Diclofenac

General characteristics. Structure:

Active ingredient: 0,025 g of diclofenac of sodium.

Excipients: sugar milk (lactose monohydrate), granulated sugar (sucrose), potato starch, polyvinylpirrolidone (povidone), stearic acid.

Structure of a kishechnorastvorimy cover: целлацефат, titanium dioxide, dye tropeolin Oh, liquid paraffin, castor oil medical.

Diclofenac possesses the antiinflammatory, anesthetizing, analgeziruyushchy and febrifugal action.

Pharmacological properties:

Pharmacodynamics. Diclofenac possesses the antiinflammatory, anesthetizing, analgeziruyushchy and febrifugal action. Not selectively oppressing cyclooxygenase 1 and 2, breaks metabolism of arachidonic acid, reduces amount of prostaglandins in the inflammation center.

At rheumatic diseases antiinflammatory and analgeziruyushchy effect of diclofenac promotes considerable reduction of expressiveness of pain, morning constraint, a swelling of joints that improves a functional condition of a joint. At injuries, in the postoperative period diclofenac reduces pain and inflammatory hypostasis. As all NPVP, drug renders anti-modular activity.

Pharmacokinetics. Absorption - bystry and full, food slows down absorption speed on 1 - 4 hour and reduces the maximum concentration of diclofenac in plasma by 40%. After oral administration of 25 mg the maximum concentration (Cmax) – 1,0 mkg/ml are reached through - 2-3 h. Concentration in plasma is in linear dependence on size of the entered dose.

Change of pharmacokinetics of diclofenac against the background of repeated introduction is not noted, diclofenac does not kumulirut. Bioavailability – 50%. Communication with proteins of plasma - more than 99% (the most part contacts albumine). Gets into synovial fluid; the maximum concentration in synovial fluid is observed on 2-4 h later, than in plasma. An elimination half-life from synovial fluid of 3-6 h (concentration of active agent in synovial fluid in 4-6 h after administration of drug is higher, than in plasma, and remains higher during 12 h).

The interrelation of concentration of diclofenac in sinovilny liquid with its clinical performance is not found out. Metabolism: 50% of active agent are exposed to metabolism during "the first passing" through a liver. Metabolism results from a repeated or single hydroxylation and a konjyugirovaniye with glucuronic acid. CYP2C9 isoenzyme takes part in metabolism of drug. Pharmacological activity of metabolites is lower, than diclofenac.

The system clearance makes 350 ml/min., distribution volume – 550 ml/kg. Plasma elimination half-life - 2 h 65% of the entered dose is removed in the form of metabolites by kidneys; less than 1% are removed in not changed look, other part of a dose is removed in the form of metabolites with bile.

At patients with the expressed renal failure (clearance of creatinine less than 10 ml/min.) removal of metabolites with bile increases, at the same time increase in their concentration in blood is not observed.

At patients with chronic hepatitis or the compensated cirrhosis pharmacokinetic parameters of diclofenac do not change. Diclofenac gets into breast milk.

Indications to use:

Inflammatory and degenerative diseases of a musculoskeletal system, including the rhematoid, psoriasis, juvenile chronic arthritis ankylosing a spondylitis (Bekhterev's disease), an osteoarthrosis, gouty arthritis, a bursitis, a tendovaginitis.

Drug is intended for symptomatic therapy, reduction of pain and an inflammation at the time of use, does not influence progressing of a disease.

Pain syndrome: head (including migraine) and a dentagra, a lumbago, an ischialgia, an ossalgiya, neuralgia, a mialgiya, an arthralgia, radiculitis, at oncological diseases, the posttraumatic and postoperative pain syndrome which is followed by an inflammation.

Algodismenorey; inflammatory processes in a small basin, including an adnexitis.

Infectious and inflammatory diseases the ENT SPECIALIST - bodies with the expressed pain syndrome (as a part of complex therapy): pharyngitis, tonsillitis, otitis.

Route of administration and doses:

Inside. For achievement of bystry desirable therapeutic effect accept in 30 min. prior to meal. In other cases accept to, in time or after food, in not chewed look, washing down with enough water.

