Dialrapid powder d / prig solution for oral administration 50 mg sachet 9 pcs. (Diclofenac)

Release form

Powder for solution for oral administration 50 mg.

Pharmacological action

The drug Dialrapid contains diclofenac potassium, a non-steroidal 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 preferred for the treatment of acute pain and inflammatory conditions. The main mechanism of action of diclofenac, established in the studies, is considered to be the inhibition of 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 when used in humans does not inhibit the biosynthesis of cartilaginous proteoglycans.

Diclofen 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 edema of the postoperative wound.

In clinical studies, it was found that diclofenac potassium is able to reduce pain and reduce blood loss in primary dysmenorrhea.

With migraine attacks, dialrapid reduces the severity of headaches and associated symptoms such as nausea and vomiting.

Pharmacokinetics

Absorption

Diclofenac is rapidly and completely absorbed. After a single oral administration of the drug in a dose of 50 mg, the maximum concentration (Cmax) of diclofenac potassium in the blood plasma is reached after 5-20 minutes and averages 5.5 μmol / L for the powder for the preparation of the oral solution. When taking the drug with food, the amount of absorbed diclofenac does not change, although the onset and rate of absorption may slow down somewhat. Diclofenac absorption is linearly dependent on the dose of the drug. About half the dose of diclofenac is metabolized during the first passage through the liver (first-pass effect), the area under the concentration-time (AUC) pharmacokinetic curve after oral or rectal administration is approximately half of the parenteral equivalent dose. After repeated use of the drug Dialrapid, pharmacokinetics do not change.

Subject to the recommended dosage regimen, no accumulation is observed.

Distribution of

Communication with serum proteins - 99.7%, mainly with albumin (99.4%). The apparent volume of distribution is 0.12-0.17 l / kg.

Diclofenac penetrates into the synovial fluid, where its maximum concentration is reached 2-4 hours later than in blood plasma. The apparent half-life of synovial fluid is 3-6 hours. 2 hours after reaching the maximum plasma concentration, the concentration of diclofenac in the synovial fluid is higher than in the blood plasma, and its values ​​remain higher for a period of time up to 12 hours.

Biotransformation / Metabolism

Diclofenac metabolism is carried out in part by glucuronidation of an 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.

Excretion

The total systemic plasma clearance of diclofenac is 263 ± 56 ml / min. The final half-life is 1-2 hours. The elimination half-life of 4 metabolites, including two pharmacologically active, is also short and makes 1-3 hours. One of the metabolites, 3'-hydroxy-4'-methoxy-diclofenac, has a longer half-life, however, this metabolite is completely inactive.

About 60% of the dose is excreted by the kidneys in the form of glucuronic conjugates of an unchanged active substance, 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 in the form of metabolites with bile.

Pharmacokinetics in special patient groups

After oral administration, there are no differences in absorption, metabolism, or excretion of the drug related to the age of the patients.

In patients with impaired renal function, cumulation of the unchanged active substance is not observed when the recommended dosage regimen is observed. With creatinine clearance less than 10 ml / min, the calculated equilibrium concentrations of diclofenac hydroxymetabolites are approximately 4 times higher than in healthy volunteers, while the metabolites are excreted exclusively with bile.

In patients with chronic hepatitis or compensated cirrhosis, 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 ligaments

postoperative pain, inflammation and swelling, for example, after dental or orthopedic surgery

pain and / or inflammation, accompanying , eg, primary dysmenorrhea or adnexitis

migraine attacks

pain syndromes from the spine

rheumatic diseases of extraarticular soft tissues.

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

Contraindications

Hypersensitivity to the active substance and other components of the drug, as well as to other non-steroidal anti-inflammatory drugs (NSAIDs)

exacerbation of gastric ulcer and duodenal ulcer, ulcerative 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 to acetylsalicylic acid or other NSAIDs (including a history of liver function) severe renal failure (GFR less than 15 ml / min / 1.73 m2)

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

clinically confirmed ischemic heart disease

peripheral arterial and cerebrovascular disease

uncontrolled arterial hypertension

III trimester of pregnancy

period of breastfeeding.

The drug should not be used in patients with phenylketonuria, since 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).

WITH CAUTION

When using the drug Dialrapid and other NSAIDs, care must be taken to carefully observe patients with symptoms / signs indicating lesions / diseases of the gastrointestinal tract (GIT) or with anamnestic data that may suspect ulceration of the stomach or intestines, bleeding or perforation in patients with Helicobacterpylori infection in the anamnesis, ulcerative colitis, Crohn’s disease, with a history of impaired liver function and in patients with complaints that suspect a disease Table of the gastrointestinal tract. The risk of developing gastrointestinal bleeding increases with an increase in the dose of NSAIDs or in the presence of a history of gastrointestinal ulcers, especially bleeding and perforation of ulcers and in elderly patients.

