Composition, form of production and packaging
Tablets of prolonged action, covered with a film membrane of reddish brown color, round, biconvex, smooth; on the fracture - a mass of white or almost white color, covered with a film shell of a reddish-brown color.
diclofenac sodium 100 mg
Excipients: sucrose, cetyl alcohol, povidone, silicon dioxide colloidal anhydrous, magnesium stearate.
The composition of the film shell: hypromellose, iron dye red oxide (E172), titanium dioxide, macrogol 6000, polysorbate 80, talc.
10 pieces. - blisters (2) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
Diclofenac is a non-steroidal anti-inflammatory drug that has analgesic, anti-inflammatory and antipyretic effects. The main mechanism of its action and associated side effects are indiscriminate inhibition of the activity of the enzyme cyclooxygenase 1 and 2 (COX1 and COX2), which leads to a disruption of the metabolism of arachidonic acid, a decrease in the synthesis of prostaglandins, prostacyclin and thromboxane. The synthesis of prostaglandins in the kidneys, mucous membrane of the stomach and synovial fluid decreases. The most effective for inflammatory pain. 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. In injuries, in the postoperative period, diclofenac reduces pain and inflammatory edema. Like all non-steroidal anti-inflammatory drugs (NSAIDs), diclofenac has antiplatelet activity. In therapeutic doses, diclofenac has virtually no effect on bleeding time. With prolonged treatment, the analgesic effect of diclofenac does not decrease.
As a result of sustained release of the drug, Cmax in the plasma is lower than that produced by the administration of a short-acting drug; however, it remains high for a long time after administration. C max - 0.5 Ојg / ml, TC max - 5 hours after taking 100 mg of prolonged action tablets. 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; Stach in the synovial fluid is observed 2-4 hours later than in the plasma. T 1/2 of the synovial fluid is 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. In the metabolism of the drug is also involved isoenzyme CYP2C9, the pharmacological activity of metabolites is less than diclofenac.
Systemic clearance is 260 ml / min. T 1/2 from 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.
- inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), gouty arthritis (in case of an acute attack it is preferable to use high-speed medicinal forms), arthritis in Reiter's disease, rheumatic soft tissue damage, osteoarthrosis peripheral joints and spine, including with radicular syndrome, tendovaginitis, periarthritis, bursitis, myositis, synovitis).
- pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboschialgia, posttraumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine (in case of an acute attack it is preferable to use high-speed medicinal forms), algodismenorea, adnexitis, proctitis, toothache, renal and biliary colic;
- in the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis);
Diclofenac is intended for symptomatic therapy and does not affect the progression of the disease.
Inside, the tablets should be swallowed whole, not liquid, squeezed enough water during or after a meal.
Naklofen CP, prolonged-action tablets, 100 mg should be used for long-term therapy. The initial and maintenance doses are 1 tablet per day. If necessary, increase the dose to 150 mg per day Naklofen CP should be combined with tablets or suppositories of Naclofen 50 mg.
Often - 1-10%; sometimes - 0.1-1%; rarely - 0.01-0.1%; very rarely - less than 0.01%, including individual cases.
On the part of the digestive system: often - epigastric pain, abdominal cramps, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases; rarely gastritis, proctitis, bleeding from the gastrointestinal tract (vomiting with blood, melena, diarrhea with a trace of blood), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, dysfunction of the liver; very rarely - stomatitis, glossitis, dryness of the mucous membranes (including the mouth), damage to the esophagus, diaphragm-like intestinal strictures (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease), constipation, pancreatitis, fulminant hepatitis).
From the nervous system: often - headache, dizziness; rarely - drowsiness; very rarely - a violation of sensitivity, incl. paresthesia, memory disorders, tremor, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia, nightmares, irritability, agitation, mental disorders.
From the senses: 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, edema.
On the part of the organs of hematopoiesis: very rarely - thrombocytopenia, leukopenia, eosinophilia, hemolytic and aplastic anemia, agranulocytosis.
Allergic reactions: anaphylactic, anaphylactoid reactions, including marked decrease in blood pressure (BP) and shock; very rarely - angioedema (including face), in some cases vasculitis.
From the cardiovascular system: very rarely - palpitations, tachycardia, extrasystole, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.
On the part of the respiratory system: rarely - cough, bronchial asthma (including dyspnea); very rarely - pneumonitis, laryngeal edema.
On the part of 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.
- period after aortocoronary shunting;
- erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding;
- Inflammatory bowel disease, in the phase of exacerbation (Nonspecific ulcerative colitis (NJC), Crohn's disease).
