Dexalgin 25,25mg 10 pcs

Pharmacotherapeutic group: Non-steroidal anti-inflammatory drugs (NSAIDs).

ATX code: M01AE17

Pharmacological properties

Pharmacodynamics

Dexketoprofen trometamol, the active ingredient of the drug Dexalgin^® 25, refers to non-steroidal anti-inflammatory drugs (NSAIDs) with 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 within 30 minutes after oral administration with a therapeutic effect duration of 4-6 hours.

Pharmacokinetics

absorption. The time to reach the maximum concentration (TSmax) of dexketoprofen in blood plasma after a single oral single dose is on average 30 min (15-60 min). Simultaneous intake of food slows down absorption of dexketoprofen. Areas under the curve “concentration-time” (AUC) after a single and repeated doses are similar, indicating that there is no cumulation of the drug.

Distribution Dexectoprofen is characterized by high degree of binding to the blood plasma proteins (99 %). The mean volume of distribution (Vd) is less than 0.25 l/kg, the half-life is about 0.35 h.

Metabolism and excretion. The main route of metabolism of dexketoprofen is its conjugation with glucuronic acid with subsequent excretion by the kidneys. The half-life (T1/2) of dexketoprofen is 1.65 h. In elderly patients the elimination half-life is prolonged up to 48% and total clearance of the drug decreases.

Indications

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

Pharmacological effect

Pharmacotherapeutic group: non-steroidal anti-inflammatory drugs (NSAIDs).

ATX code: M01AE17

Pharmacological properties

Pharmacodynamics

Dexketoprofen trometamol, the active ingredient of Dexalgin® 25, is a non-steroidal 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 taking the drug orally, the duration of the therapeutic effect is 4-6 hours.

Pharmacokinetics

Suction. The time to reach the maximum concentration (TCmax) of dexketoprofen in the blood plasma after a single oral dose averages 30 minutes (15-60 minutes). Concomitant food intake slows down the absorption of dexketoprofen. The areas under the concentration-time curve (AUC) after single and repeated doses are similar, indicating the absence of drug accumulation.

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, the half-life is about 0.35 hours.

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 elderly people, an extension of the half-life to 48% and a decrease in the overall clearance of the drug are observed.

Special instructions

Undesirable side effects can be minimized by using the drug in the lowest effective dose with the minimum duration of use necessary to relieve pain.

The risk of complications from the gastrointestinal tract 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.

For patients in the above categories, as well as patients who require the simultaneous use of low doses of acetylsalicylic acid or other drugs that increase the risk of gastrointestinal complications, additional simultaneous use of gastroprotectors (misoprostol or proton pump blockers) is recommended.

In patients simultaneously taking antiplatelet agents or anticoagulants, glucocorticosteroids, the risk of gastrointestinal bleeding also increases.

Patients with gastrointestinal disorders or a history of gastrointestinal diseases should be under close medical supervision. If gastrointestinal bleeding or ulcerative lesions occur, use of Dexalgin® 25 should be discontinued.

The drug Dexalgin ®25 should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn’s disease), since exacerbation of these diseases is possible.

All NSAIDs can inhibit platelet aggregation and prolong bleeding time by inhibiting prostaglandin synthesis. In this regard, the use of Dexalgin® 25 in patients simultaneously taking drugs that affect the hemostatic system, such as warfarin, coumarin derivatives and heparins, is not recommended.

Like other NSAIDs, Dexalgin® 25 can lead to increased concentrations of creatinine and nitrogen in the blood plasma. Like other prostaglandin synthesis inhibitors, Dexalgin® 25 may have side effects on the urinary system, which can 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 concomitantly using diuretics and patients who may develop hypovolemia, due to the increased risk of nephrotoxicity.

As with the use of other NSAIDs, during therapy with Dexalgin® 25, a slight transient increase in the activity of liver enzymes may be observed. In elderly patients, monitoring of liver and kidney function is necessary. In case of a significant increase in the corresponding indicators, the use of the drug Dexalgin® 25 should be discontinued.

Like other NSAIDs, dexketoprofen may mask the symptoms of infectious diseases. If signs of infection or deterioration in health are detected while using the drug Dexalgin® 25, the patient should immediately consult a doctor.

The drug can cause fluid retention in the body, therefore, 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 arterial hypertension, coronary artery disease, congestive heart failure, peripheral arterial disease and/or cerebrovascular disease, 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 must be exercised when prescribing Dexalgin® 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 long-term use, may lead to a small risk of acute myocardial infarction or stroke. There is insufficient data to exclude the risk of these events when using dexketoprofen.

