Piroxicam pharmacologic activity and gastrointestinal damage by oral and rectal route. Comparison with oral indometacin and phenylbutazone. 1981

P Schiantarelli, and S Cadel

An experimental comparative study was conducted on 4-hydroxy-2-methyl-N-(2-pyridyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide (piroxicam), indometacin and phenylbutazone for antiinflammatory and analgesic effects and for gastric and intestinal damage. In some of the experimental models used a comparison was made between oral and rectal piroxicam. The upshot was that: the antiinflammatory activity of piroxicam on carrageenin edema in the rat is equivalent by oral and by rectal route, about twice that of indometacin and 20 times that of phenylbutazone. The inhibition of leucocyte migration in the rat was equal to that of indometacin and 20 times that of phenylbutazone. The analgesic activity of piroxicam (phenylquinone writhings in the mouse) was about 1/4 that of indometacin and 70 times that of phenylbutazone. The ulcerogenic effect of piroxicam on the stomach of the rat was about 1/3 that of indometacin and 5 times greater than that of phenylbutazone. Rectal administration halves the ulcerogenic effect of oral piroxicam. The intestinal perforating effect of piroxicam in the rat is about 1/6 that of indometacin and about 15 times that of phenylbutazone. The therapeutic index, i.e., the ratio of antiinflammatory potency to gastrointestinal damage, proved to be appreciably higher for piroxicam than for the two reference standards. Rectal administration carries an even higher therapeutic index and so appears to be a potentially valuable alternative route in clinical practice.

UI MeSH Term Description Entries
D007213 Indomethacin A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES. Amuno,Indocid,Indocin,Indomet 140,Indometacin,Indomethacin Hydrochloride,Metindol,Osmosin
D007962 Leukocytes White blood cells. These include granular leukocytes (BASOPHILS; EOSINOPHILS; and NEUTROPHILS) as well as non-granular leukocytes (LYMPHOCYTES and MONOCYTES). Blood Cells, White,Blood Corpuscles, White,White Blood Cells,White Blood Corpuscles,Blood Cell, White,Blood Corpuscle, White,Corpuscle, White Blood,Corpuscles, White Blood,Leukocyte,White Blood Cell,White Blood Corpuscle
D008297 Male Males
D010653 Phenylbutazone A butyl-diphenyl-pyrazolidinedione that has anti-inflammatory, antipyretic, and analgesic activities. It has been used in ANKYLOSING SPONDYLITIS; RHEUMATOID ARTHRITIS; and REACTIVE ARTHRITIS. Diphenylbutazone,Fenilbutazon,Butacote,Butadion,Butadione,Butapirazol,Butapyrazole,Butazolidin
D010894 Piroxicam A cyclooxygenase inhibiting, non-steroidal anti-inflammatory agent (NSAID) that is well established in treating rheumatoid arthritis and osteoarthritis and used for musculoskeletal disorders, dysmenorrhea, and postoperative pain. Its long half-life enables it to be administered once daily. CP-16171,Feldene,CP 16171,CP16171
D011725 Pyridines Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
D012007 Rectum The distal segment of the LARGE INTESTINE, between the SIGMOID COLON and the ANAL CANAL. Rectums
D002464 Cell Migration Inhibition Phenomenon of cell-mediated immunity measured by in vitro inhibition of the migration or phagocytosis of antigen-stimulated LEUKOCYTES or MACROPHAGES. Specific CELL MIGRATION ASSAYS have been developed to estimate levels of migration inhibitory factors, immune reactivity against tumor-associated antigens, and immunosuppressive effects of infectious microorganisms. Chemotaxis Inhibition,Chemotaxis Inhibitions,Inhibition, Chemotaxis,Inhibitions, Chemotaxis
D004487 Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE. Dropsy,Hydrops,Anasarca
D005767 Gastrointestinal Diseases Diseases in any segment of the GASTROINTESTINAL TRACT from ESOPHAGUS to RECTUM. Cholera Infantum,Gastrointestinal Disorders,Functional Gastrointestinal Disorders,Gastrointestinal Disorders, Functional,Disease, Gastrointestinal,Diseases, Gastrointestinal,Functional Gastrointestinal Disorder,Gastrointestinal Disease,Gastrointestinal Disorder,Gastrointestinal Disorder, Functional

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