Chondroitin
Scientific Name(s):Chondroitin sulfate, chondroitin sulfuric acid, chonsurid, structum
Common Name(s): Chondroitin
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Uses of Chondroitin
Chondroitin has been used to treat arthritis. It has also been studied for use in drug delivery, antithrombotic and extravasation therapy.
Chondroitin Dosing
Chondroitin sulfate has been administered orally for treatment of arthritis at a dose of 800 to 1200 mg/day. Positive results often require several months to manifest, and a posttreatment effect has been observed. 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8
Contraindications
Contraindications have not yet been identified.
Pregnancy/Lactation
Information regarding safety and efficacy in pregnancy and lactation is lacking.
Chondroitin Interactions
None well documented.
Chondroitin Adverse Reactions
There are no reports in the literature of any major adverse reactions.
Toxicology
There is little information on chondroitin's long-term effects. Most reports conclude that it is not harmful.
Chondroitin is a biological polymer that acts as the flexible connecting matrix between the protein filaments in cartilage. 9 Chondroitin can be isolated from natural sources, such as shark or bovine cartilage. 10 Danaparoid sodium, a mixture of heparan sulfate, dermatan sulfate and chondroitin sulfate (21:3:1), is derived from porcine intestinal mucosa. 11
History
Chondroitin sulfates were first extracted and purified in 1960. Studies suggested that if enough chondroitin sulfate was available to cells manufacturing proteoglycan (one of the substances that forms the cartilage matrix), stimulation of matrix synthesis could occur, leading to an accelerated healing process. 12 This idea of natural regeneration of cartilage has been popularized with the publication of the book, “The Arthritis Cure.” 13
Chemistry
Chondroitin sulfate is a high-viscosity mucopolysaccharide (glycosaminoglycan) with N-acetylchondrosine as a repeating unit and one sulfate group per disaccharide unit. Its molecular weight is about 50,000, depending on product source or preparation. 9 Danaparoid sodium (a mixture containing chondroitin) has a lower molecular weight (5500 to 6000). 11 Analytical determination including HPLC, spectrophotometric analysis, chemical methods, ultraviolet spectrometry, and IR spectroscopy has been performed on chondroitin and its related structures. 14 , 15 , 16 , 17 , 18 A method for potentiometric titration of chondroitin sulfate has also been reported. 19
Chondroitin Uses and Pharmacology
The pharmacokinetics of chondroitin sulfate have been determined in rats and dogs. 20 Another pharmacokinetic study, involving eight healthy volunteers, reports similar results in metabolism to those in animals. Other parameters evaluated included half-lives of distribution and elimination, volumes of distribution, excretion values, urine and blood levels and bioavailability. 21 Another report concludes oral chondroitin sulfate B (dermatan sulfate) to reach significant plasma levels, with 7% bioavailability. 22 In 22 patients with renal failure, chondroitin sulfate half-life was prolonged, but it could be administered for clot prevention during hemodialysis in this population. 23
AntiarthriticChondroitin's role in treating arthritis has gained popularity. Ongoing research continues with some controversial outcomes.
Articular cartilage is found between joints (eg, finger, knee, hip) allowing for easy, painless movement. It contains 65% to 80% water, collagen and proteoglycans. Chondrocytes are also found within this matrix, where they produce new collagen and proteoglycans from building blocks, including chondroitin sulfate, a glycosaminoglycan (GAG). 12 Chondrocytes must derive nutrition from this synovial fluid as there is no vasculature to supply them. 24 Glucosamine, another of the beneficial substances in this area, stimulates chondrocyte activity. It is also the critical building block of proteoglycans and other matrix components. 12 Both chondroitin and glucosamine play vital roles in joint maintenance, which is the reason the combination of the two are found in many arthritic nutritional supplements (eg, “chondroitin complex” by Nature's Bounty, Bohemia, NY; 11716).
