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Active ingredients
Diclofenac
Release form
Pills
Composition
Diclofenac sodium 75 mg; Excipients: lactose monohydrate, methyl hydroxypropyl cellulose, microcrystalline cellulose, calcium hydrogen phosphate dihydrate, corn starch, sodium starch glycolate, silicon dioxide colloid, magnesium stearate, ferric oxide red.
Pharmacological effect
NSAIDs. It has a pronounced analgesic, anti-inflammatory and antipyretic effect. Indiscriminately inhibits COX-1 and COX-2, violates the metabolism of arachidonic acid, reduces the amount of prostaglandins in the focus of inflammation. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain, morning stiffness, swelling of the joints, which improves the functional state of the joint. With injuries in the postoperative period, diclofenac reduces pain and inflammatory edema.
Pharmacokinetics
Absorption; After taking the drug inside - absorption is fast and complete, food slows down the absorption rate by 1-2 hours and reduces Cmax 2 times. In the case of taking the drug with food, Cmax is achieved on average in 5-6 hours; Distribution; Diclofenac binding to plasma proteins - more than 99% (most of it is associated with albumin). Vd - 550 ml / kg; Penetrates into synovial fluid. Cmax in synovial fluid is achieved 2-4 hours later than in plasma. T1 / 2 from synovial fluid 3-6 h (the concentration of the active substance in the synovial fluid 4-6 h after administration of the drug is higher than in plasma, and remains higher for 12 more hours). The relationship of drug concentration in the synovilic fluid with the clinical efficacy of the drug has not been elucidated .; Changes in the pharmacokinetics of diclofenac against the background of repeated administration is not observed, not cumulative .; Diclofenac is excreted in breast milk .; Metabolism; 50% of the active substance is metabolized during the "first pass" through the liver. Metabolism occurs as a result of repeated or single hydroxylation and conjugation with glucuronic acid. CYP2C9 isoenzyme is involved in diclofenac metabolism. Pharmacological activity of metabolites is lower than diclofenac .; Removal; T1 / 2 from plasma - 2 h. Systemic clearance is 350 ml / min.65% of the administered dose is excreted by the kidneys as metabolites by the kidneys, less than 1% is unchanged, the rest of the dose is excreted as metabolites with bile .; Pharmacokinetics in special clinical situations; In patients with severe renal insufficiency (QC less than 10 ml / min), excretion of metabolites with bile increases, while increasing their concentration in the blood is not observed .; In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetic parameters of diclofenac do not change.
Indications
- diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis, gouty arthritis, rheumatic soft tissue damage, osteoarthritis of the peripheral joints and spinal cord, including those with radicular syndrome, tendovinitis, bursitis); - pain syndrome of weak or moderate intensity: neuralgia, myalgia, lumboischialgia, post-traumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, algomenorrhea, adnexitis, proctitis, toothache; - as part of complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain (pharyngitis, tonsillitis, otitis media); - febrile syndrome.
Contraindications
- erosive and ulcerative lesions of the digestive tract (in the acute phase); - bleeding from the digestive tract; - "aspirin" asthma; - violations of blood formation; - disorders of hemostasis (including hemophilia); - children's and teenage age up to 18 years; - pregnancy; - lactation period (breastfeeding); - hypersensitivity to the drug; - hypersensitivity to other NSAIDs .; The drug should be used with caution in anemia, bronchial asthma, congestive heart failure, arterial hypertension, edematous syndrome, hepatic or renal failure, in alcoholism, inflammatory bowel disease, erosive and ulcerative gastrointestinal lesions without exacerbation, in diabetes mellitus, after extensive surgical conditions interventions induced by porphyria in elderly patients, with diverticulitis, systemic connective tissue diseases.
Use during pregnancy and lactation
The drug is contraindicated in pregnancy and lactation (breastfeeding).
Dosage and administration
The drug is used inside, without chewing, with a small amount of water, usually during or after a meal .; Assign 75 mg (1 tab.) 1-2 times / day or 150 mg (1 tab.) 1 time / day. The maximum daily dose of the drug - 150 mg.
