Diclofenac 50 mg instructions for use. Diclofenac tablets - instructions for use. Impact on the ability to drive vehicles and operate machinery
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 a major 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). Inhibits proteoglycan synthesis in cartilage. 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. Suppresses platelet aggregation. With long-term use it has a desensitizing effect. When applied topically in ophthalmology, it reduces swelling and pain during inflammatory processes of non-infectious etiology.
Pharmacokinetics
After oral administration, it is absorbed from the gastrointestinal tract. Eating slows down the rate of absorption, but the degree of absorption does not change. About 50% active substance metabolized during the “first pass” through the liver. When administered rectally, absorption occurs more slowly. The time to reach Cmax in plasma after oral administration is 2-4 hours depending on the dosage form used, after rectal administration - 1 hour, intramuscular administration - 20 minutes. The concentration of the active substance in plasma is linearly dependent on the dose applied. Does not accumulate. Plasma protein binding is 99.7% (mainly albumin). Penetrates into synovial fluid, Cmax is reached 2-4 hours later than in plasma. It is extensively metabolized to form several metabolites, of which two are pharmacologically active, but to a lesser extent than diclofenac. Systemic clearance of the active substance is approximately 263 ml/min. T1/2 from plasma is 1-2 hours, from synovial fluid - 3-6 hours. Approximately 60% of the dose is excreted in the form of metabolites by the kidneys, less than 1% is excreted unchanged in the urine, the rest is excreted in the form of metabolites in bile.
Indications
Articular syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout), degenerative and chronic inflammatory diseases of the musculoskeletal system (osteochondrosis, osteoarthritis, periarthropathy), post-traumatic inflammation of soft tissues and the musculoskeletal system (sprains, bruises). Pain in the spine, neuralgia, myalgia, arthralgia, pain and inflammation after operations and injuries, pain with gout, migraine, algodismenorrhea, pain with adnexitis, proctitis, colic (bilious and renal), pain with infectious and inflammatory diseases of the ENT -organs For local use: inhibition of miosis during cataract surgery, prevention of cystoid macular edema associated with removal and implantation of the lens, inflammatory processes of the eye of a non-infectious nature, post-traumatic inflammatory process in penetrating and non-penetrating wounds of the eyeball.
Contraindications
Erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, “aspirin triad”, hematopoietic disorders of unknown etiology, hypersensitivity to diclofenac and components of the dosage form used, or other NSAIDs.
Use during pregnancy and breastfeeding
Use during pregnancy and lactation is possible in cases where the expected benefit to the mother outweighs the potential risk to the fetus or newborn.
Directions for use and doses
For oral administration for adults, a single dose is 25-50 mg 2-3 times a day. The frequency of administration depends on the dosage form used, the severity of the disease and is 1-3 times a day, rectally - 1 time a day. For the treatment of acute conditions or relief of exacerbation of a chronic process, a dose of 75 mg is used intramuscularly. For children over 6 years of age and adolescents, the daily dose is 2 mg/kg. Apply externally in a dose of 2-4 g (depending on the area of the painful area) to the affected area 3-4 times a day. When used in ophthalmology, the frequency and duration of administration are determined individually. The maximum daily dose for adults when taken orally is 150 mg/day.
Side effects
From the digestive system: nausea, vomiting, anorexia, pain and discomfort in the epigastric region, flatulence, constipation, diarrhea; in some cases - erosive and ulcerative lesions, bleeding and perforation of the gastrointestinal tract; rarely - liver dysfunction. When administered rectally, in isolated cases, inflammation of the colon with bleeding and exacerbation of ulcerative colitis were observed. From the central nervous system and peripheral nervous system: dizziness, headache, agitation, insomnia, irritability, feeling tired; rarely - paresthesia, visual impairment (blurredness, diplopia), tinnitus, sleep disorders, convulsions, irritability, tremor, mental disorders, depression. From the hematopoietic system: rarely - anemia, leukopenia, thrombocytopenia, agranulocytosis. From the urinary system: rarely - impaired renal function; swelling may occur in predisposed patients. Dermatological reactions: rarely - hair loss. Allergic reactions: skin rash, itching; when used in the form of eye drops - itching, redness, photosensitivity. Local reactions: a burning sensation is possible at the site of intramuscular injection, in some cases - the formation of infiltrate, abscess, necrosis of adipose tissue; with rectal administration, local irritation, the appearance of mucous discharge mixed with blood, and painful defecation are possible; when used externally in rare cases - itching, redness, rash, burning; when applied topically in ophthalmology, a transient burning sensation and/or temporary blurred vision may occur immediately after instillation. With prolonged external use and/or application to large surfaces of the body, systemic side effects are possible due to the resorptive effect of diclofenac.
Overdose
Symptoms: vomiting, bleeding from the gastrointestinal tract, diarrhea, dizziness, tinnitus, convulsions, increased blood pressure, respiratory depression, in case of significant overdose - acute renal failure, hepatotoxic effect. Treatment: gastric lavage, activated charcoal, symptomatic therapy aimed at eliminating increased blood pressure, renal dysfunction, convulsions, gastrointestinal damage, respiratory depression. Forced diuresis and hemodialysis are ineffective (due to the significant connection with proteins and intensive metabolism).
Interaction with other drugs
When used simultaneously with diclofenac, antihypertensive drugs may weaken their effect. There are isolated reports of the occurrence of seizures in patients taking NSAIDs and quinolone antibacterial drugs simultaneously. When used simultaneously with GCS, the risk of developing side effects from the digestive system. With simultaneous use of diuretics, the diuretic effect may be reduced. When used simultaneously with potassium-sparing diuretics, it is possible to increase the concentration of potassium in the blood. When used simultaneously with other NSAIDs, the risk of side effects may increase. There are reports of the development of hypoglycemia or hyperglycemia in patients with diabetes mellitus who used diclofenac simultaneously with hypoglycemic drugs. When used simultaneously with acetylsalicylic acid, the concentration of diclofenac in the blood plasma may decrease. Although clinical studies have not established the effect of diclofenac on the action of anticoagulants, isolated cases of bleeding have been described with the simultaneous use of diclofenac and warfarin. With simultaneous use, it is possible to increase the concentration of digoxin, lithium and phenytoin in the blood plasma. The absorption of diclofenac from the gastrointestinal tract is reduced when used simultaneously with cholestyramine, and to a lesser extent with colestipol. With simultaneous use, it is possible to increase the concentration of methotrexate in the blood plasma and increase its toxicity. With simultaneous use, diclofenac may not affect the bioavailability of morphine, however, the concentration of the active metabolite of morphine may remain elevated in the presence of diclofenac, which increases the risk of developing side effects of the morphine metabolite, incl. respiratory depression. When used simultaneously with pentazocine, a case of the development of a grand mal seizure has been described; with rifampicin - a decrease in the concentration of diclofenac in the blood plasma is possible; with ceftriaxone - excretion of ceftriaxone with bile increases; with cyclosporine - increased nephrotoxicity of cyclosporine is possible.
