Diclofenac retard, 100 mg 20 pcs

Pharmgroup:

NSAIDs.

Pharmic action:

Diclofenac retard is a non-steroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid; has anti-inflammatory, analgesic and antipyretic effects.
Indiscriminately inhibiting cyclooxygenase 1 and 2 (COX1 and COX2), disrupts arachidonic acid metabolism, reduces the number of prostaglandins in the inflammation. 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 swelling.

Pharmacokinetics:

Absorption is fast and complete. Food slows the rate of absorption by 1-4 h and reduces the maximum concentration (Cmax) by 40%.

As a result of the 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. In patients with severe renal insufficiency (creatinine clearance (CK) less than 10 ml/min) the excretion of metabolites in bile is increased, while there is no increase of their concentration in blood.

In patients with chronic hepatitis or compensated liver cirrhosis pharmacokinetic parameters do not change.

Diclofenac penetrates into the breast milk.

Indications

Diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Behterev’s disease); gouty arthritis; rheumatic soft tissue lesion; 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.

Active ingredient

Composition

Composition: per 1 sustained release tablet of Diclofenac retard, coated with an enteric-soluble shell:

– active ingredient:

diclofenac sodium 100 mg;

– excipients:

[hypromellose (hydroxypropyl methylcellulose),

hyetellose (hydroxyethylcellulose),

collidone SR [polyvinyl acetate 80%, povidone 19%, sodium lauryl sulfate 0.8%, silicon dioxide 0.2%],

sodium alginate, microcrystalline cellulose, magnesium stearate].

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.

Interaction

In concomitant use of the drug Diclofenac with digoxin, phenytoin or lithium drugs may increase plasma concentrations of these drugs; with diuretics and hypotensive agents – possible decrease in the effect of these drugs; with potassium-saving diuretics – possible development of hyperkalemia; with acetylsalicylic acid – decrease of diclofenac concentration in blood plasma and increased risk of side effects.

Diclofenac may increase the toxic effects of cyclosporine on the 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.

Special Instructions

Caution should be exercised when using the drug concomitantly with other NSAIDs.

Impact on driving and operating machinery

Because of the fact that when using the drug in high doses, side effects such as dizziness and fatigue may develop, in some cases, the ability to drive or operate other moving objects is impaired. These effects worsen with concomitant use of alcohol.

Contraindications

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.

Side effects

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.

Overdose

Symptoms: dizziness, headache, hyperventilation of the lungs, blurred consciousness, vomiting, gastrointestinal bleeding, diarrhea, tinnitus, seizures, in significant overdose – acute renal failure, hepatotoxic effect.
Treatment: gastric lavage, administration of activated charcoal. Symptomatic therapy is aimed at elimination of increased BP, impaired renal function, seizures, gastrointestinal irritation, respiratory depression. Forced diuresis, hemodialysis are ineffective (due to significant binding to proteins and intense metabolism).

Similarities