Flamadex tablets 25mg, No. 10

• Relief of pain syndrome of various origins (including postoperative, post-traumatic pain, pain in bone metastases, renal colic, algomenorrhea, sciatica, sciatica, neuralgia, toothache);

• symptomatic treatment of acute and chronic inflammatory, inflammatory-degenerative and metabolic diseases of the musculoskeletal system (including rheumatoid arthritis, osteoarthritis, spondyloarthritis: ankylosing spondylitis, reactive arthritis, psoriatic arthritis).

The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

Inside, during meals. Depending on the intensity of the pain syndrome, the recommended dose for adults is 12.5 mg (1/2 table) every 4-6 hours or 25 mg (1 table) every 8 hours.

The maximum daily dose is 75 mg.

Patients with impaired liver and / or kidney function, elderly people, therapy with FlamadexЃ should be started with lower doses. The maximum daily dose is 50 mg / day.

FlamadexЃ is not prescribed for long-term therapy, the course of drug treatment should not exceed 3-5 days.

Film-coated tablets

1 tab.

active substance: dexketoprofen trometamol 36.9 mg (in terms of dexketoprofen - 25 mg)

excipients: MCC - 181.89-183.84 mg; pregelatinized starch - 26.26 mg; sodium carboxymethyl starch (sodium starch glycolate) - 10.4 mg; magnesium stearate - 2.6-4.55 mg film shell: titanium dioxide - 2.5 mg; hypromellose (hypromellose 2910) - 2.5 mg; polydextrose - 2.5 mg; macrogol - 0.5 mg

• Hypersensitivity to dexketoprofen or other NSAIDs, or any of the excipients that make up the drug;

• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (history);

• erosive and ulcerative lesions of the gastrointestinal tract and duodenum in the acute stage;

• history of gastrointestinal bleeding, other active bleeding (including suspected intracranial bleeding), anticoagulant therapy;

• inflammatory bowel diseases (ulcerative colitis, Crohn's disease) in the acute stage;

• severe liver dysfunction (10-15 points on the Child-Pugh scale);

• moderate or severe renal dysfunction (Cl creatinine less than 30 ml / min);

• confirmed hyperkalemia;

• decompensated heart failure;

• period after coronary artery bypass grafting;

• hemophilia and other blood clotting disorders;

• progressive kidney disease;

• pregnancy;

• breastfeeding period;

• children under 18 years of age (there are no clinical data on the efficacy and safety of the drug in pediatric practice).

With care: gastric ulcer and duodenal ulcer; ulcerative colitis; Crohn's disease; history of liver disease; hepatic porphyria; chronic renal failure (Cl creatinine 30-60 ml / min); chronic heart failure I Ц II functional class according to NYHA classification; arterial hypertension; a significant decrease in the BCC (including after surgery); elderly patients (including those receiving diuretics, debilitated patients or those with low body weight); bronchial asthma; simultaneous administration of corticosteroids (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), SSRIs (including citalopram, fluoxetine, paroxetine, sertraline) , coronary heart disease; cerebrovascular diseases; dyslipidemia / hyperlipidemia; diabetes;peripheral arterial disease; smoking; presence of Helicobacter pylori infection; systemic connective tissue diseases; long-term use of NSAIDs; tuberculosis; severe osteoporosis; alcoholism, severe somatic diseases.

pharmachologic effect

Dexketoprofen trometamol is an 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 within 30 minutes after taking the drug inside, the duration of the therapeutic effect is 4-6 hours.

Pharmacokinetics

Suction

The time to reach Cmax of dexketoprofen in blood plasma after a single oral administration of the drug in a single dose is an average of 30 minutes (15-60 minutes). Simultaneous food intake slows down the absorption of dexketoprofen. AUC after single and repeated doses are similar, which indicates the absence of drug accumulation.

Distribution

Dexketoprofen is characterized by a high degree of binding to blood plasma proteins (99%). The average Vd value 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, followed by excretion by the kidneys. T1 / 2 of dexketoprofen is 1.65 hours.

Pharmacokinetics in special patient groups

Elderly people have an increase in T1 / 2 up to 48% and a decrease in the total clearance of the drug.

Side effect

From the hematopoietic system: very rarely - neutropenia, thrombocytopenia.

