Diclofenac Retard

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Diclofenac retard: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Diclofenac retard

ATX code: M01AB05

Active ingredient: diclofenac (diclofenac)

Manufacturer: LLC "Ozon" (Russia)

Description and photo update: 2018-21-11

Prices in pharmacies: from 29 rubles.

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Sustained-release enteric-coated tablets, Diclofenac retard

Diclofenac retard - non-steroidal anti-inflammatory drug (NSAID); derivative of phenylacetic acid.

Release form and composition

Diclofenac retard is produced in the form of tablets of prolonged action, coated with an enteric coating: biconvex, round, almost white or white, with the possible presence of a rough surface (10 or 20 pieces in a contoured cell package, 1-8, 10, 20, 40, 60, 80 or 100 packages in a cardboard box; 10, 20, 30, 40, 50 or 100 pieces in a polymer container, 1, 5, 10 or 20 containers in a cardboard box).

1 tablet contains:

active substance: diclofenac sodium - 100 mg;
additional components: microcrystalline cellulose, lactose monohydrate (milk sugar), povidone (polyvinylpyrrolidone), magnesium stearate, talc, hypromellose;
enteric coating: polysorbate-80, cellacephate, titanium dioxide.

Pharmacological properties

Pharmacodynamics

Diclofenac sodium is an NSAID that has an analgesic, anti-inflammatory, antipyretic and antiplatelet effect. By indiscriminately suppressing the activity of cyclooxygenase-1 and cyclooxygenase-2, the active substance of the drug leads to disruption of the metabolism of arachidonic acid and a decrease in the amount of prostaglandins in the focus of inflammation. The agent demonstrates the greatest effectiveness against the background of inflammatory pains.

Pharmacokinetics

Due to the sustained release, the maximum concentration (C _max) of the active substance in the plasma is lower than the concentration created when using a short-acting drug, at the same time it remains high for a long period after taking Diclofenac retard. With oral administration of a prolonged-release preparation at a dose of 100 mg, the time required to reach C _max (TC _max) is 5 hours, C _max - 0.5–1 μg / ml.

The concentration of a substance in plasma is linearly dependent on the dose taken. Changes in the pharmacokinetic parameters of diclofenac after repeated administration are not observed. If the recommended dosage regimen is followed, the substance does not cumulate. Bioavailability is 50%, the connection with proteins (mostly with albumin) exceeds 99%.

The agent penetrates into the synovial fluid and breast milk. In synovial fluid, C _{max is} reached 2–4 hours later than in plasma, and the half-life (T _½) from the articular exudate can vary from 3 to 6 hours. The level of diclofenac in the synovial fluid 4–6 hours after its administration is higher than in plasma, and remains higher for another 12 hours.

50% of the drug is metabolized during the first passage through the liver. After oral administration, the area under the concentration-time curve is 2 times less than after parenteral administration of the drug at the same dose. Biotransformation of diclofenac is carried out by single or multiple hydroxylation and conjugation with glucuronic acid. The isoenzyme CYP2C9 is also involved in metabolic transformation. Metabolites are less pharmacologically active when compared with diclofenac.

The total clearance of Diclofenac retard is 260 ml / min, T _½ from plasma is 1–2 hours. Through the kidneys in the form of metabolites, 60% of the dose is excreted, unchanged - 1%, in the form of metabolites, the rest of the dose is excreted in the bile.

In the presence of severe renal failure [creatinine clearance (CC) less than 10 ml / min], the excretion of metabolites in the bile increases, but their concentration in the blood does not increase.

Against the background of compensated liver cirrhosis or chronic hepatitis, the pharmacokinetic parameters of Diclofenac retard do not change.

Indications for use

degenerative and inflammatory diseases of the musculoskeletal system: ankylosing spondylitis (ankylosing spondylitis), rheumatoid arthritis, psoriatic arthritis, osteochondrosis, gouty arthritis, deforming osteoarthritis of the spine and peripheral joints, including with radicular syndrome, bursinitis, tendinitis;
algodismenorrhea, inflammatory processes occurring in the small pelvis, including adnexitis;
pain syndrome: headache (including migraine) and toothache, sciatica, arthralgia, neuralgia, sciatica, myalgia, ossalgia, lumbago, post-traumatic and postoperative pain syndrome, accompanied by an inflammatory process, pain associated with cancer;
diseases of the throat, ear, nose of an infectious and inflammatory nature with severe pain syndrome: tonsillitis, pharyngitis, otitis media (as part of combination therapy).

According to the instructions, Diclofenac retard is intended for symptomatic treatment, reducing the severity of pain and inflammation at the time of use. The drug does not affect the progression of the disease.

