Godara et al Journal of Drug Delivery & Therapeutics; 2013, 3(2), 145-148 145 © 2011, JDDT. All Rights Reserved ISSN: 2250-1177 CODEN (USA): JDDTAO Available online at http://jddtonline.info REVIEW ARTICLE LORNOXICAM: A REVIEW OF ITS THERAPEUTIC POTENTIAL IN DIFFERENT CLINICAL STUDIES *Dr Godara Sushila 1 , Dr Srivastava R K 1 , Dr Godara Rajesh 1 , Dr Bhutani Garima 2 1 Post Graduate Institute of Medical Sciences, Rohtak, Haryana, India 2 BPS, govt. medical college, Khanpur Kalan Sonipat, Haryana, India *Address for correspondence:58/9J, Medical Enclave, PGIMS, Rohtak, Haryana, Email: drgodarasushila@gmail.com , Email: drrajeshgodara@yahoo.co.uk LORNOXICAM Lornoxicam is a relatively new NSAID. It belongs to the oxicam group. Chemically it is a 4-hydroxycarboxamide [6-chloro-4-hydroxy-2-methyl-N-2-pyridyl-5H- thieno( 2,3-e)-[1,2]-thiazine-2-carboxamide-1,1- dioxide]. PHARMACODYNAMIC PROPERTIES As with other nonsteroidal anti-inflammatory agents (NSAIDs), lornoxicam (chlortenoxicam) inhibits prostaglandin (PG) synthesis via inhibition of cyclooxygenase, but it does not inhibit 5- lipoxygenas.lornoxicam inhibits polymorphonuclear (PMN)-leukocyte migration, inhibits the release of superoxide from human PMN-leukocytes, inhibits the release of platelet derived growth factor (PDGF) from human platelets and stimulates the synthesis of proteoglycans in cartilage in tissue culture.Lornoxicam was reported to be 100-fold more potent (on a molar basis) than tenoxicam in inhibiting PGD2 formation in rat polymorphonuclear leucocytes in vitro. 1 Besides its inhibitory effect on COX1 and COX-2 peripheral receptors, is also increases endogenous dinorphin and beta-endorphin levels promoting central analgesic and anti-inflammatory effects. Its analgesic potency in animal pain models exceeds that of tenoxicam and piroxicam by approximately 12 and 13 fold respectively; whereas it is 4 to 6 fold more potent ad compared to indomethacin and diclofenac. Intravenous lonoxicam (8mg) has been shown to be as effective as morphine (20mg), pethidine (50mg) and tramadol (50mg) in the treatment of postoperative pain. 2 PHARMACOKINETIC PROPERTIES Lornoxicam is completely absorbed after oral administration, reaching peak plasma concentrations of 280 mg/L within 2.5 hours after a 4 mg dose. 3 The area under the serum drug concentration-time curve (AUC) is proportional following lornoxicam doses between 2 to 6mg given twice daily for 2 weeks in healthy young volunteers. The Cmax and AUC of lornoxicam did indicate drug accumulation upon repeated administration. 4 Intragastric food delays and reduces the absorption of lornoxicam as demonstrated by an approximate 15% decrease in AUC and an increase in t max from 1.5 to 2.3 hours. After intramuscular injection maximum plasma concentrations are achieved after approximately 20-25 minutes. The absolute bioavailability after intramuscular injection is 97 percent. It is found in the plasma in unchanged form and as its hydroxylated metabolite. The plasma protein binding of lornoxicam is 99 per cent. The apparent volume of distribution of lornoxicam is low (0.3L/Kg). Lornoxicam is extensively metabolished in liver by cytochrome P4502DC9 to inactive metabolite 5’-hydroxy-lornoxicam. Approximately 51 percent drug is excreted in faeces and 42 percent via kidneys as inactive substance. The mean elimination half life is 3 to 4 hours. 5 The drug has been found to be safe in elderly patients, patients with impaired renal function and patients with impaired hepatic functions. 6,7 INTERACTIONS Clonazepam and diazepam inhibit metabolism of lornoxicam. It does not interact with ranitidine and antacids. Concomitant administration of lornoxicam and anticoagulants or platelet aggregation inhibitors may prolong the bleeding time. It may increase the hypoglycemic effect of sulphonylureas and decrease the efficacy of diuretics and ACE inhibitors6. Lornoxicam did not alter phenazone (antipyrine) clearance in healthy volunteers, indicating a lack of effect on hepatic drug metabolising enzymes. ABSTRACT Lornoxicam is a member of the oxicam group of nonsteroidal antiinflammatory drugs (NSAIDs), producing analgesic and antipyretic effects through the non-selective inhibition of cyclo-oxygenase-1 and -2. Besides its inhibitory effect on COX1 and COX-2 peripheral receptors, is also increases endogenous dinorphin and beta-endorphin levels promoting central analgesic and anti-inflammatory effects. Recently, lornoxicam has been introduced in Indian market in oral, intravenous and intramuscular formulations. Lornoxicam is completely absorbed after oral administration, reaching peak plasma concentrations of 280 mg/L within 2.5 hours after a 4 mg dose. After intramuscular injection maximum plasma concentrations are achieved after approximately 20-25 minutes. Lornoxicam is extensively metabolished in liver by cytochrome P4502DC9 to inactive metabolite 5’ -hydroxy-lornoxicam. The mean elimination half life is 3 to 4 hours. There is plenty of literature available on the effect of lornoxicam on chronic and acute pain management. These preliminary finding require confirmation in further comparative studies. Key words: lornoxicam, analgesic, anti inflammatory drugs.