Instructions for use Diclac ID modified-release tablets 75 mg blister No. 100
Composition
active substance: diclofenac;
1 tablet contains diclofenac sodium 75 mg or 150 mg;
excipients: lactose monohydrate, hypromellose (hydroxypropylmethylcellulose), microcrystalline cellulose, calcium hydrogen phosphate, corn starch, sodium starch glycolate (type A), colloidal anhydrous silica, magnesium stearate, iron oxide red (E 172), purified water.
Medicinal form
Tablets with modified release.
The main physical and chemical properties: two-layer tablets of white-pink color, round, flat, with beveled edges and a smooth surface, the pink layer may contain inclusions of white color.
Pharmacotherapeutic group
Non-steroidal anti-inflammatory and anti-rheumatic agents. ATX code M01A B05.
Pharmacological properties
Pharmacodynamics.
Diclofenac is a non-steroidal compound with pronounced antirheumatic, antipyretic, analgesic and anti-inflammatory properties. The mechanism of action is due to inhibition of the biosynthesis of prostaglandins, kinins and other mediators of inflammation and pain, a decrease in the permeability of capillaries, a stabilizing effect on lysosomal membranes. Suppresses platelet aggregation induced by adenosine diphosphate and collagen. In vitro, sodium diclofenac in concentrations equivalent to those achieved in the treatment of patients does not suppress the biosynthesis of proteoglycans of cartilage tissue.
In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac leads to a significant decrease in the severity of pain (both at rest and during movement), morning stiffness, swelling of the joints, and thus - to an improvement in the functional state of the patient.
In the presence of inflammation caused by trauma or surgical intervention, DyklakÒ ID quickly eliminates both spontaneous pain and pain during movement, as well as reduces inflammatory swelling of tissues and swelling in the area of the surgical wound. When used together with opioids to eliminate postoperative pain, DyklakÒ ID significantly reduces the need for opioids.
In clinical studies, it was established that DyklakÒ ID also exhibits a strong analgesic effect in moderate and severe pain sensations of non-rheumatic origin.
Pharmacokinetics
DiklakÒ ID tablets are two-layer tablets with a combination of rapid (1/6 of the total amount) and gradual release (5/6 of the total amount) of diclofenac sodium. Such a combination of effects in one tablet allows you to ensure both a quick onset of action and a long circulation of the active substance in the systemic bloodstream and a therapeutic effect during the day.
After oral administration of the drug diclofenac is completely absorbed and, depending on the duration of passage through the stomach, the maximum concentration in the blood plasma is reached after 1-16 hours, on average after 2-3 hours. The amount of absorbed active substance depends linearly on the dose of the drug. About half of diclofenac is metabolized during the first passage through the liver. Only 35-70% of the absorbed active substance reaches the posthepatic circulation unchanged. Approximately 30% of the active substance is metabolized and excreted with feces. Approximately 70% is removed by the kidneys in the form of pharmacologically inactive metabolites. The elimination half-life is about 2 hours, and this indicator does not depend on the function of the liver and kidneys. Binding to plasma proteins is approximately 99%.
Indications for use
Alleviation of pain and reduction of inflammation of varying degrees in various conditions, including:
- joint pathology: rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, acute attacks of gout;
- acute musculoskeletal diseases, such as periarthritis (for example, shoulder-scapular periarthritis), tendinitis, tendovaginitis, bursitis;
- other pathological conditions caused by injuries, including fractures, back pain, sprains, dislocations, orthopedic, dental and other minor surgical interventions.
Contraindications to use
- Hypersensitivity to the active substance or to any other component of the drug.
- Acute stomach or intestinal ulcer; gastrointestinal bleeding or perforation, gastrointestinal bleeding or perforation in history after the use of nonsteroidal anti-inflammatory drugs (NSAIDs), acute or recurrent stomach or intestinal ulcer in history (two or more separate episodes of established ulcer or bleeding in history).
- Diclofenac, like other NSAIDs, is contraindicated in patients who develop angioneurotic edema, nasal polyps, bronchial asthma attacks, urticaria, acute rhinitis and other allergic symptoms in response to the use of acetylsalicylic acid or other NSAIDs.
