Diclac gel 5%, 50 g

• Articular syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout),

• degenerative and chronic inflammatory diseases of the musculoskeletal system (osteochondrosis, osteoarthritis, periarthropathies),

• post-traumatic inflammation of soft tissues and musculoskeletal system (sprains, bruises).

• Spinal pain, neuralgia, myalgia, arthralgia,

• pain syndrome and inflammation after operations and injuries,

• pain syndrome with gout, migraine, algodismenorrhea,

• pain syndrome with adnexitis, proctitis, colic (biliary and renal),

• pain syndrome in infectious and inflammatory diseases of the ENT organs.

Outwardly.

Adults and children over 6 years of age: the drug is applied to the skin 2-3 times a day and rubbed lightly. The required amount of the drug depends on the size of the painful area. A single dose of the drug is up to 2 g (about 4 cm with a completely open tube mouth). After applying the drug, wash your hands. The duration of treatment depends on the indications and the observed effect. After 2 weeks of using the drug, you should consult your doctor.

Gel for external use 5%

1 g

active substance:

diclofenac sodium 50 mg

excipients: isopropyl alcohol; macrogol-7-glycerol cocoate; hypromellose; aromatic oil; purified water

• Erosive and ulcerative lesions of the gastrointestinal tract in the acute phase,

• 'aspirin triad',

• disorders of hematopoiesis of unknown etiology,

• hypersensitivity to diclofenac or other NSAIDs.

pharmachologic effect

NSAIDs, a derivative of phenylacetic acid. It has a pronounced anti-inflammatory, analgesic and moderate antipyretic effect. The mechanism of action is associated with inhibition of the activity of COX, the main enzyme of the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. The analgesic effect is due to two mechanisms: peripheral (indirectly, through suppression of prostaglandin synthesis) and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system).

Inhibits the synthesis of proteoglycan in cartilage.

In rheumatic diseases, it reduces joint pain at rest and during movement, as well as morning stiffness and swelling of the joints, and helps to increase the range of motion. Reduces post-traumatic and postoperative pain and inflammatory edema.

Suppresses platelet aggregation. With prolonged use, it has a desensitizing effect.

When applied topically in ophthalmology, it reduces swelling and pain in inflammatory processes of non-infectious etiology.

Pharmacokinetics

After oral administration, it is absorbed from the gastrointestinal tract. Food intake slows down the rate of absorption, while the degree of absorption does not change. About 50% of the active substance is metabolized during the 'first pass' through the liver. With rectal administration, absorption is slower. The time to reach Cmax in plasma after oral administration is 2-4 hours, depending on the dosage form used, after rectal administration - 1 hour, intramuscular administration - 20 minutes. The concentration of the active substance in the plasma is linearly dependent on the size of the applied dose.

Does not cumulate. Plasma protein binding is 99.7% (mainly albumin). Penetrates into synovial fluid, Cmax is reached 2-4 hours later than in plasma.

It is largely metabolized to form several metabolites, among which two are pharmacologically active, but to a lesser extent than diclofenac.

The systemic clearance of the active substance is approximately 263 ml / min. T1 / 2 from plasma is 1-2 hours, from synovial fluid - 3-6 hours. Approximately 60% of the dose is excreted in the form of metabolites by the kidneys, less than 1% is excreted in the urine unchanged, the rest is excreted in the form of metabolites in the bile.

Side effect

From the digestive system: nausea, vomiting, anorexia, pain and discomfort in the epigastric region, flatulence, constipation, diarrhea; in some cases - erosive and ulcerative lesions, bleeding and perforation of the gastrointestinal tract; rarely - liver dysfunction. With rectal administration, in isolated cases, there was inflammation of the colon with bleeding, exacerbation of ulcerative colitis.

From the side of the central nervous system and peripheral nervous system: dizziness, headache, agitation, insomnia, irritability, fatigue; rarely - paresthesia, visual impairment (blurredness, diplopia), tinnitus, sleep disorders, convulsions, irritability, tremors, mental disorders, depression.

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

From the urinary system: rarely - impaired renal function; edema is possible in predisposed patients.

