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).
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.
DICLOFENAC SODIUM OINTMENT 10MG 30G
Instructions
Trade name of the drug: Diclofenac sodium
Active ingredients: Diclofenac
Pharmacotherapeutic group: Non-steroidal anti-inflammatory drugs., Non-steroidal anti-inflammatory drugs.
Release form: 30 g in tubes in package No. 1.
Dosage form: Ointment for external use 10 mg/g 30 g (tubes)
Compound:
One tube (30 g of ointment) contains: active substance: diclofenac sodium - 0.3 g, excipients: dimethyl sulfoxide, propylene glycol, macrogol 1500, macrogol 400.
Pharmacological properties:
A non-steroidal anti-inflammatory drug, a derivative of phenylacetic acid, has anti-inflammatory and analgesic effects. Indiscriminately inhibiting cyclooxygenase 1 and cyclooxygenase 2, it disrupts the metabolism of arachidonic acid, reduces the number of prostaglandins, incl. at the site of inflammation.
Pharmacokinetics:
Absorption The amount of Diclofenac sodium that is absorbed through the skin is proportional to the size of the area to which the drug is applied and depends on both the total dose applied and the degree of hydration of the skin. The degree of absorption is about 6% of the applied dose after topical application of 2.5 g of the drug per 500 cm2 of skin, determined taking into account complete renal elimination, in comparison with Diclofenac tablets. A 10-hour occlusion results in a threefold increase in the amount of diclofenac absorbed. Distribution Concentrations of Diclofenac sodium were measured in plasma, synovial tissue and synovial fluid after topical application of the ointment to the joints of the hands and knees. The maximum plasma concentration is approximately 100 times lower than the concentration after oral administration of the same amount of Diclofenac sodium. 99.7% of Diclofenac sodium is bound to serum proteins, predominantly albumin (99.4%). Metabolism Biotransformation of Diclofenac sodium partly involves glucuronidation of the unchanged molecule, but predominantly single or multiple hydroxylation leads to the formation of several phenolic metabolites, most of which are converted to glucuronic conjugates. Two phenolic metabolites are biologically active, but their activity is significantly lower than that of Diclofenac sodium. Elimination The total systemic clearance of Diclofenac sodium from blood plasma is 263±56 ml/min. The terminal plasma half-life is 1-2 hours. Four of the metabolites, including two active ones, also show a short plasma half-life of 1-3 hours. One metabolite, 3′-hydroxy-4′-methoxy-diclofenac , shows a longer half-life but is effectively inactive. Diclofenac sodium and its metabolites are excreted primarily in the urine. Pharmacokinetics in certain groups of patients Accumulation of Diclofenac sodium and its metabolites is not expected in patients who suffer from renal failure. In patients with chronic hepatitis or uncompensated cirrhosis, the kinetics and metabolism of Diclofenac sodium are the same as in patients who do not have liver disease.
Indications for use:
Traumatically caused inflammation of tendons, ligaments, muscles and joints (due to sprains, stress and bruises). Localized forms of soft tissue rheumatism, such as shoulder-hand syndrome, tendovaginitis, bursitis, periarthropathy. Localized rheumatic diseases, for example, arthrosis of the joints.
Directions for use: Externally, 2-4 g of ointment (which is comparable in volume to the size of a cherry or walnut and is sufficient to treat a body surface area of 400-800 cm2) is applied in a thin layer, lightly rubbing into the skin above the inflammation, 2-3 times. per day. After applying the ointment, hands must be washed if they are not the area of treatment (for arthrosis of the fingers). The maximum daily dose is 8 g. The duration of treatment depends on the indications and the observed effect (to enhance the effect, the ointment can be used together with other dosage forms of diclofenac). It is necessary to consult a doctor after 2 weeks of using the drug.
Side effects:
From the skin: eczema, photosensitivity, contact dermatitis (itching, hyperemia, swelling of the treated skin area, papular-vesicular rashes, peeling). Allergic reactions: (itching and burning of the skin, erythematous skin rash, urticaria, angioedema, systemic anaphylactic reactions (including shock).
Contraindications:
Hypersensitivity to Diclofenac sodium or other components of the drug, acetylsalicylic acid or other NSAIDs, “aspirin” asthma, pregnancy (III trimester), lactation period, children (up to 12 years), violation of the integrity of the skin. With caution Hepatic porphyria (exacerbation), erosive and ulcerative lesions of the gastrointestinal tract, severe dysfunction of the liver and kidneys, chronic heart failure, bronchial asthma, old age, pregnancy I and II trimester.
Drug interactions:
May enhance the effect of drugs that cause photosensitivity. Use with caution with other drugs known to have hepatoxicity, for example, antibiotics, antiepileptic drugs. Clinically significant interactions with other drugs are unlikely due to negligible systemic absorption.
Special instructions:
Apply only to undamaged areas of the skin. After application, do not apply an occlusive dressing. With long-term use and/or application to large areas of the skin, the risk of developing systemic side effects increases, incl. Increased activity of liver enzymes may be observed. To minimize the possible risk of adverse reactions from the liver, Diclofenac sodium should be used in the minimum effective dose for the shortest possible period. Avoid contact of the ointment with the eyes, mucous membranes or open wounds. Apply externally only. Use during pregnancy There are no controlled clinical studies in pregnant women, therefore Diclofenac sodium should not be used during pregnancy. Use is especially dangerous in the third trimester of pregnancy due to the possible premature closure of the ductus botallus and the likelihood of suppression of labor contractions. Use during breastfeeding There is no data on the penetration of Diclofenac sodium, applied topically, into breast milk. Therefore, the drug should not be used in nursing women. If there are compelling reasons for prescribing, the drug should not be applied to the chest area; it should not be used to treat large areas of the surface or use it for a long time. The drug should not be used after the expiration date and should be stored out of the reach of children.
Overdose: Due to low systemic absorption when applying the ointment, overdose is unlikely.
Storage conditions: At a temperature not higher than 25C.
Shelf life: 2 years.
Dispensing conditions: Without a prescription.
Manufacturer: Borisov Medical Preparations Plant, JSC, Belarus
Descriptions: white or almost white ointment, with a slight specific odor
