Pharmacological authorities
Pharmacodynamics.
Diclofenac is a non-steroidal anti-inflammatory drug (NSAID) with pronounced anti-rheumatic, analgesic, anti-inflammatory and antipyretic effects. The main mechanism of action is the suppression of prostaglandin biosynthesis.
In case of inflammation caused by injuries or rheumatic illnesses, the drug should be used to reduce pain, tissue swelling and shorten the period of renewal of the function of joints, ligaments, tendons and muscles. The hostility changes within 1 year after initial application. It is important for most patients to have a small dose after 2 doses of treatment. Podlinal pain and functional impairment occurred after 4 days of treatment with the drug. Due to its water-alcohol base, the drug also exhibits a local anesthetic and cooling effect.
Pharmacokinetics.
The amount of diclofenac that is absorbed through the skin is proportional to the level of application and is stored both as a final dose of the drug and at the stage of hydration of the skin. After locally applying 2.5 g of diclofenac to a skin area of 500 cm2, its absorption rate becomes approximately 6%. Keep the occlusive dressing for 10 years until the absorption of diclofenac increases three times.
After diclofenac is applied to the scalp of the hands and knees, diclofenac is detected in blood plasma (its maximum concentration is approximately 100 times lower than after oral administration), in synovial membrane and synovial tissue. I'm home. The binding of diclofenac to proteins is 99.7%.
Diclofenac accumulates at the skin, which serves as a reservoir, and as a result, the secretion of speech occurs at the adjacent tissue. It is important to take diclofenac in deep tissues, such as sores, which lasts and is detected in concentrations up to 20 times higher than in blood plasma.
Diclofenac is metabolized mainly by hydroxylation of several phenolic compounds, 2 of which are pharmacologically active, but significantly less so than diclofenac.
Diclofenac and its metabolites are excreted by section. The initial systemic plasma clearance of diclofenac is 263±56 ml/min, and the terminal dosing period is an average of 1–3 years.
In case of liver or liver failure, the metabolism and elimination of diclofenac from the body does not change.
Characteristics of Diclofenac ointment
Diclofenac ointment is an anti-inflammatory drug for external use. The white creamy composition is distinguished by the presence of a weak specific odor.
The ointment is produced in different packaging - 40 g, 50 g, 100 g. The concentration of the active substance (diclofenac sodium) is 1 g per 100 g. Excipients - dimethyl sulfoxide, macrogol, propylene glycol.
The product is used in the following situations:
- pain syndrome in various diseases of the joints and spine of an inflammatory and degenerative nature (radiculitis, osteoarthritis, lumbago);
- pain in the joints of the upper and lower extremities, incl. for rheumatoid arthritis (the ointment also treats arthritis of the knee joint, similar processes in smaller joints of the fingers);
- Bekhterev's disease and other similar pathologies;
- injuries and bruises, swelling caused by them (with bursitis and tendovaginitis).
The ointment is prescribed for pain due to radiculitis.
Contraindications to the use of Diclofenac ointment are the same conditions as for other non-steroidal drugs. This is the “aspirin triad,” that is, attacks of acute rhinitis, urticaria or bronchial asthma that were previously recorded when taking aspirin or other NSAIDs.
In addition, since the ointment is a topical preparation, it is subject to the same restrictions as other external preparations: increased sensitivity of the skin to these substances, violation of the integrity of the skin in the area where the drug is planned to be applied.
Diclofenac ointment is prescribed with caution for hepatic porphyria if the disease is in the acute stage. Ointment with diclofenac has no effect on the gastrointestinal tract, unlike tablets with the same active ingredient.
Diclofenac ointment should not be used in the third trimester of pregnancy. It is also not used during lactation. It is allowed in the first and second trimesters, but it must be used with caution, as in people with chronic heart failure. It is not recommended for children under 6 years of age.
We suggest you familiarize yourself with Drops to calm the nerves
The ointment should not be used for acute rhinitis caused by taking NSAIDs.
The drug is not used in the 3rd trimester of pregnancy.
The ointment should not be used by older people.
Teenagers and older adults should avoid it. For these groups of patients, using the product for a long period may be risky.
Although Diclofenac ointment is a group of regenerating agents, it can also cause side effects on the skin. Sometimes it is dermatitis or erythema, sometimes it is swelling, skin rash, peeling and other unpleasant manifestations. In addition, diclofenac can cause photosensitivity reactions, that is, the skin's sensitivity to direct sunlight increases.
Rarely, side effects such as bronchospasm, asthma attacks occur, and pustular rashes are possible. If you are allergic to the drug, urticaria and angioedema may occur, which leads to respiratory failure, and in case of unfavorable developments, death. All this is the result of the action of the active component. When the first signs of an allergic reaction appear, use of the drug should be discontinued.
