Description of the drug DICLOFENAC-LF for systemic use
The dose is selected individually; it is recommended to use the drug in the minimum effective dose, with the shortest possible treatment period.
For oral and rectal use
Adults
When taken orally in the form of tablets of regular duration or rectally in the form of suppositories, the recommended initial dose is 100-150 mg/day. In relatively mild cases of the disease, as well as for long-term therapy, 75-100 mg/day is sufficient. The daily dose should be divided into several doses.
When taken in the form of extended-release tablets, the recommended initial dose is 100 mg 1 time / day. The same daily dose is used for moderately severe symptoms, as well as for long-term therapy. In cases where the symptoms of the disease are most pronounced at night or in the morning, it is advisable to take extended-release tablets at night.
To relieve night pain or morning stiffness
in addition to taking the drug during the day, diclofenac is prescribed in the form of rectal suppositories before bedtime; in this case, the total daily dose should not exceed 150 mg.
With primary dysmenorrhea
the daily dose is selected individually; usually it is 50-150 mg. The initial dose should be 50-100 mg; if necessary, over several menstrual cycles it can be increased to 150 mg/day. The drug should be started when the first symptoms appear. Depending on the dynamics of clinical symptoms, treatment can be continued for several days.
In elderly patients (65 years and older)
no adjustment of the initial dose is required.
In weakened patients, patients with low body weight
It is recommended to adhere to the minimum dose.
The drug should be used with particular caution in patients with diseases of the cardiovascular system (including uncontrolled arterial hypertension) or a high risk of developing cardiovascular diseases
. If long-term therapy (more than 4 weeks) is necessary in such patients, the drug should be used in a daily dose not exceeding 100 mg.
Children aged 1 year and older
The drug is prescribed in a dose of 0.5-2 mg/kg body weight/day (in 2-3 doses, depending on the severity of the disease). For the treatment of rheumatoid arthritis
the daily dose can be maximally increased to 3 mg/kg (in several doses). The maximum daily dose is 150 mg.
The drug in the form of extended-release tablets should not be used in children and adolescents under the age of 18 years.
For parenteral use
Adults
Injected deep into the / m. Single dose - 75 mg. If necessary, repeated administration is possible, but not earlier than after 12 hours.
Duration of use is no more than 2 days, if necessary, then switch to oral or rectal use of diclofenac.
In severe cases (for example, with colic), as an exception, 2 injections of 75 mg each can be given, with an interval of several hours (the second injection should be carried out in the opposite gluteal region). Alternatively, IM administration once a day (75 mg) can be combined with diclofenac in other dosage forms (tablets, rectal suppositories), and the total daily dose should not exceed 150 mg.
For migraine attacks
Diclofenac is recommended to be administered as early as possible after the onset of an attack, IM at a dose of 75 mg, followed by the use of suppositories at a dose of up to 100 mg on the same day, if required. The total daily dose should not exceed 175 mg on the first day.
In elderly patients (65 years and older)
no adjustment of the initial dose is required. In weakened patients and patients with low body weight, it is recommended to adhere to the minimum dose.
The drug should be used with particular caution in patients with diseases of the cardiovascular system (including uncontrolled arterial hypertension) or a high risk of developing cardiovascular diseases
. If long-term therapy (more than 4 weeks) is necessary in such patients, the drug should be used in a daily dose not exceeding 100 mg.
Children and teenagers under 18 years of age
Diclofenac should not be used intramuscularly in children and adolescents under 18 years of age due to the difficulty of dosing the drug.
Diclofenac, 75 mg/3 ml, solution for intramuscular administration, 3 ml, 5 pcs.
Damage to the gastrointestinal tract
When using diclofenac, phenomena such as bleeding or ulceration/perforation of the gastrointestinal tract, in some cases fatal, were observed. These events may occur at any time when using drugs in patients with or without previous symptoms and a history of serious gastrointestinal diseases. In elderly patients
such complications can have serious consequences. If patients receiving Diclofenac develop bleeding or ulceration of the gastrointestinal tract, the drug should be discontinued.
