What drugs are injected into the joint?
Depending on the desired effect, on the stage of gonarthrosis or coxarthrosis, on the diagnosis, drugs with the following effect are prescribed:
- local anesthetics – pain relief for a short time (combined with other drugs);
- glucocorticoids – anti-inflammatory effect lasts from a week to a month;
- chondroprotectors – stimulation of cartilage tissue restoration;
- synovial fluid prostheses – restoration of joint fluid and joint functions;
- platelet-rich plasma – stimulation of joint self-healing.
The injection drug is selected by the doctor depending on the goals and clinical picture.
Diclofenac
Dosage form
Rectal suppositories
Composition per suppository:
Active substance
: diclofenac sodium – 50 mg or 100 mg.
Excipients
: macrogol 400 (polyethylene oxide 400) - 0.1 g, solid fat (Vitepsol (brands N 15, W 35), Supposir (brands NA 15, NAS 50)) - until a suppository weighing 2.0 g is obtained.
Description
Suppositories are torpedo-shaped from white to white with a yellowish tint.
Pharmacotherapeutic group
Non-steroidal anti-inflammatory drug (NSAID).
ATX code
: M01AB05.
Pharmacological properties
Pharmacodynamics
The drug Diclofenac 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 suppress 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. The drug relieves migraine attacks when used in rectal suppositories.
Pharmacokinetics
Suction
Absorption of diclofenac from rectal suppositories begins quickly, although the rate of absorption is less than when taken orally with enteric-coated tablets. After using a rectal suppository containing 50 mg of the active substance, its maximum concentration in plasma is achieved on average within an hour, but the maximum concentration calculated per unit dose taken is approximately 2/3 of the corresponding indicator recorded after oral administration for an enteric tablet . The amount of absorbed active substance is directly 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 oral or rectal administration of the drug is approximately half that of an equivalent dose administered parenterally.
With repeated administration of the drug in the form of suppositories, the pharmacokinetic parameters do not change. Provided the recommended dosage regimen is followed, no accumulation is observed.
Distribution
Communication with serum proteins is 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 the blood plasma, the concentration of diclofenac in the synovial fluid is higher than in the blood plasma, and its values remain higher for a period of time up to 12 hours.
Diclofenac was detected at low concentrations (100 ng/ml) in the breast milk of one nursing mother. The estimated amount of diclofenac entering the child's body through breast milk is equivalent to 0.03 mg/kg/day.
Biotransformation / 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. Two of these phenolic metabolites are biologically active, but to a significantly lesser extent than diclofenac.
Removal
The total systemic plasma clearance of diclofenac is 263±56 ml/min. The terminal half-life is 1-2 hours. The half-life of 4 metabolites, including two pharmacologically active ones, is also short and amounts to 1-3 hours. One of the metabolites, 3′-hydroxy-4′-methoxy-diclofenac, has a longer half-life, but this metabolite is completely inactive. About 60% of the dose is excreted by the kidneys 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 dose is excreted as metabolites in bile.
The concentration of the active substance in the blood plasma depends linearly on the dose taken.
Pharmacokinetics in special groups of patients
Absorption, metabolism and excretion of diclofenac do not depend on age. In children, diclofenac plasma concentrations when using equivalent doses of the drug (mg/kg body weight) are similar to the corresponding indicators in adults. However, in some elderly patients, after a 15-minute intravenous infusion, an increase in the concentration of diclofenac in the blood plasma by 50% was noted compared with that of healthy younger volunteers.
In patients with impaired renal function, if the recommended dosage regimen is followed, accumulation of the unchanged active substance is not observed. When creatinine clearance is less than 10 ml/min, the calculated equilibrium concentrations of diclofenac hydroxymetabolites are approximately 4 times higher than in healthy volunteers, while the metabolites are excreted exclusively in bile.
In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetics of diclofenac are similar to those in patients with preserved liver function.
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.
- Algodismenorrhea; inflammatory processes in the pelvis, including adnexitis.
- Migraine attacks.
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, Diclofenac is contraindicated in patients with attacks of bronchial asthma, urticaria or acute rhinitis, which are provoked by the use of acetylsalicylic acid or other NSAIDs.
- Hepatic, renal (GFR less than 15 ml/min/1.73 m2) and 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.
- Proctitis.
- Chronic heart failure, functional class II-IV according to the NYHA classification; clinically confirmed coronary heart disease; diseases of peripheral arteries and cerebral vessels; uncontrolled arterial hypertension.
- Breastfeeding period.
