Diclofenac Hemofarm injection 25mg / ml amp 3ml 5 pcs

Description

Composition
Active substance:
1 ml of the solution contains 25.0 mg sodium diclofenac.
Excipients:
Benzyl alcohol, sodium metabisulfite, mannitol, sodium hydroxide, propylene glycol, water for injections.
Description:
Transparent colorless to slightly yellow colored solution with a faint characteristic odor of benzyl alcohol.
Product form:
Solution for intramuscular administration of 25 mg / ml.
3 ml of the product in clear glass ampoules of hydrolytic class I. Per vial paint brown plotted point and the ring.
5 ampoules in blisters of PVC film and aluminum foil.
Blisters together with instructions for use placed in a pile of cardboard.
Contraindications
Hypersensitivity (r. H. In other NSAIDs or auxiliary components), erosive and ulcerative lesions of the gastrointestinal tract (GIT) in the acute phase, bleeding from the gastrointestinal tract. inflammatory bowel disease in the acute phase (ulcerative colitis, Crohn’s disease), severe liver failure or liver disease in acute, severe renal impairment (creatinine clearance less than 30 mL / min), progressive kidney disease, hyperkalemia; bronchoobstruction, rhinitis, urticaria, provoked by taking aspirin or other NSAIDs (including a history..).; hemodyscrasia, disorders of hemostasis (in t. h. hemophilia), pregnancy, child (under 18 years), lactation, since the aortocoronary bypass, confirmed chronic heart failure (II-IV functional class NYHA classification), coronary heart disease, peripheral artery disease, or cerebrovascular disease; uncontrolled hypertension.
Dosage
25 mg / ml
Indications
For short-term symptomatic treatment of pain of various genesis of moderate intensity:
Inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Bechterew’s disease); gouty arthritis, rheumatic soft tissue, osteoarthritis peripheral joints and spine (including with radicular syndromes..); lumbago, sciatica, neuralgia; algomenorrhea, inflammatory pelvic incl adnexitis..; posttraumatic pain, accompanied by inflammation; renal colic; post-operative pain.
Interaction with other drugs
lithium preparations, digoxin: Diclofenac may increase the concentration of lithium and digoxin in the blood plasma; while the application is recommended to monitor the concentration of lithium and digoxin in plasma.
Diuretics and antihypertensive drugs: diclofenac, like other NSAIDs, may reduce the hypotensive action of diuretics and antihypertensives. Patients, especially the elderly, the combination should be administered with caution and regular monitoring of blood pressure. Patients should be adequately hydrated. After the beginning of and periodically during treatment, particularly with concomitant administration of diuretics, and angiotensin-converting enzyme (ACE), it is necessary to monitor renal function due to increased risk of nephrotoxicity.
Drugs that cause hyperkalemia: simultaneous application of diclofenac potassium-sparing diuretics, cyclosporine, tacrolimus, or trimethoprim can lead to increased concentration of potassium in blood serum (in the case of this combination of drugs active component should regularly monitor).
Anticoagulants and antiplatelet agents: although clinical studies have not been found to influence of diclofenac on the action of anticoagulants, there have been reports of an increased risk of bleeding in patients taking diclofenac and both these drugs. In the case of this combination of drugs recommended regular and careful monitoring of patients. Like other NSAIDs diclofenac in high doses can reversibly inhibit platelet aggregation.
NSAIDs and corticosteroids are: concurrent systemic administration of Diclofenac and other NSAIDs, including selective cyclooxygenase-2 (COX-2), or corticosteroids may increase the risk of side-effects (gastro-intestinal bleeding and ulceration); Avoid the simultaneous application of two or more NSAIDs.
Selective serotonin reuptake inhibitor (SSRI) and the simultaneous application of diclofenac formulations of SSRIs increase the risk of gastrointestinal bleeding.
Hypoglycemic drugs in clinical studies have found that the joint application of diclofenac does not affect the effectiveness of hypoglycemic drugs. However, the development of the known individual messages in cases such as hypoglycemia and hyperglycemia, which required changing the dose of hypoglycaemic agents during treatment with diclofenac. Therefore, during the joint application of diclofenac and hypoglycemic drugs recommended for monitoring blood glucose concentrations.
Methotrexate: Care must be taken when assigning diclofenac less than 24 hours before or 24 hours after methotrexate administration, as in such cases the MTX concentration may be increased in the blood (due to lower renal clearance) and amplify its toxic effects.
Cyclosporin: diclofenac influence on prostaglandin synthesis in the kidneys may enhance cyclosporine nephrotoxicity. Therefore applied dose of diclofenac should be lower than in patients who do not use cyclosporine.
Tacrolimus: nephrotoxicity may increase while the use of diclofenac.
