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

Diclofenac Stade® tablets, coated with enteric coating, 25 mg and 50 mg. Uncoated tablet: diclofenac sodium as an active ingredient 25,000 mg or 50,000 mg; as auxiliary substances: povidone K30 3,700 mg or 6,800 mg, lactose monohydrate 25,000 mg or 40,000 mg, cucumber starch 28.470 mg or 50,000 mg, silicon dioxide colloidal anhydrous 0.055 mg or 0.200 mg, microcrystalline cellulose 27,500 mg or 32.600 mg, magnesium stearate 0.275 mg or 0.400 mg. The theoretical weight of a tablet without a coat is 110,000 mg or 180,000 mg.

Film sheath: methacrylic acid and ethyl acrylate copolymer - 3,424 mg or 6,111 mg; triethyl citrate - 0.685 mg or 1.222 mg; talcum 1,143 mg or 2,037 mg, hypromellose 1,902 mg or 5,658 mg, macrogol 400 0.274 mg or 0.633 mg, macrogol 6000 0.125 mg or 0.206 mg, magnesium stearate 0.087 mg or 0.160 mg, titanium dioxide (E 171) - 0.379 mg or 0.545 mg, iron oxide red (E 172) 0.043 mg or 0.180 mg, iron oxide yellow (E 172) 0.336 mg or 0.386 mg.

The weight of the coated tablet is 118,398 mg or 197,138 mg.

Description:Round tablets of biconvex form, covered with enteric film coating, light brown color.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug.

ATX: & nbsp

S.01.B.C.03 Diclofenac

M.01.A.B.05 Diclofenac

Pharmacodynamics:Non-steroidal anti-inflammatory drug, a derivative of phenylacetic acid; has anti-inflammatory, analgesic and antipyretic effect. Indiscriminately inhibiting cycloxygenase 1 and cycloxygenase 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus. The most effective for inflammatory pain. Like all non-steroidal anti-inflammatory drugs, the drug has antiplatelet activity.

Pharmacokinetics:

Absorption is fast and complete, food slows down the absorption rate. After oral administration, 50 mg of Cmax is 1.5 μg / ml, and Tmax is 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 plasma proteins is more than 99% (most of it is associated with albumins). Penetrates into breast milk, synovial fluid; Stax in the synovial fluid is observed 2-4 hours later than in the plasma.T1 / 2 from the synovial fluid - 3-6 hours (the concentration of the drug in the synovial fluid 4-6 hours after its administration is higher than in the plasma, and remain higher for another 12 hours). 50% of the drug is metabolized during the "first pass" through the liver; AUC is 2 times less after oral administration of the drug 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 isozyme CYP2C9 also participates in the metabolism of the drug. Pharmacological activity of metabolites is less than diclofenac.

Systemic clearance is 260 ml / min. T1 / 2 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 failure (creatinine clearance less than 10 ml / min), the excretion of metabolites with bile is increased, while there is no increase in their concentration in the blood.

In patients with chronic hepatitis or compensated cirrhosis of the liver, the pharmacokinetic parameters do not change.

Indications:

Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), neuralgic amyotrophy (Pursonage-Turner's disease), osteoarthritis, rheumatism, gouty arthritis, arthritis in Reiter's disease.

Pain syndrome: headache (including migraine) and toothache, bursitis, tendonitis, lumbago, sciatica, ossalgia, neuralgia, myalgia, arthralgia, radiculitis, with oncological diseases, post-traumatic and postoperative pain syndrome accompanied by inflammation.

Algodismenorea; inflammatory processes in the small pelvis, incl. adnexitis; childbirth (as an analgesic and tocolytic agent).

Infectious and inflammatory diseases of the ENT organs with severe pain syndrome (as part of complex therapy): pharyngitis, tonsillitis, otitis media.

Feverish syndrome with "colds" and infectious diseases.

Contraindications:

- Period after aortocoronary bypass surgery;

- III trimester of pregnancy, the period of breastfeeding;

- Uncompensated heart failure;

- Hypersensitivity to the active substance or ancillary components;

- Anamnestic data on an attack of bronchial obstruction, rhinitis, hives after taking acetylsalicylic acid or other NSAIDs (complete or incomplete acetylsalicylic acid intolerance syndrome - rhinosinusitis, urticaria, polyps of the nasal mucosa, asthma);

- Erosive and ulcerative changes in the gastric mucosa or duodenum, active gastrointestinal bleeding;

- Inflammatory bowel disease (nonspecific ulcerative colitis, Crohn's disease);

- Cerebrovascular bleeding or other bleeding and hemostasis disorders;

- Severe hepatic impairment or active liver disease;

- Severe renal insufficiency (creatinine clearance less than 30 ml / min); progressive kidney disease, incl. confirmed hyperkalemia;

- Tablets of 25 mg are contraindicated to children under 6 years of age;

- Tablets of 50 mg are contraindicated in children under 15 years of age.