From the immune system: rarely - laryngeal edema; very rarely - anaphylactic reactions, including anaphylactic shock.

From the nervous system: infrequently - headache, dizziness, drowsiness; rarely - paresthesias, syncope (transient fainting).

From the side of the psyche: infrequently - insomnia, anxiety.

From the side of the organ of hearing and labyrinth disorders: infrequently - vertigo; very rarely - tinnitus.

From the side of the organ of vision: very rarely - blurred vision.

From the side of the cardiovascular system: infrequently - a feeling of palpitations, a feeling of heat, hyperemia of the skin; rarely - increased blood pressure; very rarely - tachycardia, lowering blood pressure.

From the respiratory system: rarely - bradypnea; very rarely - bronchospasm, shortness of breath.

From the gastrointestinal tract: often - nausea, vomiting, abdominal pain, dyspepsia, diarrhea; infrequently - gastritis, constipation, dry mouth, flatulence; rarely - anorexia, erosive and ulcerative lesions of the gastrointestinal tract, bleeding from an ulcer or its perforation; very rarely - damage to the pancreas.

From the liver and biliary tract: rarely - hepatitis, increased activity of liver enzymes, incl. ACT and ALT; very rarely - liver damage.

From the urinary system: rarely - polyuria, acute renal failure; very rarely - nephritis or nephrotic syndrome.

On the part of the reproductive system: rarely - in women, menstrual irregularities, in men, transient dysfunctions of the prostate gland with prolonged use.

From the musculoskeletal system: rarely - back pain.

On the part of the skin and subcutaneous tissues: infrequently - skin rash; rarely - urticaria, acne, increased sweating; very rarely - severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), angioedema of the face, allergic dermatitis, photosensitivity, pruritus.

General disorders: infrequently - increased fatigue, asthenia, chills, general malaise; very rarely - 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 diseases of the connective tissue, hematological disorders (thrombocytopenic purpura, aplastic and hemolytic anemia, in rare cases - agranulocytosis and bone hypoplasia brain).

Application during pregnancy and lactation

The use of FlamadexЃ during pregnancy and during breastfeeding is contraindicated.

Application for violations of liver function

The use of the drug is contraindicated in severe hepatic insufficiency (10-15 points on the Child-Pugh scale).

Patients with mild to moderate hepatic impairment should take the drug starting with the minimum recommended dose.

Application for impaired renal function

The use of the drug is contraindicated in chronic kidney disease: stage 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); progressive kidney disease.

With caution: chronic kidney disease, stage 2 (GFR 60Ц89 ml / min / 1.73 m2).

Application in children

The use of the drug under the age of 18 is contraindicated (due to the lack of data on efficacy and safety).

Use in elderly patients

Elderly patients (65 years and older) should take the drug starting with the minimum recommended dose.

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 gastrointestinal ulcers, in elderly patients, with an increase in the dose of NSAIDs, therefore, the use of FlamadexЃ in this category of patients should be started with the lowest recommended dose.

Patients from the categories above, as well as patients who require the simultaneous use of acetylsalicylic acid in low doses or other drugs that increase the risk of gastrointestinal complications, are advised to additionally use gastroprotective agents (misoprostol or proton pump blockers).

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

Patients with a history of gastrointestinal disorders or gastrointestinal diseases should be closely monitored. In the event of gastrointestinal bleeding or ulcerative lesions, the use of FlamadexЃ should be discontinued.

FlamadexЃ should be used with caution in patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease), since an 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 FlamadexЃ in patients who are simultaneously taking drugs that affect the hemostasis system, such as warfarin, coumarin derivatives and heparins, is not recommended.

Like other NSAIDs, FlamadexЃ can lead to an increase in the concentration of creatinine and nitrogen in the blood plasma. Like other inhibitors of prostaglandin synthesis, FlamadexЃ can 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 who are simultaneously using diuretics and in patients who may develop hypovolemia, due to an increased risk of nephrotoxicity.

As with the use of other NSAIDs, during therapy with FlamadexЃ, 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 FlamadexЃ should be discontinued.

Like other NSAIDs, dexketoprofen can mask the symptoms of infectious diseases. In case of detection of signs of infection or deterioration of health while using FlamadexЃ, 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, FlamadexЃ should be used with extreme caution. If the condition worsens, the drug 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 the development of cardiovascular diseases (arterial hypertension, hyperlipidemia, diabetes mellitus, smoking).