- Violation of hematopoiesis of unknown origin.
- Cerebrovascular bleeding or bleeding of the second type.
- Inflammatory bowel diseases (Crohn's disease or ulcerative colitis).
- Liver failure.
- Marked heart failure (NYHA III-IV).
- Congestive heart failure (NYHA II-IV).
- Ischemic heart disease in patients with angina pectoris, previous myocardial infarction.
- Diseases of peripheral arteries.
- Cerebrovascular diseases in patients who have suffered a stroke or have episodes of transient ischemic attacks.
- Treatment of perioperative pain with aorto-coronary shunting (or the use of an artificial blood circulation device).
- Treatment of postoperative pain after coronary bypass surgery (or the use of an artificial circulation device).
Interaction with other medicinal products and other types of interactions
cast With simultaneous use, diclofenac can increase the concentration of lithium in blood plasma. It is recommended to check the levels of lithium in blood plasma.
Digoxin. The concentration of digoxin in the blood plasma may increase with simultaneous use with diclofenac. It is recommended to check digoxin levels in blood plasma.
Diuretics and antihypertensive drugs. As with the use of other NSAIDs, the simultaneous use of Diklak® ID can weaken the antihypertensive effect of diuretics or antihypertensive drugs (for example, beta-blockers, angiotensin-converting enzyme (ACE) inhibitors) by inhibiting the synthesis of vasodilator prostaglandins. Therefore, such a combination should be used with caution; patients, especially the elderly, should regularly monitor their blood pressure. Patients should receive adequate hydration, and kidney function should also be checked at the beginning of combined therapy, and regularly in the future, in particular due to the increased risk of nephrotoxicity when using diuretics and ACE inhibitors.
Anticoagulants and antithrombotic agents. It is recommended to prescribe with caution, since simultaneous use may increase the risk of bleeding.
Careful monitoring of patients who simultaneously use diclofenac and anticoagulants and, if necessary, correction of the dosage of anticoagulants is recommended. Like other NSAIDs, diclofenac in high doses can selectively suppress platelet aggregation.
Other NSAIDs, including selective inhibitors of cyclooxygenase-2 (COX-2) and corticosteroids. Simultaneous use of diclofenac and other systemic NSAIDs or corticosteroids may increase the risk of gastrointestinal bleeding or ulcers. Simultaneous use of two or more NSAIDs should be avoided. Simultaneous use of diclofenac and corticosteroids may increase the frequency of adverse reactions.
Antidiabetic means. There have been separate reports of both hypoglycemic and hyperglycemic reactions after the use of diclofenac, which requires dose adjustments of antidiabetic agents. For this reason, it is recommended to monitor the level of glucose in the blood as a precautionary measure during combined therapy.
Probenecid. Medicinal products containing probenecid can delay the elimination of diclofenac.
Methotrexate. Diclofenac can suppress tubular renal clearance of methotrexate, which increases the level of methotrexate. NSAIDs, including diclofenac, should be used with caution when prescribed less than 24 hours before treatment with methotrexate, since the levels of methotrexate in blood plasma and its toxicity may increase.
Cyclosporine. Diclofenac, like other NSAIDs, can increase the nephrotoxicity of cyclosporine due to its influence on renal prostaglandins. Therefore, the drug should be used in lower doses than for patients not receiving cyclosporine.
Tacrolimus. An increase in the risk of nephrotoxicity is possible if NSAIDs are prescribed simultaneously with tacrolimus.
Antibiotics of the quinolone series. Seizures may occur due to the interaction of quinolone antibiotics and NSAIDs. This can be observed in patients with or without a history of epilepsy or seizures. Therefore, quinolone antibiotics should be used with caution in patients who are already receiving NSAIDs.
Phenytoin. With the simultaneous use of phenytoin and diclofenac, the concentration of phenytoin in blood plasma should be monitored, taking into account the expected increase in exposure to phenytoin.
Colestipol and cholestyramine. These drugs can delay or decrease the absorption of diclofenac. Despite this, it is recommended to use diclofenac at least 1 hour before or 4-6 hours after the administration of colestipol/cholestyramine.
