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Voltaren SR (Diclofenac)
NSAID, a derivative of phenylacetic acid. It has a pronounced anti-inflammatory, analgesic and moderate antipyretic effect. The mechanism of action is associated with inhibition of COX activity - the main enzyme of arachidonic acid metabolism, which is a precursor of prostaglandins that play a major role in the pathogenesis of inflammation, pain and fever. Analgesic effect is due to two mechanisms:
- peripheral (indirectly, through inhibition of prostaglandin synthesis) and central (through inhibition of prostaglandin synthesis in the central and peripheral nervous system).
Inhibits the synthesis of proteoglycan in cartilage.
In rheumatic diseases it reduces joint pain at rest and during movement, as well as morning stiffness and joint swelling, helps increase range of motion. Reduces post-traumatic and post-operative pain, as well as inflammatory edema.
Inhibits platelet aggregation. Has a desensitizing effect when used for a long time.
When used topically in ophthalmology it reduces edema and pain in inflammatory processes of non-infectious etiology.
After oral administration it is absorbed from the gastrointestinal tract. Food intake slows down the rate of absorption, the degree of absorption does not change. About 50% of the active substance is metabolized during the "first passage" through the liver. In rectal administration absorption is slower. Time of reaching Cmax in plasma after oral administration is 2-4 hours, depending on the applied dosage form, after rectal administration - 1 hour, i/m introduction - 20 minutes. Plasma concentration of the active substance is linearly related to the dose administered.
It does not cumulate. Binding to plasma proteins is 99.7% (predominantly to albumin). Permeates in synovial fluid, Cmax is reached 2-4 hours later than in plasma.
It is largely metabolized with the formation of several metabolites, among 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 h, from synovial fluid - 3-6 h. About 60% of the dose is excreted as metabolites by the kidneys, less than 1% is excreted unchanged in the urine, the rest is excreted as metabolites in the bile.
Contraindications to use
Gastrointestinal erosive-ulcerative lesions in acute phase, "aspirin triad", hematopoiesis disorders of unknown etiology, hypersensitivity to diclofenac and components of the dosage form, or other NSAIDs.
Application during pregnancy and lactation
Application during pregnancy and lactation is possible in cases when the expected benefits for a mother exceed the potential risk for a fetus or a newborn.
Administration in liver dysfunction
It is used with special caution in case of liver diseases in anamnesis.
Administration in impaired renal function
Particular caution is used in patients with a history of renal impairment.
Administration in elderly patients
Special caution should be exercised when used in elderly patients.
Administration in children
It is not recommended to use in children under 6 years of age.
Joint syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout), degenerative and chronic inflammatory diseases of the musculoskeletal system (osteochondrosis, osteoarthritis, periarthropathy), post-traumatic inflammation of soft tissue and musculoskeletal system (sprains, bruises). Spinal pain, neuralgia, myalgia, arthralgia, pain syndrome and inflammation after operations and injuries, pain syndrome with gout, migraine, algodysmenorrhea, pain syndrome with adnexitis, proctitis, colic (biliary and renal), pain syndrome with infectious and inflammatory diseases of the ENT organs.
For topical use:
- inhibition of miosis during cataract surgery, prevention of cystoid macular edema associated with lens removal and implantation, ocular inflammatory processes of non-infectious nature, post-traumatic inflammatory process in penetrating and non-penetrating wounds of the eyeball.
Oral administration for adults is a single dose of 25-50 mg 2-3 times a day. The frequency of administration depends on the dosage form used and the severity of the disease and is 1-3 times a day, rectally - once a day. To treat acute conditions or to relieve exacerbation of chronic process, a 75 mg dose is administered in m/m.
For children over 6 years of age and adolescents the daily dose is 2 mg/kg.
Outwardly it is used in a dose of 2-4 g (depending on the painful area) to the affected area 3-4 times per day.
When used in ophthalmology the frequency and duration of administration are determined individually.
Maximum daily dose for adults when administered orally is 150 mg/day.