Instructions for use DICLOBERL N 75 (DICLOBERL N 75)

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

The drug has a non-steroidal structure, has a strong analgesic and anti-inflammatory effect, and is also a prostaglandin synthetase .

Pharmacokinetics

The highest concentration in plasma after intramuscular administration is achieved after 10-20 minutes.

Blood protein binding is approximately 99.8%. Easily penetrates into the joint fluid, where its maximum concentration is recorded 3 hours later than in the blood. The half-life of the joint fluid is approximately 4-5 hours. Approximately 2 hours after the onset of maximum concentration in the blood, the content of the active substance in the synovial fluid remains higher than in the blood. This phenomenon is observed within 12 hours.

Metabolized by glucuronidation, hydroxylation and methoxylation to form a number of phenolic derivatives, the vast majority of which form complexes with glucuronic acid . The half-life from the blood is approximately one and a half hours. About 60% of the dose taken is excreted in the urine, the remaining part is evacuated through the intestines, while no more than 1% of diclofenac .

What is Dicloberl?

Dicloberl is a nonsteroidal anti-inflammatory drug (NSAID) that is used to relieve pain and reduce inflammation. Dikloberl contains the active ingredient - diclofenac. It exerts its therapeutic effect by reducing the amount of hormone-like substances in the body called prostaglandins, which cause pain and inflammation.

Dicloberl is used to relieve mild or moderate pain, to relieve fever, and also to treat rheumatic diseases (common forms of rheumatism).

Indications for use

• rheumatoid arthritis (including juvenile form), osteoarthritis , ankylosing spondylitis, spondyloarthritis;
• vertebrogenic pain syndromes;
• rheumatic diseases affecting extra-articular soft tissues;
• pain syndromes of post-traumatic and postoperative origin, accompanied by signs of inflammation, after orthopedic and dental interventions;
• acute pain syndrome of moderate severity of various origins.

The underlying disease must be treated with basic therapy. An increase in temperature in itself is not diclofenac

Contraindications

• acute ulcer , bleeding or perforation of the intestine or stomach;
• allergy to the components of the drug;
• increased risk of postoperative bleeding, hemostasis disorders, cerebrovascular bleeding or hematopoietic disorders;
• bleeding or perforation of the digestive system in the past associated with taking non-steroidal anti-inflammatory drugs;
• inflammatory bowel diseases;
• exacerbation of peptic ulcer disease, peptic ulcer bleeding, including in the past;
• third trimester of pregnancy;
• congestive heart failure;
• cerebrovascular disorders in persons who have suffered a stroke or cases of ischemic attacks;
• liver or kidney failure ;
• peripheral arterial disease;
• coronary heart disease in persons who have had a heart attack or suffer from angina pectoris ;
• treatment of pain before and after coronary artery bypass surgery;
• allergic reactions to Ibuprofen , Aspirin or other non-steroidal anti-inflammatory drugs .

Overdose

Signs of overdose: nausea, headache, epigastric pain, vomiting, bleeding from the digestive organs, drowsiness, convulsions, dizziness, diarrhea, disorientation , coma , agitation , tinnitus, liver damage, acute renal failure .

Treatment of overdose: symptomatic, gastric lavage (if no more than an hour has passed since the overdose). For frequent or prolonged convulsions, Diazepam .

Side effects

• Hematopoietic reactions: pancytopenia, thrombocytopenia, leukopenia, agranulocytosis, anemia . The first symptoms of these disorders may be pharyngitis , fever, superficial ulcerations in the mouth, nosebleeds, apathy , and skin bleeding.
• Immune reactions: skin rash, urticaria , allergic vasculitis, angioedema , itching, pneumonia .
• Mental disorders: depression , disorientation, irritability, insomnia , psychotic disorders, nightmares, other mental disorders.
• Reactions from nervous activity: dizziness, headache, agitation, dizziness, drowsiness, paresthesia, sensory disturbances, fatigue, convulsions, memory impairment, tremor , anxiety, hallucinations, taste disorders, aseptic meningitis , confusion, stroke , general malaise.
• Reactions from sensory organs: diplopia , blurred vision, optic neuritis, tinnitus, vertigo , hearing disorders.
• Circulatory reactions: arterial hypotension , heart failure, chest pain, palpitations, vasculitis, arterial hypertension, myocardial infarction.
• Respiratory reactions: pneumonitis , asthma .
• Digestive reactions: abdominal pain, vomiting, flatulence , anorexia , gastritis , dyspepsia , diarrhea , bleeding from the digestive organs, gastric ulcer (with possible perforation or bleeding), constipation , disruption of the esophagus, colitis , glossitis, stomatitis, intestinal stenosis hepatitis , increased transaminases , liver disorders, jaundice, hepatonecrosis , fulminant hepatitis , liver failure.
• Skin reactions: manifestations of eczema and erythema , hair loss, Lyell's syndrome, Stevens-Johnson syndrome, exfoliative dermatitis, purpura , photosensitivity, itching.
• Reactions from the genitourinary system: acute renal failure , edema, proteinuria, hematuria, nephrotic syndrome, interstitial nephritis, impotence, papillary necrosis of kidney tissue.