Elderly patients are especially susceptible to adverse reactions when using NSAIDs, including the risk of life-threatening gastrointestinal bleeding and perforation, and decreased renal, liver, and cardiac function. When using the drug Dexalgin® 25 in this category of patients, proper clinical monitoring is necessary.

There is evidence of rare cases of skin reactions (such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) with the use of NSAIDs. At the first manifestations of a skin rash, damage to the mucous membranes or other signs of an allergic reaction, you should immediately stop taking Dexalgin® 25 and consult a doctor.

Impact on the ability to drive vehicles and other mechanisms

Due to the possible occurrence of dizziness and drowsiness during the period of use of the drug Dexalgin® 25, the ability to concentrate and the speed of psychomotor reactions in patients may decrease, especially in the first hour after administration. Therefore, while using the drug Dexalgin® 25, care should be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Dexketoprofen

Composition

Core:

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

Excipients: microcrystalline cellulose, corn starch, sodium carboxymethyl starch (type A), glycerol distearate.

Film coating: hypromellose, titanium dioxide (E 171), macrogol 6000, propylene glycol.

Pregnancy

The use of Dexalgin® 25 during pregnancy and breastfeeding 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 to acetylsalicylic acid or other NSAIDs (including a history);
erosive and ulcerative lesions of the gastrointestinal tract in the acute stage;
history of gastrointestinal bleeding or perforation, including those associated with previous use of NSAIDs;
gastrointestinal bleeding; other active bleeding (including suspected intracranial hemorrhage);
inflammatory bowel diseases (Crohn’s disease, ulcerative colitis) in the acute stage;
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 < 30 ml/min/1.73 m2). period after coronary artery bypass surgery; severe heart failure (III-IV class according to the NYHA classification); hemorrhagic diathesis and other blood clotting disorders; age under 18 years (due to lack of data on effectiveness and safety); pregnancy and breastfeeding period.

With caution

Peptic ulcer of the stomach and duodenum, ulcerative colitis, Crohn’s disease, 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, weakened patients and low body weight), bronchial asthma, simultaneous use of glucocorticosteroids (including prednisolone), 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 disease, smoking, Helicobacter pylori infection, systemic lupus erythematosus (SLE) and other systemic connective tissue diseases, long-term use of non-steroidal anti-inflammatory drugs, tuberculosis, severe osteoporosis, alcoholism, severe somatic diseases.

Side Effects

Possible side effects are listed in accordance with 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 (< 1/10000), including some messages.

Blood and lymphatic system disorders

Very rare: neutropenia, thrombocytopenia.

Immune system disorders

Rarely: laryngeal edema;

Very rare: anaphylactic reactions, including anaphylactic shock.

Nervous system disorders

Uncommon: headache, dizziness, drowsiness;

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

Mental disorders

Uncommon: insomnia, feeling of restlessness.

Hearing and labyrinth disorders

Uncommon: vertigo;

Very rare: tinnitus.

Visual disorders

Very rare: blurred vision.

Cardiovascular disorders

Uncommon: palpitations, feeling of heat, flushing of the skin;

Rarely: increased blood pressure;

Very rare: tachycardia, decreased blood pressure.

Respiratory system disorders

Rarely: bradypnea;

Very rare: bronchospasm, shortness of breath.

Gastrointestinal disorders

Common: nausea, vomiting, abdominal pain, dyspepsia, diarrhea;

Uncommon: gastritis, constipation, dry mouth, flatulence;

Rarely: erosive and ulcerative lesions of the gastrointestinal tract (GIT), bleeding from an ulcer or its perforation;

Very rare: damage to the pancreas.

Disorders of the liver and biliary tract

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

Very rare: liver damage.

Renal and urinary tract disorders

Rarely: polyuria, acute renal failure;

Very rare: nephritis or nephrotic syndrome.

Reproductive system disorders

Rarely: in women – menstrual irregularities; in men – transient dysfunction of the prostate gland with long-term use.

Musculoskeletal system disorders

Rarely: back pain.

Skin and subcutaneous tissue disorders

Uncommon: 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, photosensitivity, pruritus.

Metabolic disorders

Rarely: anorexia.

General violations

Uncommon: increased fatigue, asthenia, chills, general malaise;

Very rare: peripheral edema.

As with the use of other NSAIDs, the following side effects may develop: 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.

