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 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 tablets p/o prolonged action 75 mg No. 10x2 in the pharmacy
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Instructions for use for Voltaren retard tablets p/o prolonged action 75 mg No. 10x2
Voltaren solution for intramuscular administration 25 mg/ml ampoule 3 ml N5
Registration Certificate Holder
NOVARTIS PHARMA (Switzerland)
Dosage form
Medicine - Voltaren®
Description
Solution for intramuscular administration
from colorless to light yellow.
1 ml
1 amp.
diclofenac sodium 25 mg 75 mg
Excipients
: mannitol - 18 mg, propylene glycol - 600 mg, benzyl alcohol - 120 mg, sodium disulfite - 2 mg, sodium hydroxide - up to pH 7.8-8.0, liquid water - up to 3 ml.
3 ml - colorless glass ampoules with a break point or break ring (5) - cardboard packs with an insert with cells for ampoules.
Indications
Inflammatory and degenerative diseases of the musculoskeletal system, incl. rheumatoid, juvenile, chronic arthritis; ankylosing spondylitis and other spondyloarthropathy; osteoarthritis; gouty arthritis; bursitis, tendovaginitis; pain syndrome from the spine (lumbago, sciatica, ossalgia, neuralgia, myalgia, arthralgia, radiculitis); post-traumatic postoperative pain syndrome accompanied by inflammation (for example, in dentistry and orthopedics); algodismenorrhea; 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, and does not affect the progression of the disease.
Contraindications for use
Hypersensitivity to diclofenac and excipients of the drug used; “aspirin triad” (attacks of bronchial asthma, urticaria and acute rhinitis when taking acetylsalicylic acid or other NSAIDs); erosive and ulcerative lesions of the gastrointestinal tract in the acute phase; proctitis (only for suppositories); pregnancy (for intramuscular administration); III trimester of pregnancy (for oral and rectal administration); children and adolescents up to 18 years of age (for intramuscular administration and for long-acting dosage forms).
Carefully :
suspicion of gastrointestinal disease; indications in the anamnesis of bleeding from the gastrointestinal tract and perforation of the ulcer (especially in elderly patients), Helicobacter pylori infections, ulcerative colitis, Crohn's disease, dysfunction; mild to moderate liver dysfunction, hepatic porphyria (diclofenac can provoke attacks of porphyria); in patients with bronchial asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (including polyps in the nasal cavity), COPD, chronic infectious diseases of the respiratory tract (especially those associated with allergic rhinitis-like symptoms); cardiovascular diseases (including coronary artery disease, cerebrovascular diseases, compensated heart failure, peripheral vascular diseases); impaired renal function, including chronic renal failure (creatinine clearance 30-60 ml/min); dyslipidemia/hyperlipilemia; diabetes; arterial hypertension; a significant decrease in blood volume of any etiology (for example, in the periods before and after major surgical interventions); violation of the hemostasis system; risk of developing thrombosis (including myocardial infarction and stroke); elderly patients, especially those who are weakened or have low body weight (diclofenac should be used in the minimum effective dose); in patients receiving drugs that increase the risk of gastrointestinal bleeding, including systemic corticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel, acetylsalicylic acid), selective inhibitors serotonin reuptake (including citalopram, fluoxetine, paroxetine, sertraline); simultaneous treatment with diuretics or other drugs that can impair renal function; when treating smoking patients or patients who abuse alcohol; when administered intramuscularly to patients with bronchial asthma due to the risk of exacerbation of the disease (since sodium bisulfite, which is contained in some dosage forms for injection, can cause severe hypersensitivity reactions).
pharmachologic effect
NSAID, phenylacetic acid derivative. It has a pronounced anti-inflammatory, analgesic and moderate antipyretic effect. The mechanism of action is associated with inhibition of the activity of COX, the main enzyme in the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play an important role in the pathogenesis of inflammation, pain and fever. The analgesic effect is due to two mechanisms: peripheral (indirectly, through suppression of prostaglandin synthesis) and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system).
In vitro, at concentrations equivalent to those achieved when treating patients, it does not inhibit the biosynthesis of cartilage tissue proteoglycans.
For rheumatic diseases, it reduces pain in the joints at rest and during movement, as well as morning stiffness and swelling of the joints, and helps to increase range of motion. Reduces post-traumatic and postoperative pain, as well as inflammatory swelling.
In case of post-traumatic and postoperative inflammatory phenomena, it quickly relieves pain (arising both at rest and during movement), reduces inflammatory swelling and swelling of the postoperative wound.
Suppresses platelet aggregation. With long-term use it has a desensitizing effect.
Drug interactions
Potent CYP2C9 inhibitors -
When diclofenac is co-administered with strong CYP2C9 inhibitors (such as voriconazole), it is possible to increase the concentration of diclofenac in the blood serum and enhance the systemic effect caused by inhibition of the metabolism of diclofenac.
Lithium, digoxin -
it is possible to increase the concentration of lithium and digoxin in plasma. 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.
Cyclosporine -
the effect of diclofenac on the activity of prostate glandins in the kidneys may enhance the nephrotoxicity of 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.
NSAIDs and GCS -
with 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
— an increased risk of bleeding cannot be excluded when diclofenac is used simultaneously with drugs from these groups.
