Composition, form of production and packaging
The solution for the / m introduction is clear, colorless or slightly yellowish in color, without visible mechanical inclusions.
1 ml of 1 amp.
diclofenac sodium 25 mg 75 mg
Excipients: benzyl alcohol, propylene glycol, sodium disulfite, sodium hydroxide, water d / u.
3 ml - ampoules (5) - blisters (1) - packs of cardboard.
3 ml - ampoules glass (5) - plastic pallets (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory and antipyretic effects.
The main mechanism of its action consists in indiscriminate inhibition of the activity of the enzyme cyclooxygenase 1 and 2 (COX1 and COX2). which leads to a disruption of the metabolism of arachnid acid, a decrease in the synthesis of prostaglandins. prostacyclin and thromboxane.
The most effective for inflammatory pain. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain, morning stiffness, swelling of the joints, which improves the functional state of the joint. In injuries, in the postoperative period, diclofenac reduces pain and inflammatory edema. Like all NSAIDs, diclofenac has antiaggregant activity. In therapeutic doses, diclofenac practically does not exert an effect on the time of bleeding. With prolonged treatment, the analgesic effect of diclofenac does not decrease.
РўC max with 75% imidazole injection - 15-30 min. Connection with plasma proteins, mainly with albumins - 99%. Diclofenac actively penetrates into the synovial fluid, where it reaches 60-70% of serum concentrations. After 3-6 hours after IM, the concentration of the active substance and metabolites in the synovial fluid is higher than in the serum. Diclofenac from the synovial fluid is excreted faster than from the serum. 50% of the drug is metabolized during the "first pass" through the liver. It is almost completely metabolized in the liver, mainly by hydroxylation, followed by conjugation with glucuronic acid and sulfation.
T 1/2 is 1-2 hours. In mild violations of the liver or kidney T 1/2 remains unchanged. In patients with severe renal failure (CC less than 10 ml / min), 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 of the liver, the pharmacokinetic parameters do not change.
Approximately 70% of diclofenac is excreted by the kidneys in the form of pharmacologically inactive metabolites. Only 1% of the drug is excreted unchanged, the rest of the metabolites through the intestine.
In elderly patients, pharmacokinetic parameters without significant changes.
Diseases that require the achievement of a rapid anti-inflammatory or analgesic effect:
- inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease), gouty arthritis, arthritis in Reiter's disease, rheumatic soft tissue damage, osteoarthrosis of peripheral joints and spine, including radicular syndrome, tendovaginitis, periarthritis, bursitis, myositis, synovitis;
- pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboschialgia, posttraumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, algodismenorea, adnexitis, proctitis, toothache, renal and biliary colic.
Diclofenac is intended for symptomatic therapy and does not affect the progression of the disease.
Intramuscularly. Single dose for adults - 75 mg (1 ampoule). If necessary, repeated administration is possible, but not earlier than 12 hours (patients with renal colic can be re-administered after 30 minutes). When using other dosage forms diclofenac should not exceed the 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.
Do not mix Naklofen with other drugs in the same syringe.
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 digestive tract (vomiting with blood, melena, diarrhea with a trace of blood), gastrointestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, impaired liver function; very rarely - stomatitis, glossitis, dryness of the mucous membranes (including oral cavity), erosive-ulcerative lesions of the esophagus, diaphragm-like intestinal strictures, non-specific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, constipation, pancreatitis, fulminant hepatitis.
From the nervous system: often - headache, dizziness; rarely solitude; 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 senses: 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.
On the part of the organs of hematopoiesis: very rarely - thrombocytopenia, leukopenia, eosinophilia, 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, extrasystole, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.
On the part of the respiratory system: rarely - cough, bronchial asthma (including dyspnea); very rarely - pneumonitis, laryngeal edema.
On the part of 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.
Other: in the place of the / m introduction, irritation, pain, swelling and redness of the skin are possible.
