Dexonal pills 25 mg, 10 pcs.

Composition

1 tablet contains:Active ingredient:dexketoprofen trometamol 36.9 mg, based on dexketoprofen 25 mg; excipients:microcrystalline cellulose, corn starch, sodium carboxymethyl starch (sodium starch glycolate), colloidal anhydrous silicon dioxide (aerosil), magnesium stearate; excipients for the shell:hypromellose (hydroxypropylmethylcellulose), macrogol 6000 (polyethylene glycol 6000), titanium dioxide. Descriptioncircular biconvex film-coated tablets of white or almost white color, with a risk. On a cross-section, the core is white or almost white in color.

Pharmacological action

Pharmacotherapy group: nonsteroidal anti-inflammatory drugs (NSAIDs). ATX code: M01AE17 Pharmacological Propertiespharmacodynamicadexketoprofen trometamol, the Active ingredient of Dexonal®, refers to nonsteroidal anti-inflammatory drugs (NSAIDs) that have analgesic, anti-inflammatory and antipyretic effects. The mechanism of action of dexketoprofen is based on inhibition of prostaglandin synthesis at the level of cyclooxygenases (COX-1 and COX-2). The analgesic effect occurs 30 minutes after oral administration of Dexonal®, the duration of therapeutic action reaches 4-6 hours. PharmacokineticAbsorption. The time to reach the maximum concentration (TMAX) of dexketoprofen in blood plasma after a single dose is on average 30 minutes (15-60 minutes). Simultaneous food intake slows down the absorption of dexketoprofen. The areas under the concentration-time curve (AUC) after single and repeated doses are similar, which indicates that there is no accumulation of the drug. Distribution. Dexketoprofen is characterized by a high degree of binding to plasma proteins (99%). The mean volume of distribution (Vd) is less than 0.25 l/kg, and the half-life is about 0.35 h. Metabolism and excretion. The main route of metabolism of dexketoprofen is its conjugation with glucuronic acid, followed by excretion by the kidneys. The half-life (T1/2) of dexketoprofen is 1.65 hours. In the elderly, there is an extension of the half-life to 48%, and a decrease in the total clearance of the drug.

Indications

Musculoskeletal pain (mild or moderate), algodismenorrhea, toothache. The drug is intended for symptomatic treatment, reducing pain and inflammation at the time of use.

Contraindications

-hypersensitivity to dexketoprofen, other components of the drug and other NSAIDs;- complete or incomplete combination of bronchial asthma, recurrent nasal and paranasal sinus polyposis, and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis);- erosive and ulcerative lesions of the gastrointestinal tract in the acute stage; – gastrointestinal bleeding or perforation in the anamnesis, including those associated with the previous use of NSAIDs;- gastrointestinal bleeding; other active bleeding (including suspected intracranial hemorrhage);- acute inflammatory bowel diseases (Crohn’s disease, ulcerative colitis); – severe liver failure (10-15 points on the Child-Pugh scale);- progressive kidney disease, confirmed hyperkalemia; – chronic kidney disease: stage 3a (glomerular filtration rate (GFR) 45-59 ml / min/1.73 m2),3B (GFR 30-44 ml / min/1.73 m2) and 4 (GFR;- severe heart failure (NYHA class III –IV);- hemorrhagic diathesis and other blood clotting disorders;- under 18 years of age (due to lack of efficacy and safety data);- pregnancy and lactation period. With caution: gastric ulcer and duodenal ulcer, ulcerative colitis, Crohn’s disease, a history of liver disease, hepatic porphyria, chronic kidney disease, stage 2 (GFR 60-89 ml/min/ 1.73 m2), chronic heart failure, arterial hypertension, significant decrease in circulating blood volume (including after surgery), elderly patients over 65 years of age (including those receiving diuretics, debilitated patients and patients with low body weight), bronchial asthma, concomitant use of glucocorticosteroids (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), coronary heart disease, cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases, smoking, the presence of Helicobacter pylori infection, systemic lupus erythematosus (SLE) and other systemic connective tissue diseases, long-term use of nonsteroidal anti-inflammatory drugs, tuberculosis, severe osteoporosis, alcoholism, severe somatic diseases.

