Please Scroll Down to See Forums Below 
rykertest
New member
My question is at the bottom regarding the highlighted area. Thanks!
ADEQUAN
--------------------------------------------------------------------------------
FAST ACCESS TO THE JOINTS: Beneficial levels of Adequan are already at work in all major joints within two hours after intramuscular injection, with even greater uptake (up to 73% higher) in joint tissues that are inflamed or diseased. LONG-TERM EFFECTS: Adequan relieves the pain and disability of joint damage, and the relief has been shown to last up to 6 months or longer. BREAKS THE DESTRUCTIVE CYCLE: Adequan binds to damaged cartilage and boosts cartilage metabolism, facilitating repair processes. At the same time, it blocks the action of destructive enzymes that promote joint inflammation, break down the synovial fluid, and attack the cartilage. RENEWS THE JOINT FLUID: Adequan stimulates the synovial membrane to manufacture new synovial fluid to replace the thin, degraded fluid of joint disease. By doing so, Adequan helps lubricate, nourish, and clean the cartilage.
First, Adequan has important antiinflammatory effects, so it is able to provide relief from the symptoms of joint damage: heat, swelling, pain and lameness. And Adequan can be found in synovial fluid at full therapeutic levels within only two hours of an intramuscular injection. Also, Adequan is a product with potent ability to block the action of the destructive enzymes that threaten to perpetuate the joint inflammation, attack the cartilage and break down synovial fluid.
Second, Adequan also stimulates the synovial membrane to manufacture new, viscous synovial fluid to replace the thin fluid that was produced when the joint became injured. By improving this fluid, Adequan helps the joint regain its ability to lubricate and guard itself against further inflammation, and helps reestablish nutrition to the cartilage.
And, Adequan attaches itself to damaged cartilage where it has a positive effect on cartilage metabolism. This should favor the cartilage repair process.
Adequan is the only joint treatment proven to reduce the inflammation and pain of degenerative joint disease, but also to help stop the degenerative process while stimulating the production of new joint fluid and new cartilage components. You are no longer just treating symptoms: you're doing something to help stop the degenerative process.
DOSAGE AND ADMINISTRATION: The recommended dose of Adequan® in horses is 250 mg (1 vial) once a week for five weeks, intra-articularly. The joint area must be shaved, cleansed and sterilized as in a surgical procedure prior to injection. Do not mix Adequan® with other drugs or solvents.
__________________
Adequan® i.m. (POLYSULFATED GLYCOSAMINOGLYCAN) Attacks Degenerative Joint Disease In Four Ways:
1)As damaging enzymes form,
Adequan blocks them.
2)When inflammation causes pain,
Adequan relieves pain.
3)If joint lubrication diminishes,
Adequan improves lubrication.
4)Before cartilage damage continues,
Adequan inhibits degeneration
ADEQUAN® is recommended for intramuscular injection for the control of signs associated with non-infectious degenerative and/or traumatic arthritis of canine synovial joints.
Pharmacology
The active ingredient in ADEQUAN® is polysulfated glycosaminoglycan (PSGAG). Polysulfated glycosaminoglycan is a semi-synthetic glycosaminoglycan prepared by extracting glycosaminoglycans (GAGs) from bovine tracheal cartilage. GAGs are polysaccharides composed of repeating disaccharide units. The GAG present in PSGAG is principally chondroitin sulfate containing 3 to 4 sulfate esters per disaccharide unit. The molecular weight for PSGAG used in the manufacture of ADEQUAN® is 3,000 to 15,000 Daltons.
The specific mechanism of action of ADEQUAN® in joints is not known. PSGAG is characterized as a "disease modifying osteoarthritis drug". Experiments conducted in vitro have shown PSGAG to inhibit certain catabolic enzymes which have increased activity in inflamed joints, and to enhance the activity of some anabolic enzymes. For example, PSGAG has been shown to significantly inhibit serine proteinases. Serine proteinases have been demonstrated to play a role in the Interleukin-1 mediated degradation of cartilage proteoglycans and collagen. PSGAG is reported to be an inhibitor of Prostaglandin E2 (PGE2) synthesis. PGE2 has been shown to increase the loss of proteoglycan from cartilage. PSGAG has been reported to inhibit some catabolic enzymes such as elastase, stromelysin, metalloproteases, cathepsin B1, and hyaluronidases, which degrade collagen, proteoglycans, and Hyaluronic acid in degenerative joint disease. Anabolic effects studied include ability to stimulate the synthesis of protein, collagen, proteoglycans, and Hyaluronic acid in various cells and tissues in vitro.
