Naklofen solution for injections 75mg/3ml in 3ml ampoules in blister №5×1

Name:
Naklofen solution din. 75mg3ml in amp. 3ml in blister. in pack. No. 5×1
Description:
Transparent, colorless or light yellow solution, practically free from particles. The main active substance Release formSolution for intramuscular injection is transparent, colorless or slightly yellowish, without visible mechanical inclusions. Dosage 75 mg 3 ml Special indications The drug when administered intramuscularly is intended for the treatment of: inflammatory and degenerative forms of rheumatism, rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, arthrosis, spondyloarthritis, vertebral pain syndrome, extra-articular rheumatism; acute attacks of gout; renal and hepatic colic; inflammation, pain and swelling after injuries and operations; severe migraine attacks. The drug, when administered as an intravenous infusion, is intended for the treatment or prevention of postoperative pain. Pharmacodynamics Diclofenac is a non-steroidal anti-inflammatory drug with analgesic, anti-inflammatory and antipyretic effects. It inhibits the activity of cyclooxygenase and therefore the synthesis of prostaglandins. During treatment with diclofenac, a decrease in prostaglandin levels is observed in urine, gastric mucus and synovial fluid. The drug is used to treat all forms of rheumatic diseases, as well as to reduce pain of various origins. Pharmacokinetics Distribution. The maximum plasma concentration is reached in half an hour. More than 99% of diclofenac binds to plasma proteins, mainly albumin. Diclofenac enters the synovial fluid, where it reaches a concentration of 60 to 70% of the plasma value. After a period of time from 3 to 6 hours, the concentration of the active substance and its metabolites in the synovial fluid is higher than in plasma. Diclofenac is more slowly excreted from synovial fluid than from plasma. Metabolism and excretion. The biological half-life (T1 / 2) is 1? 2 hours. With a mild degree of renal or hepatic dysfunction, it remains unchanged. Diclofenac is almost completely metabolized in the liver, mainly by hydroxylation and methoxylation. About 70% of the drug dose is excreted in the urine as pharmacologically inactive metabolites. Only 1% of diclofenac is excreted unchanged. The rest of the metabolites are excreted in the bile and faeces. In elderly patients, the absorption, metabolism or excretion of the drug does not change significantly. Route of administration and doses Side effects can be minimized by using the minimum effective dose for the minimum period necessary to control symptoms (see section “Precautions”). Naklofen injection can be administered intramuscularly, by deep injection into the upper outer square of the gluteus maximus muscle, or as a slow intravenous infusion after dilution, as described in the instructions. Naklofen solution for injection (for intramuscular or intravenous administration) should not be used for more than two days; if necessary, treatment can be continued with tablets, capsules or suppositories of Naklofen. Each ampoule is for single use only. The solution should be used immediately after opening the ampoule. Any unused content must be disposed of. Intramuscular injection In order to prevent damage to nerve or other tissues at the site of intramuscular injection, the following rules must be observed. The dose is usually one ampoule of 75 mg per day, by deep injection into the upper outer square of the gluteus maximus muscle. If two injections per day are required, then one injection is administered in each buttock. Alternatively, one 75 mg ampoule can be combined with other formulations of Naklofen (enteric-coated tablets, extended release tablets, capsules or suppositories) up to a maximum daily dose of 150 mg. For migraine attacks, the available clinical experience is limited to the use as follows: treatment is started as early as possible with the appointment of 1 ampoule of 75 mg, if necessary, treatment is continued with suppositories on the same day at a dose of up to 100 mg. The total dose on the first day should not exceed 175 mg. There are no data on the use of Naklofen for more than 1 day for migraine. If it is necessary to continue treatment in the following days, it should be limited to the use of suppositories in a daily dose of up to 150 mg, divided into several single doses. Intravenous infusions Naklofen, solution for injection, should not be administered as an intravenous bolus injection. Immediately before the start of intravenous infusion, Naklofen, depending on the required duration, should be diluted 100? 