Glucosamine

General Information

Common Name:
Glucosamine

Scientific Name:

2_Amino-2 deoxyglucose

Other Names:

• Chitosamine;
• Glucosamine sulphate.

What is it?

An Aminoglycoside or Aminosugar. Glucosamine is not an herbal extract. Glucosamine is prepared synthetically or extracted from shellfish. It is found in cell membranes, mucopolysaccharides, and chitin, the horny substance in the exoskeleton of crabs, beetles, and various marine invertebrates and microorganisms. It is included in this section because of its efficacy as an alternative treatment of osteoarthritis.

Arthritis Plan

(Ref: The Arthritis cure plan by Dr. Theodosakis).

Number

Action

Comment

• Consultations with a physician. The author encourages a proper diagnosis be made;
• Glucosamine and chondroitin sulphate. Doses outlined – adjusted versus symptoms and divide 2-4 time/day;
• Vitamin C 500 – 4000mg and Manganese 50mg. Antioxidants;
• Improve biomechanics. Physiotherapists/Sports medicine/Neuromuscular therapists;
• Exercise PhyPhysiotherapists/Sports medicine/ Neuromuscular therapists;
• Healthy diet. Encouraged strongly;
• Fight Depression. Very important;
• Use traditional medications. Surgery is a final option only;
• Maintain a positive attitude. Don’t obsess about the condition.

Indications & Historical Uses

Relief of osteoarthritis. Other recommended uses are for tendonitis and, bursitis. Glucosamine is sold as a dietary supplement to decrease pain and improve mobility in people suffering from osteoarthritis ,a progressive disease of cartilage degeneration. It is also billed as a chemical to support healthy joint and connective tissue. It has been suggested ,by some sources , that it may even prevent or postpone the development of osteoarthritis in certain groups ,such as the elderly and the athletes.

Contraindications & Precautions

Contraindications:
None known. See Caution.

Precautions:
Patients allergic to sulphates should take glucosamine Hydrochloride (not sulphate). Also these patients must not take Chondroitin Sulfate. Since Glucosamine is extracated from shellfish, persons who are allergic to shellfish should exercise caution, though there have been no reported cases of these allergies to glucosamine. See Caution.

Adverse Side Effects:
Rare cases of nausea, vomiting, diarrhea have been reported.

Drug Interactions:
No known drug interactions. It is safe to take glucosamine with blood pressure medications, non-steroidal anti inflammatory drugs, and for diabetics on hypoglycaemic agents. ( but close monitoring of blood sugar levels is recommended).

Dosage Information

How Supplied:

500mg capsules.

Dosage:

Daily Doses of Glucosamine and Chondroitin sulphate:

Weight Glucosamine Sulphate Chondroitin sulphate

• 1000mg 800mg;
• 120-200 pounds 1500mg 1200mg;
• >200 pounds 2000mg 1600mg.

If no effect within 12 weeks of treatment, discontinue treatment.

Pharmacology

Glucosamine, an amino sugar, is the building block for certain glyosaminoglycans. In vitro, it has been shown to stimulate proteoglycan synthesis by human chondrocytes. It also has some innate anti-inflammatory properties ,independent of prostaglandin synthesis. There are some studies ,mainly in the European literature, suggesting that 1500mg daily of glucosamine sulphate is equivalent to1200mg of ibuprofen in the control of osteoarthritis symptoms. Glucosamine is also involved in the formation of nails, tendons, skin, eyes, bones, ligaments and other connective tissues in the body . Osteoarthritis involves a progressive degeneration of cartilage glycoaminoglycans [GAGs], components of cartilage that enable joints to move smoothly. The theory behind taking glucosamine supplements ,which are critical to the synthesis of GAGs, is that by flooding the system with them the production of these GAGs will be stimulated. Theoretically, the end result would be cartilage regeneration and joint repair. Many studies have shown that glucosamine is absorbed rapidly from the intestines, and transported to the connective tissues. It helps in the restoration of damaged joint tissue in osteoarthritis, especially in conjunction with Chondroitin Sulfate or devil’s claw. Chondroitin sulphate is a glycosaminoglycan and is a main constituent of proteoglycans. Like glucosamine, it has been shown to stimulate proteoglycan synthesis by human chondrocytes. Chondroitin sulphate also has some innate anti-inflammatory properties, independent of prostaglandin synthesis. Both compounds are natural and may be beneficial in the treatment of osteoarthritis.