Special care should be taken when using the drug 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 the drug Dialrapid in patients with impaired hepatic function of mild to moderate severity, as well as in patients with hepatic porphyria, since 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 affecting the function of the kidneys, 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.

Caution is advised to use the drug Dialrapid in patients with defects in the hemostatic system.

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 the drug Dialrapid in elderly patients. This is especially true in weakened or low body weight elderly people.

Special instructions

Damage to the gastrointestinal tract

When applying all NSAIDs, including diclofenac, bleeding or ulceration / perforation of the gastrointestinal tract was noted, in some cases with fatal outcome. These phenomena can occur at any period of treatment in patients with a history or absence of previous symptoms or a gastrointestinal disease. In elderly patients, such complications can have serious consequences. With the development of patients with the use of the drug Dialrapid bleeding or ulceration of the gastrointestinal tract, the drug should be discontinued.

To reduce the risk of toxic effects on the gastrointestinal tract in patients with gastric ulcer. especially complicated bleeding or perforation in history, as well as in elderly patients, the drug should be used in a minimum effective dose.

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

Patients with a history of gastrointestinal tract damage, especially the elderly, all unusual abdominal symptoms should be reported to the doctor.

Patients with bronchial asthma

Exacerbation of bronchial asthma (NSAIDs / bronchial asthma caused by NSAIDs), Quincke edema and urticaria are most often observed in patients with bronchial asthma, seasonal allergic rhinitis, mucous membrane polyps of the nasal disease, chronic chronic respiratory infections (especially those associated with allergic rhinitis-like symptoms). In this group of patients, as well as in patients with an allergy to other drugs (rash, itching, or urticaria), special care should be taken when using the Dialra preparation (readiness for resuscitation).

Skin reactions

Serious dermatological reactions such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, in some cases with a fatal outcome, have been very rare with the use of NSAIDs, including diclofenac. The greatest risk and frequency of severe dermatological reactions were noted in the first month of diclofenac treatment. With the development in patients receiving the drug Dialrapid, the first signs of a skin rash, mucosal lesions 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.

Impact on the liver and biliary tract

Since during the use of the drug Dialrapid, also as in other NSAIDs, an increase in the activity of one or more liver enzymes may be noted, with prolonged therapy with the drug, as a precaution, control of liver function is indicated. With the preservation and progression of impaired hepatic function or the occurrence of signs of liver disease, or other symptoms (eg, eosinophilia, rash, etc.), the administration of the drug Dialrapid should be discontinued. It should be borne in mind that hepatitis with the use of the drug Dialrapid can develop without prodromal phenomena.

Effects on the kidneys

During therapy with NSAIDs, including diclofenac, fluid retention and swelling were noted, therefore, special care should be taken and it is recommended to monitor renal function in patients with hypertension, impaired

function of the heart or kidneys, elderly patients, patients receiving diuretics or other drugs that affect renal function, as well as in patients with a significant decrease in the volume of circulating blood plasma of any etiology, for example, before and after massive surgical interventions. After discontinuation of drug therapy, normalization of renal function indices to initial values ​​is usually noted.

Effects on the cardiovascular system

Therapy of NSAIDs, including diclofenac, in particular, long-term therapy and high-dose therapy, may be associated with a slight 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, smokers), the drug should be used with extreme caution, at the lowest effective dose for the shortest possible duration of treatment, since the risk of thrombotic complications increases with increasing dose and duration of treatment. With prolonged therapy (more than 4 weeks), the daily dose of diclofenacau in such patients should not exceed 100 mg. Periodically evaluate the effectiveness of treatment and the patient's need for symptomatic therapy, especially in cases where its duration is more than 4 weeks. The patient should be instructed to seek immediate medical attention if the first symptoms of thrombotic disorders appear (for example, chest pain, feeling of lack of air, weakness, speech impairment).

Impact on the hematopoietic system

The drug Dialrapid, like other NSAIDs, can temporarily inhibit platelet aggregation. Therefore, in patients with hemostatic disorders, careful monitoring of relevant 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, a systematic monitoring of the picture of peripheral blood is shown.