In inflammation and repeated wear of the joint, chondrocyte function is disturbed, altering the matrix and causing breakdown. 24 Supplementation with glycosaminoglycans (eg, chondroitin sulfate) may enable chondrocytes to replace proteoglycans, offering “chondroprotection.” 25 Cartilage contains the biological resources to enhance repair of degenerative injuries and inflammation. It has been proposed that a certain chondroitin sulfate sequence, released from cartilage proteoglycans, can inhibit elastase, regulating the matrix. 26
There is considerable controversy regarding absorption of chondroitin. Absorption of glucosamine is 90% to 98%, but chondroitin absorption is only 0% to 13% because chondroitin is 50 to 300 times larger than glucosamine. Chondroitin may be too large to be delivered to cartilage cells. In addition, there also may be purification and identification problems with some chondroitin products, some of which have tested subpotent. 12
The American College of Rheumatology has pointed out that although chondroitin sulfate is readily available in health food stores, the supplements are not regulated by the Food and Drug Administration. Longer-term clinical trials, with larger groups of people are warranted to determine whether or not it is safe and effective. They also warn against discontinuation of conventional therapy without consulting a physician and stress the importance of maintaining proper body weight and exercising. 27
General reviews are available on chondroitin sulfate and chondroitin sulfate B. 28 , 29
Animal dataResearch reveals no animal data regarding the use of chondroitin as an antiarthritic.
Clinical dataResults of a multicenter study of chondroitin sulfate in finger, knee and hip joint therapy are comparable with other international, double-blind, placebo controlled studies, all indicating beneficial results in osteoarthritis treatment. 30 An overview of chondroitin sulfate in another report, however, concluded the product has no clear value in osteoarthritis treatment. 31
AntithromboticAnimal data
Research reveals no animal data regarding the use of chondroitin as an antithrombotic.
Clinical dataChondroitin sulfate B (dermatan sulfate) has potential as an antithrombotic agent, as it inhibits venous thrombi, with less effect upon bleeding than heparin. It is an effective anticoagulant in hemodialysis. 32 Another study found dermatan sulfate to have no direct, observable relation to heparin aggregation. 33 Dermatan sulfate's efficacy, compared with heparin, has been determined in acute leukemia patients. 34
Other usesChondroitin sulfate has been used to treat extravasation after ifosfamide therapy, decreasing pain and inflammation. 35 It has also been used to treat extravasation from vindesine, 36 doxorubicin and vincristine 37 and an etoposide needlestick injury in a healthcare worker. 38
Chondroitin sulfate has been used as a drug delivery system for diclofenac and flurbiprofen. 39 Additionally, the polymer has been used as a stabilization agent for iron injection hyperalimentation. 40
Levels of chondroitin sulfate increase 10 to 100 times in tumors compared with normal tissue. In one report, all 44 cancer patients analyzed showed elevated levels of urinary chondroitin sulfate. This may provide a potential new marker for diagnosis and follow-up of cancer therapy. 41
Dosage
Chondroitin sulfate has been administered orally for treatment of arthritis at a dose of 800 to 1200 mg/day. Positive results often require several months to manifest, and a posttreatment effect has been observed. 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8
Pregnancy/Lactation
Information regarding safety and efficacy in pregnancy and lactation is lacking.
Interactions
None well documented.
Adverse Reactions
There are no reports in the literature of any major adverse reactions.
Toxicology
Little information about long-term toxic effects of chondroitin sulfate is available. Most reports conclude that it is not harmful compared with other arthritis therapies, such as NSAIDs. Because the drug is concentrated in cartilage, the theory is that it produces no toxic or teratogenic effects. 30 Long-term clinical trials with larger populations are needed to fully determine toxicity. 27
Bibliography
1. Morreale P, Manopulo R, Galati M, Boccanera L, Saponati G, Bocchi L. Comparison of the antiinflammatory efficacy of chondroitin sulfate and diclofenac sodium in patients with knee osteoarthritis. J Rheumatol . 1996;23:1385-1391.2. Mazieres B, Combe B, Phan Van A, Tondut J, Grynfeltt M. Chondroitin sulfate in osteoarthritis of the knee: a prospective, double blind, placebo controlled multicenter clinical study. J Rheumatol . 2001;28:173-181.
3. Uebelhart D, Thonar EJ, Delmas PD, Chantraine A, Vignon E. Effects of oral chondroitin sulfate on the progression of knee osteoarthritis: a pilot study. Osteoarthritis Cartilage . 1998;6(suppl A):39-46.
4. Verbruggen G, Goemaere S, Veys EM. Chondroitin sulfate: S/DMOAD (structure/disease modifying anti-osteoarthritis drug) in the treatment of finger joint OA. Osteoarthritis Cartilage . 1998;6(suppl A):37-38.