150 ml of 0.9% sodium chloride solution or with 5% glucose solution, buffered sodium bicarbonate solution for injection (0.5 ml of 8.4% solution or 1 ml of 4.2%) taken from a freshly opened container; add to this solution the contents of one ampoule of the drug Naklofen. Only clear solutions can be used. If there are crystals or sediment in the solution, then it cannot be used for infusion. Two alternative dosing regimens are recommended for Naklofen, injection. For the treatment of moderate and severe postoperative pain, 75 mg should be administered continuously from 30 minutes to 2 hours. If necessary, treatment can be repeated after a few hours, but the dose should not exceed 150 mg during any period of 24 hours. For the prevention of postoperative pain, 15 minutes to 1 hour after surgery, a loading dose of 25-50 mg should be administered, after which a continuous infusion of approximately 5 mg / hour should be used up to a maximum daily dose of 150 mg. Selected groups of patients Elderly patients (65 years and older) The use of the minimum effective dose is recommended. Patients with proven congestive heart failure (NYHA II-IV), ischemic heart disease, peripheral arterial disease and/or cerebrovascular disease Diclofenac is contraindicated in patients with proven congestive heart failure (NYHA II-IV), coronary artery disease, peripheral arterial disease and/or cerebral vessels. Patients with impaired renal function Diclofenac is contraindicated in patients with severe renal insufficiency. Since special studies have not been conducted in patients with impaired renal function, specific recommendations for dose adjustment cannot be made. Caution is advised when using diclofenac in patients with mild to moderate renal impairment. Patients with impaired liver function Diclofenac is contraindicated in patients with severe hepatic impairment. Since special studies have not been conducted in patients with impaired liver function, specific recommendations for dose adjustment cannot be made. Caution is advised when using diclofenac in patients with mild to moderate hepatic impairment. Method of application Intramuscular or intravenous administration. Application during pregnancy and lactation 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 miscarriage and / or the development of heart defects and gastroschisis after taking prostaglandin synthesis inhibitors in early pregnancy. The absolute risk of cardiovascular disease increases from less than 1% to 1.5%. It is believed that the risk increases with increasing dose and duration of therapy. It has been shown that the administration of prostaglandin synthesis inhibitors in animals leads to disruption of embryo implantation. In addition, in animals treated with a prostaglandin synthesis inhibitor during organogenesis, the incidence of various malformations, including developmental disorders of the cardiovascular system, increased. Diclofenac should not be given during the first two trimesters of pregnancy unless the benefit outweighs the risk to the fetus. If, nevertheless, Naklofen is used in a woman in the first or second trimester of pregnancy, then the dose should be minimal, and the duration of treatment? as short as possible. As with other NSAIDs, the use of the drug during the third trimester of pregnancy is contraindicated. When taking inhibitors of prostaglandin synthesis in the third trimester of pregnancy in the fetus, the following are possible: 1) premature closure of the arterial duct and pulmonary hypertension, 2) renal dysfunction, the progression of which develops renal failure with oligohydroamnion. When taking diclofenac at the end of pregnancy, the development of weak labor and an increase in the duration of labor is possible. In the mother and in the fetus / newborn, bleeding time may be prolonged, and an antiaggregatory effect may occur even after taking very low doses of diclofenac. Thus, diclofenac is contraindicated during the third trimester of pregnancy. Lactation Like other NSAIDs, a small amount of diclofenac is excreted in breast milk. Therefore, diclofenac should not be used during breastfeeding to avoid unwanted effects in the baby. Influence on fertility The use of diclofenac sodium can lead to impaired female fertility, and is not recommended for women trying to conceive a child. In women who have difficulty conceiving or who are suspected of being infertile, treatment with diclofenac sodium should be discontinued. Influence on the ability to drive vehicles and equipment Naklofen has a slight or moderate effect on the ability to drive vehicles and machines. Patients who experience dizziness and / or other undesirable effects from the central nervous system when taking diclofenac should not drive a car or work with dangerous mechanisms. Precautions Side effects of the drug can be reduced by using the lowest effective dose for the shortest period necessary to relieve symptoms. The co-administration of Naklofen with other NSAIDs, including selective cyclooxygenase-2 inhibitors, should be avoided due to the lack of evidence of synergistic effects and the occurrence of potentially dangerous additive effects. In the presence of medical indications, it is recommended to prescribe treatment with caution in elderly patients. In particular, treatment should be started with the lowest effective dose of the drug, especially in debilitated elderly patients or those with low body weight. As with other NSAIDs, diclofenac can rarely cause allergic reactions, including anaphylactic/anaphylactoid reactions. Like other NSAIDs, due to the peculiarities of the pharmacodynamic properties, diclofenac can mask the signs and symptoms of infectious diseases. Influence on the gastrointestinal tract When taking NSAIDs, including diclofenac, gastrointestinal bleeding, ulcers or perforations, sometimes fatal, were observed, which were observed regardless of the period of treatment and were accompanied / not accompanied by