Dicloberl 75 mg/3 ml No. 5 solution d/in.amp.

Instructions for medical use of the drug Diclofenac N 75 Trade name Diclofenac N 75 International nonproprietary name Diclofenac Dosage form Solution for injection 75 mg/3ml Composition One ampoule contains: active substance - diclofenac sodium, 75 mg excipients: propylene glycol, benzyl alcohol, acetylcysteine , mannitol, 1 M sodium hydroxide solution, water for injection Description Transparent colorless or almost colorless solution without visible particles Pharmacotherapeutic group Anti-inflammatory and antirheumatic drugs. Non-steroidal anti-inflammatory drugs. Acetic acid derivatives. Diclofenac. ATC code M01AB05 Pharmacological properties Pharmacokinetics After intramuscular administration of the drug, the maximum concentration is about 2.5 μg/ml (8 μmol/l), in plasma is achieved after 10 - 20 minutes, after rectal administration - after approximately 30 minutes. Immediately after its achievement, a rapid decrease in the concentration of the drug in plasma is observed. 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. After repeated use 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. Binding to serum proteins is 99.7%, it occurs mainly with albumin (99.4%). The approximate 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 approximate half-life from synovial fluid is 3-6 hours. 2 hours after reaching the maximum plasma concentration, the concentration of diclofenac in the synovial fluid is higher than in the plasma, and its values ​​remain higher up to 12 hours. The metabolism of diclofenac is carried out partly by glucuronidation of the unchanged molecule, but mainly through single and multiple 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 to glucuronide conjugates. Two of these phenolic metabolites are biologically active, but to a significantly lesser extent than diclofenac. The total systemic plasma clearance of diclofenac is 263±56 ml/min. The terminal half-life is 1-2 hours. The half-life of 4 metabolites, including two pharmacologically active ones, is also short and amounts to 1-3 hours. One of the metabolites, 3′-hydroxy-4′-methoxy-diclofenac, has a longer half-life, but this metabolite is completely inactive. About 30% of the active substance is excreted in the form of metabolites in feces. After metabolic transformations in the liver (hydroxylation and conjugation), about 70% of the active substance is excreted through the kidneys in the form of pharmacologically inactive metabolites. Pharmacokinetics in certain groups of patients In some elderly patients, a 15-minute intravenous infusion resulted in plasma concentrations that were 50% higher than those observed in young healthy individuals. In patients with impaired renal function, no accumulation of diclofenac was observed when Diclofenac was prescribed in usual single doses. However, the metabolites are ultimately excreted in the bile. In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetics of diclofenac are similar to those in patients without liver disease. Pharmacodynamics DikloberlÒN 75 contains diclofenac sodium, a non-steroidal substance that has a pronounced anti-inflammatory, analgesic and antipyretic effect. The main mechanism of action of diclofenac is considered to be inhibition of prostaglandin biosynthesis. Prostaglandins play an important role in the genesis of inflammation, pain and fever. In rheumatic diseases, the anti-inflammatory and analgesic properties of DikloberlN 75 provide a clinical effect, characterized by a significant reduction in the severity of symptoms and complaints such as pain at rest and with movement, morning stiffness and swelling of the joints, as well as improved function. Diclofenac sodium does not inhibit the biosynthesis of proteoglycans in cartilage tissue. A significant analgesic effect of the drug was revealed in moderate and severe pain syndrome of non-rheumatic origin. DicloberlÒN 75 is able to eliminate pain during primary dysmenorrhea. Diclofenac is a non-steroidal anti-inflammatory drug that has been shown to be effective in non-clinical trials; The mechanism of action of the drug is to suppress prostaglandin synthesis. Diclofenac reduces pain, swelling and fever caused by the inflammatory process. In addition, diclofenac inhibits platelet aggregation caused by ADP and collagen. Indications for use Symptomatic treatment for severe acute pain accompanying: - acute arthritis (including an attack of gout) - chronic arthritis, in particular rheumatoid arthritis (chronic polyarthritis) - ankylosing spondylitis (Bechterew's disease) and other inflammatory diseases of the spine of a rheumatic nature - irritation phenomena degenerative diseases of the joints and spine (arthrosis and spondyloarthrosis) - inflammatory diseases of soft tissues of a rheumatic nature - swelling or post-traumatic inflammation with pain syndrome Note: The injection solution is indicated only if a particularly rapid effect is required, as well as if ingestion or administration in the form of a candle is not possible. In such cases, as a rule, treatment is recommended only as a single injection as part of the initial therapy. Method of administration and dosage Adults: Dicloberl® N 75 injection is performed once. To continue treatment, dosage forms for oral or rectal administration are used. Moreover, even on the day of injection, the total dose should not exceed 150 mg. Method and duration of use Dicloberl® N 75 is injected intramuscularly deep into the buttock area. Due to the potential risk of developing anaphylactic reactions (up to shock), the patient should be monitored for at least an hour after administration of Dicloberl® N 75; at the same time, the necessary and functioning (functioning) medical instruments necessary to provide emergency care must be at the ready. The meaning of these measures must be explained to the patient. Typically, injections of the drug are prescribed for a period of 1 to 5 days. The duration of use of the drug is determined by the attending physician. Special groups of patients Elderly patients: No special dose adjustment is required. In the case of elderly patients, more careful monitoring of their condition is necessary due to possible side effects. Decreased renal and liver function: With mild to moderate decrease in renal and liver function, no dose reduction is required (recommendations for patients with severe renal failure). Side effects Very common (≥ 1/10) - gastrointestinal complaints such as nausea, vomiting and diarrhea, as well as minor gastrointestinal bleeding, in rare cases with the development of anemia Common (³ 1/100 - < 1/10) - pseudo anaphylactic reactions - hypersensitivity reactions such as skin rash and itching - central nervous system disorders such as headache, dizziness, stupor, agitation, irritability or fatigue - dyspeptic symptoms, flatulence, abdominal cramps, lack