Dialrapid oral solution powder 50mg, sachet 9pcs

Composition

1 sachet contains: Active ingredient: diclofenac potassium 50.0 mg; excipients: glyceryladibegenate 2.0 mg, sodium saccharinate 5.0 mg, anise flavor 15.0 mg, potassium bicarbonate 22.0 mg, mint flavor 35.0 mg, aspartame 50.0 mg, mannitol 721.0 mg

Pharmacological ACTION

PHARMACOTHERAPY GROUP: nonsteroidal anti-inflammatory drug (NSAID). ATX code: M 01 AB 05 PHARMACOLOGICAL PROPERTIESPHARMACODYNAMICTHE drug Dialrapid contains diclofenac potassium, a nonsteroidal substance that has a pronounced analgesic, anti-inflammatory and antipyretic effect. Due to the rapid onset of action, the use of diclofenac potassium salt is preferable for the treatment of acute pain and inflammatory conditions. The main mechanism of action of diclofenac, established in studies, is considered to inhibit the synthesis of prostaglandins, which play an important role in the pathogenesis of inflammation, pain and fever. Invitro diclofenac potassium in concentrations equivalent to those achieved in humans does not inhibit the biosynthesis of cartilage proteoglycans. Diclofenac has a pronounced analgesic effect in moderate to severe pain. In post-traumatic and postoperative inflammatory events, diclofenac quickly relieves pain (both at rest and during movement), reduces inflammatory edema and swelling of the postoperative wound. In clinical studies, diclofenac potassium has been shown to reduce pain and reduce blood loss in primary dysmenorrhea. During migraine attacks, Dialrapid reduces the severity of headaches and concomitant symptoms such as nausea and vomiting. Pharmacokineticsabsorption Diclofenac is rapidly and completely absorbed. After a single oral dose of 50 mg, the maximum concentration (Cmax) of diclofenac potassium in blood plasma is reached in 5-20 minutes and averages 5.5 mmol/l for powder for the preparation of an oral solution. When taking the drug with a meal, the amount of absorbed diclofenac does not change, although the onset and rate of absorption may slow down somewhat. The absorption of diclofenac is linearly dependent on the dose of the drug. About half of the diclofenac dose is metabolized during the first pass through the liver (the “first pass” effect), the area under the concentration – time pharmacokinetic curve (AUC) after oral or rectal use is approximately half of the equivalent dose applied parenterally. After repeated use of Dialrapid, the pharmacokinetic parameters do not change. If the recommended dosage regimen is followed, no accumulation is observed. Distribution of binding to serum proteins – 99.7%, mainly with albumin (99.4%). The apparent volume of distribution is 0.12-0.17 l / kg. Diclofenac penetrates the synovial fluid, where its maximum concentration is reached 2-4 hours later than in the blood plasma. The apparent elimination half-life from synovial fluid is 3-6 hours. 2 hours after reaching the maximum concentration in blood plasma, the concentration of diclofenac in synovial fluid is higher than in blood plasma, and its values remain higher for a period of time up to 12 hours. Biotransformation/Metabolism The metabolism of diclofenac is carried out partly by glucuronidation of the unchanged molecule, but mainly by single and multiple hydroxylation and methoxylation, which leads to the formation of several phenolic metabolites (3’-hydroxy-,4’-hydroxy-,5’-hydroxy-,4’,5-dihydroxy – and 3’-hydroxy-4’-methoxydiclofenac), most of which are converted to glucuronide conjugates. Two phenolic metabolites are biologically active, but to a much lesser extent than diclofenac. Elimination The total systemic plasma clearance of diclofenac is 263 ± 56 ml/min. The final half-life is 1-2 hours. The half-life of 4 metabolites, including two pharmacologically active ones, is also short and amounts to 1-3 hours. One of the metabolites,3’-hydroxy-4’-methoxy-diclofenac, has a longer half-life, but this metabolite is completely inactive. About 60% of the dose of the drug is excreted by the kidneys in the form of glucuronic conjugates of the unchanged Active ingredient, as well as in the form of metabolites, most of which are also glucuronic conjugates. Less than 1% of diclofenac is excreted unchanged. The remainder of the dose is excreted as metabolites in the bile. Pharmacokinetics in special groups of patients after oral use of the drug, there are no differences in absorption, metabolism or excretion of the drug associated with the age of patients. In patients with impaired renal function, no accumulation of unchanged Active ingredient is observed if the recommended dosage regimen is observed. When creatinine clearance is less than 10 ml/min, the calculated steady-state concentrations of diclofenac hydroxymetabolites are approximately 4 times higher than in healthy volunteers, and the metabolites are excreted exclusively in the bile. In patients with chronic hepatitis or compensated cirrhosis of the liver, the pharmacokinetics of diclofenac are similar to those in patients with preserved liver function.

