Amp diclofenac. 3 ml No. 5

General characteristics. Structure:

Active ingredient: sodium diclofenac; 2-[(2,6 dichlorophenyl) amine] фенилацетат sodium; 1 ml of solution contains 25 mg of diclofenac of sodium;
excipients: benzyl alcohol, dinatrium эдетат (Trilonum of B), sodium metabisulphite (Е 223), water for injections. Main physical and chemical properties: almost colourless, transparent liquid.

Pharmacological properties:

Pharmacodynamics. Sodium diclofenac – non-steroidal anti-inflammatory drug, the non-selective blocker of cyclooxygenase possessing antiinflammatory, analgesic action and febrifugal effect. Braking of biosynthesis of prostaglandins is considered the main mechanism of effect of diclofenac. Prostaglandins play an important role in genesis of an inflammation, pain and fever.
At rheumatic diseases antiinflammatory and analgetichesky properties of diclofenac of sodium provide the clinical effect which is characterized by considerable reduction of expressiveness of such symptoms and complaints as a rest pain and at the movement, morning constraint and a swelling of joints.
In vitro sodium diclofenac in concentration, equivalent subjects which are reached at treatment of patients does not suppress biosynthesis of proteoglycans of cartilaginous tissue.
At the posttraumatic and postoperative inflammatory phenomena sodium diclofenac quickly stops pain (both spontaneous, and arising at the movement), reduces inflammatory hypostasis and hypostasis of a postoperative wound.
Drug causes considerable analgetichesky effect at the moderated and strongly expressed pain syndrome of not rheumatic genesis. Diclofenac of sodium is capable to eliminate pain and to reduce expressiveness of blood loss at primary dysmenorrhea. Sodium diclofenac, besides, has favorable effect on manifestations of attacks of migraine.

Pharmacokinetics. After intramuscular introduction of 75 mg of diclofenac absorption begins immediately. The maximum concentration in a blood plasma which average value makes about 2,5 mkg/ml (8 µmol/l) is reached approximately in 20 min. Right after its achievement note bystry decrease in concentration of drug in plasma. The amount of the soaking-up active agent is in linear dependence on drug dose size.
Area size under a curve "concentration time" (AUC) after intramuscular administration of diclofenac of sodium is approximately twice more, than after its oral or rectal administration as in the last cases about a half of amount of diclofenac is metabolized at the first passing through a liver. After repeated use of drug pharmacokinetic indicators do not change. On condition of observance of the recommended intervals between administrations of drug of cumulation it is not noted.
Distribution. Linkng with serum proteins makes (99,7%), it happens, generally to albumine (99,4%). The volume of distribution makes 0,12 - 0,17 l/kg of body weight.
Diclofenac gets into synovial fluid where its maximum concentration is reached on 2 - 4 h later, than in a blood plasma. The elimination half-life makes 3 - 6 h of synovial fluid. In 2 h after achievement of the maximum concentration in a blood plasma concentration of diclofenac in synovial fluid is higher, than in a blood plasma, and its values remain higher during 12 h. Metabolism of diclofenac is carried out partially by a glyukuronization of not changed molecule, but, mainly, by means of a single and repeated metoksilirovaniye that causes formation of several phenolic metabolites (3-gidroksi-, 4-gidroksi-, 5-gidroksi-, 4, 5-digidroksi-and 3-hydroxy-4-metoksidiklofenaka), the majority of which turns into glyukuronidny conjugates. Two of these phenolic metabolites are biologically active, but it is much less, than diclofenac.
The general system plasma clearance of diclofenac makes 263 ± 56 ml/min. The final elimination half-life makes 1 - 2 h. The elimination half-life of four metabolites, including two pharmacological active, is also short and makes 1 - 3 h. One of metabolites, 3-hydroxy-4-metoksidiklofenak, has longer elimination half-life, however this metabolite is completely inactive.
Removal. About 60% of the applied dose of drug are removed with urine in the form of glucuronic conjugates of not changed active agent, and also in the form of metabolites, the majority of which  is represented by glucuronic conjugates. In not changed look less than 1% of diclofenac are removed. The rest of the applied dose of drug is removed in the form of metabolites with bile and a stake.
Pharmacokinetics in separate groups of patients. At patients with a renal failure at purpose of diclofenac of sodium in usual single doses of accumulation of diclofenac it was not noted. If the clearance of creatinine makes less than 10 ml/min., settlement equilibrium concentration of hydroxymetabolites of diclofenac are about 4 times higher, than at healthy patients. But eventually metabolites are removed with bile.
At patients with chronic hepatitis or the compensated cirrhosis indicators of pharmacokinetics of diclofenac are similar to that at patients without liver diseases.

Indications to use:

Inflammatory and degenerative forms of rheumatic diseases (the pseudorheumatism ankylosing a spondylitis, an osteoarthrosis, a spondylarthritis), pain in a backbone, the rheumatic diseases of extraarticular soft tissues, a bad attack of gout, posttraumatic and postoperative pain syndromes which are followed by an inflammation and hypostasis, migraine attacks, renal and bilious colic.