of appetite, and also gastrointestinal ulcers (with risk of bleeding and perforation) - increased transaminase activity in the blood serum - reactions at the injection site, pain at the injection site, induration at the injection site - fluid retention Sometimes (³ 1/1,000 - < 1/100) - urticaria - bloody vomiting, melena or bloody diarrhea. - impaired liver function, especially with long-term therapy, acute hepatitis with or without jaundice (in rare cases, fulminant hepatitis is possible even without previous symptoms). Therefore, during long-term treatment with the drug, liver parameters should be analyzed regularly. - alopecia - the occurrence of edema, especially in patients with arterial hypertension or renal failure Rare: (³ 1/10,000 - < 1/1,000) - edema, necrosis at the injection site - hypersensitivity reactions to benzyl alcohol are rare Very rare (< 1 /10,000), including isolated cases - abscess at the injection site - hematopoietic disorders (anemia, leukopenia, thrombocytopenia, pancytopenia, agranulocytosis), hemolytic anemia. - severe generalized hypersensitivity reactions: Quincke's edema (swelling of the face, swelling of the tongue, swelling of the internal larynx with narrowing of the airways, shortness of breath, increased heart rate, decreased blood pressure, drop in blood pressure to a critical level). - allergic vasculitis and pneumonitis - psychotic reactions, depression, anxiety, nightmares - sensory disturbances, disturbances in taste, memory, disorientation, convulsions, tremors - mental disorders such as memory impairment - visual impairment (blurred vision or diplopia) - noise in the ears, transient hearing disorders - palpitations, edema, heart failure, myocardial infarction - arterial hypertension - acute cerebrovascular accident - stomatitis, glossitis, esophageal lesions, complaints of pain in the lower abdomen (for example, bleeding with colitis or worsening ulcerative colitis /Crohn's disease), constipation, pancreatitis, diaphragm-like intestinal strictures. - exanthema, eczema, erythema multiforme, photosensitivity, purpura (including allergic purpura), bullous reactions such as Stevens-Johnson syndrome and toxic epidermal necrolysis - damage to kidney tissue (interstitial nephritis, papillary necrosis), which may be accompanied by acute renal failure, proteinuria and/or hematuria; nephrotic syndrome is an exacerbation of inflammatory processes of infectious origin (for example, the development of necrotizing fasciitis) associated with the systemic use of non-steroidal anti-inflammatory drugs. This may be due to the mechanism of action of NSAIDs. - symptoms of aseptic meningitis, such as stiff neck, headache, nausea, vomiting, fever or clouding of consciousness. Patients with autoimmune diseases (systemic lupus erythematosus, mixed collagenosis) are predisposed to the occurrence of such conditions. Contraindications Dicloberl® N 75 should not be used in the following cases: - hypersensitivity to the active substance or one of the other components of the drug - with a history of bronchospasm, asthma, rhinitis or urticaria after taking acetylsalicylic acid or other non-steroidal anti-inflammatory drugs - with unexplained hematopoietic disorders origin, disorders of hemostasis and blood coagulation - treatment of postoperative pain after coronary artery bypass surgery (or use of a heart-lung machine) - inflammatory bowel diseases (Crohn's disease or ulcerative colitis) - if there is a current or past recurrent peptic ulcer/hemorrhage (two or more individual cases of confirmed peptic ulcer disease or bleeding) - if there is a history of gastrointestinal bleeding or ulcer perforation associated with taking non-steroidal anti-inflammatory drugs - recent cerebrovascular or other bleeding - established congestive heart failure (NYHA class II-IV), coronary heart disease, diseases of peripheral arteries or cerebral vessels - severe liver or kidney dysfunction - severe heart failure - pregnancy and lactation - childhood and adolescence up to 18 years Drug interactions Other NSAIDs, including salicylates: Concomitant use of some NSAIDs may increase the risk of ulcers and gastrointestinal bleeding due to the synergistic effect of the drugs. In this regard, the combined use of diclofenac and other NSAIDs is not recommended. Digoxin, phenytoin, lithium: When administered together, Dicloberl® N 75 may increase the concentration of digoxin, phenytoin and lithium in the blood. In this regard, when treating with diclofenac, monitoring the serum concentration of lithium is mandatory, and digoxin or phenytoin is recommended. Diuretics, ACE inhibitors and angiotensin II antagonists: NSAIDs may reduce the effectiveness of diuretics and other antihypertensive drugs (such as beta blockers, angiotensin-converting enzyme (ACE) inhibitors). In some patients with reduced renal function (eg, those who are dehydrated or elderly patients with reduced renal function), further deterioration of renal function, including the possible development of acute renal failure, may occur when taking ACE inhibitors or angiotensin II antagonists with a drug that inhibits cyclooxygenase. which, however, in most cases is reversible. In this regard, these drugs should be prescribed with caution in combination with diclofenac, especially in elderly patients. When co-administering diclofenac and these drugs, it is necessary to ensure that the patient takes an adequate amount of fluid, and kidney function should also be regularly monitored after starting treatment. Concomitant use of Dicloberl® 75 and potassium-sparing diuretics can lead to the development of hyperkalemia. In this regard, it is recommended to monitor the concentration of potassium in the blood when these drugs are administered together. Glucocorticoids: When administered together with diclofenac, the risk of developing ulcers and gastrointestinal bleeding increases. Drugs that inhibit platelet aggregation (eg, acetylsalicylic acid) and selective serotonin reuptake inhibitors (SSRIs): The risk of gastrointestinal bleeding increases when administered together with diclofenac. Antidiabetic drugs: Clinical studies have shown that diclofenac can be used together with oral antidiabetic drugs without affecting their effect. However, there are isolated reports of hypoglycemic and hyperglycemic events requiring dose adjustment of antidiabetic drugs during treatment with diclofenac. For this reason, as a precaution, regular monitoring of blood glucose levels is recommended when these drugs are used concomitantly. Methotrexate: Diclofenac can suppress the renal clearance of methotrexate, leading to an increase in its level. When Dicloberl® N 75 is administered within 24 hours before or after the administration of methotrexate, the concentration of methotrexate in the blood may increase and its toxic effects may increase. Cyclosporine: NSAIDs (eg, diclofenac sodium) may enhance the nephrotoxic effect of cyclosporine. Quinolone antibiotics: Isolated cases of seizures have been reported, which could be caused by the simultaneous use of quinolones with NSAIDs. Anticoagulants: NSAIDs may enhance the effect of anticoagulants such as warfarin Sulfonylureas: There have been isolated reports of changes in blood glucose concentrations after the use of diclofenac, requiring dose adjustment of the antidiabetic drug. In this regard, during joint therapy it is recommended to monitor the concentration of glucose in the blood. Probenecid and sulfinpyrazone: Medicines containing probenecid and sulfinpyrazone may delay the elimination of diclofenac from the body. Colestipol and cholestyramine: These drugs can cause a decrease or delay in the absorption of diclofenac. For this reason, it is recommended to prescribe diclofenac at least one hour before taking colestipol/cholestyramine or 4-6 hours after it. Potent CYP2C9 inhibitors: Caution should be exercised when diclofenac is administered concomitantly with potent CYP2C9 inhibitors (such as sulfinpyrazone and voriconazole), since their simultaneous use may increase the peak plasma concentration of diclofenac and enhance its effect due to slower metabolism. Special instructions Precautions regarding the gastrointestinal tract Avoid using Dicloberl® N 75 simultaneously with other NSAIDs, including selective cyclooxygenase-2 inhibitors. Adverse effects can be minimized by administering the lowest effective dose for the shortest duration necessary to effectively control pain (gastrointestinal and cardiovascular risks are lower) Elderly Patients Elderly patients have an increased incidence of adverse reactions to NSAIDs, especially gastrointestinal bleeding and perforation, including fatal ones. Gastrointestinal bleeding, ulceration and ulcer perforation Gastrointestinal bleeding, ulceration or perforation, in some cases with fatal outcome, was observed with all NSAIDs at any stage of treatment, with or without warning symptoms and regardless of the presence or absence of a medical history serious gastrointestinal pathology. The risk of gastrointestinal bleeding, ulceration, or perforation increases with increasing doses of NSAIDs in patients with a history of ulcers, especially those complicated by bleeding or perforation. In such cases, treatment should begin with the lowest possible dose. For these patients, as well as for patients receiving low-dose aspirin or other drugs that increase the risk of GI adverse events, combination therapy with drugs that have GI protective effects (eg, misoprostol or proton pump inhibitors) should be considered. pump). Patients with a history of gastrointestinal toxicity, particularly elderly patients, should report any unusual abdominal symptoms (especially gastrointestinal bleeding); this is most important for the initial stages of treatment. The patient should be instructed that if severe upper abdominal pain, melena or vomiting occurs, stop taking the drug immediately and consult a doctor (see Side Effects). Caution should be exercised when prescribing diclofenac to patients concomitantly taking medications that may increase the risk of ulceration or bleeding; Such drugs include oral corticosteroids, anticoagulants, for example, warfarin, selective capture inhibitors of serotonin or agents that control the aggregation of platelets (antiplatelet agents), for example. aspirin. With the development of gastrointestinal bleeding against the background of treatment for Diclobertle® N 75, the drug should be canceled. Nonsteroidal anti-inflammatory drugs should be prescribed with caution to patients with a history of gastrointestinal diseases (ulcerative colitis, Crohn's disease) due to the risk of exacerbation. The effects of the cardiovascular system and cerebrovascular blood circulation of diclofenac should be caused with caution to patients with arterial hypertension and/or decompensated heart failure from mild to average severity in an anamnesis, since in the treatment of NSAIDs, liquid retention and edeck development are possible. According to the results of clinical studies and epidemiological data, the use of diclofenac, especially in high doses (150 mg / day) and for a long time, may be accompanied by a slight increase in the risk of arterial thrombosis (for example, myocardial infarction or stroke). To minimize cardiovascular risks associated with dosing and duration of Diclofenac, the drug should be used in a minimum effective dose in a short period. A repeated assessment of the need for patients to relieve symptoms and reaction to therapy should be periodically re -assessed. Patients with uncontrolled arterial hypertension, congestive heart failure established by coronary heart disease, a disease of peripheral arteries or blood vessels of the brain should be prescribed after a thorough examination. Patients with significant risk factors for the development of cardiovascular diseases (for example, arterial hypertension, hyperlipidemia, diabetes mellitus, smoking) can be treated with diclofenac only after a thorough examination. Skin reactions were reported about rare cases of serious skin reactions, sometimes with death, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis (Layella syndrome), against the background of the treatment of NSAIDs. The risk of such reactions is greatest at the beginning of treatment; Most of the described phenomena were observed in the first months of therapy. Dicloberl® N 75 should be discontinued at the first appearance of a skin rash, damage to the mucous membranes or other signs of hypersensitivity. The effects of the liver side of diclofenac should be caused with caution to patients with impaired liver function, since against the background of treatment their condition can deteriorate. If clinical signs of liver pathology appear, the drug must be discontinued. Other instructions to prevent damage to the renal tissue should regularly check the condition of the renal function. The appearance of fever, sore throat, surface wounds in the oral cavity, flu -like symptoms, severe fatigue, nasal bleeding and skin hemorrhage can be the first signs of hematopoiesis (see side effects). With prolonged treatment, a regular blood test is necessary. In the following cases, Diclobert® N 75 should only be assigned after a thorough assessment of the “General Risk” ratio:-with congenital disorders of the metabolic metabolic (for example, with acute intermittent porphyria); - with systemic lupus erythematosus (SLE) and mixed collagenosis. In the following cases, especially thorough control is required by the attending physician:-in case of violations of the gastrointestinal tract or in the presence of chronic inflammatory intestinal diseases (non-specific ulcerative colitis, Crohn's disease); - with increased blood pressure or heart