To reduce the risk of gastrointestinal toxicity in patients with gastrointestinal ulcers, especially complicated by a history of bleeding or perforation, as well as in elderly patients
the drug should be used in the minimum effective dose.
Patients at increased risk of developing gastrointestinal complications, as well as patients receiving therapy with low doses of acetylsalicylic acid (Aspirin), should take gastroprotectors (proton pump inhibitors or misoprostol) or other medications to reduce the risk of unwanted effects on the gastrointestinal tract. Patients with a history of gastrointestinal lesions, especially the elderly, should report all abdominal symptoms to the doctor.
Patients with bronchial asthma
Exacerbation of bronchial asthma (NSAID intolerance/NSAID-induced asthma), angioedema and urticaria are most often observed in patients with bronchial asthma, seasonal allergic rhinitis, nasal polyps, chronic obstructive pulmonary disease or chronic respiratory tract infections (especially those associated with allergic rhinitis-like symptoms). In this group of patients, as well as in patients with allergies to other drugs (rash, itching or urticaria), special caution should be observed when using Diclofenac (preparedness for resuscitation measures).
Skin reactions
Serious dermatological reactions such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, in some cases fatal, have been reported very rarely with the use of diclofenac. The highest risk and incidence of severe dermatological reactions were observed in the first month of treatment with diclofenac. If patients receiving Diclofenac develop the first signs of skin rash, damage to the mucous membranes or other symptoms of hypersensitivity, the drug should be discontinued. In rare cases, in patients who are not allergic to diclofenac, anaphylactic/anaphylactoid reactions may develop when using Diclofenac.
Effects on the liver
Since during the period of use of the drug Diclofenac there may be an increase in the activity of one or more liver enzymes, during long-term therapy with the drug, monitoring of liver function is indicated as a precautionary measure. If liver dysfunction persists and progresses or signs of liver disease or other symptoms (for example, eosinophilia, rash, etc.) occur, the drug should be discontinued. It should be borne in mind that hepatitis during the use of the drug Diclofenac can develop without prodromal phenomena.
Effects on the kidneys
During therapy with Diclofenac, it is recommended to monitor renal function in patients with hypertension, impaired cardiac or renal function, the elderly, patients receiving diuretics or other drugs that affect renal function, as well as in patients with a significant decrease in circulating blood plasma volume of any etiology , for example, in the period before and after major surgical interventions. After cessation of drug therapy, normalization of renal function indicators to initial values is usually observed.
Impact on the cardiovascular system
Therapy with NSAIDs, including diclofenac, particularly long-term and high-dose therapy, may be associated with a small increased risk of serious cardiovascular thrombotic events (including myocardial infarction and stroke).
In patients with diseases of the cardiovascular system and a high risk of developing diseases of the cardiovascular system (for example, with arterial hypertension, hyperlipidemia, diabetes mellitus, smokers), the drug should be used with extreme caution, at the lowest effective dose for the shortest possible duration of treatment, since the risk of thrombotic complications increases with increasing dose and duration of treatment. With long-term therapy (more than 4 weeks), the daily dose of diclofenac in such patients should not exceed 100 mg. The effectiveness of treatment and the patient's need for symptomatic therapy should be periodically assessed, especially in cases where its duration is more than 4 weeks. The patient should be instructed to immediately seek medical attention if the first symptoms of thrombotic disorders (eg, chest pain, shortness of breath, weakness, speech disturbances) appear.
Impact on the hematopoietic system
Diclofenac may temporarily inhibit platelet aggregation. Therefore, in patients with hemostasis disorders, it is necessary to carefully monitor relevant laboratory parameters. With long-term use of the drug Diclofenac, it is recommended to conduct regular clinical tests of peripheral blood.
Masking signs of an infectious process
The anti-inflammatory effect of Diclofenac may complicate the diagnosis of infectious processes.
Use simultaneously with other NSAIDs
Diclofenac should not be used concomitantly with other NSAIDs, including selective COX-2 inhibitors, due to the risk of increased adverse events.