Side effects
On the part of the digestive system:> 1% - abdominal pain, feeling of bloating, diarrhea, nausea, constipation, flatulence, increased activity of liver enzymes, peptic ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding; less than 1% - vomiting, jaundice, melena, blood in the feces, damage to the esophagus, aphthous stomatitis, dry mouth and mucous membranes, hepatitis (possibly fulminant course), necrosis of the liver, cirrhosis, hepatorenal syndrome, changes in appetite, pancreatitis, cholecystopancreatitis, colitis ; CNS:> 1% - headache, dizziness; less than 1% - sleep disturbance, drowsiness, depression, irritability, aseptic meningitis (more often in patients with SLE and other systemic diseases of the connective tissue), convulsions, weakness, disorientation, nightmares, and a sense of fear .; On the part of the senses:> 1% - tinnitus; less than 1% - blurred vision, diplopia, taste disturbance, reversible or irreversible hearing loss, scotoma .; Dermatological reactions:> 1% - pruritus, skin rash; less than 1% - alopecia, urticaria, eczema, toxic dermatitis, photosensitivity, petechial hemorrhages .; On the part of the urinary system:> 1% - fluid retention; less than 1% - nephrotic syndrome, proteinuria, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia .; From the hematopoietic system: less than 1% - anemia (including hemolytic and aplastic anemia), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura,; From the respiratory system: less than 1% - cough, bronchospasm, laryngeal swelling, pneumonitis .; Since the cardiovascular system: less than 1% - increased blood pressure, congestive heart failure, extrasystole, chest pain .; Allergic reactions: less than 1% - anaphylactoid reactions, anaphylactic shock (usually develops rapidly), swelling of the lips and tongue, allergic vasculitis, erythema multiforme exudative, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome) .; Others: less than 1% - worsening of the course of infectious processes (development of necrotizing fasciitis).
Overdose
Symptoms: vomiting, dizziness, headache, shortness of breath, clouding of consciousness, in children - myoclonic convulsions, nausea, abdominal pain, bleeding, impaired liver and kidney function .; Treatment: gastric lavage, the introduction of activated carbon, symptomatic therapy, forced diuresis. Hemodialysis is ineffective.
Interaction with other drugs
Increases plasma concentration of digoxin, methotrexate, lithium preparations and cyclosporine .; Reduces the effect of diuretics, against the background of potassium-sparing diuretics increases the risk of hyperkalemia; against the background of anticoagulants, thrombolytic agents (alteplaza, streptokinase, urokinase) - the risk of bleeding (usually from the gastrointestinal tract) .; Reduces the effects of hypotensive and hypnotic drugs .; Increases the likelihood of side effects of other NSAIDs and GCS (bleeding from the gastrointestinal tract), the toxicity of methotrexate and cyclosporine nephrotoxicity .; Acetylsalicylic acid decreases blood levels of diclofenac .; Concurrent use with paracetamol increases the risk of the development of the nephrotoxic effects of diclofenac .; Reduces the effectiveness of hypoglycemic agents .; Cefamandol, cefoperazone, cefotetan, valproic acid and plykamycin increase the incidence of hypoprothrombinemia .; Cyclosporine and gold preparations enhance the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which increases nephrotoxicity .; The simultaneous appointment with ethanol, colchicine, corticotropin and St. John's wort preparations increases the risk of bleeding from the gastrointestinal tract .; Diclofenac enhances the effects of drugs that cause photosensitization .; Drugs that block tubular secretion, increase plasma concentration of diclofenac, thereby increasing its toxicity.
special instructions
During the period of treatment, a systematic control of the pattern of peripheral blood, liver and kidney functions should be carried out, the examination of feces for the presence of blood .; When taking the drug should be excluded alcohol .; Influence on the ability to drive vehicles and control mechanisms; Patients taking the drug should refrain from activities that require high concentration of attention and quick psychomotor reactions.