Argett Duo 75mg 20 capsules — Made in Switzerland — Free Delivery

Pharmacological properties

Pharmacodynamics. Argett Duo contains diclofenac sodium, a non-steroidal compound that has a pronounced anti-inflammatory, analgesic and antipyretic effect. the main mechanism of action of diclofenac is the inhibition of prostaglandin biosynthesis. prostaglandins play an important role in the genesis of inflammation, pain and fever.

In vitro, diclofenac sodium at concentrations equivalent to those achieved in the treatment of patients does not inhibit the biosynthesis of proteoglycans in cartilage tissue.

Pharmacokinetics. After oral administration of a modified-release capsule, the maximum plasma level is reached depending on the duration of passage through the stomach, on average - after 2-3 hours.

Plasma protein binding is 99.7%, it occurs mainly with albumin (99.4%). The estimated volume of distribution is 0.12–0.17 l / kg.

Diclofenac penetrates into the synovial fluid, where its Cmax is reached 2–4 hours later than in blood plasma. The estimated T1 / 2 from the synovial fluid is 3-6 hours. 2 hours after reaching Cmax in the blood plasma, the concentration of diclofenac in the synovial fluid is higher than in the blood plasma, and its value remains higher for 12 hours.

Diclofenac metabolism is carried out in part by glucuronidation of the unchanged molecule, but mainly through single and multiple methoxylation, which leads to the formation of several phenolic metabolites (3′-hydroxy-, 4′-hydroxy-, 5′-hydroxy-, 4 ′, 5- dihydroxy- and 3'-hydroxy-4'-methoxydiclofenac), most of which are converted to glucuronide conjugates. Two of these phenolic metabolites are biologically active, but to a significantly lesser extent than diclofenac.

The total systemic plasma clearance of diclofenac is 263 ± 56 ml / min. The final T1 / 2 is 1-2 hours. T1 / 2 of 4 metabolites, including two pharmacologically active ones, is also short-lived - 1-3 hours. One of the metabolites, 3'-hydroxy-4'-methoxydiclofenac, has a longer T1 / 2, but this metabolite is completely inactive.

About 60% of the dose of the preparation is excreted in the urine in the form of glucuronic conjugates of the unchanged active substance, as well as in the form of metabolites, most of which are glucuronic conjugates. Less than 1% of diclofenac is excreted unchanged. The remaining doses of the preparation are excreted in the form of metabolites in the bile, in the feces.

Pharmacokinetics in certain groups of patients. No accumulation of diclofenac was observed in patients with impaired renal function when using Argett Duo in usual single doses. In the case when creatinine clearance is 10 ml / min, the calculated equilibrium concentrations of diclofenac hydroxymetabolites are approximately 4 times higher than in healthy volunteers. Ultimately, however, the metabolites are excreted in the bile.

In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetics of diclofenac are similar to those in patients without liver disease.

Indications

Symptomatic treatment of pain and inflammation in:

• rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, spondyloarthritis, pain syndrome of various localization, extra-articular rheumatism;
• edema with pain or post-traumatic inflammation.

Application

Argett Duo is used to treat adult patients, starting with a daily dose of 75–150 mg, depending on the severity of symptoms. with mild symptoms, as well as with prolonged therapy, a dose of 75 mg / day is sufficient. if necessary, to act on night pain or morning stiffness, the preparation should be taken before bedtime. the daily dose should not exceed 150 mg.

The preparation should be used in the minimum effective doses for the minimum period of time, taking into account the goals of treatment for each individual patient.

Arguette Duo is taken without chewing, drinking plenty of fluids with meals.

Elderly patients. No special dose adjustment is required, but the preparation should be used with caution.

Impaired renal function. Patients with mild to moderate renal impairment do not require dose reduction.

Liver dysfunction. Patients with mild to moderate hepatic impairment do not require dose reduction.

Contraindications

Hypersensitivity to diclofenac, soy, peanuts or other components of the preparation; a stomach or intestinal ulcer, gastrointestinal bleeding or perforation; patients who, in response to taking acetylsalicylic acid or other NSAIDs, have attacks of BA, urticaria, or acute rhinitis; iii trimester of pregnancy; proctitis, hemorrhoidal symptoms, rectal bleeding, or other active bleeding; severe impairment of liver or kidney function; severe dysfunction of the heart; unexplained disorders of hematopoiesis; congestive heart failure (nyha ii – iv); ischemic heart disease in patients with angina pectoris, myocardial infarction; cerebrovascular diseases in patients who have suffered a stroke or have episodes of transient ischemic attacks; peripheral arterial disease; treatment of perioperative pain with coronary artery bypass grafting (or using a heart-lung machine).

Side effects

The following categories are used to assess adverse reactions: very often (≥1 / 10); often (≥1 / 100, 1/10); rarely (from ≥1 / 1000, 1/100); isolated cases (from ≥1 / 10,000, 1/1000); very rare (1/10 000); the frequency is unknown (cannot be estimated from the available data).

