Dolaren
Dolaren: 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: Dolaren
ATX code: M01AB55
Active ingredient: paracetamol (Paracetamol) + diclofenac (Diclofenac)
Manufacturer: Nabros Pharma (India)
Description and photo updated: 2019-27-08
Dolaren is a combined pain reliever.
Release form and composition
The drug is produced in the form of tablets: biconvex, round, two-layer, on the one hand - from almost white to white, on the other - orange with splashes of dark orange and white (10 pcs. In blisters, in a cardboard box 1 or 10 blisters and instructions for the use of Dolaren).
The composition of 1 tablet contains active substances:
- Paracetamol - 500 mg;
- Diclofenac sodium - 50 mg.
Auxiliary components: starch, gelatin, talc, sodium methyl parahydroxybenzoate, magnesium stearate, sodium carboxymethyl starch, colloidal silicon dioxide, microcrystalline cellulose, sodium propyl parahydroxybenzoate, croscarmellose, sunset yellow dye.
Pharmacological properties
Pharmacodynamics
Dolaren is a combined drug, the action of which is due to the properties of the active ingredients.
Paracetamol is a non-narcotic analgesic that blocks COX-1 and -2 (cyclooxygenase 1 and 2) mainly in the central nervous system, affecting the centers of thermoregulation and pain. Cellular peroxidases in inflamed tissues neutralize the effect of paracetamol on COX, which explains the almost complete absence of anti-inflammatory action in the substance.
Diclofenac has analgesic, anti-inflammatory, antipyretic and antiplatelet effects. Indiscriminately inhibits COX-1 and -2, reduces the amount of prostaglandins in the focus of inflammation, disrupts the metabolism of arachidonic acid. In rheumatic diseases, the analgesic and anti-inflammatory effect of diclofenac contributes to a significant decrease in the severity of pain, swelling of the joints, morning stiffness, which leads to an improvement in the functional state of the joint. In patients with injuries, as well as in the postoperative period, diclofenac helps to reduce pain and inflammatory edema.
Pharmacokinetics
The absorption of Dolaren's active ingredients is fast and complete. The rate of absorption of diclofenac is influenced by food, slowing it down by 1–4 hours, and a decrease in C max (maximum concentration of the substance) by 40% is also observed.
The plasma concentration of active substances is linearly dependent on the applied dose, they do not cumulate.
Communication with plasma proteins: diclofenac - from 99% (most of it binds to albumin), paracetamol - 15%. A small amount of both Dolaren's components passes into breast milk.
Diclofenac penetrates into the synovial fluid, where its maximum concentration is determined 2-4 hours later than in plasma. T 1/2 (half-life) from the synovial fluid is in the range from 3 to 6 hours (the concentration of the substance in the synovial fluid 4–6 hours after the administration of the drug is higher than in the plasma, and remains so for another 12 hours). The relationship between the concentration of a substance in the synovial fluid and its clinical efficacy has not been clarified.
Up to 50% of diclofenac undergoes presystemic elimination during the first passage through the liver. Metabolism is carried out through multiple or single hydroxylation and conjugation with glucuronic acid. The process involves the cytochrome P450 CYP2C9 enzyme system. Metabolites have less pharmacological activity than the substance.
Systemic clearance of diclofenac - 350 ml / min, V d (volume of distribution) - 550 ml / kg, T 1/2 from plasma - 2 hours; 65% of the dose is excreted by the kidneys as metabolites, up to 1% - as an unchanged substance, the rest of the dose is excreted in the bile as metabolites.
With severe renal failure (creatinine clearance up to 10 ml / min), the excretion of metabolites in the bile increases, but no increase in their concentration in the blood was noted.
In chronic hepatitis or compensated liver cirrhosis, the pharmacokinetic parameters of diclofenac remain unchanged.
The process of metabolism of paracetamol occurs mainly in the liver (within 90–95%): up to 80% of the dose enters into conjugation reactions with sulfates and glucuronic acid, with the formation of inactive metabolites; 17% of the dose undergoes hydroxylation, resulting in the formation of 8 active metabolites, which are then conjugated with glutathione, after which inactive metabolites are formed. With a lack of glutathione, these metabolites can lead to blocking of the enzyme systems of hepatocytes and cause their necrosis.
The isoenzyme CYP2E1 is also involved in the metabolism of paracetamol. T 1/2 of the substance is in the range from 1 to 4 hours. Excretion is carried out in the form of metabolites (mainly conjugates) by the kidneys, unchanged, only 3% of the substance is excreted. In elderly patients, paracetamol clearance decreases and its T 1/2 increases.