Contraindications

Absolute:

partial or complete combination of bronchial asthma, recurrent polyposis rhinosinusitis and intolerance to acetylsalicylic acid or any other NSAID (including indications in history);
active gastrointestinal bleeding, erosive and ulcerative defects of the gastrointestinal tract and 12 duodenal ulcer;
intestinal diseases of an inflammatory nature (ulcerative colitis, Crohn's disease);
the period after the operation of coronary artery bypass grafting;
severe heart failure;
diagnosed hyperkalemia;
progressive kidney damage, severe renal failure (CC below 30 ml / min);
active liver disease or severe liver failure;
age up to 18 years;
impaired absorption of glucose-galactose, lactase deficiency, hereditary lactose intolerance;
III trimester of pregnancy;
hypersensitivity to any of their constituents or other NSAIDs.

Relative (it is recommended to use Diclofenac retard with extreme caution):

chronic heart failure, ischemic heart disease;
arterial hypertension;
peripheral arterial lesions;
chronic renal failure (CC 30-60 ml / min);
history of liver damage, hepatic porphyria;
diabetes;
dyslipidemia / hyperlipidemia;
cerebrovascular diseases;
bronchial asthma;
a history of gastrointestinal ulcer disease, presence of Helicobacter pylori infection;
a pronounced decrease in the volume of circulating blood (BCC) (including the state after extensive surgery);
smoking and / or alcoholism;
severe somatic pathologies;
long-term use of NSAIDs;
old age (including patients with low body weight, debilitated, receiving diuretics);
I – II trimesters of pregnancy;
the combined use of the following drugs: antiplatelet agents (acetylsalicylic acid, clopidogrel and others), anticoagulants (including warfarin), selective serotonin reuptake inhibitors (SSRIs) (for example, fluoxetine, citalopram, sertraline, paroxetine), oral glucocorticosteroids (glucocorticosteroids) including prednisone).

Instructions for use of Diclofenac retard: method and dosage

Diclofenac retard tablets 100 mg are taken orally, swallowed whole, without chewing or breaking, drinking plenty of water.

The drug is taken once a day, 100 mg (1 tablet). When the desired therapeutic effect is achieved, switching to maintenance therapy, the dose is gradually reduced to 50 mg (½ tablet) per day. The maximum daily dose should not exceed 150 mg.

If it is necessary to increase the daily dose to the maximum, it is allowed in addition to 1 tablet of Diclofenac retard (100 mg) to take 1 regular tablet of short-acting diclofenac (50 mg).

Side effects

nervous system: often - dizziness, headache; rarely - drowsiness; extremely rarely - insomnia, irritability, nightmares, anxiety, memory disorders, mental disorders, depression, impaired sensitivity, including paresthesia, convulsions, tremor, cerebrovascular disorders, disorientation, aseptic meningitis;
cardiovascular system: extremely rare - chest pain, palpitations, increased blood pressure, heart failure, vasculitis, myocardial infarction;
hematopoietic organs: extremely rarely - leukopenia, thrombocytopenia, aplastic and hemolytic anemia, agranulocytosis;
digestive system: often - nausea, epigastric pain, anorexia, vomiting, flatulence, dyspepsia, diarrhea, increased aminotransferase activity; rarely - proctitis, gastritis, diarrhea mixed with blood, melena, vomiting with blood, gastrointestinal ulcers (with or without bleeding or with perforation), jaundice, liver dysfunction, hepatitis; extremely rarely - glossitis, stomatitis, esophagitis, constipation, exacerbation of Crohn's disease or ulcerative colitis, nonspecific hemorrhagic colitis, fulminant hepatitis, pancreatitis;
urinary system: extremely rarely - proteinuria, hematuria, acute renal failure, nephrotic syndrome, interstitial nephritis, papillary necrosis;
respiratory system: rarely - bronchial asthma (including shortness of breath); extremely rare - pneumonitis;
sense organs: often - vertigo; extremely rarely - a violation of taste, visual impairment (diplopia, blurred vision), tinnitus, hearing impairment;
allergic reactions: anaphylactic / anaphylactoid reactions, including a marked decrease in blood pressure and shock; extremely rare - angioedema (including facial edema);
skin: often - skin rash; rarely - urticaria; extremely rarely - photosensitivity, hair loss, itching, bullous rashes, purpura, including allergic, exfoliative dermatitis, eczema, including multiforme and Stevens-Johnson syndrome, Lyell's syndrome;
others: rarely - edema.

Overdose

Symptoms of an overdose of Diclofenac retard include: epigastric pain, vomiting, diarrhea, gastrointestinal bleeding, tinnitus, dizziness, convulsions, lethargy; rarely - increased blood pressure, hepatotoxic effect, acute renal failure, respiratory depression, coma.

If this condition is suspected, gastric lavage, activated charcoal intake, symptomatic treatment aimed at eliminating an increase in blood pressure, seizures, functional renal disorders, gastrointestinal irritation, and respiratory depression are prescribed. Due to the intensive metabolism inherent in Diclofenac retard and a significant connection with proteins, the appointment of hemodialysis or forced diuresis is ineffective.

special instructions

To reduce the threat of adverse reactions from the gastrointestinal tract, it is necessary to take Diclofenac retard in the minimum effective dose for the shortest possible course.

