pharmachologic effect
Diclofenac has anti-inflammatory, analgesic and decongestant effects due to inhibition of the synthesis of prostaglandins, which play a major role in the pathogenesis of inflammation. For rheumatic diseases, it reduces pain in the joints at rest and during movement, as well as morning stiffness and swelling of the joints, and helps to increase range of motion. When applied externally, diclofenac penetrates the skin and accumulates in the underlying tissues (subcutaneous tissue, muscle tissue, joint capsule and joint cavity).
Composition and features
Diclofenac is available in several dosage forms. Apply ointment or gel externally.
The substance is diclofenac sodium, its concentration in the ointment is 10 or 20 mg per 1 g, in the gel - 10 or 50 mg per 1 g. Accordingly, the gel can be 1 or 5 percent, and the ointment 1 or 2 percent.
The auxiliary components in the gel are alcohol, propylene glycol, lavender oil, purified water and hyaetellose. The ointment additionally contains propylene glycol, dimethyl sulfoxide and macrogol.
The gel is a homogeneous transparent substance with a slight yellow tint or no color, there is a specific odor, the base is water.
The basic component of the ointment is fat; it has a thicker consistency. Therefore, it is better to use a gel for joints and deep layers of the epidermis. It spreads more easily and dries faster, does not leave stains on clothes and creates a protective film on the skin.
If the skin at the site of application is irritated and prone to peeling, then it is better to use ointment, as it additionally softens and moisturizes the skin at the site of application.
Indications for use
Diclofenac ointment and gel are prescribed for the following pathologies of bones and muscles:
- inflammatory and degenerative diseases of articular joints (osteochondrosis, radiculitis, arthrosis, arthritis, including ankylosing spondylitis);
- bruises as a result of injuries;
- rheumatic fever and inflammatory swelling of soft tissues (tenosynovitis, bursitis);
- sprains of tendons, muscles and ligaments, accompanied by an inflammatory response;
- myalgia and arthralgia provoked by heavy physical exertion.
The remedy is intended to eliminate negative symptoms, but does not affect the progression of the disease.
Can the product be used by pregnant women and children?
Pregnancy, especially the third trimester, is a contraindication to the use of Diclofenac. If treatment with the drug is necessary in the first half of pregnancy, the doctor is obliged to evaluate all the negative consequences for the fetus and the expected benefits for the woman.
The ability of the drug to pass into breast milk has not been studied, so treatment is not advisable during breastfeeding. If there are serious reasons to use a gel or ointment during lactation, do not apply the substance to large areas of the skin and do not treat it for a long time.
In pediatric practice, it is used in the treatment of children only from 12 years of age.
How to use Diclofenac gel
Instructions for use of Diclofenac gel contain detailed information on doses and methods of use of the medicine.
The gel is used only externally in adults and children over 12 years of age according to indications. Apply to the site of inflammation with light rubbing movements 2 or 3 times a day. For one application, 2 g of the drug is enough, which corresponds to a strip of 4 cm.
The maximum permissible dose per day is no more than 6 g. Duration of therapy is no more than two weeks, longer periods are possible in agreement with the attending physician. Be sure to wash your hands after using Diclofenac.
Diclofenac ointment for external use 1% tube 30g
Compound
Active substance: diclofenac sodium - 1 g.
Excipients: isopropanol - 45 g, macrogol 7 glyceryl cocoate - 6 g, hypromellose 4000 (in terms of dry matter) - 3 g, Scots pine oil - 0.15 g, lavender oil - 0.05 g , purified water - up to 100 g.
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 skin hydration. The binding of diclofenac to plasma proteins is 99.7%, mainly with albumin (99.4%). Diclofenac is preferentially 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 carried out partly by glucuronidation of the unchanged molecule, but mainly through single and multiple hydroxylation, which leads to the formation of 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.
The total systemic plasma clearance of diclofenac is 263±56 ml/min.
The final T1/2 is 1-2 hours. The T1/2 of metabolites, including two pharmacologically active ones, is also short-lived and is 1-3 hours. One of the metabolites (3′-hydroxy-4′-methoxydiclofenac) has a longer T1/2, however, this metabolite is completely inactive. Most of diclofenac and its metabolites are excreted in the urine.
Indications for use
- inflammatory diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic arthritis, juvenile chronic arthritis, ankylosing spondylitis, gouty arthritis);
- rheumatic lesions of soft tissues (tenosynovitis, bursitis, damage to periarticular tissues);
- degenerative diseases of the musculoskeletal system (deforming osteoarthritis, osteochondrosis);
- post-traumatic inflammation of tendons, ligaments, muscles and joints (as a result of injuries, stress and bruises);
- pain and swelling associated with diseases of muscles and joints (lumbago, sciatica, neuralgia, myalgia, tendinitis).
Intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.
Contraindications
- “Aspirin triad” (attacks of bronchial asthma, urticaria and acute rhinitis when taking acetylsalicylic acid or other NSAIDs);
- violation of the integrity of the skin at the site of application of the drug;
- III trimester of pregnancy;
- lactation period (breastfeeding);
- children up to 6 years of age and older, depending on the drug used;
- hypersensitivity to diclofenac, other NSAIDs or to any of the excipients of the drug used.
