Description of the drug VOLTAREN® for systemic use
The dose is selected individually; it is recommended to use the drug in the minimum effective dose, with the shortest possible treatment period.
For oral and rectal use
Adults
When taken orally in the form of tablets of regular duration or rectally in the form of suppositories, the recommended initial dose is 100-150 mg/day. In relatively mild cases of the disease, as well as for long-term therapy, 75-100 mg/day is sufficient. The daily dose should be divided into several doses.
When taken in the form of extended-release tablets, the recommended initial dose is 100 mg 1 time / day. The same daily dose is used for moderately severe symptoms, as well as for long-term therapy. In cases where the symptoms of the disease are most pronounced at night or in the morning, it is advisable to take extended-release tablets at night.
To relieve night pain or morning stiffness
in addition to taking the drug during the day, diclofenac is prescribed in the form of rectal suppositories before bedtime; in this case, the total daily dose should not exceed 150 mg.
With primary dysmenorrhea
the daily dose is selected individually; usually it is 50-150 mg. The initial dose should be 50-100 mg; if necessary, over several menstrual cycles it 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 elderly patients (65 years and older)
no adjustment of the initial dose is required.
In weakened patients, patients with low body weight
It is recommended to adhere to the minimum dose.
The drug should be used with particular caution in patients with diseases of the cardiovascular system (including uncontrolled arterial hypertension) or a high risk of developing cardiovascular diseases
. If long-term therapy (more than 4 weeks) is necessary in such patients, the drug should be used in a daily dose not exceeding 100 mg.
Children aged 1 year and older
The drug is prescribed in a dose of 0.5-2 mg/kg body weight/day (in 2-3 doses, depending on the severity of the disease). For the treatment of rheumatoid arthritis
the daily dose can be maximally increased to 3 mg/kg (in several doses). The maximum daily dose is 150 mg.
The drug in the form of extended-release tablets should not be used in children and adolescents under the age of 18 years.
For parenteral use
Adults
Injected deep into the / m. Single dose - 75 mg. If necessary, repeated administration is possible, but not earlier than after 12 hours.
Duration of use is no more than 2 days, if necessary, then switch to oral or rectal use of diclofenac.
In severe cases (for example, with colic), as an exception, 2 injections of 75 mg each can be given, with an interval of several hours (the second injection should be carried out in the opposite gluteal region). Alternatively, IM administration once a day (75 mg) can be combined with diclofenac in other dosage forms (tablets, rectal suppositories), and the total daily dose should not exceed 150 mg.
For migraine attacks
Diclofenac is recommended to be administered as early as possible after the onset of an attack, IM at a dose of 75 mg, followed by the use of suppositories at a dose of up to 100 mg on the same day, if required. The total daily dose should not exceed 175 mg on the first day.
In elderly patients (65 years and older)
no adjustment of the initial dose is required. In weakened patients and patients with low body weight, it is recommended to adhere to the minimum dose.
The drug should be used with particular caution in patients with diseases of the cardiovascular system (including uncontrolled arterial hypertension) or a high risk of developing cardiovascular diseases
. If long-term therapy (more than 4 weeks) is necessary in such patients, the drug should be used in a daily dose not exceeding 100 mg.
Children and teenagers under 18 years of age
Diclofenac should not be used intramuscularly in children and adolescents under 18 years of age due to the difficulty of dosing the drug.
Voltaren solution for injection 75 mg/3 ml in ampoules 3 ml No. 5
Name
Voltaren solution d/in.75mg/3ml in amp.3ml in pack No. 5
Description
The solution for intramuscular administration is colorless or light yellow.
Main active ingredient
Diclofenac
Release form
The solution for intramuscular administration is colorless or light yellow. 1 ml diclofenac sodium 25 mg Excipients: mannitol (pyrogen-free) - 18 mg, distilled propylene glycol - 600 mg, benzyl alcohol - 120 mg, sodium bisulfite - 2 mg, sodium hydroxide for pH - up to pH 7.8-8.0, water d/i - up to 3 ml. 3 ml - glass ampoules with a break point or break ring (5) - cardboard packs.
Dosage
75mg/3ml in amp. 3ml in pack No. 5
special instructions
Damage to the gastrointestinal tract When using diclofenac, phenomena such as bleeding or ulceration/perforation of the gastrointestinal tract were observed, in some cases with fatal outcome. These events may occur at any time when using drugs in patients with or without previous symptoms and a history of serious gastrointestinal diseases. In older patients, such complications can have serious consequences. If bleeding or gastrointestinal ulceration develops in patients receiving Voltaren®, the drug should be discontinued. To reduce the risk of toxic effects on the gastrointestinal tract, patients with gastrointestinal ulcers, especially those complicated by bleeding or a history of perforation, as well as in elderly patients, the drug should be used in the minimum effective dose. Patients at increased risk of developing gastrointestinal complications, as well as patients receiving therapy with low doses of acetylsalicylic acid (Aspirin), should take gastroprotectors (proton pump inhibitors or misoprostol) or other medications to reduce the risk of unwanted effects on the gastrointestinal tract. Patients with a history of gastrointestinal lesions, especially the elderly, should report all abdominal symptoms to the doctor. Patients with bronchial asthma Exacerbation of bronchial asthma (NSAID intolerance/bronchial asthma provoked by NSAIDs), angioedema and urticaria are most often observed in patients suffering from bronchial asthma, seasonal allergic rhinitis, nasal polyps, COPD or chronic infectious diseases of the respiratory tract (especially associated with allergic rhinitis-like symptoms). In this group of patients, as well as in patients with allergies to other drugs (rash, itching or urticaria), special caution should be observed when using the drug Voltaren® (preparedness for resuscitation measures). Skin reactions Serious dermatological reactions such as exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, in some cases fatal, have been reported very rarely with the use of diclofenac. The highest risk and incidence of severe dermatological reactions were observed in the first month of treatment with diclofenac. If patients receiving Voltaren® develop the first signs of skin rash, damage to the mucous membranes or other symptoms of hypersensitivity, the drug should be discontinued. In rare cases, in patients who are not allergic to diclofenac, anaphylactic/anaphylactoid reactions may develop when using Voltaren®. Effects on the liver Since during the period of use of the drug Voltaren® there may be an increase in the activity of one or more liver enzymes, during long-term therapy with the drug, monitoring of liver function is indicated as a precautionary measure. If liver dysfunction persists and progresses or signs of liver disease or other symptoms (for example, eosinophilia, rash, etc.) occur, the drug should be discontinued. It should be borne in mind that hepatitis during the use of the drug Voltaren® can develop without prodromal phenomena. Effects on the kidneys During therapy with Voltaren®, it is recommended to monitor renal function in patients with hypertension, impaired cardiac or renal function, the elderly, patients receiving diuretics or other drugs that affect renal function, as well as in patients with a significant decrease in circulating plasma volume blood of any etiology, for example, during the period before and after major surgical interventions. After discontinuation of drug therapy, normalization of renal function indicators to pre-baseline values is usually observed. Impact on the cardiovascular system NSAID therapy, incl. Diclofenac, particularly long-term and high-dose therapy, may be associated with a small increase in the risk of serious cardiovascular thrombotic events (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 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 periodically assessed, especially in cases where its duration is more than 4 weeks. When the first symptoms of thrombotic disorders appear (for example, chest pain, feeling short of breath, weakness, speech impairment), the patient should immediately seek medical help. Effects on the hematopoietic system Voltaren® may temporarily inhibit platelet aggregation. Therefore, in patients with hemostasis disorders, it is necessary to carefully monitor relevant laboratory parameters. With long-term use of the drug Voltaren®, it is recommended to conduct regular clinical tests of peripheral blood. Masking signs of an infectious process The anti-inflammatory effect of the drug Voltaren® may complicate the diagnosis of infectious processes. Use simultaneously with other NSAIDs Voltaren® should not be used simultaneously with NSAIDs, including selective COX-2 inhibitors, due to the risk of increased adverse events. Impact on the ability to perform potentially hazardous activities that require special attention and quick reactions (driving vehicles, working with moving mechanisms, etc.) Patients who experience visual disturbances, dizziness, drowsiness, vertigo or other disorders of the central nervous system should not drive vehicles or operate machinery.
