Dialrapid powder for solution 50mg sachet 9 inside the piece

Description

Composition
Active substance:
Diclofenac potassium 50.0 mg;
Excipients:
glyceryl dibehenate 2.0 mg Sodium saccharinate 5.0 mg Anise flavor 15.0 mg, 22.0 mg potassium carbonate, 35.0 mg peppermint flavor, aspartame 50.0 mg Mannitol 721.0 mg.
Description:
Homogeneous powder from white to light yellow in color with a specific smell.
Recycled transparent solution slightly opalescent with a specific smell.
Product form:
powder for solution for oral administration, 50 mg.
900 mg in a hermetically sealed sachet made of paper / aluminum / polyethylene, or paper / polyethylene / aluminum / LDPE tamper children.
9 sachets with instructions for use in a cardboard box.
Contraindications
Hypersensitivity to the active agent and other ingredients, as well as other non-steroidal anti-inflammatory drugs (NSAIDs);
aggravation of gastric ulcer and duodenal ulcer bleeding, perforation;
inflammatory bowel disease (Crohn’s disease, ulcerative colitis) in acute phase;
complete or partial combination of asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid or other NSAIDs (including history);
abnormal liver function severe, renal failure (GFR of less than 15 ml / min / 1.73m2);
chronic heart failure, functional class II-IV at NYHA classification;
clinically confirmed ischemic heart disease;
peripheral artery disease and cerebrovascular disease;
uncontrolled hypertension; III of trimester of pregnancy;
during breastfeeding.
The drug should not be used in patients with phenylketonuria as it contains a source of phenylalanine.
The drug is not recommended for use in children under the age of 14 years (due to the difficulty of dosing the drug).
Carefully:
In applying the drug Dialrapid and other NSAIDs caution should be exercised carefully and observe patients with symptoms / signs suggestive of injury / disease of the gastrointestinal tract (GIT), or with a history of data, allowing suspected canker of the stomach or intestine, bleeding or perforation; patients with Helicobacter pylori infection in anamnesis, ulcerative colitis, Crohn’s disease, with abnormal liver function and a history of the patients complaints, gastrointestinal disorder can be suspected. The risk of gastrointestinal bleeding increases with increasing doses of NSAIDs or in the presence of gastrointestinal ulcer history, especially bleeding and perforation of ulcers in elderly patients.
It should be particularly careful when applying Dialrapid drug in patients receiving drugs that increase the risk of gastrointestinal bleeding: systemic glucocorticosteroids (including prednisone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel , acetylsalicylic acid) or a selective serotonin reuptake inhibitor (including citalopram, fluoxetine, paroxetine, sertraline).
Caution is needed when using the drug in patients Dialrapid impaired liver function mild and moderate severity, as well as in patients with hepatic porphyria, since the drug can trigger attacks of porphyria. Particular care is required when treating patients with impaired renal function, including chronic renal failure (GFR 15-60 ml / min / 1.73m2), dyslipidemia / hyperlipidemia, diabetes, hypertension, in the treatment of smoking patients or patients who abuse alcohol, with treatment of elderly patients, patients receiving diuretics or other drugs affecting renal function as well as patients with a significant decrease in the circulating blood volume (CBV) of any etiology, for example, in the periods before and after weight sive surgery.
It should be used with caution in drug Dialrapid patients with defects of the hemostatic system.
Caution should be exercised when using the drug in patients at risk for cardiovascular thrombosis (including myocardial infarction and stroke).
Caution should be exercised when using the drug Dialrapid in elderly patients. This is especially true in debilitated or who have low weight the elderly body.
Dosage
50 mg
Indications
For short-term treatment of the following acute conditions:
posttraumatic pain, inflammation and edema, e.g., due to damage to the ligaments;
postoperative pain, inflammation and swelling, eg following dental or orthopedic surgery;
pain and / or inflammation accompanying gynecological diseases, e.g., primary dysmenorrhoea or adnexitis;
migraine attacks;
pain syndromes from the spine;
extra-articular rheumatism of soft tissues.
Isolated temperature rise is not an indication for use Dialrapid preparation.
Interaction with other drugs
The following types of drug interactions were observed when using the drug Dialrapid and / or other dosage forms of diclofenac.
