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DICLOGEN is a combined anti-inflammatory, antipyretic and analgesic drug.

Pharmacological properties

DICLOGEN® is a combined analgesic, antipyretic and anti-inflammatory drug. The mechanism of action is determined by the pharmacological properties of its constituent components. Diclofenac sodium, a derivative of phenylacetic acid, is a non-steroidal anti-inflammatory drug. The mechanism of action is associated with indiscriminate inhibition of cyclooxygenase (COX-1 and COX-2), which disrupts the metabolism of arachidonic acid and reduces the amount of prostaglandins at the site of inflammation. Most effective for inflammatory pain. It has anti-inflammatory, analgesic and antipyretic effects, and prevents platelet aggregation. Paracetamol is an aniline derivative that has an analgesic and antipyretic effect. The mechanism of the analgesic effect is associated with inhibition of prostaglandin synthesis mainly in the thermoregulation center in the hypothalamus, which explains the almost complete absence of anti-inflammatory effect. In the combined preparation DICLOGEN®, diclofenac sodium and paracetamol potentiate the clinical effects of each other.

Indications for use

Relief and elimination of pain in: - inflammatory diseases of the musculoskeletal system (rheumatoid arthritis, psoriatic, juvenile and chronic arthritis, acute gouty arthritis, ankylosing spondylitis, osteoarthritis); — degenerative diseases of the musculoskeletal system (deforming osteoarthritis, osteochondrosis, arthrosis, spondyloarthrosis); - diseases of periarticular tissues (tenosynovitis, bursitis, tendinitis, tenosynovitis); - lumbago, sciatica, neuralgia, myalgia; — post-traumatic (sprains, dislocations, sports injuries) and postoperative pain; - diseases of the ENT organs (pharyngitis, tonsillitis, otitis media) as part of complex therapy; - headache and toothache; - diseases of the female genital organs (algodismenorrhea, adnexitis); - febrile syndrome.

Directions for use and doses

The drug is taken orally, without chewing, during or after meals, with a sufficient amount of water. At the beginning of treatment, adults and adolescents over 12 years of age weighing more than 60 kg are recommended to take 2-3 DICLOGEN® tablets per day.

For moderately severe symptoms of the disease, as well as for long-term therapy, as a rule, it is enough to take 2 tablets of the drug per day - one tablet in the morning and in the evening. The maximum single dose is 2 tablets. Children over 12 years old and weighing more than 30 kg are prescribed 1/2 tablet. 2-3 times/day. The interval between each next dose is at least 4 hours. The maximum duration of treatment for adults is 7 days, for children – 3 days. If you miss another dose of the drug, you must take the next dose as soon as possible. However, you should not double the dose to compensate for the missed dose.

With long-term use of the drug, it is necessary to carry out regular monitoring for the possible occurrence of erosion of the gastrointestinal mucosa with the subsequent development of gastrointestinal bleeding, as well as perform liver function tests for the purpose of early detection of possible hepatotoxicity of the drug.

Diclofenac sodium (Diclogen) is the “gold standard” in the treatment of joint diseases

Most modern nonsteroidal anti-inflammatory drugs (NSAIDs) have high anti-inflammatory, analgesic and antipyretic activity, which makes them indispensable in the treatment of inflammatory and degenerative rheumatic diseases.
NSAIDs are the most common drugs used in clinical practice in recent decades
[1, 2].

Among the well-known NSAIDs, diclofenac sodium is one of the best representatives of this class. The combination of distinct anti-inflammatory and analgesic effects with good tolerability make it one of the most frequently prescribed and long-term drugs [8]. Despite the emergence of a new class of anti-inflammatory drugs - specific cyclooxygenase-2 inhibitors [4, 5, 6, 7], clinical practice is unlikely to be able to do without the widespread use of traditional NSAIDs.

Diclofenac sodium has been used for more than 25 years. However, in the last decade, so many brand names have appeared on the pharmaceutical market that sometimes it is not easy for a specialist to navigate this abundance of generic names for the same drug. The offered drugs of diclofenac sodium differ from each other not only in the manufacturer, but also in price, therapeutic effect, and frequency of side effects.

Our attention was drawn to diclofenac sodium under the brand name “ Diclogen”

”, produced by the company “Agio-pharmaceuticals”. Diclogen is available in enteric film-coated tablets of 50 mg, in retard form of 100 mg and as a solution for injection in ampoules of 75 mg (3 ml). There is a dosage form in the form of “Diclogen” gel. Doctors in Belarus are little familiar with Diclogen, which recently appeared in the republic; the domestic drug diclofenac sodium, ortofen, is better known.

