Diklak of an ampoule
Producer: Hexal AG (Geksal AG) Germany
Code of automatic telephone exchange: M01AB05
Release form: Liquid dosage forms. Solution for injections.
General characteristics. Structure:
Active agent: sodium diclofenac – 25 mg/ml.
Excipients: N-Acetylcysteinum, benzyl alcohol, Mannitolum, sodium hydroxide, propylene glycol, water for injections.
Diclofenac possesses the antiinflammatory, anesthetizing 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 the maximum concentration at intramuscular use in a dose of 75 mg – 15-30 min., the size of the maximum concentration – 1,9-4,8 (on average 2,7) mkg/ml. 3 hours later 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. The fermental P450 CYP2C9 system 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 hours. 65% of the entered dose are 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:
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, остероартроз peripheral joints and a backbone, including with a radicular syndrome, a tendovaginitis, a bursitis);
- neuralgia, a mialgiya, a lumbar ishialgia, the posttraumatic pain syndrome which is followed by an inflammation, postoperative pain, a headache, migraine, альгодисменорея, an adnexitis, a proctitis.
- Feverish syndrome.
Route of administration and doses:
It is entered deeply intramusculary. A single dose for adults – 75 mg (1 ampoule). If necessary perhaps repeated introduction, but not earlier than in 12 hours.
Use duration no more than 2 days, if necessary further is passed to peroral, or rectal use of diclofenac.
Features of use:
The patients using drug need to abstain from the types of activity requiring special attention and bystry mental and motor reactions, alcohol intake.
More often than 1% - abdominal pains, feeling of abdominal distention, diarrhea, nausea, a lock, a meteorism, increase in level of "hepatic" enzymes, a round ulcer with possible complications (bleeding, perforation), gastrointestinal bleeding;
More rare than 1% - vomiting, jaundice, a melena, emergence of blood to Calais, damage of a gullet, aphthous stomatitis, dryness of a mouth and mucous, hepatitis (perhaps fulminantny current), a liver necrosis, cirrhosis, a gepatorenalny syndrome, appetite change, pancreatitis, holetsistopankreatit, colitis.
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, weakness, a disorientation, dreadful dreams, feeling of fear.
More often than 1% - a skin itch, skin rash.
More rare than 1% - an alopecia, urticaria, eczema, toxic dermatitis, a mnogoformny exudative erythema, в.т.ч. Stephens-Jones's syndrome, a toxic epidermal necrolysis (Lyell's disease), the increased photosensitivity, punctulate hemorrhages.
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.
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 (development of a necrotizing fasciitis, pneumonia).
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 glucocorticoid 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.
Co-administration 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.
Hypersensitivity (в.т.ч. to other NPVP), digestive tract erosive cankers, a "aspirinovy" triad, disturbances of a hemopoiesis, disturbance of a hemostasis (including hemophilia), pregnancy, children's age (up to 18 years), the lactation period.
Anemia, bronchial asthma, congestive heart failure, arterial hypertension, edematous syndrome, liver or renal failure, alcoholism, inflammatory diseases of intestines, erosive and ulcer diseases of digestive tract 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.
Symptoms: vomiting, dizziness, a headache, short wind, consciousness opacification, children have myoclonic spasms, nausea, abdominal pain, bleedings, an abnormal liver function and kidneys.
Treatment: symptomatic therapy, artificial diuresis.
The hemodialysis is ineffective.
List B. In protected from light, the place, unavailable to children, at a temperature not above 25 °C.
According to the recipe
Solution for intramuscular introduction of 25 mg/ml.
On 3 ml in ampoules from colourless glass.
5 ampoules are placed in a cardboard box with cardboard partitions together with the application instruction.