- The use of suppositories at a dose of 50 mg in children under 14 years of age, and at a dose of 100 mg in children under 18 years of age is not recommended.
Carefully
When using the drug Diclofenac and other NSAIDs, caution should be exercised and patients with symptoms/signs indicating gastrointestinal lesions/diseases or with medical history suggestive of gastric or intestinal ulceration, bleeding or perforation should be carefully monitored; in patients with a history of Helicobacter pylori infection, ulcerative colitis, Crohn's disease, with a history of impaired liver function, 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 Diclofenac in patients receiving drugs that increase the risk of gastrointestinal bleeding: systemic glucocorticosteroids (including prednisolone), anticoagulants (including warfarin), antiplatelet agents (including clopidogrel, acetylsalicylic acid acid) or selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline). Caution is required when using Diclofenac in patients with mild to moderate liver dysfunction, 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 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 abuse alcohol, in the treatment of elderly patients, patients receiving diuretics or other drugs that affect renal function, as well as patients with a significant decrease in circulating blood volume (CBV) of any etiology, for example, in the periods before and after major surgical interventions.
Diclofenac should be used with caution in patients with defects in the hemostatic system.
Caution should be exercised when using Diclofenac in patients at risk of developing cardiovascular thrombosis (including myocardial infarction and stroke). Caution should be exercised when using Diclofenac in elderly patients. This is especially true for 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.
Use during pregnancy and breastfeeding
There is insufficient data on the safety of diclofenac in pregnant women, and therefore Diclofenac 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 Diclofenac, like other NSAIDs (inhibitors of prostaglandin synthesis), 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 the drug Diclofenac, like other NSAIDs. penetrates 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.
Because Diclofenac, like other NSAIDs, may 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.
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 with the shortest possible treatment period, in accordance with the purpose of treatment and the patient’s condition.
Suppositories must be inserted into the rectum. It is recommended to use the drug after bowel movement.
Adults
The recommended initial dose is 100-150 mg/day. In relatively mild cases of the disease, as well as for long-term therapy, 100 mg per day is usually sufficient. The daily dose should be divided into several doses. To relieve night pain or morning stiffness, Diclofenac is used as a rectal suppository before bedtime, in addition to taking the drug in tablet form during the day; 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 150 mg/day. Treatment should begin when the first symptoms appear. Depending on the dynamics of clinical symptoms, treatment can be continued for several days.
During a migraine attack
the initial dose is 100 mg. The drug is used at the first symptoms of an approaching attack. If necessary, on the same day you can additionally use the drug Diclofenac in rectal suppositories at a dose of up to 100 mg. If it is necessary to continue treatment in subsequent days, the daily dose of the drug should not exceed 150 mg (in several administrations).
Children and teenagers under 18 years of age
For children aged 18 years and older, the drug 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). For the treatment of juvenile rheumatoid arthritis, the daily dose can be increased to a maximum of 3 mg/kg (in several administrations). The maximum daily dose of 150 mg should not be exceeded.
Elderly patients (>65 years)
Initial dose 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 cardiovascular diseases or high risk of cardiovascular diseases
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.
Side effect
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” (> 1/10000, <1/1000); “very rare” (< 1/10000). 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.
Blood and lymphatic system disorders
: 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, sensitivity disorders, including paresthesia, memory disorders, tremors, convulsions, anxiety, acute cerebrovascular accidents, aseptic meningitis.
Visual disorders
: very rarely - visual impairment (blurred vision), diplopia.
Hearing and labyrinth disorders
: often – vertigo; very rarely - hearing impairment, tinnitus.
Heart disorders
: uncommon – myocardial infarction, heart failure, palpitations, chest pain.
Vascular disorders
: very rarely - increased blood pressure, vasculitis.
Respiratory, thoracic and mediastinal disorders
: 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, stomach and intestinal ulcers (with or without bleeding, stenosis or perforation, with the possible development of peritonitis), proctitis; very rarely - stomatitis, glossitis, damage to the esophagus, the occurrence of diaphragm-like strictures in the intestine, colitis (nonspecific hemorrhagic colitis, ischemic colitis, exacerbation of ulcerative colitis or Crohn's disease), constipation, pancreatitis, dysgeusia.
Disorders of the liver and biliary tract
: often - increased activity of aminotransferases in blood plasma; rarely - hepatitis, jaundice, liver dysfunction; very rarely - fulminant hepatitis, liver necrosis, liver failure.
Skin and subcutaneous tissue disorders
: 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 - kidney damage (acute renal failure), hematuria, proteinuria, tubulointerstitial nephritis, nephrotic syndrome, papillary necrosis.
