Pharmacological properties of the drug Dicloberl No. 75
Pharmacodynamics. Diclofenac sodium (sodium salt of [2-(2,6-dichloranilino)phenyl]acetic acid), belongs to the NSAID group of phenylacetic acid derivatives. Has a pronounced anti-inflammatory, analgesic and antipyretic effect, reduces tissue swelling during inflammation; the effects are associated with the ability to block prostaglandin synthesis. Inhibits platelet aggregation caused by ADP and collagen. Pharmacokinetics. After intramuscular administration, the maximum plasma concentration is reached within 10–20 minutes. Approximately 30% of the active substance is metabolized and excreted in the feces. About 70% after hydroxylation and conjugation in the liver in the form of pharmacologically inactive metabolites is excreted in the urine. T1/2 does not depend on liver and kidney function and is about 2 hours. Almost 99% is bound to blood plasma proteins. When used in humans, Dicloberl N 75 reduces the severity of pain, swelling and reduces elevated body temperature, which were caused by inflammatory processes. Dicloberl N 75 also inhibits platelet aggregation caused by ADP and collagens.
Indications
The instructions for using Dikloberl 75 injections indicate that the drug affects diseases of the musculoskeletal system and is also used for symptomatic treatment. The product helps combat the following problems:
- arthritis and gout;
- joint inflammation;
- diseases of the spine;
- inflammation of soft tissues;
- swelling due to inflammatory processes after injury.
Usually injections are given once urgently if the pills do not help.
Use of the drug Dicloberl No. 75
Usually administered deep intramuscularly (into the gluteal muscle) in a single dose of 75 mg. If long-term therapy with Dicloberl N 75 is necessary, it is continued using forms for oral or rectal use. On the day of injection of Diclofenac N 75, the total daily dose of diclofenac should not exceed 150 mg. Due to the possible development of anaphylactic reactions, up to the development of shock, the patient should be monitored for at least 1 hour after the injection, and the medical kit necessary for emergency care should be ready.
Treatment during pregnancy
If a woman becomes pregnant during treatment, this must be reported to the attending physician. This drug is allowed to be used in the early stages, but in the last trimester it is worth abandoning the drug.
As for breastfeeding women, there is no risk when taking the medicine in small doses. Although the medicine passes into the milk, it does not harm the baby. But if the treatment lasts a long time, then you need to either reduce the dosage or temporarily stop feeding the baby breast milk.
Contraindications to the use of the drug Dicloberl No. 75
Hypersensitivity to diclofenac or other NSAIDs and to the components of the drug. Hematopoietic disorders. A history of bronchospasm, asthma, rhinitis, urticaria, which develops after the use of acetylsalicylic acid or other NSAIDs. Current or past history of recurrent peptic ulcers or gastrointestinal bleeding (at least 2 unrelated episodes). A history of gastrointestinal bleeding or perforation of a hollow organ associated with the use of NSAIDs. Cerebrovascular and other acute bleeding. Severe dysfunction of the liver and kidneys. Severe heart failure. III trimester of pregnancy and breastfeeding period. Children and adolescents under 18 years of age.
Price
The drug Dicloberl Retard has different prices depending on the volume of packaging, the form of the drug, the manufacturer and the pricing policy of the pharmacy.
Conditions for dispensing from pharmacies
The drug is sold strictly according to prescription.
Average price in Russia
The average cost of a pack of 20 capsules in Russia ranges from 400 to 600 rubles .
Average cost in Ukraine
The price of a package of 20 capsules of Dicloberla Retard in Ukraine will be from 28 to 35 UAH .