Cardiac glycosides. The simultaneous use of cardiac glycosides and NSAIDs in patients can contribute to the strengthening of heart failure, a decrease in the rate of glomerular filtration, and an increase in the concentration of glycosides in blood plasma.
Mifepristone. NSAIDs should not be used for 8-12 days after taking mifepristone, since NSAIDs can reduce the effect of mifepristone.
Selective serotonin reuptake inhibitors (SSRIs). Simultaneous use of NSAIDs and SSRIs may increase the risk of gastrointestinal bleeding.
Means, the use of which can cause hyperkalemia. Concomitant treatment with potassium-sparing diuretics, cyclosporine, tacrolimus, or trimethoprim may cause an increase in serum potassium, which should be monitored.
Features of use
To reduce the risk of side effects, treatment should be started with the lowest effective dose, which should be taken for the shortest period of time to control symptoms.
General The simultaneous use of diclofenac and other systemic NSAIDs, including selective COX-2 inhibitors, should be avoided due to the lack of any evidence of a synergistic effect and due to potential additive side effects.
Elderly patients should be treated with caution in accordance with the recommendations for this group of patients. In particular, it is recommended to use the minimum effective dose in weakened elderly patients or patients with low body weight.
The use of dosage forms for oral administration, containing diclofenac quick release, can increase gastric intolerance of the drug.
When using diclofenac, like other NSAIDs, allergic reactions, including anaphylactic/anaphylactoid reactions, can rarely develop.
Like other NSAIDs, diclofenac can mask signs and symptoms of infection.
With long-term use of analgesics, headaches may occur. They cannot be treated with increased doses of diclofenac.
Alcohol consumption while taking NSAIDs, including diclofenac, may increase side effects from the gastrointestinal tract (GI) or the central nervous system (CNS).
Since DyklakÒ ID contains lactose, it is not recommended to be prescribed to patients with hereditary conditions accompanied by galactose intolerance, glucose-galactose malabsorption and lactase deficiency.
It is necessary to periodically review the needs of the patient in the use of diclofenac for symptom relief and response to therapy. Use with caution in patients over 65 years of age.
Influence on the gastrointestinal tract. When using NSAIDs, including diclofenac, gastrointestinal bleeding (hematemesis, melena), ulcer or perforation, which can have a fatal outcome, has been observed. They can occur at any time during treatment, with or without precursor symptoms and a history of serious gastrointestinal diseases. In elderly patients, such complications usually have more serious consequences. In case of gastrointestinal bleeding or ulcers, this drug should be discontinued.
Careful medical supervision and special caution are necessary when prescribing diclofenac to patients with symptoms indicating disturbances from the gastrointestinal tract, or with a suspected ulcer, bleeding, perforation of the stomach or intestines in the anamnesis. The risk of these phenomena increases with an increase in the dose of NSAIDs, as well as in patients with a history of an ulcer, in particular, complicated by bleeding or perforation.
Elderly patients have an increased frequency of adverse reactions to NSAIDs, especially gastrointestinal bleeding and perforation, which can be fatal.
To reduce the risk of side effects from the gastrointestinal tract, treatment should be started with the lowest effective dose and stick to it.
The possibility of combined therapy with the use of protective agents (for example, misoprostol or proton pump inhibitors) should be considered in such patients, as well as in patients who require the concomitant use of low doses of acetylsalicylic acid/aspirin or other drugs that may increase the risk of adverse reactions from the gastrointestinal tract.
Caution should be exercised during concomitant treatment with drugs that may increase the risk of ulceration or bleeding, such as systemic corticosteroids, anticoagulants (for example, warfarin), SSRIs, antiplatelet drugs (for example, acetylsalicylic acid).
Effect on the liver. Careful medical supervision is necessary if the drug must be prescribed to patients with impaired liver function, as their condition may worsen.
When using NSAIDs, including diclofenac, the level of one or more liver enzymes may increase. During long-term treatment with diclofenac, regular monitoring of liver function is indicated as a precautionary measure.
Especially careful supervision is necessary in case of impaired liver function immediately after major surgical interventions due to the risk of bleeding.