Active Ingredients:

Glucosamine is a combination of glucose and glutamine

Origin & Processing

Glucosamine is extracted from shellfish, and purified & standardized to form Glucosamine Sulfate. Glucosamine is also prepared synthetically.

Scientific References

Bassleer C, Malaise M, University of L B (1997): Chondroitin Sulfate: its in-vitro Effects on Human Articular Chondrocytes Cultivated in Clusters. 3rd, International Congress of the Osteoarthritis Research Society Osteoarthritis in Focus: 5, Suppl A,:69.

Bassleer C, Henrotin Y, Franchiment P. (1992): in-vitro Evaluation of Drugs Proposed as Chondroprotective Agents. Int J Tissue React, 14:231-241.

Bourgeois P I. Chales G, Dehais J, Delcambre B, Dreyfus P, Kuntz J, Rosenberg S (1997): Efficacy and Tolerability of Chondrotin Sulfate 1200mg/dfe Vs. Chondrotin Sulfate 3 x 400 mg/d Vs. Placebo. 3rd, International Congress of the Osteoarthritis Research Society Osteoarthritis in Focus: 5, Suppl A,:69.

Bucci L, Podr G et al (1997): Efficacy and Tolerability of 2 x 400 Mg Oral Chondroitin Sulfate as a Single dose in the Treatment of Knee Osteoarthritis. 3rd, International Congress of the Osteoarthritis Research Society Osteoarthritis in focus: 5, Suppl A:69.

Camus J P (1972): verification de action de l’acid Chondroitin suifurique cnez des malades arthrosiques. Laboratories Gremy-Longuet. Paris.

Crivelli E, Voy E D (1987): Etude de pnase IV sur action des soses orales del sulfate articulations. Der informaierte Artz Gazette Medicinale, 3.

Crolle G, D’Este E (1980): Glucosamine sulphate for the management of arthrosis. Current Medical Research and Opinion Vol.7, No.2.

D’Angnolo B (1986): Valutazione degli effetti coilaterali e della efficacia nel sintmo del dolore (in pazienti artosici) del galattosamino glucuronogllcano solfato. Clin. Eur. Fasc., XXV (March-April). 275-280.

Droranti A, Bignamini A A, Rorati A I, Italy (1980): Therapeutic Activity of Oral Glucosamine in Osteoarthrosis: a placebo-controlled double-blind investigation Clinical therapeutics, vol. 3, no. 4.

D’Ambrosio, Casa B, Bompani R, Scali G (1981): Glucosamine Sulphate: a Controlled Clinical Investigation in arthrosis. Pharmatheutica, 2 (8):504.

Fioravanti A., Franci A., Anselmi F., Fattorini L., Marcolongo R. (1991) Clinical Efficacy and tolerance of Galactosoaminoglucuronoglycan Sulfate in the Treatment of Osteoarthritis. Drugs Exptl. Clin. Res. XVII (1) 41-44.

Garzya G. (1986): Orale Chondroitin sulfatmedikation zur Benandung von Arthrosen: Therapiewoche, 33, 4238.

Hardingham T (1997): Chondroitin Sulphate and Joint Disease. 3rd, International Congress of the Osteoarthritis Research Society Osteoarthritis in Focus: 5, Wuppl A,:69.

Helli MP, Vignon E, annefeld M, Richard M (1996): The Effects of Glucosamine on the Human Osteoarthritic Chondrocytes. The 9th Eular Symposium, Madrid, 7-10.

Jenoure P. et al (1986): Lesions degeneratives du gerou. Der informierte Artz/Gazette Medicinale, 7.

Jimenez SA, Dodge G R, Thomas J (1996): the Effects of Glucosamine On Human Chondrocyte Gene Expression. The 9th Eular symposium, Madrid, 7-10 October, pp 8-10.

Karzel K. domenjoz R (1971): Effect of Hexosamine Derivatives and Uronic Acid Derivatives on Glycosaminoglycan Metabolism of fibroblast Cultures. Pharmacol, 5:337-345.

Kim JJ, Conrad H E (1974): Effect of D-glucosamine Concentration on the Kinetics of Mucopolysaccharides Biosynthesis in Cultured Chick Embryo Vertebral Cartilage. J Biol Chem, 249: 3091-3097.