__________________
Basskiller in no way promotes or condones steroid use without a doctor's consent. All information posted is done for entertainment and or education purposes only. It is not meant to be misconstrued as Medical advice
--------------------------------------------------------------------------------
Cultured human and rabbit chondrocytes have shown increased synthesis of proteoglycan and Hyaluronic acid in the presence of PSGAG. PSGAGs have shown a specific potentiating effect on Hyaluronic acid synthesis by synovial membrane cells in vitro.
Absorption, distribution, metabolism, and excretion of PSGAG following intramuscular injection have been studied in several species, including rats, rabbits, humans, horses and dogs.
Studies in rabbits showed maximum blood concentrations of PSGAG following IM injection were reached between 20 to 40 minutes following injection, and that the drug was distributed to all tissues studied, including Articular cartilage, synovial fluid, adrenals, thyroid, peritoneal fluid, lungs, eyes, spinal cord, kidneys, brain, liver, spleen, bone marrow, skin, and heart.
Following intramuscular injection of PSGAG in humans, the drug was found to be bound to serum proteins. PSGAG binds to both albumin and chi- and beta-globulins and the extent of the binding is suggested to be 30 to 40%. Therefore, the drug may be present in both bound and free form in the bloodstream. Because of its relatively low molecular weight, the synovial membrane is not a significant barrier to distribution of PSGAG from the bloodstream to the synovial fluid. Distribution from the synovial fluid to the cartilage takes place by diffusion. In the Articular cartilage the drug is deposited into the cartilage matrix.
Serum and synovial fluid distribution curves of PSGAG have been studied in dogs and appear similar to those found in humans and rabbits.
In rabbits, metabolism of PSGAG is reported to take place in the liver, spleen, and bone marrow. Metabolism may also occur in the kidneys. PSGAG administered intramuscularly and not protein bound or bound to other tissues is excreted primarily via the kidneys, with a small proportion excreted in the feces.
Dosage and Administration
The recommended dose of ADEQUAN® Canine is 2 mg/lb body weight (.02 mL/lb, or 1 mL per 50 lb), by intramuscular injection only, twice weekly for up to 4 weeks (maximum of 8 injections). Do not exceed the recommended dose or therapeutic regimen. Do not mix ADEQUAN® Canine with other drugs or solvents.
Contraindications
Do not use in dogs showing hypersensitivity to PSGAG. PSGAG is a synthetic heparinoid; do not use in dogs with known or suspected bleeding disorders.
Precautions
Store at room temperature 18°-25°C (64°-77°F).
Use with caution in dogs with renal or hepatic impairment.
Caution
Federal law restricts this drug to use by or on the order of a licensed veterinarian.
Warning
Keep this and all medications out of reach of children.
Side Effects
In the clinical efficacy trial, 24 dogs were treated with ADEQUAN® Canine twice weekly for 4 weeks. Possible adverse reactions were reported after 2.1% of the injections. These included transient pain at the injection site (1 incident), transient diarrhea (1 incident each in 2 dogs), and abnormal bleeding (1 incident). These effects were mild and self-limiting and did not require interruption of therapy. To report suspected adverse reactions or for a copy of the Material Safety Data Sheet for this product, contact Luitpold Pharmaceuticals, Inc. at 1-800-458-0163.