Selective serotonin reuptake inhibitors
- there may be an increased risk of gastrointestinal bleeding.
Hypoglycemic drugs -
Cases of both hypoglycemia and hyperglycemia cannot be excluded, which necessitated the need to change the dose of hypoglycemic drugs during the use of diclofenac.
Methotrexate -
when diclofenac is used within 24 hours before or within 24 hours after taking methotrexate, the concentration of methotrexate in the blood may increase and its toxic effect may increase.
Phenytoin -
the effect of phenytoin may be enhanced.
Dosage regimen
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 adolescents 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.
Side effect
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 rare (<1/10,000).
From the digestive system:
often - abdominal pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, decreased appetite, anorexia, increased aminotransferase activity in the blood serum; rarely - gastritis, gastrointestinal bleeding, vomiting blood, melena, diarrhea mixed with blood, stomach and intestinal ulcers (with or without bleeding or perforation), hepatitis, jaundice, liver dysfunction; very rarely - stomatitis, glossitis, damage to the esophagus, the occurrence of diaphragm-like strictures in the intestine, colitis (nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease), constipation, pancreatitis, fulminant hepatitis, liver necrosis, liver failure.
From the nervous system:
often - headache, dizziness; rarely - drowsiness; very rarely - sensory disturbances, including paresthesia, memory disorders, tremors, convulsions, anxiety, acute cerebrovascular accidents, aseptic meningitis; very rarely - disorientation, depression, insomnia, nightmares, irritability, mental disorders.
From the senses:
often - vertigo; very rarely - visual impairment (blurred vision), diplopia, hearing impairment, tinnitus, dysgeusia.
Dermatological reactions:
often - skin rash; rarely - urticaria; very rarely - bullous rashes, eczema, erythema, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome (toxic epidermal necrolysis), exfoliative dermatitis, itching, hair loss, photosensitivity reactions; purpura, Henoch-Schönlein purpura.
From the genitourinary system:
very rarely - acute renal failure, hematuria, proteinuria, tubulointerstitial nephritis, nephrotic syndrome, papillary necrosis.
From
the hematopoietic system:
very rarely - thrombocytopenia, leukopenia, hemolytic anemia, aplastic anemia, agranulocytosis.
Allergic reactions:
rarely - hypersensitivity, anaphylactic/anaphylactoid reactions, including decreased blood pressure and shock; very rarely - angioedema (including facial swelling).
From the cardiovascular system:
very rarely - palpitations, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.
There is evidence of a slight increase in the risk of developing cardiovascular thrombotic complications (for example, myocardial infarction), especially with long-term use of diclofenac in high doses (daily dose more than 150 mg). From the respiratory system:
rarely - asthma (including shortness of breath); very rarely - pneumonitis.
General reactions:
rarely - swelling.
special instructions
Use with extreme caution in patients with a history of liver, kidney, gastrointestinal diseases, dyspeptic symptoms, bronchial asthma, arterial hypertension, heart failure, immediately after major surgical interventions, as well as in elderly patients.
If there is a history of allergic reactions to NSAIDs and sulfites, diclofenac is used only in emergency cases. During treatment, systematic monitoring of liver and kidney function and peripheral blood patterns is necessary.
Rectal use is not recommended in patients with diseases of the anorectal region or a history of anorectal bleeding. It should be used externally only on undamaged areas of the skin.
Avoid contact of diclofenac with the eyes (except for eye drops) or mucous membranes. Patients using contact lenses should use eye drops no earlier than 5 minutes after removing the lenses.
Not recommended for use in children under 6 years of age.
During treatment with dosage forms for systemic use, alcohol consumption is not recommended.
Effect on the ability to drive vehicles and machinery
During the treatment period, the speed of psychomotor reactions may decrease. If your vision becomes blurred after using eye drops, you should not drive a car or engage in other potentially hazardous activities.
Use during pregnancy and breastfeeding
Restrictions during pregnancy - Contraindicated. Restrictions when breastfeeding - Contraindicated.
There is insufficient data on the safety of diclofenac in pregnant women. Therefore, administration in the first and second trimesters of pregnancy is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. Diclofenac (like other inhibitors of prostaglandin synthesis) is contraindicated in the third trimester of pregnancy (possible suppression of uterine contractility and premature closure of the ductus arteriosus in the fetus).
Despite the fact that diclofenac is excreted in breast milk in small quantities, use during lactation (breastfeeding) is not recommended. If use is necessary during lactation, breastfeeding should be discontinued.
Since diclofenac (like other NSAIDs) may have a negative effect on fertility, use in women planning pregnancy is not recommended.
For patients undergoing examination and treatment for infertility, the drug should be discontinued.
Use for renal impairment
Restrictions for impaired renal function - With caution.
Use with extreme caution if you have a history of kidney disease.
Use for liver dysfunction
Restrictions for liver dysfunction - With caution.
Use with extreme caution if you have a history of liver disease.
Use in elderly patients
Restrictions for elderly patients - Use with caution.
Use with extreme caution in elderly patients.
Use in children
Restrictions for children - Contraindicated.
Not recommended for use in children under 6 years of age.