The gel contains the active substance - diclofenac sodium at a level of 5.0 g. This is an NSAID, one of the most powerful painkillers in its group. It has anti-inflammatory properties, which manifest themselves in disruption of the production of arachidonic acid and prostaglandins. Excipients: ethanol, propylene glycol, water, lavender oil.
Indications for the use of Diclofenac gel are:
- diseases of muscles and joints, including osteoarthritis, rheumatoid arthritis, radiculitis;
- any muscle pain, regardless of its origin;
- rheumatic pathologies of soft tissues (bursitis and tendovaginitis);
- various types of injuries - bruises, sprains, overstrain of joints and soft tissues, causing pain reactions and leading to inflammatory processes.
Diclofenac gel is used for muscle pain of any origin.
The drug is sometimes included in complex therapy for thyroid disease such as thyroiditis. The gel is used for external application. It helps relieve or completely eliminate pain in muscles and joints, both at rest and during movement.
It is recommended to use it to reduce morning joint stiffness and swelling, and normalize range of motion. The active components quickly penetrate the tissues, but only about 6% of diclofenac is absorbed, which causes far fewer side effects than using the drug in tablet form.
Contraindications for Diclofenac gel are the same as for ointment.
Interactions with other medicinal drugs and other types of interactions
However, the systemic absorption of diclofenac due to local stagnation of the drug is very low, and the likelihood of interaction is very low.
Features of stagnation.
The drug should be carefully administered simultaneously with oral NSAIDs through the possibility of intensifying unwanted effects and preventing systemic side effects. The drug should not be combined with other methods to treat diclofenac.
The likelihood of developing systemic side effects with locally infused diclofenac is insignificant compared to ingestion of its oral forms, but it does not turn off when the drug is ingested on very large sections of the skin for three hours. u.
If any viscosities appear on the skin, the drug should be injected.
The drug is recommended to be applied only to intact areas of the skin, avoiding exposure to burnt, wounded or infected skin, as well as to areas of the skin affected by eczema. There is no contact between the drug and the presence of mucous membranes. The drug cannot be used.
The drug should not be cured under a non-permeable occlusive dressing, but it may be cured under a non-occlusive dressing. If the ties become loose, the wounded area can be tied with a bandage.
In several cases, the development of scutulo-intestinal bleeding was reported in patients with a troubling history of illness.
The drug contains propylene glycol, which can cause skin rashes, and methyl parahydroxybenzoate (E 218), which can cause allergic reactions (possibly intensified).
Suspension during pregnancy or breastfeeding.
Clinical evidence of stagnation of vaginal women's intercourse, therefore stasis of the drug
Not recommended during pregnancy. The drug is contraindicated during the third trimester of gestation due to the possible development of labor weakness, impaired fetal function with subsequent low water supply and/or premature closure of the arterial duct.
The research process on animals did not reveal any effect of diclofenac on vagusity or fetal development, pregnancy or postnatal development of the child.
It is unknown what diclofenac is like when breast milk is congested, so congestion of the drug is not recommended during breastfeeding. Prote, if there are any reasons for the drug to harden during the breastfeeding period, the drug should not be applied to the breasts or large sections of the skin and should not harden for three hours.
This is due to the impact of diclofenac on human fertility during this current stagnation period.
This is due to the fluidity of the reaction during treatment with vehicles or other mechanisms.
Doesn't flow in.
Pharmacological properties and pharmacokinetics
Diclofenac ointment is included in the clinical and pharmacological group of non-steroidal anti-inflammatory drugs. Its active ingredient blocks cyclooxygenase, an enzyme that stimulates the production of pain and inflammatory mediators (prostaglandins, cytokines, bradykinins) from arachidonic acids. This determines the diverse therapeutic effect of the drug:
- relief of acute and chronic inflammatory processes;
- reducing the severity of pain;
- prevention of edema by blocking the migration of leukocytes and macrophages into inflammatory foci.
Diclofenac sodium binds predominantly to albumin, a protein in the blood plasma. It is distributed and accumulates in soft tissues, but the highest concentration is created in joints affected by pathologies. The active ingredient of the ointment is metabolized by liver cells and then excreted from the body with urine and bile acids.
Method of congestion and dosage
Grown up.
The drug is intended for external stagnation.
Apply the gel to the affected area of the skin 3-4 times per dose, lightly rubbing into the skin. The amount of the preparation that will stagnate should be equal to the size of the affected area (2–4 g, which is similar in size to the size of a cherry or pea pea, sufficient for application to a plot with an area of 400–800 cm2).
After application of the drug, it is necessary to keep your hands off the area while the area itself is undergoing treatment.