Masking signs of an infectious process

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

Use concurrently with other NSAIDs

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

Effect on the ability to drive vehicles and / or mechanisms

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

Ingredients

1 sachet contains: active ingredient: diclofenac potassium 50.0 mg

excipients: glyceryl adibehenate 2.0 mg, sodium saccharinate 5.0 mg, anise flavor 15.0 mg, potassium hydrogen carbonate 22.0 mg, mint flavor 35.0 mg, aspartame 50.0 mg, mannitol 721.0 mg.

Dosage and administration of

The dose of Dialrapid should be selected individually, while 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 (still). The solution may remain slightly cloudy, but this does not affect the effectiveness of the drug.

In the case of moderate severity of symptoms, it is usually sufficient to use a daily dose of 50-100 mg in powder form to prepare an oral solution (1-2 sachets).

The maximum daily dose 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, usually it is 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. Taking the drug should begin when the first symptoms appear. Depending on the dynamics of the clinical symptoms, treatment can be continued for several days. With a migraine attack, the initial dose for the drug Dialrapid is 50 mg (1 sachet). The drug should be taken at the first symptoms of an approaching attack. In cases when, within 2 hours after taking the first dose, pain relief does not occur, a repeated dose of 50 mg is possible. In the future, every 4-6 hours, an additional intake of the drug Dialrapid in 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 effectiveness of the drug Dialrapid in the treatment of migraine attacks in children and adolescents has not been established.

In adolescents 14 years of age and older, the drug Dialrapid is used in a daily dose of 50-100 mg of the drug (based on 0.5-2 mg / kg of body weight per day, for the treatment of rheumatoid arthritis, the daily dose can be maximized up to 3 mg / kg) .

The drug Dialrapid should not be used in children and adolescents under 14 years of age.

Dose adjustment is not required for patients over 65 years of age. However, for general medical reasons, caution should be exercised in debilitated elderly patients or patients with low body weight.

Use the drug with extreme caution in patients at high risk of developing diseases of the cardiovascular system. If long-term therapy (more than 4 weeks) is necessary, the drug should be used in such patients 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 failure (GFR less than 15 ml / min / 1.73 m2) is contraindicated (see section "Contraindications").

Patients with impaired liver function of mild to moderate severity

There is no data on the need for dose adjustment when using the drug in patients with impaired liver function of mild to moderate severity due to the lack of studies on the safety of the drug in this category of patients.

Side effects of

The following are adverse events (AEs) that have been identified in clinical trials, as well as with the use of diclofenac in clinical practice.

The following criteria were used to evaluate the frequency of AE: “often” -> 1/100, <1/10, “infrequently” -> 1/1000, <1/100, “rarely” -> 1/10000, <1/1000 , “Very rare” - <1/10000, including isolated cases. AEs are grouped in accordance with the system-organ class of the medical dictionary for regulatory activity of MedDRA, within each class AEs are listed in decreasing order of occurrence, within each group allocated by frequency of occurrence, AEs are distributed in order of decreasing importance.

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

Immune system disorders: rarely - hypersensitivity, anaphylactic / anaphylactoid reactions, including a decrease in blood pressure (BP) and shock very rarely - angioedema (including facial edema).

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

Disorders of the nervous system: often - headache, dizziness rarely - drowsiness very rarely - sensory disturbances, including paresthesia, memory disorders, tremors, cramps, anxiety, acute cerebrovascular accident, aseptic meningitis.

Violations of the organ of vision: very rarely - visual impairment (blurred vision), diplopia.

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

Disorders from the heart: infrequently - myocardial infarction, heart failure, palpitations, chest pain.

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

Disorders of the respiratory system, mediastinal chest organs: rarely - bronchial asthma (including shortness of breath) very rarely - pneumonitis.

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

- stomatitis, glossitis, damage to the esophagus, the occurrence of diaphragm-like strictures in the intestine, colitis (nonspecific hemorrhagic colitis, ischemic colitis, exacerbation of ulcerative colitis or Crohn’s disease), constipation, pancreatitis, dysgeusia. Violations of the liver and biliary tract: often - increased activity of plasma aminotransferases rarely

- hepatitis, jaundice, impaired liver function very rarely - fulminant hepatitis, liver necrosis, liver failure. Disorders of the skin and subcutaneous tissues: often - skin rash rarely - urticaria very rarely - bullous dermatitis, eczema, erythema, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome (toxic epidermal necrolysis), exfoliative dermatitis, pruritus, alopecia, reactions photosensitivity, purple, Shenlein-Genoch purple.

Disorders from the kidneys and urinary tract: very rarely - acute kidney damage (acute renal failure), hematuria, proteinuria, tubulo-interstitial nephritis, nephrotic syndrome, papillary necrosis.

