Pharmacological properties Diclofenac 75 mg
Diclofenac is a nonsteroidal anti-inflammatory drug with pronounced anti-inflammatory, analgesic and antipyretic effect. A derivative of phenylacetic acid.
Pharmacodynamics Diclofenac 75 mg
Inhibits the activity of the enzyme cyclooxygenase and thus violates the metabolism of arachidonic acid, reducing the formation of precursors of prostaglandins and thromboxanes. Analgesic effects associated with inhibition of local synthesis of prostaglandins and other substances that increase the sensitivity of pain receptors to chemical stimulation. Antipyretic effects associated with the direct influence on the thermoregulatory center in the hypothalamus. In rheumatic diseases and anti-inflammatory effect analyeziruyuschee Diclofenac significantly less severity of pain, morning stiffness, swollen joints, improves the functional status of the patient. Trauma, postoperative Diclofenac reduces pain and inflammatory swelling.
Pharmacokinetics Diclofenac 75 mg
Following oral administration is rapidly and completely absorbed. The maximum concentration after taking the pills retard 100 mg is reached after 4 hours and 0.5 mg / ml. 99% Diclofenac binds to plasma proteins, namely albumin. Diclofenac enters the synovial fluid, where maximum concentration is achieved in 2-4 hours later than in plasma. If ingestion of about 50% Diclofenac is metabolized in the liver “first-pass”. Systemic clearance of the active substance is about 263 ml / min. Half Life – for 1-2 hours. Approximately 60% is excreted by the kidneys as metabolites, less than 1% in unchanged form excreted in the urine, the remainder excreted as metabolites in the bile.
Indications for Use Diclofenac 75 mg
Diclofenac is used for:
• acute arthritis of various origins (including the case of gout);
• chronic arthritis, especially in rheumatoid arthritis (chronic polyarthritis);
• juvenile chronic polyarthritis;
• ankylosing spondylitis (Bechterew’s disease) and other inflammatory rheumatic diseases of the spine;
• arthrosis and spondylarthrosis (state of inflammation in degenerative diseases of joints and spine);
• soft tissue rheumatism;
• painful swelling and inflammation after trauma surgery m;
• non-rheumatic inflammatory pain states.
Contraindications Diclofenac 75 mg
• erosive and ulcerative lesions of the gastrointestinal tract in acute phase;
• information about the attacks of asthma, urticaria, acute rhinitis associated with the use of aspirin or other NSAIDs;
• Hypersensitivity to Diclofenac or the drug;
• blood disorders of unknown etiology;
• III trimester of pregnancy;
• Children under 6 years old.
Cautions Diclofenac 75 mg
With extreme caution is prescribed to patients with diseases of the liver, kidneys and gastrointestinal tract in the history of bronchial asthma, allergic (“hay”), runny nose, nasal polyps, dyspeptic symptoms at the time of appointment of the drug, hypertension, heart failure, after major surgical interventions, the first and second trimesters of pregnancy and lactation, as well as the elderly. Due to the high content of active substance tablets retard 100 mg is not recommended for children under 18 years old.
Cautions
During the period of drug treatment should be systematic monitoring of peripheral blood, liver, kidney, fecal for blood. Patients taking the drug, you should refrain from acts of requiring increased attention and rapid mental and motor responses, use of alcohol.
Interaction with other medicinal products Diclofenac 75 mg
With simultaneous use of Diclofenac and:
• digoxin, phenytoin or drugs lithium – can raise the levels of plasma for these medicines;
• diuretics and antihypertensive drugs – may decrease the action of these agents;
• potassium-sparing diuretics – may experience hyperkalemia;
• glucocorticoids or other NSAIDs – increased risk of side effects from the gastrointestinal tract;
• ASA – may be a lowering of the concentration of Diclofenac in the blood serum;
• cyclosporine – may increase the toxic effect of the latter on the kidneys;
• antidiabetic agents – may cause hypo-or hyperglycemia;
• methotrexate for 24 hours before or after admission may lead to increased concentrations of methotrexate and to enhance its toxicity;
• anticoagulants – requires regular monitoring of blood clotting.
Dosage and administration Diclofenac 75 mg
The drug is taken by mouth, not chewing with sufficient quantity of liquid at the end or after a meal.
Dosage and duration of treatment determines doctor depending on the characteristics of the disease and the severity of the condition. In rheumatic diseases treatment may be prolonged. Usually the recommended adult dose ranges from 50-150 mg of Diclofenac sodium per day, divided into 2-3 doses. The maximum daily dose is 150 mg.
Retard tablets are usually given one time per day in a single dose of 100 mg. Children over 6 years the recommended dose is 1-2 mg / kg body weight per day, divided into 2-3 doses.
Side effect Diclofenac 75 mg
Gastro-intestinal: nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, constipation, and in rare cases, observed the appearance of erosive and ulcerative lesions, bleeding and perforation of the gastrointestinal tract.
The nervous system: sometimes marked headache, dizziness, sleep disturbances (insomnia or drowsiness), excitation, and in some cases, marked sensory disturbances, disorientation, impaired memory, vision, hearing, taste, tinnitus, convulsions, tremors, mental disorders, depression, anxiety, and aseptic meningitis.
Allergic reactions: skin rash, rare – rash, reported isolated cases of eczema, polymorphic erythema, erythroderma, rarely observed bronchial asthma, systemic anaphylactic reactions, in some cases – vasculitis, pneumonitis.
The kidneys: rare – swelling, in some cases, acute renal failure, interstitial nephritis, nephrotic syndrome, hematuria, proteinuria.
From the Liver: transient increase of transaminases in the blood, rarely – hepatitis, in some cases – fulminant hepatitis.
From the hemopoietic system: describes specific cases of thrombocytopenia, agranulocytosis, hemolytic anemia, aplastic anemia.
Cardio-vascular system: reported isolated cases of tachycardia, hypertension, congestive heart failure.
Overdose Diclofenac 75 mg
Symptoms: The clinical picture is determined disorders of the central nervous system (headache, dizziness, irritability, hyperventilation phenomenon with increased convulsive readiness and gastro-intestinal disorders (abdominal pain, nausea, vomiting).
Treatment: no specific antidote exists. Requires intensive medical care and symptomatic treatment.
