Dicloberl
Dikloberl: 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: Dicloberl
ATX code: M01AB05
Active ingredient: diclofenac (diclofenac)
Producer: Berlin-Chemie AG / Menarini Group (Germany)
Description and photo updated: 2018-26-11
Dicloberl is a non-steroidal anti-inflammatory drug.
Release form and composition
Dosage forms:
- enteric film coated tablets (Dikloberl 50): from light brown to yellow, with a smooth surface (10 pcs. in blisters, in a cardboard box 5 or 10 blisters);
- hard capsules of prolonged action (Dikloberl retard): gelatinous hard, size No. 2, from white to cream; inside the capsules - spherical granules of ivory or white color (10 pcs. in blisters, in a cardboard box 1, 2 or 5 blisters);
- solution for injection (Dikloberl N 75): a clear colorless or almost colorless liquid (3 ml in glass ampoules, in a cardboard box of 1 or 5 ampoules);
- rectal suppositories (Dikloberl 50 or 100): torpedo-shaped, ivory (5 pcs. in blisters, in a cardboard box 1 or 2 blisters).
1 tablet contains:
- active substance: diclofenac sodium - 50 mg;
- auxiliary components: lactose, sodium starch glycolate (type A), corn starch, magnesium stearate, povidone (K 30), 30% dispersion of methacrylate copolymer (type A), polyethylene glycol 400, polyethylene glycol 6000, simethicone emulsion, talc, hypromellose, titanium dioxide (E171), iron oxide yellow (E172).
1 capsule contains:
- active substance: diclofenac sodium - 100 mg;
- auxiliary components: corn starch, sucrose, shellac, sodium hydroxide, ammonium-methacrylate copolymer (type A), titanium dioxide (E171), gelatin, talc.
1 ampoule contains:
- active substance: diclofenac sodium - 75 mg;
- auxiliary components: sodium hydroxide solution, benzyl alcohol, beckoning, propylene glycol, acetylcysteine, water for injection.
1 suppository contains:
- active substance: diclofenac sodium - 50 mg or 100 mg;
- auxiliary components: solid fat; additionally in the composition of suppositories at a dose of 50 mg - ethanol 96%, propyl gallate, corn starch.
Pharmacological properties
Pharmacodynamics
Dicloberl is a non-steroidal anti-inflammatory drug (NSAID) with a pronounced antirheumatic, analgesic and antipyretic effect due to the properties of its active substance diclofenac. Diclofenac is a non-steroidal compound that inhibits the biosynthesis of prostaglandins, which play a significant role in the onset and development of the inflammatory process, pain syndrome and fever.
The results of laboratory studies prove the absence of the suppressive effect of therapeutic doses of sodium diclofenac on the biosynthesis of proteoglycans in cartilage tissue.
The use of Dikloberl for the treatment of rheumatic diseases contributes to a significant reduction in the severity of pain at rest and during movement, morning stiffness of the joints, their swelling.
In the treatment of inflammation caused by trauma or surgery, the anti-inflammatory and analgesic effect of Dikloberl is manifested by the rapid elimination of pain, a decrease in inflammation and swelling of damaged tissues. It also reduces the need for opioids for postoperative pain relief.
Diclofenac also exhibits pronounced analgesic activity in the case of elimination of moderate and severe pain sensations of non-rheumatic origin.
Pharmacokinetics
When taking enteric film-coated tablets, the maximum concentration (C max) of diclofenac in plasma is reached after 2 hours and averages 0.0015 mg / ml. After oral administration of capsules, as a result of the slow release of the active substance, it takes more time to reach the C max of diclofenac in plasma.
The systemic bioavailability of capsules averages 82% of the corresponding indicator after oral administration of 100 mg of diclofenac in the form of an enteric tablet. Simultaneous food intake does not clinically affect the absorption and systemic bioavailability of Dikloberl. There is a linear relationship between the dose and the amount of absorbed active substance.
After intramuscular (i / m) administration of diclofenac at a dose of 75 mg, its C max in blood plasma is reached after 10–20 minutes.
After rectal administration of suppositories at a dose of 50 mg, absorption occurs quickly, C max in blood plasma is reached after 1 hour, the maximum concentration per dose unit is 2/3 of the level after taking the tablets.
The total concentration (AUC) with intramuscular administration is almost twice as high as with oral and rectal administration of an equivalent dose of diclofenac, this is due to the fact that during the first passage through the liver, about half of the dose is metabolized.
Pharmacokinetic indices do not change with repeated use of Dicloberl.