Pharmacokinetics of Diclogen

Features of Diclogen are new coating systems for the active substance in the form of a special acid-resistant coating that protects the gastric mucosa

. Absorption of the drug occurs mainly in the small intestine. The retard form of Diclogen ensures a stable level of therapeutic concentration in the blood and a long-lasting effect of the drug. The possibility of a single daily dose greatly simplifies treatment and creates convenience for the patient.

When taken orally, Diclogen is quickly and completely absorbed from the gastrointestinal tract. Food slows down the rate of absorption, but the amount of active substance absorbed does not change. The maximum concentration in blood plasma when ingesting Diclogen tablets in a single dose of 50 mg is achieved 2 hours after administration and is 1.5 mcg/ml. The concentration of the drug in plasma is linearly dependent on the dose.

When using retard tablets, absorption of the drug occurs more slowly, and the maximum concentration is reached after 4–5 hours and is 0.45 mcg/ml. When administered intramuscularly, the area under the concentration curve is approximately 2 times greater than the corresponding value observed when taking tablets orally.

The systemic bioavailability of the retard form of Diclogen after oral administration is 82% of the corresponding figure after taking a 50 mg tablet. In blood plasma, more than 99% of the active substance is bound to albumin. The half-life of the drug is 1–2 hours. Approximately 60% of the dose is excreted in the form of metabolites by the kidneys, up to 1% is excreted unchanged. The rest is excreted as metabolites in the bile and excreted in the feces. In patients with renal failure, the proportion of metabolites excreted in bile increases, so no increase in concentration in the blood is observed. With repeated administration of the drug, its pharmacokinetics do not change.

The purpose of this work was to evaluate the effectiveness and safety of the drug Diclogen in certain rheumatic diseases.

Material and methods

We conducted an open two- to three-week study of the effectiveness and safety of different forms of the drug Diclogen. The study included 52 patients (rheumatoid arthritis - 18 people, osteoarthritis - 21, Reiter's disease - 6, glenohumeral periarthritis - 4, lateral epicondylitis - 3 people). There were 23 men, 29 women. The average age of the observed patients was 51.6 years.

In patients with rheumatoid arthritis, the 2nd degree of activity of the pathological process, II – III stages of the disease, was noted. Patients with osteoarthritis suffered predominantly from gonarthrosis and coxarthrosis of Kollgren stages II–III. Of the concomitant diseases, arterial hypertension was detected in 5 patients, chronic calculous cholecystitis in 6, chronic gastritis in 11,

For patients with rheumatoid arthritis and Reiter's disease, Diclogen was prescribed intramuscularly at 75 mg during the day and an additional 50 mg orally in the morning and evening. After 3 intramuscular injections of Diclogen, the 4th and 5th injections were performed with domestic ortofen at a dose of 75 mg (3 ml). After 5 days, intramuscular injections were stopped altogether and the patient was transferred to taking Diclogen orally at a daily dose of 100–150 mg/day. depending on the need (the severity of inflammation and pain was assessed).

For osteoarthritis, intramuscular injections were prescribed for 3 days. Additionally, 50 mg of Diclogen was administered orally in the evening. The third (last) injection, as in patients with rheumatoid arthritis, was performed using ortofen. After 3 days, the daily dose of the drug was 50–100 mg orally. For periarticular lesions (periarthritis, epicondylitis), from the first day, patients were prescribed a retard form of the drug, 100 mg orally.

On days 10–12 of treatment in all patients, Diclogen was replaced for 3 days with an appropriate dose of ortofen. Patients were asked to compare two drugs (Diclogen and Ortofen), taken both by injection and by mouth.

During the period of treatment with Diclogen, the previous basic therapy in patients with rheumatoid arthritis did not change, intra-articular injections of glucocorticoids were not performed. Previous NSAID therapy was discontinued.

Patients with rheumatoid arthritis, Reiter's disease and osteoarthritis were observed for 3 weeks; patients with periatritis and epicondylitis were analyzed after 2 weeks of treatment. During the observation process, the tolerability of Diclogen and its comparative effectiveness with ortofen were assessed.

Research results

All 52 patients completed the study. In no case did Diclogen have to be discontinued due to intolerance or side effects. According to doctors, only 2 patients had no therapeutic effect of the drug. These were patients with stage III coxarthrosis, in whom, due to the narrowing of the joint space, pain occurred with any movement in the joint after a state of rest. In general, an assessment of the effectiveness of the use of Diclogen in patients with rheumatoid arthritis, osteoarthritis, Reiter's disease and diseases of the periarticular tissues is presented in the table.

It can be stated that
“significant improvement” and “improvement” as assessed by the doctor and patients was noted in 96.2% of cases
. The results of using Diclogen as a “significant improvement” were assessed more modestly by patients compared to doctors (19% versus 25% by doctors).