Indications

For short-term treatment of the following acute conditions:

• post-traumatic pain, inflammation and swelling, for example, due to damage to the ligaments;
• post-operative pain, inflammation and swelling, for example after dental or orthopedic surgical interventions;
• pain and/or inflammation accompanying gynecological diseases, such as primary dysmenorrhea or adnexitis;
• migraines;
• pain syndromes of the spinal column;
• extra-articular rheumatic diseases of soft tissues.

An isolated increase in temperature is not an indication for the use of Dialrapid.

Contraindications

• Hypersensitivity to the Active ingredient and other components of the drug, as well as other nonsteroidal anti-inflammatory drugs (NSAIDs);

• exacerbation of gastric ulcer and duodenal ulcer, peptic ulcer bleeding, perforation;

• inflammatory bowel disease (Crohn’s disease, ulcerative colitis) in the acute phase;

• complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance of acetylsalicylic acid or other NSAIDs (including in the anamnesis);

• the liver, severe, renal failure (GFR less than 15 ml/min/1.73 m 2);

• chronic heart failure, functional class II-IV to NYHA classification;

• clinically proven coronary heart disease;

• diseases of peripheral arteries and cerebral vessels;

• uncontrolled hypertension;

• III trimester of pregnancy;

• lactation.

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 14 years of age (due to the difficulty of dosing the drug).

WITH CAUTION

Caution should be exercised when using Dialrapid and other NSAIDs and carefully monitor patients with symptoms/signs that indicate lesions/diseases of the gastrointestinal tract (GIT) or with a history of suspected gastric or intestinal ulceration, bleeding or perforation; in patients with a history of Helicobacter Pylori infection, ulcerative colitis, Crohn’s disease, with a history of hepatic impairment and in patients with complaints that the patient has a history of allowing you to suspect a gastrointestinal disease. The risk of gastrointestinal bleeding increases with increasing NSAID doses or with a history of gastrointestinal ulcers, especially bleeding and perforation of the ulcer, and in elderly patients.

Special care should be taken when using Dialrapid 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 selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline).

Caution is necessary when using Dialrapid in patients with mild to moderate hepatic impairment, as well as in patients with hepatic porphyria, as the drug can provoke attacks of porphyria. Special care is required in the treatment of patients with impaired renal function, including chronic renal failure (GFR 15-60 ml/min/1.73 m2), dyslipidemia/hyperlipidemia, diabetes mellitus, hypertension, in the treatment of smoking patients or patients who abuse alcohol, in the treatment of elderly patients, patients receiving diuretics or other drugs that affect renal function, as well as patients with a significant decrease in the volume of circulating blood (BCC) of any etiology, for example, in the periods before and after massive surgical interventions.

Dialrapid should be used with caution in patients with hemostatic system defects.

Caution should be exercised when using Voltaren Rapid in patients at risk of developing cardiovascular thrombosis (including myocardial infarction and stroke).

Caution should be exercised when using Dialrapid in elderly patients. This is especially true for weak or low-weight elderly people.

Side effects

The following are adverse events (AES) that have been identified in clinical trials, as well as when using diclofenac in clinical practice.