Antibacterials – quinolone derivatives: there are isolated reports of seizures in patients developing (including no history or indication of epilepsy seizures..), Treated with both quinolone derivatives and NSAIDs.
Phenytoin: while applying phenytoin and diclofenac need to monitor the concentration of phenytoin in blood plasma due to the possible increase of its systemic exposure.
Colestipol and colestyramine: these drugs can inhibit or reduce the absorption of diclofenac, diclofenac is therefore recommended to take at least one hour before or after 4-6 hours after ingestion of colestipol or cholestyramine. Cardiac glycosides: the simultaneous use of cardiac glycosides and NSAIDs can cause aggravation of heart failure, result in lower glomerular filtration rate and increased concentrations of cardiac glycosides in blood plasma.
Mifepristone: NSAIDs should not be used for 8-12 days after administration of mifepristone in connection with a possible decrease in the effect of mifepristone.
Strong inhibitors isoenzyme CYP2C9: caution when coadministered diclofenac and potent inhibitors of CYP2C9 (such as voriconazole) because of the possible considerable increase in the diclofenac concentration in plasma is due to inhibition of its metabolism.
Overdose
symptoms:
Vomiting, bleeding from the gastrointestinal tract, diarrhea, dizziness, headache, tinnitus, convulsions, shortness of breath, dizziness. When a large overdose – acute renal failure, hepatotoxicity.
Treatment:
There is no specific antidote. Treatment – symptomatic, aimed at the elimination of hypotension, renal failure, convulsions, gastrointestinal irritation, respiratory depression.
Forced diuresis and hemodialysis ineffective (due to significant binding to plasma proteins and intensive metabolism).
pharmachologic effect
Pharmacological group:
Nonsteroidal anti-inflammatory drug (NSAID).
Pharmacodynamics:
Diclofenac has a pronounced analgesic, antipyretic and anti-inflammatory properties. Non-selectively inhibiting cyclooxygenase 1 and 2, it gives the arachidonic acid metabolism, reduces the amount of prostaglandins in inflammation. In rheumatic diseases inflammatory and analgesic effect of diclofenac contributes to a significant reduction in the severity of pain, morning stiffness, swelling of the joints, which improves the functional state of the joint. When trauma, postoperative diclofenac reduces pain and inflammatory edema.
Pharmacokinetics:
Suction
The time to reach maximum concentration in the intramuscular application of 75 mg – 15-30 min, the maximum concentration value – 1,9-4,8 (average 2.7) mcg / ml. After 3 h after administration, plasma concentrations are on average 10% of the maximum.
Distribution
Communication with plasma proteins – more than 99% (most associated with albumin). The volume of distribution – 550 ml / kg. Diclofenac penetrates into the synovial fluid, where its maximum concentration is reached at 2-4 hours later than in blood plasma. The apparent half-life of the synovial fluid is 3-6 hours. After 2 hours, after reaching the maximum plasma concentration of diclofenac concentration in synovial fluid than in plasma, and its value remains higher over a period of 12 hours.
Metabolism
Metabolism occurs as a result of single or multiple hydroxylation and conjugation with glucuronic acid. The metabolism of the drug takes part isoenzyme cytochrome P450 CYP2C9. The pharmacological activity of the metabolites is lower than diclofenac.
breeding
Systemic clearance is 350 ml / min. . The half-life of plasma – 2 hours 65% of the administered dose excreted by the kidneys as metabolites; less than 1% is excreted in unaltered form, the remainder of the dose excreted in bile as metabolites. Diclofenac passes into breast milk.
Pharmacokinetics in specific patient groups
In patients with renal failure (less than 10 ml / min creatinine clearance) increases the excretion of metabolites in the bile, thus increasing their concentration in the blood is not observed.
In patients with chronic hepatitis or compensated cirrhosis pharmacokinetic parameters of diclofenac are not changed.
Conditions of supply of pharmacies
Prescription.
side effects
Criteria for evaluation of the incidence of side reactions very often (> 1/10), often (> 1/100, 1/1000, 1/10 Ltd.,
From the blood and lymphatic system: very rarely – thrombocytopenia, leukopenia, anemia (including haemolytic and aplastic anemia), agranulocytosis. Disorders of immune system: rarely – hypersensitivity, anaphylactic and anaphylactoid reactions (including hypotension and shock); very rarely – angioedema (including swelling of the face).
Mental disorders: very rare – confusion, depression, insomnia, nightmares, irritability, personality disorders.
Disorders of the nervous system, often – headache, dizziness; rarely – drowsiness, fatigue; very rarely – paresthesia, memory disorders, cramps, feeling of anxiety, tremor, aseptic meningitis, taste disturbances, cerebrovascular accident; the frequency is unknown – confusion, hallucinations, sensitivity disorder, weakness.
Violations by the organ of vision: rarely – visual impairment, blurred vision, double vision; the frequency is unknown – optic neuritis.
Violations by the organ of hearing and labyrinth disorders: often – vertigo; very rarely – tinnitus, hearing disorders.
Violations of the heart: very rarely – palpitations, chest pain, heart failure, myocardial infarction.
Violations by vessels: very seldom – hypertension, hypotension, vasculitis.
Violations of the respiratory system, thorax and mediastinum: rarely – bronchial asthma (including shortness of breath); very rarely – pneumonitis.
Disorders of the gastrointestinal tract: often – nausea, vomiting, diarrhea, dyspepsia, abdominal pain, bloating, anorexia; rarely – gastritis, gastrointestinal bleeding, hematemesis, melena, diarrhea mixed with blood, ulcers of the stomach and / or intestines, 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 lesion, stenosis diafragmopodobny intestine, pancreatitis; the frequency is unknown – ischemic colitis.
Violations of the liver and biliary tract: often – increased activity of “liver” transaminases; rarely – hepatitis, jaundice, abnormal liver function; very rarely – fulminant hepatitis, hepatic necrosis, hepatic failure.
Violations of the skin and subcutaneous tissue disorders: often – rash; rarely – urticaria; very rarely – bullous rash, eczema, erythema, erythema multiforme, Stevens-Johnson syndrome, Lyell syndrome (toxic epidermal necrolysis), exfoliative dermatitis, alopecia, photosensitivity reaction, purpura, allergic purpura, pruritus.
Violations by the kidneys and urinary tract ‘, rarely – acute renal failure, hematuria, proteinuria. interstitial nephritis, nephrotic syndrome, papillary necrosis.
General disorders and at the injection site: common – reaction at the injection site, pain at the injection site, infiltration at the injection site, rarely – swelling, necrosis at the injection site.
Violations by the genitals and mammary glands: rarely – impotence. Clinical trials and epidemiological data suggest that the diclofenac, particularly at high doses (150 mg daily) and prolonged use may lead to an increased risk of arterial thromboembolic events (e.g., myocardial infarction or stroke).
special instructions
The risk of side reactions during diclofenac increases with increasing dose and duration of treatment. To reduce the risk of occurrence of undesired phenomena of drug should be used in the minimum effective dose for the shortest period necessary to alleviate symptoms.
With regular use of the drug should periodically evaluate the need for relief of symptoms, response to treatment and to adjust the dose in a timely manner.
Involvement of the gastrointestinal tract
When diclofenac observed such phenomena as bleeding or ulceration / gastrointestinal perforation, in some cases, fatal. These phenomena may occur at any time in the application of drugs in patients with or without previous symptoms and serious gastro-intestinal diseases or a history without them. In elderly patients, these complications can have serious consequences. With the development in patients receiving diclofenac, bleeding or ulceration of the gastrointestinal tract drug should be discontinued. To reduce the risk of toxic effect on the gastrointestinal tract in patients with ulcerative lesions of the gastrointestinal tract. especially complicated by bleeding or perforation in history, as well as in elderly patients the drug should be used in the lowest effective dose. Patients with an increased risk of gastrointestinal complications, and patients treated with low-dose acetylsalicylic acid (aspirin), should be taken gastroprotectives (proton pump inhibitors or misoprostol) or other medicines to reduce the risk of undesirable effects on the gastrointestinal tract. Patients with lesions of the gastrointestinal tract in history, especially the elderly, should be reported to your doctor about all abdominal symptoms.
Patients with asthma
Exacerbation of asthma (intolerance to NSAID / asthma provoked by NSAID), angioedema, and urticaria most frequently reported in patients with bronchial asthma, seasonal allergic rhinitis, nasal polyps, chronic obstructive pulmonary disease or chronic infectious respiratory diseases (particularly associated with allergic rinitopodobnymi symptoms). In this group of patients, and in patients who are allergic to other drugs (rash, itching or hives) with diclofenac should take special care (readiness for resuscitation).
skin reactions
Such severe dermatologic reactions such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, in some cases fatal, against the background of the application of diclofenac observed very rarely. The greatest risk and incidence of severe dermatological reactions occurred within the first month of treatment with diclofenac. With the development in patients receiving diclofenac, the first signs of skin rash, mucosal lesions or other symptoms of hypersensitivity to the drug should be discontinued. In rare cases, anaphylactic / anaphylactoid reactions may occur in patients who do not have an allergy to diclofenac.
Effects on the liver
Since during the application of the diclofenac can be marked increase in the activity of one or more liver enzymes during prolonged drug therapy, as a precaution shows control liver function. When storing and advancing impaired liver function or liver disease symptoms occurs or other symptoms (e.g., eosinophilia, rashes, etc.. P.), The drug must be undone. Следует иметь в виду, что гепатит на фоне применения диклофенака может развиваться без продромальных явлений.
