Diclofenac retard- Acrichin pills 100mg, 20pcs

Composition

Active ingredient:  

diclofenac sodium 100 mg

Pharmacological action

Diclofenac retard is a nonsteroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid; it has anti-inflammatory, analgesic and antipyretic effects.

Indiscriminately inhibiting cyclooxygenase 1 and 2 (COX 1 and COX 2), disrupts the metabolism of arachidonic acid, reduces the amount of prostaglandins in the focus of inflammation. It is most effective for inflammatory pain. Like all NSAIDs, the drug has an antiplatelet effect. In rheumatic diseases, the anti-inflammatory and analgesic effect of diclofenac significantly reduces the severity of pain, morning stiffness, and joint swelling, which improves the functional state of the joint. In case of injuries, in the postoperative period, diclofenac reduces pain and inflammatory edema.

Pharmacokinetics: Absorption is rapid and complete. Food slows down the rate of absorption by 1-4 hours 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 created by the introduction of short-acting drugs; however, it remains high for a long time after use. Cmax – 0.5-1.0 mcg / ml, the time to reach the maximum concentration in blood plasma (TCmax) – 5 hours after taking 100 mg of long-acting tablets.

There were no changes in the pharmacokinetics of diclofenac during repeated use. It does not accumulate if the recommended interval between meals is observed. Bioavailability – 50%. Binding to plasma proteins is more than 99% (most of them are bound to albumins). Penetrates into breast milk, synovial fluid; Cmax in synovial fluid is observed 2-4 hours later than in plasma. The half-life (T 1/2) from synovial fluid is 3-6 hours (concentrations of the drug in synovial fluid 4-6 hours after its use are higher than in plasma, and remain higher for another 12 hours).

50% of the Active ingredient is metabolized during the” first pass ” through the liver. Metabolism occurs as a result of repeated or single hydroxylation and conjugation with glucuronic acid. The cytochrome P450 CYP2C9 enzyme system is involved in drug metabolism. The pharmacological activity of the metabolites is less than that of diclofenac.

Systemic clearance is 206 ml / min. T 1/2 from plasma-1-2 h. 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 severe renal insufficiency (creatinine clearance less than 10 ml / min), the excretion of metabolites in the bile increases, while an increase in their concentration in the blood is not observed.

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

Diclofenac passes into breast milk.

Indications

-Diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile chronic arthritis, ankylosing spondylitis (Ankylosing spondylitis); gouty arthritis; rheumatic soft tissue damage; osteoarthritis of the peripheral joints and spine, including those with radicular syndrome; tendovaginitis; bursitis). – Pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboishialgia, post-traumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, algodismenorrhea, adnexitis, proctitis, toothache. – As part of the complex therapy of infectious and inflammatory diseases of the ear, throat, nose with severe pain syndrome (pharyngitis, tonsillitis, otitis media). The drug Diclofenac retard is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.

Contraindications

-Erosive and ulcerative lesions of the gastrointestinal tract in the acute phase;

– “aspirin triad”;

– hematopoiesis disorders of unclear etiology;

– hypersensitivity to diclofenac and the components of the dosage form used, or other NSAIDs.

Side effects

From the digestive system:  nausea, vomiting, epigastric pain, anorexia, flatulence, constipation, gastritis up to erosive with bleeding, increased transaminase activity, drug-induced hepatitis, pancreatitis.

From the urinary system:  interstitial nephritis.

From the central nervous system:  headache, dizziness, disorientation, agitation, insomnia, irritability, fatigue, aseptic meningitis.

Respiratory system disorders:  bronchospasm.

From the hematopoietic system:  anemia, thrombocytopenia, leukopenia, agranulocytosis.

Dermatological reactions:  exanthema, erythema, eczema, hyperemia, erythroderma, photosensitization.

Allergic reactions:  erythema multiforme, Lyell’s syndrome, Stevens-Johnson syndrome, anaphylactic reactions, including shock.

Local reactions:  at the injection site, burning, infiltrate formation, and adipose tissue necrosis are possible.

Other services:  fluid retention in the body, edema, increased blood pressure.

Interaction

Concomitant use of Diclofenac with digoxin, phenytoin or lithium preparations may increase the plasma concentrations of these drugs; with diuretics and antihypertensive agents, the effect of these drugs may decrease; with potassium-sparing diuretics, hyperkalemia may develop; with acetylsalicylic acid, a decrease in the concentration of diclofenac in blood plasma and an increased risk of side effects.

Diclofenac may increase the toxic effect of cyclosporine on the kidneys.

Diclofenac can cause hypo – or hyperglycemia, so when used concomitantly with hypoglycemic agents, monitoring of blood glucose concentration is required. 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 used concomitantly with anticoagulants, regular monitoring of blood clotting parameters is necessary.

How to take, course of use and dosage

Adults are recommended to take 50 to 150 mg of diclofenac per day, divided into 2-3 separate doses. In the absence of other prescriptions, it is recommended to take as initial therapy 100-150 mg per day, and with long-term therapy-75-100 mg, divided into 2-3 separate doses.

Children over the age of 6 years are prescribed diclofenac at a dose of 2 mg/kg of body weight, and the daily dose is also divided into several doses.

Overdose

Symptoms: dizziness, headache, hyperventilation of the lungs, blurred consciousness, vomiting, bleeding from the gastrointestinal tract, diarrhea, tinnitus, convulsions, with a significant overdose – acute renal failure, hepatotoxic effect.

Treatment: gastric lavage, taking activated charcoal. Symptomatic therapy is aimed at eliminating increased blood pressure, impaired renal function, convulsions, gastrointestinal irritation, and respiratory depression. Forced diuresis and hemodialysis are ineffective (due to significant protein binding and intensive metabolism).

Special instructions

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

Influence on the ability to drive a car and manage mechanisms

Due to 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 a car or other moving objects is impaired. These phenomena are amplified when taking alcohol at the same time.

Form of production

Long-acting film-coated tablets.

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25 C. Keep out of reach of children.

Active ingredient

Diclofenac

Conditions of release from pharmacies

By prescription

Dosage form

long-acting tablets

Description

For adults, Pregnant women in the first and second trimester as prescribed by a doctor

Indications

Bursitis, Tendon Inflammation, Adnexitis, Osteoarthritis, Rheumatoid Arthritis, Migraine, Lumbago, Osteoarthritis, Gout, Swelling after Injuries and Operations, Arthritis, Periarthritis, Sciatica