Side effects

Possible side effects are listed according to the World Health Organization classification below in descending order of frequency: very common (≥1/10); common (≥1/100, <1/10); uncommon (≥ 1/1000, <1/100); rare (≥1/10000, <1/1000); very rare (From the blood and lymphatic system Very rarely: neutropenia, thrombocytopenia. Immune system disorders Occasionally: laryngeal edema. Very rare: anaphylactic reactions, including anaphylactic shock. Nervous system disorders Infrequently: headache, dizziness, drowsiness. Rare: paresthesia, syncopal states (transient short-term syncope). From the side of the psyche often: insomnia, feeling of anxiety. From the side of the organ of hearing and labyrinth disorders often: vertigo. Very rare: tinnitus. From the side of the organ of vision is very rare: blurred vision. On the part of the cardiovascular system, often: palpitation, feeling of heat, hyperemia of the skin. Rare: increased blood pressure. Very rare: tachycardia, low blood pressure. From the respiratory system Rarely: bradypnea. Very rare: bronchospasm, shortness of breath. From the gastrointestinal tract Often: nausea, vomiting, abdominal pain, dyspepsia, diarrhea. Infrequently: gastritis, constipation, dry mouth, flatulence. Rarely: erosive and ulcerative lesions of the gastrointestinal tract( GIT), bleeding from the ulcer or its perforation. Very rare: pancreatic involvement. From the liver and biliary tract Rarely: hepatitis, increased activity of “liver” enzymes (AST and ALT). Very rare: liver damage. From the side of the kidneys and urinary tract Rarely: polyuria, acute renal failure. Very rare: nephritis or nephrotic syndrome. On the part of the reproductive system is rare: in women-a violation of the menstrual cycle, in men-a transient violation of the function of the prostate gland with prolonged use. Musculoskeletal disorders Rare: back pain. Skin and subcutaneous tissue disorders: Infrequently: skin rash. Rare: hives, acne, increased sweating. Very rare: severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome)), angioedema, facial edema, allergic dermatitis, photosensitization, pruritus. From the side of metabolism: Rare: anorexia nervosa. General violations: Infrequently: increased fatigue, asthenia, chills, general malaise. Very rare: peripheral edema. As with other NSAIDs, the following side effects may occur: aseptic meningitis, which develops mainly in patients with systemic lupus erythematosus or systemic connective tissue diseases, hematological disorders (thrombocytopenic purpura, aplastic and hemolytic anemia, in rare cases-agranulocytosis and bone marrow hypoplasia).