While taking Diclogen, there was a significant positive change in pain syndrome, number, inflamed joints, and duration of morning stiffness

. The severity of starting and night pain in patients with osteoarthritis decreased or completely disappeared. The functional capabilities of patients have increased.

In patients with rheumatoid arthritis, under the influence of treatment with Diclogen, ESR significantly decreased from 41.2±2.6 to 23.4±2.1 mm/h, which confirms the good anti-inflammatory effect of the drug. No decrease in white blood cell or hemoglobin levels was observed.

Diclogen was well tolerated. Only three patients experienced side effects during the 3-week course of treatment. One patient experienced nausea, which disappeared when the dose of Diclogen was reduced to 100 mg per day (50 mg 2 times). In 2 patients, after taking the retard form of Diclogen, dizziness, sweating, and “floaters” appeared before the eyes. Transferring patients to taking the drug in tablets of 50 mg 2 times a day eliminated these side effects. It is noteworthy that in no case did we note the appearance of NSAID gastropathy, despite the presence of concomitant diseases of the gastrointestinal tract in 17 patients.

Compared with Ortofen, 49 out of 52 patients (94.2%) noted better tolerability and a more pronounced analgesic effect of Diclogen. None of the patients considered Diclogen a weaker drug than ortofen. Therefore, Diclogen is superior to Ortofen both in strength and tolerability.

Conclusion

Our data indicate that Diclogen is an effective and well-tolerated drug

for the treatment of patients with rheumatoid arthritis, osteoarthritis, reactive arthritis, periarticular lesions of soft tissues. Diclogen is superior to ortofen in effectiveness and tolerability. The possibility of using different dosage forms expands the scope of use of Diclogen, which helps to achieve the best results.

Among classical NSAIDs, diclofenac sodium reliably occupies the position of the “gold standard” when assessing the effectiveness of new NSAIDs [3]. In terms of the strength of its anti-inflammatory effect, it is second only to indomethacin, but in terms of safety it is significantly superior to it.

Diclogen, having a good anti-inflammatory effect, analgesic effect, an excellent price/efficacy profile and price/safety ratio, is superior to the cheapest and most accessible ortofen. Taking into account the above, Diclogen can be included in the group of diclofenac drugs, which are the “gold standard” for the treatment of joint diseases.

The list of references can be found on the website https://www.rmj.ru

Diclofenac sodium –

Diclogen (trade name)

(Agio Pharmaceuticals)
References:
1. Nasonov E.L. Non-steroidal anti-inflammatory drugs (Prospects for use in medicine). – M., 2000. – 262 p.

2. Nasonov E.L., Nasonova V.A. //Wedge. medicine. – 1996. – No. 8. – P. 13 – 17.

3. Nasonova V.A. 11 Scientific and practical rheumatology. – 2000. – No. 4, – P. 1 b – 21.

4. Distel MD Mueller CD Bluhmki E., Fries J, !1 Br. J. Rhewnatol. – 1996. – Vol. 35, Suppl. 1. –R. 68–71.

5. Emery P., Zeidler H.. Kvien T.K. et al. !1 Lancet. – 1999. – Vol. 354. – P. 2106 – 2111.

6. Hawkey CJ It Lancet. – 1999. – Vol. 353. – R, 307 – 314.

7. Peterson WL, Cryer V. I/ JAMA. – 1999. – Vol, 282. – P.1961 – 1963.

8. Wittmborg A., Petersen G., Lorcowski G., Branbunt T. It Z. Rheumatol. – 1998. – Bd. 57, N4.–S.215–221.

Diclofenac gel

Dosage form

Gel for external use

Composition per 100 g:

Active substance

: diclofenac sodium – 1.00 g.

Excipients

: 2-propanol – 45.00 g, macrogol 7 glyceryl cocoate – 6.00 g, hypromellose 4000 – 3.00 g, Scots pine oil – 0.15 g, lavender oil – 0.05 g, purified water – up to 100 .00 g.

Description

Colorless or with a slight yellowish tint, transparent gel with a characteristic odor.

Pharmacotherapeutic group

Non-steroidal anti-inflammatory drug (NSAID).

ATX code: M02AA15.

Pharmacological properties

Pharmacodynamics

The active component diclofenac is a non-steroidal anti-inflammatory drug with pronounced analgesic, anti-inflammatory and antipyretic properties. Indiscriminately inhibiting cyclooxygenase types 1 and 2, it disrupts the metabolism of arachidonic acid.

Diclofenac 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.