- period after aortocoronary shunting;
- erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal hemorrhage;
- Inflammatory bowel diseases (including NNC, Crohn's disease) in the phase of exacerbation;
- cerebrovascular bleeding or other bleeding and hemostasis disorders;
- severe hepatic impairment or active liver disease;
- severe renal failure (QC less than 30 ml / min), including confirmed hyperkalemia, progressive kidney disease;
Decompensated heart failure;
- oppression of bone marrow hematopoiesis,
- III trimester of pregnancy, the period of breastfeeding;
- Children's age (up to 18 years);
- hypersensitivity (including other NSAIDs), complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa and paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including in the anamnesis).
With caution: coronary heart disease, cerebrovascular disease, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance 30-60 ml / min; anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, prolonged use of NSAIDs, frequent alcohol use, severe physical illnesses, induced porphyria, epilepsy, diverticulitis, systemic connective tissue diseases, a significant decrease in BCC (including after extensive surgical interventions), elderly patients (including those receiving diuretics, weakened patients and low body weight), pregnancy (I-II trimester), concomitant therapies (eg, warfarin), anti-aggregates (eg, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (eg, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetine, paroxetine, sertraline).
To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used as little as possible.
PREGNANCY AND LACTATION
The use of diclofenac in the I-II trimesters of pregnancy is possible only if the expected benefit exceeds the potential risk to the fetus. In the III trimester and during breastfeeding, Naklofen is contraindicated.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in severe renal failure (CK less than 30 ml / min), including confirmed hyperkalemia, progressive kidney disease.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in severe hepatic insufficiency or active liver disease.
APPLICATION FOR CHILDREN
Contraindicated in children under 18 years of age
APPLICATION IN ELDERLY PATIENTS
Use with caution in elderly patients.
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.
With long-term use of diclofenac, it is possible, although in rare cases, the development of serious hepatotoxic reactions, and therefore it is recommended to regularly examine the function of the liver.
Because of the important role of prostaglandins in maintaining renal blood flow, care should be taken when administering the drug to patients with cardiac or renal insufficiency, as well as in the treatment of elderly people taking diuretics and patients who for any reason have a decrease in circulating blood volume (for example , after extensive surgical intervention). If diclofenac is prescribed in such cases, it is recommended to monitor kidney function as a precautionary measure.
Caution should be given to diclofenac in patients with violations of blood coagulation, porphyria, epilepsy, as well as in patients receiving anticoagulants or fibrinolytics.
When carrying out long-term therapy, it is necessary to monitor the picture of peripheral blood, to conduct a fecal occult blood test.
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.
Patients taking the drug should refrain from drinking alcohol.
In infectious diseases, the anti-inflammatory and antipyretic effects of diclofenac sodium can mask the symptoms of these diseases.
It is not recommended to mix the Naklofen solution with other medicines in the same syringe.
Influence on the ability to manage motor vehicles and work with mechanisms
During the treatment period, it is possible to reduce the speed of mental and motor reactions, so it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
Symptoms: for parenteral administration, an overdose is unlikely. Clinical symptoms of an overdose with parenteral administration are similar to those that can occur when using other dosage forms: vomiting, bleeding from the gastrointestinal tract, diarrhea, dizziness, tinnitus, convulsions, increased blood pressure, depression
breathing; with a significant overdose - acute renal failure, hepatotoxic effect.
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 (significant association with proteins and intensive metabolism).
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, antiplatelet agents and thrombolytic drugs (alteplase, streptokinase, urokinase) increases the risk of bleeding (more gastrointestinal).
Reduces the effect of hypotensive and hypnotic drugs.
Increases the likelihood of side effects of other NSAIDs and glucocorticosteroids (bleeding from 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 effect of hypoglycemic drugs.
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.
Selective serotonin reuptake inhibitors increase the risk of bleeding from the digestive tract.
Simultaneous administration with ethanol, colchicine, corticotropin and preparations of St. John's wort increases the risk of bleeding in the digestive tract.
Medicines that cause photosensitivity, increase the sensitizing effect of diclofenac to ultraviolet radiation.
Drugs that block tubular secretion, increase the concentration in the plasma of diclofenac, thereby increasing its toxicity.
Antibacterial drugs from the quinolone group - the risk of seizures.
Do not mix Naklofen with other drugs in the same syringe.
Patients should inform doctors about the development of side effects.
TERMS OF RELEASE FROM PHARMACY
TERMS AND CONDITIONS OF STORAGE
List B. Store at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 5 years.