Side effects of the drug Dicloberl No. 75
When analyzing side effects, the following frequency of occurrence values are taken as a basis: very often (≥10%), often (≤10% and ≥1%), sometimes (≤1% and ≥0.1%), rarely (≤0.1 % and ≥0.01%), very rare (≤0.01% or frequency unknown because available data do not allow estimation). From the heart: very rarely - a feeling of increased heartbeat, edema, heart failure, myocardial infarction. From the blood and lymphatic system: very rarely - anemia, leukopenia, thrombocytopenia, pancytopenia, agranulocytosis, hemolytic anemia. The onset of manifestations may be fever, sore throat, erosion of the oral mucosa, flu-like conditions, severe general weakness, nasal and skin (purpura, ecchymosis) bleeding. From the side of the central nervous system: often - headache, dizziness, disturbances of consciousness, agitation, irritability, increased fatigue; very rarely - sensory disturbances, taste disturbances, memory disturbances, disorientation, convulsions. From the side of the organ of vision: very rarely - visual impairment (blurred vision and diplopia). From the organ of hearing: tinnitus, transient hearing loss. From the gastrointestinal tract: very often - nausea, vomiting, diarrhea, mild bleeding, which in exceptional cases leads to anemia; often - dyspeptic disorders, flatulence, spasm of smooth muscles of the gastrointestinal tract, anorexia, formation of ulcers in the gastrointestinal tract (under certain circumstances with bleeding and perforation); sometimes - hemorrhagic vomiting, melena or hemorrhagic diarrhea; very rarely - stomatitis, glossitis, damage to the esophagus, worsening of the clinical course of nonspecific ulcerative colitis and Crohn's disease, constipation, pancreatitis. From the kidneys and urinary tract: sometimes - the development of edema, especially with hypertension (arterial hypertension) or renal failure; very rarely - interstitial nephritis or necrosis of the renal papillae, which can lead to acute renal failure, proteinuria and/or hematuria; nephrotic syndrome. From the skin and subcutaneous fat: sometimes - alopecia; very rarely - exanthema, eczema, photosensitivity, purpura (including allergic ones), Stevens-Johnson and Lyell syndrome. Disorders of infectious and parasitic origin: very rarely, in temporal interdependence with systemic use of NSAIDs, there have been reports of worsening of the clinical course of inflammatory processes of infectious origin, for example the development of necrotizing fasciitis. This is reliably related to the mechanism of action of NSAIDs. If during the use of Dicloberl N 75 the clinical course of the infection worsens, then it is necessary to immediately resolve the issue regarding the use of antibacterial agents or antibiotics. Very rarely, when using diclofenac sodium, symptoms of aseptic meningitis were observed: stiff neck, headache, nausea, vomiting, fever, disturbances of consciousness (a reliable tendency in autoimmune diseases: systemic lupus erythematosus, mixed collagenosis). Vascular disorders: very rarely - hypertension (arterial hypertension). General and local reactions: with intramuscular use, a burning sensation, aseptic abscess, necrosis of subcutaneous fatty tissue and skin may often develop at the injection site. From the immune system: often - hypersensitivity reactions in the form of skin rash and itching; sometimes - urticaria; very rarely - severe general hypersensitivity reactions in the form of swelling of the face, tongue, larynx with narrowing of the airways, shortness of breath, tachycardia, decreased blood pressure up to the development of shock; very rarely vasculitis and pneumonitis of an allergic nature develop. From the liver and biliary tract: often - increased levels of hepatic transaminases in the blood plasma; sometimes - liver damage (especially with long-term use of the drug) - acute hepatitis with or without jaundice (very rarely with a fulminant course and without a prodromal period). From the psyche: very rarely - psychotic reactions, depression, feelings of fear, nightmares. Other reactions: Hypersensitivity reactions to benzyl alcohol are rare.
Overdose
Signs of overdose
An overdose of diclofenac does not have a clinical picture unique to this drug. Signs of overdose are observed in the form of nausea, vomiting and diarrhea, headache and discomfort in the epigastric area, gastrointestinal bleeding, dizziness, coma, convulsions, etc. Severe intoxication may be accompanied by liver damage.
Treatment of overdose
Treatment of diclofenac poisoning involves both symptomatic and mandatory supportive therapy. To relieve intoxication, it is necessary to take activated charcoal or (in more severe cases) to provide gastric lavage.
Next, specific measures should be prescribed for specific pathologies (dialysis, forced diuresis or hemoperfusion).
