Pharmacodynamics and pharmacokinetics
Pharmacodynamics
The drug has a non-steroidal structure, has a strong analgesic and anti-inflammatory effect, and is also a prostaglandin synthetase .
Pharmacokinetics
The highest concentration in plasma after intramuscular administration is achieved after 10-20 minutes.
Blood protein binding is approximately 99.8%. Easily penetrates into the joint fluid, where its maximum concentration is recorded 3 hours later than in the blood. The half-life of the joint fluid is approximately 4-5 hours. Approximately 2 hours after the onset of maximum concentration in the blood, the content of the active substance in the synovial fluid remains higher than in the blood. This phenomenon is observed within 12 hours.
Metabolized by glucuronidation, hydroxylation and methoxylation to form a number of phenolic derivatives, the vast majority of which form complexes with glucuronic acid . The half-life from the blood is approximately one and a half hours. About 60% of the dose taken is excreted in the urine, the remaining part is evacuated through the intestines, while no more than 1% of diclofenac .
What is Dicloberl?
Dicloberl is a nonsteroidal anti-inflammatory drug (NSAID) that is used to relieve pain and reduce inflammation. Dikloberl contains the active ingredient - diclofenac. It exerts its therapeutic effect by reducing the amount of hormone-like substances in the body called prostaglandins, which cause pain and inflammation.
Dicloberl is used to relieve mild or moderate pain, to relieve fever, and also to treat rheumatic diseases (common forms of rheumatism).
Indications for use
- rheumatoid arthritis (including juvenile form), osteoarthritis , ankylosing spondylitis, spondyloarthritis;
- vertebrogenic pain syndromes;
- rheumatic diseases affecting extra-articular soft tissues;
- pain syndromes of post-traumatic and postoperative origin, accompanied by signs of inflammation, after orthopedic and dental interventions;
- acute pain syndrome of moderate severity of various origins.
The underlying disease must be treated with basic therapy. An increase in temperature in itself is not diclofenac
Contraindications
- acute ulcer , bleeding or perforation of the intestine or stomach;
- allergy to the components of the drug;
- increased risk of postoperative bleeding, hemostasis disorders, cerebrovascular bleeding or hematopoietic disorders;
- bleeding or perforation of the digestive system in the past associated with taking non-steroidal anti-inflammatory drugs;
- inflammatory bowel diseases;
- exacerbation of peptic ulcer disease, peptic ulcer bleeding, including in the past;
- third trimester of pregnancy;
- congestive heart failure;
- cerebrovascular disorders in persons who have suffered a stroke or cases of ischemic attacks;
- liver or kidney failure ;
- peripheral arterial disease;
- coronary heart disease in persons who have had a heart attack or suffer from angina pectoris ;
- treatment of pain before and after coronary artery bypass surgery;
- allergic reactions to Ibuprofen , Aspirin or other non-steroidal anti-inflammatory drugs .
Side effects
- Hematopoietic reactions: pancytopenia, thrombocytopenia, leukopenia, agranulocytosis, anemia . The first symptoms of these disorders may be pharyngitis , fever, superficial ulcerations in the mouth, nosebleeds, apathy , and skin bleeding.
- Immune reactions: skin rash, urticaria , allergic vasculitis, angioedema , itching, pneumonia .
- Mental disorders: depression , disorientation, irritability, insomnia , psychotic disorders, nightmares, other mental disorders.
- Reactions from nervous activity: dizziness, headache, agitation, dizziness, drowsiness, paresthesia, sensory disturbances, fatigue, convulsions, memory impairment, tremor , anxiety, hallucinations, taste disorders, aseptic meningitis , confusion, stroke , general malaise.
- Reactions from sensory organs: diplopia , blurred vision, optic neuritis, tinnitus, vertigo , hearing disorders.
- Circulatory reactions: arterial hypotension , heart failure, chest pain, palpitations, vasculitis, arterial hypertension, myocardial infarction.
- Respiratory reactions: pneumonitis , asthma .
- Digestive reactions: abdominal pain, vomiting, flatulence , anorexia , gastritis , dyspepsia , diarrhea , bleeding from the digestive organs, gastric ulcer (with possible perforation or bleeding), constipation , disruption of the esophagus, colitis , glossitis, stomatitis, intestinal stenosis hepatitis , increased transaminases , liver disorders, jaundice, hepatonecrosis , fulminant hepatitis , liver failure.
- Skin reactions: manifestations of eczema and erythema , hair loss, Lyell's syndrome, Stevens-Johnson syndrome, exfoliative dermatitis, purpura , photosensitivity, itching.
- Reactions from the genitourinary system: acute renal failure , edema, proteinuria, hematuria, nephrotic syndrome, interstitial nephritis, impotence, papillary necrosis of kidney tissue.
