YOU ARE NOW CONNECTED TO THE TOXLINE (1981 FORWARD, NON-ROYALTY) FILE. ==SULFATE CURES AND ARTHRITIS== 1 AUTHOR Rovetta G TITLE Galactosaminoglycuronoglycan sulfate (matrix) in therapy of tibiofibular osteoarthritis of the knee. SOURCE Drugs Exp Clin Res; VOL 17, ISS 1, 1991, P53-7 ABSTRACT To evaluate the efficacy and tolerance of galactosaminoglycuronoglycan sulfate (Matrix vials) in the therapy of tibiofibular arthritis of the knee, forty patients suffering from this illness at radiological stages 1 and 2 undergoing concomitant therapy with NSAIDS, were randomized into two groups of twenty. The treatment group received the drug under study and the control group received placebo. Treatment was carried out in double blind. The therapy protocol comprised 25 intramuscular injections (one injection twice a week). This cycle was repeated for 6 months, for a total of 50 injections. The patients were visited on days 0, 90, 180, 240, 330 and 360. At each visit the following symptoms were evaluated: spontaneous pain, pain on loading, on passive movement and on pressure; changes in NSAIDS posology were also recorded; lastly any possible side effects were noted. Analysis of results has shown a statistically significant higher therapeutic effect on treatment with Matrix for all the symptoms taken into consideration. No important side effects were noted, either local or systemic; in two cases only in the group treated with Matrix and in the same number in the control group slight dyspeptic symptoms were found to occur, but without requiring suspension or reduction in posology. Two patients in the Matrix group and one in the control group left the study for non-compliance with the type of administration. The good clinical results obtained, together with the excellent tolerance shown by the drug, suggest that Matrix may be the drug of choice in the "basic" therapy of osteoarthritis, with its efficacy being demonstrated in an increasing number of clinical studies. 2 AUTHOR Stockwell RA AUTHOR Sprinz R TITLE Glycosaminoglycan content and cell density of rabbit articular cartilage in experimental lipoarthrosis. SOURCE J Anat; VOL 133, ISS Pt 2, 1981, P309-15 ABSTRACT Glycosaminoglycan content and cell density of articular cartilage have been studied quantitatively in the adult rabbit in experimental lipoarthrosis. On the fourth day after injection of non-radioactive or tritium-labelled glyceryl trioleate into the synovial cavity of the knee joint, femoral condylar cartilage shows no change in cellularity. There is a 35% loss of chondroitin sulphate from the matrix, but little change in keratansulphate. The results are not affected by the presence or absence of radioactive isotope in the lipid: possible mechanisms accounting for glycosaminoglycan loss are discussed. 1 AUTHOR Kato Y AUTHOR Mukudai Y AUTHOR Okimura A AUTHOR Shimazu A AUTHOR Nakamura S TITLE Effects of hyaluronic acid on the release of cartilage matrix proteoglycan and fibronectin from the cell matrix layer of chondrocyte cultures: interactions between hyaluronic acid and chondroitin sulfate glycosaminoglycan. SOURCE J Rheumatol Suppl; VOL 43, 1995, P158-9 ABSTRACT Hyaluronic acid (HA) of large sizes suppressed the release of cartilage matrix proteoglycan, fibronectin, and other macromolecules from the cell matrix layer of chondrocyte cultures, perhaps because HA of large sizes formed a viscous barrier in the matrix by its interactions with other extracellular matrix macromolecules. To test this possibility, we determined the viscosity of solutions containing HA of various sizes in the presence of proteoglycan monomer or chondroitin sulfate glycosaminoglycan (GAG). Not only the monomer but also chondroitin sulfate increased the viscosity of HA solutions, depending on the size of HA. These findings suggest that HA of large sizes increases the viscosity near the surface of articular cartilage by sugar-sugar and by sugar-protein interactions and that the increase of viscosity is involved in the protective action of HA on arthritic cartilage. 2 AUTHOR Pipitone VR TITLE Chondroprotection with chondroitin sulfate. SOURCE Drugs Exp Clin Res 1991;17(1):3-7 ABSTRACT The remarkable insights into the pathogenesis of osteo-arthrosis (OA) have also affected the therapeutic field. Efforts have been made to find drugs which would somehow block or slow down the evolution of this disease. In this connection, a major contribution has been made by the investigations on glycosaminoglycans (GAGs), which play a crucial role in the physiology of joint cartilage. It was thus suggested that proper supplementation with GAGs might enable chondrocytes to replace the proteoglycans (PG). Galactosaminoglucuronoglycan sulfate (GAGGS) has been used for this purpose. In preliminary clinical trials, GAGGS exhibited a remarkable tolerability and good therapeutic efficacy. GAGs are generally able to inhibit certain enzymes present in the synovial fluid which may damage joint cartilage (elastase, hyaluronidase). Moreover, GAGGS has also been shown to act as an anti-inflammatory drug since it has an inhibitory effect over the complement. All these data supply evidence that, in theory, GAGGS may have a chondroprotective effect in patients with OA. In addition to the positive results of preliminary clinical trials, the use of GAGGS in OA therapy is based on the fact that this drug is absorbed by the body, is concentrated in the cartilages and produces no toxic or teratogenic effects. In the clinical studies performed so far, although of the open type, GAGGS has always yielded clinical improvement both of painful symptoms and of limited function thanks to its proven anti-inflammatory activity. Thus once the results from other ongoing trials (double blind) are available, hopefully GAGGS will in fact become a basic drug for OA therapy. 2 AUTHOR Setnikar I TITLE Antireactive properties of "chondroprotective" drugs. SOURCE Int J Tissue React; VOL 14, ISS 5, 1992, P253-61 (REF: 23) ABSTRACT The medicinal therapy of osteoarthritis is based on the use of analgesics, NSAIDs and corticosteroids to relieve pain and inflammation. In addition, "chondroprotective" agents (CPA) are used to stop the evolution of the disease. In this review the biochemical and pharmacological activities of some of the most widely used CPAs are described. All of these show more or less marked antiinflammatory activities, which for some of them are the result of an inhibition of cyclo-oxygenase and of prostaglandin biosynthesis, in which case they should be more properly classified as mild NSAIDs. Only two of the CPAs reviewed, diacerein and D-glucosamine sulfate, elicit antiinflammatory and antireactive effects without significant inhibition of the prostaglandin biosynthesis. These agents have also remarkable chondroprotective effects, and only these two agents should be classified as true CPAs. In particular glucosamine sulfate, which naturally occurs in the human body and is almost devoid of toxicity, is suitable for long-term therapeutic use. This, with its chondrometabolic, antireactive and antiarthritic properties, represents the pharmacological rationale for the use of glucosamine sulfate as a disease-modifying agent in osteoarthritis.