failure; - with a decrease in the function of the kidneys - in case of impaired liver function - immediately after extensive surgical intervention - with allergies to pollen, nose polyps and chronic obstructive diseases of the respiratory tract, since such patients have increased the risk of allergic reactions. These reactions can be manifested by attacks of asthma (the so -called analgesic asthma), Quincke's edema or urticar rash. - with allergies to other substances, since such patients have increased risk of hypersensitivity reactions, including the treatment of Diklobertle® N 75. Dicloberth® N 75 should not be introduced into the focus of inflammation or infection. Severe sharp reactions of hypersensitivity (for example, anaphylactic shock) were very rarely observed. When the first signs of the hypersensitivity reaction of Dicloberth® N 75 appear, and professional treatment has begun in accordance with the developed symptoms. For safety reasons in the treatment of elderly patients, care must be taken. In particular, weakened elderly patients and patients with a low body weight are prescribed in a minimum effective dose. Diclofenac may temporarily inhibit platelet aggregation. In this regard, it is necessary to monitor the condition of patients with bleeding disorders. Like other NSAIDs, due to its pharmacodynamic properties, diclofenac can mask the manifestations and symptoms of infection. To prevent exacerbation of inflammation of the infectious nature, which may be associated with the mechanism of action of non -steroidal anti -inflammatory drugs, the patient is recommended to consult a doctor immediately if, against the background of treatment, Diclobertle 75, symptoms of infection again arose (see side effects). With prolonged treatment, diclofenac should regularly check the function of the liver, kidneys and a general blood test. With prolonged use of painkillers, headaches may occur. You should not try to eliminate headaches by increasing the dose of the drug. With long-term use of painkillers, especially when combining several analgesic active ingredients, permanent kidney damage is possible with the risk of renal failure (analgesic nephropathy). When NSAIDs and alcohol are combined, the undesirable effects of the active substance of the drug may be enhanced, especially on the gastrointestinal tract or central nervous system. In cases of parenteral administration of diclofenac, patients with bronchial asthma should be given special caution, since the likelihood of an increase in the symptoms of the disease is not excluded. Pregnancy and lactation Pregnancy Protagandin's suppression of synthesis can adversely affect pregnancy and/or development of the embryo/fetus. According to the results of epidemiological studies, in the early stages of pregnancy, the use of drugs that suppress the synthesis of prostaglandin can increase the risk of spontaneous abortion, the occurrence of heart disease in the fetus and the front abdominal wall. Thus, the absolute risk of the formation of defects in the cardiovascular system increased from <1% to about 1.5%. It is believed that the risk of these phenomena increases with an increase in the dose of the drug and the duration of its use. The appointment of Diclofenac during the first and second trimester of pregnancy is possible only when there is an urgent need. In the case of the appointment of a diclofenac to women planning a pregnancy, either in the first and second trimester of pregnancy, you should choose the smallest possible dose and the least possible duration of treatment. In the third trimester of pregnancy, all synthesis synthesis inhibitors can lead to development of the fetus: - phenomena of cardiopulmonal toxicity (e.g., premature closure of the arterial duct and hypertension in the pulmonary artery system); - kidney dysfunction, which can progress up to renal failure with the development of low water; At the end of pregnancy, they can lead to the mother and fetus to: - lengthening the time of bleeding, an anti -aggregation effect, which can occur even when using very low doses of the drug; - suppressing the contractile activity of the uterus, which can lead to delay or delaying labor. Lactation active substance diclofenac and its decay products in small quantities fall into the mother’s milk. Diclobert® 75 fertility can reduce female fertility, and therefore it is not recommended to prescribe it to women planning pregnancy. In women experiencing difficulties with conception or undergoing infertility examination, the possibility of canceling Dicloberth® N 75 should be considered. Features of the effect of the drug on the ability to drive vehicles and maintain potentially hazardous mechanisms in the treatment of Diklobertle® N 75 in high doses may take place such side effects from the central nervous system as increased fatigue and dizziness; therefore, in some cases, patients may experience impaired reaction and deterioration in the ability to actively participate in street traffic and operate machinery. These phenomena intensify when the drug is combined with alcohol intake. Note: propylene glycol, which is part of the drug Diklobert® N 75, can cause symptoms similar to those that occur after alcohol consumption. An overdose of the symptoms: an overdose of diclofenac can manifest by disorders from the central nervous system, such as headache, dizziness, stunning and loss of consciousness (and in children even with myoclonic convulsions), as well as pain in the abdomen, nausea and vomiting. In addition, gastrointestinal bleeding is possible, as well as impaired liver and kidney function. Also, with an overdose of diclofenac, arterial hypotension, respiratory depression and cyanosis can be observed. The treatment is symptomatic: there is no specific antidote. The form of release and packaging of 3 ml in ampoules of colorless glass type I. 5 ampoules along with instructions for medical use in the state and Russian languages ​​are invested in a pack of cardboard. Storage conditions The drug should be stored at a temperature of not higher than 30 ° C. To protect against light exposure, stored the drug in the original packaging. Keep out of the reach of children! The storage period of 3 years does not apply, after the expiration date of the vacation condition from pharmacies according to the recipe, the manufacturer of Berlin-Hemi AG (Menarini Group) Glinniker Veg 125 12489 Berlin owner of the registration certificate and manufacturer of Berlin Hemi AG (Menarini Group) Gliniker Veg 125 12489 Berin. Packer A. Menarini Maineuvering Lodzhistiks Andes Speediz S.R., the address of the organization receiving in the territory of the Republic of Kazakhstan claims from consumers regarding the quality of products (goods): representative of Berlin-Hemi AG in the Republic of Kazakhstan Tel: +7 727 2446183, 2446184, 2446185 Fax: +7 727 2446180 Email