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 the history indicates allergic reactions for 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 operate 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 or engage in other potentially dangerous activities. dangerous species activities.
Active substance
Diclofenac sodium (diclofenac)
Release form, composition and packaging
10 pieces. - contour cellular packaging (1) - cardboard packs.
10 pieces. - contour cell packaging (2) - cardboard packs.
10 pieces. - contour cell packaging (3) - cardboard packs.
10 pieces. - contour cell packaging (5) - cardboard packs.
10 pieces. - contour cell packaging (10) - cardboard packs.
20 pcs. - contour cellular packaging (1) - cardboard packs.
20 pcs. - contour cell packaging (2) - cardboard packs.
20 pcs. - contour cell packaging (3) - cardboard packs.
30 pcs. - dark glass jars (1) - cardboard packs.
30 pcs. - polymer jars (1) - cardboard packs.
pharmachologic effect
Diclofenac has anti-inflammatory, analgesic and antipyretic effects. By indiscriminately inhibiting cyclooxygenase 1 and 2, it disrupts the metabolism of arachidonic acid and reduces the amount of prostaglandins at the site of inflammation. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac helps to significantly reduce the severity of pain, morning stiffness, and swelling of the joints, which improves the functional state of the joint. For injuries, in the postoperative period, diclofenac reduces pain and inflammatory swelling.
Pharmacokinetics
Absorption is fast and complete, food slows the rate of absorption by 1-4 hours and reduces Cmax by 40%. After oral administration of 25 mg, C max 1.0 mcg/ml is achieved after 2-3 hours. The concentration is linearly dependent on the size of the administered dose.
No changes in the pharmacokinetics of diclofenac are observed during repeated administration and do not accumulate.
Bioavailability - 50%. Communication with plasma proteins is more than 99% (most of it binds to). Penetrates into synovial fluid: C max in synovial fluid is observed 2-4 hours later than in plasma. T1/2 from synovial fluid 3-6 hours (the concentration of the active substance in synovial fluid 4-6 hours after administration of the drug is higher than in plasma, and remains higher for another 12 hours). The relationship between the concentration of the drug in the synovial fluid and the clinical effectiveness of the drug has not been clarified.
Metabolism 50% of the active substance is metabolized during the "first pass" through the liver. Metabolism occurs as a result of multiple or single hydroxylation and conjugation with glucuronic acid. Participates in the metabolism of the drug enzyme system P450 CYP2C9. The pharmacological activity of the metabolites is lower than that of diclofenac.
Systemic clearance is 350 ml/min, volume of distribution is 550 ml/kg, T1/2 from plasma is 2 hours. 65% of the administered dose is excreted in the form of metabolites by the kidneys; less than 1% is excreted unchanged, the rest of the dose is excreted as metabolites in the bile.
In patients with severe renal failure (creatinine clearance less than 10 ml/min), the excretion of metabolites in bile increases, but no increase in their concentration in the blood is observed.
In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetic parameters of diclofenac do not change. Diclofenac penetrates into breast milk.
Indications
- diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis; gouty arthritis, rheumatic soft tissue lesions, osteoarthritis of peripheral joints and spine, including with radicular syndrome, tenosynovitis, bursitis);
- pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboischialgia, post-traumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, algodismenorrhea, adnexitis, proctitis, toothache;
- as part of complex therapy for infectious and inflammatory diseases of the ear, nose and throat with severe pain (pharyngitis, tonsillitis, otitis media);
- febrile syndrome.
Contraindications
- erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase);
- bleeding from the gastrointestinal tract;
- "aspirin" asthma;
- hematopoietic disorders;
- hemostasis disorders (including hemophilia);
- pregnancy;
- children's age (up to 6 years);
- lactation period;
- hypersensitivity (including to other NSAIDs).
Carefully: anemia, bronchial asthma, congestive insufficiency, arterial hypertension, edema syndrome, liver or kidney failure, alcoholism, inflammatory bowel diseases, erosive and ulcerative diseases of the gastrointestinal tract without exacerbation, diabetes, condition after extensive surgery, inducible porphyria, old age, diverticulitis, systemic connective tissue diseases.
Dosage
Orally, without chewing, during or after meals, with a small amount of water. Adults and adolescents over 15 years old - 25-50 mg 2-3 times a day. When the optimal therapeutic effect is achieved, the dose is gradually reduced and switched to maintenance treatment at a dose of 50 mg/day. The maximum daily dose is 150 mg. For children (over 6 years old) a daily dose of up to 2 mg/kg body weight, divided into 2-3 doses.
At juvenile rheumatoid arthritis the daily dose can be increased to 3 mg/kg body weight.
The approximate regimen for using the drug is presented in the table:
Side effects
more often than 1% - abdominal pain, feeling of bloating, diarrhea, nausea, constipation, flatulence, increased levels of liver enzymes, peptic ulcer with possible complications(bleeding, perforation), gastrointestinal bleeding;
less than 1% - vomiting, jaundice, melena, blood in the stool, damage to the esophagus, aphthous stomatitis, dry mucous membranes (including the mouth), hepatitis (possibly fulminant), liver necrosis, cirrhosis, hepatorenal syndrome, changes in appetite, pancreatitis , cholecystopancreatitis, colitis.
Nervous system:
more often 1% - headache, dizziness;
less than 1% - sleep disturbance, drowsiness, depression, irritability, aseptic meningitis (more often in patients with systemic lupus erythematosus and other systemic connective tissue diseases), convulsions, general weakness, disorientation, nightmares, a feeling of fear.