pharmachologic effect
Voltaren® contains diclofenac sodium, a non-steroidal substance that has a pronounced anti-inflammatory, analgesic and antipyretic effect. The main mechanism of action of diclofenac, established under experimental conditions, is considered to be inhibition of prostaglandin biosynthesis. Prostaglandins play an important role in the pathogenesis of inflammation, pain and fever. In vitro, diclofenac sodium, in concentrations equivalent to those achieved during patient treatment, does not inhibit the biosynthesis of cartilage proteoglycans. In rheumatic diseases, the anti-inflammatory and analgesic properties of Voltaren provide a clinical effect, characterized by a significant reduction in the severity of such manifestations of diseases as pain at rest and during movement, morning stiffness and swelling of the joints, as well as an improvement in the functional state. A pronounced analgesic effect of the drug Voltaren® was noted for moderate and severe pain of non-rheumatic origin. Pain relief occurs within 15-30 minutes. In case of post-traumatic and postoperative inflammatory phenomena, Voltaren® quickly relieves pain, reduces inflammatory swelling and swelling of the postoperative wound. When used in combination with opioids in patients with postoperative pain, Voltaren significantly reduces the need for opioid analgesics. In addition, Voltaren® relieves migraine attacks.
Pharmacokinetics
Absorption After intramuscular (IM) administration of 75 mg of diclofenac, its absorption begins immediately. Cmax, the average value of which is about 2.5 μg/ml (8 μmol/l), is reached in approximately 20 minutes. The amount of absorbed active substance is linearly dependent on the dose of the drug. The area under the “first pass” curve through the liver. With subsequent administrations of the drug, the pharmacokinetic parameters do not change. Provided that the recommended intervals between administrations of the drug are observed, no accumulation is observed. Distribution: Connection 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 the blood plasma. The apparent half-life from synovial fluid is 3-6 hours. 2 hours after reaching the maximum concentration in plasma, the concentration of diclofenac in synovial fluid is higher than in plasma, and its values remain higher for a period of time up to 12 hours. Diclofenac was found in low concentration (100 ng/ml) in the breast milk of one of the nursing mothers. The estimated amount of the drug that enters the child's body through breast milk is equivalent to 0.03 mg/kg/day. Metabolism The metabolism of diclofenac is carried out partly by glucuronidation of the unchanged molecule, but mainly through 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. The phenolic metabolite is biologically active, but to a much lesser extent than diclofenac. Elimination The total systemic plasma clearance of diclofenac is 263±56 ml/min. The terminal half-life is 1-2 hours. T1/2 of 4 metabolites, including two pharmacologically active ones, is also short-lived and amounts to 1-3 hours. One of the metabolites, 3′-hydroxy-4′-methoxy-diclofenac, has more long half-life, but this metabolite is completely inactive. About 60% of the drug dose is excreted in the urine in the form of glucuronic conjugates of the 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 drug dose is excreted in the form of metabolites in bile. The concentration of diclofenac in plasma depends linearly on the dose taken. Pharmacokinetics in certain groups of patients Absorption, metabolism and excretion of the drug do not depend on age. However, in some elderly patients, a 15-minute IV infusion of diclofenac resulted in an increase in plasma concentrations of the drug by 50% compared with those expected in adult patients. In patients with impaired renal function, accumulation of unchanged active substance is not observed if the recommended dosage regimen is observed. With a QC of less than 10 ml/min, the calculated equilibrium concentrations of diclofenac hydroxystabolites are approximately 4 times higher than in healthy volunteers, while the metabolites are excreted exclusively in bile. In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetics of diclofenac are similar to those in patients without liver disease.
Indications for use
- inflammatory and degenerative diseases of the musculoskeletal system: rheumatoid arthritis, ankylosing spondylitis and other spondyloarthropathy; osteoarthritis; gouty arthritis; bursitis, tendovaginitis; - diseases of the spine accompanied by pain (lumbago, sciatica, ossalgia, neuralgia, myalgia, arthralgia, radiculitis); - renal and biliary colic; - post-traumatic and postoperative pain syndromes accompanied by inflammation (for example, in dentistry and orthopedics); - severe migraine attacks.
