Diclofenac - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Diclofenac has anti-inflammatory, analgesic and antipyretic effects. Indiscriminately inhibiting cyclooxygenase 1 and 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac promotes a significant reduction in the severity of pain, morning stiffness,swelling of the joints, which improves the functional state of the joint. With injuries, in the postoperative period diclofenac reduces pain and inflammatory swelling.

Pharmacokinetics:

The time to reach the maximum concentration with intramuscular application at a dose of 75 mg is 15-30 minutes, the maximum concentration is 1.9-4.8 (on average 2.7 μg / ml). After 3 hours after administration, the plasma concentration averages 10% of the maximum.

The connection with plasma proteins is more than 99% (most of it is associated with albumins). Metabolism occurs as a result of multiple or one-time hydroxylation and conjugation with glucuronic acid. The enzyme system P450 CYP2C9 takes part in the metabolism of the drug. The pharmacological activity of metabolites is lower than that of diclofenac.

The system clearance is 350 ml / min, the volume of distribution is 550 ml / kg. Half-life from the plasma - 2 hours 65% of the administered dose is excreted as metabolites by the kidneys; less than 1% is unchanged, the rest of the dose is excreted as metabolites with bile.

In patients with severe renal failure (creatinine clearance less than 10 ml / min), the excretion of metabolites with bile is increased, while there is no increase in their concentration in the blood.

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

Indications:

For short-term treatment of pain of different genesis of moderate intensity:

- diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis, gouty arthritis, rheumatic soft tissue damage, osteoarthrosis of the peripheral joints and spine (including radicular syndrome);

- lumbago, sciatica, neuralgia;

- algodismenorea, inflammatory processes of the pelvic organs, including adnexitis;

- post-traumatic pain syndrome, accompanied by inflammation;

- postoperative pain.

Contraindications:Hypersensitivity (including other NSAIDs or ancillary components), erosive-ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), bleeding from the gastrointestinal tract, inflammatory bowel disease in the phase of exacerbation (ulcerative colitis, Crohn's disease ), severe hepatic insufficiency, liver disease in acute period,expressed renal insufficiency (creatinine clearance less than 30 ml / min), hyperkalemia, complete or incomplete combination of bronchial asthma, recurrent nasal polyposis and paranasal sinuses and intolerance to acetylsalicylic acid, etc. NSAIDs (including in history), hematopoiesis, disorders hemostasis (including hemophilia), pregnancy (III trimester), children's age (up to 18 years), lactation period, period after aortocoronary shunting, patients with an increased risk of arterial thrombosis and thromboembolism, chronic heart nososudic insufficiency, ischemic heart disease, peripheral arterial disease and cerebrovascular disease.

Carefully:

Anemia, bronchial asthma, cerebrovascular diseases, ischemic heart disease, congestive heart failure, hypertension, peripheral arterial disease, edematous syndrome, hepatic or renal insufficiency, dyslipidemia / hyperlipidemia, diabetes, smoking, inflammatory diseases, alcoholism, inflammatory bowel disease, condition after extensive surgical interventions, induced porphyria,elderly age, diverticulitis, systemic connective tissue diseases, pregnancy I-II trimester, creatinine clearance less than 60 ml / min.

Anamnestic data on the development of gastrointestinal ulcer, presence of Helicobacter pylori infection, old age, prolonged use of NSAIDs, frequent alcohol consumption, severe physical illnesses.

Simultaneous therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).

Dosing and Administration:It is administered intramuscularly. Single dose for adults - 75 mg (1 ampoule). If necessary, repeated administration is possible, but not earlier than 12 hours later. When using other dosage forms, diclofenac should not be exceeded by a maximum daily dose of 150 mg.

Duration of use no more than 2 days, if necessary, further pass to oral, or rectal administration of diclofenac.

Side effects:

To reduce the risk of developing adverse events, use a minimally effective dose with a short course.

Often - 1-10%; sometimes 0.1-1%; rarely - 0,01-0,1%; very rarely - less than 0.01%, including individual cases.

From the digestive system: often - epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased activity of aminotransferases; rarely - gastritis, proctitis, bleeding from the gastrointestinal tract (vomiting with blood, melena, diarrhea with a trace of blood), ulcers of the gastrointestinal tract (with or without bleeding or perforation), hepatitis, jaundice, impaired liver function; very rarely - stomatitis, glossitis, damages of the esophagus, diaphragm-like intestinal textures (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease), constipation, pancreatitis, fulminant hepatitis.