Sense organs:
more often than 1% - tinnitus,
less than 1% - blurred vision, diplopia, taste disturbance, reversible or irreversible hearing loss, scotoma.
Skin:
more often 1% - skin itching, skin rash;
less than 1% - alopecia, urticaria, eczema, toxic dermatitis, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), increased photosensitivity, pinpoint hemorrhages.
Genitourinary system:
more often than 1% - fluid retention,
less than 1% - nephrotic syndrome, proteinuria, oliguria, hematuria, interstitial nephritis, papillary necrosis, acute renal failure, azotemia
Hematopoietic organs and immune system:
less than 1% - anemia (including hemolytic and aplastic anemia), leukopenia, thrombocytopenia, eosinophilia, agranulocytosis, thrombocytopenic purpura, worsening of infectious processes (including the development of necrotizing fasciitis).
Respiratory system:
less than 1% - cough, bronchospasm, laryngeal edema, pneumonitis.
The cardiovascular system:
less often 1% - increased blood pressure; congestive heart failure, extrasystole, chest pain.
Allergic reactions:
less often 1% - anaphylactoid reactions, anaphylactic shock(usually develops rapidly), swelling of the lips and tongue, allergic vasculitis.
Overdose
Symptoms: vomiting, dizziness, headache, shortness of breath, clouding of consciousness, in children - myoclonic convulsions, nausea, abdominal pain, bleeding, impaired liver and kidney function.
Treatment: gastric lavage, administration of activated carbon, symptomatic therapy, forced diuresis. Hemodialysis is ineffective.
Drug interactions
Increases plasma concentrations of digoxin. lithium and cyclosporine drugs.
Reduces the effect of diuretics; against the background of potassium-sparing diuretics, the risk of hyperkalemia increases; against the background of anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) - the risk of bleeding (usually from gastrointestinal tract).
Reduces the effects of antihypertensive and hypnotic drugs.
Increases the likelihood of side effects of other NSAIDs and glucocorticosteroids (bleeding in the gastrointestinal tract), the toxicity of methotrexate and the nephrotoxicity of cyclosporine.
Reduces the concentration of diclofenac in the blood.
Concomitant use with paracetamol increases the risk of developing nephrotoxic effects of diclofenac.
Reduces the effect of hypoglycemic drugs.
Cefamandole, cefoperazone, cefotetan, and plicamycin increase the incidence of hypoprothrombinemia.
Cyclosporine and gold preparations increase the effect of diclofenac on the synthesis of prostaglandins in the kidneys, which increases nephrotoxicity.
Simultaneous administration with ethanol, colchicine, corticotropin and St. John's wort preparations increases the risk of bleeding in the gastrointestinal tract.
Diclofenac enhances the effect of drugs that cause photosensitivity. Drugs that block tubular secretion increase the plasma concentration of diclofenac, thereby increasing its toxicity.
Instructions
Tradename
Diclofenac
International nonproprietary name
Diclofenac
Dosage form
Rectal suppositories 50 mg, 100 mg
Compound
One suppository contains
A active substance sodium diclofenac 50 mg or 100 mg,
Excipients - alcohol cetyl,
suppository base (for 100 mg) - semi-synthetic glycerides (Hard fat),
suppository base (for 50 mg) - suppotsir AM (solid fat).
Description
White or white with a yellowish tint, cylindrical-conical suppositories. The cut is allowed to have an airy and porous core and a funnel-shaped depression.
Pharmacotherapeutic group
Non-steroidal anti-inflammatory drugs. Acetic acid derivatives.
ATC code M01AB05.
Pharmacological properties
Pharmacokinetics
Absorption is fast and complete, with rectal administration - 30 minutes. The concentration of the drug in plasma is linearly dependent on the size of the administered dose. Communication with blood plasma proteins is more than 99%. Penetrates into breast milk and synovial fluid. The maximum concentration in synovial fluid is reached 2 to 4 hours later than in blood plasma. The half-life from plasma is 1-2 hours, from synovial fluid - 3-6 hours. Metabolized in the liver. If the recommended interval between doses is observed, the drug does not accumulate. About 60% of the administered dose is excreted as metabolites through the kidneys; less than 1% is excreted unchanged, the rest is excreted as metabolites in the bile. In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetic parameters of diclofenac are the same as in patients without liver disease. In patients with severe renal failure (creatinine clearance less than 10 ml/min), the excretion of metabolites in bile increases, but no increase in their concentration in the blood is observed.
Pharmacodynamics
Diclofenac indiscriminately inhibits the activity of COX1 and COX2, disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever; inhibits the synthesis of inflammatory mediators and reduces pain sensitivity at the site of inflammation. Reduces capillary permeability, suppresses platelet aggregation, restores impaired microcirculation. In rheumatic diseases, anti-inflammatory and analgesic properties cause a decrease in pain, especially pain in the joints at rest and during movement, a decrease in morning rigidity, swelling of the joints, and an improvement in motor activity. It has a pronounced analgesic effect for moderate and severe pain. In inflammatory processes that occur after operations and injuries, it quickly relieves both spontaneous pain and pain during movement, and reduces inflammatory swelling at the wound site. For primary dysmenorrhea, the drug can relieve pain. The anti-inflammatory effect occurs by the end of the first week of treatment.
Indications for use
Inflammatory and degenerative rheumatic diseases (rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, spondyloarthritis)
Pain syndromes in diseases of the spine
Rheumatic diseases of extra-articular soft tissues
Acute attack of gout
Post-traumatic and postoperative pain syndromes accompanied by inflammation and swelling
Severe migraine attacks
Renal and biliary colic
Gynecological diseases accompanied by pain and inflammation (primary algodismenorrhea and adnexitis)
As an adjuvant for severe diseases of the ear, nose and throat, accompanied by pain (pharyngitis, tonsillitis, otitis media).
Directions for use and doses
Rectally.
For adults: 1 suppository of 100 mg - 1 time per day, 1 suppository of 50 mg - 2-3 times per day. The daily dose is 100 -150 mg. The maximum daily dose of the drug should not exceed 150 mg.
In mild cases and with long-term therapy, the daily dose is 50-100 mg per day. The duration of the course of therapy is determined individually.
