Pharmacological properties
Artiflex
Pharmacodynamics. Artiflex is a drug that affects the metabolism in cartilage tissue. Glucosamine sulfate is a salt of the natural aminomonosaccharide glucosamine with a low molecular weight, carefully purified from macromolecular components. The drug fills the endogenous deficiency of glucosamine, stimulates the synthesis of proteoglycans of hyaluronic acid of synovial fluid. Increases the permeability of the joint capsule, restores enzymatic processes in the cells of the synovial membrane and articular cartilage. The anti-inflammatory effect of glucosamine sulfate is due to blocking the formation of superoxide radicals by macrophages and inhibition of lysosomal enzymes. The drug promotes the fixation of sulfur in the process of chondroitin sulfate synthesis, facilitates the absorption of calcium in bone tissue, inhibits the development of degenerative processes in the joints, restores their function, reducing joint pain. Sulfates are also involved in the synthesis of glycosaminoglycans and the metabolism of cartilage tissue. The sulfate esters of the side chains in the proteoglycans are of great importance for maintaining the elasticity and water-holding capacity of the cartilage matrix. The severity of clinical symptoms usually decreases 2 weeks after the start of treatment, with the effect remaining for 8 weeks after drug withdrawal.
Pharmacokinetics. Glucosamine sulfate is rapidly and completely absorbed in the small intestine (90%). It easily passes through biological barriers and penetrates into tissues, mainly articular cartilage. T ½ - 68 hours.
Artiflex Chondro
Pharmacodynamics. The main active ingredients of the drug are sodium salt of chondroitin sulfate A and C (average molecular weight - 11,000 Da). Chondroitin sulfate is a high-molecular mucopolysaccharide, which is the main component of proteoglycans, which together with collagen fibers form the cartilage matrix.
The drug inhibits the process of degeneration and stimulates the regeneration of cartilage tissue, has chondroprotective, anti-inflammatory, analgesic properties; replaces chondroitin sulfate in articular cartilage, catabolized by the pathological process; inhibits the activity of enzymes that cause degradation of articular cartilage: inhibits metalloproteinases, namely leukocyte elastase; reduces the activity of hyaluronidase; partially blocks the release of free oxygen radicals; helps block chemotaxis, antigenic determinants; stimulates the synthesis of proteoglycans by chondrocytes; affects phosphorus-calcium metabolism in cartilage tissue; allows you to restore the mechanical and elastic integrity of the cartilage matrix. Anti-inflammatory and analgesic effects are achieved by reducing the release of inflammatory mediators and pain factors into the synovial fluid by synoviocytes and macrophages of the synovial membrane, as well as by inhibiting the secretion of leukotriene B and prostaglandin E.
The drug helps restore the joint capsule and cartilaginous surfaces of the joints, reduces pain intensity, prevents compression of connective tissue, acts as a lubricant for the joint surfaces, normalizes the production of joint fluid, and improves joint mobility and quality of life.
Artiflex Chondro slows down bone resorption and reduces calcium loss, accelerating the process of bone tissue repair.
Pharmacokinetics. After i / m administration, chondroitin sulfate penetrates into the synovial fluid. C max in the synovial fluid is reached 4-5 hours after injection. It is excreted from the body within 24 hours. It is eliminated mainly by the kidneys.
Indication
Artiflex
Treatment of osteoarthritis and/or its symptoms, i.e. pain and functional limitation.
Artiflex Chondro
Degenerative-dystrophic diseases of the joints and spine (primary arthrosis, intervertebral osteochondrosis, osteoarthritis), osteoporosis, periodontal diseases, fractures (to accelerate the formation of bone callus), as well as for the purpose of treating the consequences of surgical interventions on the joints.
Application
Artiflex
Apply internally.
Adult patients and the elderly: the contents of 1 packet are equivalent to 1.5 g of glucosamine sulfate, dissolve in a glass of water and take once a day, preferably with a meal.
The course of treatment is 4-12 weeks or longer (if necessary). As prescribed by a doctor, the therapy can be repeated 2-3 times a year with an interval of 2 months, as well as in case of relapse of the disease.
