Diclovit rectal suppositories 50mg №5×2

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Diklovit supp.rect. 50mg in a box No. 5×2
Description:
Suppositories of white or almost white color, torpedo-shaped. The appearance of white plaque on the surface of the suppository is allowed. The main active substance Diclofenac Release form suppositories Dosage 50 mg Pharmacological properties Pharmacodynamics Diclofenac sodium is a non-steroidal substance with a pronounced anti-inflammatory, analgesic and antipyretic effect. The main mechanism of action established in the experimental conditions is the inhibition of prostaglandin biosynthesis. Prostaglandins play an important role in the genesis of inflammation, pain and fever. It has been established that sodium diclofenac has a pronounced analgesic effect in moderate and severe pain syndrome. In post-traumatic and postoperative inflammatory phenomena, diclofenac sodium quickly relieves pain (both spontaneous and arising from movement), reduces inflammatory edema and swelling of the postoperative wound. Pharmacokinetics After rectal administration, diclofenac is rapidly absorbed, the maximum plasma concentration is reached on average within 1 hour after the administration of 50 mg suppositories. The maximum concentration is linearly dependent on the dose used. Changes in the pharmacokinetics of diclofenac against the background of repeated administration are not observed, do not cumulate. Communication with plasma proteins – more than 99% (most of it binds to albumin). Penetrates into the synovial fluid. The maximum concentration in synovial fluid is observed 2-4 hours later than in plasma. The half-life from the synovial fluid is 3-6 hours (the concentration of the active substance in the synovial fluid 4-6 hours after the administration of the drug is higher than in plasma, and remains higher for another 12 hours). The relationship between the concentration of the drug in the synovial fluid and the clinical efficacy of the drug has not been elucidated. Metabolism: 50% of the active substance is metabolized during the “first pass” through the liver. Metabolism occurs as a result of multiple or single 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 plasma half-life is 2 hours. 65% of the administered dose is excreted as metabolites by the kidneys; less than 1% is excreted unchanged, the rest of the dose is excreted as metabolites in the bile. In patients with severe renal insufficiency (creatinine clearance less than 10 ml / min), the excretion of metabolites in the bile increases, while an increase in their concentration in the blood is not observed. In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetic parameters of diclofenac do not change. Diclofenac passes into breast milk. Indications for use Diseases that require rapid anti-inflammatory and / or analgesic effects: inflammatory rheumatic diseases (rheumatoid arthritis, spondyloarthritis, chronic juvenile arthritis and arthritis of other etiologies); degenerative rheumatism of the musculoskeletal system (arthrosis, spondylosis); microcrystalline arthritis (gouty arthritis, pseudogouty arthritis); extra-articular rheumatism (periarthritis, bursitis, myositis, tendinitis, synovitis); other inflammatory diseases of the musculoskeletal system, accompanied by pain. As an analgesic, the drug can be used for soft tissue injuries, in the postpartum period in the absence of breastfeeding, for primary and secondary dysmenorrhea, in dentistry and after surgical interventions. In accordance with general therapeutic principles, the underlying disease should be treated with basic therapy. Fever in itself is not an indication for the use of the drug. Dosing and Administration Suppositories are intended for rectal administration only. In order to reduce the risk of developing adverse events, the drug should be used at the lowest effective dose for the shortest period of time necessary to relieve symptoms. The suppository is released from the contour packaging and injected into the rectum, preferably after spontaneous bowel movements or a cleansing enema. After the introduction of the suppository, it is recommended to stay in bed for 20-30 minutes. Adults: 1 suppository 2-3 times a day. Perhaps the simultaneous use of the drug Diclovit® with oral forms of diclofenac. In this case, the total daily dose of diclofenac should not exceed 150 mg. Elderly patients Although there are no clinically significant changes in the pharmacokinetics of diclofenac in the elderly, non-steroidal anti-inflammatory drugs (NSAIDs) should be used in such patients with extreme caution due to a higher risk of adverse reactions. In particular, in debilitated elderly or underweight patients, it is recommended to use diclofenac at the lowest effective dose. In addition, such patients should be carefully monitored for bleeding from the gastrointestinal tract (GIT) during NSAID therapy in these patients. Patients with impaired renal function The use of diclofenac in patients with severe renal insufficiency is contraindicated. Special studies in patients with impaired renal function have not been conducted, so there are no specific