With primary algodismenorrhea(when the first symptoms appear): 50 - 100 mg per day, if necessary, the dose can be increased to 150 mg.
During a migraine attack: 100 mg at the first sign of an attack; if necessary, the dose can be increased to 150 mg.
Teens over 16up to 18 years old: 50 mg 1-2 times a day.
Suppositories must be inserted into the rectum as deeply as possible, preferably after cleansing the intestines. Suppositories should not be cut into pieces, since such a change in the storage conditions of the drug can lead to disruption of the distribution of the active substance.
Side effects
- local reactions: irritation, mucous discharge mixed with blood, pain during defecation, local allergic reactions.
With long-term use it is possible systemic reactions:
Pain in the epigastric region, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia, increased aminotransferase activity
Headache, dizziness
Visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, taste disturbance
Skin rash
Gastritis
Gastrointestinal bleeding (vomiting blood, melena, bloody diarrhea)
Ulcers of the stomach and intestines, with or without bleeding or perforation
Hepatitis (including fulminant hepatitis), jaundice, liver dysfunction
Drowsiness
Hives
Severe bronchospasm, angioedema, systemic anaphylactic/anaphylactoid reactions, including hypotension and shock
Palpitations, chest pain, hypertension, vasculitis, heart failure, myocardial infarction
Bronchial asthma, pneumonitis
Edema, hyperkalemia
In some cases:
Aphthous stomatitis, glossitis, esophagitis
The appearance of diaphragm-like strictures in the intestine
Lower bowel disorders such as nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease
Pancreatitis
Proctitis, exacerbation of hemorrhoids
Sensory disturbances, including paresthesia, memory impairment, tremor, convulsions, anxiety, cerebrovascular disorders, disorientation, insomnia, irritability, depression, anxiety, nightmares, mental disorders, aseptic meningitis
Bullous rashes, erythema multiforme, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome (acute toxic epidermal necrolysis), erythroderma (exfoliative dermatitis), itching, hair loss, photosensitivity, purpura, including allergic
Acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis
Thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis
Contraindications
Increased sensitivity to diclofenac and/or components of the drug and other non-steroidal anti-inflammatory drugs (NSAIDs), attacks of bronchial asthma, urticaria, acute rhinitis in history, occurring in response to taking acetylsalicylic acid or other NSAIDs
Erosions and ulcers, as well as inflammatory diseases of the gastrointestinal tract in the acute phase
Active gastrointestinal bleeding, incl. rectal
Hematopoietic disorder of unknown etiology
Severe liver failure, active liver disease
Severe renal failure (creatinine clearance less than 30 ml/min)
Severe heart failure
Confirmed hyperkalemia
Proctitis, hemorrhoids in the acute stage
III trimester of pregnancy (possible suppression of uterine contractility and premature closure of the ductus arteriosus in the fetus) and lactation period
Children's and adolescence up to 16 years old.
Drug interactions
Diclofenac, when used together, increases the plasma concentration of lithium, digoxin, indirect anticoagulants, oral antidiabetic drugs (both hypo- and hyperglycemia are possible), quinolones.
Increases the toxicity of methotrexate, cyclosporine, increases the likelihood of developing side effects of glucocorticoids (gastrointestinal bleeding), the risk of hyperkalemia against the background of potassium-sparing diuretics, reduces the effect of diuretics. Plasma concentrations of diclofenac are reduced with simultaneous use of acetylsalicylic acid.
special instructions
Carefully used for erosive and ulcerative lesions of the gastrointestinal tract in the anamnesis, the presence of infection Helicobacter pylori; history of liver disease, hepatic porphyria, chronic renal failure; bronchial asthma, allergic rhinitis, polyps of the nasal mucosa, obstructive diseases respiratory tract; arterial hypertension, chronic heart failure, coronary heart disease, significant reduction in circulating blood volume; immediately immediately after surgery; for cerebrovascular diseases, dyslipidemia/hyperlipidemia, diabetes mellitus, peripheral arterial diseases; in elderly patients (including those receiving diuretics, weakened patients and those with low body weight), with indications of a history of allergic reactions (urticaria, Quincke's edema, etc.), while taking glucocorticosteroid drugs (incl. prednisolone), anticoagulants (including warfarin), antiplatelet agents (including acetylsalicylic acid, clopidogrel), selective serotonin reuptake inhibitors (including citalopram, fluoxetine, paroxetine, sertraline), long-term use of non-steroidal anti-inflammatory drugs drugs, alcoholism, severe somatic diseases.
When carrying out long-term therapy, it is necessary to monitor liver function, peripheral blood patterns, and stool analysis for occult blood.
Simultaneous administration with ethanol increases the risk of bleeding in the gastrointestinal tract.
If side effects occur, stop taking the drug.
To reduce the risk of developing adverse events from the gastrointestinal tract, the minimum effective dose should be used for the shortest possible short course.
Pregnancy and lactation
The use of the drug in the first and second trimesters of pregnancy is possible only if the expected benefit to the mother outweighs the possible risk to the fetus. If it is necessary to prescribe the drug to women during lactation, the issue of stopping breastfeeding should be decided.
Features of the effect of the drug on the ability to drive a vehicle orpotentially dangerousmechanisms
Patients who experience dizziness or blurred vision while using Diclofenac should not drive a vehicle or operate potentially dangerous machinery. .
Overdose
Symptoms: headache, dizziness, loss of consciousness, abdominal pain, nausea, vomiting, gastrointestinal disorders, including bleeding; arterial hypotension, acute renal failure, convulsions, respiratory depression.
Treatment: supportive and symptomatic therapy.
Forced diuresis and hemodialysis are ineffective.
Release form and packaging
Rectal suppositories containing 100 mg diclofenac: 5 or 6 suppositories in blister packs made of polyvinyl chloride film laminated with polyethylene.
1 or 2 blister packs together with instructions for use in the state and Russian languages are placed in a cardboard pack.
Rectal suppositories containing 50 mg diclofenac: 6 suppositories in blister packs made of polyvinyl chloride film laminated with polyethylene.
1 blister pack along with instructions for medical use in the state and Russian languages is placed in a cardboard pack.
Storage conditions
In a dry place, protected from light, at a temperature of 15 to 25 ° C.
