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Ortholord Tablets

INTRODUCTION

Osteoarthritis (OA) is the most common chronic (long-lasting) joint condition. Osteoarthritis is the most common form of arthritis, affecting millions of people worldwide. It occurs when the protective cartilage that cushions the ends of your bones wears down over time. Osteoarthritis (OA) is caused by aging joints, injury, and obesity. A joint is where two bones come together. The ends of these bones are covered with a protective tissue called cartilage. With OA, this cartilage breaks down, causing the bones within the joint to rub together. Some people call it a degenerative joint disease or “wear and tear” arthritis. Osteoarthritis (OA) is the most common form of frequently in the hands, hips, and knees. These changes usually develop slowly and get worse over time. OA occurs most often in older people, although it can occur in adults of any age. OA is also called degenerative joint disease, degenerative arthritis, and wear-and-tear arthritis. A leading cause of disability, OA affects more than 30 million men and women in the United States. OA can cause pain, stiffness, and swelling. In some cases it also causes reduced function and disability; some people are no longer able to do daily tasks or work.

CAUSES OA is caused by joint damage. This damage can accumulate over time, which is why age is one of the main causes of the joint damage leading to osteoarthritis. Osteoarthritis occurs when the cartilage that cushions the ends of bones in your joints gradually deteriorates. Cartilage is a firm, slippery tissue that enables nearly frictionless joint motion. Eventually, if the cartilage wears down completely, bone will rub on bone. The older you are, the more wear and tear you’ve had on your joints. Other causes of joint damage include past injury, such as: 	Torn cartilage 	Dislocated joints 	Ligament injuries They also include joint malformation, obesity, and poor posture. Certain risk factors, such as family history and gender, increase your risk of osteoarthritis. But besides the breakdown of cartilage, osteoarthritis affects the entire joint. It causes changes in the bone and deterioration of the connective tissues that hold the joint together and attach muscle to bone. It also causes inflammation of the joint lining. SYMPTOMS 	stiffness 	inflammation 	tenderness (discomfort when pressing on the area with your fingers) Osteoarthritis symptoms often develop slowly and worsen over time. Signs and symptoms of osteoarthritis include: 	Pain: Affected joints might hurt during or after movement. 	Stiffness: Joint stiffness might be most noticeable upon awakening or after being inactive. 	Tenderness: Your joint might feel tender when you apply light pressure to or near it. 	Loss of flexibility: You might not be able to move your joint through its full range of motion. 	Grating sensation: You might feel a grating sensation when you use the joint, and you might hear popping or crackling. 	Bone spurs: These extra bits of bone, which feel like hard lumps, can form around the affected joint. 	Swelling: This might be caused by soft tissue inflammation around the joint.

OSTEOARTHRITIS OF THE HIP The hip joint shown on the left side of the image is normal, but the hip joint shown on the right side of the image shows deterioration of cartilage and the formation of bone spurs due to osteoarthritis.

STAGES OA is a progressive condition with five stages, from 0 to 4. The first stage (0) represents a normal joint. Stage 4 represents severe OA. Not everyone who has OA will progress all the way to stage 4. The condition often stabilizes long before reaching this stage.

STAGE 1 – MINOR This is the least severe stage of OA. Patients in stage 1 will develop minor wear-and-tear in their joints, but typically feel little to no pain in the affected area. If you have no history of OA, a doctor will most likely leave your symptoms untreated, but they may advise you take supplements or change up your exercise routine.

STAGE 2 – MILD This is when X-rays will start to show more noticeable bone spur growths (growths that often develop where bones meet each other in the joint). The affected area will start to feel stiff after long, sedentary periods, and will become uncomfortable. Your doctor might suggest a stricter workout routine or a fitted brace to wear.

STAGE 3 – MODERATE In stage 3, the cartilage in the affected area starts to erode and narrow the gap between bone and joint. The joint becomes inflamed and starts causing discomfort during normal daily activity. Some treatments include over the counter pain medications, prescription pain relievers, and in severe cases, hyaluronic injections.

STAGE 4 – SEVERE This is the most severe stage of OA, which means it is also the most painful. At this point, the cartilage is almost completely gone, leading to an inflammatory response from the joint. The bone spurs that developed in the earlier stages have now multiplied, often causing excruciating pain. There are various treatment options that generally include bone realignment surgery and knee/hip replacement.