If the change in liver function indicators persists or worsens, clinical signs or symptoms of liver disease appear, or other manifestations (eosinophilia, rash) are observed, the use of the drug should be discontinued.
Hepatitis without prodromal symptoms may develop while taking diclofenac.
Effects on the kidneys. Since fluid retention and edema have been observed during the use of NSAIDs, special caution should be observed in patients with impaired heart or kidney function, a history of arterial hypertension, elderly patients, patients receiving concomitant treatment with diuretics or drugs that can significantly affect renal function, as well as patients with a significant decrease in the volume of extracellular fluid for any reason (for example, before or after surgery). In such cases, when using diclofenac, it is recommended to monitor renal function as a precautionary measure. After stopping therapy, the patient's condition, as a rule, normalizes.
In general, the habitual use of analgesics, especially in combination with several painkillers, can lead to long-term damage to the kidneys with the risk of developing renal failure (analgesic nephropathy);
Effect on the skin. Serious skin reactions (some of which have been fatal) have been reported, including exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis, which have been observed very rarely with diclofenac. The highest risk of these reactions occurs at the beginning of therapy, and their development is noted in most cases during the first month of treatment. Patients with allergic reactions to other substances require especially careful observation. You should stop taking the drug at the first signs of hypersensitivity.
Systemic lupus erythematosus and mixed connective tissue diseases. Patients with systemic lupus erythematosus and mixed diseases of connective tissue (collagenosis) may have an increased risk of aseptic meningitis.
Cardiovascular and cerebrovascular manifestations. There is an increased risk of thrombotic cardiovascular and cerebrovascular complications (including myocardial infarction and stroke) due to the use of NSAIDs, including diclofenac, especially during long-term treatment with high doses.
Treatment with diclofenac is usually not recommended for patients with established cardiovascular diseases (congestive heart failure, ischemic heart disease, peripheral artery disease) or uncontrolled arterial hypertension. Such patients, as well as patients with significant risk factors for cardiovascular events (for example, hypertension, hyperlipidemia, diabetes mellitus, smoking), can be prescribed diclofenac only after careful clinical evaluation.
Since the cardiovascular risks of diclofenac can increase with an increase in the dose and duration of treatment, it should be used for as short a period as possible and in the lowest effective dose. The dose of the drug should be periodically reviewed, especially if the treatment lasts more than 4 weeks.
Patients should be informed about the signs and symptoms of serious cardiovascular thrombotic complications (for example, chest pain, shortness of breath, weakness, slurred speech), which may occur suddenly. If such symptoms appear, you should immediately consult a doctor.
Patients with mild or moderate hypertension and/or congestive heart failure in the anamnesis require appropriate medical supervision and counseling, as fluid retention and edema have been observed during the use of NSAIDs.
Hematological manifestations. During long-term treatment with diclofenac, it is recommended to monitor blood parameters with determination of the number of formed elements. Diclofenac can selectively suppress the aggregation of platelets. Patients with hemostasis disorders, hemorrhagic diathesis, or hematological abnormalities require careful observation.
Respiratory manifestations. In patients with asthma, seasonal allergic rhinitis, edema of the nasal mucosa (for example, nasal polyps), chronic obstructive pulmonary disease or chronic respiratory tract infections (especially if there is a connection with symptoms similar to allergic rhinitis), reactions to NSAIDs similar to asthma exacerbations (the so-called aspirin-intolerant asthma), Quincke's edema and urticaria occur more often than in others patients In this regard, such patients are recommended to take special precautions (readiness to provide emergency care). This also applies to patients who have allergic reactions to other substances on the skin.
Like other drugs that suppress the activity of prostaglandin synthetase, diclofenac can cause bronchospasm when prescribed to patients with asthma (including a history of it).
Female fertility. There is data that the use of NSAIDs can negatively affect the fertility of women, so drugs of this group are not recommended to be prescribed to women planning pregnancy or to patients suffering from infertility.
