Diclofenac-Akrikhin retard tab.prolonged.d.p.p.o. 100 mg N20 ext.
Indications for use Symptomatic treatment of diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic arthritis, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease); gouty arthritis, rheumatic soft tissue lesions, osteoarthritis of peripheral joints and spine, including with radicular syndrome, tenosynovitis , bursitis). The drug relieves or reduces pain and inflammation during the treatment period, but does not affect the progression of the disease. Pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboischialgia, post-traumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, algomenorrhea, adnexitis, proctitis, toothache. As part of complex therapy for infectious and inflammatory diseases of the ear, nose and throat with severe pain (pharyngitis, tonsillitis, otitis media). Contraindications - Hypersensitivity to the active substance (including other NSAIDs) or auxiliary components; — Anamnestic data on an attack of bronchial obstruction, rhinitis, urticaria after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, nasal polyps, asthma); — Erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding; - Inflammatory bowel diseases (ulcerative colitis, Crohn's disease) in the acute phase; — The period after coronary artery bypass surgery; — III trimester of pregnancy, breastfeeding period; — Decompensated heart failure; — Hematopoietic disorders, hemostasis disorders (including hemophilia); — Severe liver failure or active liver disease; — Severe renal failure (creatinine clearance less than 30 ml/min); progressive kidney diseases, incl. confirmed hyperkalemia; - Children under 15 years of age - for tablets of 50 mg and up to 18 years of age - for tablets of 100 mg; — Patients with rare hereditary diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption are contraindicated to take the drug (50 mg tablets).
With caution Anemia, bronchial asthma, cerebrovascular diseases, coronary heart disease, congestive heart failure, arterial hypertension, peripheral arterial disease, edema syndrome, liver or renal failure (creatinine clearance less than 60 ml/min), dyslipidemia/hyperlipidemia, diabetes mellitus, smoking , inflammatory bowel diseases, condition after major surgical interventions, inducible porphyria. diverticulitis, systemic connective tissue diseases, pregnancy I–II trimester. Anamnestic data on the development of peptic ulcer disease of the gastrointestinal tract, the presence of Helicobacter pylori infection, old age, long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases. Concomitant therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).
Diclofenac retard-Akrikhin
Registration number: P N002242/01 Trade name: Diclofenac Retard-Akrikhin
International nonproprietary name (INN): diclofenac
Dosage form: extended-release, film-coated tablets
Compound. One tablet contains: active substance: diclofenac sodium in terms of 100% substance - 100 mg, excipients: ludipress LCE [lactose monohydrate 94.7-98.3%, povidone 3-4%], hypromellose (hydroxypropyl methylcellulose), microcrystalline cellulose , magnesium stearate, colloidal silicon dioxide (Aerosil 200), stearic acid. Shell composition: hypromellose (hydroxypropyl methylcellulose), macrogol (polyethylene glycol 6000), glycerol (glycerin), talc, titanium dioxide, red iron oxide dye.
Description: Film-coated tablets of light brown or pinkish-brown color, round, biconvex. Roughness is allowed. On the break, the tablet is white with a creamy or yellowish tint.
Pharmacotherapeutic group Non-steroidal anti-inflammatory drug (NSAID)
ATX code: М01АВ05
Pharmacological action Pharmacodynamics Non-steroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid. It has anti-inflammatory, analgesic, antipyretic and antiplatelet effects. By indiscriminately inhibiting cycloxygenases 1 and 2, it disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins (Pg) at the site of inflammation, and suppresses the exudative and proliferative phases of inflammation. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac helps to significantly reduce the severity of pain, morning stiffness, and swelling of the joints, which improves the condition of the joint.
For injuries, in the postoperative period, diclofenac reduces pain and inflammatory swelling.
Pharmacokinetics Absorption is rapid and complete, food slows the rate of absorption. Plasma concentration is linearly dependent on the administered dose.
There are no changes in the pharmacokinetics of diclofenac following repeated administration.
Does not accumulate if the recommended interval between doses is observed.