Overdose
Signs of overdose: nausea, headache, epigastric pain, vomiting, bleeding from the digestive organs, drowsiness, convulsions, dizziness, diarrhea, disorientation , coma , tinnitus, liver damage, acute renal failure .
Treatment of overdose: symptomatic, cleansing enema (if no more than an hour has passed since the overdose). For frequent or prolonged convulsions, Diazepam .
Instructions for injections Dicloberl N 75 (Method and dosage)
To reduce the risk of adverse reactions, the lowest possible effective dose should be used for the shortest possible period of time.
Dicloberl injections, instructions for use
Treatment with the drug is recommended to be carried out using a single injection. The solution is injected deep into the buttock muscle. If long-term therapy is needed, it is continued with oral or rectal forms of diclofenac . On the day the drug was injected, the total daily dose should not exceed 150 mg.
Elderly patients
Dicloberl injections should be used with caution in this group of people, since the majority of them are more prone to adverse reactions. Frail elderly patients or patients with low weight should be prescribed the lowest effective doses of the drug.
Note!
Description of the drug Dicloberl 50 supp. 50 mg No. 10 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
Interaction
With simultaneous use, Dicloberl can increase the lithium in the blood. In such cases, monitoring of lithium in the blood is recommended.
When used together with Digoxin, an increase in the concentration of the latter in the blood is possible. In such cases, monitoring the concentration of Digoxin in the blood is recommended.
Concomitant use of diclofenac with antihypertensive drugs and diuretics may lead to a weakening of their antihypertensive effect due to suppression of the synthesis of angiodilating prostaglandins . Patients should receive adequate amounts of fluids, and regular monitoring of kidney function is also recommended after starting such treatment.
Concomitant use with Cyclosporine , potassium-sparing diuretics , Trimethoprim or Tacrolimus may increase potassium in the blood, so the condition of such patients should be monitored more often.
Concomitant use with anticoagulants may increase the risk of bleeding, since diclofenac in large doses can reversibly inhibit platelet adhesion, so such patients should be carefully monitored regularly.
Concomitant use of diclofenac and other non-steroidal anti-inflammatory drugs or glucocorticosteroids may increase the likelihood of ulcers or gastrointestinal bleeding. Therefore, simultaneous use of two or more anti-inflammatory nonsteroidal drugs should be avoided.
Concomitant use of non-steroidal anti-inflammatory drugs and serotonin reuptake blockers increases the risk of bleeding from the digestive organs.
Diclofenac can be prescribed together with oral forms of hypoglycemic agents and this does not affect their therapeutic effect. But there are some reports of the occurrence of hyperglycemia and hypoglycemia , which necessitated adjustment of the dosage of antidiabetic agents while taking diclofenac . Therefore, it is recommended to monitor glucose during combination treatment.
Diclofenac can reduce the rate of elimination of Methotrexate , which leads to an increase in the level of the latter in the blood. Diclofenac should be used no earlier than 24 hours before taking Methotrexate to avoid cases of increased concentration of the latter and increased toxic effects.
Concomitant use with cyclosporines can increase their nephrotoxicity, which is why diclofenac should be prescribed in reduced doses.
When using anti-inflammatory non-steroidal drugs with Tacrolimus , the risk of nephrotoxicity may increase.
It is possible that seizures may develop in people who simultaneously use quinolone derivatives and Dicloberl. This phenomenon can be observed in patients with or without a history of seizures. Caution should be exercised when deciding whether to prescribe quinolones to patients already receiving anti -inflammatory non-steroidal drugs.
When taking Phenytoin together with diclofenac , it is necessary to monitor the content of the former in the blood due to a possible increase in its content.
Medicines containing probenecid slow down the elimination of diclofenac from the body.
The simultaneous administration of cardiac glycosides and anti-inflammatory non-steroidal drugs can aggravate heart failure, inhibit the glomerular filtration process and increase the content of glycosides in the blood.
Diclofenac should not be used within 9-12 days after the last dose of Mifepristone , since diclofenac can weaken the effect of the latter.
Caution is recommended when using diclofenac with strong CYP2C9 inhibitors , as this may lead to an increase in the concentration of diclofenac in the blood due to inhibition of its metabolism.
What you need to know before you start taking Dicloberl
If you have an allergic reaction to Dicloberl or if bronchospasm occurs, you should stop using it further, and also consult your doctor to select another medication that is more suitable for you.
Dicloberl may not be safe for use if you have a history of the following conditions:
- heart disease, high blood pressure;
- stomach and duodenal ulcers;
- bronchial asthma;
- inflammatory diseases of the kidneys and/or liver;
- if you have bad habits (smoking).
Note! Taking Dicloberl during the last 3 months of pregnancy may harm the unborn baby.