Isoenzyme inhibitors of CYP2C9. Caution must be exercised while the use of diclofenac isoenzyme inhibitors and CYP2C9 (such as voriconazole) due to a possible increase in the plasma concentration of diclofenac and its exposure.
Lithium, digoxin. Since the diclofenac can increase the concentration of lithium and digoxin in blood plasma, it is advisable to measure the concentration of lithium in the blood and digoxin when applied simultaneously with diclofenac.
Diuretic and antihypertensive agents. While the use of diuretics and antihypertensive agents (e.g., beta-blockers, ACE inhibitors) diclofenac, like other NSAIDs, may reduce their hypotensive effects, so patients, especially the elderly, while the use of diclofenac and diuretic or antihypertensive drugs should regularly measuring blood pressure monitor renal function and the degree of hydration (especially in combination with diuretics and ACE inhibitors due to increased risk of nephrotoxicity).
Cyclosporine and tacrolimus. Effect on diclofenac prostaglandin activity in the kidney may enhance the nephrotoxicity of cyclosporin and tacrolimus. In connection with the above dose of diclofenac in patients receiving cyclosporin or tacrolimus, should be lower than in patients not treated with these drugs.
Drugs that can cause hyperkalemia. Simultaneous application of diclofenac potassium-sparing diuretics, cyclosporine, tacrolimus and trimethoprim may increase the content of potassium in the blood plasma (in the case of the simultaneous application of the indicator should be monitored frequently).
Antibacterials – quinolone derivatives. There are isolated reports of seizures develop in patients receiving quinolone derivatives and diclofenac at a time.
alleged cooperation
NSAIDs and corticosteroids
Simultaneous systemic administration of diclofenac and other systemic NSAIDs or corticosteroids may increase the incidence of gastrointestinal AEs.
Antiokoagupyanty and antiplatelet agents. Although clinical studies have not been found to influence of diclofenac on the action of anticoagulants, there are isolated reports of an increased risk of bleeding in patients taking this combination of drugs. patients should be carefully monitored, receiving concomitant treatment with these drugs.
Selective serotonin reuptake inhibitor. Simultaneous application of diclofenac with selective serotonin reuptake inhibitor increases the risk of gastrointestinal bleeding.
Hypoglycemic agents. In clinical studies have shown that while the application of diclofenac does not affect the effectiveness of oral hypoglycemic drugs. However, there are isolated reports of the development of both hypoglycemic and hyperglycemic conditions during treatment with diclofenac, requiring a change in the dose of hypoglycemic drugs. Patients receiving concomitant treatment with diclofenac and hypoglycemic drugs, periodic measurement of blood glucose concentration.
Received isolated reports of the development of metabolic acidosis, while the use of diclofenac with metformin, particularly in patients with impaired renal function.
Methotrexate. Caution must be exercised when applying NSAIDs including diclofenac, less than 24 hours before or after methotrexate, since in such cases the MTX concentration may be increased in the blood and increases its toxic effects.
Phenytoin. With simultaneous application of diclofenac, phenytoin and phenytoin necessary to control the concentration in the blood plasma of the possible amplification of its systemic exposure.
Isoenzyme inducers of CYP2C9. Caution must be exercised simultaneously with diclofenac isoenzyme inducers CYP2C9 (such as rifampin), as this may lead to a significant reduction of diclofenac concentration in the blood plasma, and reduce its exposure.
Overdose
Symptoms: vomiting, gastrointestinal bleeding, diarrhea, dizziness, tinnitus, convulsions. In the event of significant poisoning, may develop acute renal failure and liver damage.
Treatment: supportive and symptomatic treatment is indicated in complications such as decreased blood pressure, renal failure, convulsions, disorders of the gastrointestinal and respiratory depression. Forced diuresis, hemodialysis or haemoperfusion for diclofenac ineffective because NSAIDs are largely bound to plasma proteins and undergo intensive metabolism.
In the case of life-threatening overdose ingestion of the drug, in order to prevent a speedy absorption of diclofenac to gastric lavage should be followed by the application of activated carbon.
pharmachologic effect
Pharmacological group:
nonsteroidal anti-inflammatory drug (NSAID).
Code: M01AV05
Pharmacodynamics:
Dialrapid preparation contains diclofenac potassium, nonsteroidal structure substances which have a pronounced analgesic, antiinflammatory and antipyretic action.
