Diclofenac - instructions for use, dose, side effects, contraindications

Excipients: 2-propanol 45.00 g, macrogol 7 glyceryl cocoate 6.00 g, hypromellose 4000 3.00 g, pine needles oil 0.15 g, lavender oil 0.05 g, purified water 100, 00

Description:

Colorless or with a weak yellowish tinge transparent gel with a characteristic odor.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)

ATX: & nbsp

S.01.B.C.03 Diclofenac

M.01.A.B.05 Diclofenac

Pharmacodynamics:

Active component diclofenac - non-steroidal anti-inflammatory drug, which has pronounced analgesic, anti-inflammatory and antipyretic properties. Indiscriminately inhibiting cyclooxygenase 1 and 2 types, disrupts the metabolism of arachidonic acid.

Diclofenac is used to eliminate pain syndrome and inflammation in the joints, muscles and ligaments of traumatic or rheumatic origin, contributing to the reduction of pain and swelling associated with the inflammatory process, increasing the mobility of the joints.

Due to its water-alcohol basis Diclofenac has a calming and cooling effect.

Pharmacokinetics:

The amount of diclofenac absorbed through the skin is proportional to the area of the treated surface and depends on both the total dose of the drug applied and the degree of hydration of the skin. After application to the skin surface area of 400 cm²Diclofenac, gel for external use 1% (4 applications per day), the concentration of the active substance in the plasma corresponds to its concentration with the use of 2% gel diclofenac (2 applications per day). On the 7th day, the relative bioavailability of the drug (ratio AUC) is 4.5% (for an equivalent dose of the sodium salt of diclofenac). When wearing a moisture-permeable bandage, the absorption did not change. 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. The maximum concentrations in the plasma were approximately 100 times lower than after oral administration of the same amount of diclofenac. 99.7% of diclofenac is bound by plasma proteins, mainly with albumins (99.4%).

Diclofenac is predominantly distributed and retained deep in tissues prone to inflammation, such as joints, where its concentration is 20 times higher than in plasma.

The metabolism of diclofenac is partly due to glucuronization of the unmodified molecule, but mainly through single and multiple hydroxylation, which leads to the formation of several phenolic metabolites, most of which are converted into glucuronide conjugates. Two phenolic metabolites are biologically active, but to a much lesser extent than diclofenac.

The total systemic plasma clearance of diclofenac is 263 ± 56 ml / min. The final half-life is 1-2 hours. The half-life of metabolites, including two pharmacologically active metabolites, is also short-lived and is 1-3 hours. One of the metabolites (3'-hydroxy-4'-methoxydiclofenac) has a longer half-life, however, this the metabolite is completely inactive. Most of the diclofenac and its metabolites are excreted in the urine.

Indications:

- Back pain in inflammatory and degenerative diseases of the spine (radiculitis, osteoarthritis, lumbago, sciatica),

- Pain in the joints (joints of the fingers, knees, etc.) with osteoarthritis,

- Pain in the muscles (due to stretching, overstrain, bruises, injuries),

- Inflammation and swelling of soft tissues and joints due to injuries and rheumatic diseases (tendovaginitis, bursitis, lesions of periarticular tissues, wrist syndrome).

Contraindications:

Hypersensitivity to diclofenac or other components of the drug; propensity to occurrence of attacks of a bronchial asthma, skin rashes or sharp rhinitis at application of an acetylsalicylic acid or other NSAIDs; pregnancy (III trimester), breastfeeding; children's age (up to 12 years); violation of the integrity of the skin in the intended site of application.

Carefully:

Hepatic porphyria (exacerbation), erosive and ulcerative lesions of the gastrointestinal tract, severe violations of the liver and kidney function, blood clotting disorders (including hemophilia, prolonged bleeding time, a tendency to bleeding), chronic heart failure, bronchial asthma, advanced age, pregnancy (I and II trimester).

Pregnancy and lactation:

Due to the lack of application data Diclofenac in pregnant women, the use of the drug during the first and second trimester of pregnancy is recommended only for the doctor's prescription, comparing the benefits to the mother and the risk to the fetus.

The drug is contraindicated in the third trimester of pregnancy in connection with the possibility of lowering the tone of the uterus, impaired fetal kidney function followed by the development of low salinity and / or premature closure of the arterial duct of the fetus.

