Diclofenac-Teva, gel 1% 40 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

Swelling after injuries and operations, Arthritis, Lumbago, Sciatica, Gout, Pain after injuries and operations, Rheumatoid arthritis, Inflamed tendons, Neck pain, Neuralgia, Periarthritis, Myalgia (muscle pain), Arthrosis, Osteoarthritis, Bursitis, Back pain, Joint pain (arthralgia), Pain

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

Diclofenac

Composition

100 g of the drug contain:

the active ingredient: diclofenac sodium 1,000 g;

excipients: diisopropyladipinate 5,000 g; hyprolose 2,000 g; lactic acid 90% 0.044 g; sodium disulfite 0.050 g; isopropanol 40,000 g; purified water 51.906 g.

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 not 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

Diclofenac may increase the effect of drugs that cause photosensitization. Clinically significant interaction with other drugs has not been described.

Special Instructions

Avoid getting the drug in the eyes, on mucous membranes or open wounds.
Diclofenac-Teva gel should be applied only to intact skin areas. After application of the drug it is allowed to apply a bandage, but you should not apply airtight occlusive dressings. Patients with gastric and duodenal ulcer disease, disorders of liver, kidney or hematopoietic system, as well as patients with concomitant use of other NSAIDs should consult a physician before using.
When using the drug together with other diclofenac dosage forms the maximum daily dose should be considered.
In case of long-term use and/or application on large surfaces the development of systemic side effects due to resorptive action is possible.
If during the treatment with Diclofenac-Teva gel there appear episodes of bronchial asthma, hypersensitivity reactions, edema of the skin, mucous membranes, skin rashes, the drug should be stopped.

Influence on ability to drive vehicles and mechanisms
The drug does not affect the ability to perform potentially dangerous activities requiring high concentration and rapid psychomotor reactions (driving motor transport, operating moving mechanisms).

Synopsis

transparent colorless gel with a characteristic odor.

Contraindications

– Hypersensitivity to diclofenac or other components of the drug, as well as to acetylsalicylic acid, other NSAIDs.
– Prone to bronchial asthma attacks, skin rashes or acute rhinitis when using acetylsalicylic acid or other NSAIDs.
– Pregnancy (III trimester).
– Childhood (under 14 years).
– Violation of the integrity of the skin in the intended place of application.
– The period of breastfeeding.

With caution
. Hepatic porphyria (acute condition), gastrointestinal erosive-ulcerative lesions, severe liver and renal dysfunctions, bleeding disorders (including hemophilia, prolongation of bleeding time, susceptibility to bleeding), chronic heart failure, bronchial asthma, elderly age, pregnancy (I and II trimester).

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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 rarely, pustular rashes.

On the immune system:very rarely – generalized skin rash, allergic reactions (urticaria, hypersensitivity (including urticaria), angioedema).

In the respiratory system: very rarely – bronchial asthma.

Skin and subcutaneous tissue: frequent erythema, dermatitis, (including contact dermatitis, itching, hyperemia, swelling of the treated skin area, papulose – vesicular rashes, exfoliation); rarely – bullous dermatitis; very rare – photosensitization reactions.

If any of the side effects listed in the instructions worsen, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

Due to low systemic absorption of the active ingredient when used topically, overdose is unlikely. Nausea, vomiting and systemic adverse reactions characteristic of NSAIDs may develop if used improperly or swallowed accidentally.
Symptoms: nausea, vomiting, epigastric pain, diarrhea.
If symptoms of overdose appear, consult a physician.
In case of oral administration of the drug, in order to prevent the absorption of diclofenac as soon as possible, gastric lavage followed by the use of activated charcoal should be performed, symptomatic therapy is indicated.
Hemodialysis and forced diuresis are not effective for diclofenac excretion due to high degree of diclofenac binding to blood plasma proteins (about 99%).

Pregnancy use

Pregnancy
Due to the lack of data on the use of diclofenac in pregnant women the use of the drug during I and II trimester of pregnancy is recommended only by doctor’s prescription, comparing the benefit to the mother and the risk to the fetus.
The drug is contraindicated during the third trimester of pregnancy (suppression of uterine contractility, prolongation of bleeding time, anti-aggregation effect, renal dysfunction in the fetus with subsequent haemoptysis and/or premature closure of the fetal arterial duct may occur).

Breastfeeding period
Due to the presence of data that diclofenac in small amounts penetrates into the mother’s milk, it is not recommended to use it during breastfeeding.
During breastfeeding the drug should not be applied to the mammary gland area or to a large skin surface and should not be used for a long time.

Similarities

Diclac, Diclofenac-Teva, Diclo-F, Orthofen, Diclovit, Voltaren, Voltaren Emulsgel, Diclofenac, Voltaren Patch, Dicloran Plus, Orthofen, Diclofenac-Altfarm, Diclofenac-SOLofarm, Dialrapid