Diclofenac retard Obolenskoye, 100 mg 20 pcs
Diclofenac retard is a nonsteroidal anti-inflammatory drug (NSAID), a phenylacetic acid derivative; it has anti-inflammatory, analgesic and antipyretic effects.
Inhibiting cyclooxygenase 1 and 2 (COX1 and COX2) indiscriminately, it disrupts arachidonic acid metabolism, reduces the amount of prostaglandins in the inflammation focus. It is most effective for pain of inflammatory nature. Like all NSAIDs, the drug has anti-aggregant effect. In rheumatic diseases, anti-inflammatory and analgesic effect of diclofenac contributes to a significant reduction in the severity of pain, morning stiffness, joint swelling, which improves the functional state of the joint. In case of injuries, in post-operative period diclofenac reduces pain and inflammatory edema.
Absorption is rapid and complete. Food slows the rate of absorption by 1-4 h and reduces the maximum concentration (Cmax) by 40%.
As a result of delayed release of the drug, Cmax in plasma is lower than that produced by short-acting drugs (drugs); however, it remains high for a long time after administration. Cmax is 0.5-1.0 mcg/ml, time to reach maximum plasma concentration (TCmax) is 5 h after administration of 100 mg long-acting tablets.
There is no change in pharmacokinetics of diclofenac on repeated administration. It does not cumulate if the recommended interval between meals is observed.
The bioavailability is 50%. Binding with plasma proteins is more than 99% (most of it is bound with albumin). It penetrates into breast milk and synovial fluid; Cmax in synovial fluid is observed 2-4 hours later than in plasma. Period of half-life (T1/2) from synovial fluid – 3-6 h (concentration of the drug in synovial fluid 4-6 h after administration is higher than in plasma and stays higher during 12 h).
50% of the active substance is metabolized during the “first passage” through the liver. Metabolism occurs as a result of multiple or single hydroxylation and conjugation with glucuronic acid. The enzyme system of cytochrome P 450 CYP2C9 is involved in metabolism of the drug. The pharmacological activity of the metabolites is less than that of diclofenac.
The systemic clearance is 206 ml/min. T1/2 from plasma is 1-2 hours. 60% of the administered dose is excreted as metabolites through the kidneys; less than 1% is excreted unchanged, the rest of the dose is excreted as metabolites in the bile.
In patients with significant renal insufficiency (creatinine clearance (CK) less than 10 ml/min) excretion of metabolites in bile is increased, while there is no increase of their concentrations in blood.
In patients with chronic hepatitis or compensated liver cirrhosis pharmacokinetic parameters are not changed.
Diclofenac penetrates into the breast milk.
Osteoarthritis, Bursitis, Arthritis, Pain, Swelling after injuries and operations, Pain after injuries and operations, Adnexitis, Sciatica, Rheumatoid arthritis, Tendon inflammation, Pain in neck, Periarthritis, Myalgia (pain in muscles), Back pain, Neuralgia, Pain in joints (arthralgia), Arthrosis, Painful menstruation (algodysmenorrhea), Lumbago
Diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Behterev’s disease); gouty arthritis; rheumatic soft tissue disease; osteoarthritis of peripheral joints and spine, including radicular syndrome; tendovaginitis; bursitis).
Pain syndrome of mild to moderate severity: neuralgia, myalgia, lumboishyalgia, post-traumatic pain syndrome accompanied by inflammation, post-operative pain, headache, migraine, algodysmenorrhea, adnexitis, proctitis, toothache.
In the complex treatment of infectious and inflammatory diseases of the ear, throat, nose with a pronounced pain syndrome (pharyngitis, tonsillitis, otitis).
The drug Diclofenac retard is intended as symptomatic therapy, reducing pain and inflammation at the time of use, has no effect on the progression of the disease.
diclofenac sodium 100 mg
How to take, the dosage
Adults are recommended to take 50 to 150 mg of diclofenac daily divided into 2-3 separate doses.
In the absence of other prescriptions, it is recommended to take 100-150 mg daily as initial therapy and 75-100 mg divided into 2-3 separate doses for long-term therapy.
Children over 6 years of age are prescribed diclofenac at a dose of 2 mg/kg body weight, with the daily dose also divided into several doses.
In concomitant use of the drug Diclofenac with digoxin, phenytoin or lithium preparations, an increase in plasma concentrations of these drugs is possible; with diuretics and hypotensive agents – the effect of these drugs may decrease; with potassium-saving diuretics – hyperkalemia may develop; with acetylsalicylic acid – decrease in plasma concentration of diclofenac and increased risk of side effects.
Diclofenac may increase toxic effect of cyclosporine on kidneys.
Diclofenac may cause hypo- or hyperglycemia, therefore concomitant use with hypoglycemic agents requires control of blood glucose concentration.
When using methotrexate for 24 hours before or after taking Diclofenac it is possible to increase the concentration of methotrexate and increase its toxic effect.
When concomitant use with anticoagulants regular monitoring of blood clotting is required.
With special caution is prescribed in severe renal, hepatic and cardiac insufficiency. Prolonged use of Diclofenac sodium may cause renal, hepatic and gastrointestinal disorders. Patients in whom deterioration of liver function is observed during the use of Diclofenac Sodium, or in whom increased liver enzymes activity is recorded, should stop using the drug.
Patients should take Diclofenac after meals to avoid irritation in the gastrointestinal tract.
The use of Diclofenac sodium requires caution when driving and operating machinery because of its effect on the central nervous system.
Errotic and ulcerative lesions of the gastrointestinal tract in the acute phase, “aspirin triad”, blood disorders of unclear etiology, hypersensitivity to diclofenac and components of the drug formulation used, or other NSAIDs.
Digestive system disorders: nausea, vomiting, epigastric pain, anorexia, flatulence, constipation, gastritis up to erosive with bleeding, increased transaminase activity, drug-induced hepatitis, pancreatitis.
Urinary system disorders: interstitial nephritis.
CNS disorders: headache, dizziness, disorientation, agitation, insomnia, irritability, fatigue, aseptic meningitis.
Respiratory system: bronchospasm.
Hematopoietic system disorders: anemia, thrombocytopenia, leukopenia, agranulocytosis.
Dermatological reactions: exanthema, erythema, eczema, hyperemia, erythrodermia, photosensitization.
Allergic reactions: erythema multiforme, Lyell’s syndrome, Stevens-Johnson syndrome, anaphylactic reactions, including shock.
Local reactions: burning, infiltrate formation, necrosis of adipose tissue possible at the injection site.
Others: fluid retention in the body, edema, increased BP.
In acute Diclofenac poisoning treatment mainly consists of supportive and symptomatic measures.
Gastric lavage is used to reduce absorption.
Diclofenac should not be taken during pregnancy; it is prescribed only in emergency cases. It is excreted in breast milk, so it should not be taken while breastfeeding.
Diclac, Diclofenac-Teva, Diclo-F, Orthofen, Diclovit, Voltaren, Voltaren Emulsgel, Diclofenac, Voltaren Patch, Dicloran Plus, Orthofen, Diclofenac-Altfarm, Diclofenac-SOLofarm, Dialrapid
|Conditions of storage|
In a dry, light-protected place at a temperature below 25 °C
Obolenskoe FP JSC, Russia
enteric soluble tablets
Obolenskoe FP JSC
Buy Diclofenac retard Obolenskoye, 100 mg 20 pcs with delivery to USA, UK, Europe and over 120 other countries.