Dexonal - instructions for use, doses, side effects, contraindications

Excipients: microcrystalline cellulose, corn starch, carboxymethyl starch sodium (sodium starch glycolate), silicon dioxide colloidal anhydrous (aerosil), magnesium stearate;

excipients for the shell: hypromellose (hydroxypropylmethylcellulose), macrogol 6000 (polyethylene glycol 6000), titanium dioxide.

Description:Round biconvex tablets covered with a film coat of white or almost white color, with a risk. On the cross section, the nucleus is white or almost white in color.

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

ATX: & nbsp

M.01.A.E Propionic acid derivatives

M.01.A.E.17 Dexketoprofen

Pharmacodynamics:

Dexketoprofen trometamol, the active substance of the drug Dexonal®, refers to non-steroidal anti-inflammatory drugs (NSAIDs), which exerts an analgesic, anti-inflammatory and antipyretic effect. The mechanism of action of dexketoprofen is based on inhibiting the synthesis of prostaglandins at the level of cyclooxygenases (COX-1 and COX-2).

The analgesic effect occurs 30 minutes after the administration of the drug Dexonal® inside, the duration of the therapeutic action reaches 4-6 hours.

Pharmacokinetics:

Suction. The time to reach the maximum concentration (TC_m_Oh) Dexketoprofen in the blood plasma after a single dose is an average of 30 minutes (15 - 60 minutes). Simultaneous food intake slows down the absorption of dexketoprofen. The area under the concentration-time curve (AUC) after a single and repeated procedures are similar, which indicates the absence of cumulation of the drug.

Distribution. Dexketoprofen is characterized by a high degree of binding to plasma proteins (99%). Average distribution volume (Vd) is less than 0.25 l / kg, the half-distribution period is about 0.35 h.

Metabolism and excretion. The main way of metabolism of dexketoprofen is its conjugation with glucuronic acid, followed by excretion by the kidneys. The half-life period (T1 / 2) of dexketoprofen is 1.65 hours. In elderly people, the half-life is prolonged to 48%, and the overall clearance of the drug decreases.

Indications:

Musculoskeletal pain (mild or moderately severe), algodismenorea, toothache.

The drug is intended for symptomatic treatment, reducing pain and inflammation at the time of application.

Contraindications:

- Hypersensitivity to dexketoprofen, other components of the drug and other NSAIDs;

- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis);

- erosive-ulcerative lesions of the gastrointestinal tract in the stage of exacerbation;

- gastrointestinal hemorrhages or perforations in the anamnesis, including those associated with prior NSAID administration;

- gastrointestinal bleeding; other active bleeding (including a suspicion of intracranial hemorrhage);

- Inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute stage;

- Hepatic insufficiency of severe severity (10-15 points on the Child-Pugh scale);

- progressive kidney disease, confirmed hyperkalemia;

- chronic kidney disease: stage 3a (glomerular filtration rate (GFR) 45-55 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 aortocoronary shunting;

- severe heart failure (III -IV class by classification NYHA);

- hemorrhagic diathesis and other disorders of blood coagulation;

- age under 18 years (due to lack of data on efficiency and safety);

- Pregnancy and the period of breastfeeding.

Carefully:

Stomach and duodenal ulcer, ulcerative colitis, Crohn's disease, liver disease in history, hepatic porphyria, chronic kidney disease, stage 2 (GFR 60-89 ml / min / 1.73 m²), chronic heart failure, arterial hypertension, a significant decrease in the volume of circulating blood (including after surgery), elderly patients over 65 years of age (incl.weakened patients and patients with low body weight), bronchial asthma, simultaneous reception of glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiaggregants (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, infection Helicobacter pylori, systemic lupus erythematosus (SLE) and other systemic diseases of connective tissue, long-term use of non-steroidal anti-inflammatory drugs, tuberculosis, severe osteoporosis, alcoholism, severe somatic diseases.

Pregnancy and lactation:

The use of the drug Dexonal ® during pregnancy and during breastfeeding is contraindicated.

Dosing and Administration:

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

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

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

Patients with hepatic insufficiency

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

The use of the drug 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 with the minimum recommended dose. The maximum daily dose is 50 mg. The 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 <30 ml / min / 1.73 m²) is contraindicated.

Side effects:

Possible side effects are given in accordance with the classification of the World Health Organization below the descending frequency of occurrence: very often (≥1 / 10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10000, <1/1000); very rarely (<1/10000), including individual messages.

On the part of the blood and lymphatic system

Rarely: neutropenia, thrombocytopenia.

From the immune system

Rarely: swelling of the larynx.

Rarely: anaphylactic reactions, including anaphylactic shock.

From the nervous system

Infrequently: headache, dizziness, drowsiness.

Rarely: paresthesia, syncopal conditions (transient brief syncope).

From the side of the psyche

Infrequently: insomnia, a feeling of anxiety.