Special instructions for the use of the drug Dicloberl No. 75
The drug Diclofenac N 75 is used only when a rapid onset of effect is necessary, and also when the use of other dosage forms of diclofenac sodium is impossible, and it is recommended to limit it to a single injection to begin therapy. It is necessary to avoid the use of Dicloberl N 75 in combination with other NSAIDs, including selective COX-2 inhibitors. With a history of peptic ulcer disease and in elderly patients, the risk of complications from the gastrointestinal tract increases with increasing doses of NSAIDs, so in such cases it is recommended to start treatment with a minimum dose. For this category of patients, as well as if it is necessary to simultaneously use acetylsalicylic acid in low doses or other drugs that increase the risk of developing gastrointestinal complications, it is necessary to consider combining them with drugs that have a protective effect on the gastrointestinal tract (misoprostol or proton pump inhibitors) . Patients with a history of gastrointestinal diseases, especially older people, should be informed about the appearance of minor changes in the gastrointestinal tract, especially gastrointestinal bleeding, especially at the beginning of treatment. The use of Dicloberl N 75 is stopped immediately if bleeding or an ulcer develops in the gastrointestinal tract. Patients with a history of hypertension (arterial hypertension) who have experienced edema, or patients with a history of decompensated heart failure require careful monitoring. It should be taken into account that there is a significant relationship between the use of diclofenac sodium in high doses (150 mg/day) or its long-term use and a slight increase in the risk of arterial thromboembolism with the possible development of myocardial infarction and/or stroke. Dicloberl N 75 should be prescribed only after a thorough analysis of the benefit/risk ratio for congenital disorders of porphyrin metabolism (for example, acute intermittent porphyria), systemic lupus erythematosus, mixed collagen diseases, hypertension (arterial hypertension), heart failure, coronary artery disease, obliterating endarteritis, cerebrovascular pathology, hyperlipidemia , diabetes mellitus and if the patient smokes. Special monitoring is necessary when using the drug in persons with gastrointestinal complaints or chronic inflammatory bowel diseases (nonspecific ulcerative colitis and Crohn's disease); in patients with hypertension (arterial hypertension) or heart failure; with impaired renal function; in case of liver dysfunction; immediately after major surgical interventions; in patients with hay fever, nasal polyposis or chronic obstructive respiratory diseases; with a history of allergic reactions, since this increases the risk of developing allergic reactions (aspirin asthma, Quincke's edema or urticaria). Diclofenac sodium may inhibit platelet aggregation, so patients with coagulation disorders should be closely monitored. With long-term use of the drug, periodic monitoring of liver and kidney functions and hemogram is required. With prolonged use of analgesics, a headache may occur, for the relief of which the drug cannot be used in increased doses. Habitual use of analgesics, especially when combining several painkillers, can lead to permanent kidney damage, which is accompanied by the risk of developing kidney failure (analgesic nephropathy). Concomitant use of alcohol may increase the side effects of diclofenac sodium, especially from the gastrointestinal tract and central nervous system. Due to the possible development of allergic reactions, including anaphylactic shock, the patient should be under medical supervision for at least 1 hour after the injection. In elderly people there is no need for dose adjustment, but constant monitoring of the patient's health is required due to the possible development of side effects. In cases of mild to moderate renal and liver dysfunction, there is no need to adjust the dose. With long-term use of Dicloberl N 75, it is necessary to regularly monitor liver and kidney function indicators, as well as blood composition and glucose levels. Use during pregnancy and lactation. Diclofenac sodium is not recommended for use in women planning pregnancy or in women undergoing examination for infertility. In the first and second trimesters of pregnancy, diclofenac is prescribed only in cases of extreme necessity, while the dose of the drug and duration of use are reduced to a minimum. During breastfeeding, diclofenac sodium may not be discontinued if the treatment is short-term. But with long-term use of the drug or when using it in high doses, it is necessary to stop breastfeeding in advance. In the third trimester of pregnancy, diclofenac sodium is contraindicated. Use in children and adolescents under 18 years of age is contraindicated. The ability to influence reaction speed when driving vehicles or working with machinery. Since the use of diclofenac sodium may develop side effects from the central nervous system (increased fatigue, dizziness), in isolated cases the reaction may change and the ability to actively participate in driving vehicles or working with machinery may decrease. This is especially noted when used simultaneously with alcohol. Propylene glycol, which is part of the drug, can cause symptoms similar to alcohol intoxication.
Features of pharmacokinetics: different groups of patients
The individual age of the patient does not serve as a factor influencing the metabolism, absorption and elimination of diclofenac.
In patients with renal dysfunction, at adequate doses, accumulation of diclofenac is not observed. When creatinine clearance is less than 10 ml/min. a significant increase in plasma (almost 4 times) in the volume of hydroxylated metabolites was detected.