General and administration site disorders
: often - irritation at the injection site, rarely - swelling.
Disorders of the cardiovascular system.
Data from clinical studies indicate 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).
Visual impairment
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.
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.
Interaction with other drugs
Identified interactions
CYP2C9 isoenzyme inhibitors
. Caution should be exercised when using diclofenac concomitantly with CYP2C9 isoenzyme inhibitors (such as voriconazole) due to a possible increase in diclofenac serum concentrations and exposure.
Lithium, digoxin
. Diclofenac may increase the lithium content and digoxin concentration in the blood plume. 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 – quinolone derivatives
. There are isolated reports of the development of seizures in patients receiving concomitant quinolone derivatives and diclofenac.
Proposed interactions
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 simultaneously with inducers of the CYP2C9 isoenzyme (such as rifamricin), as this may lead to a significant decrease in the concentration of diclofenac in the blood plasma and a decrease in its exposure.
special instructions
Gastrointestinal lesions
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 elderly patients, such complications can have serious consequences; if bleeding or gastrointestinal ulceration develops in patients receiving Diclofenac, 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 drugs 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 those associated with allergic diseases). rhinitis-like symptoms). In this group of patients, as well as in patients with allergies to other drugs (skin rash and itching or urticaria), when using the drug Voltaren 1, special care should be taken (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 Diclofenac 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 Diclofenac, 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 Diclofenac 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 use of the drug should be discontinued. It should be borne in mind that hepatitis during the use of the drug Diclofenac can develop without prodromal phenomena.
Effects on the kidneys
During therapy with Diclofenac, 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 the volume of extracellular fluid of any etiology, for example, in the period before and after major surgical interventions. After cessation of drug therapy, normalization of renal function indicators to initial values is usually observed.
Effects on the cardiovascular system
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 Diclofenac may temporarily inhibit platelet aggregation, and therefore in patients with hemostasis disorders it is necessary to carefully monitor relevant laboratory parameters.
With long-term use of the drug Diclofenac, it is recommended to conduct regular clinical tests of peripheral blood.
Masking signs of an infectious process
The anti-inflammatory effect of Diclofenac may complicate the diagnosis of infectious processes.
Use simultaneously with other NSAIDs
Diclofenac should not be used concomitantly with other NSAIDs, including selective COX-2 inhibitors due to the risk of adverse events.
The effect of the drug on the ability to drive vehicles and machinery
Patients who experience visual disturbances, dizziness, drowsiness, vertigo or other disorders of the central nervous system while using the drug Diclofenac should not drive vehicles or operate machinery.
Release form
Rectal suppositories 50 mg, 100 mg.
1, 2, 3, 4. 5, 6, 7, 8, 9, 10 suppositories in a blister pack made of a two-layer film or a film made of PVC/PE polymer materials or a white combined PVC/PE film or a polyvinyl chloride film.
1, 2, 3 blister packs together with instructions for medical use of the drug are placed in a cardboard pack.
1, 2, 3, 4, 5, b, 7 suppositories in a blister pack made of a two-layer film or a film made of PVC/PE polymer materials or a white combined PVC/PE film or a polyvinyl chloride film.
4 blister packs along with instructions for medical use of the drug are placed in a cardboard pack.
1, 2, 3, 4, 5, 6 suppositories in a blister pack made of a two-layer film or a film made of PVC/PE polymer materials or a white combined PVC/PE film or a polyvinyl chloride film.
5 blister packs along with instructions for medical use of the drug are placed in a cardboard pack.
1, 2, 3, 4, 5 suppositories in blister packs made of two-layer film or I3 film of PVC/PE polymer materials or white combined PVC/PE film or polyvinyl chloride film.
6 blister packs along with instructions for medical use of the drug are placed in a cardboard pack.
1, 2, 3, 4 suppositories in a blister pack made of a two-layer film or a film made of polymer materials PVC-YUE or a white PVC/PE film combined or a polyvinyl chloride film.
7 blister packs along with instructions for medical use of the drug are placed in a cardboard pack.
1, 2, 3 suppositories in a blister pack made of a two-layer film or a film made of PVC/PE polymer materials or a white combined PVC/PE film or a polyvinyl chloride film.
8, 9, 10 blister packs along with instructions for medical use of the drug are placed in a cardboard pack.
Storage conditions
At a temperature not exceeding 30 °C.
Keep out of the reach of children.
Best before date
3 years.
Do not use after the expiration date stated on the packaging.
Vacation conditions
By doctor's prescription.
In what cases are hormones prescribed?
