analgesic efficacy of oral dexketoprofen trometamol 10 and 20mg is superior to that of placebo and similar to that of ibuprofen 400mg in patients with moderate to severe pain after third molar extn. The time to onset of pain relief appeared to be shorter in patients treated with dexketoprofen trometamol than in those treated with ibuprofen 400mg. Dexketoprofen trometamol was well tolerated, with a reported incidence of adverse events in similar to that of placebo. .