Interaction

The following interactions are common to all NSAIDs. Undesirable combinations with other NSAIDs, including salicylates in high doses (more than 3 g / day): simultaneous use of several NSAIDs due to the synergistic effect increases the risk of gastrointestinal bleeding and ulceration. With anticoagulants: dexketoprofen, like other NSAIDs, may enhance the effect of anticoagulants such as warfarin due to a high degree of binding to plasma proteins, inhibition of platelet aggregation and damage to the gastrointestinal mucosa. If simultaneous use is necessary, careful monitoring of the patient’s condition and regular monitoring of laboratory parameters is necessary. With heparin: concomitant use increases the risk of bleeding (due to inhibition of platelet aggregation and damaging effect on the gastrointestinal mucosa). If simultaneous use is necessary, careful monitoring of the patient’s condition and regular monitoring of laboratory parameters is necessary. With glucocorticosteroids: concomitant use increases the risk of gastrointestinal ulceration and bleeding. With lithium preparations: NSAIDs increase the concentration of lithium in blood plasma up to toxic, and therefore this indicator should be monitored when used with dexketoprofen, changing the dosage, as well as after discontinuation of NSAIDs. With methotrexate in high doses (15 mg / week or more): It is possible to increase the hematological toxicity of methotrexate due to a decrease in its renal clearance when used simultaneously with NSAIDs. With hydantoins and sulfonamides: their toxic effects may be increased.Combinations requiring caution with diuretics, angiotensin-converting enzyme (ACE) inhibitors, aminoglycoside antibiotics, angiotensin II receptor antagonists: concomitant use with NSAIDs is associated with the risk of acute renal failure in dehydrated patients (reduced glomerular filtration rate due to reduced prostaglandin synthesis). When used concomitantly, NSAIDs may reduce the antihypertensive effect of certain medications. When dexketoprofen is used concomitantly with diuretics, it is necessary to make sure that the patient does not show signs of dehydration, and also to monitor renal function at the beginning of simultaneous use. With methotrexate in low doses (less than 15 mg / week): it is possible to increase the hematological toxicity of methotrexate due to a decrease in its renal clearance against the background of simultaneous use with NSAIDs. It is necessary to count blood cells at the beginning of simultaneous use. In the presence of impaired renal function, even in a mild degree, as well as in the elderly, careful medical supervision is necessary. With pentoxifylline: there may be an increased risk of bleeding. Careful clinical monitoring and regular checking of the bleeding time (blood clotting time)is required. With zidovudine: there is a risk of increased toxic effects on red blood cells due to exposure to reticulocytes, with the development of severe anemia one week after the start of NSAID use. It is necessary to conduct a general blood test with counting the number of reticulocytes 1-2 weeks after the start of NSAID therapy. With oral hypoglycemic agents: NSAIDs may increase the hypoglycemic effect of sulfonylureas due to the displacement of sulfonylureas from the sites of binding to plasma proteins. Combinations to take into account with beta-blockers: when used concomitantly with NSAIDs, the antihypertensive effect of beta-blockers may decrease due to inhibition of prostaglandin synthesis. With cyclosporine and tacrolimus: NSAIDs may increase nephrotoxicity, which is mediated by the action of renal prostaglandins. When used concomitantly, renal function should be monitored. With thrombolytics: increased risk of bleeding. The risk of gastrointestinal bleeding increases when used concomitantly with serotonin reuptake inhibitors (citalopram, fluoxetine, sertraline) and anticoagulants. With probenecid: it is possible to increase the concentration of NSAIDs in blood plasma, which may be due to the inhibitory effect of probenecid on renal tubular secretion and/or conjugation with glucuronic acid; it may be necessary to adjust the dose of NSAIDs. With cardiac glycosides: Concomitant use with NSAIDs may lead to an increase in the concentration of glycosides in blood plasma. With mifepristone: due to the theoretical risk of changing the effectiveness of mifepristone under the influence of prostaglandin synthesis inhibitors, NSAIDs should not be used earlier than 8-12 days after mifepristone withdrawal. With quinolones: data obtained in experimental animal studies indicate a high risk of seizures when using NSAIDs with high doses of quinolones. If you need to use Dexonal® concomitantly with the above medications, you should consult your doctor.

How to take, course of administration and dosage

Dexonal® is taken orally with a meal. Simultaneous food intake slows down the absorption of dexketoprofen, so in case of acute pain, it is recommended to use the drug at least 30 minutes before meals.

Depending on the intensity of the pain syndrome, the recommended adult dose is 12.5 mg dexketoprofen (1/2 tablet Dexonal®) every 4-6 hours or 25 mg dexketoprofen (1 tablet Dexonal®) every 8 hours.

The maximum daily dose is 75 mg.

The drug is not intended for long-term therapy, the course of treatment with the drug should not exceed 3-5 days.

Patients 65 years and older

Elderly patients should take the drug starting from the minimum recommended dose. The maximum daily dose is 50 mg. In case of good tolerability, the recommended doses for the general population can be used.

Patients with hepatic insufficiency

Patients with mild to moderate hepatic insufficiency should take the drug starting from the minimum recommended dose. The maximum daily dose is 50 mg.

The use of Dexonal® in patients with severe hepatic insufficiency is contraindicated.

Patients with renal insufficiency

Patients with mild renal insufficiency – chronic kidney disease, stage 2 (GFR 60-89 ml / min/ 1.73 m2) should take the drug starting from the minimum recommended dose. The maximum daily dose is 50 mg. Use of the drug in patients with chronic kidney disease stages 3a (GFR 45-59 ml / min/1.73 m2),3B (GFR 30-44 ml / min/1.73 m2) and 4 (GFR

Overdose

Symptoms: nausea, anorexia, abdominal pain, headache, dizziness, disorientation, insomnia. Treatment: symptomatic therapy, if necessary — gastric lavage, taking activated charcoal, hemodialysis is ineffective.