The following criteria were used to assess the frequency of AES: “often” – >1/100, ><1/10, “infrequently” ->1/1000, <1/10, “infrequently” – ><1/100, “rarely” – >1/10000, <1/100, “rarely” – ><1/1000, “very rarely” – AES are grouped according to the system-organ class of the MedDRA medical dictionary for regulatory activities. Within each class, AES are listed in descending order of frequency of occurrence, and within each group allocated by frequency of occurrence, AES are distributed in decreasing order of their importance.

Disorders of the blood and lymphatic system: very rarely – thrombocytopenia, leukopenia, hemolytic anemia, aplastic anemia, agranulocytosis.

Immune system disorders:rarely – hypersensitivity, anaphylactic/anaphylactoid reactions, including lowering of blood pressure (BP) and shock; very rarely-angioedema (including facial edema).

Mental disorders: very rarely – disorientation, depression, insomnia, nightmares, irritability, mental disorders.

Nervous system disorders: often-headache, dizziness; rarely-drowsiness; very rarely-sensitivity disorders, including paresthesia, memory disorders, tremor, convulsions, anxiety, acute cerebral circulation disorders, aseptic meningitis.

Visual disturbances:very rarely-visual disturbances (blurred vision), diplopia.

Hearing disorders and labyrinth disorders: often-vertigo; very rarely-hearing disorders, tinnitus.

Cardiac disorders: infrequently – myocardial infarction, heart failure, palpitation, chest pain.

Vascular disorders: very rarely – increased blood pressure, vasculitis.

Respiratory and mediastinal disorders: rarely-bronchial asthma (including shortness of breath); very rarely – pneumonitis.

Violations of the gastrointestinal tract: often – abdominal pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, loss of appetite; rarely – gastritis, gastrointestinal bleeding, vomiting blood, melena, diarrhea mixed with blood, ulcers of the stomach and intestines (with or without bleeding, stenosis, or perforation with possible development of peritonitis); very rarely

– stomatitis, glossitis, esophageal injury, the occurrence of diaphragmatic strictures in the intestines, colitis (nonspecific haemorrhagic colitis, ischemic colitis, exacerbation of ulcerative colitis or Crohn’s disease), constipation, pancreatitis, dysgeusia. Liver and biliary tract disorders:often-increased aminotransferase activity in blood plasma; rarely

-hepatitis, jaundice, liver function disorders; very rarely-lightning-fast hepatitis, liver necrosis, liver failure. Skin and subcutaneous tissue disorders: often-skin rash; rarely-urticaria; very rarely-bullous dermatitis, eczema, erythema multiforme, Stevens-Johnson syndrome, Lyell’s syndrome (toxic epidermal necrolysis), exfoliative dermatitis, pruritus, alopecia, photosensitivity reactions, purpura, Schonlein-Henoch purpura.

Kidney and urinary tract disorders:very rarely-acute kidney injury (acute renal failure), hematuria, proteinuria, tubulo-interstitial nephritis, nephrotic syndrome, papillary necrosis.

General disorders and disorders at the injection site: rarely-edema.

Disorders of the cardiovascular system

Data from clinical studies indicate a slight increase in the risk of developing cardiovascular thrombotic complications (for example, myocardial infarction), especially with prolonged use of diclofenac in high doses (daily dose of more than 150 mg).

Visual disturbances

Visual disturbances, such as visual impairment, blurred vision, or diplopia, appear to be class-effects of NSAIDs, and are reversible after discontinuation of use. A possible mechanism for the development of such disorders is inhibition of the synthesis of prostaglandins and other concomitant substances, which changes the regulation of blood flow in the retina, which is manifested by potential visual disorders. If such symptoms develop during diclofenac therapy, an ophthalmological examination should be considered to rule out any other causes.

If any of the side effects listed in the instructions appear, or you notice any other side effects that are not listed in the instructions, tell your doctor.

