Diclofenac-UBF - instructions for use, dose, side effects, contraindications

Excipients: lactose, potato starch, polyvinylpyrrolidone, low molecular medicine, stearic acid or calcium stearate, kollikut MAE 100 P, talc, titanium dioxide pigment, polyethylene, silicone emulsion, tropeolin O, acid red.

Description:Tablets, film-coated, yellow-orange or orange. Two layers are visible on the cross-section.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).

ATX: & nbsp

S.01.B.C.03 Diclofenac

M.01.A.B.05 Diclofenac

Pharmacodynamics:It has anti-inflammatory, analgesic, antipyretic effect. Inhibiting cyclooxygenase 1 and 2, gives the metabolism of arachidonic acid, prostaglandins decreases the amount (Pg) both in inflammation and in healthy tissue, inhibits the exudative and the proliferative phases of inflammation. Has antiaggregant effect.

Pharmacokinetics:Absorption is fast and complete, food slows down the absorption rate. After oral administration, 50 mg the maximum concentration (Cmax) - 1.5 μg / ml is achieved after - 2-3 hours. The concentration in the plasma is linear depending on the amount of the administered dose. Changes in the pharmacokinetics of diclofenac against the background of repeated administration are not noted. Do not cumulate while observing the recommended interval between meals.

Bioavailability - 50%. The connection with proteins is 95-98% (most of it is associated with albumins). Penetrates into the synovial fluid; The maximum concentration in the synovial fluid is observed 2-4 hours later than in the plasma. The half-life of the synovial fluid is 3-6 hours (the concentration of the active substance in the synovial fluid 4-6 hours after the administration of the drug is higher than in the plasma, and remains higher for another 12 hours).

Metabolism: 50% of the active substance is metabolized during the "first pass" through the liver. The area under the concentration curve is 2 times less after oral administration of the preparation than after parenteral administration of the same dose. Metabolism occurs as a result of multiple or one-time hydroxylation and conjugation with glucuronic acid. The pharmacological activity of metabolites is lower than that of diclofenac.

Systemic clearance is 260 ml / min. Half-life from the plasma - 1-2 hours 60% of the administered dose is excreted as metabolites through the kidneys; less than 1% is unchanged, the rest of the dose is excreted as metabolites with bile. In patients with severe renal dysfunction, (creatinine clearance less than 10 ml / min), the excretion of metabolites with bile is increased, while the increase in their concentration in the blood is not observed.

In patients with chronic hepatitis or compensated cirrhosis, the pharmacokinetic parameters of diclofenac are the same as in patients without liver disease.

Indications:

Inflammatory diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis, gouty arthritis).

Degenerative diseases of the musculoskeletal system (deforming osteoarthritis, osteochondrosis).

Lumbago, sciatica, neuralgia, myalgia, tendovaginitis, bursitis.

Post-traumatic pain syndrome, accompanied by inflammation, post-operative pain, migraine, renal colic; primary algodismenorea, adnexitis, proctitis.

In the complex therapy of infectious and inflammatory diseases of the ENT organs with severe pain syndrome (pharyngitis, tonsillitis, otitis).

Contraindications:Hypersensitivity (including to other NSAIDs), erosive and ulcerative lesions of the gastrointestinal tract (gastrointestinal tract) (in the phase of exacerbation), aspirin asthma, hematopoiesis disorders, pregnancy, younger children (up to 6 years), period lactation.

Carefully:Induced acute liver porphyria, severe violations of liver and kidney function, heart failure, elderly age.

Dosing and Administration:

Inside, without chewing, during or after a meal, with a small amount of water. Adults - 25-50 mg 2-3 times a day. When the optimal therapeutic effect is achieved, the dose is gradually reduced and switched to maintenance treatment at a dose of 50 mg / day. The maximum daily dose is 150 mg. For children over 12 years of age, the daily dose to 2 mg / kg of a child.

With juvenile rheumatoid arthritis, the daily dose can be increased to 3 mg / kg.

Side effects:

From the digestive system: gastralgia, nausea, vomiting, diarrhea, flatulence, anorexia, increased activity of "liver" transaminases, gastrointestinal bleeding (hematemesis, melena), hepatitis with jaundice or without jaundice, fulminant hepatitis, pancreatitis, nonspecific colitis with bleeding, erosive and ulcerative lesions of the digestive tract, aphthous stomatitis, glossitis, constipation, abdominal pain, dry mouth.