Indications for use
- Neuralgia, lumboishalgia, myalgia, accompanied by inflammation, post-traumatic pain syndrome, migraine, algomenorrhea, proctitis, adnexitis; postoperative headache and toothache;
- Pain syndrome in rheumatic diseases, including osteoarthritis, rheumatoid arthritis (for short-term therapy);
- Infectious and inflammatory diseases of the ear, throat, nose with severe febrile and painful syndrome, including tonsillitis, pharyngitis, otitis media (simultaneously with other drugs).
Contraindications
- Erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase);
- Bleeding from the gastrointestinal tract;
- Inflammatory bowel disease in the acute phase;
- Anamnesis data on attacks of bronchial obstruction, rhinitis, urticaria associated with the intake of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (incomplete or complete acetylsalicylic acid intolerance syndrome - nasal mucosa polyps, rhinosinusitis, bronchial asthma, urticaria);
- Active liver disease, severe liver failure;
- Hematopoiesis and / or hemostasis disorders (including hemophilia);
- Progressive kidney disease, severe renal failure (creatinine clearance less than 30 ml per minute);
- The period after coronary artery bypass grafting;
- Pregnancy and lactation;
- Childhood;
- Hypersensitivity to Dolaren's components (including other non-steroidal anti-inflammatory drugs).
Dolaren tablets should be taken with caution in the following diseases / conditions:
- Cardiac ischemia;
- Congestive heart failure;
- Cerebrovascular disease;
- Bronchial asthma;
- Anemia;
- Hyperlipidemia / dyslipidemia;
- Edematous syndrome;
- Arterial hypertension;
- Benign hyperbilirubinemia (including Gilbert's syndrome);
- Renal or hepatic impairment;
- Peripheral artery disease;
- Alcoholism;
- Erosive and ulcerative diseases of the gastrointestinal tract without exacerbation;
- Diabetes;
- Induced porphyria;
- Condition after extensive surgical interventions;
- Systemic connective tissue diseases;
- Elderly age.
Dolaren, instructions for use: method and dosage
Dolaren tablets are taken orally during or after a meal, without chewing and drinking a little water.
Adults are usually prescribed 1 tablet 2-3 times a day.
The duration of therapy is up to 7 days.
Side effects
During therapy, it is possible for the development of disorders on the part of some body systems, manifesting themselves with different frequencies (often in more than 1% of cases, rarely in less than 1% of cases):
- Nervous system: often - dizziness, headache; rarely - depression, sleep disturbance, drowsiness, irritability, aseptic meningitis (more often in patients with systemic lupus erythematosus and other systemic diseases of the connective tissue), general weakness, convulsions, nightmares, disorientation, a sense of fear;
- Gastrointestinal tract: often - a feeling of bloating, abdominal pain, flatulence, diarrhea, constipation, nausea, gastrointestinal bleeding, increased levels of "liver" enzymes, peptic ulcer with possible complications (perforation, bleeding); rarely - vomiting, melena, jaundice, aphthous stomatitis, blood in the stool, damage to the esophagus, cholecystopancreatitis, dry mucous membranes (including the mouth), liver necrosis, hepatitis (possibly fulminant course), cirrhosis, hepatorenal syndrome, pancreatitis, changes in appetite, colitis;
- Cardiovascular system: rarely - extrasystole, increased blood pressure, congestive heart failure, chest pain;
- Respiratory system: rarely - bronchospasm, cough, pneumonitis, laryngeal edema;
- Immune system and hematopoietic organs: rarely - thrombocytopenic purpura, anemia (including hemolytic and aplastic anemia), thrombocytopenia, leukopenia, agranulocytosis, eosinophilia, worsening of infectious processes (including the development of necrotizing fasciitis);
- Genitourinary system: often - fluid retention; rarely - papillary necrosis, nephrotic syndrome, oliguria, proteinuria, interstitial nephritis, hematuria, azotemia, acute renal failure;
- Skin: often - skin rash, itching; rarely - urticaria, alopecia, eczema, increased photosensitivity, toxic dermatitis, toxic epidermal necrolysis (Lyell's syndrome), exudative erythema multiforme (including Stevens-Johnson syndrome), pinpoint hemorrhages;
- Sense organs: often - tinnitus; rarely - diplopia, scotoma, blurred vision, impaired taste, irreversible or reversible hearing loss;
- Allergic reactions: rarely - anaphylactoid reactions, swelling of the tongue and lips, anaphylactic shock (usually developing rapidly), allergic vasculitis.
Overdose
The severity of Dolaren's overdose is due mainly to paracetamol, which is part of the drug.
The main symptoms: during the first 24 hours after administration - vomiting, nausea, anorexia, pallor of the skin, abdominal pain, metabolic acidosis, impaired glucose metabolism. Symptoms of impaired hepatic function may appear 12–48 hours after an overdose. In severe cases, hepatic failure develops (with progressive encephalopathy, coma, death is possible), acute renal failure in combination with tubular necrosis (including in the absence of severe liver damage), pancreatitis, arrhythmia. In adults, the hepatotoxic effect of paracetamol appears after taking 10 g or more.