As a result of the delayed release of the active substance, the maximum plasma concentration is lower than that obtained with the administration of a short-acting drug, but it remains high for a long time after administration. The maximum concentration is 0.5-1 mcg/ml, the time to reach the maximum concentration is 5 hours after taking 100 mg of extended-release tablets. Bioavailability - 50%. Communication with plasma proteins is more than 99% (most of it is associated with albumin). Penetrates into synovial fluid, the maximum concentration in synovial fluid is observed 2-4 hours later than in plasma. The half-life from synovial fluid is 3-6 hours (concentrations of the active substance in synovial fluid 4-6 hours after administration of the drug are higher than in plasma, and remain higher for another 12 hours).
Metabolism: 50% of the active substance is metabolized during the “first pass” through the liver. Metabolism occurs as a result of multiple or single hydroxylation and conjugation with glucuronic acid. The CYP2C9 isoenzyme is also involved in the metabolism of diclofenac. The pharmacological activity of the metabolites is lower than that of diclofenac.
Systemic clearance is 260 ml/min. The half-life from plasma is 1-2 hours. 60% of the administered dose is excreted in the form of metabolites through the kidneys, less than 1% is excreted unchanged, the rest of the dose is excreted in the form of metabolites in the bile. In patients with severe renal impairment, the excretion of metabolites in bile increases, but no increase in their concentration in the blood is observed. In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetic parameters are the same as in patients without liver disease.
Indications for use: Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic arthritis, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), gouty arthritis (in case of an acute attack of gout, fast-acting dosage forms are preferred), rheumatic lesions of soft tissues, peripheral osteoarthritis joints and spine, including those with radicular syndrome, tenosynovitis, bursitis. The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and does not affect the progression of the disease.
Pain syndrome of mild or moderate severity: lumbago, sciatica, neuralgia, myalgia, post-traumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, toothache, algodismenorrhea, adnexitis, proctitis.
As part of complex therapy for infectious and inflammatory diseases of the ENT organs with severe pain syndrome (pharyngitis, tonsillitis, otitis).
Contraindications: • hypersensitivity to the active substance (including other NSAIDs) or excipients, • complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including including a history), •erosive and ulcerative lesions of the gastric or duodenal mucosa, active gastrointestinal bleeding, •inflammatory bowel diseases (ulcerative colitis, Crohn's disease) in the acute phase, •the period after coronary artery bypass surgery, •III trimester pregnancy, lactation, • decompensated heart failure, • hematopoietic disorders, hemostasis disorders (including hemophilia), • severe liver failure or active liver disease, • severe renal failure (creatinine clearance less than 30 ml/min), progressive diseases kidneys, confirmed hyperkalemia, • children under 18 years of age, • hereditary lactose intolerance, impaired absorption of glucose-galactose, lactase deficiency.
Carefully. Anemia, bronchial asthma, cerebrovascular diseases, coronary heart disease, chronic heart failure, arterial hypertension, peripheral arterial diseases, edema syndrome, liver and kidney failure (creatinine clearance 30-60 ml/min), dyslipidemia/hyperlipidemia, diabetes mellitus, smoking, inflammatory bowel diseases, conditions after major surgical interventions, inducible porphyria, diverticulitis, systemic connective tissue diseases, pregnancy I-II trimester. Anamnestic data on the development of peptic ulcer disease of the gastrointestinal tract, the presence of Helicobacter pylori infection, old age, long-term use of NSAIDs, alcoholism, severe somatic diseases.
Concomitant use of glucocorticosteroids (for example, prednisolone), anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).
Method of administration and dose. Orally, without chewing, during or after meals, with a small amount of water. Adults - 100 mg 1 time per day. For algodismenorrhea and migraine attacks - up to 200 mg/day for no more than 1-2 days. When taking 100 mg of extended-release tablets, if it is necessary to increase the daily dose to 150 mg/day, you can additionally take 1 regular tablet (50 mg). The maximum daily dose is 150 mg.
Side effect. Often -1-10%, sometimes -0.1-1%, rarely - 0.01-0.1%, very rarely - less than 0.001%, including individual cases. From the digestive system: often - epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased aminotransferase activity, rarely - gastritis, proctitis, bleeding from the gastrointestinal tract (vomiting of blood, melena, diarrhea mixed with blood), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, impaired liver function, very rarely - stomatitis, glossitis, esophagitis, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, pancreatitis, fulminant hepatitis
From the nervous system: often - headache, dizziness, rarely - drowsiness, very rarely - sensory disturbances (including paresthesia), memory disorders, tremor, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia , night “nightmares”, irritability, mental disorders.