Directions for use and doses
Voltaren®, solution for intramuscular injection, should be administered 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. Voltaren® ampoules are particularly suitable for the initial treatment of inflammatory and degenerative rheumatic diseases, as well as pain due to inflammation of non-rheumatic origin. Voltaren® is administered by deep injection into the gluteal muscle. Voltaren® injections should not be used for more than 2 days in a row. If necessary, treatment can be continued with Voltaren® in tablets or rectal suppositories. When performing an intramuscular injection, in order to avoid damage to the nerve or other tissues, it is recommended to adhere to the following rules. The drug should be injected deep IM into the upper outer quadrant of the gluteal region. The dose is usually 75 mg (contents of 1 ampoule) 1 time/day. In severe cases (for example, with colic), as an exception, 2 injections of 75 mg each can be given, with an interval of several hours (the second injection should be carried out in the opposite gluteal region). Alternatively, one injection of the drug per day (75 mg) can be combined with other dosage forms of Voltaren® (tablets, rectal suppositories), and the total daily dose should not exceed 150 mg. During migraine attacks, the best result is achieved if Voltaren® is administered as early as possible after the onset of the attack, IM at a dose of 75 mg (1 amp.), followed by the use of suppositories at a dose of up to 100 mg on the same day, if required. The total daily dose should not exceed 175 mg on the first day. The drug solution should be transparent. Do not use a solution with crystalline or other sediment. The drug ampoule should be used only once. The solution must be administered immediately after opening the ampoule. After a single use, the remaining Voltaren® solution unused for treatment is no longer used. Do not mix the solution of Voltaren® contained in ampoules with solutions of other drugs for injection. Children and adolescents under 18 years of age Voltaren® injection solution should not be used in children and adolescents under 18 years of age due to the difficulty of dosing the drug; If treatment is necessary in this category of patients, Voltaren® can be used in tablets or suppositories. Elderly patients (> 65 years) No initial dose adjustment is required in patients aged 65 years and older. In weakened patients and patients with low body weight, it is recommended to adhere to the minimum dose. Patients with diseases of the cardiovascular system or a high risk of diseases of the cardiovascular system The drug should be used with extreme caution in patients with diseases of the cardiovascular system (including uncontrolled arterial hypertension) or a high risk of developing diseases of the cardiovascular system. If long-term therapy (more than 4 weeks) is necessary in such patients, the drug should be used in a daily dose not exceeding 100 mg. Patients with mild to moderate renal impairment There is no data on the need for dose adjustment when using the drug in patients with mild to moderate renal impairment due to the lack of safety studies of the drug in this category of patients. Patients with mild to moderate liver dysfunction There is no data on the need for dose adjustment when using the drug in patients with mild to moderate liver dysfunction due to the lack of safety studies of the drug in this category of patients.
Use during pregnancy and lactation
There is insufficient data on the safety of diclofenac in pregnant women. Voltaren® should be prescribed in the first and second trimesters of pregnancy only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. Voltaren®, like other inhibitors of prostaglandin synthesis, is contraindicated in the last 3 months of pregnancy (possible suppression of uterine contractility and premature closure of the ductus arteriosus in the fetus). Despite the fact that Voltaren®, like other NSAIDs, passes into breast milk in small quantities, the drug should not be prescribed to nursing women to prevent undesirable effects on the baby. If it is necessary to use the drug Voltaren® in a nursing woman, stop breastfeeding. Since Voltaren®, like other NSAIDs, can have a negative effect on fertility, women planning pregnancy are not recommended to take the drug. For patients undergoing examination and treatment for infertility, the drug should be discontinued.
Precautionary measures
When using the drug Voltaren® and other NSAIDs, careful medical monitoring is necessary for patients with gastric or intestinal ulcers, Helicobacter pylori infection, ulcerative colitis, Crohn's disease, a history of liver dysfunction, or patients with complaints indicating gastrointestinal diseases. The risk of developing gastrointestinal bleeding increases with increasing doses of NSAIDs or with a history of ulcers, especially bleeding and perforation of the ulcer and in elderly patients. Particular caution should be exercised when using the drug Voltaren® in patients receiving drugs that increase the risk of gastrointestinal bleeding: systemic corticosteroids (including prednisolone), anticoagulants (including warfarn), antiplatelet agents (including clopidogrel, acetylsalicylic acid) or selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline). Caution is necessary when prescribing Voltarsn® in patients with mild to moderate liver dysfunction, as well as in patients with hepatic porphyria, because the drug can provoke attacks of porphyria. The drug should be used with caution in patients with bronchial asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (including nasal polyps), COPD, chronic infectious diseases of the respiratory tract (especially those associated with allergic rhinitis-like symptoms). Particular caution is required when treating patients with cardiovascular diseases (including ischemic heart disease, cerebrovascular diseases, compensated heart failure, peripheral vascular disease), impaired renal function, including chronic renal failure (creatinine clearance 30-60 ml/mn), dielnpidemia/psherlipidemia, diabetes mellitus diabetes, hypertension, when treating smoking patients or patients who abuse alcohol, when treating elderly patients receiving diuretics or other drugs that affect the function of points, as well as patients with a significant decrease in the volume of extracellular fluid of any etiology, for example, in the periods before and after massive surgical interventions. Voltarev® should be used with caution in patients with defects in the hemostatic system. Caution should be exercised when using Voltiren® in patients at risk of developing cardiovascular thrombosis (including myocardial infarction and stroke). Caution should be exercised when using Voltaren® in elderly patients. This is especially true in frail or low-weight elderly people; they are recommended to prescribe the drug at the minimum effective dose. Particular caution should be observed when administering the drug Voltaren® intramuscularly to patients with bronchial asthma due to the risk of exacerbation of the disease, because Sodium bisulfite contained in the drug can cause severe hypersensitivity reactions.
Interaction with other drugs
Identified interactions Potent inhibitors of CYP2C9. Caution should be exercised when co-administering diclofenac and strong CYP2C9 inhibitors (such as voriconazole) due to the possible increase in diclofenac serum concentrations and increased systemic effects caused by inhibition of diclofenac metabolism. Lithium, digoxip. Diclofenac may increase plasma concentrations of lithium and digoxin. It is recommended to monitor the concentration of lithium and digoxin in the blood serum. Diuretics and antihypertensive drugs. When used simultaneously with diuretics and antihypertensive drugs (for example, beta-blockers, ACE inhibitors), diclofenac may reduce their hypotensive effect. Therefore, in patients, especially elderly patients, when diclofenac is co-administered with diuretics or antihypertensive drugs, blood pressure should be regularly measured, renal function and hydration levels monitored (especially when combined with diuretics and ACE inhibitors due to the increased risk of nephrotoxicity). Cyclosporine. The effect of diclofenac on the activity of prostate glandins in the kidneys may enhance the nephrotoxicity of cyclosporine. Therefore, the doses of diclofenac used should be lower than in patients not using cyclosporine. Drugs that can cause hyperkalemia: Concomitant use of diclofenac with potassium-sparing diuretics, cyclosporine, tacrolimus and trimethoprim may lead to an increase in plasma potassium levels (in the case of such a combination, this indicator should be monitored frequently). Antibacterial agents quinolone derivatives. There are isolated reports of the development of seizures in patients receiving quinolone derivatives and diclofecac simultaneously. Potential interactions between NSAIDs and corticosteroids. The simultaneous systemic use of diclofenac and other systemic NSAIDs or corticosteroids may increase the incidence of adverse events (in particular, from the gastrointestinal tract). Anticoagulants and antiplatelet agents. It is necessary to combine diclofenac with drugs of these groups with caution due to the risk of bleeding. Despite the fact that 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. Therefore, in the case of such a combination of drugs, careful monitoring of patients is recommended. Selective serotonin reuptake inhibitors. Concomitant use of diclofenac with selective serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding. Hypoglycemic drugs. Clinical studies have established that simultaneous use of diclofenac and hypoglycemic drugs is possible, while the effectiveness of the latter does not change. However, there are isolated reports of the development in such cases of both hypoglycemia and hyperglycemia, which necessitated the need to change the dose of hypoglycemic drugs during the use of diclofenac. Therefore, during the temporary combined use of diclofenac and hypoglycemic drugs, it is recommended to monitor blood glucose concentrations. Methotrexate. Caution should be exercised when prescribing diclofenac less than 24 hours before or 24 hours after taking methotrexate, because in such cases, the concentration of methotrexate in the blood may increase and its toxic effect may increase. Fenitoip. When using fenntoin and diclofenac simultaneously, it is necessary to monitor the concentration of phenytoin in the blood plasma due to a possible increase in its systemic effect.