With caution: hepatic porphyria (in the acute phase); erosive and ulcerative lesions of the gastrointestinal tract; severe dysfunction of the liver and kidneys; chronic heart failure; bronchial asthma; bleeding disorders (including hemophilia, prolongation of bleeding time, bleeding tendency); I and II trimesters of pregnancy; elderly patients.
Directions for use and doses
Externally.
For adults and children over 12 years of age, the drug is applied to the skin 2-3 times a day, at a dose of 2-4 g (about 4 cm with the neck of the tube completely open). Apply a thin layer to the skin above the inflammation and rub in lightly.
For children from 6 to 12 years old, use no more than 2 times a day, a single dose of the drug is up to 1 g (about 2 cm with the neck of the tube completely open). The maximum daily dose of the gel should not exceed 8 g.
The course of treatment is no more than 14 days. The need for longer-term use of the drug is determined by the doctor. After applying the gel, you must wash your hands.
Use in minimally effective doses for a minimally short course.
Storage conditions
In a place protected from light at a temperature not exceeding 25° C.
Keep out of the reach of children.
Best before date
3 years. Do not use after the expiration date.
special instructions
Apply externally only. The gel can only be applied to intact areas of the skin. After applying the gel, you should not apply an occlusive dressing. Before use, patients with gastric and duodenal ulcers, impaired liver, kidney or hematopoietic function, as well as concomitant use of other non-steroidal anti-inflammatory drugs, should consult a doctor. When using the drug together with other dosage forms of diclofenac, the maximum daily dose should be taken into account.
With long-term use and/or application to large surfaces, systemic side effects may develop due to the resorptive effect. Avoid contact of the drug with the eyes, mucous membranes or open wounds.
Description
Non-steroidal anti-inflammatory drug (NSAID).
Dosage form
Gel for external use 1% colorless or with a slight yellowish tint, transparent, odorless.
Use in children
Not recommended for use in children under 6 years of age.
Pharmacodynamics
NSAID for external use, a derivative of phenylacetic acid. Has anti-inflammatory and analgesic effects. The mechanism of action is due to inhibition of the activity of COX-1 and COX-2, which leads to disruption of the metabolism of arachidonic acid and the synthesis of prostaglandins, which are the main link in the development of inflammation.
When used externally, it leads to the disappearance or weakening of pain at the site of application, reduces pain in the joints at rest and during movement, as well as morning stiffness and swelling of the joints. Helps increase range of motion in affected joints.
Side effects
The incidence of side effects is classified according to the recommendations of the World Health Organization: characterized as very common - at least 10%; often - at least 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than <0.1%; very rare, including individual messages - less than 0.01%.
Local reactions: infrequently - exudative erythema multiforme (including Stevens-Johnson syndrome), eczema, very rarely - contact dermatitis (itching, hyperemia, swelling of the treated skin area, papular-vesicular rashes, peeling).
When applying the gel to large surfaces of the skin over a long period of time, systemic side effects of diclofenac may develop.
Systemic reactions: rarely - generalized skin rash, allergic reactions (urticaria, angioedema, bronchospastic reactions), rarely - photosensitivity, very rarely - anaphylactic reactions (including shock).
Use during pregnancy and breastfeeding
Use is contraindicated in the third trimester of pregnancy due to the possibility of decreased uterine tone and/or premature closure of the fetal ductus arteriosus.
Use in the first and second trimesters of pregnancy is possible in cases where the potential benefit to the mother outweighs the potential risk to the fetus or infant.
Use during lactation (breastfeeding) is contraindicated.
Interaction
The use of the drug with other non-steroidal anti-inflammatory drugs is not recommended.
Diclofenac may enhance the effect of drugs that cause photosensitivity. Clinically significant interactions with other drugs have not been described.
Overdose
Due to the low systemic absorption upon application of the gel, overdose is unlikely.
In case of accidental ingestion, systemic adverse reactions may develop. Symptoms: nausea and vomiting.
Treatment: gastric lavage, induction of vomiting, activated charcoal, forced diuresis, symptomatic therapy.
Hemodialysis is not effective due to the high degree of protein binding of diclofenac (about 99%).
Impact on the ability to drive vehicles and operate machinery
The drug does not affect the ability to drive a car or use other mechanical means.
Contraindications and side effects
According to the instructions for Diclofenac ointment, treatment with the drug is contraindicated for:
- high sensitivity to the constituent substances, aspirin or other non-steroidal anti-inflammatory drugs;
- complete or incomplete combination of bronchial asthma with recurrent polyposis of the nose and paranasal sinuses, angioedema or urticaria;
- late pregnancy and lactation;
- treatment of children under 6 years of age;
- open wound surfaces on the skin at the site of application.
Contraindications also apply to the use of the gel, which is prohibited in the treatment of children under 12 years of age.
The drug is prescribed with caution in the early stages of pregnancy, for erosions and ulcers of the stomach and intestines, for chronic dysfunction of the heart and bronchial asthma, severe dysfunction of the liver and kidneys, with a tendency to bleeding, in the treatment of elderly patients.
When applied topically, undesirable reactions may occur:
- rash, burning and redness at the application site;
- urticaria and angioedema with hypersensitivity to the components of the drug;
- with prolonged use, in rare cases, the development of bronchial asthma is possible.