Diclofenac retard-Akrikhin
Diclofenac retard-Akrikhin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Diclofenac retard-Akrikhin
ATX code: M01AB05
Active ingredient: diclofenac (Diclofenac)
Manufacturer: JSC "AKRIKHIN" (Russia)
Description and photo update: 2020-09-07
Prices in pharmacies: from 38 rubles.
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Diclofenac retard-Akrikhin is a non-steroidal anti-inflammatory drug (NSAID) that has anti-inflammatory, analgesic, antipyretic and antiplatelet effects.
Release form and composition
The drug is produced in the form of tablets of prolonged action, film-coated: biconvex, round, surface roughness is possible, the core of the tablet is white with a cream or yellow tint, the film shell is pinkish-brown or light brown (10 pcs. In blisters, in a cardboard box 1, 2 or 3 packages and instructions for the use of Diclofenac retard-Akrikhin).
1 tablet contains:
- active substance: diclofenac sodium - 100 mg;
- auxiliary components: ludipress LCE (lactose monohydrate 94.7-98.3%, povidone 3-4%), microcrystalline cellulose, hydroxypropyl methylcellulose (hypromellose), Aerosil 200 (colloidal silicon dioxide), magnesium stearate, stearic acid;
- film shell: glycerol (glycerin), hypromellose (hydroxypropyl methylcellulose), titanium dioxide, macrogol (polyethylene glycol 6000), dye iron oxide red, talc.
Pharmacological properties
Pharmacodynamics
Diclofenac retard-Akrikhin is a non-steroidal anti-inflammatory drug that has anti-inflammatory, analgesic, antipyretic and antiplatelet effects. Its active ingredient, diclofenac, is a phenylacetic acid derivative that suppresses the exudative and proliferative phase of inflammation. The mechanism of action is due to the property of diclofenac to non-selectively inhibit cyclooxygenases 1 and 2, disrupt the metabolism of arachidonic acid and reduce the amount of prostaglandins in the focus of inflammation.
Taking the drug for rheumatic diseases helps to improve the condition of the joint. The anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain syndrome, morning stiffness and swelling of the joints.
The use of diclofenac in the postoperative period or with injuries provides a decrease in inflammatory edema and a decrease in pain.
Pharmacokinetics
After oral administration, diclofenac is rapidly absorbed in full. Simultaneous food intake slows down the rate of absorption. The maximum concentration (C max) in blood plasma is reached within about 5 hours and is 0.5–1 μg / ml.
The bioavailability of the active substance is 50%. As a result of the sustained release of diclofenac, the C max in plasma is lower than that achieved by taking a short-acting dosage form, but after taking a single dose of sustained-release tablets, it remains high for a longer period. The concentration of the active substance in the plasma is linearly dependent on the dose taken. Against the background of repeated administration, the pharmacokinetics of diclofenac does not change. Subject to the recommended dosage regimen, the drug does not cumulate.
Plasma protein binding (mainly albumin) - more than 99%.
Diclofenac penetrates into the synovial fluid, where its maximum concentration is reached 2–4 hours later than in plasma. The level of the active substance in the synovial fluid 4-6 hours after taking the pill and over the next 12 hours is higher than in plasma. The half-life (T 1/2) from the synovial fluid is 3-6 hours.
Diclofenac is metabolized in the process of multiple or single hydroxylation and conjugation with glucuronic acid, with the participation of the isoenzyme CYP2C9, with the formation of metabolites, the pharmacological activity of which is lower than that of diclofenac. Up to 50% of the dose taken undergoes biotransformation during the first passage through the liver.
The systemic clearance of the drug is 260 ml / min, T 1/2 from plasma is 1–2 hours.
The substance is excreted through the kidneys in the form of metabolites up to 60% of the received dose and less than 1% - unchanged. The rest of the drug is excreted as metabolites through the intestines
With pronounced impairment of renal function, there is no increase in the concentration of metabolites in the blood. In this category of patients, the proportion of metabolites excreted from the body with bile increases.
In chronic hepatitis or compensated cirrhosis of the liver, the pharmacokinetic parameters of the drug do not change.
Indications for use
The use of Diclofenac retard-Akrikhin is indicated for symptomatic therapy, reduction of pain and inflammation at the time of use for the following diseases and conditions:
- degenerative diseases and inflammatory processes of the musculoskeletal system: osteoarthritis, rheumatoid arthritis, tendovaginitis, bursitis, ankylosing spondylitis and other spondyloarthropathies;
- spinal diseases accompanied by pain syndrome: arthralgia, neuralgia, myalgia, sciatica, lumbago, ossalgia, radiculitis;
- post-traumatic and postoperative pain syndromes accompanied by inflammatory processes (in dentistry, in orthopedics, etc.);
- algodismenorrhea; inflammation in the small pelvis, including adnexitis.
Diclofenac retard-Akrikhin has no effect on the progression of the disease.