Due to the rapid onset of action, the use of the potassium salt of diclofenac, preferably for the treatment of acute pain and inflammatory conditions. The main mechanism of action of diclofenac, set in the research, it is believed inhibition of the synthesis of prostaglandins, which play an important role in the pathogenesis of inflammation, pain and fever.
In vitro diclofenac potassium at concentrations equivalent to those obtained using a human, does not inhibit the biosynthesis of cartilage proteoglycans.
Diclofenac has a strong analgesic effect with moderate to severe pain syndrome. In post-traumatic and post-operative inflammation diclofenac rapidly relieves pain (both at rest and in motion), reduces the inflammatory edema and swelling of the surgical wound.
In clinical studies, it has been found that potassium diclofenac can reduce pain and reduce blood loss in primary dysmenorrhea.
When migraine attacks Dialrapid reduces the severity of headache and associated symptoms such as nausea and vomiting.
Pharmacokinetics:
Suction
Diclofenac is rapidly and completely absorbed. After a single dose of the drug into a dose of 50 mg maximum concentration (Cmax) of diclofenac potassium plasma levels achieved after 5-20 minutes, with an average of 5.5 mol / l for the preparation of a powder for oral solution. While taking the drug during the meal intake of diclofenac does not change, although the onset and rate of absorption can be slowed down somewhat. Absorption of diclofenac depends linearly on the dose. About half of the dose of diclofenac is metabolised during the first pass through the liver (the effect of “first pass”), area under the curve “concentration – time» (AUC) after oral administration or rectal approximately half the equivalent dose, administered parenterally. After repeated use of the drug Dialrapid pharmacokinetics do not change.
Under the recommended dosing regimen drug accumulation is not observed.
Distribution
Contact with serum proteins – 99.7%, preferably albumin (99.4%). Apparent volume of distribution is 0,12-0,17 l / 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 a maximum concentration in the blood plasma concentration of diclofenac in synovial fluid than in blood plasma, and its value remains higher over time period to 12 hours.
Biotransformation / Metabolism
Metabolism of diclofenac is achieved partly by glyukuronirovaniya unmodified molecule, but preferably by means of single and multiple hydroxylation and methoxylation, that leads to formation of several phenolic metabolites (Z’-hydroxy-, 4′-hydroxy-, 5-hydroxy-, 4 ‘, 5- dihydroxy- and 3′-hydroxy-4′-metoksidiklofenaka), most of which is converted to glucuronide conjugates. Two phenolic metabolites are biologically active, but to a much lesser extent than diclofenac.
breeding
Total systemic plasma clearance of diclofenac is 263 ± 56 mL / min. Terminal half-life is 1-2 hours. Half-life of four metabolites, including the two active pharmacologically, and also of short duration is 1-3 hours. One of the metabolites, 3′-hydroxy-4’-methoxy-diclofenac, has a longer half-life, but this is completely inactive metabolite.
About 60% of the dose excreted by the kidneys in unchanged form conjugates glucuronic active substance, as well as metabolites, most of which also represent glucuronic conjugates. In the unchanged output of less than 1% of diclofenac. The remainder of the dose excreted as metabolites in the bile.
Pharmacokinetics in special patient groups
After taking the drug inside the differences in absorption, metabolism or excretion of the drug associated with age, not marked.
In patients with impaired renal function is not marked accumulation of the unchanged active substance in compliance with the recommended dosing regimen. If creatinine clearance less than 10 mL / min calculated equilibrium concentrations of diclofenac gidroksimetabolitov approximately 4-fold higher than in healthy volunteers, and the metabolites are excreted exclusively with bile.
In patients with chronic hepatitis or compensated cirrhosis pharmacokinetics of diclofenac are similar to those in patients with preserved liver function.
Pregnancy and breast-feeding
It is not enough safety data The use of diclofenac in pregnant women, so apply Dialrapid drug in I and II trimesters of pregnancy should be only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. Preparation Dialrapid, like other NSAIDs (prostaglandin synthesis inhibitors), contraindicated in last 3 months of pregnancy (possibly suppressing uterine capacity, impaired kidney function in fetal followed oligohydramnios (oligogidroamnion) and / or premature closure of the ductus arteriosus in the fetus).
Despite the fact that Dialrapid drug, like other NSAIDs passes into breast milk in small amounts, it should not be used during breast-feeding in order to avoid undue influence on the child. Diclofenac has been found in low concentrations (100 ng / ml) in the breast milk of a lactating mothers. Estimated amount of drug entering through breast milk in the baby is equivalent to 0.03 mg / kg / day.