Contraindications
- stomach or intestinal ulcer; - hypersensitivity to diclofenac and any other ingredients of the drug, including sodium metabisulfite; — Voltaren® is contraindicated in patients in whom attacks of bronchial asthma, urticaria or acute rhinitis are provoked by acetylsalicylic acid or other NSAIDs, as well as any drugs that suppress the production of prostaglandins; — Voltaren® solution for injection is not prescribed to children and adolescents under the age of 18 years; — Voltaren® solution for injection is not prescribed during pregnancy.
Compound
1 ml diclofenac sodium 25 mg Excipients: mannitol (pyrogen-free) - 18 mg, distilled propylene glycol - 600 mg, benzyl alcohol - 120 mg, sodium bisulfite - 2 mg, sodium hydroxide for pH - up to pH 7.8-8.0, water d/i - up to 3 ml.
Overdose
Symptoms: vomiting, gastrointestinal bleeding, diarrhea, dizziness, tinnitus, convulsions. In case of significant poisoning, acute renal failure and liver damage may develop. Treatment: supportive and symptomatic treatment is indicated for complications such as decreased blood pressure, renal failure, seizures, gastrointestinal disorders and respiratory depression. Forced diuresis, hemodialysis or hemoperfusion are ineffective for dnclofenac, because the active substances of these drugs are largely bound to plasma proteins and undergo intensive metabolism.
Side effect
Below are the adverse events that were identified during clinical studies, as well as when using diclofenac in clinical practice. To assess the frequency of adverse events, the following criteria were used: very often (>1/10), often (>1/100, 1/1000, 1/10,000,
Storage conditions
At a temperature not higher than 30°C. Protect from exposure to light and high temperatures. The drug should be stored out of the reach of children.
Voltaren Emulgel for back pain, muscles and joints, gel 1% 75g
A country
Switzerland
The country of production may vary depending on the batch of goods. Please check with the operator for detailed information when confirming your order.
Active substance
Diclofenac
Description
Voltaren Emulgel 75g with an innovative applicator cap - convenient to apply, leaving your hands clean.
Voltaren Emulgel is intended for pain in the joints, back, muscles, as well as inflammation and swelling of soft tissues and joints. Voltaren Emulgel has a triple effect! 1: against pain 2: against inflammation * 3: to speed up recovery ** The active substance diclofenac is a non-steroidal anti-inflammatory drug with pronounced analgesic and anti-inflammatory properties, penetrates deep into the skin, acting on both pain and its cause - inflammation. * * Instructions for medical use, RU No. P N016030/01 dated 09.09.2009 ** Limit. Musculoskeletal disorders. 2013, 14:250. Compared to using placebo.
Compound
100 g of the drug contains: Active ingredient: 1.16 g of diclofenac diethylamine, which corresponds to 1 g of diclofenac sodium. Excipients: carbomers (carbopol 974 R) 1.20 g, macrogol cetostearate (cetomacrogol 1000) 2.00 g, cocoyl caprylocaprate (cetiol LC) 2.50 g, diethylamine 0.90 g, isopropanol 20.00 g, liquid paraffin 2.50 g, aromatic cream 45 (contains benzyl benzoate) 0.10 g, propylene glycol 5.00 g, water 64.64 g.
Product description
Homogeneous, creamy gel, color from white to yellowish.
pharmachologic effect
The active component diclofenac is a non-steroidal anti-inflammatory drug with pronounced analgesic, anti-inflammatory and antipyretic properties.
By indiscriminately inhibiting cyclooxygenase types 1 and 2, it disrupts the metabolism of arachidonic acid. Voltaren Emulgel is used to eliminate pain and reduce swelling associated with the inflammatory process. Thanks to its water-alcohol base, Voltaren Emulgel has a calming and cooling effect. Pharmacokinetics Absorption The amount of diclofenac absorbed through the skin is proportional to the area of the treated surface and depends both on the total dose of the drug applied and on the degree of skin hydration. After applying 2.5 g of Voltaren Emulgel to a skin area of 500 cm2, absorption is about 6% of the applied dose of diclofenac compared to Voltaren tablets. Distribution: 99.7% of diclofenac is bound to plasma proteins, mainly albumin (99.4%). The concentration of diclofenac in plasma, synovial membrane and synovial fluid was measured when the drug was applied to the area of the affected joint. Maximum plasma concentrations were approximately 100 times lower than after oral administration of the same amount of diclofenac. Diclofenac accumulates in the skin, which plays the role of a reservoir that releases the active substance into the tissue. When applied to the area of the affected joint, the concentration of synovial fluid is higher than in plasma. Diclofenac is preferentially distributed and retained deep in tissues prone to inflammation (such as joints) rather than in the bloodstream. The concentration of diclofenac in tissues is up to 20 times higher than in plasma. Metabolism The metabolism of diclofenac is carried out partly by glucuronidation of the unchanged molecule, but mainly through single and multiple hydroxylation. Excretion Most of diclofenac and its metabolites are excreted in the urine. The total systemic plasma clearance of diclofenac is 263±56 ml/min. The terminal half-life is 1-2 hours. The half-life of metabolites, including two pharmacologically active ones, is also short and amounts to 1-3 hours. One of the metabolites (3'-hydroxy-4'-methoxydiclofenac) has a longer half-life, however , this metabolite is completely inactive. Patients with renal and hepatic impairment Accumulation of diclofenac and its metabolites is not expected in patients suffering from renal impairment. In patients with chronic hepatitis or uncompensated cirrhosis, the kinetics and metabolism of diclofenac are the same as in patients without liver disease
Indications for use
Back pain due to inflammatory and degenerative diseases of the spine (sciatica, osteoarthritis, lumbago, sciatica), - joint pain (joints of the fingers, knees, etc.) with osteoarthritis, - muscle pain (due to sprains, strains, bruises, injuries) , - inflammation and swelling of soft tissues and joints due to injuries and rheumatic diseases (tenosynovitis, bursitis, lesions of periarticular tissues)
Contraindications
Hypersensitivity to diclofenac or other components of the drug; a tendency to develop attacks of bronchial asthma, Quincke's edema, urticaria or acute rhinitis when using acetylsalicylic acid or other NSAIDs; pregnancy (III trimester), breastfeeding; children's age (up to 12 years); violation of the integrity of the skin at the intended site of application.