Clinical research data and epidemiological data indicate an increased risk of thrombotic complications (for example, myocardial infarction or stroke) associated with the use of diclofenac, in particular in high therapeutic doses (150 mg / day) and with prolonged use.

From the digestive system: often - pain in the epigastric region, nausea, vomiting, diarrhea, abdominal cramps, dyspepsia, bloating, anorexia; infrequently - gastrointestinal bleeding (bloody vomiting, melena, diarrhea mixed with blood), stomach and intestinal ulcers, accompanied or not accompanied by bleeding or perforation; isolated - stomatitis, glossitis, lesions of the esophageal mucosa, adhesions in the intestine, hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, pancreatitis.

From the side of the central nervous system: often - headache, dizziness, severe dizziness; infrequently - drowsiness; isolated - impaired sensitivity, including paresthesias, memory disorders, disorientation, insomnia, irritability, convulsions, depression, anxiety, nightmares, tremors, psychotic reactions, aseptic meningitis.

From the senses: isolated - visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, impaired taste.

From the side of the skin and its derivatives: often - skin rash; infrequently - urticaria; single - blistering rash, eczema, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome (acute toxic epidermal necrolysis), erythroderma (exfoliative dermatitis), hair loss, photosensitive reactions; purpura, including allergic.

From the side of the kidneys: often - edema; isolated - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

From the liver: often - an increase in the level of aminotransferases in the blood plasma; infrequently - hepatitis with or without jaundice; isolated - fulminant hepatitis.

From the hematopoietic system: single - thrombocytopenia, leukopenia, hemolytic anemia, aplastic anemia, agranulocytosis.

Hypersensitivity reactions: infrequently - BA; systemic anaphylactic / anaphylactoid reactions, including hypotension; isolated - vasculitis, pneumonitis.

From the side of the cardiovascular system: single - palpitations, chest pain, hypertension, congestive heart failure.

Special instructions

Since the release of the active substance from the preparation Argett Duo occurs with a delay, this dosage form is not optimal when it is necessary to obtain a rapid analgesic or anti-inflammatory effect.

Elderly patients. With the use of NSAIDs in elderly patients, side effects occur more often, especially gastrointestinal bleeding and perforation, which can sometimes be fatal.

Effect on the gastrointestinal tract. The use of diclofenac sodium in combination with other NSAIDs, including selective COX-2 inhibitors, should be avoided. The severity of unwanted effects can be reduced by taking the lowest effective dose for the shortest period necessary to control symptoms.

Gastrointestinal bleeding, ulceration and perforation. With all NSAIDs, gastrointestinal bleeding, ulcers or perforations, sometimes fatal, have been reported. Their appearance at any stage of treatment was accompanied or not accompanied by preliminary warning symptoms or the presence of serious gastrointestinal events in the history.

Patients with a history of gastrointestinal toxicity, especially the elderly, should report any unusual abdominal symptoms (especially gastrointestinal bleeding).

Caution is advised in patients who are concomitantly taking medications that increase the risk of ulcers or bleeding, such as oral corticosteroids, anticoagulants such as warfarin, selective serotonin reuptake inhibitors, or platelet aggregation inhibitors such as acetylsalicylic acid.

If gastrointestinal bleeding or ulceration occurs in patients taking diclofenac, treatment should be discontinued.

NSAIDs should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease), as their condition may worsen.

Cardiovascular and cerebrovascular effects. Patients with hypertension and / or a history of mild to moderate congestive heart failure should be monitored and consulted as there are reports of fluid retention and edema associated with NSAID therapy.

Patients with uncontrolled hypertension, heart failure, coronary artery disease, blockage of peripheral arteries and / or cerebrovascular disease should be treated with diclofenac only after a thorough examination. The same examination should be carried out before starting long-term therapy of patients with risk factors for cardiovascular events (such as hypertension, hyperlipidemia, diabetes mellitus, smoking).

Skin reactions. Serious skin reactions have been reported very rarely with NSAIDs, some of which have been fatal, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis (Lyell's syndrome). The risk of such reactions may be highest at the beginning of treatment, since in most cases these reactions occurred in the first month of treatment. The preparation should be discontinued at the first signs of a skin rash, mucosal lesions or other signs of a hypersensitivity reaction.

Effects on the liver. Caution should be exercised before starting treatment in patients with impaired liver function, as their condition may worsen with treatment with diclofenac. With prolonged use of the preparation, it is necessary to regularly monitor liver function. If clinical signs of liver disease are detected, Argett Duo should be canceled immediately.

Other features. The preparation should be used only after a careful assessment of the risk / benefit ratio in congenital disorders of porphyrin metabolism (for example, acute intermittent porphyria), as well as in systemic lupus erythematosus or mixed connective tissue disease.

Particularly careful medical supervision is necessary in the following cases: impaired renal function; impaired liver function; immediately after major surgical interventions; hay fever, nasal polyps, or chronic obstructive pulmonary disease, as there is a risk of allergic reactions. They can manifest as asthma attacks (analgesic asthma), Quincke's edema, urticaria; allergic reactions to other substances, since there is an increased risk of hypersensitivity reactions when using Argett Duo.

