NSAIDs, a derivative of phenylacetic acid. Has a pronounced anti-inflammatory, analgesic and mild antipyretic effect. The mechanism of action is associated with inhibition of COX - basic enzyme of arachidonic acid metabolism, which is the precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. Analgesic effect is due to two mechanisms: peripheral (indirect, via inhibition of prostaglandin synthesis) and Central (due to inhibition of prostaglandin synthesis in the Central and peripheral nervous system).
Inhibits synthesis of proteoglycan in cartilage.
In rheumatic diseases reduces joint pain at rest and during movement, as well as morning stiffness and swelling of the joints, helps to increase range of motion. Reduces post-traumatic and postoperative pain, and inflammatory edema.
Inhibits platelet aggregation. Long-term use has a desensitizing effect.
The local application in ophthalmology reduces swelling and pain in inflammatory processes of non-infectious etiology.
Once inside absorbed from the digestive tract. Eating slows the rate of absorption, extent of absorption is not changed. About 50% of the active substance is metabolized in the "first pass" through the liver. In a rectal absorption is slower. The time to reach Cmax in plasma after ingestion is 2-4 hours depending on the dosage form, after rectal administration - 1 h in/m introduction - 20 minutes the Concentration of active substance in plasma is linearly dependent on the magnitude of the applied dose.
Do not cumulate. Linking plasma protein is 99.7% (mainly to albumin). Penetrates into synovial fluid, Cmax is achieved in 2-4 h later than in plasma.
Is largely metabolized with the formation of several metabolites, including two 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 h, from the synovial fluid is 3-6 h. Approximately 60% of the dose is excreted as metabolites by the kidneys, less than 1% excreted in the urine unchanged, and the remainder is excreted as metabolites in the bile. Dosage
For oral administration for adults, a single dose is 25-50 mg 2-3 times/day. The frequency of administration depends on the dosage form, severity of the disease and is 1-3 times/day, rectally - 1 times/day. For the treatment of acute conditions or edema worsening chronic use b/m in a dose of 75 mg.
For children over 6 years and adolescents daily dose of 2 mg/kg.
Topically applied dose of 2-4 g (depending on the area affected area) on the affected area 3-4 times per day.
When used in ophthalmology frequency and duration of administration are determined individually.
Maximum daily dose for adults when administered at 150 mg/day.
Together with the use of NSAID antihypertensive drugs may weaken their actions.
There are few reports on the occurrence of seizures in patients simultaneously taking NSAIDs and antibiotics quinoline series.
Together with the use of corticosteroids increases the risk of side effects from the digestive system.
While the use of diuretics may decrease diuretic effect. With the simultaneous use of potassium-sparing diuretics may increase the concentration of potassium in the blood.
In concurrent use with other NSAIDs may increase the risk of side effects.
There have been reports of the development of hypoglycemia or hyperglycemia in patients with diabetes who used diclofenac simultaneously with hypoglycemic drugs.
Together with the use of acetylsalicylic acid may reduce the concentration of diclofenac in plasma.
In concurrent use may increase the concentration of digoxin, lithium and phenytoin in plasma.
The absorption of diclofenac from the digestive tract is reduced with concomitant use of cholestyramine, to a lesser extent with colestipol.
In concurrent use may increase the concentration of methotrexate in plasma and increased its toxicity.
Simultaneous use of 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 side effects metabolite of morphine, including respiratory depression.
While the use of pentazocine described a case of development of large-convulsive seizure; with rifampicin - may decrease the concentration of diclofenac in plasma; with Ceftriaxone - increases excretion of Ceftriaxone with bile; with cyclosporine - may increase cyclosporine nephrotoxicity. Pregnancy and lactation
Use in pregnancy and lactation is possible in cases where the potential benefit to the mother outweighs the potential risk to the fetus or newborn.
Digestive system: nausea, vomiting, anorexia, pain and discomfort in the epigastrium, flatulence, constipation, diarrhea; in some cases - erosive-ulcerative lesions, bleeding and perforation of the gastrointestinal tract; rare - violation of the liver. When rectally administered in a few cases it was noted inflammation of the colon bleeding, exacerbation of ulcerative colitis.
Of the Central nervous system and peripheral nervous system: dizziness, headache, agitation, insomnia, irritability, fatigue; rarely, paresthesia, visual disturbances (blurred, double vision), tinnitus, sleep disorders, convulsions, irritability, tremor, mental disorders, depression.
On the part of hematopoiesis: rarely - anemia, leukopenia, thrombocytopenia, agranulocytosis.
Urinary system: rare - violation of the kidney; in predisposed patients swelling.
Dermatological reactions: rare - hair loss.
Allergic reactions: skin rash, itching; when applied in the form of eye drops - itching, redness, photosensitivity.
Local reactions: in in/m introduction possible burning, in some cases, the formation of infiltration, abscess, necrosis of adipose tissue; by rectal administration may be local irritation, the appearance of mucous discharge mixed with blood, painful defecation; when applied topically in rare cases, itching, redness, rash, burning; the local application in ophthalmology possible transient burning sensation and/or temporary blurred vision immediately after instillation.
With long-term exterior use and/or installation of large body surface are possible systemic side effects due to resorptive action of diclofenac.
Articular syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout), degenerative and chronic inflammatory diseases of the musculoskeletal system (osteochondrosis, osteoarthritis, periarteritis), post-traumatic inflammation of soft tissues and the musculoskeletal system (sprains, contusions). Pain in the spine, neuralgia, myalgia, arthralgia, pain and inflammation after surgery and trauma, pain gout, migraine, algomenorrhea, pain in adnexitis, proctitis, colic (biliary and renal), pain syndrome in infectious-inflammatory diseases of ENT-organs.
For local use: inhibition of Misa during the operation for cataract, prevention of cystoid macular edema associated with removal and lens implantation, inflammation of the eye non-infectious nature, posttraumatic inflammatory process in penetrating and non-penetrating wounds of the eyeball.
Erosive-ulcerative lesions of the gastrointestinal tract in acute phase, "aspirin triad", a violation of hematopoiesis unknown etiology, hypersensitivity to diclofenac or components of the dosage form, or other NSAIDs.
With caution used in diseases of liver, kidney, gastrointestinal disorder, dyspepsia, asthma, hypertension, heart failure, immediately after a serious surgery, and in elderly patients.
When referring to the history of allergic reactions to NSAIDs and sulfites diclofenac used only in emergency cases. During treatment requires systematic monitoring of the liver and kidney, peripheral blood picture.
Not recommended for rectal application in patients with diseases of the anorectal area or anorectal bleeding disorder. Externally should be applied only to intact skin.
Avoid contact of diclofenac in the eye (except eye drops) or on mucous membranes. Patients who use contact lenses must apply eye drops no earlier than 5 min after removing the lenses.
Not recommended for use in children under 6 years.
During the period of treatment dosage forms for systemic use is not recommended the use of alcohol.
Effects on ability to drive vehicles and management mechanisms
During the period of treatment may reduce the speed of psychomotor reactions. With deteriorating vision clarity after applying eye drops you should not drive or engage in other potentially hazardous activities.
When kidney functions
With caution used in kidney diseases in anamnesis. When human liver
With caution used in liver diseases in history.
Use in the elderly
With extreme use caution in elderly patients.
Use in children
Not recommended for use in children under 6 years.
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