Route of administration and doses:

Apply the adult in the form of intramuscular injections. It is not necessary to apply sodium diclofenac injections more than 2 days in a row. In need of treatment continuation drug is used in the form of tablets or suppositories rectal.
When carrying out intramuscular injections to avoid injury of nerves or other fabrics to the place of an injection, it is recommended to follow the following rules:
the drug should be administered deeply intramusculary in an upper outside quadrant of a gluteus, the dose usually makes 75 mg (contents of 1 ampoule) of 1 times a day, in hard cases (for example, at gripes) as the exception can be made 2 injections on 75 mg with an interval in several hours (the second injection needs to be made in other buttock); as the alternative, solution can be combined with other dosage forms of means (tablets, suppositories rectal), at the same time the maximum daily dose should not exceed 150 mg.

Incompatibility. It is not necessary to mix sodium diclofenac solution with solutions of other medicines for injections.

Features of use:

During treatment gastrointestinal bleeding can arise sodium diclofenac at any time or develop the digestive tract ulcer which sometimes is complicated by perforation; and not always symptoms harbingers of these complications or existence of anamnestic data on a canker take place. More serious effects of these complications can be noted at patients of advanced age. In some cases, when at the patients receiving sodium diclofenac these complications, treatment by drug develop it is necessary to cancel.
At the patients who were earlier not receiving sodium diclofenac during treatment by drug, as well as during therapy by other NPVP, allergic reactions, including anaphylactic and anaphylactoid reactions in rare instances can develop.
Sodium diclofenac, thanks to the pharmakodinamichesky properties, can mask the complaints and symptoms characteristic of infectious and inflammatory diseases.
Development of reactions of hypersensitivity to the sodium metabisulphite which is a part of injection solution is possible.
During use of diclofenac of sodium careful medical observation of patients with diseases of digestive tract or a canker of a stomach or intestines in the anamnesis is necessary; patients with ulcer colitis or disease Krone, and also patients with abnormal liver functions.
During use of diclofenac of sodium as well as other NPVP, the level of one or several liver enzymes can increase. Therefore at long therapy by diclofenac of sodium the regular research of function of a liver is necessary. If disturbances from functional indicators of a liver remain or amplify, appear complaints or the symptoms indicating liver diseases develop and also if there are other by-effects (for example, an eosinophilia, rash, etc.), reception of diclofenac of sodium should be cancelled. It must be kept in mind that hepatitis against the background of reception of diclofenac of sodium can arise without the prodromal phenomena.
Care is necessary at purpose of diclofenac of sodium for patients with a hepatic porphyria as drug can provoke porphyria attacks. As prostaglandins play an important role in maintenance of a renal blood-groove, extra care is required at treatment of patients with dysfunctions of heart or kidneys, patients of advanced age, the patients receiving diuretic means, and also patients who have a considerable reduction of volume of the circulating plasma of any etiology, for example during the period before and after massive surgical interventions. In these cases during use of diclofenac of sodium regular control of function of kidneys is recommended as a precautionary measure. Drug phase-out usually causes recovery of function of kidneys to initial level. At prolonged use of diclofenac of sodium, as well as other NPVP, systematic control of a picture of peripheral blood is shown.
Sodium diclofenac, as well as other NPVP, can temporarily inhibit aggregation of thrombocytes. Therefore at patients with disturbances of a hemostasis careful control of the corresponding laboratory indicators is necessary.
Considering the general medical provisions, care at use of diclofenac of sodium is necessary also at patients of advanced age. It is especially urgent at patients of advanced age who are weakened or have insufficient body weight, they are recommended to appoint drug in a minimal effective dose.
It is necessary to be especially careful at intramuscular administration of diclofenac of sodium by the patient with bronchial asthma (because of risk of strengthening of expressiveness of symptoms of a disease), and also to patients with allergic rhinitis (including seasonal) and polyps of a mucous membrane of a nose.

Ability to influence speed of response at control of motor transport or work with other mechanisms. At use of drug it is necessary to refrain from management of transport and performance of other potentially dangerous types of activity which require special attention and speed of psychomotor reactions.

Use during pregnancy or feeding by a breast. During pregnancy use of drug is contraindicated. In need of purpose of drug in the period of a lactation feeding by a breast needs to be stopped.

Children. To children aged up to 18 years appoint sodium diclofenac in other dosage form.