From the nervous systemheadache, dizziness, fatigue, impaired perception, paresthesia, memory loss, loss of orientation, decreased visual acuity, diplopia, hearing loss, tinnitus, insomnia, irritability, convulsions, depression, anxiety, nightmarish dreams, tremor, psychotic reactions, violation of taste sensations, aseptic meningitis, scotoma.

From the skin side: skin itching, skin rash (mainly erythematous and urticaria), angioedema, eczema, allergic purpura, erythema multiforme exudative (eg Stevens-Johnson syndrome), erythroderma, toxic epidermal necrolysis (Lyell's syndrome), alopecia, photosensitization.

From the urinary system: acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis, oliguria, cystitis.

On the part of the organs of hematopoiesis: thrombocytopenia, leukopenia, agranulocytosis, hemolytic anemia, aplastic anemia.

From the cardiovascular system: heart palpitations, chest pain, arrhythmia, increased blood pressure.

Other: impotence, edema, bronchospasm, systemic anaphylactic reactions (including shock).

Overdose:

Symptoms: dizziness, headache, hyperventilation of the lungs, confusion, in children - myoclonic cramps, nausea, vomiting, abdominal pain, bleeding, impaired liver and kidney function.

Treatment: gastric lavage, the introduction of activated charcoal, symptomatic therapy aimed at eliminating the increase in blood pressure, impaired renal function, seizures, gastrointestinal irritation, respiratory depression. Forced diuresis, hemodialysis are ineffective.

Interaction:

Increases plasma concentrations of digoxin, lithium and cyclosporine.

Against the background of potassium-sparing diuretics, the risk of hyperkalemia increases, against the background of

anticoagulants - risk of bleeding.

Reduces the effects of diuretic, hypotensive and hypnotics.Increases the likelihood of side effects of NSAIDs and glucocorticosteroids (gastrointestinal bleeding), toxicity of methotrexate and nephrotoxicity of cyclosporine.

Acetylsalicylic acid reduces the concentration of diclofenac in the blood.

With simultaneous use with oral antidiabetic drugs

both hypo- and hyperglycemia are possible.

Against a background of thrombolytic agents (alteplase, streptokinase, urokinase) - the risk of bleeding (often GIT).

Cefamandol, cefoperazone, cefotetan, valproic acid, plikamycin increase the frequency of hypoprothrombinemia.

Cyclosporine and gold preparations potentiate the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which increases the nephrotoxicity of diclofenac. Simultaneous use with paracetamol increases the risk of developing nephrotoxic effects of diclofenac.

Simultaneous use with alcohol, glucocorticosteroids, colchicine, corticotropin and preparations of St. John's wort increases the risk of development of gutrointestinal complications accompanied by bleeding. Reduces the hypotensive activity of vasodilators.

Special instructions:

To quickly achieve the desired therapeutic effect taken for 30 minutes. before meals. In other cases, take before, during or after a meal in undiluted form, with plenty of water.

Because of the important role of prostaglandins in maintaining renal blood flow, caution should be exercised in appointing patients with cardiac or renal insufficiency, as well as in the treatment of elderly people taking diuretics, and patients who for any reason have a decrease in circulating blood volume for example, after major surgery). If in such cases appoint diclofenac, recommend as a precautionary measure to monitor kidney function.

In patients with renal insufficiency (chronic hepatitis, compensated cirrhosis), the kinetics and metabolism do not differ from similar processes in patients with normal liver function. When performing long-term therapy, it is necessary to monitor liver function, the picture of peripheral blood, the analysis of feces for latent blood.

It is necessary to refrain from engaging in potentially dangerous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Tablets coated with enteric coating, 25 mg.

Packaging:

10 tablets per contour cell pack. By 10, 20, 25, 30, 40, 50, 60 tablets in cans of polymeric.

Each jar or 1, 2, 3, 5 contour squares with instructions for use are placed in a bundle.

Storage conditions:

List B.

In a dry, dark place, out of the reach of children.

Shelf life:3 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N003921 / 01

Date of registration:15.03.2010

The owner of the registration certificate:URALBIOFARM, OJSC URALBIOFARM, OJSC Russia

Manufacturer: & nbsp

URALBIOFARM, OJSC Russia

Information update date: & nbsp19.02.2016

Illustrated instructions

Instructions

Diclofenac-UBF (Diclofenac-UBF)