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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 an important 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 (due to inhibition of prostaglandin synthesis in central and peripheral nervous system).
In vitro in concentrations equivalent to those achieved by treating patients does not inhibit cartilage proteoglycan biosynthesis.
In rheumatic diseases, it reduces joint pain at rest and on movement, as well as morning stiffness and joint swelling, and helps increase range of motion. It reduces post-traumatic and post-operative pain, as well as inflammatory swelling.
In case of post-traumatic and post-operative inflammatory phenomena it quickly relieves pain (occurring both at rest and during movement), reduces inflammatory swelling and edema of the postoperative wound.
Inhibits platelet aggregation. During long-term use it has a desensitizing effect.
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 "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. Approximately 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
Hypersensitivity to diclofenac and excipients of the drug used; "aspirin triad" (attacks of bronchial asthma, urticaria and acute rhinitis while taking acetylsalicylic acid or other NSAIDs); erosive-ulcerative lesions of the GI tract in the acute phase; proctitis (only for suppositories); pregnancy (for intravenous administration); III trimester of pregnancy (for oral and rectal administration); children and teenagers under 18 years old (for intravenous administration and for sustained-action dosage forms).
With caution: suspected GI disease; history of GI bleeding and ulcer perforation (especially in elderly patients), Helicobacter pylori infections, ulcerative colitis, Crohn's disease, dysfunction; mild to moderate hepatic dysfunction, hepatic porphyria (diclofenac can provoke porphyria attacks); in patients with bronchial asthma, seasonal allergic rhinitis, nasal mucosal edema (incl. ч. with nasal polyps), COPD, chronic infectious respiratory diseases (especially associated with allergic rhinitis-like symptoms); cardiovascular diseases (including CHD, cerebrovascular disease, compensated heart failure, peripheral vascular disease); renal dysfunction, including chronic renal failure (CK 30-60 ml/min); dyslipidemia/hyperlipidemia; diabetes mellitus; arterial hypertension; significant reduction of the BOD of any etiology (for example, in periods before and after massive surgical interventions); hemostasis disorders; risk of thrombosis (incl. patients who receive medications that increase the risk of gastrointestinal bleeding, including systemic GBS (including prednisolone); patients who receive medications that increase the risk of gastrointestinal bleeding, including systemic GBS (including prednisolone); patients who receive medications that increase the risk of gastrointestinal bleeding (e.g., diclofenac). anticoagulants (including warfarin), antiplatelet agents (including clopidogrel, acetylsalicylic acid), selective serotonin reuptake inhibitors (including citalopram, fluoropolymer, and acetylsalicylic acid) and inhibitors of gastrointestinal bleeding. including citalopram, fluoxetine, paroxetine, sertraline); concomitant treatment with diuretics or other drugs that can impair renal function; during treatment of patients who smoke or abuse alcohol; when administered by injection in patients with bronchial asthma due to the risk of exacerbation of the disease (because sodium bisulfite contained in some dosage forms for injection can cause severe hypersensitivity reactions).
Administration during pregnancy and lactation
There is insufficient data on the safety of diclofenac use in pregnant women. Therefore, administration in I and II trimesters of pregnancy is possible only in cases when the expected benefit to the mother exceeds the potential risk to the fetus. Diclofenac (as other inhibitors of prostaglandin synthesis) is contraindicated in the III trimester of pregnancy (suppression of uterine contractility and premature closure of the fetal arterial duct may occur).
Despite the fact that diclofenac is excreted with breast milk in small amounts, use during lactation (breastfeeding) is not recommended. If it is necessary to use during lactation, breastfeeding should be stopped.
Since diclofenac (like other NSAIDs) may have an adverse effect on fertility, it is not recommended for women planning to become pregnant.
Patients undergoing examination and treatment for infertility should discontinue the drug.
Administration in patients with liver dysfunction
It is used with special caution in case of liver diseases in the anamnesis.
Administration in patients with impaired renal function
Use with special caution in patients with a history of renal disorders.
Administration in children
It is not recommended to use in children under 6 years of age.
Active ingredient indications of Voltaren
Inflammatory and degenerative musculoskeletal system diseases, including Rheumatoid, juvenile and chronic arthritis, ankylosing spondylitis and other spondyloarthropathies, osteoarthritis, gouty arthritis, bursitis, tendovaginitis, spine pain syndrome (lumbago, sciatica, ossalgia, neuralgia, myalgia, arthralgia, radiculitis); Post-traumatic postoperative pain syndrome with inflammation (e.g., in dentistry and orthopedics); algodysmenorrhea; pelvic inflammatory processes (including adnexitis); and including adnexitis); infectious inflammatory diseases of ENT organs with a pronounced pain syndrome (as part of complex therapy): pharyngitis, tonsillitis, otitis media.
Isolated fever is not an indication for using the drug.
The drug is intended for symptomatic therapy, reduction of pain and inflammation at the time of use, does not affect the progression of the disease.
The optimal dosing regimen is determined by the doctor. Should be strictly in accordance with the drug used dosage form of a particular drug indications for use and the dosing regimen.
The dose is chosen individually, it is recommended to use the drug in the lowest effective dose, with the shortest possible treatment period.