Artiflex Chondro
The drug is administered to adults intramuscularly 1 ml every other day. In case of good tolerance, the dose is increased to 2 ml, starting from the 4th injection. The course of treatment is 25-35 injections. Repeated courses are after 6 months.
Contraindication
Hypersensitivity to any of the components of the drug.
Artiflex
Phenylketonuria. Pregnancy and breastfeeding.
Artiflex Chondro
Bleeding tendency, thrombophlebitis, renal failure.
Side effects
Artiflex
Gastrointestinal: stomach pain, flatulence, diarrhea, constipation, nausea, vomiting.
From the nervous system: headache, drowsiness, general weakness.
On the part of the immune system: allergic reactions in the form of various skin rashes and itching.
On the part of the organ of vision: visual impairment.
Skin: hair loss.
Artiflex Chondro
When using the drug in people with hypersensitivity to the drug, the following disorders are possible:
Skin and subcutaneous tissue disorders: rash, itching, erythema, urticaria, dermatitis, alopecia; redness and itching may occur at the injection site;
Gastrointestinal: nausea, vomiting, abdominal pain, flatulence, dyspeptic symptoms;
others: visual disturbances, keratopathy, dizziness, peripheral edema.
Special instructions
Use during pregnancy or breastfeeding. Do not use.
Children: The drug is not used.
The ability to influence the reaction speed when driving vehicles or working with other mechanisms. Does not affect.
Artiflex
As a result of the fact that glucosamine is derived from shellfish shells, patients with shellfish allergies should take Artiflex with caution.
The oral powder contains sorbitol. Patients with rare hereditary problems of fructose intolerance should not use this medicine.
Patients on a controlled sodium diet should take into account the presence of sodium in the oral dosage form (151 mg per 1500 mg daily dose).
At the beginning of treatment, it is advisable to monitor blood glucose levels in patients with diabetes.
In patients with severe hepatic or renal insufficiency, the drug should be used only under the supervision of a physician.
Artiflex is contraindicated for patients with phenylketonuria because it contains aspartame.
Artiflex Chondro
To achieve a stable clinical effect, at least 25 injections of the drug are required. The effect persists for many months after the end of treatment. Repeated courses of treatment are used to prevent exacerbations. It is recommended to increase the dose under the supervision of a physician for patients with excess body weight, gastric or duodenal ulcer, while taking diuretics, as well as at the beginning of treatment if a rapid clinical response is required.
In case of allergic reactions or hemorrhages, treatment must be discontinued.
Interactions
Artiflex
With simultaneous use, an increase in the effect of coumarin anticoagulants has been noted. In this regard, it is advisable to monitor coagulation parameters in patients.
Possible increase in gastrointestinal absorption of tetracycline. The drug is compatible with nonsteroidal anti-inflammatory drugs and corticosteroids.
Artiflex Chondro
When used simultaneously with glucocorticosteroids and nonsteroidal anti-inflammatory drugs, chondroitin sulfate can reduce the need for their use, as well as for painkillers. It has a synergistic effect when used simultaneously with glucosamine and other chondroprotectors. The effectiveness of treatment increases when the diet is enriched with vitamins A, C and salts of manganese, magnesium, copper, zinc and selenium.
When taken simultaneously with acetylsalicylic acid or other anticoagulants or antiplatelet agents, it is recommended to monitor blood clotting.
Overdose
No cases of overdose were noted.
Artiflex
In case of accidental overdose, gastric lavage and symptomatic treatment are performed.
Artiflex Chondro
It is assumed that if the daily dose is exceeded, the severity of side effects of the drug may increase. Treatment is symptomatic.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Current information
Artiflex is a complex drug for the treatment of musculoskeletal pathologies. For the most effective use, it is available in two forms - a cream for topical application and a soluble powder for oral administration.
Mechanism of action and therapeutic effects of glucosamine
The main active ingredient of Artiflex, powder for oral solution, is glucosamine hydrochloride.