Keep out of the reach of children!
Shelf life
Do not use after expiration date.
Conditions for dispensing from pharmacies
On prescription
Manufacturer
Rectal suppositories containing 50 mg diclofenac
LLC "PHARMAPRIM"
MD-4829, Republic of Moldova,
st. Krinilor, 5, p. Porumbeni, Criuleni district,
tel.: (+373-22)-28-18-45, tel./fax: (+373-22)-28-18-46,
www.farmaprim.md
Rectal suppositories containing 100 mg diclofenac
LLC "PHARMAPRIM"
MD-2028, Republic of Moldova,
Chisinau, st. G. Tudor, 3
tel/fax: (+37322) 20-86-72
www.farmaprim.md
Registration Certificate Holder
FARMAPRIM LLC, Moldova
Address of the organization that accepts claims from consumers regarding the quality of products (products) on the territory of the Republic of Kazakhstan:
Representative office of Pharmaprim LLC in the Republic of Kazakhstan, Almaty, st. Gogolya, 86, of. 528, tel. 8-727-2796518, [email protected]
Attached files
| 445195951477977175_ru.doc | 70.5 kb |
| 502729321477978342_kz.doc | 81.5 kb |
Identification and classification
Registration number
International nonproprietary name
diclofenac
Dosage form
Enteric tablets, film-coated
Compound
One enteric film-coated tablet contains:
active substance: diclofenac sodium 50 mg;
Excipients: lactose monohydrate, corn starch, povidone K-30, sodium lauryl sulfate, sodium carboxymethyl starch, colloidal silicon dioxide, magnesium stearate; shell: methacrylic acid and ethyl acrylate copolymer, macrogol 6000, talc, titanium dioxide E 171 CI 77891, sunset yellow dye.
Description
Round biconvex film-coated tablets orange color, on the fracture from white to almost white.
Pharmacotherapeutic group
Nonsteroidal anti-inflammatory drug (NSAID)
Pharmacological properties
Pharmacodynamics
Non-steroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid. Diclofenac has anti-inflammatory, analgesic, antiplatelet and antipyretic effects. By indiscriminately inhibiting cyclooxygenase 1 and 2 (COX1 and COX2), it disrupts the metabolism of arachidonic acid and reduces the amount of prostaglandins at the site of inflammation. Most effective for inflammatory pain.
In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac helps to significantly reduce the severity of pain, morning stiffness, and swelling of the joints, which improves the functional state of the joint. For injuries, in the postoperative period, diclofenac reduces pain and inflammatory swelling.
Pharmacokinetics
Absorption is rapid and complete, food slows the rate of absorption by 1–4 hours and reduces the maximum concentration (Cmax) by 40%. After oral administration of 50 mg, the maximum concentration (C max) of 1.5 μg/ml is achieved after 2-3 hours. The plasma concentration is linearly dependent on the size of the administered dose.
There are no changes in the pharmacokinetics of diclofenac following repeated administration. Does not accumulate if the recommended interval between doses is observed. Bioavailability - 50%. Communication with plasma proteins is more than 99% (most of it is associated with albumin). Penetrates into synovial fluid; Cmax in synovial fluid is observed 2-4 hours later than in plasma. The half-life (T½) from synovial fluid is 3-6 hours (the concentration of the active substance in synovial fluid 4-6 hours after administration of the drug is higher than in plasma, and remains higher for another 12 hours). The relationship between the concentration of the drug in the synovial fluid and the clinical effectiveness of the drug has not been clarified.
Metabolism: 50% of the active substance is metabolized during the “first pass” through the liver. Metabolism occurs as a result of multiple or single hydroxylation and conjugation with glucuronic acid. The CYP2C9 isoenzyme takes part in the metabolism of the drug. The pharmacological activity of the metabolites is lower than that of diclofenac.
Systemic clearance is approximately 260±50 ml/min, volume of distribution is 550 ml/kg. T½ from plasma averages about 2.5 hours. 65% of the administered dose is excreted in the form of metabolites by the kidneys; less than 1% is excreted unchanged, the rest of the dose is excreted as metabolites in the bile.
In patients with severe renal failure (creatinine clearance (CC) less than 10 ml/min), the excretion of metabolites in bile increases, but no increase in their concentration in the blood is observed.
In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetic parameters of diclofenac do not change.
Diclofenac passes into breast milk.
Indications for use
Symptomatic treatment of diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic arthritis, juvenile chronic arthritis, ankylosing spondylitis (Bechterew's disease); gouty arthritis, rheumatic soft tissue disease, osteoarthritis of peripheral joints and spine, including with radicular syndrome, tenosynovitis, bursitis) .
The drug relieves or reduces pain and inflammation during the treatment period, but does not affect the progression of the disease.
Pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboischialgia, post-traumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, algomenorrhea, adnexitis, proctitis, toothache.
Contraindications
- Hypersensitivity to diclofenac and any other components of the drug;
- Complete or incomplete combination of bronchial asthma, recurrent polyposis of the nose and paranasal sinuses and intolerance to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs (including a history);
- Erosive and ulcerative changes in the mucous membrane of the stomach or duodenum, active gastrointestinal bleeding;
- Inflammatory bowel diseases (ulcerative colitis, Crohn's disease) in the acute phase;
- The period after coronary artery bypass surgery;
- III trimester of pregnancy, breastfeeding period;
- Confirmed chronic heart failure (II-IV functional class according to the NYHA classification);
- Clinically proven ischemic disease hearts;
- Peripheral arterial disease or cerebrovascular disorders;
- Increased risk of arterial thrombosis and thromboembolism;
- Uncontrolled arterial hypertension;
- Hematopoietic disorders, hemostasis disorders (including hemophilia);
- Severe liver failure or active liver disease;
- Severe renal failure (creatinine clearance less than 30 ml/min); progressive kidney disease;
- Confirmed hyperkalemia;
- Lactose intolerance, lactase deficiency, glucose-galactose malabsorption (the drug contains lactose);
- Children's age up to 14 years.
