Dexalgin 25, pills 25 mg, 10 pcs.

Composition

Core:

Active ingredient: Dexketoprofen trometamol – 36.90 mg, (dexketoprofen equivalent) – 25.00 mg.

Auxiliary substances: microcrystalline cellulose – 141.20 mg, corn starch-49.60 mg, sodium carboxymethyl starch (type A) – 27.10 mg, glycerol distearate-5.20 mg.

Film shell: Hypromellose – 1.34 mg, titanium dioxide (E 171) – 0.36 mg, macrogol 6000-0.60 mg, propylene glycol-0.42 mg

. Pharmacological action

Pharmacotherapy group: nonsteroidal anti-inflammatory drugs (NSAIDs).

ATX code: M 01 AE 17

Pharmacological properties

Pharmacodynamics

Dexketoprofen trometamol, the Active ingredient of Dexalgin ® 25, is a nonsteroidal anti-inflammatory drug (NSAID) that has 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 ingestion of the drug, the duration of therapeutic action is 4-6 hours

. Pharmacokinetics

Suction.  The time to reach the maximum concentration (TMAX) of dexketoprofen in blood plasma after a single oral 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 average volume of distribution (Vd) is less than 0.25 l / kg, with a half-life of about 0.35 hours.

Metabolism and elimination.  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.

Use during pregnancy and lactation

The use of Dexalgin ® 25 during pregnancy and lactation is contraindicated.

Contraindications

• hypersensitivity to dexketoprofen, other components of the drug and other NSAIDs;
• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance of acetylsalicylic acid or other NSAIDs (including in the anamnesis);
• erosive-ulcerative lesions of the gastrointestinal tract in the acute stage;
• gastrointestinal bleeding or perforation in history, including previous use of NSAIDs;
• gastrointestinal bleeding; other active bleeding (including suspected intracranial hemorrhage);
• inflammatory bowel disease (Crohn’s disease, ulcerative colitis) in the acute phase;
• liver failure severe severity (10-15 points on a scale child-Pugh);
• progressive kidney diseases, confirmed hyperkalemia;
• chronic kidney disease: stage 3 a (glomerular filtration rate (GFR) 45-59 ml/min/1.73 m 2),3 b (GFR 30-44 ml/min/1.73 m 2) and 4 (GFR < 30 ml/min/1.73 m 2).
• the period after coronary artery bypass grafting;
• severe heart failure (NYHA class III-IV);
• hemorrhagic diathesis and other blood clotting disorders;
• age up to 18 years (due to lack of data on efficacy and safety);
• pregnancy and lactation.

With caution

Peptic ulcer of the stomach and duodenum, 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 the volume of circulating blood (including after surgery), elderly patients over 65 years (including those receiving diuretics, weakened patients and low body weight), bronchial asthma 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 classifications 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 (

Disorders of the blood and lymphatic system

Very rare: neutropenia, thrombocytopenia.

Immune system disorders

Rarely: laryngeal edema;

Very rare: anaphylactic reactions, including anaphylactic shock.

Nervous system disorders

Infrequently: headache, dizziness, drowsiness;

Rarely: paresthesia, syncopal states (transient short-term syncope).

Mental disorders

Infrequently: insomnia, feeling restless.

Hearing disorders and labyrinth disorders

Infrequently: vertigo.

Very rare: tinnitus.

Visual disturbances

Very rare: blurred vision.

Disorders of the cardiovascular system

Infrequently: palpitation of the heart, feeling of heat, hyperemia of the skin;

Rarely: increased blood pressure;

Very rare: tachycardia, low blood pressure.

Respiratory system disorders

Rarely: bradypnea;

Very rare: bronchospasm, shortness of breath.

Gastrointestinal disorders

are Common: 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: damage to the pancreas.

Liver and biliary tract disorders

Rarely: hepatitis, increased activity of “liver” enzymes (ALT, AST);

Very rare: liver damage.

Kidney and urinary tract disorders

Rarely: polyuria, acute renal failure;

Very rare: nephritis or nephrotic syndrome.

Reproductive system disorders

Rarely: in women-a violation of the menstrual cycle, in men-a temporary violation of the function of the prostate gland with prolonged use.

Musculoskeletal system disorders

Rarely: back pain.

Skin and subcutaneous tissue disorders

Infrequently: skin rash;

Rarely: urticaria, acne, increased sweating;

Very rare: severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome)), angioedema, facial edema, allergic dermatitis, photosensitization, pruritus.