Interaction

The following types of drug interactions have been reported with the use of Dialrapid and / or other dosage forms of diclofenac. Identified interactions with inhibitors of the CYP2C9 isoenzyme. Caution should be exercised when concomitantly using diclofenac and inhibitors of the CYP2C9 isoenzyme (such as voriconazole) due to the possible increase in the concentration of diclofenac in blood plasma and its exposure. Lithium, digoxin. Since diclofenac may increase plasma concentrations of lithium and digoxin, it is recommended to measure the concentration of lithium and digoxin in the blood when used concomitantly with diclofenac. Diuretics and antihypertensive agents. When used concomitantly with diuretics and antihypertensive drugs (for example, beta-blockers, ACE inhibitors), diclofenac, like other NSAIDs, may reduce their hypotensive effect, so in patients, especially the elderly, when using diclofenac simultaneously with diuretics or antihypertensive drugs, blood pressure should be regularly measured, renal function and hydration should be monitored (especially when combined with diuretics and ACE inhibitors due to an increased risk of nephrotoxicity). Cyclosporine and tacrolimus. Effect of diclofenacan prostaglandin activity in the kidneys may increase the nephrotoxicity of cyclosporine and tacrolimus. Therefore, the dose of diclofenac in patients receiving cyclosporine or tacrolimus should be lower than in patients not receiving these drugs. Drugs that can cause hyperkalemia. Concomitant use of diclofenac with potassium-sparing diuretics, cyclosporine, tacrolimus and trimethoprim may lead to an increase in the potassium content in the blood plasma (in the case of such simultaneous use, this indicator should be monitored frequently). Antibacterial agents – quinolone derivatives. There have been isolated reports of seizures in patients treated concomitantly with quinolone derivatives and diclofenac. Suspected interactions of HDL and glucocorticosteroids. Concomitant systemic use of diclofenac and other systemic NSAIDs or glucocorticosteroids may increase the incidence of gastrointestinal AES. Anticoagulants and antiplatelet agents. Although clinical studies have not established the effect 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 receiving concomitant treatment with these medications should be carefully monitored. Selective serotonin reuptake inhibitors. Concomitant use of diclofenac with selective serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding. Hypoglycemic drugs. Clinical studies have shown that concomitant use of diclofenacne affects the effectiveness of oral hypoglycemic drugs. However, there are isolated reports of the development of both hypoglycemic and hyperglycemic conditions with the use of diclofenac, which require a change in the dose of hypoglycemic drugs. Patients receiving concomitant treatment with hypoglycemic drugs and diclofenac should have their blood glucose measured regularly. There have been isolated reports of the development of metabolic acidosis with concomitant use of diclofenac with metformin. especially in patients with impaired renal function. Methotrexate. Caution should be exercised when using PVP, including diclofenac, less than 24 hours before or after taking methotrexate, as in such cases, the concentration of methotrexate in the blood may increase and its toxic effect may increase. Phenytoin. With simultaneous use of phenytoin and diclofenac, it is necessary to monitor the concentration of phenytoin in blood plasma due to the possible increase in its systemic effects. Inducers of the CYP2C9 isoenzyme. Caution should be exercised when using diclofenac concomitantly with inducers of the CYP2C9 isoenzyme (such as rifampicin), as this can lead to a significant decrease in the concentration of diclofenac in blood plasma and reduce its exposure.