If necessary, use a nursing woman breast feeding is stopped.
Since Dialrapid, like other NSAIDs, can have an adverse effect on fertility, it is not recommended to use the drug in patients who are planning a pregnancy.
In patients undergoing examination and treatment for infertility, the drug should be discontinued.
Conditions of supply of pharmacies
On prescription
side effects
Below adverse events (AEs) which were discovered during clinical trials, as well as diclofenac in clinical practice.
The following criteria for evaluating the frequency of adverse events used: “often” -> 1/100, 1/1000,
special instructions
Involvement of the gastrointestinal tract
In the application of all NSAIDs, including diclofenac, marked bleeding or ulceration / perforation of the gastrointestinal tract, in some cases fatal. These phenomena may occur at any time during the treatment of patients with or without previous symptoms or gastrointestinal disease history. In elderly patients, these complications can have serious consequences. With the development in patients during treatment with the drug Dialrapid bleeding or ulceration of the gastrointestinal 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 high risk of gastrointestinal complications, as well as patients receiving therapy with low doses of aspirin or other drugs capable of enhancing the risk of digestive tract, gastroprotectives to be taken (e.g., proton pump inhibitors or misoprostol).
Patients with lesions of the gastrointestinal tract in history, especially the elderly, should be reported to your doctor about any unusual abdominal symptoms.
Patients with asthma
Обострение бронхиальной астмы (непереносимость НПВП/бронхиальная астма, провоцируемая приемом НПВП), отек Квинке и крапивница наиболее часто отмечаются у пациентов, с бронхиальной астмой, сезонным аллергическим ринитом, полипами слизистой оболочки полости носа, хронической обструктивной болезнью легких или хроническими инфекционными заболеваниями дыхательных путей (особенно связанными с аллергическими ринитоподобными симптомами). У данной группы пациентов, а также у пациентов с аллергией на другие препараты (сыпь, зуд или крапивница) при применении препарата Диалрапид следует соблюдать особую осторожность (готовность к проведению реанимационных мероприятий).
Кожные реакции
Такие серьезные дерматологические реакции как эксфолиативный дерматит, синдром Стивенса-Джонсона, токсический эпидермальный некролиз, в некоторых случаях со смертельным исходом, на фоне применения НПВП, включая диклофенак, отмечались очень редко. The greatest risk and incidence of severe dermatological reactions occurred within the first month of treatment with diclofenac. При развитии у пациентов, получающих препарат Диалрапид, первых признаков кожной сыпи, поражения слизистых или других симптомов гиперчувствительности препарат должен быть отменен. В редких случаях у пациентов, не имеющих аллергии на диклофенак, при применении препарата Диалрапид могут развиваться анафилактические/анафилактоидные реакции.
Воздействие на печень и желчевыводящие пути
Поскольку в период применения препарата Диалрапид, так же, как и в других НПВП, может отмечаться повышение активности одного или нескольких печеночных ферментов, при длительной терапии препаратом, в качестве меры предосторожности, показан контроль функции печени. При сохранении и прогрессировании нарушений печеночной функции или возникновении признаков заболеваний печени, или других симптомов (например, эозинофилии, сыпи и т.п.), прием препарата Диалрапид необходимо отменить. Следует иметь в виду, что гепатит на фоне применения препарата Диалрапид может развиваться без продромальных явлений.
Воздействие на почки
На фоне терапии НПВП, включая диклофенак, отмечались задержка жидкости и отеки, поэтому следует соблюдать особую осторожность и рекомендуется проводить контроль функции почек у пациентов с гипертонической болезнью, нарушениями функции сердца или почек, пожилых пациентов, 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. After the cessation of drug therapy is usually marked by normalization of renal function prior to the initial values.
Воздействие на сердечно-сосудистую систему
NSAID therapy, including diclofenac, particularly long-term treatment and therapy with the use of high doses may be associated with a small increased risk of serious cardiovascular thrombotic events (including myocardial infarction and stroke).