The difficulty of therapy depends on the nature of illness and the effectiveness of treatment. The drug should not be taken longer than 14 days after sleep. If the symptoms of illness do not change or worsen after 7 days of treatment, please consult a doctor.
Summer age patients.
Such patients will not require dose adjustment of the drug.
Patients with nitric deficiency.
There are no reasons why patients with nicotine deficiency will require special dosage selection.
Patients with liver failure.
There are no reasons why patients with liver failure will require special dosage selection.
Children.
Recommendations for dosing and therapeutic indications for administration of the drug to children up to 18 days of age.
Side effects
From the gastrointestinal tract, the following phenomena are possible:
- nausea
- dyspepsia
- diarrhea
- vomit
- flatulence
Rarely, hepatitis and gastric bleeding may occur.
From the central nervous system the following may be observed:
- headache
- insomnia
- drowsiness
- dizziness
- tremor
- depression
- visual impairment
Renal failure, anemia, hypotension or hypertension, and menstrual irregularities may also occur. According to recent studies, long-term treatment with diclofenac increases the risk of heart attack by 40%. Therefore, long-term treatment with the drug can be carried out only if there are no alternatives.
It is extremely rare, usually when the dosage regimen is violated or medical recommendations are not followed, systemic adverse reactions occur. They are manifested by attacks of suffocation, bronchospasms, urticaria, hypersensitivity, and angioedema. Local allergic reactions occur more often. Their characteristic symptoms are: irritation and swelling of the skin, rash, itching, peeling, and less commonly, photosensitivity.
Overdose
Overdosing is less likely due to low absorption of diclofenac into the systemic bloodstream during local congestion. In cases of epilepsy, follow the procedure so that 1 tube of the drug, 45 g each, contains the equivalent of 2.25 g of diclofenac sodium; This may result in the development of systemic adverse reactions.
In the event of a seizure, the drug should be immediately emptied and the adsorbent taken. Symptomatic treatment of stagnant therapeutic approaches is indicated for the treatment of severe NSAIDs.
Description and principle of operation
The drug was first introduced in 1973 by the Swiss pharmaceutical company Novartis and has since gained popularity as one of the most effective non-steroidal anti-inflammatory drugs.
According to its chemical structure, the active substance of the drug belongs to acetic acid derivatives. Its exact name is 2-(2,6-dichloraniline) phenylacetic acid. Medicines contain the sodium salt of this acid - diclofenac sodium.
Diclofenac has three types of action:
- Anti-inflammatory
- Antipyretic
- Painkiller
The anti-inflammatory properties of Diclofenac are especially strong. Its antipyretic effect is also quite strong. Often the drug helps when other means do not work. Diclofenac can also relieve pain, although its analgesic effect is not so powerful, so the drug is more suitable for relieving mild to moderate pain.
Side effects
The drug should be well tolerated. Unusual reactions include mild temporary reactions of the skin at the site of application. In rare cases, allergic reactions may be avoided.
Adverse reactions are classified according to frequency: very often: (>1/10); often (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rarely (≥1/10000, <1/1000); very rare (<1/10000); frequency unknown (frequency cannot be estimated based on available data).
Infections and invasions:
very rarely - pustular viscera.
On the side of the immune system:
very rarely - hypersensitivity reactions (including kropiv'yanka), angioneurotic pimples, buttocks.
On the side of the respiratory system, the organs of the chest and the mediastinum:
very rarely – bronchial asthma.
From the side of the skin and under the skin:
often – rash, redness, eczema, exanthema, erythema, dermatitis (including contact dermatitis), itching, liver, appearance of bumps and vesicles, papules, pustules, peeling and dry skin; rarely – bullous dermatitis; very rarely – light sensitivity reactions, such as hepatic skin inflammation, generalized skin irritation.
On the side of the herbal tract, adverse reactions occur even rarely after local stagnation of drugs such as diclofenac.
When the drug is administered in high doses or applied to large areas of the skin, it is not possible to exclude the possibility of systemic side reactions, as well as hypersensitivity reactions in the form of angioedema, dyspnea.
Information about suspected adverse reactions.
Information about suspected adverse reactions that occurred after drug registration is extremely important. This allows me to continuously monitor the balance of the measles/risks of the medicinal person. Health care professionals are asked to report any suspected adverse reactions through the national reporting system.
Which is better - Diclofenac ointment or gel?
For joint diseases, both forms are used. And there is no clear answer to the question which one is better. The gel is often prescribed due to the fact that it contains a large dose of the active substance and is better absorbed.
We invite you to familiarize yourself with Drugs for the treatment of the small intestine
As for skin reactions, when the gel is applied to the surface for some time, a film remains, permeable to air, but causing dry skin. A fat-based ointment creates an airtight layer, but moisturizes the skin.