Toxicology
In a subacute toxicity study, 32 adult beagle dogs (4 males and 4 females per treatment group) received either 0.9% saline solution or PSGAG at a dose of 5 mg, 15 mg, or 50 mg per kg of body weight (approximately 2.3, 6.8, or 22.7 mg/lb), via intramuscular injection twice weekly for 13 weeks. PSGAG doses represent approximately 1X, 3X, and 10X the recommended dosage of 2 mg/lb, and more than 3 times the recommended 4-week duration of treatment. Necropsies were performed 24 hours after the final treatment. During week 12, one dog in the 50 mg/kg dosage group developed a large hematoma at the injection site which necessitated euthanasia. No other mortalities occurred during the treatment period. Statistically significant changes in the 50 mg/kg group included increased prothrombin time, reduced platelet count, an increase in ALT and cholesterol, and increased liver and kidney weights. Increased cholesterol and kidney weights were also noted in the 15 mg/kg group. Microscopic lesions were noted in the liver (Kupffer cells containing eosinophilic foamy cytoplasm), kidneys (swollen, foamy cells in the proximal convoluted tubules), and lymph nodes (macrophages with eosinophilic foamy cytoplasm) in the 15 mg/kg and 50 mg/kg groups. Intramuscular inflammation, hemorrhage, and degeneration were seen in all 3 PSGAG treated groups; the incidence and severity appeared dose related. Trial Data
Efficacy of ADEQUAN® Canine was demonstrated in two studies. A laboratory study using radio labeled PSGAG established distribution of PSGAG into canine serum and synovial fluid following a single intramuscular injection of 2 mg/lb. A clinical field trial was conducted in dogs diagnosed with radio graphically-confirmed traumatic and/or degenerative joint disease of 1 or 2 joints. Joints evaluated included hips, stifles, shoulders, hocks and elbows. Fifty-one dogs were randomly assigned to receive either ADEQUAN® Canine at 2 mg/lb of body weight or 0.9% saline. Both treatments were administered by intramuscular injection twice weekly for 4 weeks (8 injections total). Investigators administering treatment and evaluating the dogs were unaware of the treatment assignment. A total of 71 limbs in 51 dogs were evaluated. Of these, 35 limbs in 24 dogs were in the ADEQUAN® Canine treated group. Each lame limb was scored for lameness at a walk, lameness at a trot, pain, range of motion, and functional disability. The scores for the individual parameters were combined to determine a total orthopedic score. At the end of the treatment period, dogs treated with ADEQUAN® Canine showed a statistically significant improvement in range of motion and total orthopedic score over placebo treated control dogs.
Studies to establish the safety of ADEQUAN® Canine in breeding, pregnant, or lactating dogs have not been conducted.
Presentation
ADEQUAN® Solution 100 mg/mL in a 5 mL preserved multiple dose vial.
Studies
http://www.fda.gov/cvm/efoi/section2/141038071597
What would be a dosage for say a human that wants to get some knee relief? Also, how would the be compared with the side effects noted above? I was a little concerned about some of those sides, but I don't know if those doses are super high and would not be an issue for the doses I would be taking for knee repair. Also, is AFLUTOP a vet compound also? Thanks!
ADEQUAN
--------------------------------------------------------------------------------
FAST ACCESS TO THE JOINTS: Beneficial levels of Adequan are already at work in all major joints within two hours after intramuscular injection, with even greater uptake (up to 73% higher) in joint tissues that are inflamed or diseased. LONG-TERM EFFECTS: Adequan relieves the pain and disability of joint damage, and the relief has been shown to last up to 6 months or longer. BREAKS THE DESTRUCTIVE CYCLE: Adequan binds to damaged cartilage and boosts cartilage metabolism, facilitating repair processes. At the same time, it blocks the action of destructive enzymes that promote joint inflammation, break down the synovial fluid, and attack the cartilage. RENEWS THE JOINT FLUID: Adequan stimulates the synovial membrane to manufacture new synovial fluid to replace the thin, degraded fluid of joint disease. By doing so, Adequan helps lubricate, nourish, and clean the cartilage.
First, Adequan has important antiinflammatory effects, so it is able to provide relief from the symptoms of joint damage: heat, swelling, pain and lameness. And Adequan can be found in synovial fluid at full therapeutic levels within only two hours of an intramuscular injection. Also, Adequan is a product with potent ability to block the action of the destructive enzymes that threaten to perpetuate the joint inflammation, attack the cartilage and break down synovial fluid.
Second, Adequan also stimulates the synovial membrane to manufacture new, viscous synovial fluid to replace the thin fluid that was produced when the joint became injured. By improving this fluid, Adequan helps the joint regain its ability to lubricate and guard itself against further inflammation, and helps reestablish nutrition to the cartilage.
And, Adequan attaches itself to damaged cartilage where it has a positive effect on cartilage metabolism. This should favor the cartilage repair process.
Adequan is the only joint treatment proven to reduce the inflammation and pain of degenerative joint disease, but also to help stop the degenerative process while stimulating the production of new joint fluid and new cartilage components. You are no longer just treating symptoms: you're doing something to help stop the degenerative process.
DOSAGE AND ADMINISTRATION: The recommended dose of Adequan® in horses is 250 mg (1 vial) once a week for five weeks, intra-articularly. The joint area must be shaved, cleansed and sterilized as in a surgical procedure prior to injection. Do not mix Adequan® with other drugs or solvents.