How to take it, course of administration and dosage

The dose of Dialrapid should be selected individually, and in order to reduce the risk of side effects, it is recommended to use the minimum effective dose, if possible, with the shortest possible treatment period, in accordance with the purpose of treatment and the patient’s condition. Preferably taken before meals. The contents of the sachet should be dissolved, stirring, in a glass of water (non-carbonated). The solution may remain slightly cloudy, but this does not affect the effectiveness of the drug. In the case of moderate symptoms, it is usually sufficient to use a daily dose of 50-100 mg in the form of powder to prepare a solution for oral administration (1-2 sachets). The maximum daily dose of the drug should not exceed 150 mg / day. The daily dose should be divided into 3 doses. In primary dysmenorrhea, the daily dose of Dialrapid should be selected individually; it is usually 50-150 mg.The initial dose is 50-100 mg (1-2 sachets); if necessary, for several menstrual cycles, the dose can be increased to 150 mg / day. The drug should be started when the first symptoms appear. Depending on the dynamics of clinical symptoms, treatment can be continued for several days. In case of a migraine attack, the initial dose for Dialrapid is 50 mg (1 sachet). The drug should be taken at the first symptoms of an approaching attack. In cases where pain relief does not occur within 2 hours after taking the first dose, it is possible to re-take the drug at a dose of 50 mg. In the future, every 4-6 hours, an additional intake of Dialrapid at a dose of 50 mg is possible. The total dose of the drug should not exceed 150 mg per day (for no more than 2 days). The efficacy of Dialrapid in the treatment of migraine attacks in children and adolescents has not been established. In adolescents 14 years and older, the drug Dialrapid is used in a daily dose of 50-100 mg of the drug (at the rate of 0.5-2 mg/kg of body weight per day, for the treatment of rheumatoid arthritis, the daily dose can be maximized to 3 mg/kg). Dialrapid should not be used in children and adolescents under 14 years of age. No dose adjustment is required for patients over 65 years of age. However, based on general medical considerations, caution should be exercised in debilitated elderly patients or patients with low body weight. The drug should be used with extreme caution in patients with a high risk of developing diseases of the cardiovascular system. If long-term therapy (more than 4 weeks) is required in such patients, the drug should be used in a daily dose not exceeding 100 mg. Patients with impaired renal function There is no data on the need for dose adjustment when using the drug in patients with impaired renal function due to the lack of studies on the safety of the drug in patients of this category. Caution should be exercised when using the drug in patients with impaired renal function. The use of the drug in patients with renal insufficiency (GFR less than 15 ml / min/1.73 m2) is contraindicated (see the section “Contraindications”). Patients with mild to moderate hepatic impairment There is no data on the need for dose adjustment when using the drug in patients with mild to moderate hepatic impairment due to the lack of safety studies of the drug in this category of patients.

Overdose

Symptoms:vomiting, gastrointestinal bleeding, diarrhea, dizziness, tinnitus, seizures. In case of significant poisoning, acute renal failure and liver damage may develop. Treatment:supportive and symptomatic treatment is indicated for such complications as decreased blood pressure, renal failure, convulsions, gastrointestinal disorders, and respiratory depression. Forced diuresis, hemodialysis, or hemoperfusion are ineffective for diclofenac, since NSAIDs are largely bound to plasma proteins and undergo intensive metabolism. In case of a life-threatening overdose when taking the drug orally, in order to prevent the absorption of diclofenac as soon as possible, gastric lavage should be performed, followed by the use of activated charcoal.

Special instructions

Damage to the gastrointestinal tract

All NSAIDs, including diclofenac, have been associated with bleeding or ulceration/perforation of the gastrointestinal tract, in some cases fatal. These events can occur during any period of treatment in patients with the presence or absence of previous symptoms or a history of gastrointestinal diseases. In elderly patients, such complications can have serious consequences. If patients develop bleeding or ulceration of the gastrointestinal tract while using the drug, the drug should be discontinued.

To reduce the risk of toxic effects on the gastrointestinal tract in patients with ulcerative lesions of the gastrointestinal tract. especially complicated by bleeding or perforation in the anamnesis, as well as in elderly patients, the drug should be used at the minimum effective dose.

Patients with an increased risk of developing gastrointestinal complications, as well as patients receiving therapy with low doses of acetylsalicylic acid or other medications that may increase the risk of gastrointestinal damage, should take gastroprotectors (for example, proton pump inhibitors or misoprostol).

Patients with a history of gastrointestinal disorders, especially the elderly, should report any unusual abdominal symptoms to their doctor.

Patients with bronchial asthma

Exacerbation of bronchial asthma (NSAID intolerance/NSAID-induced asthma), Quincke’s edema, and urticaria are most commonly reported in patients with bronchial asthma, seasonal allergic rhinitis, nasal mucosal polyps, chronic obstructive pulmonary disease, or chronic respiratory tract infections (especially those associated with allergic rhinitis-like symptoms). In this group of patients, as well as in patients with allergies to other drugs (rash, pruritus or urticaria), special care should be taken when using the drug Dialra – pid (readiness for resuscitation measures).