recommendations for dose adjustment in patients in this group. Diclofenac should be used with caution in patients with mild to moderate renal insufficiency. Patients with impaired liver function The use of diclofenac in patients with severe hepatic impairment is contraindicated. Special studies in patients with impaired liver function have not been conducted, so there are no specific recommendations for dose adjustment in patients in this group. Diclofenac should be used with caution in patients with mild to moderate hepatic impairment. Use in children Use in children is contraindicated. Application during pregnancy and lactation Pregnancy Suppression of prostaglandin synthesis can adversely affect the course of pregnancy and intrauterine development of the fetus. Data from epidemiological studies indicate an increased risk of spontaneous abortion and / or the development of heart defects and gastroschisis after the use of prostaglandin synthesis inhibitors in early pregnancy. It is believed that the risk increases with increasing dose and duration of therapy. In animal studies, the administration of prostaglandin synthesis inhibitors has been associated with disruption of embryo implantation. In addition, in animals treated with inhibitors of prostaglandin synthesis during organogenesis, the incidence of various malformations, including developmental disorders of the cardiovascular system, increased. Diclofenac should not be taken during the first two trimesters of pregnancy unless the benefit outweighs the risk to the fetus. When prescribing diclofenac to women planning a pregnancy, or in the first and second trimesters of pregnancy, the lowest possible dose and the shortest duration of treatment should be chosen. When using prostaglandin synthesis inhibitors in the third trimester of pregnancy in the fetus, the following are possible: cardiopulmonary toxicity (with premature closure of the arterial duct and pulmonary hypertension); renal dysfunction, which can progress to renal failure with the development of oligohydramnios. The use of diclofenac at the end of pregnancy can cause: prolongation of bleeding time in the mother and newborn, antiplatelet effect may occur even after the use of very low doses of diclofenac; weakness of labor activity and an increase in the duration of labor. In this regard, the use of the drug Diclovit® in the third trimester of pregnancy is contraindicated. Lactation Diclofenac, like other NSAIDs, passes in small amounts into breast milk. To avoid possible undesirable effects on the child, the drug should not be administered to lactating women. If necessary, the use of the drug during lactation, breastfeeding should be discontinued. Precautions To reduce the risk of adverse events, the drug should be used at the lowest effective dose for the shortest period necessary to relieve symptoms. The simultaneous use of diclofenac with systemic NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided due to the lack of any synergistic effect and the possibility of developing additional side effects. Caution should be exercised when prescribing the drug to elderly patients. The lowest effective dose should be used in debilitated elderly and low body weight patients. Diclofenac, like other NSAIDs, can cause allergic reactions, including anaphylactic / anaphylactoid reactions, even if the drug has not been previously used by the patient. Like other NSAIDs, diclofenac, due to its pharmacodynamic properties, may mask the signs and symptoms of infection. Influence on the gastrointestinal tract Diclofenac, like other NSAIDs, can cause gastrointestinal bleeding (hemesis, melena, bloody diarrhea), ulcers and perforations that can develop at any time during treatment, regardless of the presence of gastrointestinal lesions in history and may not show symptoms. As a rule, such phenomena are most dangerous for elderly patients. With the development of gastrointestinal bleeding or ulceration, the drug should be discontinued. Careful medical supervision is necessary when prescribing diclofenac to patients with symptoms of gastrointestinal dysfunction or with a history of gastrointestinal ulcers, bleeding or perforation in history. The risk of gastrointestinal bleeding, ulceration or perforation increases with increasing doses of NSAIDs, including diclofenac, as well as in patients with a history of gastrointestinal ulcers, especially if they are complicated by bleeding or perforation. Elderly patients are more likely to develop side effects when using NSAIDs, especially for bleeding from the gastrointestinal tract and perforations, which can be fatal. To reduce the risk of gastrointestinal toxicity in patients, especially those with a history of ulcers, gastrointestinal bleeding and perforation, as well as in elderly patients, treatment should be started with the lowest effective dose and followed thereafter. For such patients, as well as for patients receiving concomitant therapy with acetylsalicylic acid or other drugs that may increase the risk of side effects from the gastrointestinal tract, it is necessary to consider combination treatment with gastroprotective agents (for