__________________
Adequan® i.m. (POLYSULFATED GLYCOSAMINOGLYCAN) Attacks Degenerative Joint Disease In Four Ways:
1)As damaging enzymes form,
Adequan blocks them.
2)When inflammation causes pain,
Adequan relieves pain.
3)If joint lubrication diminishes,
Adequan improves lubrication.
4)Before cartilage damage continues,
Adequan inhibits degeneration
ADEQUAN® is recommended for intramuscular injection for the control of signs associated with non-infectious degenerative and/or traumatic arthritis of canine synovial joints.
Pharmacology
The active ingredient in ADEQUAN® is polysulfated glycosaminoglycan (PSGAG). Polysulfated glycosaminoglycan is a semi-synthetic glycosaminoglycan prepared by extracting glycosaminoglycans (GAGs) from bovine tracheal cartilage. GAGs are polysaccharides composed of repeating disaccharide units. The GAG present in PSGAG is principally chondroitin sulfate containing 3 to 4 sulfate esters per disaccharide unit. The molecular weight for PSGAG used in the manufacture of ADEQUAN® is 3,000 to 15,000 Daltons.
The specific mechanism of action of ADEQUAN® in joints is not known. PSGAG is characterized as a "disease modifying osteoarthritis drug". Experiments conducted in vitro have shown PSGAG to inhibit certain catabolic enzymes which have increased activity in inflamed joints, and to enhance the activity of some anabolic enzymes. For example, PSGAG has been shown to significantly inhibit serine proteinases. Serine proteinases have been demonstrated to play a role in the Interleukin-1 mediated degradation of cartilage proteoglycans and collagen. PSGAG is reported to be an inhibitor of Prostaglandin E2 (PGE2) synthesis. PGE2 has been shown to increase the loss of proteoglycan from cartilage. PSGAG has been reported to inhibit some catabolic enzymes such as elastase, stromelysin, metalloproteases, cathepsin B1, and hyaluronidases, which degrade collagen, proteoglycans, and Hyaluronic acid in degenerative joint disease. Anabolic effects studied include ability to stimulate the synthesis of protein, collagen, proteoglycans, and Hyaluronic acid in various cells and tissues in vitro.
__________________
Basskiller in no way promotes or condones steroid use without a doctor's consent. All information posted is done for entertainment and or education purposes only. It is not meant to be misconstrued as Medical advice
--------------------------------------------------------------------------------
Cultured human and rabbit chondrocytes have shown increased synthesis of proteoglycan and Hyaluronic acid in the presence of PSGAG. PSGAGs have shown a specific potentiating effect on Hyaluronic acid synthesis by synovial membrane cells in vitro.
Absorption, distribution, metabolism, and excretion of PSGAG following intramuscular injection have been studied in several species, including rats, rabbits, humans, horses and dogs.
Studies in rabbits showed maximum blood concentrations of PSGAG following IM injection were reached between 20 to 40 minutes following injection, and that the drug was distributed to all tissues studied, including Articular cartilage, synovial fluid, adrenals, thyroid, peritoneal fluid, lungs, eyes, spinal cord, kidneys, brain, liver, spleen, bone marrow, skin, and heart.
Following intramuscular injection of PSGAG in humans, the drug was found to be bound to serum proteins. PSGAG binds to both albumin and chi- and beta-globulins and the extent of the binding is suggested to be 30 to 40%. Therefore, the drug may be present in both bound and free form in the bloodstream. Because of its relatively low molecular weight, the synovial membrane is not a significant barrier to distribution of PSGAG from the bloodstream to the synovial fluid. Distribution from the synovial fluid to the cartilage takes place by diffusion. In the Articular cartilage the drug is deposited into the cartilage matrix.
Serum and synovial fluid distribution curves of PSGAG have been studied in dogs and appear similar to those found in humans and rabbits.
In rabbits, metabolism of PSGAG is reported to take place in the liver, spleen, and bone marrow. Metabolism may also occur in the kidneys. PSGAG administered intramuscularly and not protein bound or bound to other tissues is excreted primarily via the kidneys, with a small proportion excreted in the feces.