- cerebrovascular bleeding or other bleeding and hemostasis disorders;
- severe hepatic impairment or active liver disease;
- severe renal failure (creatinine clearance less than 30 ml / min), including confirmed hyperkalemia, progressive kidney disease;
Decompensated heart failure;
- oppression of bone marrow hematopoiesis;
- III trimester of pregnancy, the period of breastfeeding;
- Children's age (up to 18 years);
hypersensitivity to diclofenac; complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including in the anamnesis).
With caution: coronary heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance less than 60 ml / min; anamnestic data on the development of gastrointestinal ulcer, presence of Helicobacter pylori infection, advanced age, long-term use of nonsteroidal anti-inflammatory drugs (NSAIDs), frequent alcohol use, severe somatic diseases, induced porphyria, epilepsy, advanced age, diverticulitis, systemic connective tissue diseases , a significant decrease in the volume of circulating blood (BCC) (including after massive surgery), elderly patients (appointed in more(including those receiving diuretics, weakened patients and low body weight), concomitant therapy with the following drugs: anticoagulants (eg, warfarin), antiaggregants (eg, acetylsalicylic acid, clopidogrel), fibrinolytics, oral glucocorticoids (eg, prednisolone) , selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline). To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used as little as possible. Pregnancy I-II trimester.
PREGNANCY AND LACTATION
The use of diclofenac in pregnant women is possible only when the expected benefit exceeds the potential risk to the fetus. Diclofenac is not recommended for use during the last trimester of pregnancy.
Despite the fact that diclofenac is found in breast milk in small amounts, its use during breast-feeding is not recommended.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal failure (creatinine clearance less than 30 ml / min), including confirmed hyperkalemia, progressive kidney disease;
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe hepatic impairment or with active liver disease.
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years.
APPLICATION IN ELDERLY PATIENTS
Use with caution in elderly patients
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.
Caution should be used for ulcerative colitis and Crohn's disease because of a possible exacerbation of the disease.
With long-term use of diclofenac, it is possible, although in rare cases, the development of serious hepatotoxic reactions, and therefore it is recommended to regularly examine the function of the liver.
Because of the important role of prostaglandins in maintaining renal blood flow, care should be taken when administering the drug to 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 a major surgical intervention). If diclofenac is prescribed in such cases, it is recommended to monitor kidney function as a precautionary measure.
With caution, diclofenac should be prescribed in patients with severe renal or hepatic insufficiency, heart failure, blood clotting disorders, porphyria, epilepsy, and patients receiving anticoagulants or fibrinolytics.
When carrying out long-term therapy, it is necessary to monitor the picture of peripheral blood, to conduct a fecal occult blood test.
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.
Patients taking the drug should refrain from drinking alcohol.
In infectious diseases, the anti-inflammatory and antipyretic effects of diclofenac sodium can mask the symptoms of these diseases.
The amount of sucrose contained in the preparation does not affect patients with the following conditions: lactase enzyme deficiency, ralactosemia, and glucose / galactose uptake syndrome.
Impact on the ability to drive a car or other mechanical means
During the treatment period, it is possible to reduce the speed of mental and motor reactions, so it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
Symptoms: vomiting, nausea, abdominal pain, bleeding from the gastrointestinal tract, diarrhea, headache, dizziness, tinnitus, increased excitability, hyperventilation with increased convulsive readiness, convulsions, with a significant overdose - acute renal failure, hepatotoxic effect.
Treatment: gastric lavage, activated charcoal, symptomatic therapy aimed at eliminating blood pressure increase, renal dysfunction, seizures, gastrointestinal irritation, respiratory depression. Forced diuresis, hemodialysis are ineffective (significant association with proteins and intensive metabolism).
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; against the background of anticoagulants, antiplatelet agents and thrombolytic drugs (alteplase, streptokinase, urokinase) increases the risk of bleeding (more gastrointestinal).
Reduces the effect of hypotensive and hypnotic drugs.
Increases the likelihood of side effects of other NSAIDs and glucocorticosteroids (bleeding from 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.
Hypoglycemic agents - hypo- or hyperglycemia can be observed. With this combination of funds, it is necessary to monitor the concentration of glucose in the blood.
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 is manifested by increased nephrotoxicity.
Selective serotonin reuptake inhibitors increase the risk of bleeding from the digestive tract.
Simultaneous administration with ethanol, colchicine, corticotropin and preparations of St. John's wort increases the risk of bleeding in the digestive 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 toxicity.
Antibacterial drugs from the quinolone group - the risk of seizures.
TERMS OF RELEASE FROM PHARMACY
TERMS AND CONDITIONS OF STORAGE
Store in a dry place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 5 years.