example, misoprostol or proton pump inhibitors). Patients with a history of episodes of gastrointestinal toxicity, especially the elderly, should report all unusual abdominal symptoms (especially gastrointestinal bleeding). It is recommended that diclofenac be used with caution in patients receiving concomitant therapy with drugs that may increase the risk of ulceration or bleeding, including systemic corticosteroids, anticoagulants (including warfarin), selective serotonin reuptake inhibitors (SSRIs) or antiplatelet agents (in including acetylsalicylic acid). In patients with ulcerative colitis and Crohn’s disease, due to the possibility of an exacerbation of the disease, diclofenac should be used with caution and careful medical supervision should be carried out. Influence on liver function When prescribing diclofenac to patients with impaired liver function, careful medical supervision is necessary due to the possibility of an exacerbation of the disease. When using diclofenac and other NSAIDs, the level of one or more “liver” enzymes may increase. With prolonged therapy, a regular study of liver function is indicated. If violations of liver function parameters persist or increase, or if signs or symptoms develop that indicate liver disease, as well as if other side effects occur (for example, eosinophilia, rash, etc.), treatment with diclofenac should be discontinued. When using diclofenac, hepatitis can develop without prodromal symptoms. Caution is necessary when prescribing diclofenac to patients with hepatic porphyria, since the drug can provoke attacks of porphyria. Influence on renal function Due to the fact that there are reports of cases of fluid retention and edema associated with the use of NSAIDs, including diclofenac, caution should be exercised when using the drug in patients with impaired cardiac or renal function, arterial hypertension, elderly patients, patients receiving concomitant treatment with diuretics or drugs that may impair kidney function, and in patients with extracellular fluid volume depletion due to any cause (eg, before or after major surgery). In these cases, it is necessary to monitor kidney function. Stopping treatment usually results in restoration of function to its original level. Skin reactions With the use of NSAIDs, including diclofenac, very rarely reported severe, in some cases fatal, skin reactions, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. The greatest risk of developing these reactions was noted at the beginning of the course of therapy, during the first month of treatment. Diclofenac should be discontinued at the first appearance of a skin rash, mucosal lesions, or any other sign of hypersensitivity. Patients with systemic lupus erythematosus (SLE) and systemic connective tissue diseases have an increased risk of developing aseptic meningitis. Influence on the cardiovascular system Patients with significant risk factors for the development of cardiovascular complications (for example, arterial hypertension, hyperlipidemia, diabetes mellitus, smoking) should be prescribed diclofenac only after a thorough assessment of the benefit / risk ratio. Due to the possible increased risk of cardiovascular events with long-term or high dose use, diclofenac should be administered at the lowest effective dose for the shortest time necessary to reduce symptoms. The need for relief of symptoms and the effectiveness of treatment should be periodically reassessed. Due to the fact that cases of fluid retention and edema have been reported with the use of NSAIDs, including diclofenac, patients with arterial hypertension and / or mild to moderate heart failure should be carefully monitored. Clinical studies and epidemiological data indicate a possible increased risk of arterial thrombosis (eg, myocardial infarction or stroke) with the use of diclofenac, especially with prolonged use or use at high doses (150 mg per day). Patients with uncontrolled hypertension, congestive heart failure, established coronary artery disease, peripheral arterial disease and/or cerebrovascular disease should only be treated with diclofenac after a careful benefit/risk assessment. Influence on hematological parameters With a long course of treatment with diclofenac, as with other NSAIDs, monitoring of hematological parameters is necessary. Diclofenac, like other NSAIDs, can reversibly inhibit platelet aggregation. Careful monitoring of patients with impaired hemostasis, hemorrhagic diathesis or hematological disorders is necessary. Patients with bronchial asthma Patients with bronchial asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (including nasal polyps), chronic obstructive pulmonary disease or chronic respiratory tract infections (especially if they are accompanied by symptoms of rhinitis that has an allergic character) more often than in other patients, when using NSAIDs, adverse reactions develop according to the type of bronchospasm (the so-called intolerance to acetylsalicylic acid or other NSAIDs, “aspirin” asthma), Quincke’s edema or urticaria. The drug should be used with extreme caution in these patients (you must be prepared to provide emergency assistance). These