Carefully
Hepatic porphyria (exacerbation), erosive and ulcerative lesions of the gastrointestinal tract, severe dysfunction of the liver and kidneys, chronic heart failure, bronchial asthma, old age, pregnancy (I and II trimester).
Use during pregnancy and lactation
Due to the lack of data on the use of Voltaren Emulgel in pregnant women, the use of the drug during the first and second trimester of pregnancy is recommended only as prescribed by a doctor, weighing the benefits for the mother and the risk for the fetus. The drug is contraindicated in the third trimester of pregnancy due to the possibility of decreased uterine tone, impaired fetal renal function with subsequent development of oligohydramnios and/or premature closure of the fetal ductus arteriosus. Due to the lack of data on the penetration of Voltaren Emulgel into breast milk, the use of the drug during breastfeeding is recommended only as prescribed by a doctor, weighing the benefits for the mother and the risk to the fetus. If it is still necessary to use the drug, it should not be applied to the mammary glands or large surface areas of the skin and should not be used for a long time. There are no data on the use of Voltaren Emulgel and its effect on fertility in humans.
Directions for use and doses
Externally. For adults and children over 12 years of age, the drug is applied to the skin 3-4 times a day and lightly rubbed. The required amount of the drug depends on the size of the painful area. A single dose of the drug - 2-4 g (which is comparable in volume to the size of a cherry or walnut, respectively) is sufficient to treat an area of 400-800 cm2. If your hands are not the area where pain is localized, your hands should be washed after applying the drug. The duration of treatment depends on the indications and the observed effect (to enhance the effect, the gel can be used together with other dosage forms of Voltaren). If after 7 days of use the therapeutic effect is not observed or the condition worsens, you should consult a doctor. The product should not be used for more than 14 days for post-traumatic inflammation and rheumatic diseases of soft tissues. Laminated tubes: To remove the protective membrane, use the screw cap as a key (the recess with ridges on the outside of the cap). Align the indentation on the outside of the cap with the shaped protective membrane of the tube and turn. The membrane should separate from the tube. Laminated tubes can have either a regular cap (round shape) or an innovative cap (triangular shape), which is especially convenient for use with limited mobility of the joints of the hands due to osteoarthritis or other joint diseases or injuries, as well as an applicator cap. Aluminum tubes: Before first use, the protective membrane of the tube must be pierced using the special protrusion on the outside of the polypropylene screw cap. Aluminum bottles: The drug is applied to the skin 3-4 times a day. Spray on the painful area for 3-6 seconds, lightly rub into the skin until the solution is completely absorbed. The required amount of the drug depends on the size of the painful area. If your hands are not the area where pain is localized, your hands should be washed after applying the drug.
Side effect
Classification of the frequency of occurrence of adverse reactions: very often (≥1/10); often (≥1/100, Infectious and parasitic diseases: Very rare: pustular rash. Immune system disorders: Very rare: hypersensitivity reactions (including urticaria), angioedema. Respiratory, thoracic and mediastinal disorders: Very rare: bronchial asthma Disorders of the skin and subcutaneous tissues: Common: dermatitis (including contact dermatitis), rash, erythema, eczema, itching Rare: bullous dermatitis Very rare: photosensitivity reactions If any of the side effects indicated in the instructions are aggravated , or you notice any other side effects not listed in the instructions, tell your doctor.
Overdose
The extremely low systemic absorption of the active components of the drug when used externally makes overdose almost impossible. However, with accidental ingestion of 100 g of gel, equivalent to 1 g of diclofenac sodium, systemic adverse reactions may develop. Treatment for accidental ingestion: gastric lavage, induction of vomiting, activated charcoal, symptomatic therapy. Hemodialysis is ineffective due to the high degree of protein binding of diclofenac (about 99%)
Interaction with other drugs
Voltaren Emulgel may enhance the effect of drugs that cause photosensitivity. Clinically significant interactions with other drugs have not been described.
special instructions
Voltaren Emulgel should be applied only to intact skin, avoiding contact with open wounds. After application, do not apply an occlusive dressing. Do not allow the drug to come into contact with the eyes or mucous membranes, and do not swallow. The drug contains propylene glycol and benzyl benzoate, which in some cases may cause mild local skin irritation. Treatment should be discontinued if a skin rash develops after application of the drug. The possibility of systemic adverse reactions (associated with the use of systemic forms of diclofenac) should be considered if diclofenac for external use is used at a higher dose or for a longer time than recommended.
Release form
Gel for external use 1%. 75 g each in an aluminum tube equipped with a protective aluminum membrane, with a screw-on plastic cap (white or blue) with a protrusion for perforating the membrane on the outside. The tube along with instructions for use are placed in a cardboard box. 75 g in a laminated tube (low-density polyethylene, aluminum, high-density polyethylene) with a shoulder and a one-piece shaped protective membrane made of high-density polyethylene and a polypropylene screw cap (white or blue), round or triangular, or with a screw-on applicator cap with transparent protective cap. The cover on the outside is equipped with a key (a recess with protrusions) for opening the protective membrane of the tube. The tube along with instructions for use are placed in a cardboard box. 75 ml in a pressurized aluminum bottle (about 73 g and 97 g, respectively), with a plastic pump dispenser on a polyethylene ring and a protective cap. The bottle along with instructions for use is placed in a cardboard box. Secondary packaging is allowed to have a first-opening control.
Storage conditions
At a temperature not exceeding 30 C, out of the reach of children.
Best before date
3 years. The drug should not be used after the expiration date indicated on the package.
Indications for use of the drug Voltaren emulgel
Symptomatic treatment of pain, inflammation and swelling in:
- soft tissue damage: injuries to tendons, ligaments, muscles and joints (for example due to dislocation, sprain, hematoma); sports injuries;
- localized forms of rheumatic diseases of soft tissues: tendonitis including tennis elbow, bursitis, shoulder-hand syndrome, periarthritis;
Side effects of the drug Voltaren emulgel
Voltaren Emulgel is usually well tolerated. Adverse reactions include mild transient reactions on the skin at the site of application. In rare cases, allergic reactions have occurred. Infections and infestations: very rarely - pustular rashes. From the immune system: very rarely - hypersensitivity reactions, angioedema. From the respiratory system: very rarely - bronchial asthma. From the skin and connective tissue: often - rashes, erythema, eczema, dermatitis, including contact; rarely - bullous dermatitis; very rarely - photosensitivity reactions, itching, burning sensation of the skin.
Voltaren retard tablets p/o prolonged action 75 mg No. 10x2
Name
Voltaren retard.
Release forms
Pills.
INN
Diclofenac
FTG
Npvp.
Compound
active ingredient: diclofenac sodium; Each tablet contains diclofenac sodium 75 mg; excipients: tablet core - magnesium stearate, anhydrous colloidal silicon dioxide, povidone, cetyl alcohol, sucrose; tablet coating - hypromellose, red iron oxide (E 172), polysorbate 80, talc, titanium dioxide (E 171), macrogol 8000, sucrose, black ink (shellac, isopropyl alcohol, black iron oxide E172, butyl alcohol, propylene glycol, ammonium hydroxide ).
Pharmacotherapeutic group
Nonsteroidal anti-inflammatory and antirheumatic drugs. Derivatives of acetic acid. ATS code M01A B05. Clinical characteristics
Indications for use
Inflammatory and degenerative rheumatic diseases: rheumatoid arthritis, ankylosing spondylitis; arthrosis; extra-articular rheumatism. Pain and inflammation of non-rheumatic or post-traumatic origin. Symptomatic treatment of primary dysmenorrhea.
Contraindications
Known hypersensitivity to the active substance or other components of the drug, to other analgesics, antipyretics, non-steroidal anti-inflammatory drugs (NSAIDs) and, in particular, to acetylsalicylic acid; Active stomach or intestinal ulcer, bleeding or perforation. Inflammatory bowel diseases (such as Crohn's disease or ulcerative colitis); Last trimester of pregnancy; Liver failure; Renal failure (GFR
Directions for use and doses
The tablets should be taken whole, without chewing or breaking, with liquid, preferably with meals. The dose should be selected individually. Side effects can be minimized by using the lowest effective dose for the minimum period necessary to control symptoms (see Precautions). The recommended initial dose of the drug for adults is 75 - 150 mg per day (1-2 tablets of Voltaren Retard 75 mg), depending on the severity of the symptoms of the disease. For long-term therapy, as a rule, the use of 1 tablet of Voltaren Retard 75 mg per day is sufficient. If the symptoms of the disease are most pronounced at night or in the morning, Voltaren Retard should be taken in the evening. Use in special groups of patients. Children (under 18 years of age) Voltaren retard tablets, film-coated, prolonged action 75 mg are not recommended for use in children due to the high content of the active substance. Elderly patients (65 years and older). For elderly patients, no adjustment of the starting dose is usually required. However, based on generally accepted approaches, caution is required when prescribing the drug, especially in weakened or low-weight elderly patients. Patients with congestive heart failure (NYHA-I) or significant cardiovascular risk factors In patients with congestive heart failure (NYHA-I) or uncontrolled hypertension, therapy with Voltaren is generally not recommended. If necessary, the drug is prescribed to patients with cardiovascular diseases or with significant risk factors for their development only after a thorough assessment, and for a duration of therapy of more than 4 weeks - only in doses
Side effects
Adverse reactions to the drug, depending on the frequency, are described in the following order: very often (> 1/10); often (> 1/100, 1/1000, 1/10000,
Overdose
There is no typical clinical picture of diclofenac overdose. Symptoms of a diclofenac overdose may include vomiting, gastrointestinal bleeding, diarrhea, dizziness, tinnitus, and convulsions. In case of significant poisoning, acute renal failure and liver damage are possible. Treatment of acute NSAID poisoning consists of the use of supportive and symptomatic therapy. Supportive and symptomatic treatment is indicated for complications such as hypotension, renal failure, seizures, gastrointestinal disorders and respiratory depression. It is unlikely that specific therapeutic measures such 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. Activated charcoal may be used after a potentially toxic overdose, as well as gastric decontamination (eg, vomiting, gastric lavage) after a potentially life-threatening overdose. Women of childbearing age, pregnancy, breastfeeding, fertility There are no data to support any recommendations for women of childbearing age. Suppression of prostaglandin synthesis can adversely affect the course of pregnancy and intrauterine development of the fetus. Epidemiological studies suggest an increased risk of miscarriage and/or fetal heart defects and gastroschisis after taking prostaglandin synthesis inhibitors in early pregnancy, but aggregated data are inconclusive. The absolute risk of cardiovascular defects increased from less than 1% to 1.5%. The risk is believed to increase with increasing dose and duration of therapy. It has been shown that in animals, the administration of prostaglandin synthesis inhibitors leads to disruption of embryo implantation. In addition, in animals receiving a prostaglandin synthesis inhibitor during the period of organogenesis, the incidence of various malformations, including developmental disorders of the cardiovascular system, increased. The use of diclofenac in pregnant women has not been studied. Therefore, Voltaren Retard should not be prescribed during the first two trimesters of pregnancy, unless the benefits of its use outweigh the risks to the fetus. As with other NSAIDs, use of the drug during the third trimester of pregnancy is contraindicated. When taking prostaglandin synthesis inhibitors in the third trimester of pregnancy, the fetus may experience: premature closure of the ductus arteriosus and pulmonary hypertension, renal dysfunction, with the progression of which renal failure with oligohydroamnion develops. When taking diclofenac at the end of pregnancy, labor weakness may develop and the duration of labor may increase. In the mother and in the fetus/newborn, bleeding time may be prolonged; the antiplatelet effect may occur even after taking very low doses of diclofenac. Thus, diclofenac is contraindicated in the third trimester of pregnancy. Like other NSAIDs, diclofenac is excreted in small quantities into breast milk. Thus, Voltaren Retard should not be used during breastfeeding in order to prevent unwanted reactions in the child. Like other NSAIDs, Voltaren Retard can adversely affect female fertility, so it is not recommended to prescribe the drug to women planning a pregnancy. In women who have difficulty conceiving or are undergoing examination for infertility, the advisability of discontinuing the drug should be considered.