symptoms and a history of serious gastrointestinal disturbances. As a rule, they have more serious consequences in older people. If ulcer or gastrointestinal bleeding occurs in patients receiving diclofenac, the drug should be discontinued. As with other NSAIDs, including diclofenac, medical supervision is necessary, especially caution should be exercised when prescribing diclofenac in patients with symptoms suggestive of gastrointestinal disorders, patients with stomach or intestinal ulcers, bleeding or perforation in history. The risk of gastrointestinal bleeding increases with increasing dose of NSAIDs, especially in patients with a history of ulcer complicated by hemorrhage or perforation. Elderly patients have a higher incidence of adverse reactions when taking NSAIDs, especially gastrointestinal bleeding and perforation, sometimes fatal. To reduce the risk of gastrointestinal toxicity in patients with a history of peptic ulcer disease (complicated by bleeding or perforation) and in elderly patients, treatment should begin with the lowest effective dose of the drug. These patients should consider combination therapy with protective agents (eg, misoprostol or proton pump inhibitors), as well as patients taking drugs containing acetylsalicylic acid in low doses (acetylsalicylic acid drugs/aspirin increase the risk of gastrointestinal disorders). Patients, especially the elderly, should report any unusual abdominal symptoms (especially bleeding) to the physician. Naklofen should be administered with caution to patients who are simultaneously taking medicinal products that may increase the risk of bleeding and ulcers, such as systemic corticosteroids, anticoagulants, selective serotonin reuptake inhibitors, or antiplatelet agents. Careful medical supervision is necessary for patients suffering from ulcerative colitis or Crohn’s disease, since the course of these diseases may worsen. Influence on the liver Careful medical supervision is necessary for patients with impaired liver function, tk. their condition may worsen. During therapy with diclofenac, an increase in the activity of liver enzymes may be observed. Diclofenac should be discontinued immediately if elevated liver enzymes persist or increase, clinical signs consistent with liver disease, or other manifestations (eg, eosinophilia, rash) appear. With prolonged use of diclofenac, regular monitoring of liver function is recommended. When taking diclofenac, hepatitis can occur without previous symptoms. Caution should be exercised when prescribing diclofenac to patients with hepatic porphyria, tk. this can exacerbate the disease. Effects on kidney function Cases of fluid retention and edema have been reported with NSAIDs, including diclofenac. Particular caution should be exercised in patients with impaired cardiac or renal function, patients with a history of arterial hypertension, in the appointment of elderly patients receiving concomitant therapy in the form of diuretics or drugs that can significantly affect renal function and patients with significant depletion of extracellular volume, associated with various causes, such as before or after major surgery. When prescribing diclofenac, regular monitoring of kidney function is recommended. Cancellation of therapy is usually accompanied by the normalization of their functions. Effects on the skin and subcutaneous tissue In rare cases, the use of NSAIDs, there were serious skin reactions, some fatal, including exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis. Patients are most at risk at the beginning of therapy: in most cases, the observed adverse reactions occurred in the first month of treatment. Treatment with Naklofen should be discontinued at the first signs of skin and mucosal rash, as well as other signs of hypersensitivity. Influence on the cardiovascular and cerebrovascular systems Patients with arterial hypertension and / or mild congestive heart failure require careful monitoring due to the possible development of fluid retention in the body and edema during treatment with non-selective non-steroidal anti-inflammatory drugs (NSAIDs). Results, clinical trials and epidemiological data suggest an increased risk of arterial thromboembolic complications (eg, myocardial infarction or stroke) associated with the use of diclofenac, especially at high doses (150 mg per day) and with long-term treatment. In patients at high risk of cardiovascular events (eg, arterial hypertension, hyperlipidemia, diabetes mellitus, smoking), diclofenac is prescribed only after a thorough examination. The risk of cardiovascular events depends on the dose and duration of treatment with diclofenac, therefore, it is necessary to use the lowest effective dose, the shortest duration of treatment. Depending on the relief of symptoms and the condition of the patient, the dose of the drug should be reviewed periodically. Hematological effects Diclofenac is recommended for short-term use only. During long-term therapy, careful monitoring of blood counts is necessary. Like other NSAIDs, diclofenac may temporarily inhibit platelet aggregation. Patients with hemostasis disorders should be carefully monitored. Pre-existing asthma In patients with asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (i.e. nasal polyps), chronic