Skin reactions

Serious dermatological reactions such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, and in some cases fatal, have been reported very rarely with NSAIDs, including diclofenac. The greatest risk and frequency of severe dermatological reactions were observed in the first month of diclofenac treatment. If patients receiving Dialrapid develop the first signs of skin rash, mucosal damage, or other symptoms of hypersensitivity, the drug should be discontinued. In rare cases, patients who are not allergic to diclofenac may develop anaphylactic/anaphylactoid reactions when using Dialrapid.

Effects on the liver and biliary tract

Since an increase in the activity of one or more liver enzymes may occur during the use of Dialrapid, as well as in other NSAIDs, long-term therapy with the drug, as a precautionary measure, monitoring of liver function is indicated. If liver function disorders persist and progress, or if signs of liver disease or other symptoms occur (for example, eosinophilia, rash, etc. ), Dialrapid should not be discontinued. It should be borne in mind that hepatitis against the background of the use of the drug Dialrapid can develop without prodromal phenomena.

Effects on the kidneys

During therapy with NSAIDs, including diclofenac, was marked fluid retention and swelling, so you should be very careful it is recommended to monitor renal function in patients with hypertension, disorders of the

heart or kidney disease, elderly patients, patients receiving diuretics or other drugs affecting renal function and in patients with a significant decrease in the volume of circulating blood plasma of any etiology, for example, in the period before and after a massive surgery. After discontinuation of therapy with the drug, normalization of renal function indicators to baseline values is usually noted.

Effects on the cardiovascular system

NSAID therapy, including diclofenac, especially long-term and high-dose therapy, may be associated with a small increase in the risk of serious cardiovascular thrombotic complications (including myocardial infarction and stroke).

In patients with diseases of the cardiovascular system and a high risk of developing diseases of the cardiovascular system (for example, with arterial hypertension, hyperlipidemia, diabetes mellitus, smoking), the drug should be used with extreme caution, at the lowest effective dose with the shortest possible duration of treatment, since the risk of thrombotic complications increases with increasing dose and duration of treatment. For long-term therapy (more than 4 weeks) the daily dose of diclofenac in such patients should not exceed 100 mg. The effectiveness of treatment and the patient’s need for symptomatic therapy should be evaluated periodically, especially in cases where the duration of treatment is longer than 4 weeks. The patient should be instructed to seek immediate medical attention when the first symptoms of thrombotic disorders appear (for example, chest pain, shortness of breath, weakness, speech disorders).

Impact on the hematopoietic system

Dialrapid, like other NSAIDs, may temporarily inhibit platelet aggregation. Therefore, in patients with hemostatic disorders, careful monitoring of appropriate laboratory parameters is necessary. The drug Dialrapid is recommended only for short-term treatment, however, with prolonged use of the drug Dialrapid, ’like other NSAIDs, systematic monitoring of the peripheral blood picture is indicated.

Masking signs of an infectious process

The drug Dialrapid, like other NSAIDs due to its pharmacodynamic properties, can mask the manifestations of infectious diseases.

Concomitant use with other NSAIDs

Do not use Dialrapid concomitantly with other NSAIDs, including selective COX-2 inhibitors, because of the risk of increasing the frequency of adverse events.

Influence on the ability to drive vehicles and / or mechanisms

Patients who experience visual disturbances, dizziness, drowsiness, vertigo, or other central nervous system disorders due to the use of Dialrapid should not drive vehicles or work with mechanisms.

Form of production

Powder for the preparation of a solution for oral use of 50 mg.

Storage conditions

In a dry place at a temperature not exceeding 25°C. The drug should be kept out of the reach of children.

Shelf

life is 3 years.

Active ingredient

Diclofenac

Conditions of release from pharmacies

By prescription

Dosage form

Oral powder