Instructions for injections Dicloberl N 75 (Method and dosage)

To reduce the risk of adverse reactions, the lowest possible effective dose should be used for the shortest possible period of time.

Dicloberl injections, instructions for use

Treatment with the drug is recommended to be carried out using a single injection. The solution is injected deep into the buttock muscle. If long-term therapy is needed, it is continued with oral or rectal forms of diclofenac . On the day the drug was injected, the total daily dose should not exceed 150 mg.

Elderly patients

Dicloberl injections should be used with caution in this group of people, since the majority of them are more prone to adverse reactions. Frail elderly patients or patients with low weight should be prescribed the lowest effective doses of the drug.

Interaction of Dicloberl with other drugs and substances

Before using Dicloberl, consult your doctor if you are taking antidepressants. Taking some antidepressants with NSAIDs may cause bruising or bleeding.

Check with your doctor about the safety of taking Dicloberl if you are using any of these medications:

• blood pressure lowering agents (antihypertensives and diuretics);
• other drugs from the NSAID group (aspirin, ibuprofen, nimesulide);
• anticoagulants (drugs that inhibit the activity of the blood coagulation system and prevent the formation of blood clots - Warfarin, Coumadin, Jantoven).

This list is not complete. Other drugs may interact with Dicloberl, including medicines and dietary supplements. For more detailed information, please consult your doctor.

Interaction

With simultaneous use, Dicloberl can increase the lithium in the blood. In such cases, monitoring of lithium in the blood is recommended.

When used together with Digoxin, an increase in the concentration of the latter in the blood is possible. In such cases, monitoring the concentration of Digoxin in the blood is recommended.

