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Role of Glucosamine in Osteoarthritis
Dr.Muhammad Lipu SarwerMedical Services Officer Medical DepartmentBeximco Pharma
Osteoarthritis
Osteoarthritis is an idiopathic diseaseCharacterized by degeneration of articular cartilageLeads to fibrillation, fissures, gross ulceration and finally disappearance of the full thickness of articular cartilage
Treatment Algorithm
Glucosamine
A building block for articular cartilage’s extracellular matrix
Synthesized by chondrocytes
90% absorption by oral administration
26% available for processing by the body’s tissue
Glucosamine
1. Glucosamine sulfate (most common form)2. Glucosamine hydrochrolide3. Glucosamine hydroiodide
• Sulfur is an essential nutrient for the stabilization of the connective tissue matrix.
• Glucosamie sulfate stimulates the uptake of sulfate ions -> indicater of GAG synthesis by chondrocytes.
• Glucosamine also hinders hyaluronidase (tissue damaging enzyme)
• Glucosamine sulfate improves the lubricant properties of synovial fluid.
Source
Present in meat, fish, poultry.Synthesized in the body. Manufactured from chitin, a substance found in shrimp, crab, and lobster shells. marine exoskeletons. Synthetic glucosamine is also available Chemically synthesized.
Safety
The clinical studies have consistently reported that glucosamine appears safe.
No allergic reactions have been reported although glucosamine is derived from shellfish
Allergy to shellfish may wish to avoid glucosamine.
May not have acute oral toxicity in animal
Glucosamine may increase on insulin resistance
Diacerein
Diacerein is distinct from all other painkillers & joints treatments due to its ability to reduce joint inflammation and pain, without having negative side effects on the stomach, blood pressure or heart.
Diacerein inhibits the production of ‘Interleukin – 1 beta’, the protein in the human body, which causes osteoarthritis and joint inflammation
Pharmacokinetics
Diacerein has efficacy on functional manifestations of osteoarthritis and on structural component.
The absorption in systemic circulation is delayed with meal but is associated with 25% increase in amount absorbed.
Though dose modification is required in mild to severe renal insufficiency, no reduction in initial dose is proposed in liver cirrhosis.
Diacerein – Long Carry Over Effect
In a randomized, multicenter, double-blind, placebo-controlled trial patients were given diacerein or placebo for 3 months after a 1-week nonsteroidal anti-inflammatory drug washout period, followed by an off-treatment period of 3 months. Result revealed that Diacerein can carry-over the improvement throughout the off-treament period.
Diacerein: More efficient Pain relief
The onset of action of diacerein is delayed compared with that of the NSAIDs, but the extent of pain reduction is better on long term use
The primary efficacy parameter (pain on WOMAC Index A) decreased to a similar extent in both groups until week 16 (end of treatment). At week 20, the improvement persisted for Diacerein (79.3%), while it decreased from 84.9 to 57.7% for Piroxicam. At week 24 (eight weeks post-treatment), the per cent improvement remained stable for Diacerein (80.6%), while it fell to 35.4% for Piroxicam (p<0.0001).42 VAS = visual analogue scale.
Features
Jointec Max is a symptomatic slow-acting drug
(SYSADO). Unlike the symptomatic rapid-acting drugs
(SYRADOAs) this combination have symptom-
modifying effects i.e. reduce the patient’s symptoms,
particularly pain and impaired physical function, with
positive effects, or at least no negative effects.
Benefits over NSAIDs
NSAIDsNSAIDs Jointec MaxJointec Max
Rapid onset of activityImmediate symptoms reappearanceCause serious GI, renal and vascular adverse eventsNo underlying structural damage improvementTreat symptomsHostile to cartilageLimited long term use
Slow onset of efficacy Long carry-over effectNo GI, renal and vascular adverse eventsImproves underlying structural damageModifies symptomsRepairs cartilageSuitable for long term use
Dosage and Administration
The usual dose of Joiintec Max is 1 tablet twice daily (12 hourly) taken with food for 30 to 90 days.
In case of patients with severe renal failure to 25 mg per day.
Adverse Reactions
Glucosamine: nausea, heartburn, diarrhea, and constipation. Uncommon side effects are drowsiness, skin reactions, and headache. These are rare.
Diacerein: Diarrhoea, epigastric pain, nausea, vomiting, intense yellow coloring of urine.
Contraindications
Jointec Max is contra indicated in pregnancy, lactation and in case of hypersensitivity.Pregnant women and nursing mothers should not take glucosamine due to a lack of scientific data regarding its effects on unborn babies and infants.Diacerein is contraindicated in pregnancy, lactation and hypersensitivity to anthraquinone derivatives
Interactions with Drugs
May increase risk of side effects Diuretics :
May increase risk of bleeding when taken with drugs that increase the risk of bleeding
Aspirin, anticoagulants (blood thinners): warfarin, (coumadin) or heparin, anti-platelet: clopidogrel, (plavix), non-steroidal anti-inflammatory: ibuprofen (Motrin, Advil) or naproxen (Naprosyn, Aleve)