Side effects:

At assessment of frequency of various side reactions  such gradation are used: often –> 10%, sometimes –> 1 - 10%, is rare –> 0,001 - 1%, in some cases – <0,001%.
From digestive tract: sometimes – pain in epigastric area, nausea, vomiting, diarrhea, spasms in a stomach, dyspepsia, abdominal distention, anorexia; seldom – gastrointestinal bleeding (a hematemesis, a melena, diarrhea with blood impurity), stomach ulcer and intestines which are followed or are not followed by bleeding or perforation; in some cases – aphthous stomatitis, a glossitis, changes from a gullet, formation of diafragmopodobny strictures in intestines, disturbances from lower parts of intestines, such as nonspecific hemorrhagic colitis, exacerbation of nonspecific ulcer colitis or disease Krone, locks, pancreatitis.
From TsNS: sometimes – a headache, dizziness; seldom – drowsiness; in some cases – sensitivity disturbances, including paresthesia, dysmnesias, a disorientation, sleeplessness, irritability, spasms, a depression, feeling of alarm, nightmares, a tremor, psychotic reactions, aseptic meningitis.
From sense bodys: in some cases – vision disorders (sight misting, a diplopia), hearing disorder, a sonitus, disturbances of flavoring feelings.
Dermatological reactions: sometimes – skin rash; seldom – a small tortoiseshell; in some cases – rashes in the form of bubbles, eczema, a multiformny erythema, Stephens-Johnson's syndrome, a Lyell's disease (an acute toxic epidermolysis), an erythrosis (exfoliative dermatitis), a hair loss, photosensitive reactions; purpura, including allergic.
From kidneys: seldom – hypostases; in some cases – an acute renal failure, changes of an urocheras (a hamaturia and a proteinuria), intersticial nephrite; nephrotic syndrome; papillary necrosis.
From a liver: sometimes – increase in level of aminotransferases in blood serum;
seldom – the hepatitis which is followed or not followed by jaundice; in some cases – fulminant hepatitis.
From system of a hemopoiesis: in some cases – thrombocytopenia, a leukopenia, hemolitic anemia, aplastic anemia, an agranulocytosis.
Hypersensitivity reactions: seldom – hypersensitivity reactions, such as bronchial asthma, system anaphylactic/anaphylactoid reactions, including arterial hypotension; in some cases – a vasculitis, pneumonia.
From cardiovascular system: in some cases – tachycardia, a stethalgia, arterial hypertension, congestive heart failure.
Others: sometimes – reactions in the place of an intramuscular injection in the form of local pain and consolidation; in some cases – local abscesses and necroses in the place of an intramuscular injection.

Interaction with other medicines:

Lithium, digoxin. Diclofenac of sodium can increase concentration of lithium and digoxin in a blood plasma.
Diuretic means. Diclofenac of sodium as well as other NPVP, can reduce expressiveness of diuretic action. Simultaneous use of kaliysberegayushchy diuretics can cause increase in level of potassium in blood serum (in case of such combination of medicines this indicator should be controlled often).
NPVP. The combined system use of NPVP can increase the frequency of emergence of the undesirable phenomena.
Anticoagulants. There are separate messages on increase in risk of bleedings at the patients accepting at the same time diclofenac of sodium and anticoagulants. Therefore in case of such combination careful and regular observation of patients is recommended.
Antidiabetic drugs. Perhaps simultaneous use of diclofenac of sodium and antidiabetic drugs, at the same time efficiency of the last does not change. However separate messages on development in such cases both a hypoglycemia, and a hyperglycemia are known that caused need of change of a dose of sugar-lowering drugs during sodium diclofenac use.
Methotrexate. It is necessary to be careful at purpose of NPVP less than for 24 h to or after reception of a methotrexate as in such cases increase in concentration of a methotrexate in blood and strengthening of its toxic action is possible.
Cyclosporine. Influence of NPVP on synthesis of prostaglandins in kidneys can increase nephrotoxicity of cyclosporine.
Antibacterial agents – derivatives of a hinolon. The patients receiving at the same time derivative hinolon and NPVP have separate messages on development судорг.

Contraindications:

Hypersensitivity to diclofenac of sodium and other components of drug, and also to other non-steroidal anti-inflammatory drugs. Digestive tract erosive cankers (in an aggravation phase), "acetilsalicylic" asthma, a "acetilsalicylic" triad (simultaneous development of bronchial asthma, recurrent a polypose of a nose and okolonosovy bosoms, intolerance of acetylsalicylic acid and drugs of a pyrazolon row), oppression of a marrowy hemopoiesis. Period of pregnancy and feeding by a breast. Children's age up to 18 years.

Overdose:

Symptoms: dizziness, a headache, consciousness opacification, nausea, vomiting, pains in epigastric area, a sonitus, excitement, respiratory depression, spasms, an abnormal liver function and kidneys, arterial hypotension.
Treatment: Treatment of overdose of NPVP (non-steroidal anti-inflammatory drugs) is the cornerstone of the supporting and symptomatic therapy. The artificial diuresis, a hemodialysis or hemoperfusion for removal of NPVP are inefficient as active agents of these drugs substantially contact proteins of plasma and are exposed to intensive metabolism.

Storage conditions:

To store in the place protected from light at a temperature not above 25 °C.
To store in the place, unavailable to children.

Period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

On 3 ml in ampoules; on 5 ampoules in a pack cardboard; on 100 ampoules in a box cardboard.