Thanks to its hydroalcoholic base, 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 skin hydration. After applying Diclofenac, gel for external use 1% (4 applications per day) to a skin surface area of 400 cm2, the concentration of the active substance in the plasma corresponds to its concentration when using 2% diclofenac gel (2 applications per day). On day 7, the relative bioavailability of the drug (AUC ratio) is 4.5% (for an equivalent dose of diclofenac sodium salt). When wearing a moisture-permeable dressing, suction 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. Maximum plasma concentrations were approximately 100 times lower than after oral administration of the same amount of diclofenac. 99.7% of diclofenac is bound to plasma proteins, mainly to 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 terminal half-life is 1-2 hours. The half-life of metabolites, including two pharmacologically active ones, is also short and amounts to 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 diclofenac and its metabolites are excreted in the urine.

Indications for use

• Back pain due to inflammatory and degenerative diseases of the spine (sciatica, osteoarthritis, lumbago, sciatica),

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

• Muscle pain (due to sprains, strains, bruises, injuries),

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

Contraindications

Hypersensitivity to diclofenac or other components of the drug; tendency to develop attacks of bronchial asthma, skin rashes or acute rhinitis when using acetylsalicylic acid or other NSAIDs; pregnancy (III trimester), breastfeeding; children's age (up to 12 years); violation of the integrity of the skin at the intended site of application.

Carefully

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

Use during pregnancy and breastfeeding

Due to the lack of data on the use of Diclofenac in pregnant women, the use of the drug during the first and second trimesters of pregnancy is recommended only as prescribed by a doctor, weighing the benefits for the mother and the risk for the fetus.

The drug is contraindicated in the third trimester of pregnancy due to the possibility of decreased uterine tone, impaired fetal renal function with subsequent development of oligohydramnios and/or premature closure of the fetal ductus arteriosus.

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

There are no data on the use of Diclofenac and its effect on fertility in humans.

Directions for use and doses

Externally.

For adults and children over 12 years of age, the drug is applied to the skin 2 times a day (every 12 hours: preferably morning and 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 twice the size of a cherry or walnut) is enough to treat an area of 400-800 cm2. If your hands are not the area where pain is localized, then after applying the drug they should be washed. The duration of treatment depends on the indications and the observed effect. The gel should not be used for more than 14 days for post-traumatic inflammation and rheumatic diseases of soft tissues without a doctor’s recommendation. If after 7 days of use the therapeutic effect is not observed or the condition worsens, you should consult a doctor.

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

The tubes can have either a regular cap (round shape) or an innovative cap (triangular shape), which is especially convenient for use when the mobility of the hand joints is limited due to osteoarthritis or other joint diseases or injuries.

Side effect

Classification of the frequency of occurrence of adverse reactions:

very often (> 1/10); often (> 1/100, < 1/10); uncommon (> 1/1000, < 1/100); rare (> 1/10000, < 1/1000); very rare (< 1/10000), including isolated reports.

Infectious and parasitic diseases:

Very rare: pustular rash.

Immune system disorders:

Very rare: hypersensitivity reactions (including urticaria), angioedema. Respiratory, thoracic and mediastinal disorders: Very rare: asthma.

Disorders of the skin and subcutaneous tissues:

Common: dermatitis (including contact dermatitis), rash, erythema, eczema, itching.

Rarely: bullous dermatitis.

Very rare: photosensitivity reactions.

If any side effects occur, including those not indicated in the instructions, you must stop using the drug and consult a doctor.

Overdose

Due to the low systemic absorption when applying the gel, overdose is unlikely.

In case of accidental ingestion, systemic adverse reactions may develop. Treatment of overdose due to accidental ingestion: gastric lavage, induction of vomiting, activated charcoal, symptomatic therapy. Dialysis and forced diuresis are not effective due to the high degree of binding of diclofenac to plasma proteins (about 99%).

Interaction with other drugs

The drug may enhance the effect of drugs that cause photosensitivity. Clinically significant interactions with other drugs have not been described.

special instructions

Diclofenac should be applied only to intact skin, avoiding contact with open wounds. The drug should not come into contact with the mouth, eyes or mucous membranes. After applying the drug, a bandage may be applied, but airtight occlusive dressings should not be applied. If a skin rash develops after application of the drug, its use should be discontinued.

The effect of the drug on the ability to drive vehicles and machinery

Does not affect.

Release form

Gel for external use 1%.

5, 10, 15, 20, 25, 30, 35, 40, 50, 60, 70, 80, 90, 100 g in orange glass jars with a triangular rim and a lid that is tensioned with a sealing element.

5, 10, 15, 20, 25, 30, 35, 40, 50, 60, 70, 80, 90, 100 g in polymer jars complete with lids or in polyethylene terephthalate jars with closures.

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

Each jar and tube, along with instructions for use, is placed in a cardboard pack.

Storage conditions

At a temperature not higher than 25 °C.

Keep out of the reach of children.

Best before date

3 years.

Do not use after the expiration date stated on the packaging.

Vacation conditions

Available without a prescription.