Undesirable combinations

With other NSAIDs, including salicylates in high doses (more than 3 g/day): simultaneous use of several NSAIDs due to a synergistic effect increases the risk of gastrointestinal bleeding and ulcers.

With anticoagulants: dexketoprofen, like other NSAIDs, may enhance the effect of anticoagulants such as warfarin due to its 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: with simultaneous use, the risk of bleeding increases (due to inhibition of platelet aggregation and damaging effects on the mucous membrane of the gastrointestinal tract). If simultaneous use is necessary, careful monitoring of the patient’s condition and regular monitoring of laboratory parameters is necessary.

With glucocorticosteroids: with simultaneous use, the risk of ulcerative lesions of the gastrointestinal tract and bleeding increases.

With lithium preparations: NSAIDs increase the concentration of lithium in the blood plasma up to toxic levels, and therefore this indicator must be monitored when used simultaneously with dexketoprofen, changing the dosage, and also after discontinuation of NSAIDs.

With methotrexate in high doses (15 mg/week or more): the hematological toxicity of methotrexate may increase due to a decrease in its renal clearance when used simultaneously with NSAIDs.

With hydantoins and sulfonamides: their toxic effects may be enhanced.

Combinations requiring caution

With diuretics, angiotensin-converting enzyme (ACE) inhibitors, aminoglycoside antibiotics, angiotensin-II receptor antagonists: simultaneous use with NSAIDs is associated with the risk of developing acute renal failure in dehydrated patients (decreased glomerular filtration rate due to decreased synthesis of prostaglandins). When used concomitantly, NSAIDs may reduce the antihypertensive effect of some drugs. When using dexketoprofen and diuretics simultaneously, it is necessary to ensure that the patient has no signs of dehydration, and also monitor renal function at the beginning of simultaneous use.

With methotrexate in low doses (less than 15 mg/week): an increase in the hematological toxicity of methotrexate is possible due to a decrease in its renal clearance during simultaneous use with NSAIDs. A blood cell count is necessary when coadministration is initiated. In the presence of even mild renal dysfunction, as well as in elderly people, careful medical supervision is necessary.

With pentoxifylline: there may be an increased risk of bleeding. Close clinical monitoring and regular checking of bleeding time (blood clotting time) is necessary.

With zidovudine: there is a risk of increased toxicity to red blood cells due to effects on reticulocytes, with the development of severe anemia one week after starting NSAID use. It is necessary to conduct a general blood test with counting the number of reticulocytes 1-2 weeks after starting NSAID therapy.

With oral hypoglycemic agents: NSAIDs may enhance the hypoglycemic effect of sulfonylureas due to the displacement of sulfonylurea from sites of binding to plasma proteins.

Combinations to consider

With beta-blockers: When used concomitantly with NSAIDs, the antihypertensive effect of beta-blockers may be reduced due to inhibition of prostaglandin synthesis.

With cyclosporine and tacrolimus: NSAIDs may increase nephrotoxicity, which is mediated by the action of renal prostaglandins. During simultaneous use, it is necessary to monitor renal function.

With thrombolytics: the risk of bleeding increases.

The risk of bleeding from the gastrointestinal tract increases when used simultaneously with serotonin reuptake inhibitors (citalopram, fluoxetine, sertraline) and anticoagulants.

With probenecid: an increase in the concentration of NSAIDs in the blood plasma is possible, which may be due to the inhibitory effect of probenecid on renal tubular secretion and/or conjugation with glucuronic acid; NSAID dose adjustment may be required.

With cardiac glycosides: simultaneous use with NSAIDs may lead to an increase in the concentration of cardiac glycosides in the blood plasma.

With mifepristone: due to the theoretical risk of changes in the effectiveness of mifepristone under the influence of prostaglandin synthesis inhibitors, NSAIDs should not be used earlier than 8-12 days after discontinuation of mifepristone.

With quinolones: data obtained from experimental studies in animals indicate a high risk of developing seizures when NSAIDs are used concomitantly with quinolones in high doses.

If it is necessary to use Dexalgin® 25 simultaneously with the above medications, you should consult your doctor.

Overdose

Symptoms: nausea, anorexia, abdominal pain, headache, dizziness, disorientation, insomnia.

Treatment: symptomatic therapy, if necessary – gastric lavage, taking activated charcoal; hemodialysis is ineffective.

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 higher than 30 oC.

Keep the medicine out of the reach of children!

Shelf life

Blister [PVC/aluminum foil] – 2 years.

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

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

Manufacturer

Laboratorios Menarini S.A., Spain