Since glucosamine is a structural component of the cartilage matrix of joints, traditionally the treatment of joint pathology was associated with its additional intake from the outside. Further studies were conducted on the biochemical principles of glucosamine action. The mechanism of its anti-inflammatory effect is based on the inhibition of such pro-inflammatory mediators as NO, cyclooxygenase (COX)-2 and matrix metalloproteinases. In addition, this effect is associated with the reduction of nuclear factor κβ, which is activated by interleukin-1 (Gouze JN, 2006). Studies (Nakamura H., 2004) also demonstrated that glucosamine inhibits the production of catabolic enzymes and markers of inflammation (for example, prostaglandin E 2) by chondrocytes and synovial cells stimulated by interleukin-1.
In addition, glucosamine is a precursor of glycosaminoglycans (in particular hyaluronic acid and keratan sulfates) and proteoglycans, which are contained in articular cartilage, intervertebral discs and synovial fluid (Henrotin Y., 2012). This property is used, including in cosmetology - by increasing the synthesis of hyaluronic acid, glucosamine accelerates wound healing, moisturizes the skin and helps reduce the number of wrinkles (Bissett DL, 2006). In addition, it acts as a tyrosinase inhibitor, i.e. indirectly reduces melanin production, therefore it allows you to resist the development of hyperpigmentation.
Studies (Hua J., 2005) have shown that topical application of glucosamine significantly reduces the severity of adjuvant arthritis (an experimental model of arthritis of any joint in the body, which is similar in pathogenesis to rheumatoid arthritis).
According to a Cochrane review (Towheed T., 2009), glucosamine is the drug of choice in the treatment of osteoarthritis, as it helps to improve joint function, increase the volume of active and passive movements (da Camara CC, 1998), reduces pain and hyperesthesia, and also, probably, does not cause side effects. The FDA refers to glucosamine as a dietary supplement, but this agent is characterized by the ability to reduce pain, inhibit the development of damage and even restore cartilage in patients with osteoarthritis or other joint diseases (Kirkham SG, 2009). Real-time studies (Bruyère O., 2016) demonstrate that the systematic use of glucosamine in patients with osteoarthritis removes the need for additional painkillers. It promotes the restructuring of not only cartilage and synovial tissue, but also subchondral bone areas (Henrotin Y., 2012).
When choosing a therapeutic dose, it should be taken into account that to achieve an effect with systemic use (for example, in the form of tablets or powder for preparing a solution), the daily dose of glucosamine should be at least 1500 mg. However, a tablet containing 1.5 g of the active substance may seem very large to the patient, and several smaller tablets (and accordingly with a lower content of the active substance) may produce a subjective impression of an overdose with subsequent non-compliance by the patient with the doctor's prescriptions (Aghazadeh-Habashi A., 2011). That is why Artiflex is available in the form of a powder for preparing a solution. One dose contains the equivalent of 1500 mg of glucosamine. A portion of the powder is dissolved in a glass of clean water and taken orally once a day. To achieve a stable therapeutic effect, the drug must be taken in long courses - 4-12 weeks each. Such courses can be repeated 2-3 times a year, with an interval of 2 months between courses.
Possible scope of application of glucosamine-based drugs:
- cervical spondylosis (Li Y., 2018);
- osteochondrosis (localized or widespread);
- osteoarthritis (Matheson AJ, 2003), especially of the hip and knee joints;
- other inflammatory-degenerative diseases of the musculoskeletal system;
- after surgical interventions on the joints, including meniscus plastic surgery and total joint replacement;
- due to its healing properties, glucosamine can be used as an adjunct to the treatment of inflammatory bowel diseases (e.g. Crohn's disease) (Bissett DL, 2006);
- glucosamine is used in cosmetology to reduce skin pigmentation and reduce the number of wrinkles (Bissett DL, 2006).
Characteristics of the components of Artiflex cream
Methylpyrrolidone is a drug from the ketopyrrole group. In its chemical structure, it is close to β-lactams, and in addition, it is a universal solvent. In medicine, it is used as an inert universal carrier for transdermal penetration, i.e. it improves the penetration of substances applied to the skin into the tissues (Ameen D. 2017). It has moderate immunomodulatory activity, which causes potentiation of the therapeutic effect in local inflammatory processes. This substance is non-toxic and non-carcinogenic to humans (Schortt J., 2014), however, if Artiflex in the form of a cream is used for a long time and in large quantities, a peculiar yellow color of urine may be observed.
