Diclofenac

General characteristics. Structure:

Active agent: 1 ml 1 amp. contains diclofenac of sodium of 25 mg; 75 mg

Excipients: benzyl alcohol, sodium metabisulphite, Mannitolum, sodium hydroxide, propylene glycol, water for and.

Pharmacological properties:

Diclofenac possesses antiinflammatory, 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.

Pharmacokinetics. Time of achievement of Cmax at use in oil in a dose of 75 mg - 15-30 min., the size Cmax – 1.9-4.8 (on average 2.7) mkg/ml. Later 3 h after introduction plasma concentration average 10% of maximum.
Communication with proteins of plasma - more than 99% (the most part contacts albumine).
Metabolism results from a repeated or single hydroxylation and a konjyugirovaniye with glucuronic acid. CYP2C9 takes part in metabolism of drug. Pharmacological activity of metabolites is lower, than diclofenac.
The system clearance makes 350 ml/min., Vd - 550 ml/kg. T1/2 - 2 h 65% of the entered dose is brought out of plasma 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:

For short-term treatment of pains of various genesis of moderate intensity:
— musculoskeletal system diseases (a pseudorheumatism, the psoriasis, juvenile chronic arthritis ankylosing a spondylarthritis; gouty arthritis, rheumatic defeat of soft tissues, an osteoarthrosis of peripheral joints and a backbone, including with a radicular syndrome);
— lumbago, sciatica, neuralgia;
— альгодисменорся, inflammatory processes of bodies of a small pelvis, including adnexitis;
— the posttraumatic pain syndrome which is followed by an inflammation;
— postoperative pain.

Route of administration and doses:

It is entered deeply in oil. A single dose for adults - 75 mg (1 ampoule). If necessary perhaps repeated introduction, but not earlier than in 12 h.
Use duration no more than 2 days, if necessary is daleeperekhodit on peroral, or rectal use of diclofenac.

Features of use:

Influence on ability to driving of motor transport and to control of mechanisms
The patients using drug need to abstain from the types of activity demanding the increased concentration of attention and bystry mental and motor reactions, alcohol intake.

Side effects:

From the alimentary system:> 1% - abdominal pains, feeling of abdominal distention, diarrhea, digestion disturbances, nausea, a lock, a meteorism, increase in activity of liver enzymes, a round ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding; <1% - vomiting, jaundice, a melena, emergence of blood to Calais, damage of a gullet, aphthous stomatitis, dryness of a mouth and mucous membranes, hepatitis (perhaps fulminantny current), a liver necrosis, cirrhosis, a gepatorenalny syndrome, appetite change, pancreatitis, holetsistopankreatit, colitis.

From nervous system:> 1% - a headache, dizziness; <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, weakness, a disorientation, dreadful dreams, feeling of fear.

From sense bodys:> 1% - a sonitus; <1% - a sight illegibility, a diplopia, taste disturbance, reversible or irreversible decrease in hearing, scotoma.

From integuments:> 1% - a skin itch, skin rash; <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:> 1% - a liquid delay; <1% - a nephrotic syndrome, a proteinuria, an oliguria, a hamaturia, intersticial nephrite, a papillary necrosis, an acute renal failure, an azotemia.

From system of a hemopoiesis: <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 (development of a necrotizing fasciitis, pneumonia).

From respiratory system: <1% - cough, a bronchospasm, throat hypostasis, a pneumonitis.

From cardiovascular system: <1% - increase in the ABP, congestive heart failure, premature ventricular contraction, thorax pain.

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

Local reactions at introduction in oil: burning, infiltrate, aseptic necrosis, necrosis of fatty tissue.

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 a GIT).

Reduces effects hypotensive and hypnagogues.

Increases probability of emergence of side effects of other non-steroidal anti-inflammatory drugs and glucocorticosteroid means (bleeding in a GIT), 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.

Co-administration with ethanol, colchicine, corticotropin and drugs of a St. John's Wort increases risk of development of bleedings in a GIT.

Diclofenac strengthens effect of the drugs causing a photosensitization.

The drugs blocking canalicular secretion increase concentration in diclofenac plasma, thereby, increasing its toxicity.

Contraindications:

— GIT erosive cankers (in an aggravation phase);
— bleedings from a GIT;
— "an aspirinovy triad";
— hemopoiesis disturbances;
— disturbances of a hemostasis (including hemophilia);
— pregnancy;
— lactation period;
— children's age (up to 18 years);
— hypersensitivity (including to other NPVP).

With care: anemia, bronchial asthma, congestive heart failure, arterial hypertension, an edematous syndrome, a liver or renal failure, alcoholism, inflammatory diseases of intestines, erosive and ulcer gastrointestinal diseases out of an aggravation, a diabetes mellitus, a state after extensive surgical interventions, the induced porphyria, advanced age, a diverticulitis, general diseases of connecting fabric.

Use of the drug DICLOFENAC for introduction in oil at pregnancy and feeding by a breast
It is contraindicated at pregnancy and in the period of a lactation.

Use at abnormal liver functions
With care: liver failure.

Use at renal failures
With care: renal failure.

Use for elderly patients
With care: advanced age.

Use for children
It is contraindicated to children up to 18 years.

Overdose:

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

Treatment: symptomatic therapy, artificial diuresis. The hemodialysis is ineffective.

Storage conditions:

List B. To store in the place, unavailable to children, at a temperature from 15 °C to 25 °C.

Issue conditions:

According to the recipe

Packaging:

Solution for introduction of 75 mg in oil / 3 ml: amp. 5 pieces.