recommendations also apply to patients who have a history of allergic reactions to other substances, such as skin rash, itching, urticaria. Like other drugs that inhibit the activity of cyclooxygenases, diclofenac and other NSAIDs can cause bronchospasm in patients with a history of bronchial asthma. Influence on fertility in women Due to the fact that the use of diclofenac may impair fertility, women planning pregnancy, the drug is not recommended. In patients with infertility (including those undergoing examination in connection with this), it is recommended to consider the possibility of discontinuing the drug. Use in children The use of the drug in children is contraindicated. Influence on the ability to drive vehicles or other mechanisms Patients who notice dizziness, drowsiness, other symptoms of impaired activity of the central nervous system, weakness or visual impairment during the use of the drug are not recommended to drive vehicles or other mechanisms. Interaction with other drugs If you are taking any drugs, tell your doctor. Lithium, Digoxin: Diclofenac may increase plasma concentrations of lithium and digoxin. It is recommended to monitor the concentration of lithium and digoxin in plasma while using Diclovit®. Diuretics and antihypertensive drugs: diclofenac, like other NSAIDs, may reduce the hypotensive effect of diuretic and antihypertensive drugs. Patients, especially the elderly, these combinations should be administered with caution and regularly monitor blood pressure. Patients must be adequately hydrated. After the start and periodically during treatment, especially with the simultaneous appointment of diuretics and angiotensin-converting enzyme (ACE) inhibitors, it is necessary to monitor renal function due to an increased risk of nephrotoxicity. Drugs that cause hyperkalemia: the simultaneous use of diclofenac with potassium-sparing diuretics, cyclosporine, tacrolimus or trimethoprim can lead to an increase in the concentration of potassium in the blood serum (in the case of using such a combination of drugs, this indicator should be regularly monitored). Anticoagulants and antiplatelet agents: Although clinical studies have not established the effect of diclofenac on the action of anticoagulants, there are separate reports of an increased risk of bleeding in patients taking diclofenac and these drugs at the same time. In the case of such a combination of drugs, regular and careful monitoring of patients is recommended. NSAIDs and corticosteroids: The simultaneous systemic use of diclofenac and other NSAIDs, including selective cyclooxygenase-2 inhibitors, or corticosteroids may increase the risk of side effects (gastrointestinal bleeding and ulceration). Selective serotonin reuptake inhibitors (SSRIs): the simultaneous use of diclofenac and drugs from the SSRI group increases the risk of gastrointestinal bleeding. Antidiabetic drugs: In clinical studies, diclofenac has not been found to interfere with the effectiveness of oral antidiabetic drugs when used together. However, there are separate reports of the development of both hypoglycemia and hyperglycemia, which required a change in the dose of hypoglycemic drugs during diclofenac therapy. Patients taking antidiabetic drugs and diclofenac at the same time should regularly monitor their blood glucose levels. Methotrexate: Caution is required when prescribing NSAIDs less than 24 hours before or after taking methotrexate, because in such cases, the concentration of methotrexate in the blood may increase (due to a decrease in renal clearance) and its toxic effect may increase. Cyclosporine: The effect of NSAIDs on the synthesis of prostaglandins in the kidneys may increase the nephrotoxicity of cyclosporine. In this regard, the dose of diclofenac in patients receiving cyclosporine should be lower than in patients not receiving cyclosporine. Tacrolimus: possible increase in nephrotoxicity with simultaneous use with diclofenac. Quinolone antibacterial agents: there are separate reports of the development of seizures in patients (including those without a history of indications of epilepsy or seizures) who received both quinolone derivatives and NSAIDs. Phenytoin: With the simultaneous use of phenytoin and diclofenac, it is necessary to control the concentration of phenytoin in the blood plasma due to the possible increase in its systemic effects. Colestipol and cholestyramine: These drugs can slow down or reduce the absorption of diclofenac, so it is recommended to take diclofenac at least one hour before or 4-6 hours after taking colestipol or cholestyramine. Cardiac glycosides: the simultaneous use of cardiac glycosides and NSAIDs can cause an exacerbation of heart failure, lead to a decrease in the glomerular filtration rate and an increase in the concentration of cardiac glycosides in the blood plasma. Mifepristone: NSAIDs should not be used within 8 to 12 days of mifepristone use due to possible decreased effect of mifepristone. Strong inhibitors of the CYP2C9 isoenzyme: Caution should be exercised when co-administering diclofenac and strong inhibitors of the CYP2C9 isoenzyme (such as voriconazole) due to the possible