Maier R, Wilhelmi G (1982): Neue experimentelle Ergebnisse uber korperdestruktion und Protektion. Der Kassernartz, 22. 16.

McCarty MF (1994): the Neglect of Glucosamine as a Treatment for Osteoarthritis – a Personal Perspective. Medical Hypotheses, 42:323-327.

Muller-fabender Hans, Gerhard L, Bach, Wolfgang Haase, Rovati L C (1994): Glucosamine sulfate Compared to Ibuprofen in Osteoarthritis of the Knee. Osteoarthritis and Cartilage 2, 61-69.

Nerucci F, Fioravanti A, Bisogno S, Spinelli G, Marcolongo R, (1997): evaluation of the Chondroitin Sulfate Effects on Chondrocytes’ cultures Placed in a Pressurization System. 3rd, International Congress of the Osteoarthritis Research society Osteoarthritis in Focus: 5, Suppl A, :69, May.

Noack W, Fischer M, Forster K K, Rovati, L C , Setnikar I (1994): Glucosamine Sulfate in Osteoarthritis of the Knee. Osteoarthritis Cartilage (United Kingdom), 2/1 (51-59).

Oliviero U, sorrentino GP, De Paola P, Tranfaglia E, D’alessandro A, Carifi S, Porfido FA, Cerio R, Grasso A M, Policicchio D, Di Grezia F, Sorrentino P, Lingetti M (1991): Effects of the Treatment with Matrix on Elderly People with Chronic Articular Degeneration Drugs Exptl-Clin. Res. XVII (1) 45-51.

Paroli E, Antonilli L and Biffoni M (1991): a Pharmacological Approach to Glycosaminoglycans. Drugs under Experimental and Clinical Research, XVII (1):9-20.

Rietro M, Manopulo R, Galati M, Boccanera L, Saponati G and Bocchi L (1996): Comparison of the Antiinflammatory Efficacy of Chondroitin Sulfate and Diclofenac Sodium in Patients with Knee Osteoarthxifis. J Rheumaro I, 23: 1385-91.

Pujalte J M, Llavore E P, and Ylescupidez F R, (1980): double-blind Clinical Evaluation of Oral Glucosamine Sulphate in the Basic Treatment of Osteoarthrosis Current Medical Research and Opinion Vol.7, No.2.

Raiss R (1985): Effect of D-glucosamine on Experimentally Injured Articular Cartilage. Comparative Morphometry of the Ultra Structure of Chondrocytes. Fortschritte Der Medizin. 103 (24) 658.

Reichelt A, Fbrsterc KK, Fischer M B, Rovatie L C, and Setnikar I (1994): Efficacy and Safety of Intramuscular Glucosamine Sulfate in Oseoarthritis of the Knee. Arzneim. Forsch./Drug Res. 44 (1), Nr. 1.

Roden, L (1956): Effect of Hexosamines on the Synthesis of Chondroitin sulphuric Acid in-vitro. Ark. Kemi., 10, 345.

Ronca G (1997): Anti-inflammatory Activity of chondroitin sulfate. 3rd, International Congress of the International Congress of the Osteoarthritis Research Society Osteoarthritis in Focus: 5, Suppl A, :69.

Rovetta G (1991): Galactosaminoglycuronoglycan Sulfate (Matrix) in Therapy of Tibiofibular Osteoarthritis of The Knee. Drugs Exptl. Clin. Res. XVII (1) 53-57.

Serni U (1993): Profile of Glucosamine as a Example of Slow Acting Drug in Osteoarthritis. In: Proceedings of the Xviii th Congress of Rheumatology. Rev Esp Reumatol, 20(suppl):222.

Setnikar I, Cerada R, Pacinic M A, et al. (1991 b): Antireactive Properties of Glucosamine sulfate. Arzneimittel-forshung, 41 (1), Nr. 2, 157-161.

Tapadinhas M J (1982): Oral glucosamine sulphate in the management of arthrosis: report on a multi-centre open investigation in Portugal. Pharmatherapeutica, 3, 157.

Uebelhart D, Zhang J, Thonar E, Williams J (1997): Acute Degradation of Articular Cartilage in the Rabbit: Protective Effect of Chondroitin 4 & 6 sulfate. 3rd, International Congress of the Osteoarthritis Research Society Osteoarthritis Focus: 5, Suppl A, :69.

