pharmachologic effect
Diclofenac retard is a non-steroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid; has anti-inflammatory, analgesic and antipyretic effects.
By indiscriminately inhibiting cyclooxygenase 1 and 2 (COX1 and COX2), it disrupts the metabolism of arachidonic acid and reduces the amount of prostaglandins at the site of inflammation. Most effective for inflammatory pain. Like all NSAIDs, the drug has an antiplatelet effect. 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 functional state 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 by 1-4 hours and reduces the maximum concentration (Cmax) by 40%. As a result of the delayed release of the drug, Cmax in plasma is lower than that created by the administration of short-acting drugs; however, it remains high for a long time after administration. Cmax – 0.5-1.0 mcg/ml, time to reach maximum concentration in blood plasma (TCmax) – 5 hours after taking 100 mg extended-release tablets.
There are no changes in the pharmacokinetics of diclofenac following repeated administration. Does not accumulate if the recommended interval between meals is observed.
Bioavailability – 50%. Communication with plasma proteins is more than 99% (most of it is associated with albumin). Penetrates into breast milk and synovial fluid; Cmax in synovial fluid is observed 2-4 hours later than in plasma. The half-life (T1/2) from synovial fluid is 3-6 hours (concentrations of the drug in synovial fluid 4-6 hours after its administration are higher than in plasma and remain higher for another 12 hours).
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 enzyme system of cytochrome P 450 CYP2C9 takes part in the metabolism of the drug. The pharmacological activity of the metabolites is less than that of diclofenac.
Systemic clearance is 206 ml/min. T1/2 from plasma - 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 as metabolites in the bile.
In patients with severe renal failure (creatinine clearance (CC) less than 10 ml/min), 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, pharmacokinetic parameters do not change.
Diclofenac passes into breast milk.
Diclofenac-Akrikhin retard tablets 100 mg No. 20
A country
Russia
The country of production may vary depending on the batch of goods. Please check with the operator for detailed information when confirming your order.
Active substance
Diclofenac
Compound
1 tablet contains: diclofenac sodium 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. Extended-release tablets, film-coated, light brown or pinkish-brown in color, round, biconvex. Roughness is allowed. On the fracture it is white with a creamy or yellowish tint.
pharmachologic effect
Nonsteroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid. It has anti-inflammatory, analgesic, antipyretic and antiplatelet effects. By indiscriminately inhibiting COX-1 and COX-2, it disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in 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.
Indications for use
Inflammatory and degenerative diseases of the musculoskeletal system: - rheumatoid arthritis; - psoriatic arthritis; - juvenile chronic arthritis; - ankylosing spondylitis (ankylosing spondylitis); - gouty arthritis (in case of an acute attack of gout, fast-acting dosage forms are preferred); - rheumatic lesions of soft tissues; — osteoarthritis of peripheral joints and spine, incl. with radicular syndrome; - tendovaginitis, 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: - pharyngitis; - tonsillitis; - otitis media
Side effects
Determination of the frequency of adverse reactions: - often - 1-10%; - sometimes - 0.1-1%; - rarely - 0.01-0.1%; - very rare - less than 0.001%, including isolated 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 with 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, nightmares, irritability, mental disorders. From the senses: - often - vertigo; - very rarely - visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, impaired sense of 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 allastic anemia, agranulocytosis. 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 - pneumonitis. From the skin: - often - skin rash; - very rarely - erythema, bullous rashes, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic. Allergic reactions: - anaphylactic/anaphylactoid reactions, including a pronounced decrease in blood pressure and shock; - rarely - urticaria; - very rarely - erythema multiforme and Stevens-Johnson syndrome, Lyell's syndrome, angioedema (including the face).
Contraindications
- 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 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 grafting; - 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; - confirmed hyperkalemia; — III trimester of pregnancy; - lactation period; - children and adolescents up to 18 years of age; - hereditary lactose intolerance, impaired absorption of glucose-galactose, lactase deficiency; - hypersensitivity to the active substance (including other NSAIDs) or excipients. With caution Anemia, bronchial asthma, cerebrovascular diseases, coronary artery disease, chronic heart failure, arterial hypertension, peripheral arterial disease, edema syndrome, liver and kidney failure (creatinine clearance 30-60 ml/min), dyslipidemia/hyperlipidemia, diabetes mellitus, inflammatory bowel disease , conditions after extensive surgery, inducible porphyria, diverticulitis, systemic connective tissue diseases, anamnestic data on the development of gastrointestinal ulcers, the presence of Helicobacter pylori infection, long-term use of NSAIDs, alcoholism, severe somatic diseases, concomitant use of corticosteroids (for example, prednisolone), anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline), smoking, I and II trimesters of pregnancy, old age. Use during pregnancy and breastfeeding The use of the drug in the third trimester of pregnancy and lactation is contraindicated. The drug should be prescribed with caution in the first and second trimesters of pregnancy.
Use in children The use of the drug in children and adolescents under 18 years of age is contraindicated.
Use in elderly patients The drug should be prescribed to elderly patients with caution.
Mode of application
The drug is taken orally, during or after meals. The tablets should be swallowed without chewing and washed down with a small amount of water. Adults are prescribed 100 mg 1 time/day. For algodismenorrhea and migraine attacks - up to 200 mg/day for no more than 1-2 days. When taking 100 mg extended-release tablets, if you need 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.
special instructions
To quickly achieve the desired therapeutic effect, it is recommended to take the drug 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 heart or renal failure, as well as when treating the elderly, taking diuretics, and patients who, for any reason, have a decrease in 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 drug should be used in the minimum effective dose for the shortest possible short course. Patients taking the drug must refrain from drinking alcohol. Impact on the ability to drive vehicles and operate machinery It is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Overdose
Symptoms: vomiting, bleeding from the gastrointestinal tract, epigastric pain, diarrhea, dizziness, tinnitus, convulsions, increased blood pressure, respiratory depression, in case of significant overdose - acute renal failure, hepatotoxic effect. Treatment: - gastric lavage, administration of activated carbon; - carrying out symptomatic therapy aimed at eliminating arterial hypertension, renal dysfunction, seizures, gastrointestinal irritation, respiratory depression. Forced diuresis and hemodialysis are ineffective (due to a significant degree of protein binding and intensive metabolism).
Interaction with other drugs
Diclofenac increases plasma concentrations of digoxin, methotrexate, lithium and cyclosporine. Diclofenac reduces the effect of diuretics. With the simultaneous use of potassium-sparing diuretics, the risk of hyperkalemia increases. With the simultaneous use of anticoagulants and thrombolytic agents (alteplase, streptokinase, urokinase), the risk of bleeding increases (usually from the gastrointestinal tract). Diclofenac reduces the effects of antihypertensive and hypnotic drugs. Diclofenac increases the likelihood of side effects of other NSAIDs and GCS (gastrointestinal bleeding), the toxicity of methotrexate and the nephrotoxicity of cyclosporine. Acetylsalicylic acid reduces the concentration of diclofenac in the blood. Paracetamol increases the risk of developing nephrotoxic effects of diclofenac. 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. Concomitant 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. When used simultaneously with diclofenac, antibacterial drugs from the quinolone group increase the risk of developing seizures.
Dispensing conditions in pharmacies
On prescription
Indications for use
- Diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, 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).
- 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).
- The drug Diclofenac retard is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and does not affect the progression of the disease.