Dicloberl has a more prolonged (long-lasting) effect, which means that it has a long-lasting effect and is slowly eliminated from the body. Therefore, it is believed that it passes into breast milk in significant concentrations and is incompatible with breastfeeding.
Dicloberl can cause stomach or intestinal bleeding, which can lead to serious negative consequences, including death. If you have a history of peptic ulcer disease, then you should take this drug under the protection of a medicinal group of antiulcer drugs, such as misoprostol, omez, which have a protective effect on the gastric mucosa.
Dicloberl is approved for use by people over 18 years of age.
special instructions
In order to reduce the risk of adverse reactions, treatment should begin with the minimum effective dose, which should be taken in the shortest course necessary to relieve symptoms.
systemic anti-inflammatory non-steroidal drugs should be avoided due to a possible increase in side effects.
Due to its pharmacological properties, the drug Dicloberl is able to mask the signs of infection.
With the use of all non-steroidal anti-inflammatory drugs, cases of bleeding from the digestive organs, perforation and ulceration, which can be fatal, have been identified. If such disorders are diagnosed in patients receiving diclofenac , its use should be discontinued immediately.
Elderly patients have an increased risk of adverse reactions to non-steroidal anti-inflammatory drugs , especially bleeding and perforation. For this group of patients, as well as for those in need of simultaneous use of acetylsalicylic acid , the issue of prescribing combination therapy using gastroprotective agents ( proton pump inhibitors or Misoprostol ) should be decided.
Close medical supervision is necessary when prescribing Dicloberl to patients with liver disease, due to the possible deterioration of their condition.
During long-term treatment with the described drug, constant monitoring of liver function and liver enzyme levels is prescribed. If liver dysfunction persists or worsens, or clinical signs appear that are thought to be related to disease progression, use of Dicloberl should be discontinued immediately.
Since an increase in the frequency and severity of edema has been reported during therapy with anti-inflammatory non-steroidal drugs , special attention should be paid to persons with arterial hypertension , cardiac or renal dysfunction, the elderly, those receiving diuretics or nephrotoxic agents , and before or after major surgery.
In patients with systemic lupus erythematosus or other connective tissue diseases, an increased risk of aseptic meningitis .
The use of diclofenac may be associated with an increased likelihood of thrombotic events ( heart attack or stroke ).
Patients with peripheral artery disease, coronary heart disease , congestive heart failure, severe arterial hypertension , cerebrovascular disease are not recommended to prescribe the drug; in extreme cases, it can be used in a dosage of up to 100 mg per day.
When taking this drug for a long time, regular monitoring of blood tests is necessary.
Patients with bleeding diathesis, impaired hemostasis or hematological disorders taking Dicloberl should be closely monitored.
Patients with chronic obstructive pulmonary disease, asthma, allergic rhinitis, nasal polyps or chronic respiratory tract infections are more likely to experience side effects ( asthma , Quincke's edema , urticaria ) due to taking non-steroidal anti-inflammatory drugs . This also applies to persons with allergic reactions to other substances, such as itching, rash, hives .
With prolonged use of painkillers, a headache may occur, which should not be treated by increasing the dosage of the medication.
vertigo during treatment with the drug should not drive.
Analogs
Level 4 ATC code matches:
Voltaren
Rapten
Zerodol
Dickloberl Retard
Dicloberl
Ketanov
Dolak
Panoxen
Ketorolac
Naklofen Duo
Naklofen
Olfen-100
Olfen-75
Neurodiclovit
Nizilat
Fanigan
Aertal
Methindol retard
Ortofen
The most common analogues of Dikloberl are listed below: Almiral, Arguette Rapid, Bioran, Voltaren, Diclofenac, Diclak, Diclobry, Ketarolak, Naklofen, Olfen, Ortofen, Ibuprofen, Rapten, Feloran.
During pregnancy and lactation
In the first two trimesters of pregnancy, Dicloberl is allowed to be prescribed only under strict indications and under medical supervision, and the duration of therapy should be as short as possible. In the last trimester of pregnancy, the use of the drug is prohibited due to the risk of inhibition of uterine contractility and early closure of the ductus arteriosus.
Diclofenac can pass into milk during breastfeeding, so the drug should not be used during lactation to avoid negative effects on the baby.
Dicloberl can also negatively affect fertility in women, so it is not recommended for use by women planning pregnancy.
What you need to know about the drug Dicloberl
Dicloberl is a non-selective inhibitor of cyclooxygenase (an enzyme that inhibits the production of prostaglandins), due to this its negative effect on the gastrointestinal tract is most pronounced, which in turn can lead to gastric bleeding and subsequent negative consequences.
Dicloberl is also slowly eliminated from the body, as a result of which it is necessary to strictly adhere to the dosage schedule and certain intervals between doses in order to avoid negative consequences for the cardiovascular system and gastrointestinal tract, as well as the body as a whole.