In patients with heart or renal failure, in the elderly receiving diuretics, as well as in patients with a marked decrease in BCC (including due to extensive surgical intervention), when prescribing diclofenac, it is necessary to monitor renal function as a precautionary measure (since prostaglandins play important role in maintaining renal blood flow).

Against the background of long-term use of Diclofenac retard, it is required to monitor the indicators of hepatic function, the picture of peripheral blood, and the analysis of feces for occult blood.

For the relief of an acute attack of gout, it is advisable to use fast-acting dosage forms.

Diclofenac is able to influence the serum transaminase values, in the case when this effect is prolonged or complications arise, it is necessary to refuse to take the drug. Also, taking Diclofenac retard can increase potassium levels.

Influence on the ability to drive vehicles and complex mechanisms

During the period of therapy, one should refrain from driving vehicles and any other complex mechanisms due to a possible decrease in the speed of motor and mental reactions.

Application during pregnancy and lactation

In the III trimester of pregnancy, the drug is contraindicated, in the I – II trimesters it should be taken with caution.

If you need to take Diclofenac retard during lactation, you must stop breastfeeding.

It is not recommended to use the drug for women planning a pregnancy, as it negatively affects fertility. Patients with infertility (including those undergoing examination) should also cancel Diclofenac retard.

Pediatric use

Diclofenac retard is contraindicated for children and adolescents under 18 years of age.

With impaired renal function

The use of Diclofenac retard is contraindicated against the background of progressive kidney disease or severe renal failure (CC below 30 ml / min). In chronic renal failure (CC from 30 to 60 ml / min), the agent should be used with caution.

For violations of liver function

In the presence of active liver disease or severe hepatic insufficiency, Diclofenac retard is contraindicated. If there is a history of liver damage or hepatic porphyria, the drug is prescribed with caution.

Use in the elderly

Elderly patients are advised to use Diclofenac retard with caution.

Drug interactions

lithium preparations, methotrexate, digoxin, cyclosporin - the plasma concentration of these substances increases;
diuretics - their effect decreases;
acetylsalicylic acid - the level of diclofenac in the blood decreases;
potassium-sparing diuretics - the threat of hyperkalemia is aggravated;
cyclosporine - its nephrotoxicity increases;
thrombolytic agents (urokinase, streptokinase, alteplase), anticoagulants, corticosteroids, other NSAIDs - the risk of bleeding increases (mainly from the gastrointestinal tract);
methotrexate - its toxicity increases;
hypnotics and antihypertensive drugs - their effect is weakened;
paracetamol - the likelihood of the nephrotoxic effect of diclofenac increases;
hypoglycemic drugs - their effect decreases;
valproic acid, cefotetan, cefoperazone, cefamandol, plikamycin - the incidence of hypoprothrombinemia increases;
gold preparations, cyclosporine - the effect of diclofenac on the production of prostaglandins in the kidneys increases, which contributes to an increase in its nephrotoxicity;
colchicine, ethanol, corticotropin, SSRIs, St. John's wort preparations - the risk of bleeding in the gastrointestinal tract increases;
antibiotics from the quinolone group - the threat of seizures is aggravated;
drugs that block tubular secretion - the level of diclofenac in the plasma increases, which leads to an increase in its toxicity;
agents that cause photosensitization - the sensitizing effect of diclofenac to UV radiation increases.

Analogs

Diclofenac retard analogs are: Diclac Lipogel, Voltaren Emulgel, Voltaren, Diklak, Diclo-F, Diclobene, Dicloran, Diclovit, Diclonat, Diclogen, Diclofenac, Diclofenac retard Obolenskoe, Diclofeniklofenka Diclofenac Sandoz, Diclofenac-MFF, Diclofenac-Altfarm, Diclofenac-Akrikhin, Diclofenac-Eskom, Diclofenac-ratiopharm, Diclofenac-FPO, Diclofenaklong, Diclofenaco, Dorofenaclofentou, Naklofenaklong, Rapten Duo, Penceid, Flotak.

Terms and conditions of storage

Store out of the reach of children, protected from moisture and light, at a temperature not exceeding 25 ° C.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Diclofenac retard

According to reviews, Diclofenac retard is an effective remedy with a wide range of applications. The reviews indicate that the drug well relieves bone pain in osteochondrosis, osteoarthritis and arthritis, toothache, pain against the background of otitis media, pharyngitis, tonsillitis, migraine headache. To the advantages of the drug, patients consider its prolonged action, convenient mode of administration, and low cost. In some cases, to increase the effectiveness of the drug for pain in joints and soft tissues, it was used in combination with ointments and gels containing diclofenac.

The disadvantages of Diclofenac retard are considered possible serious side effects and a large list of contraindications, and therefore patients recommend using the drug only with minimal courses in the smallest doses.

The price of Diclofenac retard in pharmacies

The approximate price for Diclofenac retard 100 mg per pack containing 20 tablets can be about 30 rubles.