Carefully:

Anemia, bronchial asthma, cerebrovascular diseases, ischemic heart disease, congestive heart failure, arterial hypertension, peripheral arterial disease, edematous syndrome,hepatic or renal insufficiency, dyslipidemia / hyperlipidemia, diabetes mellitus, smoking, inflammatory bowel disease, condition after extensive surgical interventions, porphyria induced, elderly age, diverticulitis, systemic connective tissue diseases, creatinine clearance less than 60 ml / min.

Anamnestic data on the development of gastrointestinal ulcer, presence of Helicobacter pylori infection, old age, prolonged use of NSAIDs, frequent alcohol consumption, severe physical illnesses. Simultaneous therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

Dosing and Administration:

Inside, not liquid, during or after a meal, 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 6 years and adolescents, 25 mg tablets are used; The daily dose is 2 mg / kg of the baby.

With juvenile rheumatoid arthritis, the daily dose can be increased to 3 mg / kg. Tablets should be taken whole, not liquid, fasting, with a small amount of liquid.

Side effects:

Often - 1-10%; sometimes - 0.1-1%; rarely - 0.01-0.1%; very rarely - less than 0.001%, including individual cases.

From the digestive system: often - epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases; rarely

- gastritis, proctitis, bleeding from the gastrointestinal (vomiting blood, melena, bloody diarrhea), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, liver dysfunction; very rarely - stomatitis, glossitis, oesophageal damage, diaphragm-like intestinal strictures (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease), constipation, pancreatitis, fulminant hepatitis, exacerbation of hemorrhoids (for rectal suppositories).

From the nervous system: often - headache, dizziness; rarely - drowsiness; very rarely - a violation of sensitivity, incl.paresthesia, memory disorders, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia, nightmares, irritability, mental disorders.

From the sense organs: often - vertigo; very rarely - visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, a violation of taste sensations.

From the urinary system: very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

On the part of the organs of hematopoiesis: very rarely - thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis.

Allergic reactions: anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure and shock; very rarely - angioedema (including face).

From the cardiovascular system: very rarely - palpitations, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.

From the respiratory system: rarely - bronchial asthma (including dyspnea); very rarely - pneumonitis.

From the skin: often - skin rash; rarely - hives; very rarely - bullous eruptions, eczema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.

Overdose:

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

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

Interaction:

Increases the concentration in the plasma digoxin, methotrexate, lithium and cyclosporine.

Reduces the effect of diuretics, against the background of potassium-sparing diuretics increases the risk of hyperkalemia; on the background of anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) - the risk of bleeding (more often from the gastrointestinal tract).Reduces the effects of hypotensive and hypnotics.

Increases the likelihood of side effects of other non-steroidal anti-inflammatory drugs and glucocorticosteroid agents (bleeding in the gastrointestinal tract), toxicity of methotrexate and nephrotoxicity of cyclosporine.

Acetylsalicylic acid reduces the concentration of diclofenac in the blood.

Simultaneous use with paracetamol increases the risk of developing nephrotoxic effects of diclofenac. Reduces the effect of hypoglycemic agents.

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

Cyclosporine and gold preparations increase the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which increases nephrotoxicity.

Simultaneous administration with ethanol, colchicine, corticotropin, serotonin reuptake inhibitors and St. John's wort increases the risk of bleeding in the gastrointestinal tract.

Diclofenac enhances the effect of drugs that cause photosensitivity. Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby,increasing its toxicity.

Antibacterial drugs from the quinolone group - the risk of seizures. Effect on the results of laboratory tests: diclofenac may affect serum transaminase levels (if this effect is long-lasting or if complications occur, treatment should be discontinued), and may cause an increase in potassium concentration.

Special instructions:

In order to quickly achieve the desired therapeutic effect take 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, and also in the treatment of elderly patients taking diuretics and patients who for any reason have a decrease in circulating blood volume (for example , after a major surgical intervention). If in such cases appoint diclofenac, recommend as a precautionary measure to monitor kidney function.

In patients with renal insufficiency with creatinine clearance less than 10 ml / min Css metabolites in plasma should theoretically be significantly higher than in patients with normal renal function, however this is not really observed, since in this situation the excretion of metabolites with bile is enhanced.

In patients with hepatic 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.

During the treatment period, it is possible to reduce the speed of mental and motor reactions, so it is necessary to refrain from driving motor vehicles and practicing other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Diclofenac Stade® tablets, coated with enteric film coating, 25 mg and 50 mg.

Packaging:10 tablets per contour cell pack.2 or 5 contiguous cell packs (for a dosage of 25 mg) and 2, 5 or 10 contiguous cell packs (for a dosage of 50 mg), together with instructions for medical use of the drug, are placed in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

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

Terms of leave from pharmacies:On prescription

Registration number:П N013804 / 03

Date of registration:29.08.2008

The owner of the registration certificate:SHTADA Artznajmittel AGSHTADA Artznajmittel AG Germany

Manufacturer: & nbsp

STADA Arzneimittel, AG Germany

Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia

Information update date: & nbsp27.02.2016

Illustrated instructions

Instructions

Diclofenac Stade® (Diclofenac Stada®)