Subject to the dosing regimen, the accumulation of the active substance is not observed.
Serum protein binding - 99.7%, to a greater extent (99.4%) with albumin.
The volume of distribution (V d) is 0.12–0.17 l / kg.
Penetrates into synovial fluid, to achieve C max in synovial fluid it takes 2–4 hours more than in blood plasma.
The half-life (T 1/2) from the synovial fluid is 3-6 hours. The content of diclofenac in the synovial fluid begins to exceed C max in the blood plasma 2 hours after it is reached and continues to remain higher for 12 hours.
Diclofenac is biotransformed mainly by single and multiple methoxylation and hydroxylation to form several phenolic metabolites and partly by glucuronidation of an unchanged molecule. Most of the phenolic metabolites (3 - hydroxy, 4 - hydroxy, 5 - hydroxy, 4 ՛, 5 - dihydroxy - and 3 - hydroxy-4 - methoxy-diclofenac) are conjugated with glucuronic acid. Two of them are pharmacologically active, but significantly inferior to the action of diclofenac.
(T 1/2) from plasma - 1–2 hours.
About 60% of the dose of the drug is excreted through the kidneys in the form of inactive metabolites and less than 1% - unchanged. The rest is through the intestines.
In case of impaired renal function, the use of therapeutic doses of Dikloberl does not cause accumulation of the active substance. When creatinine clearance (CC) is less than 10 ml / min, the calculated equilibrium concentrations of hydroxylated metabolites in blood plasma are approximately 4 times higher than the level of similar indicators with normal renal function. This excess has no clinical significance; all metabolites are then excreted in the bile.
In chronic hepatitis, compensated liver cirrhosis, the pharmacokinetic parameters of diclofenac metabolism do not differ from those in patients without liver dysfunction.
In elderly patients, changes in the absorption, metabolism and excretion of the drug were not observed.
Indications for use
- rheumatic diseases of inflammatory and degenerative genesis, including rheumatoid arthritis, ankylosing spondylitis (ankylosing spondylitis), acute attacks of gout, osteoarthritis, spondyloarthritis;
- rheumatic diseases of extra-articular soft tissues, including periarthritis of the shoulder scapula, tendinitis, tendovaginitis, bursitis;
- pain syndromes from the spine;
- inflammation after trauma, including sprains, dislocations, fractures.
In addition, Dikloberl tablets, capsules and suppositories are used to relieve pain syndrome of post-traumatic and postoperative genesis, which is accompanied by inflammation and edema, including conditions after orthopedic and dental surgery.
Additional indications for Dicloberl tablets and suppositories:
- primary dysmenorrhea, adnexitis and other gynecological pathologies accompanied by inflammation and pain syndrome;
- severe form of pharyngotonsillitis, otitis media and other inflammatory diseases in otorhinolaryngology, accompanied by severe pain syndrome (as an adjunct in complex therapy).
Contraindications
- acute stomach or intestinal ulcer;
- III trimester of pregnancy;
- breast-feeding;
- individual intolerance to the components of the drug.
It is not recommended to prescribe Dicloberl in the I and II trimesters of pregnancy, unless the expected effect of the drug for the mother exceeds the potential threat to the fetus.
It is recommended to use Dikloberl with caution for the treatment of elderly patients, debilitated patients or patients with a low body weight.
In addition, there are additional contraindications for certain dosage forms of Dikloberl.
Tablets, capsules and suppositories
- gastrointestinal bleeding or perforation;
- the presence of high risk factors for blood clotting, the development of postoperative or cerebrovascular bleeding, hematopoietic disorders or hemostasis disorders;
- an indication in the history of the development of bleeding or perforation of the gastrointestinal tract due to previous treatment with NSAIDs;
- an indication of a history of two or more separate episodes of diagnosed ulcer or bleeding;
- active or recurrent form of peptic ulcer disease or bleeding;
- Crohn's disease, ulcerative colitis and other intestinal diseases of inflammatory etiology;
- renal and / or hepatic impairment;
- congestive heart failure II – IV functional class according to NYHA classification (New York Heart Association);
- ischemic heart disease with angina pectoris, myocardial infarction;
- cerebrovascular disease in patients with episodes of transient ischemic attacks or stroke;
- peripheral arterial disease;
- treatment of perioperative pain with coronary artery bypass grafting or the use of a heart-lung machine;
- established hypersensitivity to ibuprofen, acetylsalicylic acid and other NSAIDs, accompanied by the development of attacks of bronchial asthma, urticaria, acute rhinitis or angioedema;
- proctitis;
- children under 14 years of age for the appointment of suppositories at a dose of 50 mg;
- age up to 18 years.