RISK FACTORS Factors that can increase your risk of osteoarthritis include: 	Older age: The risk of osteoarthritis increases with age. 	Sex: Women are more likely to develop osteoarthritis, though it isn't clear why. 	Obesity: Carrying extra body weight contributes to osteoarthritis in several ways, and the more you weigh, the greater your risk. Increased weight adds stress to weight-bearing joints, such as your hips and knees. Also, fat tissue produces proteins that can cause harmful inflammation in and around your joints. 	Joint injuries: Injuries, such as those that occur when playing sports or from an accident, can increase the risk of osteoarthritis. Even injuries that occurred many years ago and seemingly healed can increase your risk of osteoarthritis. 	Repeated stress on the joint: If your job or a sport you play places repetitive stress on a joint, that joint might eventually develop osteoarthritis. 	Genetics: Some people inherit a tendency to develop osteoarthritis. 	Bone deformities: Some people are born with malformed joints or defective cartilage. 	Certain metabolic diseases: These include diabetes and a condition in which your body has too much iron (hemochromatosis). COMPLICATIONS Osteoarthritis is a degenerative disease that worsens over time, often resulting in chronic pain. Joint pain and stiffness can become severe enough to make daily tasks difficult. Depression and sleep disturbances can result from the pain and disability of osteoarthritis. DIAGNOSIS During the physical exam, your doctor will check your affected joint for tenderness, swelling, redness, and flexibility. Imaging tests To get pictures of the affected joint, your doctor might recommend:

	X-rays: Cartilage doesn't show up on X-ray images, but cartilage loss is revealed by a narrowing of the space between the bones in your joint. An X-ray can also show bone spurs around a joint. 	Magnetic resonance imaging (MRI): An MRI uses radio waves and a strong magnetic field to produce detailed images of bone and soft tissues, including cartilage. An MRI isn't commonly needed to diagnose osteoarthritis but can help provide more information in complex cases. LAB TESTS Analyzing your blood or joint fluid can help confirm the diagnosis. 	Blood tests: Although there's no blood test for osteoarthritis, certain tests can help rule out other causes of joint pain, such as rheumatoid arthritis. 	Joint fluid analysis: Your doctor might use a needle to draw fluid from an affected joint. The fluid is then tested for inflammation and to determine whether your pain is caused by gout or infection rather than osteoarthritis.

TREATEMENT

GLUCOSAMINE SULPHATE Glucosamine sulfate is a naturally occurring chemical found in the human body. It is in the fluid around joints. Glucosamine also exists in other places in nature. For example, glucosamine sulfate used in dietary supplements is often obtained from the shells of shellfish. Glucosamine sulfate used in dietary supplements does not always come from natural sources. It can also be made in a laboratory. Glucosamine is commonly used as a treatment for osteoarthritis, although its acceptance as a medical therapy varies. It is an amino sugar and precursor of glycosylated proteins and lipids. Since glucosamine is a precursor for glycosaminoglycans, and glycosaminoglycans are a major component of joint cartilage, supplemental glucosamine may help to rebuild cartilage and treat arthritis. STRUCTURE

WEIGHT: 456.42 CHEMICAL FORMULA: C12H28N2O14S SIDE EFFECTS Side effects of taking glucosamine are reported to be mild and infrequent, but they can include: 	Stomach upsets 	Constipation 	Diarrhea 	Headaches 	Rashes