Vidal Y., Plana R R, Bizzarri D, Rovatie A I, (1978): Articular Cartilage Pharmacology, I. In-vitro Studies on Glucosamine and Nonsteroidal Anti-inflammatory Drugs. Pharmacol. Res. Comm., 10, 557.

Vajaradul Y (1981): Double-Blind Clincal Evaluation of Intra-Articular Glucosamine in Outpatients with Gonarthrosis. Clinical Therapeutics/vol. 3, No. 5.

Vaz A L (1982): Double-Blind Clinical Evaluation of the Relative Efficacy of Ibuprofen and Glucosamine Sulphate in the Management of Osteoarthrosis of the Knee in Out-patients. Current Medical Research and Opinion: Vol. 8, 145.

Weyers W, Iseli D (1987): Pharmakologische Untersuchungen zur antiphalogistisch Wirksamkeit Von Chondroitinsulfat. II Mittelung. Therapiewoche Schweiz, 3, 864.

EVIDENCE OF BIOAVAILABILITY.

Setnikar I, Giachetti C, Zanolo G. (1986): Pharmacokinetics of Glucosamine in the Dog and in Man. Drug Research, 36 (1):729-735.

Setnikar I, Giachetti C and Zanolo G. (1984): Absorption, Distribution and Excretion of Radioactivity after a Single Intravenous or Oral Parmatherapeutica, 3, (8)538.

Setnikar I, R. Palumbo, S. Canali, and G. Zanolo, (1993): Pharmacokinetics of Glucosamine in Man. Arzneim-Forsch / Drug Res. 43(II), Nr 10.

Conte A (1995), Volpi N, Palmiera L, et Al. Biochemical and Pharmacokinetic Aspects of Oral Treatment with Chondroitin Sulfate. Arzneimittel-forshung, 45: 918-925.

Palmieri L. Conte A. Giovannini L. Lualdi P. Ronca G. (1990): Metabolic Fate of Exogenous Chondroitin Sulfate in the Experimental Animal. Arzneimittel-forschung. 40(3):319-23.

CURRENT CLINICAL TRIAL ON GLUCOSAMINE AND CHONDROITIN.

HUMAN CLINICAL TRIAL #1.

Principal investigator: Amal K. Das, Jr., M.D.(an orthopedic surgeon).

Institiution: Henderson Orthopedic Research Associates, North Carolina. Study design: Almost 100 patients with chronic pain and osteoarthritis (confirmed by X-Ray) in a double-blinded, placebo-controlled, six-month clinical trial using Cosamin DS (combination of 1,500 milligrams glucosamine and 1,200 milligrams of chondroitin daily).

Results: Knee osteoarthritis symptoms were measured by summary disease scores and patient assessment of treatment effect, recorded at clinic visits and in a dairy. The summary disease score incorporated pain, stiffness and function using validated questionnaires. Adverse events: Recorded, if any, in a daily dairy specifying severity and no adverse reactions were note. More details to follow up0on the publication of this study.

HUMAN CLINICAL TRIAL #2.

Prinicpal investigators: Dr. Alan Philippi, LCDR, MC, USNR and Dr. Christopher Leffler, MD.

Institution: Medical Department Naval Special Warfare (SEAL). Group Two, Naval Amphibious Base, Little Creek. Study design: 16-week, randomized, double-blinded,placebo-controlled crossover design in 34 Navy SEALs, and divers by the Portsmouth Naval Medical Center in Virginia.

Results: Significant relief of knee pain but no improvement in function after eight weeks on the supplements. More details to follow upon the publication of this study.

HUMAN CLINICAL TRIAL #3.

Principal investigators: Dr. Joseph B. Houpt (Toronto, Canada).

Study design: Double-blinded, placebo-controlled using glucosamine in patients with oseoarthritis.

Results: Still pending.

HUMAN CLINICAL TRIAL #4.

Principal investigators: Jason Theodosakis, M.D.,James Weaver, D.D.S.

Study design: Double-blinded, placebo-controlled using glucosamine and chondroitin for prevention and treatment of osteoarthritis in the TMJ.

Results: Study is still in design and approval phase.

Several new university-based, large animal studies, along with basic science research continues to point to the disease-modifying benefits of the two supplements on joint cartilage. For example, Dr. Louis Lippiello, Ph.D., the Director of Basic Science at the Harrington Arthritis Research Center in Phoenix, has found that glucosamine and chondroitin work synergistically in promoting cartilage cell activity

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