It is contraindicated to prescribe Dicloberl tablets to patients with glucose-galactose malabsorption syndrome, hereditary galactose intolerance, lactase deficiency.
Injection
- disorders of blood clotting and the function of the hematopoietic system of unknown origin;
- gastrointestinal, cerebral and other active bleeding;
- bronchial asthma;
- age up to 18 years.
Under medical supervision, it is recommended to use Dicloberl N 75 for porphyria, systemic lupus erythematosus, mixed collagenoses, high blood pressure (BP), heart failure, renal dysfunction, severe liver dysfunction, hay fever, nasal polyps or obstructive respiratory tract diseases, in patients with ulcerative colitis, Crohn's disease or gastric ulcer and intestinal ulcer (including history), in the period after major surgical operations.
Instructions for the use of Dikloberl: method and dosage
To reduce the risk of side effects of diclofenac, it is recommended to use the minimum effective dose of Dicloberl for a short period of time.
The doctor prescribes the dosage form, dose and treatment period individually, taking into account clinical indications.
For the treatment of elderly patients, debilitated patients or patients with low body weight, it is recommended to use the lowest effective dose.
Pills
Dikloberl tablets are taken orally, swallowing whole, preferably before meals, with a sufficient amount of liquid.
The integrity of the enteric coating must not be violated.
The initial dose is 1 pc. 2-3 times a day.
To prevent nighttime pain or joint stiffness in the morning, pill treatment can be combined with rectal suppositories at a dose of 50 mg at bedtime. The total daily dose of diclofenac should not exceed 150 mg.
The recommended dosage of Dikloberl for the treatment of primary dysmenorrhea: initial dose - 1 pc. 2-3 times a day. The dose is selected individually, taking into account the severity of the pain syndrome, if necessary, within several menstrual cycles, it can be increased to the maximum daily dose - 4 pcs. It is recommended to start taking pills when the first pain symptoms occur. Continue taking for no more than a few days.
Capsules
Dikloberl capsules are taken orally, without chewing, with a sufficient amount of liquid, preferably with meals.
Recommended dosage: 1 pc. in a day.
If the symptoms of the disease are most pronounced at night and in the morning, capsules should be taken in the evening.
Injection
The solution is intended for deep intramuscular injection, which is performed in the gluteus muscle.
The recommended dosage of Dikloberl is 75 mg once.
If more prolonged therapy is necessary, treatment should be continued with the use of oral or rectal forms of Dicloberl. The total daily dose when using several dosage forms of the drug should not exceed 150 mg of diclofenac.
Suppositories
Suppositories are used only rectally by deep insertion into the rectum. It is advisable to pre-clean the intestines.
The initial daily dose of Dikloberl is 100-150 mg, with mild symptoms of the disease or long-term treatment, 75-100 mg per day is sufficient, the dose is divided into 2-3 injections.
Recommended dosage:
- primary dysmenorrhea: 50–150 mg daily. In the absence of the desired therapeutic effect, the initial daily dose can be increased to 200 mg over several menstrual cycles. The use of suppositories should be started when the first pain symptoms appear. The duration of treatment depends on the dynamics of pain syndrome regression;
- migraine attacks: the initial dose is 100 mg per day. To achieve a clinical effect, repeated administration of Dikloberl at a dose of 100 mg on the first day of treatment is allowed. In the following days, if necessary, treatment can be continued (the daily dose should not exceed 150 mg, it is divided into 2-3 injections);
- juvenile rheumatoid arthritis: children over the age of 14 are prescribed Dicloberl 50 suppositories at the rate of no more than 3 mg per 1 kg of the child's weight. The maximum daily dose is 150 mg.