In patients with liver cirrhosis (compensated) or a history of chronic hepatitis, the pharmacokinetics of diclofenac are identical to patients without such diseases.
Interactions of the drug Dicloberl No. 75
The simultaneous use of Dicloberl N 75 with drugs such as digoxin, phenytoin or lithium compounds may increase their levels in the blood plasma. Dicloberl N 75 may weaken the effect of diuretics and antihypertensive drugs. The simultaneous use of Dicloberl N 75 and potassium-sparing diuretics can cause hyperkalemia. Dicloberl N 75 may weaken the effect of ACE inhibitors. The combined use of Dicloberl N 75 with ACE inhibitors increases the risk of renal dysfunction. When using Dicloberl N 75 with other NSAIDs or with corticosteroids, the risk of developing side effects from the digestive tract increases. Taking Dicloberl N 75 within 24 hours before or after taking methotrexate can lead to an increase in its concentration in the blood plasma and the manifestation of toxic effects. With the simultaneous use of diclofenac sodium and platelet aggregation inhibitors (acetylsalicylic acid) or selective serotonin reuptake inhibitors, the risk of gastrointestinal bleeding increases; when prescribing such combinations, it is recommended to constantly monitor blood coagulation parameters. Diclofenac sodium may enhance the effect of anticoagulants such as warfarin. Dicloberl N 75 may increase the nephrotoxic effect of cyclosporine. Medicines that contain probenecid may slow down the elimination of Dicloberl N 75. Isolated cases of changes in the concentration of glucose in the blood serum after the use of diclofenac sodium, which required dose adjustment of antidiabetic drugs (sulfonylureas), have been described. Probenecid and sulfinpyrazone may slow down the elimination of diclofenac sodium from the body. When taken in combination, diclofenac reduces the severity of the effects of furosemide and antihypertensive drugs and increases the concentration of digoxin in the blood plasma. Concomitant use with potassium-sparing diuretics can lead to the development of hyperkalemia. When combined with other NSAIDs or corticosteroids, the risk of gastrointestinal bleeding increases. Combination with methotrexate and cyclosporine is undesirable. If renal function is impaired (for example, with dehydration or in elderly people with reduced renal function), the simultaneous use of ACE inhibitors or angiotensin II receptor antagonists with drugs that suppress COX may lead to further progression of renal dysfunction, including the development of reversible acute renal failure. These patients need to ensure adequate fluid intake, as well as regular monitoring of renal function.
Release form and composition
The drug is available in the following dosage forms:
- Dicloberl 50 – film-coated tablets of 50 mg. One blister contains 50 or 100 tablets;
- Dicloberl 75 – solution for parenteral administration in ampoules of 3 ml, 5 ampoules in a cardboard box;
- Dicloberl retard - capsules with a longer period of therapeutic action, 100 mg in blisters of 10, 20 or 50 pieces;
- Dicloberl 50 and 100 – suppositories for rectal administration, 5 or 10 pieces in blisters.
The active ingredient of the drug is diclofenac sodium. Auxiliary components of the injection solution are sodium hydroxide, acetylcysteine, benzyl alcohol, mannitol, propylene glycol and purified water.
The composition of Dikloberl 50 tablets additionally includes lactose monohydrate, methacrylic acid, sodium salt of carboxymethyl starch, talc, povidone K30, magnesium stearate, corn starch, iron acid pigment yellow, titanium dioxide, macrogol 400, macrogol 6000, simethicone emulsion and hypromellose.
Auxiliary ingredients of Dikloberl retard capsules are substances such as shellac, corn starch, titanium dioxide, Eudragit RL12.5, talc, sucrose and white gelatin.
The inactive components of Dicloberl 50 rectal suppositories include propyl gallate, solid fat, 96% ethyl alcohol and corn starch.
Analogs
Analogues of this drug include:
- Diclofenac sodium solution;
- Diclopol 100 mg;
- Catafast;
- Voltaren Retard;
- Hyalgel;
- Ortofen;
- Ketorol;
- Aertal;
- Indomethacin;
- Ketorolac;
- Ecodax;
- Propranolol;
- Almiral;
- Diklak;
- Diklo-F.
You can use analogues after consulting a doctor to select a more suitable drug.