To adults and teenagers since 15 years - on 25-50 mg 2-3 times a day. At achievement of optimum therapeutic effect the dose is gradually reduced and pass to the supporting treatment in a dose 50 mg/days.

The maximum daily dose - 150 mg. 

At a juvenile pseudorheumatism the daily dose can be increased to 3 mg/kg of body weight.

Approximate mode of use of drug:
Age (body weight, kg)                   Single dose                                           Daily dose
                                              (quantity of tablets, [mg])                 (quantity of tablets, [mg])
6-7 years                                  (20-24) 1                                                  [25] 1 [25]

8-11 years                                 (25-37) 1                                               [25] 2-3 [50-75]

12-14 years                                                                      (38-50) 1-2 [25-50] 3-4 [75-100]

15 years and adults                  1-2 [25-50]                                         2-6 [50-150] are more senior

Features of use:

At patients with a liver failure (chronic hepatitis, the compensated cirrhosis) the kinetics and metabolism do not differ from similar processes at patients with normal function of a liver. When performing long therapy it is necessary to control function of a liver, a picture of peripheral blood, the analysis a calla on the occult blood.

During treatment reduction of speed of mental and motor reactions therefore it is necessary to abstain from driving of motor transport and occupations other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions is possible.

Use at pregnancy and during breastfeeding. In I and II trimesters of pregnancy it has to be applied according to strict indications and in the smallest dosage. Diclofenac gets into breast milk. In need of purpose of drug in the period of a lactation breastfeeding should be stopped.

Side effects:

From gastrointestinal trakta:chashche 1% - abdominal pain or a spasm, feeling of abdominal distention, diarrhea, nausea, a lock, a meteorism, increase in activity "hepatic" транаминаз, a round ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding without ulcer; more rare than 1% - vomiting, jaundice, a melena, emergence of blood to Calais, damage of a gullet, aphthous stomatitis, dryness of mucous membranes (including oral cavities), hepatitis (perhaps fulminant current), a liver necrosis, cirrhosis, a gepatorenalny syndrome, appetite change, pancreatitis (including with the accompanying hepatitis), holetsistopankreatit, colitis.

From a nervous system: more often than 1% - a headache, dizziness; more rare than 1% - a sleep disorder, drowsiness, a depression, irritability, aseptic meningitis (is more often at patients with a system lupus erythematosus and other general diseases of connecting fabric), spasms, the general weakness, a disorientation, dreadful dreams, feeling of fear.

From sense bodys: more often than 1% - a sonitus; more rare than 1% - an illegibility of visual perception, a diplopia, taste disturbance, reversible or irreversible decrease in hearing, scotoma.

From integuments: more often than 1% - a skin itch, skin rash; more rare than 1% - an alopecia, urticaria, eczema, toxic dermatitis, a mnogoformny exudative erythema (including Stephens-Johnson's syndrome), a toxic epidermal necrolysis (Lyell's disease), the increased photosensitivity, punctulate hemorrhages.

From urinogenital system: more often than 1% - a liquid delay; more rare than 1% - a nephrotic syndrome, a proteinuria, an oliguria, a hamaturia, intersticial nephrite, a papillary necrosis, an acute renal failure, an azotemia.

From bodies of a hemopoiesis and immune system: more rare than 1% - anemia (including hemolitic and aplastic anemias), a leukopenia, thrombocytopenia, an eosinophilia, an agranulocytosis, a Werlhof's disease, deterioration in a course of infectious processes (including development of a necrotic fasciitis).

From respiratory system: more rare than 1% - cough, a bronchospasm, throat hypostasis, a pneumonitis.

From cardiovascular system: more rare than 1% - increase in arterial pressure; congestive heart failure, premature ventricular contraction, thorax pain.

Allergic reactions: more rare than 1% - anaphylactoid reactions, an acute anaphylaxis (usually develops promptly), hypostasis of lips and language, an allergic vasculitis.

Interaction with other medicines:

Increases concentration in plasma of digoxin, a methotrexate, drugs of lithium and cyclosporine.