Side effects
- from the lymphatic system and the blood system: leukopenia, thrombocytopenia, agranulocytosis, pancytopenia, aplastic anemia, hemolytic anemia;
- on the part of the cardiovascular system: chest pain, palpitations, heart failure, arterial hypotension, arterial hypertension, vasculitis, myocardial infarction;
- from the immune system: hypersensitivity reactions in the form of skin rash, itching, urticaria, anaphylactic and anaphylactoid reactions (including heart palpitations, hypotension, narrowing of the airways, respiratory arrest, shock), allergic vasculitis, angioedema (including edema of the tongue, face, edema pharynx), pneumonia;
- from the nervous system: general malaise, drowsiness, headache, agitation, dizziness, fatigue, anxiety, paresthesia, memory impairment, confusion, tremors, convulsions, hallucinations, impaired sensitivity, stroke, aseptic meningitis;
- mental disorders: insomnia, irritability, psychotic disturbances, nightmares, disorientation, depression;
- on the part of the organs of vision: blurred vision, visual disturbances, optic neuritis, diplopia;
- from the hearing organs and the labyrinth: hearing disorders, ringing in the ears, vertigo;
- from the respiratory system, chest and mediastinal organs: shortness of breath, asthma, pneumonitis;
- from the hepatobiliary system: an increase in the level of transaminases, liver dysfunction, jaundice, hepatitis, fulminant hepatitis, hepatonecrosis, liver failure;
- from the gastrointestinal tract: taste disturbances, nausea, vomiting, abdominal pain, constipation, glossitis, stomatitis, ulcerative stomatitis, esophageal dysfunction, diarrhea, gastritis, dyspepsia, flatulence, diaphragmatic type of intestinal stenosis, colitis (including hemorrhagic colitis, Crohn's disease), pancreatitis, gastric and / or intestinal ulcers (including bleeding or perforation, including fatal, especially in elderly patients), gastrointestinal bleeding (vomit and diarrhea mixed with blood, melena);
- dermatological reactions: itching, photosensitivity, hair loss, erythema, exanthema, eczema, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), erythema polymorphism, exfoliative dermatitis, purpura (including allergic purpura);
- from the urinary system: edema (more often with arterial hypertension or renal failure), interstitial nephritis, acute renal failure, proteinuria, hematuria, papillary necrosis of the kidney, nephrotic syndrome;
- infections and infections: symptoms of aseptic meningitis (very rare) - neck stiffness, headache, nausea, vomiting, fever, confusion;
- from the reproductive system and mammary glands: impotence;
- general disorders: edema;
- local reactions: burning at the injection site, sometimes damage to the skin can be observed with the formation of sterile abscesses, necrosis of adipose tissue.
Overdose
Symptoms: disorientation, drowsiness, agitation, nausea, vomiting, tinnitus, headache, epigastric pain, diarrhea, dizziness, gastrointestinal bleeding, convulsions, coma. In severe intoxication - liver damage, acute renal failure.
Treatment: there is no specific antidote. You should immediately (within one hour after taking the ultra-high dose of diclofenac) wash the stomach or induce artificial vomiting, then take activated charcoal. Provide medical monitoring of the patient's condition. This is followed by the appointment of symptomatic therapy, supportive measures for arterial hypotension, respiratory depression, renal failure, gastrointestinal disorders, convulsions.
The use of forced diuresis, dialysis or hemoperfusion is ineffective.
special instructions
Particular care should be taken when treating patients with allergic reactions to drugs because of the drug's ability to significantly increase hyperergic reactions. In addition, the risk group includes patients with bronchial asthma, seasonal allergic rhinitis, polyps, chronic obstructive pulmonary disease or respiratory tract infections, allergic reactions to other substances.
The introduction of Dicloberl's solution is shown only as a single injection in cases of need for a very rapid onset of action or when oral and rectal administration is impossible. It is usually prescribed at the beginning of the course of therapy. Due to the possible development of allergic reactions (including shock), it is necessary to monitor the patient's condition for one hour after the injection.
If you experience gastrointestinal ulcers or bleeding, you must stop using Dicloberl.
Caution should be exercised when treating elderly patients due to the increased risk of adverse reactions from the gastrointestinal tract, including bleeding and perforation.
Treatment should be accompanied by careful monitoring of kidney and liver function, liver enzyme levels, and monitoring of a complete blood count.
If symptoms of hypersensitivity (skin rashes, mucosal lesions) appear, Dicloberl should be canceled.
Consideration should be given to the increased risk of aseptic meningitis in patients with systemic lupus erythematosus and mixed connective tissue diseases.
Long-term use of high doses of Dikloberl can cause myocardial infarction or stroke.
Alcohol consumption is contraindicated during the period of NSAID treatment.
Influence on the ability to drive vehicles and complex mechanisms
According to the instructions, Dikloberl can have a negative effect on the body and cause side effects in the form of dizziness and drowsiness, visual impairment. In this regard, during the period of treatment, it is recommended to be careful and avoid working with complex mechanisms and driving.
Application during pregnancy and lactation
The use of Dikloberl is contraindicated in the third trimester of pregnancy and during breastfeeding.