Care must be taken when prescribing FlamadexЃ 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 small risk of developing acute myocardial infarction or stroke. There are insufficient data to exclude the risk of these events when using dexketoprofen.

Elderly patients are especially susceptible to adverse reactions when using NSAIDs, incl. the risk of gastrointestinal bleeding and perforation, life-threatening the patient, decreased kidney, liver and heart function. When using FlamadexЃ in this category of patients, proper clinical control is required.

There is evidence of 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 manifestations of a skin rash, mucosal lesions or other signs of an allergic reaction, the patient should immediately stop using FlamadexЃ and consult a doctor.

Influence on the ability to drive vehicles and mechanisms

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

Overdose

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

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

Drug interactions

The following interactions are typical for all NSAIDs.

Undesirable combinations

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

With anticoagulants: dexketoprofen, like other NSAIDs, can enhance the effect of anticoagulants such as warfarin, due to the high degree of binding to blood plasma proteins, inhibition of platelet aggregation and damage to the gastrointestinal mucosa. If necessary, simultaneous use requires careful monitoring of the patient's condition and regular monitoring of laboratory parameters.

With heparin: with simultaneous use, the risk of bleeding increases (due to inhibition of platelet aggregation and a damaging effect on the gastrointestinal mucosa). If necessary, simultaneous use requires careful monitoring of the patient's condition and regular monitoring of laboratory parameters.

With GCS: 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, and therefore this indicator must be monitored with simultaneous use with dexketoprofen, changing the dose, and also after discontinuation of NSAIDs.

With methotrexate in high doses (15 mg / week or more): an increase in the hematological toxicity of methotrexate is possible due to a decrease in its renal clearance with the simultaneous use of NSAIDs.

With hydantoins and sulfonamides: it is possible to increase their toxic effect.

Combinations requiring caution

With diuretics, ACE inhibitors, antibiotics from the aminoglycoside group, angiotensin II receptor antagonists: simultaneous use with NSAIDs is associated with the risk of developing acute renal failure in patients with dehydration (decreased glomerular filtration due to decreased synthesis of prostaglandins). With the simultaneous use of NSAIDs, they can reduce the antihypertensive effect of some drugs. With the simultaneous use of dexketoprofen and diuretics, it is necessary to make sure that the patient does not have 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): an increase in the hematological toxicity of methotrexate is possible 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 even mild renal dysfunction, as well as in the elderly, careful medical supervision is necessary.

With pentoxifylline: the risk of bleeding may increase. Close clinical monitoring and regular checking of bleeding time (blood clotting time) is necessary.

With zidovudine: there is a risk of increased toxic effects on erythrocytes, due to exposure to reticulocytes, with the development of severe anemia a week after starting the use of NSAIDs. 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 can enhance the hypoglycemic effect of sulfonylureas due to the displacement of sulfonylureas from the sites of binding to blood plasma proteins.

Combinations to be taken into account

With beta-blockers: when used simultaneously with NSAIDs, the antihypertensive effect of beta-blockers may decrease due to inhibition of prostaglandin synthesis.

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— тромболитиками: повышаетс¤ риск развити¤ кровотечени¤.

”величиваетс¤ риск развити¤ кровотечени¤ из ? “ при одновременном применении с ингибиторами обратного захвата серотонина (циталопрам, флуоксетин, сертралин) и антикоагул¤нтами.

— пробенецидом: возможно повышение концентрации Ќѕ¬ѕ в плазме крови, что может быть обусловлено ингибирующим эффектом пробенецида на почечную тубул¤рную секрецию и/или конъюгацию с глюкуроновой кислотой; может потребоватьс¤ коррекци¤ дозы Ќѕ¬ѕ.

— сердечными гликозидами: одновременное применение с Ќѕ¬ѕ может приводить к повышению концентрации сердечных гликозидов в плазме крови.

With mifepristone: due to the theoretical risk of changes in the efficacy of mifepristone under the influence of inhibitors of prostaglandin synthesis, NSAIDs should not be used earlier than 8Ц12 days after discontinuation of mifepristone.

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

If it is necessary to simultaneously use the drug FlamadexЃ with the drugs listed above, the patient should consult a doctor.