From the nervous system: often - headache, dizziness; rarely - drowsiness; very rarely - a violation of sensitivity, incl. paresthesia, memory disorders, tremors, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis, disorientation, depression, insomnia, nightmares, irritability, mental disorders.

From the sense organs: often - vertigo; very rarely - visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, a violation of taste sensations.

From the urinary system: very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.

From the hematopoiesis: very rarely - thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis.

Allergic reactions: anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure and shock; very rarely - angioedema (including face).

From the cardiovascular system: very rarely - palpitations, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.

From the respiratory system: rarely - bronchial asthma (including dyspnea); very rarely - pneumonitis.

From the skin: often - skin rash; rarely - hives; very rarely - bullous eruptions, erythema, incl. multiform and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.

Local reactions with intramuscular injection: burning, infiltration, aseptic necrosis, necrosis of adipose tissue.

Overdose:

Symptoms: vomiting, dizziness, headache, dyspnea, confusion, in children - myoclonic cramps, nausea, vomiting, abdominal pain, bleeding, impaired liver and kidney function.

Treatment: symptomatic therapy, forced diuresis. Hemodialysis is ineffective.

Interaction:

Increases the concentration in the plasma digoxin, methotrexate, lithium and cyclosporine.

Reduces the effect of diuretics, against the background of potassium-sparing diuretics increases the risk of hyperkalemia; on the background of anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) - the risk of bleeding (more often from the gastrointestinal tract). Reduces the effects of hypotensive and hypnotics.

Increases the likelihood of side effects of other non-steroidal anti-inflammatory drugs and glucocorticosteroid agents (bleeding in the gastrointestinal tract), toxicity of methotrexate and nephrotoxicity of cyclosporine.

Acetylsalicylic acid reduces the concentration of diclofenac in the blood. Reduces the effect of hypoglycemic agents.

Cefamandol, cefoperazone, cefotetan, valproic acid and plikamycin increase the incidence of hypoprothrombinemia.

Cyclosporine and gold preparations increase the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which increases nephrotoxicity.

Simultaneous administration with ethanol, colchicine, corticotropin, selective serotonin reuptake inhibitors, St. John's wort increases the risk of bleeding in the gastrointestinal tract.

Diclofenac enhances the effect of drugs that cause photosensitivity. Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.

Special instructions:

To reduce the risk of developing adverse events from the gastrointestinal tract, a minimum effective dose should be used with the minimum possible short course.

Because of the important role of prostaglandins in maintaining renal blood flow, caution should be exercised in appointing patients with cardiac or renal insufficiency, and also in the treatment of elderly patients taking diuretics and patients who for any reason have a decrease in circulating blood volume (in t.ch.after extensive surgical intervention). If in such cases appoint diclofenac, recommend as a precautionary measure to monitor kidney function.

If the increase in the activity of "liver" transaminases persists or increases during the administration of the drug, if clinical symptoms of hepatotoxicity (including nausea, fatigue, drowsiness, diarrhea, pruritus, jaundice) are noted, treatment should be discontinued.

Diclofenac (like other NSAIDs) can cause hyperkalemia.

When performing long-term therapy, it is necessary to monitor liver function, the picture of peripheral blood, the analysis of feces for latent blood.

In connection with the negative effect on fertility, women who want to become pregnant, the drug is not recommended. In patients with infertility (including undergoing examination) it is recommended to cancel the drug. During the treatment period, it is possible to reduce the speed of mental and motor reactions, so it is necessary to refrain from driving transport and occupations with other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Solution for intramuscular injection 25 mg / ml.

Packaging:

3 ml in neutral glass ampoules. For 10 ampoules together with a vial for opening ampoules or a scarifier ampoule and instructions for use in a cardboard box. 5 ampoules are placed in a contour mesh package made of a polyvinyl chloride film.

1 or 2 contour mesh packages together with a vial for opening ampoules or a scarifier ampoule and instructions for use are placed in a pack of cardboard. When using ampoules with notches, rings and break points, the ampoule opener opener or ampoule scarifier is allowed not to be inserted.

Storage conditions:In the dark place at a temperature of 5 to 25 ° C. Keep out of the reach of children.

Shelf life:2 of the year. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001224

Date of registration:16.11.2011

Date of cancellation:2016-11-16

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Information update date: & nbsp09.02.2016

Illustrated instructions

Instructions

Diclofenac (Diclofenac)