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 (Bechterew’s disease); gouty arthritis; rheumatic soft tissue lesions; osteoarthritis of peripheral joints and spine, including with radicular syndrome; tenosynovitis; bursitis).
Pain syndrome of mild or moderate severity: neuralgia, myalgia, lumboischialgia, post-traumatic pain syndrome accompanied by inflammation, postoperative pain, headache, migraine, algomenorrhea, adnexitis, proctitis, toothache.

As part of complex therapy for infectious and inflammatory diseases of the ear, nose and throat with severe pain (pharyngitis, tonsillitis, otitis media).

The drug Diclofenac retard is intended for symptomatic therapy, reducing pain and inflammation at the time of use, and does not affect the progression of the disease.

Pharmacological effect

Pharmaceutical group:

NSAIDs.

Pharmaceutical action:

Diclofenac retard is a non-steroidal anti-inflammatory drug (NSAID), a derivative of phenylacetic acid; has anti-inflammatory, analgesic and antipyretic effects.
By indiscriminately inhibiting cyclooxygenase 1 and 2 (COX1 and COX2), it disrupts the metabolism of arachidonic acid and reduces the amount of prostaglandins at the site of inflammation. 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 helps to significantly reduce the severity of pain, morning stiffness, and swelling of the joints, which improves the functional state of the joint. For injuries, in the postoperative period, diclofenac reduces pain and inflammatory swelling.

Pharmacokinetics:

Absorption is fast and complete. Food slows 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 administration of short-acting drugs; however, it remains high for a long time after administration. Cmax – 0.5-1.0 mcg/ml, time to reach maximum concentration in blood plasma (TCmax) – 5 hours after taking 100 mg extended-release tablets.

There are no changes in the pharmacokinetics of diclofenac following repeated administration. Does not accumulate if the recommended interval between meals is observed.

Bioavailability – 50%. Communication with plasma proteins is more than 99% (most of it is associated with albumin). Penetrates into breast milk and synovial fluid; Cmax in synovial fluid is observed 2-4 hours later than in plasma. The half-life (T1/2) from synovial fluid is 3-6 hours (concentrations of the drug in synovial fluid 4-6 hours after its administration are higher than in plasma and remain higher for another 12 hours).

50% of the active substance is metabolized during the “first pass” 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 takes part in the metabolism of the drug. The pharmacological activity of the metabolites is less than that of diclofenac.

Systemic clearance is 206 ml/min. T1/2 from plasma – 1-2 hours. 60% of the administered dose is excreted in the form of metabolites through the kidneys; less than 1% is excreted unchanged, the rest of the dose is excreted as metabolites in bile.
In patients with severe renal failure (creatinine clearance (CC) less than 10 ml/min), the excretion of metabolites in bile increases, but no increase in their concentration in the blood is observed.

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

Diclofenac passes into breast milk.

Special instructions

Use the drug with caution simultaneously with other NSAIDs.

Effect on the ability to drive a car and operate machinery

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 enhanced by simultaneous intake of alcohol.

Active ingredient

Diclofenac

Composition

Composition: for 1 tablet of extended-release Diclofenac retard, enteric-coated:

– active substance:

diclofenac sodium 100 mg;

– excipients:

[hypromellose (hydroxypropyl methylcellulose),

hyaetellose (hydroxyethylcellulose),

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

sodium alginate, microcrystalline cellulose, magnesium stearate].

Contraindications

Erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, “aspirin triad”, hematopoietic disorders of unknown etiology, hypersensitivity to diclofenac and 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 side of the central nervous system: headache, dizziness, disorientation, agitation, insomnia, irritability, fatigue, aseptic meningitis.

From the respiratory system: bronchospasm.

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

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

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

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

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

Interaction

With the simultaneous use of Diclofenac with digoxin, phenytoin or lithium preparations, it is possible to increase the plasma concentrations of these drugs; with diuretics and antihypertensive drugs – the effect of these drugs may be reduced; with potassium-sparing diuretics – hyperkalemia may develop; with acetisalicylic acid – a decrease in the concentration of diclofenac in the blood plasma and an increased risk of side effects.

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

Diclofenc can cause hypo- or hyperglycemia, therefore, when used simultaneously with hypoglycemic agents, monitoring of blood glucose concentrations is required.

When using methotrexate within 24 hours before or after taking Diclofenac, the concentration of methotrexate may increase and its toxic effect may increase.

When used simultaneously with anticoagulants, regular monitoring of blood clotting parameters is necessary.

Overdose

Symptoms: dizziness, headache, hyperventilation, clouding of consciousness, vomiting, bleeding from the gastrointestinal tract, diarrhea, tinnitus, convulsions, in case of significant overdose – acute renal failure, hepatotoxic effect.
Treatment: gastric lavage, taking activated carbon. Symptomatic therapy is aimed at eliminating increased blood pressure, impaired renal function, seizures, gastrointestinal irritation, and respiratory depression. Forced diuresis and hemodialysis are ineffective (due to the significant connection with proteins and intensive metabolism).

Storage conditions

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

Manufacturer

Ozon, Russia