Metabolic disorders

Rarely: 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 other 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.

Unwanted combinations

With other NSAIDs, including high-dose salicylates (more than 3 g / day): concomitant use of several NSAIDs increases the risk of gastrointestinal bleeding and ulceration due to the synergistic effect.

With anticoagulants: dexketoprofen, like other NSAIDs, can enhance the effect of anticoagulants such as warfarin due to the 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: when used concomitantly, the risk of bleeding increases (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 simultaneously 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: it is possible to increase their toxic effect.

Combinations that require caution

With diuretics, angiotensin-converting enzyme (ACE) inhibitors, aminoglycoside antibiotics, and 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 low-dose methotrexate (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 renal dysfunction, even mild, 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 necessary.

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 can increase nephrotoxicity, which is mediated by the action of renal prostaglandins. When used concomitantly, renal function should be monitored.

With thrombolytics: the risk of bleeding increases.

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 cardiac 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 NSAIDs are co-administered with high-dose quinolones.

If the concomitant use of Dexalgin ® 25 with the above medications is necessary, consult your doctor.

How to take, course of administration and dosage

Dexalgin 25 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 of Dexalgin® 25) every 4-6 hours or 25 mg dexketoprofen (1 tablet of Dexalgin® 25) every 8 hours.

The maximum daily dose is 75 mg.

The drug Dexalgin® 25 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 Dexalgin 25 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 Dexalgin ® 25, starting with the minimum recommended dose. The maximum daily dose is 50 mg.

The use of Dexalgin 25 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 Dexalgin ® 25, starting with the minimum recommended dose. The maximum daily dose is 50 mg. Use of Dexalgin 25 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.

Description

round biconvex tablets, film-coated in white, with a risk on both sides of the tablet.

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 Dexalgin® 25 in this category of patients should begin with the lowest recommended dose.

Patients of the above categories, as well as patients who require simultaneous use of low doses of acetylsalicylic acid or other agents that increase the risk of gastrointestinal complications, are recommended to additionally use 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 gastrointestinal disorders or a history of gastrointestinal diseases should be closely monitored. In case of gastrointestinal bleeding or ulcerative lesions, the use of Dexalgin® 25 should be discontinued.

Dexalgin 25 should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn’s disease), as these diseases may worsen.

All NSAIDs can inhibit platelet aggregation and increase bleeding time by inhibiting prostaglandin synthesis. Therefore, the use of Dexalgin 25 in patients taking concomitant medications that affect the hemostatic system, such as warfarin, coumarin derivatives and heparins, is not recommended.

Like other NSAIDs, Dexalgin 25 may lead to increased plasma creatinine and nitrogen concentrations. Like other prostaglandin synthesis inhibitors, Dexalgin ® 25 may have a side effect 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, there may be a slight transient increase in the activity of “liver” enzymes during Dexalgin 25 therapy. In elderly patients, monitoring of liver and kidney function is necessary. In case of a significant increase in the corresponding indicators, the use of Dexalgin® 25 should be discontinued.

Like other NSAIDs, dexketoprofen may mask the symptoms of infectious diseases. In case of signs of infection or deterioration of health during the use of Dexalgin® 25, 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, Dexalgin® 25 should be used with extreme caution. If the condition worsens, the use of Dexalgin ® 25 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 Dexalgin ® 25 to patients with a history of cardiovascular disease, 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 Dexalgin ® 25 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, Dexalgin® 25 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 during the use of Dexalgin® 25, the ability to concentrate and speed of psychomotor reactions in patients may decrease, especially in the first hour after administration. Therefore, when using Dexalgin® 25, caution should be exercised 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 25 mg.

10 tablets in a contour cell pack (blister) [PVC/aluminum foil or aluminum foil/aluminum foil].

1,3 or 5 blisters with instructions for use in a cardboard box.

Storage conditions

Blister [PVC / aluminum foil]

In a dry place protected from light at a temperature not exceeding 25 ° C.

Blister [aluminum foil/aluminum foil]

At a temperature not exceeding 30 ° C.

Keep the medicine out of the reach of children!

Expiration date

Blister [PVC / aluminum foil] – 2 years.

Blister [aluminum foil/aluminum foil] – 3 years.

Do not use after the expiration date indicated on the package.

Active ingredient

Dexketoprofen

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Sciatica, Sciatica, Osteochondrosis, Trigeminal Neuralgia, Osteoarthritis, Lumbago, Arthritis, Rheumatoid Arthritis

Weight

Weight: 8 gr.