Diklovit, rectal 50 mg 10 pcs.

Diclofenac has anti-inflammatory, analgesic and antipyretic effects.

Inhibiting cyclooxygenase 1 and 2 indiscriminately, it disrupts arachidonic acid metabolism, reduces the amount of prostaglandins in the focus of inflammation.

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 injury and in the postoperative period diclofenac reduces pain and inflammatory swelling.

In primary algodysmenorrhea, it relieves pain and bleeding.

The maximum plasma concentration is established after 30-40 minutes and is in a linear relationship to the dose used.

There are no changes in the pharmacokinetics of diclofenac on repeated administration; it does not cumulate.

The binding to plasma proteins is more than 99% (most of it binds with albumin).

It penetrates into the synovial fluid. Maximum concentration in synovial fluid is observed 2-4 hours later than in plasma.

The half-life of synovial fluid is H-b (the concentration of the active substance in synovial fluid is higher than in plasma 4-6 hours after administration and stays higher for 12 hours).

The relationship between the concentration of the drug in synovial fluid and the clinical efficacy of the drug has not been elucidated.

Metabolism: 50% of the active substance is metabolized during “first passage” through the liver.

Metabolism occurs as a result of multiple or single hydroxylation and conjugation with glucuronic acid.

The enzyme system P450 CYP2C9 is involved in metabolism of the drug. The pharmacological activity of the metabolites is lower than that of diclofenac.

The plasma elimination half-life is 2 hours. 65% of the administered dose is excreted as metabolites by 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) 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 of diclofenac are not changed.

Diclofenac penetrates into breast milk.

Indications

Active ingredient

Composition

One suppository contains:

The active ingredient – diclofenac sodium – 50 mg;

The base for the suppositories – solid fat (Vitepsol brand H 15, W 35, Supposir brand NA 15, NAS 50) – to obtain a suppository weight of 1.26 g.

How to take, the dosage

Rectally. Suppositories are inserted into the rectum, preferably after spontaneous bowel emptying or purging enema. After insertion of the suppository it is recommended to stay in bed for 20-30 minutes.

Adults and adolescents from 15 years of age: 1 suppository 2-3 times a day.

Dicklovit® may be used simultaneously with oral forms of diclofenac sodium. In this case, the total daily dose of diclofenac sodium should not exceed 150 mg.

In case of algodysmenorrhea (at the appearance of the first symptoms) the initial dose is 50-100 mg/day (1 suppository 1-2 times/day); if necessary the dose is increased during several menstrual cycles up to 150 mg (1 suppository 3 times/day).

Migraine attacks – 100 mg (2 suppositories) at the first signs of an attack. If necessary, repeat 100 mg (2 suppositories). If it is necessary to continue treatment on subsequent days, the daily dose should not exceed 150 mg (3 suppositories) per day.

The duration of treatment is determined by the doctor depending on the severity of the disease.

Interaction

Increases the plasma concentration of digoxin, methotrexate, lithium drugs and cyclosporine.

Decreases the effect of diuretics, against potassium-saving diuretics the risk of hyperkalemia increases; against anticoagulants, thrombolytic agents (alteplase, streptokinase, urokinase) – risk of bleeding (often from the gastrointestinal tract).

Limits the effects of hypotensive and sleeping pills.

Induces side effects of other nonsteroidal anti-inflammatory drugs and glucocorticosteroids (gastrointestinal bleeding), methotrexate toxicity and cyclosporine nephrotoxicity.

Acetylsalicylic acid reduces the blood concentration of diclofenac.

Concomitant use with paracetamol increases the risk of nephrotoxic effects of diclofenac.

Decreases the effect of hypoglycemic agents.

Cefamandole, cefoperazone, cefotetan, valproic acid and plikamycin increase the incidence of hypoprothrombinemia.

Cyclosporine and gold drugs increase the effect of diclofenac on prostaglandin synthesis in the kidneys, which increases nephrotoxicity.

Concomitant administration with ethanol, colchicine, corticotropin and St John’s wort preparations increases the risk of gastrointestinal bleeding.

Diclofenac increases the effect of drugs that cause photosensitization.

Drugs that block tubular secretion increase the plasma concentration of diclofenac, thereby increasing its toxicity.

Special Instructions

Patients taking the drug should refrain from activities that require increased attention and rapid mental and motor reactions, drinking alcohol.

Contraindications

Side effects

Overdose

Similarities