Very rarely, severe hypersensitivity reactions (for example, anaphylactic shock) are noted. When the first signs of a hypersensitivity reaction appear after taking Argett Duo, its use should be discontinued. Medical personnel should initiate the necessary medical procedures according to the symptoms.

Diclofenac may temporarily inhibit platelet aggregation. Therefore, patients with bleeding disorders should be closely monitored.

As with other NSAIDs, the pharmacodynamic properties of diclofenac can mask the signs and symptoms of infection.

Therefore, the patient is advised to immediately consult a doctor if signs of infection appear or intensify while using Argett Duo. It is necessary to check the appropriateness of the use of antibiotic therapy.

With prolonged use of the preparation, it is necessary to regularly monitor kidney function and blood counts.

The use of analgesics, especially when several analgesic active ingredients are combined, can lead to kidney damage with the risk of developing renal failure (analgesic nephropathy).

The use of NSAIDs simultaneously with alcohol can potentiate the undesirable effects caused by the active substance, especially those affecting the gastrointestinal tract or central nervous system.

Prescribing diclofenac to patients with significant risk factors for cardiovascular events (for example, hypertension, hyperlipidemia, diabetes mellitus, smoking) can only be after a thorough clinical assessment. Since the cardiovascular risks of diclofenac may increase with increasing dose and duration of treatment, it should be used for the shortest possible period and at the lowest effective dose. The patient's needs for the use of diclofenac should be periodically reviewed to reduce the severity of symptoms and the response to therapy should be assessed. Use with caution in patients over the age of 65 years.

Use during pregnancy and lactation. In the I – II trimester of pregnancy, it is possible to use the preparation, taking into account the risk / benefit ratio. In the third trimester of pregnancy, the use of Argett Duo is contraindicated.

The preparation is contraindicated during lactation. It can negatively affect female fertility, therefore it is not recommended to prescribe the preparation to women planning pregnancy. In women who have problems conceiving or are undergoing studies for infertility, the feasibility of discontinuing Argett Duo should be considered.

Children. Do not use.

The ability to influence the reaction rate when driving or working with other mechanisms. For the period of treatment, you should refrain from driving or working with mechanisms.

Interactions

NSAIDs, including salicylates. Because of the synergistic effect, the simultaneous use of several NSAIDs may increase the risk of gastrointestinal ulcers and bleeding. therefore, it is not recommended to use diclofenac and other NSAIDs at the same time.

Digoxin, phenytoin, lithium. The simultaneous use of diclofenac and digoxin, phenytoin or lithium can increase the concentration of these preparations in the blood. It is necessary to monitor the level of lithium in the blood plasma. Monitoring of serum digoxin and phenytoin levels is recommended.

Diuretics, ACE inhibitors and angiotensin II antagonists. NSAIDs can weaken the effect of diuretics and antihypertensive preparations. In patients with impaired renal function (for example, patients with dehydration or elderly people with impaired renal function), the use of ACE inhibitors or angiotensin II antagonists concurrently with a preparation that inhibits COX may further impair renal function or lead to acute renal failure, which is usually reversible ... Therefore, such combinations should be prescribed with caution, especially in elderly patients. Patients should be advised to consume adequate amounts of fluids. After the start of combination therapy, it is necessary to regularly monitor the indicators of renal function.

The use of Argett Duo at the same time as potassium-sparing diuretics can lead to hyperkalemia. With the simultaneous use of such preparations, the level of potassium should be monitored.

GKS. Increased risk of gastrointestinal ulcers or bleeding.

Platelet aggregation inhibitors such as acetylsalicylic acid and selective serotonin reuptake inhibitors. Increased risk of gastrointestinal bleeding.

Methotrexate. The use of dicolfenac for less than 24 hours before or after taking methotrexate can increase the concentration of methotrexate in the blood and increase its toxic effect.

Cyclosporine. NSAIDs (such as diclofenac sodium) can increase the nephrotoxicity of cyclosporine.

Anticoagulants. NSAIDs can enhance the effect of anticoagulants such as warfarin.

Probenecid and sulfinpyrazone. Medicines containing probenecid or sulfinpyrazone may delay the elimination of diclofenac.

Overdose

There is no typical clinical picture characteristic of diclofenac overdose. overdose may be accompanied by symptoms such as vomiting, gastrointestinal bleeding, diarrhea, dizziness, tinnitus, or seizures.

In the case of severe poisoning, the development of acute renal failure and liver damage is possible.

Treatment. Treatment of acute NSAID poisoning consists in the use of supportive and symptomatic therapy. Supportive and symptomatic treatment is indicated for complications such as arterial hypotension, renal failure, convulsions, gastrointestinal disorders and respiratory depression. It is unlikely that forced diuresis, hemodialysis or hemoperfusion will be effective for removing NSAIDs, since the active substances of these preparations are largely bound to blood plasma proteins and are extensively metabolized.

Storage conditions

At a temperature not exceeding 25 ° c. store in original packaging to protect from moisture.