Carefully
Anemia, bronchial asthma, confirmed chronic heart failure of functional class I according to the NYHA classification, arterial hypertension, edema syndrome, liver or kidney failure (creatinine clearance 30-60 ml/min), dyslipidemia, hyperlipoproteinemia, diabetes mellitus, smoking, inflammatory bowel diseases, condition after extensive surgical interventions, inducible porphyria, diverticulitis, systemic connective tissue diseases, pregnancy I-II trimester.
Anamnestic data on the development of peptic ulcer disease of the gastrointestinal tract, the presence of Helicobacter pylori infection, old age, long-term use of NSAIDs, frequent alcohol consumption, severe somatic diseases.
Concomitant therapy with anticoagulants (for example, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).
In patients with seasonal allergic rhinitis, swelling of the nasal mucosa (including nasal polyps), chronic obstructive pulmonary disease, chronic respiratory tract infections (especially associated with allergic rhinitis-like symptoms), with allergies to other medications In patients with a significant decrease in circulating blood volume, diclofenac should be used with caution.
Use during pregnancy and breastfeeding
There is insufficient data on the safety of diclofenac in pregnant women. Therefore, diclofenac should be prescribed in the first and second trimesters of pregnancy only in cases where the expected benefit to the mother outweighs the potential risk to the fetus. Diclofenac, like other inhibitors of prostaglandin synthesis, is contraindicated in the last 3 months of pregnancy (possible suppression of uterine contractility and premature closure of the ductus arteriosus in the fetus).
Diclofenac gets into small quantities into breast milk. To prevent undesirable effects on the child, the drug should not be prescribed to nursing women. If necessary, use the drug breast-feeding should be stopped.
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 and teenagers from 14 years old. The recommended dose is 100-150 mg/day. 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.
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.
For the treatment of rheumatoid arthritis the daily dose can be maximally increased to 3 mg/kg (in several doses). The maximum daily dose should not exceed 150 mg.
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 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 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 (creatinine clearance less than 30 ml/min) is contraindicated (see section "Contraindications").
Patients with liver dysfunction
There is no data on the need for dose adjustment when using the drug in patients with impaired function lung liver And medium degree severity due to the lack of safety studies of the drug in this category of patients.
The use of the drug in patients with severe liver dysfunction is contraindicated (see section “Contraindications”).
Side effect
Criteria for assessing the frequency of adverse reactions: very often (>1/10), often (≥1/100,<1/10), нечасто (≥1/1000, <1/100), редко (≥1/10 000, <1/1000), очень редко (<1/10 000); частота неизвестна - по имеющимся данным установить частоту возникновения не представляется возможным.
Gastrointestinal disorders: often - epigastric pain, nausea, vomiting, diarrhea, dyspepsia, flatulence, anorexia; rarely - gastritis, proctitis, bleeding from the gastrointestinal tract (gastrointestinal tract) (vomiting with blood, melena, diarrhea mixed with blood), gastrointestinal ulcers (with or without bleeding or perforation); very rarely - stomatitis, glossitis, esophagitis, nonspecific hemorrhagic colitis, exacerbation of ulcerative colitis or Crohn's disease, the occurrence of diaphragm-like strictures in the intestine, constipation, pancreatitis; frequency unknown - ischemic colitis.
Disorders of the liver and biliary tract: often - increased aminotransferase activity; rarely - hepatitis, jaundice, liver dysfunction; very rarely - fulminant hepatitis, liver necrosis, liver failure.
Nervous system disorders: often - headache, dizziness; rarely - drowsiness; very rarely - sensory disturbance, incl. paresthesia, memory disorders, tremor, convulsions, anxiety, cerebrovascular disorders, aseptic meningitis.
Mental disorders: very rarely - disorientation, depression, insomnia, night “nightmares”, irritability, mental disorders.
Sensory organ disorders: often - vertigo; very rarely - visual impairment (blurred vision, diplopia), hearing impairment, tinnitus, impaired taste.
Renal and urinary tract disorders: very rarely - acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis.
Blood and lymphatic system disorders: very rarely - thrombocytopenia, leukopenia, hemolytic and aplastic anemia, agranulocytosis, eosinophilia.
Immune system disorders: anaphylactic/anaphylactoid reactions, including a marked decrease in blood pressure (BP) and shock; very rarely - angioedema (including the face).
Cardiovascular system disorders: very rarely - palpitations, chest pain, increased blood pressure, vasculitis, heart failure, myocardial infarction.
Disorders of the respiratory system, chest and mediastinal organs: rarely - exacerbation of bronchial asthma, cough, laryngeal edema; very rarely - pneumonitis.
Disorders of the skin and subcutaneous tissues: often - skin rash; rarely - urticaria; very rarely - bullous rashes, eczema, incl. multiforme and Stevens-Johnson syndrome, Lyell's syndrome, exfoliative dermatitis, itching, hair loss, photosensitivity, purpura, incl. allergic.
General disorders and disorders at the injection site: rarely - swelling.
Overdose
Symptoms: nausea, vomiting, epigastric pain, bleeding from the gastrointestinal tract, diarrhea, dizziness, headache, tinnitus, convulsions, decreased blood pressure, respiratory depression, in case of significant overdose - acute renal failure, hepatotoxic effect.
Treatment: gastric lavage, activated charcoal, symptomatic therapy aimed at eliminating arterial hypotension, renal dysfunction, convulsions, gastrointestinal damage, respiratory depression. Forced diuresis and hemodialysis are ineffective (due to the significant connection with proteins and intensive metabolism).
Interaction with other drugs
Lithium preparations, digoxin: Diclofenac may increase plasma concentrations of lithium and digoxin. Monitoring plasma concentrations of lithium and digoxin is recommended when used concomitantly with diclofenac.
Methotrexate: Caution is required when prescribing diclofenac less than 24 hours before or 24 hours after taking methotrexate, because in such cases, the concentration of methotrexate in the blood may increase and its toxic effect may increase.
Cyclosporine: the effect of diclofenac on the synthesis of prostaglandins in the kidneys may enhance the nephrotoxicity of cyclosporine. Therefore, the doses of diclofenac used should be lower than in patients not using cyclosporine.
Diuretic and antihypertensive drugs: diclofenac may reduce the hypotensive effect of diuretics and antihypertensive drugs (for example, beta-blockers, angiotensin-converting enzyme inhibitors - ACE inhibitors). In patients, especially elderly patients, these combinations should be prescribed with caution and blood pressure should be regularly monitored. Patients should be adequately hydrated. After initiation and periodically during treatment, especially when diuretics and ACE inhibitors are coadministered, renal function should be monitored due to the increased risk of nephrotoxicity.