Contraindications
Absolute:
- gastrointestinal bleeding in the active phase, erosive and ulcerative disorders of the mucous membrane of the stomach or duodenum;
- exacerbation of inflammatory bowel diseases (Crohn's disease, ulcerative colitis);
- complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including history);
- hemophilia and other hemostasis disorders, hematopoiesis disorders;
- decompensated heart failure;
- period after coronary artery bypass grafting;
- severe liver failure, active liver disease;
- progressive kidney disease, severe renal failure with creatinine clearance (CC) less than 30 ml / min, confirmed hyperkalemia;
- impaired absorption of glucose-galactose, hereditary lactose intolerance, lactase deficiency;
- III trimester of pregnancy;
- breast-feeding;
- age up to 18 years;
- hypersensitivity to other NSAIDs or drug components.
It is recommended to prescribe Diclofenac retard-Akrikhin tablets with caution for ischemic heart disease, chronic heart failure, arterial hypertension, cerebrovascular pathologies, peripheral arterial diseases, dyslipidemia or hyperlipidemia, anemia, edema syndrome, bronchial asthma, liver failure, renal failure (CC ml / min), diabetes mellitus, inflammatory bowel diseases, a history of gastrointestinal (GI) ulcers, conditions after extensive surgery, diverticulitis, induced porphyria, systemic connective tissue diseases, Helicobacter pylori infection, smoking, alcoholism, severe somatic diseases, long-term use of NSAIDs, in the I and II trimesters of pregnancy, in old age.
In addition, caution should be exercised if it is necessary to combine Diclofenac retard-Akrikhin with prednisolone and other glucocorticosteroids (GCS), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel) or selective serotralin reuptake inhibitors, including phytalotonin paroxetine).
Diclofenac retard-Akrikhin, instructions for use: method and dosage
Diclofenac retard-Akrikhin tablets are taken orally, during or immediately after a meal, swallowing whole (without violating the integrity of the film shell) and drinking plenty of water.
For adult patients, it is recommended to take 1 extended-release tablet (100 mg) once a day.
For the treatment of migraine attacks and algodismenorrhea, the drug is taken 1 time per day at a dose of up to 150 mg. If it is necessary to use diclofenac in a daily dose of 150 mg, you can combine the intake of one tablet (100 mg) of prolonged action with a regular tablet at a dose of 50 mg. The duration of the course is no more than 2 days.
The maximum daily dose of Diclofenac retard-Akrikhin is 150 mg.
Side effects
- from the nervous system: often - dizziness, headache; rarely - drowsiness; very rarely - anxiety, irritability, insomnia, nightmares, mental disorders, depression, impaired sensitivity (including paresthesias), tremors, seizures, memory impairment, disorientation, cerebrovascular disorders, aseptic meningitis;
- on the part of the hematopoietic organs: very rarely - leukopenia, thrombocytopenia, agranulocytosis, hemolytic anemia, aplastic anemia;
- from the digestive system: often - epigastric pain, nausea, vomiting, dyspepsia, flatulence, diarrhea, anorexia, increased aminotransferase activity; rarely - gastritis, gastrointestinal tract manifestation (including bleeding or perforation), gastrointestinal bleeding (melena, diarrhea mixed with blood, vomiting of blood), proctitis, liver dysfunction, hepatitis, jaundice; very rarely - stomatitis, glossitis, esophagitis, constipation, exacerbation of ulcerative colitis or Crohn's disease, pancreatitis, nonspecific hemorrhagic colitis, fulminant hepatitis;
- from the senses: often - vertigo; very rarely - blurred vision, diplopia, impaired taste, tinnitus, hearing impairment;
- on the part of the cardiovascular system: very rarely - increased blood pressure (BP), chest pain, palpitations, heart failure, vasculitis, myocardial infarction;
- from the urinary system: very rarely - hematuria, proteinuria, acute renal failure, interstitial nephritis, papillary necrosis, nephrotic syndrome;
- from the respiratory system: rarely - shortness of breath, exacerbation of bronchial asthma; very rarely - pneumonitis;
- allergic reactions: anaphylactic and anaphylactoid reactions (including a pronounced decrease in blood pressure, shock); very rarely - angioedema (including facial edema);
- dermatological reactions: often - skin rash; rarely - urticaria; very rarely - itching, bullous eruptions, erythema, erythema multiforme, Lyell's syndrome, Stevens-Johnson syndrome, exfoliative dermatitis, photosensitivity, hair loss, purpura, allergic purpura.
Overdose
Symptoms of a diclofenac overdose: epigastric pain, vomiting, dizziness, increased blood pressure, bleeding from the gastrointestinal tract, diarrhea, convulsions, tinnitus, respiratory depression. In cases of significant overdose, acute renal failure develops, the hepatotoxic effect of Diclofenac retard-Akrihin is manifested.
Treatment: immediate gastric lavage, intake of activated charcoal. Appointment of symptomatic therapy. The use of forced diuresis and hemodialysis is ineffective.
special instructions
If it is necessary to achieve a quick therapeutic effect, the tablet can be taken 0.5 hours before meals. To reduce the risk of side effects from the gastrointestinal tract, the course of treatment should consist of the minimum effective dose for a short period.
To relieve pain in an acute attack of gout, it is preferable to take diclofenac in rapid-acting dosage forms.