From the side of the hearing organ and labyrinthine disorders

Infrequently: Vertigo.

Rarely: noise in ears.

From the side of the organ of vision

Rarely: blurred vision.

From the side of the cardiovascular system

Infrequently: feeling of palpitation, a feeling of heat, hyperemia of the skin.

Rarely: increase in blood pressure.

Rarely: tachycardia, lowering blood pressure.

From the respiratory system

Rarely: bradypnoe.

Rarely: bronchospasm, shortness of breath.

From the gastrointestinal tract

Often: nausea, vomiting, abdominal pain, indigestion, diarrhea.

Infrequently: gastritis, constipation, dry mouth, flatulence.

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

Rarely: defeat of the pancreas.

From the liver and biliary tract

Rarely: hepatitis, increased activity of "liver" enzymes (ACT and ALT).

Rarely: liver damage.

From the side of the kidneys and urinary tract

Rarely: polyuria, acute renal failure.

Rarely: nephritis or nephrotic syndrome.

From the side of the reproductive system

Rarely: in women - a menstrual cycle, in men - transient dysfunction of the prostate gland with prolonged use.

From the side of the musculoskeletal system

Rarely: backache.

From the skin and subcutaneous tissues:

Infrequently: skin rash.

Rarely: urticaria, acne, increased sweating.

Rarely: severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome)), angioedema, facial edema, allergic dermatitis, photosensitivity, skin itching.

From the side of metabolism:

Rarely: anorexia.

Common violations:

Infrequently: increased fatigue, asthenia, chills, general malaise.

Rarely: peripheral edema.

As with other NSAIDs, the following side effects may develop: aseptic meningitis, which develops mainly in patients with systemic lupus erythematosus or systemic connective tissue diseases, hematologic disorders (thrombocytopenic purpura, aplastic and hemolytic anemia, in rare cases, agranulocytosis and bone marrow hypoplasia).

Overdose:

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

Treatment: symptomatic therapy, if necessary - gastric lavage, reception of activated charcoal, hemodialysis is ineffective.

Interaction:

The following interactions are typical for all NSAIDs.

Unwanted combinations

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

With anticoagulants: dexketoprofen, like other NSAIDs, can enhance the effect of anticoagulants, such as warfarin in connection with the high degree of binding to blood plasma proteins, inhibition of platelet aggregation and damage to the mucous membrane of the gastrointestinal tract. In the case of the need for simultaneous use, careful monitoring of the patient's condition and regular monitoring of laboratory parameters are necessary.

FROM heparin: with simultaneous use increases the risk of bleeding (due to the inhibition of platelet aggregation and damage to the mucosa of the gastrointestinal tract). In the case of the need for simultaneous use, careful monitoring of the patient's condition and regular monitoring of laboratory parameters are necessary.

With glucocorticosteroids: With simultaneous application, the risk is increased ulcerative lesions of the gastrointestinal tract and bleeding.

With lithium preparations: NSAIDs increase the concentration of lithium in the blood plasma down to toxic in connection, which should be monitored when used with dexketoprofen, dosage changes, and after the abolition 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 with simultaneous application with NSAIDs.

With hydantoins and sulfonamides: it is possible to intensify their toxic effects.

Combinations, requiring caution

With diuretics, angiotensin-converting enzyme (ACE) inhibitors, antibiotics from the aminoglycoside group, angiotensin II receptor antagonists: concurrent use with NSAIDs is associated with a risk of developing acute renal failure in dehydrated patients (reduced glomerular filtration due to reduced synthesis of prostaglandins). With the simultaneous use of NSAIDs can reduce the antihypertensive effect of certain drugs. With the simultaneous use of dexketoprofen and diuretics, it is necessary to make sure that the patient does not show signs of dehydration,and also in the beginning of simultaneous application to control the function of the kidneys.

With methotrexate in low doses (less than 15 mg / week): possibly increasing hematological toxicity of methotrexate in connection with a decrease in its renal clearance against the background of simultaneous use with NSAIDs. It is necessary to count the blood cells at the beginning of the simultaneous application. In the presence of a violation of kidney function, even in mild cases, as well as in the elderly, careful medical supervision is necessary.

With pentoxifylline: possibly increased risk of bleeding. A thorough clinical monitoring and regular checking of bleeding time (blood clotting time) is necessary.

With zidovudinom: there is a risk of increasing the toxic effect on erythrocytes due to exposure to reticulocytes, with the development of severe anemia a week after the initiation of NSAID use. It is necessary to conduct a general blood test with counting the number of reticulocytes 1-2 weeks after the initiation of therapy with NSAIDs.

With oral hypoglycemic agents: NSAIDs can enhance hypoglycemic effect of sulfonylurea preparations due to displacementSulfonylureas from binding sites with plasma proteins.