Concomitant use of diclofenac with antihypertensive drugs and diuretics may lead to a weakening of their antihypertensive effect due to suppression of the synthesis of angiodilating prostaglandins . Patients should receive adequate amounts of fluids, and regular monitoring of kidney function is also recommended after starting such treatment.

Concomitant use with Cyclosporine , potassium-sparing diuretics , Trimethoprim or Tacrolimus may increase potassium in the blood, so the condition of such patients should be monitored more often.

Concomitant use with anticoagulants may increase the risk of bleeding, since diclofenac in large doses can reversibly inhibit platelet adhesion, so such patients should be carefully monitored regularly.

Concomitant use of diclofenac and other non-steroidal anti-inflammatory drugs or glucocorticosteroids may increase the likelihood of ulcers or gastrointestinal bleeding. Therefore, simultaneous use of two or more anti-inflammatory nonsteroidal drugs should be avoided.

Concomitant use of non-steroidal anti-inflammatory drugs and serotonin reuptake blockers increases the risk of bleeding from the digestive organs.

Diclofenac can be prescribed together with oral forms of hypoglycemic agents and this does not affect their therapeutic effect. But there are some reports of the occurrence of hyperglycemia and hypoglycemia , which necessitated adjustment of the dosage of antidiabetic agents while taking diclofenac . Therefore, it is recommended to monitor glucose during combination treatment.

Diclofenac can reduce the rate of elimination of Methotrexate , which leads to an increase in the level of the latter in the blood. Diclofenac should be used no earlier than 24 hours before taking Methotrexate to avoid cases of increased concentration of the latter and increased toxic effects.

Concomitant use with cyclosporines can increase their nephrotoxicity, which is why diclofenac should be prescribed in reduced doses.

When using anti-inflammatory non-steroidal drugs with Tacrolimus , the risk of nephrotoxicity may increase.

It is possible that seizures may develop in people who simultaneously use quinolone derivatives and Dicloberl. This phenomenon can be observed in patients with or without a history of seizures. Caution should be exercised when deciding whether to prescribe quinolones to patients already receiving anti -inflammatory non-steroidal drugs.

When taking Phenytoin together with diclofenac , it is necessary to monitor the content of the former in the blood due to a possible increase in its content.

Medicines containing probenecid slow down the elimination of diclofenac from the body.

The simultaneous administration of cardiac glycosides and anti-inflammatory non-steroidal drugs can aggravate heart failure, inhibit the glomerular filtration process and increase the content of glycosides in the blood.

Diclofenac should not be used within 9-12 days after the last dose of Mifepristone , since diclofenac can weaken the effect of the latter.

Caution is recommended when using diclofenac with strong CYP2C9 inhibitors , as this may lead to an increase in the concentration of diclofenac in the blood due to inhibition of its metabolism.

What you need to know before you start taking Dicloberl

If you have an allergic reaction to Dicloberl or if bronchospasm occurs, you should stop using it further, and also consult your doctor to select another medication that is more suitable for you.

Dicloberl may not be safe for use if you have a history of the following conditions:

• heart disease, high blood pressure;
• stomach and duodenal ulcers;
• bronchial asthma;
• inflammatory diseases of the kidneys and/or liver;
• if you have bad habits (smoking).

Note! Taking Dicloberl during the last 3 months of pregnancy may harm the unborn baby.

Dicloberl has a more prolonged (long-lasting) effect, which means that it has a long-lasting effect and is slowly eliminated from the body. Therefore, it is believed that it passes into breast milk in significant concentrations and is incompatible with breastfeeding.

Dicloberl can cause stomach or intestinal bleeding, which can lead to serious negative consequences, including death. If you have a history of peptic ulcer disease, then you should take this drug under the protection of a medicinal group of antiulcer drugs, such as misoprostol, omez, which have a protective effect on the gastric mucosa.

Dicloberl is approved for use by people over 18 years of age.

special instructions

In order to reduce the risk of adverse reactions, treatment should begin with the minimum effective dose, which should be taken in the shortest course necessary to relieve symptoms.

systemic anti-inflammatory non-steroidal drugs should be avoided due to a possible increase in side effects.

Due to its pharmacological properties, the drug Dicloberl is able to mask the signs of infection.

With the use of all non-steroidal anti-inflammatory drugs, cases of bleeding from the digestive organs, perforation and ulceration, which can be fatal, have been identified. If such disorders are diagnosed in patients receiving diclofenac , its use should be discontinued immediately.

Elderly patients have an increased risk of adverse reactions to non-steroidal anti-inflammatory drugs , especially bleeding and perforation. For this group of patients, as well as for those in need of simultaneous use of acetylsalicylic acid , the issue of prescribing combination therapy using gastroprotective agents ( proton pump inhibitors or Misoprostol ) should be decided.

Close medical supervision is necessary when prescribing Dicloberl to patients with liver disease, due to the possible deterioration of their condition.

During long-term treatment with the described drug, constant monitoring of liver function and liver enzyme levels is prescribed. If liver dysfunction persists or worsens, or clinical signs appear that are thought to be related to disease progression, use of Dicloberl should be discontinued immediately.