Special instructions

Undesirable side effects can be minimized by using the drug in the lowest effective dose with the minimum duration of use necessary for the relief of pain. The risk of gastrointestinal complications increases in patients with a history of ulcerative lesions of the gastrointestinal tract, in elderly patients, with an increase in the dose of NSAIDs; therefore, the use of the drug in this category of patients should begin with the lowest recommended dose. Patients of the above categories, as well as patients who require concomitant use of low doses of acetylsalicylic acid or other agents that increase the risk of gastrointestinal complications, are recommended to use additional gastroprotectors (misoprostol or proton pump blockers). Patients taking concomitant antiplatelet agents or anticoagulants, as well as glucocorticosteroids, also have an increased risk of gastrointestinal bleeding. Patients with a history of gastrointestinal disorders or gastrointestinal diseases should be closely monitored. In case of gastrointestinal bleeding or ulcerative lesions, the use of the drug should be discontinued. The drug should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn’s disease), since these diseases may worsen. All NSAIDs can inhibit platelet aggregation and increase bleeding time by inhibiting prostaglandin synthesis. Therefore, the use of Dexonal® in patients taking concomitant medications that affect the hemostatic system, such as warfarin, coumarin derivatives and heparins, is not recommended. As with other NSAIDs, Dexonal may lead to increased plasma creatinine and nitrogen concentrations. Like other prostaglandin synthesis inhibitors, Dexonal® may have side effects on the urinary system, which may lead to the development of glomerulonephritis, interstitial nephritis, papillary necrosis, nephrotic syndrome, and acute renal failure. Caution should be exercised when using the drug in patients who are simultaneously using diuretics and patients who may develop hypovolemia, due to an increased risk of nephrotoxicity. As with other NSAIDs, when using Dexonal® there may be a slight transient increase in some “liver” enzymes. In the elderly, monitoring of liver and kidney function is necessary. In case of a significant increase in the corresponding indicators, the use of prepart Dexonal® should be discontinued. Like other NSAIDs, dexketoprofen may mask the symptoms of infectious diseases. If signs of infection or deterioration of health are detected during the use of Dexonal®, the patient should immediately consult a doctor. The drug may cause fluid retention in the body, so in patients with arterial hypertension, renal and/or heart failure, Dexonal® should be used with extreme caution. If the condition worsens, the drug should be discontinued. In patients with uncontrolled hypertension, coronary heart disease, congestive heart failure, peripheral arterial diseases and / or cerebrovascular diseases, the drug should be used with caution. A similar approach is applicable to patients with risk factors for developing cardiovascular diseases (arterial hypertension, hyperlipidemia, diabetes mellitus, smoking). Caution should be exercised when prescribing the drug to patients with a history of cardiovascular diseases, especially patients with heart failure, due to the possible risk of progression. Clinical studies and epidemiological data suggest that NSAIDs, especially in high doses and with prolonged use, may lead to a low risk of developing acute myocardial infarction or stroke. Data are not sufficient to exclude the risk of these events when using dexketoprofen. Elderly patients are particularly susceptible to adverse reactions when using NSAIDs, including the risk of gastrointestinal bleeding and perforation, which threatens the patient’s life, reduced kidney, liver and heart function. When using Dexonal® in this category of patients, proper clinical monitoring is necessary.There are data on the occurrence of rare cases of skin reactions (such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) with the use of NSAIDs. At the first appearance of skin rash, mucosal lesions, or other signs of an allergic reaction, Dexonal® should be discontinued immediately and a doctor should be consulted. Influence on the ability to drive vehicles and other mechanisms. Due to the possible occurrence of dizziness and drowsiness while taking the drug, the ability to concentrate and the speed of psychomotor reactions in patients may decrease, especially in the first hour after taking the drug. Therefore, during the use of the drug, care should be taken when driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

film-coated tablets

Storage conditions

At a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 3 years. Do not use the product after the expiration date indicated on the package.

Active ingredient

Dexketoprofen

Dosage form

Tablets

Weight

Weight: 10 g.