Dosage and Administration
The recommended dose of ADEQUAN® Canine is 2 mg/lb body weight (.02 mL/lb, or 1 mL per 50 lb), by intramuscular injection only, twice weekly for up to 4 weeks (maximum of 8 injections). Do not exceed the recommended dose or therapeutic regimen. Do not mix ADEQUAN® Canine with other drugs or solvents.
Contraindications
Do not use in dogs showing hypersensitivity to PSGAG. PSGAG is a synthetic heparinoid; do not use in dogs with known or suspected bleeding disorders.
Precautions
Store at room temperature 18°-25°C (64°-77°F).
Use with caution in dogs with renal or hepatic impairment.
Caution
Federal law restricts this drug to use by or on the order of a licensed veterinarian.
Warning
Keep this and all medications out of reach of children.
Side Effects
In the clinical efficacy trial, 24 dogs were treated with ADEQUAN® Canine twice weekly for 4 weeks. Possible adverse reactions were reported after 2.1% of the injections. These included transient pain at the injection site (1 incident), transient diarrhea (1 incident each in 2 dogs), and abnormal bleeding (1 incident). These effects were mild and self-limiting and did not require interruption of therapy. To report suspected adverse reactions or for a copy of the Material Safety Data Sheet for this product, contact Luitpold Pharmaceuticals, Inc. at 1-800-458-0163.
Toxicology
In a subacute toxicity study, 32 adult beagle dogs (4 males and 4 females per treatment group) received either 0.9% saline solution or PSGAG at a dose of 5 mg, 15 mg, or 50 mg per kg of body weight (approximately 2.3, 6.8, or 22.7 mg/lb), via intramuscular injection twice weekly for 13 weeks. PSGAG doses represent approximately 1X, 3X, and 10X the recommended dosage of 2 mg/lb, and more than 3 times the recommended 4-week duration of treatment. Necropsies were performed 24 hours after the final treatment. During week 12, one dog in the 50 mg/kg dosage group developed a large hematoma at the injection site which necessitated euthanasia. No other mortalities occurred during the treatment period. Statistically significant changes in the 50 mg/kg group included increased prothrombin time, reduced platelet count, an increase in ALT and cholesterol, and increased liver and kidney weights. Increased cholesterol and kidney weights were also noted in the 15 mg/kg group. Microscopic lesions were noted in the liver (Kupffer cells containing eosinophilic foamy cytoplasm), kidneys (swollen, foamy cells in the proximal convoluted tubules), and lymph nodes (macrophages with eosinophilic foamy cytoplasm) in the 15 mg/kg and 50 mg/kg groups. Intramuscular inflammation, hemorrhage, and degeneration were seen in all 3 PSGAG treated groups; the incidence and severity appeared dose related. Trial Data
Efficacy of ADEQUAN® Canine was demonstrated in two studies. A laboratory study using radio labeled PSGAG established distribution of PSGAG into canine serum and synovial fluid following a single intramuscular injection of 2 mg/lb. A clinical field trial was conducted in dogs diagnosed with radio graphically-confirmed traumatic and/or degenerative joint disease of 1 or 2 joints. Joints evaluated included hips, stifles, shoulders, hocks and elbows. Fifty-one dogs were randomly assigned to receive either ADEQUAN® Canine at 2 mg/lb of body weight or 0.9% saline. Both treatments were administered by intramuscular injection twice weekly for 4 weeks (8 injections total). Investigators administering treatment and evaluating the dogs were unaware of the treatment assignment. A total of 71 limbs in 51 dogs were evaluated. Of these, 35 limbs in 24 dogs were in the ADEQUAN® Canine treated group. Each lame limb was scored for lameness at a walk, lameness at a trot, pain, range of motion, and functional disability. The scores for the individual parameters were combined to determine a total orthopedic score. At the end of the treatment period, dogs treated with ADEQUAN® Canine showed a statistically significant improvement in range of motion and total orthopedic score over placebo treated control dogs.
Studies to establish the safety of ADEQUAN® Canine in breeding, pregnant, or lactating dogs have not been conducted.
Presentation
ADEQUAN® Solution 100 mg/mL in a 5 mL preserved multiple dose vial.
Studies
http://www.fda.gov/cvm/efoi/section2/141038071597
What would be a dosage for say a human that wants to get some knee relief? Also, how would the be compared with the side effects noted above? I was a little concerned about some of those sides, but I don't know if those doses are super high and would not be an issue for the doses I would be taking for knee repair. Also, is AFLUTOP a vet compound also? Thanks!