Therapy includes the use of SH-group donors and precursors of glutathione synthesis: 8-9 hours after overdose - methionine, 12 hours - acetylcysteine. The need for additional therapeutic measures (further use of these drugs) is determined by the concentration of paracetamol in the blood, as well as the time that has passed after its administration.
special instructions
While taking Dolaren, it is necessary to monitor kidney and liver function, peripheral blood patterns and feces for the presence of blood.
Due to the increased risk of developing adverse reactions, the simultaneous administration of Dolaren with non-steroidal anti-inflammatory drugs is not recommended.
When Dolaren is used, laboratory parameters may be distorted in the quantitative determination of uric acid and glucose in plasma.
Influence on the ability to drive vehicles and complex mechanisms
Patients taking Dolaren are advised to refrain from performing work requiring increased attention and quick motor and mental reactions, as well as from drinking alcohol.
Application during pregnancy and lactation
Dolaren is not prescribed during pregnancy / lactation.
Pediatric use
Dolar is contraindicated in pediatric patients.
With impaired renal function
- Severe renal failure (with creatinine clearance up to 30 ml / min), progressive kidney disease: Dolaren is contraindicated;
- Renal failure: therapy should be carried out under medical supervision.
For violations of liver function
- Severe liver failure, active liver disease: Dolaren is contraindicated;
- Liver failure: therapy should be performed under medical supervision.
Use in the elderly
Elderly patients should use Dolaren with caution.
Drug interactions
With the simultaneous use of Dolaren with some drugs, undesirable effects may occur (due to the active substances included in the drug: diclofenac and paracetamol):
- Digoxin, lithium preparations: increasing their concentration in plasma;
- Anticoagulants, antiplatelet and thrombolytic drugs (streptokinase, alteplase, urokinase): increased risk of bleeding (more often the gastrointestinal tract);
- Diuretics: a decrease in their effect (with the use of potassium-sparing diuretics - an increased risk of hyperkalemia);
- Antihypertensive and hypnotic drugs: reducing their effect;
- Methotrexate: an increase in the likelihood of increasing its toxicity (due to an increase in its concentration in plasma);
- Other nonsteroidal anti-inflammatory drugs and glucocorticosteroids: an increase in the likelihood of side effects (bleeding into the gastrointestinal tract);
- Acetylsalicylic acid: a decrease in the concentration of diclofenac in the blood;
- Cyclosporine: an increase in the likelihood of increasing its nephrotoxicity (due to an increase in its concentration in plasma);
- Cefoperazone, cefamandol, cefootstan, plikamycin and valproic acid: an increase in the incidence of hypoprothrombinemia;
- Hypoglycemic drugs: reducing their effect;
- Selective serotonin reuptake inhibitors: increased risk of bleeding from the gastrointestinal tract;
- Gold preparations and cyclosporine: an increase in the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which leads to an increase in nephrotoxicity;
- Drugs causing photosensitization: increasing the sensitizing effect of diclofenac to ultraviolet radiation;
- Ethanol, colchicine, corticotropin and St. John's wort preparations: increased risk of bleeding in the gastrointestinal tract;
- Quinolone antibacterial drugs: increased risk of seizures;
- Medicines that block tubular secretion: increasing the concentration of diclofenac in plasma, which increases its toxicity and effectiveness;
- Anticoagulant drugs: an increase in their effect (when using high doses of paracetamol);
- Uricosuric medicines: decrease in their effectiveness;
- Barbiturates (long-term use): decreased effectiveness of paracetamol;
- Diflunisal: a significant increase in the plasma concentration of paracetamol and the risk of developing hepatotoxicity;
- Inducers of microsomal oxidation in the liver (ethanol, phenytoin, barbiturates, rifampicin, tricyclic antidepressants, phenylbutazone), hepatotoxic drugs: an increase in the production of hydroxylated active metabolites (the possibility of developing severe intoxications even with a slight overdose);
- Ethanol: increased risk of liver damage and acute pancreatitis;
- Salicylates: an increased risk of bladder or kidney cancer (with prolonged use of high doses of paracetamol);
- Inhibitors of microsomal oxidation (including cimetidine): reducing the risk of hepatotoxic effects;
- Myelotoxic drugs: increased manifestations of paracetamol hematotoxicity.
Analogs
Dolaren's analogue is Panoxen.
Terms and conditions of storage
Store in a dark, dry place out of reach of children at temperatures up to 25 ° C.
Shelf life is 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
About Dolaren
The reviews about Dolaren are mostly positive. Patients point to its high efficiency, while especially note the long-term analgesic effect. The drug is not intended for long-term use, since in this case the development of side effects is observed.
The price for Dolaren in pharmacies
The approximate price for Dolaren (10 tablets) is 93-108 rubles.
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!