Воздействие на почки
На фоне терапии диклофенаком рекомендуется проводить контроль функции почек у пациентов с гипертонической болезнью, нарушениями функции сердца или почек, пожилых, пациентов, получающих диуретики или другие препараты, влияющие на почечную функцию, а также у пациентов со значительным уменьшением объема циркулирующей плазмы крови любой этиологии, например, в период до и после массивных хирургических вмешательств. После прекращения терапии препаратом обычно отмечается нормализация показателей почечной функции до исходных значений.
Воздействие на сердечно-сосудистую систему
Терапия НПВП, в т. ч. диклофенаком, в особенности длительная терапия и терапия с использованием высоких доз, может быть ассоциирована с небольшим возрастанием риска развития серьезных сердечно-сосудистых тромботических осложнений (включая инфаркт миокарда в инсульт). Пациентам с заболеваниями сердечно-сосудистой системы и высоким риском развития заболеваний сердечно-сосудистой системы (например, с артериальной гипертензией, гиперлипидемией, сахарным диабетом, курящим) следует назначать препарат только после тщательного рассмотрения и применять его с особой осторожностью, в самой низкой эффективной дозе при минимально возможной длительности лечения, поскольку риск возникновения тромботических осложнений возрастает при увеличении дозы и продолжительности лечения. При длительной терапии (более 4 недель) суточная доза диклофенака у таких пациентов не должна превышать 100 мг. Следует периодически проводить оценку эффективности лечения и потребности пациента в симптоматической терапии, особенно в тех случаях, когда ее продолжительность составляет более 4 недель. Пациент должен быть проинструктирован о незамедлительном обращении за медицинской помощью при появлении первых симптомов тромботических нарушений (например, боли в груди, чувства нехватки воздуха, слабости, нарушения речи).
Воздействие на систему кроветворения
Диклофенак может временно ингибировать агрегацию тромбоцитов. Поэтому у пациентов с нарушениями гемостаза необходимо проводить тщательный контроль соответствующих лабораторных показателей. При длительном применении диклофенака рекомендуется проводить регулярные клинические анализы периферической крови.
Маскирование признаков инфекционного процесса
Противовоспалительное действие диклофенака может затруднять диагностику инфекционных процессов. Применение одновременно с другими НПВП Не следует применять диклофенак одновременно с другими НПВП, включая селективные ингибиторы ЦОГ-2 из-за риска увеличения нежелательных явлений.
Влияние на фертильность женщин
Диклофенак может оказывать отрицательное влияние на фертильность женщин, поэтому женщинам, желающим забеременеть, диклофенак применять не рекомендуется. У женщин, испытывающих трудности с зачатием (в т. ч. проходящих обследование), необходимо рассмотреть возможность прекращения применения диклофенака. Входящий в состав препарата натрия метабисульфит редко может вызвать тяжелые реакции гиперчувствительности и бронхоспазм.
Информация для пациентов, соблюдающих диету с контролируемым содержанием натрия Содержание натрия в одной ампуле (3 мл) препарата Диклофенак раствор для инъекций не превышает 1 ммоль (23 мг), т.е. практически «без натрия».
Пациентам, у которых на фоне применения диклофенака возникают зрительные нарушения, головокружение, сонливость, вертиго или другие нарушения со стороны центральной нервной системы, не следует управлять транспортными средствами и работать с механизмами.
Storage conditions
At a temperature of 15 to 25 ° C.
Keep out of the reach of children!.
Dosing and Administration
С целью снижения риска развития нежелательных явлений препарат рекомендуется применять в минимальной эффективной дозе в течение самого короткого периода времени, необходимого для облегчения симптомов.
Для того, чтобы избежать повреждения нерва или других тканей в месте введения следует точно соблюдать инструкцию по проведению внутримышечной инъекции.
Инъекционный раствор вводится глубоко внутримышечно (в верхний наружный квадрант ягодичной области). Разовая доза для взрослых — 75 мг (1 ампула). При необходимости возможно повторное введение, но не ранее, чем через 12 часов. Вторая инъекция должна проводиться в противоположную ягодичную область.
Максимальная рекомендуемая суточная доза препарата Диклофенак раствор для внутримышечного введения составляет 150 мг. Длительность использования не более 2 дней, при необходимости далее переходят на пероральное, либо ректальное применение диклофенака.
Одну ампулу 75 мг препарата можно комбинировать с другими лекарственными формами диклофенака (таблетки, покрытые кишечнорастворимой оболочкой, суппозитории ректальные), при этом следует обратить внимание на то, что максимальная суточная доза диклофенака не должна превышать 150 мг.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist