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 tablets 50 mg No. 20
Compound
1 enteric-coated tablet contains: active ingredient: diclofenac sodium 25.00/50.00 mg;
excipients: colloidal silicon dioxide anhydrous 6.0/6.0 mg, microcrystalline cellulose 10.0/10.0 mg, lactose monohydrate 16.0/25.0 mg, magnesium stearate 1.0/1.5 mg, starch corn 50.0/74.5 mg, povidone K 30 2.0/3.0 mg, sodium carboxymethyl starch 20.0/20.0 mg; shell: hypromellose 1.90/3.29 mg, macrogol glyceryl hydroxystearate 0.09/0.15 mg, iron oxide red dye -/0.02 mg, iron oxide yellow dye 0.18/0.31 mg, talc 1, 70/2.92 mg, titanium dioxide 0.13/0.31 mg;
enteric coating - methacrylic acid and ethyl acrylate copolymer [1:1] 8.28/12.42 mg, macrogol 8000 0.83/1.24 mg, silicone antifoam emulsion SE 2 0.06/0.10 mg, talc 0, 83/1.24 mg;
colored shell - hypromellose 0.95/1.41 mg, macrogol glyceryl hydroxystearate 0.04/0.07 mg, red iron oxide dye -/0.01 mg, yellow iron oxide dye 0.09/0.13 mg, talc 0 .85/1.25 mg, titanium dioxide 0.07/0.13 mg.
Indications for use
— Inflammatory and degenerative diseases of the musculoskeletal system, including: rheumatoid, juvenile chronic arthritis; ankylosing spondylitis and other spondyloarthropathy; osteoarthritis; gouty arthritis; bursitis, tendovaginitis. — Pain syndromes from the spine (lumbago, sciatica, ossalgia, neuralgia, myalgia, arthralgia, radiculitis). — Post-traumatic and postoperative pain syndrome, accompanied by inflammation, for example, in dentistry and orthopedics. - Algomenorrhea; inflammatory processes in the pelvis, including adnexitis. — Infectious and inflammatory diseases of the ENT organs with severe pain syndrome (as part of complex therapy): pharyngitis, tonsillitis, otitis media. Isolated fever is not an indication for the use of the drug. The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.
Contraindications
— Exacerbation of gastric and duodenal ulcers, bleeding from the gastrointestinal tract (GIT), perforation of the GIT organs. - Hypersensitivity to diclofenac and any other components of the drug. - III trimester of pregnancy. — Like other NSAIDs, Voltaren® is contraindicated in patients with a complete or incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including a history). — Severe liver dysfunction, renal failure (GFR less than 15 ml/min/1.73 m2), chronic heart failure (functional class IV according to the NYHA classification). — Conditions accompanied by a risk of bleeding. - Confirmed hyperkalemia. — Coronary artery bypass grafting (perioperative period). - Inflammatory bowel diseases (Crohn's disease, ulcerative colitis) in the acute phase. — Active liver diseases. - Breastfeeding period. — Hereditary severe lactose intolerance, lactase deficiency and glucose-galactose malabsorption (since the dosage form contains lactose). — The use of the drug Voltaren, enteric-coated tablets, 25 mg, is not recommended in children under 6 years of age. — The use of Voltaren, enteric-coated tablets, 50 mg, is not recommended in children under 14 years of age.
With caution: When using the drug Voltaren and other NSAIDs, it is necessary to exercise caution and carefully monitor patients with symptoms/signs indicating lesions/diseases of the gastrointestinal tract or with anamnestic data suggesting ulcerative lesions of the stomach or intestines, bleeding or perforation; patients with a history of Helicobacter pylori infection, ulcerative colitis, Crohn's disease, a history of liver dysfunction, and in patients with complaints suggesting gastrointestinal diseases. The risk of developing gastrointestinal bleeding increases with increasing doses of NSAIDs or with a history of ulcerative lesions, 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 glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel, acetylsalicylic acid) or selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline). Caution is required when using the drug Voltaren® in patients with mild to moderate liver function, as well as in patients with hepatic porphyria, since 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), chronic obstructive pulmonary disease, 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 coronary heart disease, cerebrovascular diseases, compensated heart failure, peripheral vascular disease), impaired renal function, including chronic renal failure (GFR 15-60 ml/min/1.73 m2 ), dyslipidemia/hyperlipidemia, diabetes mellitus, hypertension, when treating patients who smoke or drink alcohol, when treating elderly patients, patients receiving diuretics or other drugs that affect renal function, as well as patients with a significant decrease in circulating blood volume ( BCC) of any etiology, for example, in the periods before and after major surgical interventions. Voltaren® should be used with caution in patients with defects in the hemostatic system. Caution should be exercised when using Voltaren® 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 elderly people who are weakened or have low body weight; in patients in this category, it is recommended to use the drug in the minimum effective dose.
Directions for use and doses
The dose of the drug is selected individually, and in order to reduce the risk of side effects, it is recommended to use the minimum effective dose, if possible, with the shortest possible treatment period in accordance with the purpose of treatment and the patient’s condition. The tablets should be swallowed whole with liquid, preferably before meals. Do not split or chew the tablets. Adults. 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 per day is sufficient.
The daily dose should be divided into several doses. To relieve night pain or morning stiffness, in addition to taking the drug during the day, use diclofenac in the form of rectal suppositories before bedtime; in this case, the total daily dose should not exceed 150 mg. For 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 200 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 children aged 6 years and older, the drug Voltaren in the form of enteric-coated tablets, 25 mg, is used at the rate of 0.5-2 mg/kg body weight per day (the daily dose, depending on the severity of the disease, should be divided into 2- 3 single doses). In children under 6 years of age, the drug should be used in a different dosage form. For the treatment of rheumatoid arthritis, the daily dose can be increased to a maximum of 3 mg/kg (in several doses). The maximum daily dose should not exceed 150 mg.
Elderly patients (≥65 years) Initial dosage adjustment is generally not required in patients aged 65 years and older. However, based on general medical considerations, caution should be exercised in frail elderly patients or patients with low body weight. 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 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 safety studies of the drug in patients in 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 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.
Storage conditions
Store in a dry place, at a temperature not exceeding 30°C. Keep out of the reach of children.
Best before date
3 years. Do not use after expiration date.
special instructions
Damage to the gastrointestinal tract When using diclofenac, like other NSAIDs, phenomena such as bleeding or ulceration/perforation of the gastrointestinal tract, in some cases with fatal outcome, were observed. These phenomena may occur at any time when using these drugs with or without previous symptoms or 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 in patients with ulcerative lesions of the gastrointestinal tract, especially those complicated by bleeding or perforation in history, as well as in elderly patients, the drug should be used in the minimum effective dose. In patients with an increased risk of developing gastrointestinal complications, as well as in patients receiving therapy with low doses of acetylsalicylic acid, gastroprotectors (proton pump inhibitors or misoprostol) or other medications should be used during drug therapy to reduce the risk of undesirable 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 with bronchial asthma, seasonal allergic rhinitis, nasal polyps, chronic obstructive pulmonary disease 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 (skin rash and 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 a patient receiving Voltaren develops the first signs of a skin rash, damage to the mucous membranes or other symptoms of hypersensitivity, the drug should be discontinued. In rare cases, when using Voltaren, like other NSAIDs, anaphylactic/anaphylactoid reactions may develop in patients who have not previously received diclofenac.
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, monitoring of liver function is indicated as a precautionary measure during long-term therapy with the drug. If liver dysfunction persists and progresses or signs of liver disease or other symptoms occur (for example, eosinophilia, rash, etc.), 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, elderly patients, patients receiving diuretics or other drugs that affect renal function, as well as in patients with a significant decrease in extracellular volume. fluids of any etiology, for example, during the period before and after major surgical interventions. After cessation of drug therapy, normalization of renal function indicators to initial values is usually observed.
Cardiovascular effects Therapy with NSAIDs, including diclofenac, particularly long-term and high-dose therapy, may be associated with a small increased 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. Impact on the hematopoietic system The drug Voltaren can temporarily inhibit platelet aggregation, therefore, in patients with hemostasis disorders, it is necessary to carefully monitor the 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 can complicate the diagnosis of infectious processes. Use simultaneously with other NSAIDs Voltaren should not be used simultaneously with other NSAIDs, including selective COX-2 inhibitors, due to the risk of adverse events.
Description
Tablets 25 mg: round, biconvex, yellow, beveled. “CG” is embossed on one side of the tablet and “BZ” on the other side.
Tablets 50 mg: round, biconvex, light brown, beveled. The tablet has “CG” stamped on one side and “GT” on the other side.
Conditions for dispensing from pharmacies
On prescription
Dosage form
Enteric-coated tablets.
Manufacturer and organization accepting consumer complaints
Novartis Pharma, LLC
Pharmacodynamics
The drug 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 in studies, 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 when used in humans does not inhibit the biosynthesis of proteoglycans in cartilage tissue.
In rheumatic diseases, the anti-inflammatory and analgesic properties of the drug provide a clinical effect, characterized by a significant decrease in the severity of such manifestations as pain at rest and with movement, morning stiffness and swelling of the joints, as well as an improvement in the functional state.
In case of post-traumatic and postoperative inflammatory phenomena, diclofenac quickly relieves pain (both at rest and during movement), reduces inflammatory swelling and swelling of the postoperative wound.
When using the drug, a pronounced analgesic effect was observed for moderate and severe pain of non-rheumatic origin. It has also been established that diclofenac is able to reduce pain and reduce blood loss during primary dysmenorrhea.
Side effects
Below are the adverse events (AEs) that were identified during clinical trials, as well as when using diclofenac in clinical practice. To assess the frequency of AEs, the following criteria were used: “very often” (?1/10); “often” (?1/100, <1/10); “infrequently” (?1/1000. <1/100); “rarely” (?1/10,000, <1/1000); “very rare” (<1/10,000). AEs are grouped in accordance with the system-organ class of the medical dictionary for regulatory activities MedDRA; within each class, AEs are listed in descending order of frequency of occurrence; within each group, allocated by frequency of occurrence, AEs are distributed in decreasing order of their importance.
Disorders of the blood and lymphatic system: very rarely - thrombocytopenia, leukopenia, hemolytic anemia, aplastic anemia, agranulocytosis.
Immune system disorders: rarely - hypersensitivity, anaphylactic/anaphylactoid reactions, including decreased blood pressure (BP) and shock; very rarely - angioedema (including facial swelling).
Mental disorders: very rarely - disorientation, depression, insomnia, nightmares, irritability, mental disorders.
Nervous system disorders: often - headache, dizziness; rarely - drowsiness; very rarely - sensory disturbances, including paresthesia, memory disorders, tremors, convulsions, anxiety, acute cerebrovascular accidents, aseptic meningitis.
Visual disturbances: very rarely - visual disturbances (blurred vision), diplopia.
Hearing and labyrinthine disorders: often - vertigo; very rarely - hearing impairment, tinnitus.
Cardiac disorders: uncommon - myocardial infarction, heart failure, palpitations, chest pain. Vascular disorders: very rarely - increased blood pressure, vasculitis.
Disorders of the respiratory system, chest and mediastinal organs: rarely - bronchial asthma (including shortness of breath); very rarely - pneumonitis. Gastrointestinal disorders: often - abdominal pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, loss of appetite; rarely - gastritis, gastrointestinal bleeding, vomiting blood, melena, diarrhea mixed with blood, gastric and intestinal ulcers (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. Disorders of the liver and biliary tract: often - increased activity of aminotransferases in the blood plasma; rarely - hepatitis, jaundice, liver dysfunction; 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, itching, alopecia, photosensitivity reactions, purpura, Henoch-Schönlein purpura. Renal and urinary tract disorders: very rarely - acute kidney injury (acute renal failure), hematuria, proteinuria, tubulointerstitial nephritis, nephrotic syndrome, papillary necrosis. General disorders and disorders at the injection site: rarely - swelling.
Cardiovascular disorders: Clinical trial data indicate a slight increase in the risk of cardiovascular thrombotic complications (for example, myocardial infarction), especially with long-term use of diclofenac in high doses (daily dose 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 upon discontinuation of use. A possible mechanism for the development of such disorders is inhibition of the synthesis of prostaglandins and other related substances, which alters the regulation of retinal blood flow, which is manifested by potential visual disturbances. If such symptoms develop during diclofenac therapy, an ophthalmological examination should be considered to exclude any other causes. If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, tell your doctor.
Use during pregnancy and breastfeeding
There is insufficient data on the safety of diclofenac in pregnant women, and therefore Voltaren should be used 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. The drug Voltaren, like other NSAIDs (prostaglandin synthesis inhibitors), is contraindicated in the last 3 months of pregnancy (possible suppression of uterine contractility, impaired renal function in the fetus with subsequent oligohydramnios (oligohydroamnion) and/or 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 used during breastfeeding to avoid undesirable effects on the baby. If it is necessary to use the drug in a woman during this period, breastfeeding is stopped. Since Voltaren, like other NSAIDs, can have a negative effect on fertility, women planning pregnancy are not recommended to take the drug. In patients undergoing examination and treatment for infertility, the drug should be discontinued.
Interaction
Identified interactions. Inhibitors of the CYP2C9 isoenzyme. Caution should be exercised when using diclofenac concomitantly with CYP2C9 inhibitors (such as voriconazole) due to the possible increase in diclofenac serum concentrations and exposure. Lithium, digoxin. Diclofenac may increase lithium levels and digoxin concentrations in blood plasma. It is recommended to monitor lithium levels and digoxin concentrations in the blood serum. Diuretics and antihypertensive drugs.
When used simultaneously with diuretics and antihypertensive drugs (for example, beta-blockers, angiotensin-converting enzyme inhibitors - ACE inhibitors), diclofenac may reduce their hypotensive effect. In connection with the above, in patients, especially elderly patients, when diclofenac is used concomitantly with diuretics or antihypertensive drugs, blood pressure should be regularly measured, renal function and hydration levels monitored (due to an increased risk of nephrotoxicity).
Cyclosporine and tacrolimus. The effect of diclofenac on the activity of prostaglandins in the kidneys may enhance the nephrotoxicity of cyclosporine and tacrolimus. In connection with the above, the dose of diclofenac in patients receiving cyclosporine or tacrolimus should be lower than in patients not receiving these drugs. Drugs that can cause hyperkalemia. The simultaneous use of diclofenac with potassium-sparing diuretics, cyclosporine, tacrolimus and trimethoprim may lead to an increase in the level of potassium in the blood plasma (in the case of such simultaneous use, this indicator should be monitored frequently). Antibacterial agents are quinolone derivatives. There are isolated reports of the development of seizures in patients receiving concomitant quinolone derivatives and diclofenac.
Potential interactions between NSAIDs and glucocorticosteroids. The simultaneous systemic use of diclofenac and other systemic NSAIDs or glucocorticosteroids may increase the incidence of adverse events (in particular, from the gastrointestinal tract). Anticoagulants and antiplatelet agents. It is necessary to use diclofenac with caution with drugs of these groups 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. Patients receiving concomitant treatment with these drugs should be carefully monitored. Selective serotonin reuptake inhibitors.
Concomitant use of diclofenac with selective serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding. Hypoglycemic drugs. Clinical studies have 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. In connection with the above, during the simultaneous use of diclofenac and hypoglycemic drugs, it is recommended to monitor the concentration of glucose in the blood. There have been isolated reports of the development of metabolic acidosis with the simultaneous use of diclofenac with metformin, especially in patients with impaired renal function. Methotrexate. Caution should be exercised when using diclofenac less than 24 hours before or 24 hours after taking methotrexate, since in such cases the concentration of methotrexate in the blood may increase and its toxic effect may increase. Phenytoin. When using phenytoin and diclofenac simultaneously, it is necessary to monitor the concentration of phenytoin in the blood plasma due to a possible increase in its systemic exposure.
Inducers of the CYP2C9 isoenzyme. Caution should be exercised when using diclofenac concomitantly with inducers of the CYP2C9 isoenzyme (such as rifampicin), as this may lead to a significant decrease in the concentration of diclofenac in the blood plasma and a decrease in its exposure.
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 to remove NSAIDs, incl. diclofenac from the body are ineffective, since the active substances of these drugs are largely bound to blood plasma proteins and undergo intensive metabolism. In case of a life-threatening overdose when taking the drug orally, in order to quickly prevent the absorption of diclofenac, gastric lavage should be performed and activated charcoal should be prescribed.
Impact on the ability to drive vehicles and operate machinery
Patients who experience visual disturbances, dizziness, drowsiness, vertigo or other disorders of the central nervous system while using the drug Voltaren should not drive vehicles or operate machinery.
Voltaren Emulgel gel for external use 2% 50g
Compound
Active substance: diclofenac sodium - 2 g.
Excipients: carbomers * - 1.1-1.7 g, cetostearomacrogol - 2 g, cocoyl caprylocaprate - 2.5 g, diethylamine * - 0.89-1.37 g, isopropanol - 17.5 g, liquid paraffin - 2.5 g, oleyl alcohol - 0.75 g, eucalyptus flavor - 0.1 g, propylene glycol - 5 g, butylated hydroxytoluene - 0.02 g, purified water* - 64.22-65.32 g.
* when using different production equipment and different batch sizes (1000 kg and 2500 kg), the amounts of carbomers, diethyleneamine and purified water may be slightly adjusted within the indicated figures.
Pharmacokinetics
Suction
The amount of diclofenac absorbed through the skin is proportional to the area of the treated surface and depends on both the total dose of the drug applied and the degree of skin hydration. After applying Voltaren® Emulgel®, gel for external use 2% (2 applications per day) to a skin surface area of 400 cm2, the concentration of the active substance in plasma corresponds to its concentration when using 1% diclofenac gel (4 applications per day). On day 7, the relative bioavailability of the drug (AUC ratio) is 4.5% (for an equivalent dose of diclofenac sodium salt). When wearing a moisture-permeable dressing, suction did not change.
Distribution
When applying the drug to the area of the affected joint, the concentration of diclofenac in plasma, synovial membrane and synovial fluid was determined. Cmax in plasma was approximately 100 times lower than after oral administration of the same amount of diclofenac.
The binding of diclofenac to plasma proteins is 99.7%, mainly with albumin (99.4%).
Diclofenac is preferentially distributed and retained deep in tissues prone to inflammation, such as joints, where its concentration is 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, which leads to the formation of several phenolic metabolites, most of which are converted to glucuronide conjugates. Two phenolic metabolites are biologically active, but to a much lesser extent than diclofenac.
Removal
The total systemic plasma clearance of diclofenac is 263±56 ml/min.
The final T1/2 is 1-2 hours. The T1/2 of metabolites, including two pharmacologically active ones, is also short-lived and is 1-3 hours. One of the metabolites (3′-hydroxy-4′-methoxydiclofenac) has a longer T1/2, however, this metabolite is completely inactive. Most of diclofenac and its metabolites are excreted in the urine.
Indications for use
- back pain due to inflammatory and degenerative diseases of the spine (sciatica, osteoarthritis, lumbago, sciatica);
- pain in the joints (including finger joints, knees) due to rheumatoid arthritis, 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, wrist syndrome).
Contraindications
- hypersensitivity to diclofenac or other components of the drug;
- tendency to develop attacks of bronchial asthma, skin rashes or acute rhinitis when using acetylsalicylic acid or other NSAIDs;
- violation of the integrity of the skin at the intended site of application;
- III trimester of pregnancy;
- lactation period (breastfeeding);
- children's age up to 12 years.
Carefully
the drug should be prescribed for hepatic porphyria (in the acute phase), erosive and ulcerative lesions of the gastrointestinal tract, severe liver and kidney dysfunction, chronic heart failure, bronchial asthma, as well as in the first and second trimesters of pregnancy and elderly patients.
Directions for use and doses
For adults and children over 12 years of age, the drug is applied to the skin 2 times a day (every 12 hours: preferably morning and evening), lightly rubbing into the skin.
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) - is enough to treat an area of 400-800 cm2.
If your hands are not the area where pain is localized, then after applying the drug they should be washed.
The duration of treatment depends on the indications and the observed effect. The gel should not be used for more than 14 days for post-traumatic inflammation and rheumatic diseases of soft tissues without a doctor’s recommendation. If after 7 days of use the therapeutic effect is not observed or the condition worsens, the patient should consult a doctor.
To remove the protective membrane, use the screw cap as a key (the recess with protrusions 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.
The tubes can have either a regular cap (round shape) or an innovative cap (triangular shape), which is especially convenient for use when the mobility of the hand joints is limited due to osteoarthritis or other joint diseases or injuries.
Storage conditions
Store out of the reach of children at a temperature not exceeding 30 °C.
Best before date
3 years. The drug should not be used after the expiration date indicated on the package.
special instructions
Voltaren® Emulgel® should be applied only to intact skin, avoiding contact with open wounds.
The drug should not come into contact with the eyes and mucous membranes.
After applying the gel for external use 1%, you should not apply an occlusive dressing.
After applying the gel for external use 2%, a bandage may be applied, but airtight occlusive dressings should not be applied.
If a skin rash develops after application of the drug, its use should be discontinued.
This medicine contains propylene glycol, which may cause mild local irritation in some people. It also contains butylated hydroxytoluene, which may cause local skin reactions (eg contact dermatitis) or irritation of the eyes and mucous membranes.
Description
NSAIDs for external use.
Dosage form
Gel for external use 2% is homogeneous, creamy, white to white with a yellowish tint.
Use in children
Contraindicated: children under 12 years of age.
Pharmacodynamics
NSAIDs for external use. Diclofenac has a pronounced analgesic, anti-inflammatory and antipyretic effect. By indiscriminately inhibiting COX-1 and COX-2, it disrupts the metabolism of arachidonic acid. Voltaren® Emulgel® is used to eliminate pain and inflammation in joints, muscles and ligaments of traumatic or rheumatic origin, helping to reduce pain and swelling associated with the inflammatory process, increasing joint mobility.
Thanks to its hydroalcoholic base, Voltaren® Emulgel® has a calming and cooling effect.
Side effects
Determination of the frequency of adverse reactions: very often (≥1/10), often (≥1/100, <1/10), infrequently (≥1/1000, <1/100), rarely (≥1/10,000, <1 /1000), very rarely (<1/10,000), including isolated reports.
Infectious and parasitic diseases: very rarely: pustular rash.
From the immune system: very rarely - hypersensitivity reactions (including urticaria), angioedema.
From the respiratory system: very rarely - asthma.
From the skin and subcutaneous tissues: often - dermatitis (including contact dermatitis), rash, erythema, eczema, itching; rarely - bullous dermatitis; very rarely - photosensitivity reactions.
If any of the above adverse reactions worsen, or the patient notices any other adverse reactions, the doctor should be informed.
Use during pregnancy and breastfeeding
Due to the lack of data on the use of the drug Voltaren® Emulgel® during pregnancy, the use of the drug in the first and second trimesters 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 release of the active substance of Voltaren® Emulgel® into breast milk, the drug is not recommended for use during breastfeeding. 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 effect of the drug on fertility.
Interaction
Voltaren® Emulgel® may enhance the effect of drugs that cause photosensitivity.
Clinically significant interactions with other drugs have not been described.
Overdose
Due to the extremely low systemic absorption when applying the gel, overdose is unlikely.
Symptoms: accidental ingestion may cause systemic adverse reactions.
Treatment of overdose due to accidental ingestion: gastric lavage, induction of vomiting, activated charcoal, symptomatic therapy. Dialysis and forced diuresis are not effective due to the high degree of binding of diclofenac to plasma proteins (about 99%).
Impact on the ability to drive vehicles and operate machinery
Does not affect.