Due to the lack of data on penetration Diclofenac in the breast milk the drug is not recommended for use during breastfeeding. If nevertheless it is necessary to use the drug, it should not be applied to the mammary glands or to a large surface of the skin and not to be used for a long time.

Application data Diclofenac and its effect on fertility in humans are absent.

Dosing and Administration:

Outwardly.

Adults and children over 12 years of age, the drug is applied to the skin 2 times a day (every 12 hours: preferably in the morning and in the evening), lightly rubbing into the skin.

The required amount of the drug depends on the size of the painful area. A single dose of the drug - 4-8 g (which is comparable in volume to the double size of a cherry or walnut, respectively) is sufficient for processing the area of 400-800cm². If the hands are not a zone of pain localization, then after applying the drug, they must be washed. The duration of treatment depends on the indications and the effect observed. The gel should not be used for more than 14 days with post-traumatic inflammations and rheumatic diseases of soft tissues without a doctor's recommendation. If after 7 days of application the therapeutic effect is not observed or the condition worsens, you should consult a doctor.

To remove the protective membrane, use a screw cap as a key (a recess with protrusions on the outside of the cover). Align the recess on the outside of the lid with the tubular protective membrane and turn. The membrane must separate from the tube.

Tubes can have both a conventional lid (round shape) and an innovative lid (triangular shape), which is especially convenient for use with limited mobility of the joints of the hands due to osteoarthritis or other joint diseases or injuries.

Side effects:

Classification of incidence of adverse reactions:

very often (≥ 1/10); often (≥ 1/100, <1/10); infrequently (≥ 1/1000, <1/100); rarely (≥ 1/10000, <1/1000); very rarely (<1/10000), including individual messages.

Infectious and parasitic diseases:

Very rarely: pustular rash.

Immune system disorders:

Very rarely: hypersensitivity reactions (including urticaria), angioedema.

Disturbances from the respiratory system, chest and mediastinal organs:

Very rarely: asthma.

Disturbances from the skin and subcutaneous tissues:

Often: dermatitis (including contact dermatitis), rash, erythema, eczema, pruritus.

Rarely: bullous dermatitis.

Very rarely: photosensitization reactions.

If you experience any side effects, including those not listed in the instructions, you should stop using the drug and consult a doctor.

Overdose:

Due to low systemic absorption during the application of the gel, an overdose is unlikely. With accidental ingestion, it is possible to develop systemic adverse reactions. Treatment of an overdose with accidental ingestion: gastric lavage, induction of vomiting, Activated carbon, symptomatic therapy. Dialysis and forced diuresis are not effective due to the high degree of binding of diclofenac to plasma proteins (about 99%).

Interaction:

The drug can enhance the effect of drugs that cause photosensitivity.Clinically significant interaction with other drugs is not described.

Special instructions:

Diclofenac should be applied only to intact skin, avoiding contact with open wounds. Do not allow the drug to enter the mouth, eyes and mucous membranes. After applying the drug, a bandage bandage is allowed, but no airtight occlusive dressings should be applied. In the case of development after application of the skin rash, its use should be discontinued.

Effect on the ability to drive transp. cf. and fur:

Does not affect.

Form release / dosage:

Gel for external use 1%.

Packaging:

5, 10, 15, 20, 25, 30, 35, 40, 50, 60, 70, 80, 90, 100 g into cans of orange glass with a triangular aureole with a lid tightened with a sealing element.

5, 10, 15, 20, 25, 30, 35, 40, 50, 60, 70, 80, 90, 100 g into cans of polymer complete with lids or cans of polyethylene terephthalate with the means of corking.

20, 25, 30, 35, 40, 50, 60, 70, 80, 100 g in aluminum tubes coated with BF-2 varnish, with high-density polyethylene caps or polymer tubes with polyethylene screw caps.

Each jar and tube together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-004835

Date of registration:07.05.2018

Expiration Date:07.05.2023

The owner of the registration certificate:TULA PHARMACEUTICAL FACTORY, LTD. TULA PHARMACEUTICAL FACTORY, LTD. Russia

Manufacturer: & nbsp

TULA PHARMACEUTICAL FACTORY, LTD. Russia

Information update date: & nbsp28.05.2018

Illustrated instructions

Instructions

Diclofenac (Diclofenac)