In the later stages of arthrosis of the hip joint or any other, when pain almost always bothers the patient and painkillers do not help, a stronger remedy may be prescribed. This is an emergency treatment measure that can quickly relieve pain and improve well-being. Unfortunately, this coin also has a downside, especially if you resort to this method more often than necessary.
Kenalog, diprospan and other corticosteroid drugs quickly stop inflammation, eliminate edema and swelling. However, they do not cure arthrosis at all, do not restore nutrition to the cartilage and do not improve the condition of the joint. This is only an ambulance - a powerful blow to the body, especially if you resort to such treatment for osteoarthritis too often.
No organism can withstand frequent injections of hormonal drugs.
What rules should you follow if you have been prescribed hormone injections into a joint?
If you cannot do without hormone injections, remember this:
- Keep a break of at least 2 weeks between injections. The drug does not start working instantly, so you need to wait a while for the doctor to evaluate its effectiveness.
- Remember that the first injection is the most effective. If there is no relief after the first injection, avoid repeated injections in the same place. It would be more correct to change the injection site or choose a different drug.
- You should not give hormone injections to one knee more than 4-5 times, as the risk of complications increases. Each time, the likelihood of needle injury, infection, or ligament damage increases.
Hormone injections are a last resort for arthrosis
In the video you will see how a synovial fluid prosthesis is injected into the knee joint in a medical office:
Is there an alternative?
Hormone injections reduce pain due to arthrosis of the ankle, knee, and hip, but also have a negative effect on the body. They are especially dangerous in case of diabetes mellitus, arterial hypertension, stomach ulcers, and also if the patient’s kidney function is impaired. In addition, corticosteroids only temporarily relieve pain, which means that a person will need a larger dose each time.
Instead of harmful corticosteroids, which also do not cure, you can choose other therapeutic methods:
- injections of chondroprotectors, which are aimed at restoring damaged cartilage tissue and normalizing metabolism in the joint (the course ranges from 3 to 15 injections);
- injection of a synovial fluid prosthesis, such as Noltrex, which expands the damaged cartilage surfaces, mixes with the joint fluid and returns the joint to normal functioning.
The course of injections of synovial fluid prosthesis is 2-5 procedures. After this, you can forget about arthrosis for 1-1.5 years. The drug based on hyaluronic acid or synthetic Noltrex is safe for the gastrointestinal tract and other body systems and will not harm diabetics or people with high blood pressure.
If you are experiencing severe joint pain, do not rush to relieve it with hormones. Consider a future-proof treatment option instead of drugging your body with corticosteroids for a long time.
Diclofenac 25 mg/ml 3 ml ampoules 10 pcs. solution for intramuscular administration in Moscow
- Hypersensitivity to diclofenac or to any other drug from the group of non-steroidal anti-inflammatory drugs (NSAIDs), as well as to any of the excipients of the drug; erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase), bleeding from the gastrointestinal tract, inflammatory bowel diseases (nonspecific ulcerative colitis, Crohn's disease); severe liver failure, liver disease in the acute period;
- severe renal failure (creatinine clearance less than 30 ml/min), hyperkalemia;
- complete or incomplete acetylsalicylic acid intolerance syndrome (rhinosinusitis, urticaria, nasal polyps, bronchial asthma that occurs when taking acetylsalicylic acid or other NSAIDs);
- hematopoietic disorders, hemostasis disorders (including hemophilia);
- pregnancy, breastfeeding period,
- children under 18 years of age;
- period after coronary artery bypass surgery;
- with an increased risk of arterial thrombosis and thromboembolism;
- chronic heart failure, functional class II-IV according to the NYHA classification;
- clinically confirmed coronary heart disease;
- diseases of peripheral arteries and cerebral vessels; uncontrolled arterial hypertension.
With caution:
coronary heart disease, cerebrovascular diseases, congestive heart failure, arterial hypertension, significant decrease in circulating blood volume (including after major surgery), edema syndrome, peripheral arterial disease, dyslipidemia, diabetes mellitus, anemia, bronchial asthma , renal failure (creatinine clearance less than 60 ml/min), alcoholism, erosive and ulcerative diseases of the gastrointestinal tract without exacerbation, history of liver disease, diverticulitis, condition after extensive surgery, inducible porphyria, old age, smoking, severe somatic diseases , systemic connective tissue diseases, long-term use of nonsteroidal anti-inflammatory drugs, simultaneous use of glucocorticosteroids, anticoagulants, antiplatelet agents, selective serotonin reuptake inhibitors, hyperlipidemia, the presence of
Helicobacter pylori infection.