Diclofenac-Teva, gel 1% 100 g

Pharmacotherapeutic group: nonsteroidal anti-inflammatory drug (NSAIDs)

ATX code: M02AA15

Pharmacological properties.

Pharmacodynamics

The active ingredient diclofenac is a non-steroidal anti-inflammatory drug (NSAID) with pronounced analgesic, anti-inflammatory and antipyretic properties. Indiscriminately inhibiting cyclooxygenase 1 and 2 types, disrupts the metabolism of arachidonic acid and the synthesis of prostaglandins in the inflammation focus. Diclofenac gel for external use is used to eliminate pain and inflammation in joints, muscles and ligaments of traumatic or rheumatic origin, helping to reduce pain and swelling associated with the inflammatory process, increasing joint mobility.

Pharmacokinetics

Assimilation. The amount of diclofenac absorbed through the skin is proportional to the surface area treated and depends on both the total dose of the drug applied and the degree of hydration of the skin. With the recommended method of application no more than 6% of diclofenac is absorbed.

Distribution The concentration of diclofenac in plasma, synovial membrane and synovial fluid was measured when the drug was applied to the area of the affected joint. Maximum concentrations in plasma were approximately 100 times lower than after oral administration of the same amount of diclofenac. Binding with plasma proteins is 99% (predominantly with albumin). Diclofenac is mainly distributed and retained deep in the tissues subject to inflammation, such as joints, where its concentration is 20 times higher than in plasma.

Biotransformation / metabolism

Diclofenac is metabolized partly by glucuronidation of the unchanged molecule, but predominantly by single and multiple hydroxylation, resulting in several phenolic metabolites, most of which are converted to glucuronide conjugates. Two phenolic metabolites are biologically active, but to a much lesser extent than diclofenac.

Extractions. Total systemic plasma clearance of diclofenac is 263±56 ml/min. Final elimination half-life is 1-2 hours. Half-life of metabolites, including two pharmacologically active ones, is also short and is 1-3 hours. One of the metabolites (3′-hydroxy-4′-methoxydiclofenac) has a longer half-life, however, this metabolite is completely inactive. It is excreted by the kidneys (about 65%) and with the bile (about 35%) in the form of inactive compounds with glucuronic acid.

Indications

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

Active ingredient

How to take, the dosage

Externally.

To remove the protective membrane, use the screw-on cap as a key (indentation with protrusions on the outside of the cap). Align the recess on the outside of the cap with the shaped protective membrane on the tube and twist. The membrane should separate from the tube.

Adults

The product is applied in a thin layer to the painful area of the skin 3 times a day, gently rubbing into the skin.

The amount of product needed depends on the size of the painful area. A single dose of the preparation is 3 g (which is the size of a cherry or walnut), enough to treat an area of 400-800 cm2. The maximum daily dose is 9 g. If the hands are not the localized area of pain, they should be washed after applying the drug.

Apply in the lowest effective doses for the shortest possible course.

The course of treatment is no more than 14 days. The need for longer use of the drug is determined by the physician.

Children over 14 years of age

The course of treatment is not more than 7 days. If after 7 days of use the therapeutic effect is not observed or the condition worsens, a physician should be consulted.

The use of the drug in children under 14 years of age is not recommended.

Interaction

Special Instructions

Use only externally.

Avoid contact of the drug with eyes, mucous membranes or open wounds.

Diclofenac-Teva Gel should only be applied to intact skin areas. After application of the drug it is allowed to apply a bandage, but airtight occlusive dressings should not be applied. Patients with gastric and duodenal ulcer disease, hepatic, renal or hematopoietic disorders, as well as patients with concomitant use of other NSAIDs should consult a physician before use.

When using the drug together with other diclofenac dosage forms, the maximum daily dose should be considered.

Long-term use and/or application to large surfaces may lead to systemic side effects due to the resorptive action.

If during treatment with Diclofenac-Teva gel bronchial asthma attacks, hypersensitivity reactions, swelling of the skin, mucous membranes, skin rashes occur, treatment with the drug should be stopped.

Influence on driving and operating ability

The drug does not affect the ability to perform potentially hazardous activities requiring increased concentration and rapid psychomotor reactions (driving, operating moving machinery).

Synopsis

Contraindications

With caution

Hepatic porphyria (exacerbation), erosive-ulcerative lesions of the gastrointestinal tract, severe hepatic and renal dysfunction, clotting disorders (including hemophilia, prolongation of bleeding time, tendency to bleed), chronic heart failure, bronchial asthma, advanced age, pregnancy (I and II trimester).

Side effects

The frequency of side effects is classified according to World Health Organization recommendations: very common (≥ 1/10); common (≥ 1/100, but < 1/10); infrequent (≥ 1/1000, but < 1/100); rare (≥ 1/10000, but < 1/1000); very rare (< 1/10000), including individual reports; frequency unknown – frequency cannot be estimated from available data.
Infectious and parasitic diseases: very rare – pustular rash.
Immune system: very rare – generalized skin rash, allergic reactions (urticaria, hypersensitivity (including urticaria), angioedema).
Respiratory system: very rare – bronchial asthma.
Skin and subcutaneous tissue: frequently – erythema, dermatitis (including contact dermatitis, itching, hyperemia, edema of the treated skin area, papulose-vesicular rash, exfoliation), rarely – bullous dermatitis, very rare – photosensitization reactions.
If any of the side effects mentioned in the instructions worsen, or if you notice any other side effects not mentioned in the instructions, tell your doctor.

Overdose

In view of the low systemic absorption of the active component of the drug in external use, overdose is unlikely. In case of improper use or accidental swallowing, nausea, vomiting and systemic adverse reactions characteristic of NSAIDs may develop.

Symptoms: nausea, vomiting, epigastric pain, diarrhea.

In case of symptoms of overdose, consult a doctor.

If swallowed, gastric lavage followed by activated charcoal should be performed to prevent diclofenac from being absorbed as soon as possible, and symptomatic therapy is indicated.

Hemodialysis and forced diuresis are not effective for diclofenac excretion due to high degree of binding of diclofenac with blood plasma proteins (about 99%).

Pregnancy use

Pregnancy

In the absence of data on the use of diclofenac in pregnant women, the use of the drug during the I and II trimesters of pregnancy is recommended only by prescription, comparing the benefit to the mother and the risk to the fetus.

The use of the drug is contraindicated in the III trimester of pregnancy (suppression of uterine contractility, prolongation of bleeding time, anti-aggregation effect, impaired renal function in the fetus with subsequent haemoptysis and/or premature closure of the fetal arterial duct are possible).

Period of breastfeeding

In view of the data that diclofenac penetrates into maternal milk in small amounts, it is not recommended to use it during breastfeeding.

The drug should not be applied to the mammary gland area or a large area of the skin while breastfeeding and should not be used for prolonged periods of time.

Similarities