Drugs that can cause hyperkalemia: simultaneous use of diclofenac with potassium-sparing diuretics, cyclosporine, tacrolimus or trimethoprim may lead to an increase in the concentration of potassium in the blood serum (if this combination of drugs is used, this indicator should be regularly monitored).
Antibacterial agents - quinolone derivatives: There are isolated reports of the development of seizures in patients receiving concomitant quinolone derivatives and diclofenac.
Anticoagulants and antiplatelet agents: It is necessary to combine diclofenac with caution with drugs of these groups due to the risk of bleeding. Although clinical studies have not established the effect of diclofenac on the action of anticoagulants, there are isolated reports of an increased risk of bleeding in patients taking this combination of drugs. Therefore, in the case of this combination of drugs, regular and careful monitoring of patients is recommended. Like other NSAIDs, diclofenac in high doses can reversibly inhibit platelet aggregation.
Acetylsalicylic acid reduces the concentration of diclofenac in the blood.
NSAIDs and corticosteroids: simultaneous systemic use of diclofenac and other systemic NSAIDs or corticosteroids may increase the incidence of side effects (particularly from the gastrointestinal tract).
Selective serotonin reuptake inhibitors (SSRIs): simultaneous use of diclofenac and drugs from the SSRI group increases the risk of gastrointestinal bleeding.
Hypoglycemic drugs: Clinical studies have shown that when used together, diclofenac does not affect the effectiveness of hypoglycemic drugs. However, there are isolated reports of the development of both hypoglycemia and hyperglycemia in such cases, which required changing the dose of hypoglycemic drugs during diclofenac therapy. Therefore, during the combined use of diclofenac and hypoglycemic drugs, it is recommended to monitor blood glucose concentrations.
Phenytoin: with simultaneous use of phenytoin and diclofenac, it is necessary to monitor the concentration of phenytoin in the blood plasma due to a possible increase in its systemic effect.
Tacrolimus: increased nephrotoxicity is possible when used simultaneously with diclofenac.
Cefamandole, cefoperazone, cefotetan, valproic acid And plicamycin increase the incidence of hypoprothrombinemia.
The effect of diclofenac on the synthesis of prostaglandins in the kidneys may increase the toxic effect gold preparations. Simultaneous use with ethanol, colchicine, corticotropin and preparations of St. John's wort increases the risk of bleeding in the gastrointestinal tract.
Potent inhibitors of the CYP2C9 isoenzyme: Caution should be exercised when co-prescribing diclofenac and potent inhibitors of the CYP2C9 isoenzyme (such as voriconazole) due to the possible increase in diclofenac serum concentrations and increased systemic effects.
special instructions
In order to reduce the risk of adverse events, the drug should be used at the lowest effective dose for the shortest period necessary to relieve symptoms.
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 significant risk factors for cardiovascular events (eg hypertension, hyperlipoproteinemia, diabetes mellitus and smoking), treatment with diclofenac-containing products should only be initiated after careful evaluation and analysis.
Because of the important role of prostaglandins in maintaining renal blood flow, special caution should be exercised when prescribing the drug to patients with cardiac or renal failure, hypertension, elderly patients, patients taking diuretics or other drugs that affect renal function, and patients with For some reason, there is a decrease in circulating blood volume (for example, after extensive surgery). If diclofenac is prescribed in such cases, monitoring of renal function is recommended as a precaution. After cessation of drug therapy, normalization of renal function indicators to initial values is usually observed.
When using diclofenac, phenomena such as bleeding or ulceration/perforation of the gastrointestinal tract, in some cases fatal, were observed. These phenomena may occur at any time when using the drug in patients with or without previous symptoms and a history of serious gastrointestinal diseases. In elderly patients, such complications can have serious consequences. If patients receiving diclofenac develop bleeding or ulceration of the gastrointestinal tract, the drug should be discontinued. To reduce the risk of toxic effects on the gastrointestinal tract, the drug should be used in the minimum effective dose for the shortest possible time, especially for patients with ulcerative lesions of the gastrointestinal tract, especially complicated by a history of bleeding or perforation, as well as elderly patients.
Patients with an increased risk of developing gastrointestinal complications, as well as those receiving therapy with low doses of acetylsalicylic acid or other drugs that can increase the risk of damage to the gastrointestinal tract, should take gastroprotectors.
Patients with a history of gastrointestinal disorders, especially the elderly, should report all symptoms of the digestive system to their doctor.
When carrying out long-term therapy, it is necessary to monitor liver function, peripheral blood patterns, and stool analysis for occult blood.
With long-term use of diclofenac, there may be an increase in the activity of one or more liver enzymes. If liver dysfunction persists or 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 diclofenac can develop without prodromal phenomena.
Caution must be exercised when using diclofenac in patients with hepatic porphyria, since the drug can provoke attacks of porphyria. Diclofenac can reversibly inhibit platelet aggregation, therefore, in patients with hemostasis disorders with long-term use, careful monitoring of relevant laboratory parameters is necessary.
In patients with bronchial asthma, seasonal allergic rhinitis, swelling of the nasal mucosa (including nasal polyps), chronic obstructive pulmonary disease, chronic respiratory tract infections (especially those associated with allergic rhinitis-like symptoms), as well as in patients with allergies to other medications (rash, itching, urticaria) when prescribing diclofenac, special care should be taken (preparedness for resuscitation measures).
Severe, in some cases fatal, skin reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, have been very rarely reported with the use of diclofenac. The highest risk and incidence of severe dermatological reactions were observed in the first month of treatment with diclofenac. If patients receiving the drug develop the first signs of skin rash, damage to the mucous membranes or other symptoms of hypersensitivity, diclofenac should be discontinued.
The anti-inflammatory effect of NSAIDs, including diclofenac, may complicate the diagnosis of infectious processes.
Due to the negative effect on fertility, the drug is not recommended for women planning pregnancy. In patients with infertility (including those undergoing examination), it is recommended to discontinue the drug.