PHARMACODYNAMICS Osteoarthritis is characterized by the progressive degeneration of cartilage glycosaminoglycans. The formation of glucosamine is the rate limiting step in glycosaminoglycans synthesis thus the addition is glucosamine, would in theory provide a building block towards the synthesis of glycosaminoglycans and thus slow down the progression of osteoarthritis. Thus far however, the results have not been conclusive HOW DOES IT WORK? Glucosamine sulfate is a chemical found in the human body. It is used by the body to produce a variety of other chemicals that are involved in building tendons, ligaments, cartilage, and the thick fluid that surrounds joints. Joints are cushioned by the fluid and cartilage that surround them. In some people with osteoarthritis, the cartilage breaks down and becomes thin. This results in more joint friction, pain, and stiffness. MECHANISM OF ACTION Glucosamine is a precursor of glycosylated proteins and lipids. Oral glucosamine is commonly used for the treatment of osteoarthritis. Since glucosamine is a precursor for glycosaminoglycans, and glycosaminoglycans are a major component of joint cartilage, supplemental glucosamine may help to rebuild cartilage and treat arthritis. Its use as a therapy for osteoarthritis appears safe, but there is conflicting evidence as to its effectiveness with more recent studies showing limited to no clinical benefit of use. Glucosamine is not FDA approved for use in humans. Since glucosamine is classified as a dietary supplement, safety and formulation are solely the responsibility of the manufacturer; evidence of safety and efficacy is not required as long as it is not advertised as a treatment for a medical condition. PHARMACOKINETICS ABSORPTION When taken orally, glucosamine sulfate is absorbed readily into the system and can be traced to cartilage as soon as four hours after consumption. ... Additionally, in some laboratory tests, the glucosamine supplement demonstrated a protective effect on the cartilage as well. HALF LIFE: Glucosamine elimination half-life was only tentatively estimated to average 15 h. METABOLISM A significant fraction of orally administered glucosamine undergoes first-pass metabolism in the liver. Blood levels achieved after oral glucosamine are only 20% those achieved with intravenous glucosamine ELIMINATION In humans, 90% of orally administered glucosamine is absorbed from the small intestine. After metabolism in liver, the metabolites of glucosamine are excreted mainly in urine along with the unchanged glucosamine, with a small amount eliminated in the faeces METHYLSULFONYLMETHANE (MSM) Methylsulfonylmethane (MSM) is an organosulfur compound. It is also known by several other names including methyl sulfone and dimethyl sulfone (DMSO2). USE MSM is commonly used for osteoarthritis, but may also benefit in alleviating GI upset, musculoskeletal pain, and allergies, boosting the immune system, and fighting microbial infections. MSM is widely used in the alternative medicine field and by people looking for a natural way to relieve joint pain, reduce inflammation and boost immunity. MECHANISM OF ACTION It also inhibits the breakdown of cartilage, a flexible tissue that protects the ends of your bones in joints. MSM improved symptoms of pain and physical function during the short intervention without major adverse events. The benefits and safety of MSM in managing OA. The data from the more rigorous MSM trials provide positive evidence in the treatment of mild to moderate OA of the knee. CHONDROITIN SULFATE SODIUM Chondroitin sulfate is a chemical that is normally found in cartilage around joints in the body. Chondroitin sulfate is usually manufactured from animal sources, such as shark and cow cartilage. Chondroitin sulfate is used for osteoarthritis and cataracts. Chondroitin sulfate is a glycosaminoglycan considered as a symptomatic slow-acting drug for osteoarthritis. It is suggested a pain relief and increased joint. USE Chondroitin is used in dietary supplements as an alternative medicine to treat osteoarthritis and also approved and regulated as a symptomatic slow-acting drug for this disease (SYSADOA). It is commonly sold together with glucosamine. Chondroitin, along with commonly used glucosamine, should not be used to treat people who have symptomatic osteoarthritis of the knee as evidence shows that these treatments fail to provide relief for that condition. MECHANISM OF ACTION The anti-inflammatory effect of chondroitin sulfate is thought to be caused by the inhibition of the synthesis of inflammatory intermediates such as the inhibition of nitric oxide synthase, COX-2, microsomal prostaglandin synthase 1 and prostaglandin E2. Chondroitin sulfate (CS) is recommended as a therapeutic intervention in the multimodal approach of osteoarthritis (OA) management. CS has been studied extensively to describe its pharmacology (pharmacokinetic, in vitro and in vivo effects) and its clinical efficacy.Clinical evidence is in favour of a slow-acting effect on symptoms in moderate knee OA COLLAGEN PEPTIDE Collagen Peptides is the hydrolyzed form of Collagen. After hydrolysis, the product loses its gelling ability and makes it soluble in cold water. Collagen Peptides is also known as 'Collagen hydrolysate'. Collagen peptides are a versatile source of protein and an important element of healthy nutrition. Their nutritional and physiological properties promote the health of bones and joints, and contribute to beautiful skin. The study clearly demonstrates are effective supplements for the improvement in overall physical problems associated with OA and thereby help to improve the quality of life. It is hypothesised that the supplementation of collagen peptide regulates chondrocyte differentiation and stimulates synthesis of proteoglycans, resulting in the initiation of repair processes in cartilage tissue. HYALURONIC ACID DESCRIPTION Hyaluronic acid (HA) is an anionic, nonsulfated glycosaminoglycan distributed widely throughout