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

Disorders from the cardiovascular system

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

Visual disturbances

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

If any of the side effects indicated in the instructions are aggravated, or you notice any other side effects not listed in the instructions, inform your doctor.

Drug Interactions

The following types of drug interactions have been reported with Dialrapid and / or other dosage forms of diclofenac.

Identified interactions

Inhibitors of the CYP2C9 isoenzyme. Caution should be exercised while the use of diclofenac and inhibitors of the isoenzyme CYP2C9 (such as voriconazole) due to a possible increase in the concentration of diclofenac in blood plasma and its exposure.

Lithium, digoxin. Since diclofenac can increase the concentration of lithium and digoxin in blood plasma, it is recommended to measure the concentration of lithium and digoxin in the blood while using it with diclofenac.

Diuretic and antihypertensive drugs. When used simultaneously with diuretics and antihypertensive drugs (for example, beta-blockers, ACE inhibitors), diclofenac, like other NSAIDs, can reduce their hypotensive effect, therefore, in patients, especially in elderly patients, while diclofen is used diuretics or antihypertensive drugs should regularly measure blood pressure, monitor renal function and degree of hydration (especially when combined with diuretics and ACE inhibitors due to increased risk of nephrotoxicity).

Cyclosporine and tacrolimus. The effect of diclofenacan on the activity of prostaglandins in the kidneys may enhance the nephrotoxicity of cyclosporin and tacrolimus. In connection with the foregoing, the dose of diclofenacau in patients receiving cyclosporine or tacrolimus should be lower than in patients not receiving these drugs.

Drugs that can cause hyperkalemia. The simultaneous use of diclofenac with potassium-sparing diuretics, cyclosporine, tacrolimus and trimethoprim can lead to an increase in the potassium content in blood plasma (in the case of such simultaneous use, this indicator should often be monitored).

Antibacterial agents - quinolone derivatives. There are separate reports of the development of seizures in patients receiving both quinolone derivatives and diclofenac.

Suspected interactions of

NSAIDs and glucocorticosteroids.

The simultaneous systemic use of diclofenac and other systemic NSAIDs or glucocorticosteroids can increase the incidence of AE from the gastrointestinal tract.

Antioxidants and antiplatelet agents. Although clinical studies have not established the effect of diclofenac on the action of anticoagulants, there are some reports of an increased risk of bleeding in patients taking this combination of drugs. Patients receiving concurrent treatment with these drugs should be carefully monitored.

Selective serotonin reuptake inhibitors. The simultaneous use of diclofenacas with selective serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.

Hypoglycemic drugs. Clinical studies have found that the simultaneous use of diclofenacne affects the effectiveness of oral hypoglycemic drugs. However, there are separate reports of the development of both hypoglycemic and hyperglycemic conditions with diclofenac, requiring a change in the dose of hypoglycemic drugs. In patients receiving simultaneous treatment with hypoglycemic drugs and diclofenac, blood glucose concentration should be regularly measured.

Separate reports on the development of metabolic acidosis with the simultaneous use of diclofenac with metformin have been received. 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, since in such cases the concentration of methotrexate in the blood may increase and its toxic effect may increase.

phenytoin. With the simultaneous use of phenytoin and diclofenac, it is necessary to control the concentration of phenytoin in blood plasma due to the possible increase in its systemic effect.

Inducers of CYP2C9 isoenzyme Caution should be exercised when using diclofenac at the same time as inducers of CYP2C9 isoenzyme (such as rifampicin), since this can lead to a significant decrease in the concentration of diclofenac in blood plasma and a decrease in its exposure.

Overdose

Symptoms: vomiting, gastrointestinal bleeding, diarrhea, dizziness, tinnitus, cramps. In case of significant poisoning, the development of acute renal failure and liver damage is possible.

Treatment: supportive and symptomatic treatment is indicated for complications such as decreased blood pressure, renal failure, convulsions, gastrointestinal disorders, and respiratory depression. Forced diuresis, hemodialysis, or hemoperfusion are ineffective for diclofenac, since NSAIDs bind to a large extent to plasma proteins and undergo intensive metabolism.

In case of a life-threatening overdose when taking the drug inside, in order to prevent diclofenac absorption as soon as possible, gastric lavage should be performed, followed by the use of activated charcoal.

Storage conditions

In a dry place at a temperature not exceeding 25 ° C.

The drug should be stored out of the reach of children.

Expiration

3 years.

Active ingredient

Diclofenac



pharmacy terms for prescription

Dosage form

powder for ingestion



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