Ibuprofen belongs to the group of nonsteroidal anti-inflammatory drugs and is a derivative of propionic acid. Its anti-inflammatory and analgesic effect is based on the inhibition of the synthesis of prostaglandins E and F, and the action is carried out both at the peripheral and central levels. This mechanism is implemented by non-selective blocking of the enzymes COX-1 and COX-2. Due to the reduction in the synthesis of prostaglandins, such manifestations of the inflammatory process as hyperemia and pain are reduced. Moreover, the analgesic effect is provided by a complex mechanism: prostaglandins increase the irritability of sensitive nerve fibers (Ershad M., 2019). In addition, the antiplatelet activity inherent in ibuprofen allows you to improve local capillary blood circulation.
Allantoin is an anti-inflammatory agent of plant or animal origin. Today, it is most often obtained by extracting it from the roots of the comfrey plant (Symphytum), better known to the people as comfrey. This agent is also known for its astringent and analgesic, antioxidant and cytoprotective (da Silva DM, 2018) properties. The analgesic effect of allantoin is provided by the effect on peripheral opioid receptors (Florentino IF, 2016). In addition, allantoin is characterized by such effects as reducing irritation, keratolytic activity, and stimulation of cell mitosis (Araujo A., 2010).
application features
Since glucosamine is a low-molecular carbohydrate derivative, it is likely that it can be involved in carbohydrate metabolism and influence blood glucose levels. Animal experiments have shown that glucosamine is involved in glucose metabolism through the biosynthesis of hexosamine (Dostrovsky NR, 2011). In addition, the results of experimental studies on animals (Kajinuma H., 1975) demonstrate an increase in the blood level of immunoreactive glucagon (which is a counterinsular hormone) when exogenous glucosamine is administered to the body.
Therefore, the use of glucosamine requires caution in patients with diabetes (Stumph JL, 2006). In such cases, it is recommended to monitor the level of glucose and glycosylated hemoglobin in the blood, as well as adjust the dose of insulin or other sugar-lowering drugs.
In addition, since glucosamine in the modern pharmaceutical industry is produced by hydrolysis of crustacean exoskeletons, it should be prescribed with caution to patients with food allergies to fish and shellfish (Dahmer S., 2008).
There are isolated reports of glucosamine potentiating the action of warfarin (Dahmer S., 2008), so patients receiving anticoagulants require monitoring of blood coagulation parameters.
Since high doses of methylpyrrolidone are characterized by teratogenic effects (Shortt J., 2014), the use of Artiflex cream during pregnancy is contraindicated.
Due to the local application of ibuprofen in Artiflex cream, its systemic effect is small. However, it is necessary to remember the undesirable effects characteristic of all non-steroidal anti-inflammatory drugs: gastropathic manifestations (pain in the stomach, nausea, heartburn), decreased blood clotting, as well as nephrotoxicity.
Since glucosamine is a non-toxic substance, there have been no cases of overdose with Artiflex. However, patients should be aware that a short-term excess of the recommended dose will not lead to an increase in the therapeutic effect. This is due to the fact that the regeneration of cartilage and synovial tissue occurs slowly - over several months.
conclusion
Degenerative-dystrophic diseases of the musculoskeletal system are one of the leading medical and social problems in the modern world. Osteoarthritis in the general population affects approximately 10% of men and 18% of women over the age of 60 (OARSI, 2016), and 80% of them have mobility limitations, significantly impairing the quality of life. It is worth noting that the incidence of osteoarthritis is steadily increasing due to the aging of the population and the increase in the prevalence of obesity (ESCEO, 2019). The search for optimal strategies for the treatment of osteoarthritis includes reducing the severity of symptoms and, ultimately, slowing the progression of the pathology.
The use of glucosamine-based drugs is of interest due to their effects aimed at maintaining the normal structure of cartilage and joint function along with alleviating the symptoms of the disease. The two forms of the drug Artiflex allow you to create a convenient therapeutic combination that provides both systemic and local effects on the pathological process in diseases of the musculoskeletal system. And the absence of the risk of overdose and a minimum of side effects make Artiflex a promising tool for long-term use.
