Diclofenac

General characteristics. Structure:

Active ingredient: 25 mg of diclofenac of sodium.

Excipients: propylene glycol, mannitol, benzyl alcohol, sodium sulfite, feast; natron caustic 1M solution (sodium hydroxide), water for injections.

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

Pharmacological properties:

Pharmakodimika. NPVP derivative of phenylacetic acid, possesses antiinflammatory and obezbolivayuyoshchy action. Not selectively oppressing (TsOG) 1 and 2 cyclooxygenase, breaks metabolism of arachidonic acid, reduces quantity of prostaglanidin in the inflammation center. At a local primeyoneniye reduces hypostasis and pain at inflammatory processes of a noninfectious etiology.

Pharmacokinetics. It is quickly soaked up after intramuscular introduction. Time of achievement of the maximum kontsentrayotion at use in a dose of 75 mg of 15-30 min., the size of the maximum concentration - 1,9-4,8 (on average 2,7) mkg/ml. Later 3 h after introduction plasma concentration average 10% of maksimalyyony. Is exposed to metabolism in a liver, mainly, by oxidation and conjugation.

Approximately for 99,7% contacts plasma proteins, mainly, with albumine. About 2/3 entered doses are removed with urine, and other quantity with bile. In 72 h after introduction nearly 90% of the entered dose are brought out of an orgayonizm. In synovial fluid creates high concentration.

In insignificant quantity gets into breast milk. Patients with a renal failure at clearance of creatinine have less than 10 ml/min., equilibrium concentration of metabolites in plasma has to be theoretically much higher, than at patients with normal function of kidneys, however it really is not observed as in this situation removal of metabolites with bile usilivayotsya.

Indications to use:

Inflammatory diseases of a musculoskeletal system (pseudorheumatism, the psoriasis, yuvenialny chronic arthritis ankylosing a spondylitis, gouty arthritis).

Inflammatory processes in a small basin, an adnexitis, primary альгодисменорея, migraine, renal or bilious colic, a proctitis.

Pain syndrome (lumbago, sciatica, neuralgia, mialgiya, tendovaginitis, bursitis, rheumatic defeat of soft tissues, tooth and headache, migraine, etc. genesis of pain of moderate expressiveness); degenerativyony diseases basic двигателыюго the device (the deforming osteoarthrosis, osteochondrosis), the posttravyomatichesky pain syndrome which is followed by an inflammation; postoperative pains.

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, further is passed to oral administration.

Features of use:

Diclofenac is intended only for treatment of acute states. After subsiding of sharpness of a proyotsess it is necessary to pass to treatment with other forms of drug (tablets, suppositories, gel).

Duration of treatment should not exceed 2 days since there is an increased risk of development of by-effects. During treatment drug recommends to stop breastfeeding, and its vozobnovleyony has to be not earlier than 72 hours after the last administrations of drug.

When performing long therapy it is necessary to control function of a liver, a picture of periferiyochesky 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 occupations potentially dangerous types of activity, trebuyushchiyom of the increased concentration of attention and speed of psychomotor reactions is possible.

Side effects:

Frequent side reactions - develop more than in 1 case on 100 appointments, infrequent - frequency a razyovitiya less than 1 case on 100, but more than 1 cases on 1000 appointments, and rare - development frequency less than 1 case on 1000 appointments.

From the alimentary system: frequent - the NPVP-gastropathy (a gastralgia, nausea, vomiting, diarrhea, abdominal pain, a meteorism), digestive tract erosive cankers, bleeding from digestive tract (гематсмезис. a melena), nonspecific colitis with bleeding, dryness in a mouth, locks; infrequent - pancreatitis, afrotizny stomatitis, a glossitis, increase in activity of "hepatic" transaminases, toxic hepatitis (with jaundice or without jaundice), fulminant hepatitis.

From a nervous system: frequent - a headache, dizziness, increased fatigue, sleeplessness, uneasiness, "dreadful" dreams, disturbances of flavoring feelings; infrequent — a narusheyoniya of perception, paresthesia, decrease in memory, a disorientation, irritability, depressions, psychotic reactions, a loss of appetite; rare - spasms, a tremor, aseptic meningitis.

From sense bodys: infrequent - decrease in visual acuity, a diplopia, scotoma, decrease in hearing, a sonitus.

From integuments: frequent - a skin itch, skin rash (preferential erythematic and urtikarny), a Quincke's disease: infrequent - eczema, a photosensitization, an allergic purpura, a mnogoformny exudative erythema (including Stephens-Johnson's syndrome); seldom - an erythrosis, an alopeyotion, a toxic epidzhermalny necrolysis (Lyell's disease).

From an urinary system: frequent - a nephrotic syndrome (hypostases); infrequent - an acute renal failure, a hamaturia, a proteinuria. oliguria, intersticial nephrite, papillary necrosis, cystitis.

From bodies of a hemopoiesis: infrequent — thrombocytopenia, a leukopenia, anemia; rare - an agranulocytosis, a leukopenia, anemia; rare - an agranulocytosis, hemolitic anemia, aplastic anemia.

From a respiratory organs: infrequent - a bronchospasm. From CCC: frequent - heartbeat, a stethalgia, arrhythmias; infrequent - increase in the ABP, system anaphylactic reactions (including shock).

Endocrine frustration: rare - impotence. In the place in oil of introduction - 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 krovoyotecheniye (is more often from digestive tract).

Reduces effects hypotensive and hypnagogues. Increases probability of emergence of side effects of other NPVP and glucocorticosteroids (bleeding from a GIT), toxicity of a methotrexate and nephrotoxicity of cyclosporine.

Acetylsalicylic acid reduces concentration of diclofenac in blood. The simultaneous ispolzoyovaniye with paracetamol increases risk of development of nephrotoxic effects of diclofenac. Reduces gipokaliyemichesky effect of hypoglycemic means.

Tsefamandol, цефоперазон, цефотетан, valproic acid and пликамицин increase frequency razviyoty prothrombinopenias.

Cyclosporine and drugs of gold increase influence of diclofenac on synthesis of prostaglandin in kidneys that is shown by increase in nephrotoxicity.

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

Contraindications:

Hypersensitivity (including to other non-steroidal anti-inflammatory drugs), digestive tract erosive cankers (in an aggravation phase), "aspirinovy" asthma, hemopoiesis disturbances, pregnancy, children's age (up to 15 years), the lactation period.

With care - the induced acute hepatic porphyrias, heavy abnormal liver functions and kidneys, heart failure, advanced age.

Overdose:

Symptoms: dizziness, a headache, a hyperventilation of lungs, consciousness opacification, children have myoclonic spasms, nausea, vomiting, abdominal pains, bleedings, abnormal liver functions and kidneys.

Treatment: the symptomatic therapy directed to elimination of increase in the ABP, a naruyosheniye of function of kidneys, spasms, irritations of a GIT, respiratory depression. An artificial diuresis, гемоди­ализ are ineffective.

Storage conditions:

List B. In the place protected from light at a temperature not above 25 °C. In the place, unavailable to children, the Period of validity 2 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for intramuscular introduction. On 3 ml in ampoules. On 5 ampoules place in a blister strip packaging. 2 blister strip packagings in a pack from a cardboard for a retail container. On 10 ampoules will prevent in a box from a cardboard. On 10 ampoules place in a pack from a cardboard for a retail container with partitions or lattices, or a separator from a cardboard for a retail container or paper bag. Put the instruction on a medical use, a knife in each box, a pack ampoule or the scarificator ampoule. When using ampoules with notches, rings or points for a break the knife ampoule or the scarificator ampoule is not put.