Impact on the ability to drive vehicles and operate machinery
Instructions for use Diclofenac
Buy Diclofenac sup 50mg
Dosage forms
rectal suppositories 50 mg
Manufacturers
GlaxoSmithKline Pharmaceuticals S.A. (Poland)
Group
Anti-inflammatory drugs - phenylacetic acid derivatives
Compound
The active substance is diclofenac sodium.
International nonproprietary name
Diclofenac
Synonyms
Voltaren, Voltaren Akti, Voltaren Ofta, Voltaren Rapid, Voltaren Emulgel, Diklak, Diklak Lipogel, Diklo-F, Diclobene, Diclovit, Diclogen, Diclonate P, Dicloran, Diclofenac sodium, Diclofenac retard, Diclofenac retard Obolenskoye, Diclofenac Sandoz, Diclofenac Stada, Diclofenac-Acos, Diclofenac-Acri, Diclofenac-Acri retard, Diclofenac-Altfarm, Diclofenac-MFF, Diclofenac-Ratiopharm, Diclofenac-UBF, Diclofenac-FPO, Diclofenac-Eskom, Diclofenacol, Dorosan, Naklofen, Naklofen Duo, Naklofen SR, Ortofen , Ortofer, Ortoflex, Panamor AT-50, Rapten Duo, Rapten rapid
pharmachologic effect
Non-steroidal anti-inflammatory drug. Inhibits the biosynthesis of prostaglandins. Prostaglandins play a major role in the development of the main symptoms of inflammation (swelling, temperature, pain). In rheumatic diseases, anti-inflammatory and analgesic properties cause a reduction in symptoms such as pain at rest and with movement, morning stiffness, and swelling of the joints. It has a pronounced analgesic effect for moderate and severe pain of a non-rheumatic nature. In inflammatory processes that occur after operations and injuries, it quickly relieves both spontaneous pain and pain during movement, and reduces inflammatory swelling at the wound site. In primary dysmenorrhea, it relieves pain and reduces bleeding. Suppresses platelet aggregation. With long-term use it has a desensitizing effect. In ophthalmology - eliminates miosis, reduces the likelihood of developing cystoid macular edema during cataract surgery. Absorption is rapid and complete; food slows down the rate of absorption. The maximum plasma concentration is achieved after 1-2 hours. As a result of the delayed release of the active substance, the maximum concentration of extended-release diclofenac in the blood plasma is lower than that formed when the short-acting drug is administered. With intramuscular administration, maximum plasma concentration is achieved after 10-20 minutes, with rectal administration - after 30 minutes. Bioavailability - 50%. Communication with blood plasma proteins is over 99%. When applied topically, the active substance is partially absorbed through the skin. When instilled into the eye, the onset of maximum concentration in the cornea and conjunctiva is 30 minutes, penetrates into the anterior chamber of the eye, and does not penetrate into the systemic circulation in therapeutically significant concentrations. Does not cumulate. It is excreted in the form of metabolites through the kidneys and bile.
Indications for use
Inflammatory joint diseases (rheumatoid arthritis, rheumatism, ankylosing spondylitis, chronic gouty arthritis), degenerative diseases (deforming osteoarthritis, osteochondrosis), lumbago, sciatica, neuralgia, myalgia, diseases of extra-articular tissues (tenosynovitis, bursitis, rheumatic soft tissue lesions), post-traumatic pain syndromes accompanied by inflammation, postoperative pain, acute attack of gout, primary dysmenorrhea, adnexitis, migraine attacks, renal and hepatic colic, infections of the ENT organs, residual effects of pneumonia. Locally - injuries of tendons, ligaments, muscles and joints, localized forms of soft tissue rheumatism. In ophthalmology - non-infectious conjunctivitis, post-traumatic inflammation after penetrating and non-penetrating wounds of the eyeball, pain syndrome when using an excimer laser, during surgery for removal and implantation of the lens (pre- and postoperative prevention of miosis, cystoid edema of the optic nerve).
Contraindications
Hypersensitivity, hematopoietic disorders, stomach and duodenal ulcers, aspirin-induced bronchial asthma, children (up to 6 years), last trimester of pregnancy.
Side effect
From the gastrointestinal tract: gastralgia, nausea, vomiting, diarrhea, stomach cramps, dyspepsia, flatulence, anorexia. From the side of the central nervous system: headache, dizziness, fatigue. From the hematopoietic organs: thrombocytopenia, leukopenia, agranulocytosis, hemolytic anemia. There is a burning sensation at the site of intramuscular injection. When using suppositories - local irritation. Skin: skin rashes, urticaria, itching, burning. With long-term use and/or application to large surfaces, systemic side effects due to resorptive effects occur. Immediately after instillation into the eyes - a passing burning sensation and/or blurred vision.
Interaction
Increases the blood concentration of lithium, digoxin, indirect anticoagulants, oral antidiabetic drugs (both hypo- and hyperglycemia are possible), quinolone derivatives. Increases the toxicity of methotrexate, cyclosporine, the likelihood of developing side effects of glucocorticoids (gastrointestinal bleeding), the risk of hyperkalemia against the background of potassium-sparing diuretics, reduces the effect of diuretics. Plasma concentrations decrease with the use of acetylsalicylic acid.
Directions for use and dosage
Rectally, 1 sup. (100 mg) per day or 2 supp. (50 mg) per day. The daily dose does not exceed 150 mg.
Overdose
When taken orally: Symptoms: dizziness, headaches, hyperventilation, clouding of consciousness, in children - myoclonic convulsions, disorders of the gastrointestinal tract, liver and kidney functions. Treatment: symptomatic therapy.
special instructions
In order to quickly achieve the desired effect, oral forms of diclofenac are taken 30 minutes before meals. After removing contact lenses, instillation is performed after 5 minutes. Preparations for topical use are applied only to intact areas of the skin. With long-term treatment, periodic examination of the blood count and liver function, and stool analysis for occult blood are necessary. In the first 6 months of pregnancy it should be used according to strict indications and in the lowest dosage. Due to a decrease in reaction speed, driving vehicles and operating machinery is not recommended. Restrictions on use. Impaired liver and kidney function, heart failure, porphyria, work requiring increased attention, pregnancy, breastfeeding (breastfeeding should be avoided).
Storage conditions
In a dry place, protected from light, at room temperature.
