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

1 ml of the solution contains 25 mg of diclofenac sodium and ancillary components: benzyl alcohol, propylene glycol, sodium hydroxide, mannitol, sodium pyrosulfite (sodium metabisulphite), water for injection.

Description:

Transparent lightly colored liquid with a weak smell of benzyl alcohol.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID).

ATX: & nbsp

S.01.B.C.03 Diclofenac

M.01.A.B.05 Diclofenac

Pharmacodynamics:

Diclofenac has an anti-inflammatory and analgesic effect. Indiscriminately inhibiting cyclooxygenase (COX) 1 and 2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the inflammatory focus.

Pharmacokinetics:

Quickly absorbed after intramuscular injection. The time to reach the maximum concentration when administered at a dose of 75 mg is 15-30 minutes, the maximum concentration is 1.9-4.8 (mean 2.7) μg / ml.After 3 hours after administration, plasma concentrations averaged 10% of the maximum.

It is metabolized in the liver mainly by oxidation and conjugation. About 99% is associated with plasma proteins, mainly with albumins. Approximately 2/3 of the administered dose is excreted in the urine, and the rest with bile. 72 hours after administration, almost 90% of the administered dose is excreted from the body. In the synovial fluid creates high concentrations. In a small amount penetrates into breast milk. 50% of the drug is metabolized by the "first pass" through the liver. The area under the concentration-time curve (AUC) is 2 times less after oral administration of the drug than after parenteral administration of the same dose. In patients with chronic hepatitis or compensated cirrhosis of the liver, the pharmacokinetic parameters do not change.

In patients with renal insufficiency with creatinine clearance less than 10 ml / min, the introduction of metabolites with bile is increased, so there is no increase in their concentration in the plasma.

Indications:

Inflammatory diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis, gouty arthritis, rheumatic soft tissue damage).

Degenerative diseases of the musculoskeletal apparatus (deforming osteoarthritis, osteochondrosis).

Lumbago, sciatica, neuralgia, myalgia, tendovaginitis, bursitis

Post-traumatic pain syndrome, accompanied by inflammation, post-operative pain, migraine, renal colic; primary algodismenorea, adnexitis, proctitis.

In the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis).

Feverish syndrome.

Contraindications:

Hypersensitivity (including to other NSAIDs), erosive and ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), bleeding from the gastrointestinal tract, "aspirin" asthma, hematopoiesis disorders, hemostasis disorders (incl. hemophilia), pregnancy, children's age (up to 15 years), lactation.

Carefully:anemia, bronchial asthma, congestive heart failure, arterial hypertension, edematous syndrome, hepatic or renal insufficiency, alcoholism, diverticulitis, erosive and ulcerative diseases of the gastrointestinal tract without exacerbation, diabetes, postoperative period,induced acute hepatic porphyria, elderly age.

Pregnancy and lactation:

Dosing and Administration:

It is administered intramuscularly. Single dose for adults - 75 mg (one ampoule). If necessary, repeated administration is possible, but not earlier than 12 hours later.

The duration of intramuscular injection of the drug should not exceed 2 days, then switch to oral administration.

Side effects:

Frequent adverse reactions - develop in more than 1 case for 100 appointments, not frequent - the frequency of development is less than 1 case per 100, but more than 1 case per 1000 prescriptions, and rare - the incidence of less than 1 case per 1000 prescriptions.

Co side of the digestive system:

frequent - NSAID-gastropathy (gastralgia and discomfort in the epigastric region, nausea, a feeling of stomach overflow, belching, heartburn, diarrhea, abdominal pain, flatulence), erosive and ulcerative lesions of the digestive tract (including lesions of the esophagus, stomach, peptic ulcer, multiple gastrointestinal lesions) ; perforation of the intestinal wall, bleeding from the gastrointestinal tract, dry mouth, constipation, pancreatitis, toxic hepatitis.

infrequent - vomiting, colitis or exacerbation, decreased appetite or anorexia, stomatitis, glossitis.

Co side of the nervous system:

frequent - headache, dizziness;

infrequent - cramps, aseptic meningitis, memory loss, depression, psychotic reactions, peripheral polyneuropathy (hyposthenia, tremor, pain or weakness in the muscles of the hands and feet), drowsiness, irritability and nervousness, fear, insomnia, weakness and fatigue.

Co side of the senses:

infrequent - toxic optic neuritis, decreased visual acuity, diplopia, scotoma, hearing loss and other hearing impairment, ringing and tinnitus.

Co skin: frequent - skin itch, skin rash (mainly erythematous and urticaria), ecchymosis, skin hyperemia;

infrequent - multi-form exudative erythema, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), photodermatitis.

Co the side of the genitourinary system: frequent - fluid retention;

infrequent - dysmenorrhea, hematuria, cystitis, pollakiuria, proteinuria, interstitial nephritis, nephrotic syndrome, oliguria or anuria, acute renal failure, peripheral edema.

Co sides of hemopoiesis: not frequent - agranulocytosis, hemolytic anemia, aplastic anemia, anemia associated with internal bleeding, ecchymosis, leukopenia, neutropenia, thrombocytopenia with or without purpura.

Co the respiratory system:

infrequent - shortness of breath.

Co cardiovascular system: frequent - increased blood pressure;

infrequent - arrhythmias, cardialgia, lowering blood pressure;

rare - chest pain, nasal bleeding, worsening of congestive heart failure.

Endocrine Disorders: rare - weight loss.

Allergic reactions: rare - anaphylaxis and anaphylactoid reactions, anaphylactic shock (usually develops rapidly), bronchospastic allergic reactions.

Other: rare - changes in the results of laboratory tests.

In the place of intramuscular injection: burning, infiltration, aseptic necrosis, necrosis of adipose tissue.

Overdose:Symptoms: dizziness, headache, dyspnea, turbidity, in children - myoclonic cramps, nausea, vomiting, abdominal pain, bleeding, impaired liver and kidney function. Treatment: symptomatic therapy aimed at eliminating the increase in blood pressure, violations of kidney function, seizures, irritation of the gastrointestinal tract, respiratory depression. Forced diuresis, hemodialysis are 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; against 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 glycocorticosteroid agents (bleeding in the gastrointestinal tract), toxicity of methotrexate and nephrotoxicity of cyclosporine.

Acetylsalicylic acid reduces the concentration of diclofenac in the blood.

Simultaneous use with paracetamol increases the risk of developing nephrotoxic effects of diclofenac.

Reduces the effectiveness 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 is manifested by increased nephrotoxicity.

Simultaneous administration with ethanol, colchicine, corticotropin and preparations of 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:

During the treatment with the drug should be a systematic control of the picture of peripheral blood, liver function, kidneys, examination of feces for the presence of blood.

Patients using the drug should refrain from activities that require increased attention and rapid mental and motor reactions, as well as from the use of alcohol.

Form release / dosage:

Solution for intramuscular injection 25 mg / ml.

Packaging:

For 3 ml in ampoules with a capacity of 3 ml or 5 ml of glass grade USP-1, HC-3 or X'G-1.

10 ampoules together with a knife or scarifier for opening ampoules and instructions for medical use are placed in a box of cardboard with a corrugated liner of corrugating paper.

In the case of using ampoules with a kink ring or with a notch and a break point, the insertion of a knife or scarifier for opening ampoules is not provided.

Storage conditions:List B.In a dark place out of the reach of children.

Shelf life:2 years. Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N016156 / 01

Date of registration:24.03.2010

The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Manufacturer: & nbsp

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Information update date: & nbsp17.02.2016

Illustrated instructions

Instructions

Diclofenac (Diclofenac)