Dermatological reactions: rarely - hair loss.

Allergic reactions: skin rash, itching; when applied in the form of eye drops - itching, redness, photosensitivity.

Local reactions: at the place of intramuscular injection, burning is possible, in some cases - the formation of infiltration, abscess, necrosis of adipose tissue; with rectal administration, local irritation, the appearance of mucous secretions mixed with blood, painful defecation are possible; when applied externally in rare cases - itching, redness, rash, burning; when applied topically in ophthalmology, a transient burning sensation and / or temporary blurred vision may occur immediately after instillation.

With prolonged external use and / or application to extensive body surfaces, systemic side effects are possible due to the resorptive action of diclofenac.

Application during pregnancy and lactation

Application during pregnancy and lactation is possible in cases where the intended benefit to the mother outweighs the potential risk to the fetus or newborn.

Application for violations of liver function

Use with extreme caution in case of liver disease in history.

Application for impaired renal function

Use with extreme caution in case of a history of kidney disease.

Application in children

Not recommended for use in children under 6 years of age.

Use in elderly patients

Use with extreme caution in elderly patients.

special instructions

It is used with extreme caution in case of liver, kidney, gastrointestinal tract diseases in history, dyspeptic symptoms, bronchial asthma, arterial hypertension, heart failure, immediately after serious surgical interventions, as well as in elderly patients.

If there is a history of allergic reactions to NSAIDs and sulfites, diclofenac is used only in urgent cases. In the course of treatment, systematic monitoring of the function of the liver and kidneys, and the picture of peripheral blood is necessary.

Rectal administration is not recommended in patients with a history of anorectal disease or anorectal bleeding. Externally should be used only on intact skin areas.

Avoid getting diclofenac in the eyes (with the exception of eye drops) or on mucous membranes. Patients using contact lenses should apply eye drops no earlier than 5 minutes after removing the lenses.

Not recommended for use in children under 6 years of age.

During the period of treatment with dosage forms for systemic use, alcohol is not recommended.

Influence on the ability to drive vehicles and mechanisms

During the treatment period, a decrease in the speed of psychomotor reactions is possible. If the clarity of vision deteriorates after using the eye drops, do not drive or engage in other potentially hazardous activities.

Drug interactions

With the simultaneous use of antihypertensive drugs with diclofenac, their effect may be weakened.

There are isolated reports of seizures in patients taking NSAIDs and quinolone antibacterial drugs at the same time.

With simultaneous use with GCS, the risk of side effects from the digestive system increases.

With the simultaneous use of diuretics, it is possible to reduce the diuretic effect. With simultaneous use with potassium-sparing diuretics, an increase in the concentration of potassium in the blood is possible.

With simultaneous use with other NSAIDs, the risk of side effects may increase.

There are reports of the development of hypoglycemia or hyperglycemia in patients with diabetes mellitus who used diclofenac simultaneously with hypoglycemic drugs.

With simultaneous use with acetylsalicylic acid, it is possible to reduce the concentration of diclofenac in blood plasma.

Although clinical studies have not established the effect of diclofenac on the action of anticoagulants, isolated cases of bleeding have been described with the simultaneous use of diclofenac and warfarin.

With simultaneous use, it is possible to increase the concentration of digoxin, lithium and phenytoin in the blood plasma.

The absorption of diclofenac from the gastrointestinal tract decreases with simultaneous use with cholestyramine, to a lesser extent with colestipol.

With simultaneous use, it is possible to increase the concentration of methotrexate in the blood plasma and increase its toxicity.

With the simultaneous use of diclofenac may not affect the bioavailability of morphine, however, the concentration of the active metabolite of morphine may remain elevated in the presence of diclofenac, which increases the risk of side effects of the morphine metabolite, incl. respiratory depression.

With simultaneous use with pentazocine, a case of the development of a large seizure has been described; with rifampicin - a decrease in the concentration of diclofenac in blood plasma is possible; with ceftriaxone - increased excretion of ceftriaxone with bile; with cyclosporine - an increase in the nephrotoxicity of cyclosporine is possible.