When prescribing the drug to patients with heart or renal failure, reduced circulating blood volume (including after major surgery), elderly people taking diuretics, it is recommended to take special care and accompany the treatment by monitoring renal function.
With prolonged use of Diclofenac retard-Akrikhin, it is necessary to analyze feces for occult blood, control the picture of peripheral blood and liver function.
During the treatment period, it is recommended to refrain from drinking alcoholic beverages.
Influence on the ability to drive vehicles and complex mechanisms
The use of Diclofenac retard-Akrikhin has a negative effect on the ability of patients to perform potentially hazardous activities that depend on concentration and require a high speed of psychomotor reactions. Therefore, during the period of treatment, patients should refrain from driving vehicles and other complex mechanisms.
Application during pregnancy and lactation
The use of Diclofenac retard-Akrikhin in the third trimester of gestation and during breastfeeding is contraindicated.
The drug should be prescribed with caution in the first and second trimesters of pregnancy.
Diclofenac has a negative effect on fertility, so it is not recommended to use it when planning conception.
Pediatric use
The use of Diclofenac retard-Akrikhin in children and adolescents under the age of 18 is contraindicated.
With impaired renal function
The use of Diclofenac retard-Akrikhin is contraindicated in patients with progressive kidney disease, renal failure with CC less than 30 ml / min.
The drug should be prescribed with caution in renal failure (CC 30-60 ml / min).
For violations of liver function
The use of Diclofenac retard-Akrikhin is contraindicated in case of severe hepatic failure and / or active liver diseases.
The drug should be prescribed with caution in patients with hepatic impairment.
Use in the elderly
Diclofenac retard-Akrikhin should be prescribed with caution in elderly patients.
Drug interactions
With simultaneous use with Diclofenac retard-Akrikhin:
- digoxin, methotrexate, cyclosporin, lithium preparations: diclofenac increases the level of their concentration in plasma;
- diuretics: the effectiveness of diuretic drugs may decrease in the case of combined use with diclofenac;
- potassium-sparing diuretics: diclofenac increases the risk of hyperkalemia;
- anticoagulants, thrombolytic agents (streptokinase, alteplase, urokinase): concomitant therapy with each of these drugs increases the likelihood of bleeding, especially from the gastrointestinal tract;
- antihypertensive and hypnotics: it is possible to reduce their therapeutic effect;
- other NSAIDs, GCS: the combined use of diclofenac with other NSAIDs or with GCS increases the risk of gastrointestinal bleeding;
- methotrexate: diclofenac may increase its toxicity, which should be considered;
- cyclosporine: increased nephrotoxicity of cyclosporine;
- acetylsalicylic acid: the combination with acetylsalicylic acid causes a decrease in the level of diclofenac in the blood;
- paracetamol: taking paracetamol increases the risk of developing nephrotoxic effects of diclofenac;
- hypoglycemic drugs: their effectiveness decreases;
- cefotetan, cefamandol, cefoperazone, plikamycin, valproic acid: against the background of concomitant therapy with one of these drugs, the likelihood of developing hypoprothrombinemia increases;
- cyclosporine, gold preparations: can increase the nephrotoxicity of diclofenac;
- ethanol, selective serotonin reuptake inhibitors, colchicine, corticotropin, St. John's wort preparations: increase the risk of gastrointestinal bleeding;
- drugs that cause photosensitization: diclofenac may enhance their effect;
- drugs that block tubular secretion: increase the level of diclofenac in plasma and enhance its toxic effect;
- quinolones: combination with antibacterial agents in this group increases the risk of seizures.
Analogs
Diclofenac retard-Akrikhin analogs are Diclofenac, Diclofenac Stada, Diclofenac-Teva, Argett Duo, Argett Rapid, Voltaren, Voltaren-Flotak, Voltaren Rapid, Voltaren Emulgel, Diclofenac, Diclaclothicolat., Dorosan, Naklofen, Ortofen, Ortofer, Penseid, Rapten Duo, Rapten Rapid, Flector, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ºC, protected from moisture and light.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Diclofenac retard-Akrikhin
Reviews about Diclofenac retard-Akrikhin are positive. Patients indicate the high efficacy of the drug in relieving pain and relieving inflammation of any etiology (including acute pain in the joints and lower back, gout, osteochondrosis, toothache, headache, post-traumatic pain syndrome). Its advantages include fast and long-lasting action, the possibility of taking it once a day, and an affordable cost.
The main disadvantage of the drug is considered a large list of contraindications and the development of side effects, especially from the digestive system.
The price of Diclofenac retard-Akrikhin in pharmacies
The price of Diclofenac retard-Akrikhin, tablets of prolonged action, film-coated, 100 mg, per pack containing 20 pcs., Can range from 39 rubles.
Diclofenac retard-Akrikhin: prices in online pharmacies
Drug name Price Pharmacy |
Diclofenac Retard-Akrihin tablets p.p. with prolonged release. 100mg 20 pcs. RUB 38 Buy |
Diclofenac retard-Akrihin 100 mg film-coated tablets of prolonged action 20 pcs. RUB 38 Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!