У пациентов с заболеваниями сердечно-сосудистой системы и высоким риском развития заболеваний сердечно-сосудистой системы (например, с артериальной гипертензией, гиперлипидемией, сахарным диабетом, курящим) следует применять препарат 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
Препарат Диалрапид, так же, как и другие НПВП, может временно ингибировать агрегацию тромбоцитов. Поэтому у пациентов с нарушениями гемостаза необходим тщательный контроль соответствующих лабораторных показателей. Препарат Диалрапид рекомендован только для краткосрочного лечения, однако при продолжительном применении препарата Диалрапид, как и других НПВП, показан систематический контроль картины периферической крови.
Маскирование признаков инфекционного процесса
Препарат Диалрапид, как и другие НПВП вследствие своих фармакодинамических свойств, может маскировать проявления инфекционных заболеваний.
Применение одновременно с другими НПВП
Не следует применять препарат Диалрапид одновременно с другими НПВП, включая селективные ингибиторы ЦОГ-2 из-за риска увеличения частоты нежелательных явлений.
Impact on the ability of management and road machinery
Пациентам, у которых на фоне применения препарата Диалрапид 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
In a dry place at a temperature not higher than 25 ° C.
The drug should be stored out of reach of children.
Dosing and Administration
Дозу препарата Диалрапид следует подбирать индивидуально, при этом с целью снижения риска развития побочных эффектов рекомендуется применение минимальной эффективной дозы, по возможности, с максимально коротким периодом лечения, в соответствии с целью лечения и состоянием пациента.
Предпочтительно принимать перед едой. Содержимое саше следует растворить, помешивая, в стакане воды (негазированной). Раствор может оставаться слегка мутным, но это не влияет на эффективность препарата.
В случае умеренной выраженности симптомов обычно бывает достаточно применения в суточной дозе 50-100 мг в форме порошка для приготовления раствора для приема внутрь (1-2 саше).
Максимальная суточная доза препарата не должна превышать 150 мг/сут. Суточную дозу следует делить на 3 приема.
При первичной дисменорее суточную дозу препарата Диалрапид следует подбирать индивидуально; обычно она составляет 50-150 мг. Начальная доза — 50-100 мг (1-2 саше); при необходимости в течение нескольких менструальных циклов дозу можно повысить до 150 мг/сут. Прием препарата следует начинать при появлении первых симптомов. В зависимости от динамики клинических симптомов лечение можно продолжать в течение нескольких дней.
При приступе мигрени начальная доза для препарата Диалрапид составляет 50 мг (1 саше). Препарат следует принимать при первых симптомах приближающегося приступа. В случаях, когда в течение 2 часов после приема первой дозы не происходит облегчения боли, возможен повторный прием препарата в дозе 50 мг. В дальнейшем через каждые 4-6 часов возможен дополнительный прием препарата Диалрапид в дозе 50 мг. Суммарная доза препарата не должна превышать 150 мг в сутки (в течение не более 2 дней). Эффективность препарата Диалрапид при лечении приступов мигрени у детей и подростков не установлена.
У подростков 14 лет и старше препарат Диалрапид применяют в суточной дозе 50-100 мг препарата (из расчета 0,5-2 мг/кг массы тела в сутки, для лечения ревматоидного артрита суточная доза может быть максимально увеличена до 3 мг/кг).
Препарат Диалрапид не следует применять у детей и подростков младше 14 лет.
Пациентам старше 65 лет коррекции дозы не требуется. Однако, исходя из общих медицинских соображений, следует соблюдать осторожность у ослабленных пожилых пациентов или пациентов с низкой массой тела.
Следует с особой осторожностью применять препарат у пациентов с высоким риском развития заболеваний сердечно-сосудистой системы. При необходимости длительной терапии (более 4 недель) у таких пациентов следует применять препарат в суточной дозе, не превышающей 100 мг.
Patients with impaired renal function
Нет данных о необходимости коррекции дозы при применении препарата у пациентов с нарушениями функции почек в связи с отсутствием исследований безопасности применения препарата у пациентов данной категории.
Следует соблюдать осторожность при применении препарата у пациентов с нарушением функции почек.
Применение препарата у пациентов с почечной недостаточностью (СКФ менее 15 мл/мин/1,73м2) противопоказано (см. раздел «Противопоказания»).
Пациенты с нарушением функции печени легкой и средней степени тяжести
Нет данных о необходимости коррекции дозы при применении препарата у пациентов с нарушениями функции печени легкой и средней степени тяжести в связи с отсутствием исследований безопасности применения препарата у данной категории пациентов.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist