Composition, form of production and packaging
Capsules 1 tab.
diclofenac sodium 50 mg
10 pieces. - blisters (2) - packs of cardboard.
10 pieces. - blisters (3) - packs of cardboard.
10 pieces. - blisters (5) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Has anti-inflammatory, analgesic and antipyretic effect. By indiscriminately inhibiting cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2), it breaks 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 (NSAIDs), the drug has antiplatelet activity.
PHARMACOKINETICS
Suction: after oral administration, diclofenac is easily absorbed into the systemic circulation. Eating, does not affect the degree of absorption of the drug, but slows the rate of absorption. Depending on the filling of the stomach, C max is reached on average after 2-3 hours. The concentration in the plasma is in
linear dependence on the amount of the administered dose.
Distribution: communication with plasma proteins - more than 99% (most of it binds to albumins). The apparent volume of distribution of diclofenac in the body is on average 0.12-0.55 l / kg. Penetrates into breast milk, synovial fluid; C max in synovial fluid is observed 2-4 hours later than in plasma. T 1/2 from synovial fluid - 3-6 h (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 12h)
Metabolism: 50% of the drug is metabolized during the "first pass" through the liver. 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. The main metabolite of the drug (4'-hydroxydiclofenac) has a slight anti-inflammatory activity.
Excretion: Systemic, clearance is 260 ml / min. T 1/2 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
Symptomatic treatment of pain syndrome and inflammation, such as:
- arthritis (including rheumatoid arthritis), osteoarthritis, gout attacks;
- periarthritis, tendonitis, tenosynovitis, bursitis;
- post-traumatic and postoperative pain syndrome,
accompanied by inflammation.
DOSING MODE
Inside, entirely, on an empty stomach, without chewing and washing down with the necessary amount of liquid.
Dosage depends on the severity of clinical manifestations. The recommended dose for adults and adolescents over 15 years is 75 to 150 mg of diclofenac per day in one or two doses. The maximum single dose is 75 mg.
With rheumatic diseases, it may be necessary to take diclofenac for a long time. In such cases it is recommended to reduce the daily dose of the drug as much as possible (up to 75 mg / day).
SIDE EFFECT
Often - 1-10%; not often - 0.1-1%, rarely - 0.01-0.1%, very rarely - less than 0.001%, including individual cases.
It should be remembered that the intensity of side effects depends on the dose and varies in different patients. The risk of GI loss directly depends on the dose and duration of administration. The most common side effects are gastrointestinal lesions.
From the digestive system : often - nausea, vomiting and diarrhea, dyspepsia, flatulence, anorexia, abdominal pain, increased activity of aminotransferases; rarely - gastrointestinal ulcers (with or without bleeding or perforation), gastritis, gastrointestinal bleeding, bloody vomiting, melena or bloody diarrhea, hepatitis, jaundice;very rarely - colitis (including colitis with blood, exacerbation of ulcerative colitis or Crohn's disease), constipation, stomatitis, glossitis, esophageal damage, narrowing of the intestinal lumen, pancreatitis, fulminant hepatitis.
From the nervous system: often - headache, dizziness, weakness; rarely - drowsiness; very rarely - sensitivity disorders (including paresthesia), memory disorders, convulsions, anxiety, tremor, aseptic meningitis, night "nightmares", depression, disorientation.
From the senses: often - vertigo; very rarely - visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, a violation of taste sensations.
From the side of 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 - hematopoietic disorders (hemolytic and aplastic anemia, leukopenia, agranulocytosis, thrombocytopenia).
Allergic reactions: rarely anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure (BP) and shock; very rarely - angioedema (including face).
From the cardiovascular system: very rarely - palpitations, chest pain, heart failure, increased blood pressure, vasculitis, myocardial infarction.
On the part of the respiratory system: rarely - bronchial asthma (including dyspnea); very rarely - pneumonia.
On the side of the leather cover: often - a rash; rarely - hives; very rarely - bullous eruptions, erythema, including multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, including allergic.
Other: rarely - swelling.
CONTRAINDICATIONS
- erosive-ulcerative lesions of the gastrointestinal tract, inflammatory bowel disease in the acute stage;
- cerebrovascular bleeding or existing disorders
blood coagulability;
- oppression of bone marrow hematopoiesis;
- acute heart failure;
Decompensated heart failure;
- complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid (ASA) or other NSAIDs (including in the anamnesis);
- condition after aorto-coronary bypass surgery;
- marked renal failure (clearance of cretinin less than 30 ml / min), progressive kidney disease;
- severe hepatic impairment or active liver disease;
- confirmed hyperkalemia;
- III trimester of pregnancy and lactation;
- Children's age (up to 15 years);
- known hypersensitivity to diclofenac or to any of the
auxiliary substances;
With caution: ulcerative colitis, anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, Crohn's disease, chronic hepatic insufficiency, liver disease in history, hepatic porphyria, chronic heart failure, arterial hypertension, a significant decrease in the volume of circulating blood (including after extensive surgical intervention), cerebrovascular disease, coronary heart disease, peripheral arterial disease, elderly patients (including those receiving d urethics, weakened patients and with low body weight), bronchial asthma, simultaneous reception of glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including: acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors ( including citalopram, fluoxetine, paroxetine, sertraline), dyslipidemia / hyperlipidemia, diabetes mellitus, the presence of Helicobacter pylori infection, prolonged use of NSAIDs, chronic renal failure (creatinine clearance her 60 ml / min), smoking, frequent use of alcohol, severe somatic diseases, pregnancy I-II trimester.
PREGNANCY AND LACTATION
Complete data on the use of diclofenac during pregnancy are absent. Experiments on animals showed reproductive toxicity. The potential risk to humans is unknown. If possible, diclofenac should be avoided in the first and second trimesters of pregnancy. In cases of extreme need, diclofenac should be taken at minimal therapeutic doses for a short period of time.
Diclofenac is contraindicated in the third trimester of pregnancy. In connection with its mechanism of action, it is possible to suppress the ability of the myometrium to contract, prolong the period of pregnancy and childbirth, cardiovascular and renal toxicity of the fetus, and the appearance of tendencies for bleeding in the mother and child.
Diclofenac and its derivatives penetrate breast milk in small amounts, and therefore a short-term drug intake without interruption of feeding is possible. In cases where a longer
reception, as well as taking high doses, it is recommended to stop breastfeeding for a while.
In connection with the negative effect on fertility, women who want to become pregnant, the drug is not recommended. In patients with infertility (including undergoing examination) it is recommended to cancel the drug.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution in chronic kidney failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution in chronic liver failure, liver disease in history, hepatic porphyria.
APPLICATION FOR CHILDREN
Contraindicated for children under 15 years.
APPLICATION IN ELDERLY PATIENTS
With caution in elderly patients.
SPECIAL INSTRUCTIONS
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 (in including after extensive surgical intervention). If in such cases diclofenac is prescribed, it is recommended to monitor the kidney function as a precautionary measure.
In patients with renal insufficiency with CC less than 10 ml / min, the equilibrium concentration of metabolites in plasma should theoretically be significantly higher than in patients with normal renal function, but 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. To reduce the risk of developing adverse events from the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.
Influence on the ability to drive vehicles and drive mechanisms: during the treatment period, it is possible to reduce the speed of mental and motor reactions, so it is necessary to refrain from driving vehicles and practicing other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.
OVERDOSE
Symptoms: CNS disorders, such as headache, dizziness, drowsiness and loss of concentration. Pain in the abdomen, nausea, vomiting. There may also be bleeding in the digestive tract and impaired liver and kidney function.
Treatment: therapeutic measures for overdose. There is no special antidote.
DRUG INTERACTION
The intake of diclofenac raises the concentration in the plasma of digoxin of lithium preparations.
Reduces the effect of diuretics, against the background of potassium-sparing diuretics increases the risk of hyperkalemia; against the background of anticoagulants, antiaggregant and thrombolytic drugs (alteplase, streptokinase, urokinase) increases the risk of bleeding (more often in the gastrointestinal tract).
Reduces the effect of hypotensive and hypnotic drugs. Increases the likelihood of side effects (bleeding in the gastrointestinal tract) of other NSAIDs and glucocorticosteroids (GCS); toxicity of methotrexate and nephrotoxicity of cyclosporine due to an increase in their concentration in plasma.
ASA 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 drugs. Cefamandol, cefoperazone, cefotetan, valproic acid and plikamycin increase the incidence of hypoprothrombinemia.
Selective serotonin reuptake inhibitors increase the risk of bleeding in the gastrointestinal tract. Simultaneous administration with ethanol, colchicine, corticotropin and preparations of St. John's wort increases the risk of bleeding in the gastrointestinal tract.
Medicines that cause photosensitivity, increase the sensitizing effect of diclofenac to ultraviolet radiation.
Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its effectiveness and toxicity.
Antibacterial drugs from the quinolone group increase the risk of seizures.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
At a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 4 years.