connective, epithelial, and neural tissues. It is unique among glycosaminoglycans in that it is nonsulfated, forms in the plasma membrane instead of the Golgi, and can be very large, with its molecular weight often reaching the millions. One of the chief components of the extracellular matrix, hyaluronic acid contributes significantly to cell proliferation and migration, and may also be involved in the progression of some malignant tumors. MECHANISM OF ACTION Hyaluronic acid works by acting as a cushion and lubricant in the joints and other tissues. In addition, it might affect the way the body responds to injury. Hyaluronic acid is a polysaccharide which is distributed widely in the extracellular matrix of connective tissue in man. It forms a viscoelastic solution in water which makes it suitable for aqueous and vitreous humor in ophthalmic surgery. It is suggested to provide mechanical protection for ocular tissues and cell layers due to its high viscosity. USES Hyaluronic acid is well known for its skin benefits, especially alleviating dry skin, reducing the appearance of fine lines and wrinkles and speeding up wound healing. It can also help relieve joint pain in people with osteoarthritis. Hyaluronic acid is a potential bright spot for helping lower the side effects. Its effectiveness is due to the many methods of actions it deploys, including lubrication, anti-inflammatory and chondroprotective effects. CURCUMINOID These compounds are natural phenols and produce a pronounced yellow color. . They have poor solubility in water at acidic and physiological pH, and also hydrolyze rapidly in alkaline solutions. Therefore, curcumin derivatives are synthesized to increase their solubility and hence bioavailability. MOA Curcumin blocks the formation of reactive-oxygen species, possesses anti-inflammatory properties as a result of inhibition of cyclooxygenases (COX) and other enzymes involved in inflammation; and disrupts cell signal transduction by various mechanisms including inhibition of protein kinase C. USES Use of curcumin as a folk remedy continues today. As part of the ancient Indian medical system, Ayurveda, a poultice of turmeric paste is used to treat common eye infections, and to dress wounds, treat bites, burns, acne and various skin diseases. Turmeric and especially its most active compound curcumin have many scientifically-proven health benefits, such as the potential to prevent heart disease, Alzheimer's and cancer. It's a potent anti-inflammatory and antioxidant and may also help improve symptoms of depression and arthritis. VITAMIN C A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant. MECHANISM OF ACTION In humans, an exogenous source of ascorbic acid is required for collagen formation and tissue repair by acting as a cofactor in the posttranslational formation of 4-hydroxyproline in -Xaa-Pro-Gly- sequences in collagens and other proteins. Ascorbic acid is reversibly oxidized to dehydroascorbic acid in the body. These two forms of the vitamin are believed to be important in oxidation-reduction reactions. The vitamin is involved in tyrosine metabolism, conversion of folic acid to folinic acid, carbohydrate metabolism, synthesis of lipids and proteins, iron metabolism, resistance to infections, and cellular respiration. Vitamin C also protects an important protein in your bones and joints. vitamin C deficit can negatively influence collagen production and inflammation control, as well as oxidative reactions, while its carefully construed administration is found to yield multiple potential pain-reducing benefits. Vitamin C reduces the oxidative stress and inflammatory response of muscles in the context of postoperative care. BOSWELLIA SERATA Boswellia serrata is a plant that produces Indian frankincense. It is also known as Indian olibanum, Salai guggul, and Sallaki in Sanskrit. USES Boswellia, also known as Indian frankincense, is an herbal extract taken from the Boswellia serrata tree. Resin made from Boswellia extract has been used for centuries in Asian and African folk medicine. It's believed to treat chronic inflammatory illnesses as well as a number of other health conditions. This study provides important information about the efficacy and safety of in the treatment of OA, which may be useful in promoting as a promising alternative therapeutic strategy that may be used as a nutritional supplement against OA. PIPERIN It is an alkaloid isolated from the plant Piper nigrum. It has a role as an NF-kappaB inhibitor, a plant metabolite, a food component, and a human blood serum metabolite. It is a member of benzodioxoles, an N-acylpiperidine, a piperidine alkaloid, and a tertiary carboxamide. It derives from an (E, E)-piperic acid. Aside from its use as a magnifier for other dietary supplements, piperine can also benefit the body on its own, and also it increases the bioavailability of nutritional supplements. MECHANISM OF ACTION Piperine has long been known as an anti-inflammatory agent. It also works as a pain reliever by blocking the expression of a gene that causes arthritis pain. It reduces the amount of pain the body feels, making things like arthritis and other injuries easier to withstand. Piperazine blocks the response of the worm muscle to acetylcholine, presumably by causing hyperpolarization of nerve endings, resulting in flaccid paralysis of the worm. USES Piperine is a major alkaloid found in black pepper (Piper nigrum), and the alkaloid is used as an herbal product for its purported anti-inflammatory, antioxidant, and antitumor properties. Curcumin, a demonstrates potential as a treatment agent for osteoarthritis, a disease with an underlying inflammatory cause. Its efficacy in reducing pain, physical function, and quality of life among osteoarthritic patients have been demonstrated in many clinical trials. The effects of curcumin on osteoarthritis can be attributed to its ability to prevent apoptosis of chondrocytes due to inflammation predominantly, and oxidative stress to a lesser extent.