It is not recommended to prescribe diclofenac in the I and II trimesters of pregnancy, unless the expected effect of the drug for the mother outweighs the potential threat to the fetus.
The use of the drug can have a negative effect on female fertility, therefore, if there are problems with conception or during pregnancy planning, women are not recommended to prescribe Dicloberl.
Pediatric use
The use of tablets, capsules, solution and suppositories in a dose of 100 mg for the treatment of children under the age of 18 is contraindicated.
Prescription of suppositories at a dose of 50 mg is indicated for children over 14 years of age. The dose of Dikloberl is determined individually at the rate of no more than 3 mg per 1 kg of the child's weight. The maximum daily dose is 150 mg.
With impaired renal function
The use of tablets, capsules and suppositories for the treatment of patients with renal insufficiency is contraindicated.
Dicloberl solution should be prescribed with caution in case of impaired renal function.
For violations of liver function
The use of tablets, capsules and suppositories is contraindicated for liver failure.
With caution, Dikloberl solution 75 mg should be prescribed for severe liver dysfunction.
Use in the elderly
Elderly patients should use Dikloberl with caution. The lowest effective dose is recommended for treatment. Beforehand, it is necessary to conduct an examination for the state of the gastrointestinal tract in order to exclude the presence of gastrointestinal bleeding.
Drug interactions
Interactions observed with the simultaneous use of Dicloberl:
- potent inhibitors of CYP2C9, including voriconazole: have a depressing effect on the metabolism of diclofenac, increasing the risk of a significant increase in the level of its concentrations in blood plasma;
- lithium preparations, digoxin: it is necessary to control the content of lithium and digoxin in the blood plasma due to the existing risk of an increase in the level of their concentration;
- beta-blockers, angiotensin-converting enzyme (ACE) inhibitors and other diuretics or antihypertensive drugs: the risk of a decrease in the antihypertensive effect of these drugs increases (if this combination is necessary, treatment should be accompanied by appropriate hydration and careful monitoring of patients for blood pressure, especially patients in the elderly);
- potassium-sparing diuretics, tacrolimus, trimethoprim, cyclosporine: an increase in serum potassium levels is possible;
- anticoagulants, antithrombotic agents: can contribute to the development of bleeding;
- selective inhibitors of COX-2 (cyclooxygenase-2), corticosteroids and other NSAIDs, selective serotonin reuptake inhibitors (SSRIs): significantly increase the risk of gastrointestinal bleeding and ulcers;
- oral hypoglycemic agents: it is necessary to carefully monitor the level of glucose in the blood, since hypoglycemia or hyperglycemia may develop;
- methotrexate: there is an increase in the toxicity of methotrexate, due to the suppression of its clearance in the renal tubules by the action of diclofenac (it is recommended to avoid the combination of the drug with methotrexate, given that with an interval between their intake of 24 hours, the likelihood of methotrexate toxicity remains);
- cyclosporine, tacrolimus: their nephrotoxicity may increase, it is recommended to reduce the dose of diclofenac;
- antibacterial quinolones: the risk of seizures increases;
- phenytoin: an increase in the level of concentration of phenytoin in blood plasma is possible;
- probenecid: helps to delay the elimination of sodium diclofenac from the body;
- colestipol, cholestyramine: disrupt the absorption of diclofenac (to avoid this, these funds should be taken one hour after diclofenac or 4 hours before taking it);
- cardiac glycosides: contribute to an increase in heart failure, a decrease in the glomerular filtration rate, an increase in the level of glycosides in the blood plasma;
- mifepristone: the effect of the drug can reduce the therapeutic effect of mifepristone, therefore, the combination and administration of diclofenac up to 192 hours after discontinuation of mifepristone is contraindicated.
Analogs
Diclofenac's analogs are: Diclofenac, Diklak, Almiral, Bioran, Argett Rapid, Voltaren, Diclobru, Olfen, Ortofen, Naklofen, Rapten, Indomethacin, Ketorolac, Feloran.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperature: tablets - up to 30 ° C, capsules, solution, suppositories - up to 25 ° C. The solution should be stored in a dark place, not allowed to freeze.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Dikloberl
Reviews about Dikloberl regarding the effectiveness of the drug are mostly positive. Patients report a rapid pain relieving effect of the drug.
The disadvantages include the frequent development of adverse events, especially against the background of the use of oral forms.
The price of Dicloberl in pharmacies
The price of Dicloberl for a package containing 10 suppositories at a dose of 50 mg can be from 260 rubles, at a dose of 100 mg - from 400 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