Use during pregnancy or breastfeeding
pregnancy Inhibition of prostaglandin synthesis may adversely affect pregnancy and/or embryonic/fetal development. Data from epidemiological studies indicate an increased risk of miscarriage and/or heart disease and gastroschisis after the use of prostaglandin synthesis inhibitors in the early stages of pregnancy. It is believed that the risk increases with an increase in the dose and duration of therapy.
During the III trimester of pregnancy, all inhibitors of prostaglandin synthesis can affect the fetus in the following way:
- cardiopulmonary toxicity (with premature closure of the arterial duct and pulmonary hypertension);
- impaired kidney function, which can progress to renal failure with oligohydroamniosis.
At the end of pregnancy, the following phenomena may occur:
- possible prolongation of bleeding time, antiplatelet effect can be observed even at very low doses;
- inhibition of uterine contraction, which leads to delay or prolongation of labor.
Consequently, DyklakÒ ID is contraindicated in the III trimester of pregnancy.
Breast feeding
Like other NSAIDs, diclofenac penetrates into breast milk in small quantities, so this drug is contraindicated during breastfeeding.
Female fertility
Like other NSAIDs, diclofenac can affect female fertility and is therefore not recommended for women planning pregnancy. Consideration should be given to stopping the use of diclofenac in women who cannot become pregnant, as well as in women who are being examined for infertility.
The ability to influence the speed of reaction when driving a motor vehicle or other mechanisms
It is not recommended for patients who experience dizziness, vertigo, drowsiness, lethargy or fatigue, disorders of the central nervous system, including impaired vision, to drive vehicles or other mechanisms while taking the drug.
Method of application and dosage
The dose of the drug is selected individually, starting with the minimum effective dose. To minimize side effects, the lowest effective dose should be used for the shortest period of time to control symptoms, taking into account the treatment goals of each individual patient.
The recommended starting dose of the drug for adults is 75-150 mg per day, depending on the severity of the symptoms of the disease. With long-term therapy, as a rule, the use of 1 tablet (75 mg) per day is sufficient. If the symptoms of the disease are most pronounced during the night or in the morning, DyklakÒ ID should be used in the evening.
The maximum daily dose is 150 mg and should not be exceeded. DiklakÒ ID is intended for short-term use (maximum 2 weeks).
The duration of treatment is determined by the doctor.
Tablets should be swallowed whole, without chewing, with a sufficient amount of liquid, preferably during or after a meal.
Children: DiklakÒ ID is not recommended for use by children.
Elderly patients: no clinically significant changes in pharmacokinetics were observed when the drug was used in elderly patients. But in such patients, NSAIDs should be used with special caution, since they are more prone to side effects. It is recommended to take the minimum effective dose for elderly patients or patients with low body weight, as well as for patients who need constant monitoring to detect possible gastrointestinal bleeding when using NSAIDs.
Patients with established cardiovascular diseases and a significant risk of their occurrence. Diclofenac treatment is usually not recommended for such patients, as well as for patients with uncontrolled arterial hypertension. If necessary, the drug can be prescribed only after a careful evaluation of the risk-benefit ratio in a dose of ≤ 100 mg per day and a treatment duration of no more than 4 weeks.
Patients with impaired kidney function. Diclofenac is contraindicated in renal failure. For the treatment of patients with impaired kidney function of a weak or moderate degree, the drug should be used with caution.
Patients with impaired liver function. Diclofenac is contraindicated in liver failure. For the treatment of patients with impaired liver function of a weak or moderate degree, the drug should be used with caution.
Children
DyklakÒ ID is contraindicated for the treatment of children due to the high content of the active substance in the tablet.
Overdose
Treatment of acute NSAID poisoning consists in the use of supportive and symptomatic therapy measures. Symptomatic and supportive measures are indicated for complications such as arterial hypotension, renal failure, seizure syndrome, disorders of the gastrointestinal tract and respiratory depression. It is unlikely that such specific medical measures as forced diuresis, dialysis, or hemoperfusion will be useful for the elimination of NSAIDs, since the active substances of these drugs are largely bound to blood proteins and undergo intensive metabolism. After taking potentially toxic doses, activated charcoal can be used, and after taking potentially life-threatening doses, perform gastric decontamination (inducing vomiting, gastric lavage).