Reduces effect of diuretics, against the background of kaliysberegayushchy diuretics the risk of a hyperpotassemia amplifies; against the background of anticoagulants, thrombolytic means (an alteplaza, Streptokinasa, an urokinase) - risk of bleedings (is more often from digestive tract).

Reduces effects hypotensive and hypnagogues. Increases probability of emergence of side effects of other NPVP and glucocorticosteroid means (bleeding in digestive tract), toxicity of a methotrexate and nephrotoxicity of cyclosporine.

Acetylsalicylic acid reduces concentration of diclofenac in blood.

Simultaneous use with paracetamol increases risk of development of nephrotoxic effects of diclofenac. Reduces effect of hypoglycemic means.

Tsefamandol, цефоперазон, цефотетан, valproic acid and пликамицин increase the frequency of development of a prothrombinopenia.

Cyclosporine and drugs of gold increase influence of diclofenac on synthesis of prostaglandins in kidneys that increases nephrotoxicity. Simultaneous use with ethanol, colchicine, corticotropin and drugs of a St. John's Wort increases risk of development of bleedings in digestive tract.

Diclofenac strengthens effect of the drugs causing a photosensitization. The drugs blocking canalicular secretion increase concentration in diclofenac plasma, thereby, increasing its toxicity.

Antibacterial medicines from group of a hinolon – risk of development of spasms.

Contraindications:

Hypersensitivity (including to other NPVP), a full or incomplete combination of bronchial asthma, the nose recuring a polypose and okolonosovy bosoms and intolerance of acetylsalicylic acid (ASK) or other NPVP (including in the anamnesis), erosive cankers of a stomach and a 12-perstny gut, active gastrointestinal bleeding, inflammatory diseases of intestines, heavy liver and heart failure; the period after performing aortocoronary shunting; a heavy renal failure (the clearance of creatinine (CC) less than 30 ml/min.), the progressing diseases of kidneys, an active disease of a liver, the confirmed hyperpotassemia, pregnancy (the III trimester), the lactation period, children's age (up to 6 years – for the tablets covered with a kishechnorastvorimy cover of 25 mg).

Hereditary lactose intolerance, glucose galactose absorption disturbance, insufficiency of lactase.

With care. Peptic ulcer of a stomach and 12-perstny gut, ulcer colitis, disease Krone, liver diseases in the anamnesis, a hepatic porphyria, the chronic heart failure (CHF), arterial hypertension, considerable decrease in the volume of the circulating blood (VCB) (including after extensive surgical intervention), elderly patients (including the receiving diuretics weakened patients and patients with low body weight), bronchial asthma, a concomitant use of glucocorticosteroids (GKS) (including Prednisolonum), anticoagulants (including warfarin), antiagregant (including ASK, a klopidogrela), selective serotonin reuptake inhibitors (including a tsitaloprama, fluoxetine, a paroksetin, sertraline), the coronary heart disease (CHD), cerebrovascular diseases, a dislipidemiya/giper-lipidemiya, a diabetes mellitus, diseases of peripheral arteries, smoking, the chronic renal failure (CRF) (KK of 30-60 ml/min.), existence of an infection of Helicobacter pylori, prolonged use NPVP, alcoholism, heavy somatopathies.

Overdose:

Symptoms: vomiting, dizziness, a headache, short wind, stupefaction, children have myoclonic spasms, nausea, vomiting, abdominal pain, bleedings, an abnormal liver function and kidneys.

Treatment: a gastric lavage, administration of absorbent carbon, the symptomatic therapy directed to elimination of increase in arterial pressure, a renal failure, spasms, irritation of digestive tract, respiratory depression. The artificial diuresis, a hemodialysis are ineffective.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. In the place, unavailable to children, the Period of validity 3 years. Not to use after the expiry date specified on packaging

Issue conditions:

According to the recipe

Packaging:

The tablets covered with a kishechnorastvorimy cover of 25 mg. On 10 tablets in blister strip packagings. 3 planimetric packagings together with the application instruction place in a pack.