Combinations that need to be taken into account

FROM βadrenoblockers: when used simultaneously with NSAIDs, the antihypertensive effect may decrease βadrenoblockers due to inhibition of prostaglandin synthesis.

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

With thrombolytics: increased risk of bleeding.

The risk of bleeding from the gastrointestinal tract increases with simultaneous use 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; may need to adjust the dose of NSAIDs.

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

FROM mifepristone: in connection with the theoretical risk of changing the effectiveness of mifepristone under the influence of inhibitors of prostaglandin synthesis, NSAIDs should not be used earlier than 8-12 days after the withdrawal of mifepristone.

With quinolones: the data obtained in experimental studies on animals indicate a high risk of seizures when using NSAIDs with quinolones in high doses.

If it is necessary to simultaneously use the drug Dexonal® with the above medicines, you should consult your doctor.

Special instructions:

Unwanted side effects can be minimized by using the drug at the lowest effective dose with the minimum duration of application necessary to relieve the pain syndrome.

The risk of complications from the gastrointestinal tract is increased in patients with peptic ulcer disease in the anamnesis, in elderly patients, with an increase in the dose of NSAIDs; so the use of the drug in this category of patients should start with the lowest recommended dose.

Patients in 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 complications from the gastrointestinal tract,recommended additional use of gastroprotectors (misoprostol or proton pump blockers).

In patients who simultaneously take antiplatelet or anticoagulants, glucocorticosteroids also increase the risk of gastrointestinal bleeding.

Patients with gastrointestinal disorders or gastrointestinal diseases in a history should be under close medical supervision. In case of gastrointestinal bleeding or ulcerative lesion, the drug should be discontinued.

The drug should be used with caution in patients with gastrointestinal ailments in history (ulcerative colitis, Crohn's disease), as possible exacerbation of these diseases.

All NSAIDs can inhibit platelet aggregation and increase bleeding time by inhibiting the synthesis of prostaglandins. In this regard, the use of the drug Dexonal ® in patients who simultaneously take drugs that affect the hemostasis system, such as warfarin, coumarin derivatives and heparins, is not recommended.

Like other NSAIDs, the drug Dexonal® can lead to an increase in the concentration of creatinine and nitrogen in the blood plasma.Like other inhibitors of prostaglandin synthesis, the drug Dexonal® can have a side effect on the urinary system, which can lead to the development of glomerulonephritis, interstitial nephritis, papillary necrosis, nephrotic syndrome, and acute renal failure. Care should be taken when using the drug in patients who simultaneously use diuretics and patients who may develop hypovolemia, due to the increased risk of nephrotoxicity.

As with the use of other NSAIDs, against the background of the use of the drug Dexonal ® there may be a slight transient increase in some "hepatic" enzymes. Elderly people need to monitor liver and kidney function. In the case of a significant increase in the relevant indicators, the use of the pre-order Dexonal® should be discontinued.

Like other NSAIDs, dexketoprofen can mask the symptoms of infectious diseases. In case of signs of infection or deterioration of well-being against the background of the use of the drug Dexonal®, the patient should immediately consult a doctor.The drug can cause fluid retention in the body, so in patients with hypertension, with 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, ischemic heart 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 (hypertension, hyperlipidemia, diabetes, smoking).

Caution should be exercised in prescribing patients with a history of cardiovascular disease, especially in patients with heart failure, because of the possible risk of progression.

Clinical studies and epidemiological data suggest that NSAIDs, especially in high doses and with long-term use, can lead to an insignificant risk of developing acute myocardial infarction or stroke.To exclude the risk of these events, the use of dexketoprofen does not suffice.

Elderly patients are particularly susceptible to adverse reactions with NSAIDs, including the risk of gastrointestinal bleeding and perforation, life-threatening patients, impaired renal, hepatic and cardiac function. When using the drug Dexonal in this category of patients requires proper clinical control.

There are data on the occurrence of rare cases of skin reactions (such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) in the application of NSAIDs. At the first manifestations of skin rash, lesions of mucous membranes or other signs of an allergic reaction, taking the drug Dexonal® should be stopped immediately and consult a doctor.

Effect on the ability to drive transp. cf. and fur:

In connection with the possible occurrence of dizziness and drowsiness during the period of taking the drug, the ability to concentrate and speed of psychomotor reactions in patients may decline, especially in the first hour after admission. Therefore, during the period of drug use, care should be taken when driving vehicles and engaging in potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Film-coated tablets, 25 mg.

Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 1, 3, 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

Blister (PVC / aluminum foil).

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use the product after the expiration date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-003762

Date of registration:29.07.2016 / 16.01.2017

Expiration Date:29.07.2021

The owner of the registration certificate:OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Manufacturer: & nbsp

OBOLENSKOE PHARMACEUTICAL ENTERPRISE, CJSC Russia

Information update date: & nbsp15.03.2018

Illustrated instructions

Instructions

Dexonal® (Dexonal)