obstructive pulmonary disease, or chronic respiratory infections (especially those associated with allergic rhinitis or having similar symptoms) more often than other patients, there are exacerbations of bronchial asthma (the so-called intolerance to analgesics), Quincke’s edema or urticaria. Therefore, such patients, as well as patients allergic to other substances with skin reactions, itching or urticaria, are advised to take special precautions. Information on excipients 3 ml of solution (one ampoule) contains 120 mg of benzyl alcohol. Benzyl alcohol is contraindicated in newborns and children under 3 years of age. In susceptible individuals, especially those with a history of asthma and allergies, metabisulphite may cause allergic-type reactions, including symptoms of an anaphylactic reaction and bronchospasm. Naklofen contains less than 1 mmol (23 mg) sodium per dose, i.e. essentially “sodium-free”. Interaction with other drugs Lithium: co-administration may increase the plasma concentration of lithium. Therefore, monitoring of serum lithium levels is recommended. Digoxin: Co-administration may increase the plasma concentration of digoxin. Therefore, monitoring of serum digoxin levels is recommended. Diuretics and antihypertensive drugs: Like other NSAIDs, co-administration of diclofenac with diuretics or antihypertensive agents (eg, beta-blockers, angiotensin-converting enzyme inhibitors (ACE)) may lead to a decrease in their antihypertensive effect. Therefore, when combining these drugs, caution should be exercised, especially in elderly patients, and periodic monitoring of blood pressure is also necessary. After the start of concomitant therapy and periodically with its further continuation due to an increased risk of developing a sufficient amount of fluid in the joint intake of diuretics with potassium-sparing drugs in the blood serum. Therefore, frequent monitoring of potassium levels is necessary. Other NSAIDs and corticosteroids: Co-administration of diclofenac and other systemic NSAIDs or corticosteroids may increase the incidence of adverse gastrointestinal effects. Anticoagulants and antiplatelet agents: It is recommended to use with caution, because. co-administration may increase the risk of bleeding. Despite the fact that clinical studies have not revealed the effect of diclofenac on the action of anticoagulants, there are separate reports of an increased risk of bleeding in patients receiving diclofenac and anticoagulants at the same time. Such patients should be carefully monitored. Selective serotonin reuptake inhibitors (SSRIs): Concomitant use of systemic NSAIDs, including diclofenac, and SSRIs may increase the risk of gastrointestinal bleeding. Antidiabetic drugs: Clinical studies have shown that diclofenac does not interfere with the clinical effects of oral antidiabetic agents. However, there are separate reports of hypoglycemic and hyperglycemic effects requiring a change in the dosage of antidiabetic drugs during treatment with diclofenac. Therefore, during concomitant therapy, glucose monitoring is recommended as a precautionary measure. Methotrexate: Diclofenac can inhibit the tubular renal clearance of methotrexate and thereby increase its level. With concomitant therapy, it is recommended to use NSAIDs, including diclofenac, with caution. Since diclofenac can increase the concentration, and therefore the toxicity of methotrexate, this drug is administered at least 24 hours before or after treatment with methotrexate. Cyclosporins: Diclofenac, like other NSAIDs, may increase nephrotoxicity due to effects on renal prostaglandins. Diclofenac is recommended to be administered at doses lower than those that would be used in patients not receiving cyclosporins. Quinolone antibacterials: There have been isolated reports of seizures that may have been associated with the concomitant use of quinolones and NSAIDs. Phenytoin: When taking phenytoin together, periodic monitoring of plasma phenytoin concentrations is recommended due to a possible increase in phenytoin. Colestipol and cholestyramine: These agents may delay or decrease the absorption of diclofenac. Therefore, it is recommended to administer diclofenac at least one hour before or 4 to 6 hours after the administration of colestipol/cholestyramine. Potent CYP2C9 inhibitors: Caution is advised when diclofenac is used with potent CYP2C9 inhibitors (eg, sulfinpyrazone and voriconazole), as there may be a significant increase in maximum plasma concentration and exposure to diclofenac due to inhibition of its metabolism. Use with caution with other drugs known to be hepatotoxic, eg antibiotics, antiepileptic drugs. Contraindications Hypersensitivity to diclofenac, sodium metabisulphite, or other components of the drug. Like other non-steroidal anti-inflammatory drugs, diclofenac is contraindicated in patients in whom hypersensitivity to salicylates or other inhibitors of prostaglandin synthesis manifests itself in the form of bronchial asthma, urticaria or rhinitis. Liver failure (Child-Pugh Class C) (cirrhosis of the liver and ascites). Renal failure (creatinine clearance < 30 ml min.). Last trimester of pregnancy. Ulcerative lesions of the stomach or duodenum, gastrointestinal bleeding or perforation. Proven congestive heart failure (NYHA II-IV), ischemic heart disease, peripheral arterial and/or cerebrovascular disease. In patients with a high risk of postoperative bleeding, anticoagulation, incomplete hemostasis, impaired hematopoiesis or cerebrovascular bleeding. Treatment of postoperative pain after coronary artery bypass grafting (or using a heart-lung machine). Inflammatory bowel disease (eg Crohn's disease and ulcerative colitis). Children's age up to 18 years. Composition 3 ml of solution (1 ampoule) contains: Active substance: diclofenac sodium 75 mg. Excipients: benzyl alcohol, propylene glycol, sodium metabisulphite, sodium hydroxide, water for injection. OverdosageSymptoms There is no typical clinical picture of diclofenac overdose. Overdose may cause symptoms such as vomiting, gastrointestinal disturbances, diarrhoea, dizziness, tinnitus or convulsions. In case of severe poisoning? acute renal failure, possibly liver damage. Therapeutic measures The therapeutic tactics of acute poisoning with NSAIDs, including diclofenac, consists of supportive and symptomatic therapy. Supportive and symptomatic therapy should be carried out for such complications as hypotension, renal failure, convulsions, disorders of the gastrointestinal tract, respiratory depression. Special measures such as forced diuresis, dialysis, or hemoperfusion are likely to have little effect in eliminating NSAIDs, including diclofenac, due to high protein binding and extensive metabolism. Treatment is symptomatic. Side effects Side effects that occur during treatment with diclofenac sodium are classified into appropriate groups depending on the frequency of occurrence: very common (? 1/10), frequent (? 1/100 to < 1/10), infrequent (? 1/1000 to < 1/100), rare (? 1/10000 to < 1/1000), very rare (< 1/10000), unknown (cannot be assumed from the available data). Within each group, side effects of the drug are presented in order of decreasing significance. The most common side effects are gastrointestinal disturbances. Gastrointestinal bleeding, peptic ulcer, perforation, sometimes fatal, are more common in the elderly. The frequency of side effects is listed for individual organ systems. Blood and lymphatic system disorders Very rare: anemia (including hemolytic and aplastic), thrombocytopenia, leukopenia, agranulocytosis. Immune system disorders Rare: hypersensitivity reactions, anaphylactic and anaphylactoid reactions (including bronchospasm, hypotension, shock); Very rare: angioedema (including swelling of the face). Psychiatric disorders Very rare: confusion, depression, insomnia, nightmares, irritability, psychotic reactions. Nervous system disorders Common: headache, dizziness; Rare: dizziness, fatigue; Very rare: paresthesia, memory impairment, convulsions, anxiety, tremor, aseptic meningitis, taste disturbance, cerebrovascular accident. Visual disturbances Very rare: blurred vision, blurred vision, diplopia. Hearing and labyrinth system disorders Frequent vertigo; Very rare: tinnitus, hearing impairment. Cardiac disorders Very rare: palpitations, chest pain, heart failure, myocardial infarction. Vascular disorders Very rare: hypertension, vasculitis. Respiratory, thoracic and mediastinal disorders Rare: asthma (including shortness of breath); Very rare: pneumonia. Gastrointestinal disorders Common : nausea, vomiting, diarrhea, dyspepsia, abdominal pain, flatulence, anorexia; Infrequent: constipation; Rare: Gastritis, gastrointestinal bleeding, hematemesis, melena, hemorrhagic diarrhea, gastrointestinal ulcer with or without bleeding or perforation; Very rare: Colitis (including hemorrhagic, exacerbation of ulcerative colitis or Crohn's disease), stomatitis (including ulcerative), glossitis, disorders of the sides of the esophagus, stricture-like changes in the small intestine, pancreatitis. Disorders of the hepatobiliary system Common: increased levels of transaminases; Rare: jaundice, asymptomatic hepatitis, acute hepatitis, chronic active hepatitis, hepatocellular necrosis, cholestasis; Very rare: fulminant hepatitis, liver failure. Skin and subcutaneous tissue disorders Common: rash; Rare: urticaria; Very rare: bullous reactions, eczema, erythema, erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, hair loss, photosensitivity reactions, purpura, allergic purpura, pruritus. Renal and urinary tract disorders Very rare: renal failure, acute renal failure, hematuria, interstitial nephritis, nephrotic syndrome, papillary necrolysis, proteinuria. General and administration site disorders Common: injection site reaction injection, pain at the injection site, induration at the injection site; Rare: edema, necrosis at the injection site. Infections and invasions Very rare: abscess at the injection site. Based on clinical trial data and epidemiological data, it can be assumed that the use of diclofenac, especially at high doses (150 mg daily), over a long period of time may be associated with a slight increase in the risk of thrombosis arteries (for example, the risk of developing a myocardial infarction or stroke). If serious adverse effects occur, treatment should be discontinued. Storage conditionsStore at a temperature not exceeding 25 °C. Keep out of the reach of children. Buy Naklofen injection solution 75mg/3ml in 3ml ampoules in blister №5x1 3ml in blister №5x1