Children
Voltaren Retard is not recommended for the treatment of children aged 14-18 years due to the high content of the active substance in the tablet. The drug is contraindicated in children under 14 years of age. Precautions Gastrointestinal effects With all NSAIDs, gastrointestinal bleeding, ulceration and perforation are possible, which can be fatal and occur during treatment with or without a history of warning symptoms or serious gastrointestinal disorders. In general, such phenomena are most dangerous for elderly patients. In isolated cases, when patients taking Voltaren Retard develop these complications, treatment with this drug should be discontinued. While taking the drug Voltaren Retard, medical supervision is necessary for patients who have diseases of the gastrointestinal tract or a history of gastric or intestinal ulcers, ulcerative colitis or Crohn's disease. The risk of gastrointestinal bleeding increases with increasing doses of NSAIDs and in patients with a history of ulcers, especially if the ulcer was complicated by bleeding or perforation or occurred in the elderly. To reduce the risk of toxic effects on the gastrointestinal tract in patients with a history of peptic ulcer, in particular, complicated by bleeding and perforation, as well as in elderly patients, treatment should be started with the lowest effective dose and maintained thereafter. In the above patients and patients requiring concomitant use of low doses of acetylsalicylic acid or other drugs that may increase the risk of developing adverse reactions from the gastrointestinal tract, combination therapy in combination with protective drugs (for example, proton pump inhibitors or misoprostol) should be considered. . Caution is advised in patients receiving concomitant therapy with systemic corticosteroids, anticoagulants, antiplatelet agents, or selective serotonin reuptake inhibitors. Cardiovascular Effects: Clinical studies and epidemiological data strongly suggest an increased risk of arterial thrombotic events (eg, myocardial infarction or stroke) that may be associated with the use of diclofenac, particularly when used in high doses (150 mg daily) and with long-term use. In patients with significant risk factors for cardiovascular complications (eg, hypertension, hyperlipidemia, diabetes mellitus, smoking), diclofenac should be prescribed only after careful consideration of this possibility. Due to the possible increased risk of cardiovascular events with long-term use or high doses of the drug, patients should be prescribed diclofenac at the minimum effective dose and take it for the shortest time necessary to reduce the severity of symptoms. The need for symptom relief and response to treatment should be periodically re-evaluated. In patients with congestive heart failure (NYHA-I) or significant risk factors for cardiovascular events (eg, hypertension, hyperlipidemia, diabetes mellitus, smoking), diclofenac should be used only after careful evaluation, and if the duration of therapy is more than 4 weeks - only in doses
Impact on the ability to drive vehicles and operate machinery
Patients who experience dizziness or other unpleasant sensations from the central nervous system, including visual disturbances, while taking Voltaren Retard, are not recommended to drive a car or operate machinery.
Interaction with other drugs
Caution is recommended when co-administering Voltaren Retard with CYP2C9 inhibitors (such as voriconazole), which may lead to a significant increase in peak plasma concentrations and exposure of diclofenac. Voltaren Retard may increase plasma concentrations of lithium and digoxin. It is recommended to monitor serum lithium and digoxin levels. Voltaren Retard, like other NSAIDs, may inhibit the activity of diuretics or antihypertensive drugs (for example, beta blockers, angiotensin-converting enzyme (ACE) inhibitors). Therefore, the combination should be used with caution and the blood pressure of patients, especially the elderly, should be monitored periodically. Patients should receive adequate fluid intake, and monitoring of renal function is recommended upon initiation of concomitant therapy and on a regular basis thereafter, especially when using diuretics and ACE inhibitors due to the increased risk of nephrotoxicity. Concomitant use of potassium-sparing diuretics, cyclosporine, tacrolimus or trimethoprim may lead to an increase in serum potassium levels (this indicator should be regularly monitored). Concomitant use with other systemic NSAIDs or corticosteroids may increase the incidence of adverse reactions of Voltaren Retard from the gastrointestinal tract. Concomitant use of systemic NSAIDs and SSRIs may increase the risk of bleeding in the digestive tract. Although clinical studies have not established the effect of Voltaren Retard on the action of anticoagulants, there are isolated reports of an increased risk of bleeding in patients taking Voltaren Retard and anticoagulants simultaneously. Therefore, close monitoring of such patients is recommended. Clinical studies have shown that Voltaren Retard can be used in conjunction with oral antidiabetic agents and does not change their therapeutic effect. However, there are isolated reports of the development in such cases of both hypoglycemia and hyperglycemia, which led to changes in the dose of glucose-lowering drugs during the use of Voltaren Retard. For this reason, monitoring of blood glucose levels is recommended as a precaution during concomitant therapy. Caution should be exercised when prescribing NSAIDs 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. The effect of NSAIDs, including Voltaren Retard, on the synthesis of prostaglandins in the kidneys may enhance the nephrotoxicity of cyclosporine. In this regard, Voltaren Retard should be used in lower doses than in patients who do not receive cyclosporine. When using phenytoin together with Voltaren Retard, it is recommended to monitor the concentration of phenytoin in the blood plasma due to a possible increase in phenytoin exposure. Colestipol and cholestyramine may delay or reduce the absorption of diclofenac. It is recommended to take diclofenac at least one hour before or 4-6 hours after colestipol/cholestyramine. There are isolated reports of the development of seizures in patients receiving concomitant quinolone derivatives and NSAIDs.