Impact on the ability to perform potentially hazardous activities that require special attention and quick reactions (driving vehicles, working with moving mechanisms, etc.)
Patients who experience visual disturbances, dizziness, drowsiness, vertigo or other central nervous system disorders while taking diclofenac should not drive or operate machinery.
Diclofenac solution for injection 25mg/ml 3ml amp 5 pcs Grotex
Pharmacological group:
Non-steroidal anti-inflammatory drug (NSAID).
ATX code: M01AB05. Pharmacodynamics:
Diclofenac has anti-inflammatory, analgesic and antipyretic effects. By indiscriminately inhibiting cyclooxygenase 1 and 2, it disrupts the metabolism of arachidonic acid and reduces the amount of prostaglandins at the site of inflammation. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac helps to significantly reduce the severity of pain, morning stiffness, and swelling of the joints, which improves the functional state of the joint. For injuries, in the postoperative period, diclofenac reduces pain and inflammatory swelling.
Pharmacokinetics:
Suction
After intramuscular administration of diclofenac, its absorption begins immediately.
The maximum plasma concentration (Cmax), the average value of which is about 2.5 μg/ml (8 μmol/l), is reached after approximately 20 minutes. The amount of absorbed active substance is linearly dependent on the dose of the drug.
The area under the concentration-time curve (AUC) after intramuscular administration of diclofenac is approximately 2 times greater than after its oral or rectal administration, since in the latter cases, about half of the amount of diclofenac is metabolized during the “first pass” through the liver.
With subsequent administrations of the drug, the pharmacokinetic parameters do not change.
Provided that the recommended intervals between administrations of the drug are observed, no accumulation is observed.
Distribution
Communication with serum proteins is 99.7%, mainly with albumin (99.4%).
The apparent volume of distribution is 0.12-0.17 l/kg.
Diclofenac penetrates into the synovial fluid, where its maximum concentration is reached 2-4 hours later than in the blood plasma. The apparent half-life (T1/2) from synovial fluid is 3-6 hours. 2 hours after reaching the maximum concentration in the blood plasma, the concentration of diclofenac in the synovial fluid is higher than in the plasma, and its values remain higher over a period of time, up to 12 hours.
Metabolism
The metabolism of diclofenac is carried out partly by glucuronidation of the unchanged molecule, but mainly through single and multiple hydroxylation and methoxylation, which leads to the formation of several phenolic metabolites (3-hydroxy-, 4-hydroxy-, 5-hydroxy-, 4, 5-dihydroxy- and 3-hydroxy-4-methoxydiclofenac), most of which are converted into glucuronide conjugates. Two phenolic metabolites are biologically active, but to a much lesser extent than diclofenac. The CYP2C9 isoenzyme takes part in the metabolism of the drug.
Removal
The total systemic plasma clearance of diclofenac is 263 + 56 ml/min.
The final T1/2 is 1-2 hours. T1/2 of 4 metabolites, including two pharmacologically active ones, is also short-lived and amounts to 1-3 hours. One of the metabolites, 3-hydroxy-4-methoxydiclofenac, has a longer half-life, but this metabolite is completely inactive.
About 60% of the drug dose is excreted through the kidneys in the form of glucuronic conjugates of the unchanged active substance, as well as in the form of metabolites, most of which are also glucuronic conjugates. Less than 1% of diclofenac is excreted unchanged. The remainder of the drug dose is excreted in the form of metabolites in bile.
Pharmacokinetics in selected patient groups
The pharmacokinetic parameters of diclofenac in elderly patients do not change.
In patients with impaired renal function, accumulation of unchanged active substance is not observed if the recommended dosage regimen is observed. When creatinine clearance is less than 10 ml/min, the calculated equilibrium concentrations of diclofenac hydroxymetabolites are approximately 4 times higher than in healthy volunteers, while the metabolites are excreted exclusively in bile.
In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetics of diclofenac are similar to those in patients without liver disease.
Diclofenac passes into breast milk.