From the senses: often - vertigo, very rarely - visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, impaired taste.
From the urinary system: very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.
From the hematopoietic organs: very rarely - thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis.
Allergic reactions: anaphylactic/anaphylactoid reactions, including a marked decrease in blood pressure and shock, very rarely - angioedema (including facial edema).
From the cardiovascular system: very rarely - palpitations, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.
From the respiratory system: rarely - exacerbation of bronchial asthma (including shortness of breath), very rarely - pneumonia.
From the skin: often - skin rash, rarely - urticaria, very rarely - bullous rashes, erythema, incl. multiforme and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.
Overdose Symptoms: vomiting, bleeding from the gastrointestinal tract, epigastric pain, diarrhea, dizziness, tinnitus, convulsions, increased blood pressure (BP), respiratory depression, in case of significant overdose - acute renal failure, hepatotoxic effect. Treatment: gastric lavage, administration of activated carbon, symptomatic therapy aimed at eliminating increased blood pressure, renal dysfunction, convulsions, gastrointestinal irritation, respiratory depression. Forced diuresis and hemodialysis are ineffective (due to the significant connection with proteins and intensive metabolism).
Interaction with other drugs •Increases plasma concentrations of digoxin, methotrexate, lithium and cyclosporine. •Reduces the effect of diuretics; against the background of potassium-sparing diuretics, the risk of hyperkalemia increases; against the background of anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) - the risk of bleeding (usually from the gastrointestinal tract). •Reduces the effects of antihypertensive and hypnotic drugs. •Increases the likelihood of side effects of other NSAIDs and glucocorticosteroids (gastrointestinal bleeding), methotrexate toxicity and cyclosporine nephrotoxicity. •Acetylsalicylic acid reduces the concentration of diclofenac in the blood. •Paracetamol increases the risk of developing nephrotoxic effects of diclofenac. •Reduces the effect of hypoglycemic drugs. •Cefamandole, cefaperazone, cefotetan, valproic acid and plicamycin increase the incidence of hypoprothrombinemia. •Cyclosporine and gold preparations increase the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which increases nephrotoxicity. • Simultaneous use with ethanol, colchicine, corticotropin, selective serotonin reuptake inhibitors and St. John's wort preparations increases the risk of bleeding in the gastrointestinal tract. •Diclofenac enhances the effect of drugs that cause photosensitivity. •Drugs that block tubular secretion increase the plasma concentration of diclofenac, thereby increasing its toxicity. •Antibacterial drugs from the quinolone group—risk of developing seizures.
Special instructions • To quickly achieve the desired therapeutic effect, take 30 minutes before meals. In other cases, take before, during or after meals, without chewing, with a sufficient amount of water. •Because of the important role of prostaglandins in maintaining renal blood flow, special caution should be exercised when prescribing to patients with cardiac or renal failure, as well as when treating the elderly, taking diuretics, and patients who, for any reason, have a decrease in circulating blood volume (for example, after major surgery). If diclofenac is prescribed in such cases, monitoring of renal function is recommended as a precaution. •In patients with liver failure (chronic hepatitis, compensated cirrhosis of the liver), the kinetics and metabolism do not differ from similar processes in patients with normal liver function. When carrying out long-term therapy, it is necessary to monitor liver function, peripheral blood patterns, and stool analysis for occult blood. •Due to the negative effect on fertility, the drug is not recommended for women wishing to become pregnant. In patients with infertility (including those undergoing examination), it is recommended to discontinue the drug. •To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used for the shortest possible short course. •It is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions. •Patients taking the drug should refrain from drinking alcohol.
Release form: Long-acting, film-coated tablets, 100 mg. 10 tablets in a blister pack. 1, 2 or 3 blister packs along with instructions for use in a cardboard pack.
Storage conditions: In a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children.
Shelf life: 3 years. Do not use after the expiration date.
Conditions for dispensing from pharmacies: By prescription.