Pharmacological properties
Pharmacodynamics. Diclofenac, the active substance of Voltaren Retard, is a non-steroidal compound with pronounced antirheumatic, anti-inflammatory, analgesic and antipyretic effects. The main mechanism of action of diclofenac, established under experimental conditions, is considered to be inhibition of prostaglandin biosynthesis. Prostaglandins play an important role in the genesis of inflammation, pain and fever. In vitro, diclofenac sodium in concentrations equivalent to those achieved in the treatment of patients does not suppress the biosynthesis of proteoglycans in cartilage tissue. Voltaren Retard is suitable for patients in whom a daily dose of 75 mg is appropriate, taking into account the clinical picture. The ability to prescribe a drug that allows for a single dose of the entire daily dose greatly simplifies long-term treatment and helps avoid possible dosage errors. Voltaren Retard allows the use of a maximum daily dose of 150 mg in a balanced regimen twice a day. In rheumatic diseases, the anti-inflammatory and analgesic properties of Voltaren Retard provide a significant reduction in the severity of pain (both at rest and during movement), morning stiffness, swelling of the joints and, thus, improving the functional state of the patient. In the presence of inflammation caused by injury or surgery, Voltaren Retard quickly eliminates both spontaneous pain and pain during movement, and also reduces inflammatory tissue swelling and swelling at the site of the surgical wound. In clinical studies, it was found that Voltaren Retard also exhibits a strong analgesic effect in moderate and severe pain of non-rheumatic origin. Pharmacokinetics. Analysis of unchanged diclofenac and its hydroxylated metabolites excreted in urine showed that the amount of diclofenac released and absorbed was the same as when taking an equivalent dose of diclofenac sodium in the form of enteric-coated tablets. However, the systemic bioavailability of diclofenac (released from Voltaren Retard) is, on average, 82% of that after oral administration of Voltaren enteric tablets at the same dose. Due to the prolonged release of the active substance from Voltaren Retard, the maximum drug concentrations achieved in plasma are lower than after taking enteric-coated tablets. The average peak concentration of 0.4 mcg/ml or 0.5 mcg/ml (1.25 or 1.6 μmol/L) is achieved, on average, 4 hours after taking the 75 mg or 100 mg tablet. Eating does not clinically affect the absorption and systemic bioavailability of Voltaren Retard. On the other hand, a mean plasma concentration of 13 ng/mL (40 nmol/L) may be observed 24 hours (16 hours) after taking Voltaren Retard 75 mg. The amount of absorbed active substance is linearly dependent on the dose of the drug. Since about half of diclofenac is metabolized during the first passage through the liver (“first pass effect”), the area under the concentration/time curve (AUC) after taking Voltaren Retard tablet is almost half that of parenteral administration of an equivalent dose of the drug. After repeated administration of Voltaren Retard, the pharmacokinetics do not change. If the recommended intervals between doses of the drug are observed, no accumulation is observed. The corresponding concentrations are 22 ng/ml or 25 ng/ml (70 nmol/l or 80 nmol/l) when taking Voltaren Retard 75 mg 2 times a day. Pharmacokinetic behavior does not change after repeated use. There is no accumulation provided that the recommended intervals between applications are observed. Distribution. 99.7% of diclofenac is bound to serum proteins, mainly albumin (99.4%). The 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 plasma. The apparent half-life from synovial fluid is 3-6 hours. 2 hours after reaching maximum plasma concentrations, the concentration of the active substance in the synovial fluid is higher than in the plasma, and remains higher for 12 hours. Diclofenac was detected at low concentrations (100 ng/ml) in the breast milk of one breastfeeding woman. The amount consumed by the infant through breast milk is equivalent to a dose of 0.03 mg/kg/day. Biotransformation. Biotransformation of diclofenac occurs partly through glucuronidation of the unchanged molecule, but mainly through 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 conjugated with glucuronic acid. Two of these phenolic metabolites are pharmacologically active, but to a significantly lesser extent than diclofenac. Excretion. The total systemic plasma clearance of diclofenac is 263 ± 56 ml/min. The terminal half-life in plasma is 1-2 hours. The half-life of 4 metabolites, including 2 pharmacologically active ones, is also short and amounts to 1-3 hours. One of the metabolites, 3′-hydroxy-4′-methoxydiclofenac, has a longer half-life. However, this metabolite is completely inactive pharmacologically. About 60% of the applied dose of the drug is excreted in the urine in the form of glucuronic conjugates of the intact molecule of the active substance, as well as in the form of metabolites, most of which are also converted into glucuronic conjugates. Less than 1% of diclofenac is excreted unchanged. The remainder of the applied dose of the drug is excreted in the form of metabolites through bile and feces. Linearity. The amount absorbed is linearly related to the dosage. Special groups of patents. No age-related differences in drug absorption, metabolism or excretion were identified. However, in several elderly patients, a 15-minute intravenous infusion resulted in plasma concentrations 50% higher than expected based on data obtained in young healthy subjects. In patients with impaired renal function, no accumulation of unchanged active substance was detected based on single-dose kinetics data using the usual dosage regimen. When creatinine clearance is less than 10 ml/min, the calculated equilibrium levels of hydroxymetabolites in blood plasma are approximately 4 times higher than in healthy individuals. Metabolites are finally excreted in bile. In patients with chronic hepatitis or uncompensated cirrhosis, the kinetics and metabolism of diclofenac are the same as in patients without liver disease.
Pharmaceutical characteristics
Basic physical and chemical properties: tablets are pale pink, triangular, biconvex, with beveled edges, with the inscription “ID” on one side and “CG” on the other in black ink.
Best before date
3 years. Do not use after the expiration date stated on the package.
Storage conditions
Store at a temperature not exceeding 30°C, in the original packaging to protect from moisture. Keep out of the reach of children.
Package
10 tablets in a blister, 2 blisters in a cardboard box along with an insert.
Conditions for dispensing from pharmacies
On prescription.
Buy Voltaren retard tablet p/o extended d-i 75 mg in blister pack No. 10x2 in the pharmacy
Price for Voltaren retard tablet p/o extended d-i 75 mg in sheets in pack No. 10x2
Instructions for use for Voltaren retard tablet p/o extended d-ya 75 mg in sheets in pack No. 10x2
Pharmacological properties of the drug Voltaren emulgel
Diclofenac is an NSAID with pronounced antirheumatic, anti-inflammatory, analgesic and antipyretic effects. The main mechanism of its action is to suppress the biosynthesis of prostaglandins. The use of Voltaren Emulgel for inflammation caused by injury or rheumatic disease leads to a reduction in tissue swelling, pain and promotes rapid restoration of the functions of damaged joints, ligaments, tendons and muscles. Thanks to its water-alcohol base, the drug also has a local anesthetic and cooling effect. The amount of diclofenac resorbed through the skin is proportional to the area to which it is applied, and also depends on the total dose of the drug and the degree of skin hydration. After topical application of 2.5 g of Voltaren Emulgel to a skin surface area of 500 cm2, the absorption of diclofenac is approximately 6%. The use of an occlusive dressing for 10 hours leads to a threefold increase in the resorption of diclofenac. After applying Voltaren Emulgel to the skin of the joints of the hand and knee, diclofenac is determined in the blood plasma (its maximum concentration is approximately 100 times lower than after oral administration), synovial membrane and synovial fluid. The binding of diclofenac to plasma proteins (mainly albumin) is 99.7%. Diclofenac is metabolized primarily by hydroxylation to form several derivatives, two of which are pharmacologically active, but to a significantly lesser extent than diclofenac. Diclofenac and its metabolites are excreted primarily in the urine. The total systemic clearance of diclofenac in blood plasma averages 263±56 ml/min, and the final half-life is 1–3 hours. In patients with kidney disease, accumulation of diclofenac and its metabolites was not observed. In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetics and metabolism of diclofenac do not change.