5. Bucsi L, Poor G. Efficacy and tolerability of oral chondroitin sulfate as a symptomatic slow-acting drug for osteoarthritis (SYSADOA) in the treatment of knee osteoarthritis. Osteoarthritis Cartilage . 1998;6(suppl A):31-36.
6. Bourgeois P, Chales G, Dehais G, Delcambre B, Kuntz JL, Rozenberg S. Efficacy and tolerability of chondroitin sulfate 1200 mg/day vs chondroitin sulfate 3 × 400 mg/day vs placebo. Osteoarthritis Cartilage . 1998;6(suppl A):25-30.
7. Das A Jr, et al. Efficacy of a combination of FCHG49 glucosamine hydrochloride, TRH122 low molecular weight sodium chondroitin sulfate and manganese ascorbate in the management of knee osteoarthritis. Osteoarthritis Cartilage . 2000;8:343-350.
8. Conrozier T. Anti-arthrosis treatments: efficacy and tolerance of chondroitin sulfates (CS 4&6) [in French]. Presse Med . 1998;27:1862-1865.
9. Budavari S, et al, eds. The Merck Index , 11th ed. Rahway: Merck and Co., 1989.
10. Ma S, et al. Chin Pharm J . 1993 Dec 28;741-43.
11. Reynolds J, ed. Martindale, the Extra Pharmacopoeia , 13th ed. London: Royal Pharmaceutial Society, 1996.
12. Benedikt H. Nat Pharm . 1997;1(8):1,22.
13. Theodosakis J. The Arthritis Cure. New York, NY: St. Martin's Press, 1997.
14. Murata K, et al. J Biochem Biophys Methods . 1987;15(1):23-32.
15. Fabregas, et al. Pharm Acta Helvetiae . 1981;56(9-10):265-67.
16. Volpi N, et al. Farmaco . 1992 May;47 Suppl:841–53.
17. Brizzi V. Farmacia e Clinica . 1990;29(1):3-8.
18. Ovsepyan A, et al. Pharm Chem J . 1979 Sep;13:986-90.
19. Mascellani G, et al. Farmaco Ed Prat . 1988 May;43:165-75.
20. Conte A, et al. Arzneimittel-Forschung . 1995;45(8):918-25
21. Conte A, et al. Arzneimittel-Forschung . 1991;41(7):768-72.
22. Dawes J, et al. Br J Clin Pharm . 1991 Sep;32:361-6.
23. Gianese F, et al. Br J Clin Pharm . 1993 Mar;35:335-39.
24. Krane S, et al. Eur J Rheumatol Inflamm . 1990;10(1):4-9.
25. Pipitone V. Drugs Exp Clin Res . 1991;17(1):3-7.
26. Paroli E. Int J Clin Pharmacol Res . 1993;13 Suppl:1-9.
27. American College of Rheumatology Patient Information WEB page (60 Executive Park S. Ste. 150, Atlanta, GA 30329), 1997. http://www.rheumatology.org/patients/factsheets.html .
28. Dosa E, et al. Acta Pharm Hungarica . 1977 May;47:102-12.
29. Tamagnone G, et al. Drugs of the Future . 1994 Jul;19:638-40.
30. Leeb B, et al. Wien Med Wochenschr . 1996;146(24):609-14.
31. Anonymous. Prescrire Int . 1995;4(20):165-67.
32. Lane D, et al. Lancet . 1992 Feb 8;339:334-5.
33. Racey T, et al. J Pharm Sci . 1989 Mar;78:214-18.
34. Cofrancesco E. Lancet . 1992 May 9;339:1177-78.
35. Mateu J, et al. Ann Pharmacother . 1994 Nov;28:1243-44.
36. Mateu J, et al. Ann Pharmacother . 1994 Jul-Aug;28:967-68.
37. Comas D, et al. Ann Pharmacother . 1996 Mar;30:244-46.
38. Mateu J, et al. Am J Health-System Pharm . 1996 May 1;53:1068,1071.
39. Murata Y, et al. J Controlled Release . 1996 Feb;38:101-8.
40. Yamaji A, et al. J Nippon Hosp Pharm Assoc . 1979 Jan;5:30-35.
41. Dietrich C, et al. Lab Invest . 1993;68(4):439-45.
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