Since an increase in the frequency and severity of edema has been reported during therapy with anti-inflammatory non-steroidal drugs , special attention should be paid to persons with arterial hypertension , cardiac or renal dysfunction, the elderly, those receiving diuretics or nephrotoxic agents , and before or after major surgery.

In patients with systemic lupus erythematosus or other connective tissue diseases, an increased risk of aseptic meningitis .

The use of diclofenac may be associated with an increased likelihood of thrombotic events ( heart attack or stroke ).

Patients with peripheral artery disease, coronary heart disease , congestive heart failure, severe arterial hypertension , cerebrovascular disease are not recommended to prescribe the drug; in extreme cases, it can be used in a dosage of up to 100 mg per day.

When taking this drug for a long time, regular monitoring of blood tests is necessary.

Patients with bleeding diathesis, impaired hemostasis or hematological disorders taking Dicloberl should be closely monitored.

Patients with chronic obstructive pulmonary disease, asthma, allergic rhinitis, nasal polyps or chronic respiratory tract infections are more likely to experience side effects ( asthma , Quincke's edema , urticaria ) due to taking non-steroidal anti-inflammatory drugs . This also applies to persons with allergic reactions to other substances, such as itching, rash, hives .

With prolonged use of painkillers, a headache may occur, which should not be treated by increasing the dosage of the medication.

vertigo during treatment with the drug should not drive.

What are the side effects of Dicloberl?

Get emergency medical help right away if you have the following signs of an allergic reaction to Dicloberl:

• nettle rash;
• difficulty breathing, swelling of the face or throat;
• serious skin reaction (high temperature, sore throat, burning eyes, skin pain, blistering of the skin surface and peeling).

You should urgently call an ambulance if you have signs of a heart attack or stroke :

• chest pain spreading to your jaw or shoulder;
• sudden weakness, numbness in the arm and/or leg;
• impairment of speech and/or understanding;
• dizziness;
• sudden loss of consciousness;
• numbness of the lip or half of the face, often with facial distortion;
• dyspnea.

Before the ambulance arrives, the patient should be positioned so that the head lies at an angle of 30 degrees to the horizontal surface. It is necessary to ensure a flow of fresh air, remove tight clothing, and carefully measure blood pressure without unnecessary worry (if it is elevated, take the medication that the patient usually takes in this case).

Be careful! Stop using this drug and call your doctor at once if you experience these side effects:

• skin rash, from mild to severe;
• general malaise;
• cardiovascular disorders (swelling, shortness of breath, weight gain);
• disorders of the urinary system (painful or difficult urination or its complete absence);
• problems with the hepatobiliary system (liver) - nausea, pain in the right hypochondrium, fatigue, itching, dark urine, yellowing of the skin or whites of the eyes;
• stomach bleeding (bloody or tarry stools, coughing up blood, or vomit that looks like coffee grounds).

Common side effects of Dicloberl may include:

• indigestion, flatulence (gas formation in the intestines), nausea, vomiting, stomach pain;
• diarrhea, constipation;
• headache, dizziness, drowsiness;
• deterioration of laboratory tests;
• itching, sweating;
• nasal congestion;
• high blood pressure;
• swelling or pain in the upper and lower extremities.

For a more detailed list of side effects, consult your doctor, as these list only commonly occurring side effects. If one or more side effects occur, stop using it and seek emergency medical attention.

Analogs

Level 4 ATC code matches:
Voltaren

Rapten

Zerodol

Dickloberl Retard

Dicloberl

Ketanov

Dolak

Panoxen

Ketorolac

Naklofen Duo

Naklofen

Olfen-100

Olfen-75

Neurodiclovit

Nizilat

Fanigan

Aertal

Methindol retard

Ortofen

The most common analogues of Dikloberl are listed below: Almiral, Arguette Rapid, Bioran, Voltaren, Diclofenac, Diclak, Diclobry, Ketarolak, Naklofen, Olfen, Ortofen, Ibuprofen, Rapten, Feloran.

During pregnancy and lactation

In the first two trimesters of pregnancy, Dicloberl is allowed to be prescribed only under strict indications and under medical supervision, and the duration of therapy should be as short as possible. In the last trimester of pregnancy, the use of the drug is prohibited due to the risk of inhibition of uterine contractility and early closure of the ductus arteriosus.

Diclofenac can pass into milk during breastfeeding, so the drug should not be used during lactation to avoid negative effects on the baby.

Dicloberl can also negatively affect fertility in women, so it is not recommended for use by women planning pregnancy.

What you need to know about the drug Dicloberl

Dicloberl is a non-selective inhibitor of cyclooxygenase (an enzyme that inhibits the production of prostaglandins), due to this its negative effect on the gastrointestinal tract is most pronounced, which in turn can lead to gastric bleeding and subsequent negative consequences.

Dicloberl is also slowly eliminated from the body, as a result of which it is necessary to strictly adhere to the dosage schedule and certain intervals between doses in order to avoid negative consequences for the cardiovascular system and gastrointestinal tract, as well as the body as a whole.