significant increase in plasma concentrations of diclofenac due to inhibition of its metabolism. Contraindications Hypersensitivity (including to other non-steroidal anti-inflammatory drugs), complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including history), erosive and ulcerative lesions gastrointestinal tract (in the acute phase), active gastrointestinal bleeding, a history of or recurrent gastric or duodenal ulcer with or without episodes of bleeding (two or more separate confirmed episodes of ulceration or bleeding); inflammatory bowel disease (Crohn’s disease, ulcerative colitis), severe liver failure; congestive heart failure (functional class II-IV according to the classification of the New York Heart Association (NYHA)), coronary heart disease; peripheral arterial disease or cerebrovascular disease; treatment of postoperative pain after coronary artery bypass surgery or when using a heart-lung machine; severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, active liver disease, confirmed hyperkalemia; rectal bleeding, hemorrhoids, trauma or inflammation of the rectal mucosa, proctitis; pregnancy (III trimester), lactation period; childhood. Composition One suppository contains: active ingredient: diclofenac sodium – 50 mg; excipient: solid fat – to obtain a suppository weighing 1.26 g. , hepatotoxic effect, respiratory depression, coma. Treatment: symptomatic therapy aimed at eliminating arterial hypotension, impaired renal function, convulsions, irritation of the gastrointestinal tract, respiratory depression. Forced diuresis, hemodialysis are ineffective (due to a significant connection with proteins and intensive metabolism). Side effect Criteria for assessing the frequency of adverse reactions: very often (more than 1/10), often (more than or equal to 1/100, less than 1/10), infrequently (more than or equal to 1/1000, less than 1/100), rarely (more than or equal to equal to 1/10000, less than 1/1000), very rarely (less than 1/10000); not known (cannot be estimated from available data). On the part of the blood and lymphatic system: very rarely – thrombocytopenia, leukopenia, anemia (including hemolytic and aplastic anemia), agranulocytosis. Immune system disorders: rarely – hypersensitivity, anaphylactic and anaphylactoid reactions (including arterial hypotension and shock); very rarely – angioedema (including swelling of the face). Mental disorders: very rarely – disorientation, depression, insomnia, nightmares, irritability, psychotic disorders. Nervous system disorders: often – headache, dizziness; rarely – drowsiness, increased fatigue; very rarely – paresthesia, memory impairment, convulsions, anxiety, tremor, aseptic meningitis, taste disorders, acute cerebrovascular accident; not known – confusion, hallucinations, perceptual disturbances, malaise. On the part of the organ of vision: very rarely – visual disturbances, blurred vision, diplopia; not known – optic neuritis. Hearing disorders and labyrinth disorders: often – vertigo; very rarely – tinnitus, hearing impairment. Cardiac disorders: very rarely – palpitations, chest pain, heart failure, myocardial infarction. Vascular disorders: very rarely – arterial hypertension, hypotension, vasculitis. Respiratory system, chest and mediastinal disorders: rarely – bronchospasm, shortness of breath; very rarely – pneumonitis. Gastrointestinal disorders: often – nausea, vomiting, diarrhea, dyspepsia, abdominal pain, bloating, anorexia; rarely – gastritis, gastrointestinal bleeding (bloody vomiting, melena, diarrhea mixed with blood), stomach and / or intestinal ulcers, accompanied or not accompanied by bleeding or perforation (in some cases fatal, especially in elderly patients); very rarely – colitis (including hemorrhagic colitis and exacerbation of ulcerative colitis or Crohn’s disease), constipation, stomatitis (including ulcerative stomatitis), glossitis, esophageal dysfunction, diaphragm-like intestinal stenosis, pancreatitis. Liver and biliary tract disorders: often – increased activity of “liver” transaminases; rarely – hepatitis, jaundice, impaired liver function; very rarely – fulminant hepatitis, liver necrosis, liver failure. Skin and subcutaneous tissue disorders: often – rash; rarely – urticaria; very rarely – bullous rash, eczema, erythema, erythema multiforme, Stevens-Johnson syndrome, Lyell’s syndrome (toxic epidermal necrolysis), exfoliative dermatitis, hair loss, photosensitivity reactions; purpura, including allergic, itching. Renal and urinary disorders: very rarely – acute renal failure, hematuria, proteinuria, interstitial nephritis; nephrotic syndrome; papillary necrosis. General disorders and disorders at the injection site: rarely – irritation in the area of application, swelling. Violations of the genital organs and mammary glands: very rarely – impotence. Clinical studies and epidemiological data suggest that diclofenac, especially at high doses (150 mg per day) and with prolonged use, may lead to an increased risk of arterial thromboembolism (for example, myocardial infarction or stroke). place, at a temperature not exceeding 25 ° C. 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