Adverse reactions
From the digestive tract: nausea, vomiting, diarrhea, dyspepsia, abdominal pain, abdominal cramps, flatulence, loss of appetite, gastritis, gastrointestinal bleeding, hematemesis, hemorrhagic diarrhea, melena, stomach and intestinal ulcers with or without bleeding or perforation (sometimes with a fatal outcome, especially in elderly patients), colitis (including hemorrhagic colitis and exacerbation ulcerative colitis, or Crohn's disease), constipation, stomatitis (including ulcerative stomatitis), glossitis, esophageal disorders, the formation of diaphragm-like strictures in the intestines, pancreatitis.
From the side of the nervous system: headache, dizziness, drowsiness, increased fatigue, paresthesia, memory impairment, convulsions, feeling of anxiety, tremor, impaired taste, impaired cerebral circulation, confusion of consciousness, hallucinations, impaired sensitivity, general malaise, apoplexy.
Mental disorders: disorientation, depression, insomnia, nightmares, irritability, psychotic disorders.
From the cardiovascular system: palpitation, chest pain, heart failure, myocardial infarction, arterial hypertension, hypotension, vasculitis.
On the part of the organs of vision: vision impairment, blurred vision, diplopia, optic neuritis.
On the part of the organs of hearing: vertigo, ringing in the ears, hearing loss.
From the skin and subcutaneous tissue: inflammatory skin changes, rash, urticaria, bullous rash, eczema, erythema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, erythroderma, hair loss, photosensitivity reactions, purpura, allergic purpura, itching;
On the part of the kidneys and urinary tract: acute renal failure, hematuria, proteinuria, nephrotic syndrome, interstitial nephritis, papillary necrosis of the kidney, fluid retention in the body, edema.
On the part of the hepatobiliary system: increased activity of transaminases, hepatitis, jaundice, impaired liver function, fulminant hepatitis, liver necrosis, liver failure.
From the blood and lymphatic system: thrombocytopenia, leukopenia, anemia (including hemolytic and aplastic anemia), pancytopenia, agranulocytosis.
The first signs of disorders of the blood and lymphatic system may be: fever, sore throat, superficial wounds in the oral cavity, flu-like symptoms, fatigue, nosebleeds, skin hemorrhages.
From the respiratory system: bronchial asthma (including dyspnea), pneumonitis.
On the part of the immune system: hypersensitivity reactions, anaphylactic and anaphylactoid reactions (including arterial hypotension and shock), angioedema (including swelling of the face, tongue, larynx).
From the side of the reproductive system: impotence.
Infectious diseases: exacerbation of inflammation associated with infections (for example, the development of necrotic fasciitis), symptoms of aseptic meningitis.
Data from clinical studies and epidemiological data indicate an increased risk of thrombotic complications (for example, myocardial infarction or stroke) associated with the use of diclofenac, in particular in high therapeutic doses (150 mg/day) and with long-term use.
Expiration date
3 years.
Storage conditions
Store at a temperature not higher than 25 °C.
Store in a place inaccessible to children.
Packaging
10 tablets in a blister; 2 (10 2) or 10 (10 10 10) blisters in a cardboard box.
Leave category
According to the recipe.
For tablets of 75 mg:
Manufacturer
Salutas Pharma GmbH, Germany/Salutas Pharma GmbH, Germany.
The location of the producer and its address of the place of implementation of activity
Otto-von-Guericke-Allee 1, 39179 Barleben, Germany/Otto-von-Guericke-Allee 1, 39179 Barleben, Germany.
For tablets of 150 mg:
Manufacturers
Salutas Pharma GmbH, Germany (bulk production, packaging, batch production).
Lek S. A., Poland/Lek SA, Poland (packaging, serial release).
Location of manufacturers and their addresses of places of operation
Otto-von-Guericke-Allee 1, 39179 Barleben, Germany/Otto-von-Guericke-Allee 1, 39179 Barleben, Germany.
50 C, st. Domaniewska, 02-672 Warsaw, Poland/50 C, Domaniewska Str., 02-672 Warsaw, Poland.
