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Pharmacology: Pharmacodynamics: Glucosamine is a natural substance found in chitin, mucoproteins, and mucopolysaccharides. It is involved in the manufacture of glycosaminoglycan, which forms cartilage tissue in the body; Glucosamine is also present in tendons and ligaments. Glucosamine must be synthesized by the body but the ability to do this declines with age. Glucosamine and its salts have therefore been advocated in the treatment of rheumatic disorders including osteoarthritis. Glucosamine also acts to improve the viscosity of synovial fluid by increasing synovial fluid production, thereby providing lubricant activity.
Methylsulfonylmethane (MSM) is an organic sulfur-containing compound that occurs naturally in a variety of fruits, vegetables, grains and animals including humans. It blocks the inflammatory process and enhances the activity of cortisol, a natural anti-inflammatory hormone produced in the body. MSM is an effective natural analgesic and has been used as an application for pain relief over arthritis joints.
Chondroitin is an acid mucopolysaccharide that is a constituent of most cartilaginous tissues. It is given orally in reactive arthritides such as gonococcal arthritis and given with Glucosamine for its supposed chondroprotective action in bone, joint, and connective tissue disorders. Chondroitin is an important structural component of cartilage and provides much of its resistance to compression. This combination therapy works synergistically to stimulate cartilage cell growth and provide strength to cartilage.
Pharmacokinetics: Absorption: After oral administration, bioavailability of Glucosamine is low due to first-pass hepatic metabolism ~26%. The gastrointestinal absorption is close to 90%.
Distribution: Glucosamine is not protein-bound, but rather incorporates into plasma proteins (primarily globulins). Volume of distribution is 2.5 liters.
Metabolism: Liver, extensive. The first-pass effect in the liver in which more than 70% of Glucosamine is metabolized.
Excretion: Renal excretion 10%; Faeces 11%.
Metabolism and excretion of MSM found the primary metabolite became detectable in serum approximately 2 hours after ingestion of MSM. With continued MSM ingestion, metabolite maintained a steady concentration in the serum. When MSM was stopped after 14 days, the mean metabolite concentration declined slowly over the subsequent 96 hours, and only trace amounts were detectable after 5 days. The decline in serum metabolite was linear, and its half-life appeared to be about 38 hours. Metabolite has been shown to persist in the blood up to 5 times longer than MSM.
Earlier studies using high molecular weight Chondroitin concluded that there was no significant absorption of the high molecular weight version of Chroindoitin. More recent studies demonstrate that there is probably significant absorption of low molecular weight Chondroitin. Absorption appears to occur from the stomach and small intestine. There is also an indication that some Chondroitin, after absorption, does enter the joint space. In a study using depolymerized shark Chondroitin, approximately 30% of the administered drug (as high and low molecular weight derivatives) was absorbed. Once absorbed, the Chondroitin is incorporated into glycosaminoglycan-rich tissues such as joint cartilage.
