The instruction for medical use
of DikloberlÒ medicine, retard
A trade name
of DikloberlÒ, retard
the International unlicensed
name Diclofenac Dosage Form of the Capsule of the prolonged action, 100 mg
One capsule contains
active agent diclofenac of sodium of 100 mg
excipients: sucrose, starch corn, talc, shellac, Eudragit of RL PO (methacrylate ammonium copolymer, type A), gelatin, the titan dioxide (E 171)
Solid gelatin capsules of 2 in size, from white till cream color (coloring not more intensively, than RAL 9001).
Contents of capsules: spherical granules from white color to color of ivory (coloring not more intensively, than RAL 1014).
Non-steroidal anti-inflammatory drugs. Anti-inflammatory and antirheumatic drugs. Acetic acid derivatives. Diclofenac.
The ATX M01AB05 code
Pharmacokinetics Later properties of oral administration of the usual dosage forms resistant to influence of gastric juice, diclofenac is completely soaked up in intestines. Depending on duration of a gastric passage, the maximum concentration of drug in plasma are reached in 1-16 hours, on average 2-3 hours later after reception. After intramuscular introduction the maximum concentration in plasma are reached in 10-20 minutes, and after rectal administration approximately in 30 minutes. At oral administration, diclofenac is exposed to noticeable changes in result of effect of the first passing through a liver (first-pass-effect) then 35 70% of the soaked-up active ingredient come to blood in not changed look. About 30% of active ingredient are removed with a stake in the form of metabolites.
About 70% of active ingredient after biotransformation in a liver (hydroxylation and conjugation) are removed through kidneys in the form of pharmacological inactive metabolites. Honor elimination half-life irrespective of function of a liver and kidneys makes about 2 hours. Linking with proteins of plasma makes about 99%.
Diclofenac represents non-steroidal anti-inflammatory drug. The mechanism of effect of diclofenac is based on suppression of synthesis of prostaglandins. At use, diclofenac reduces the pains caused by inflammatory processes, hypostases and fever. Besides, as well as other anti-inflammatory nonsteroid drugs diclofenac (in a dose of 1.1 mg/kg of body weight) suppresses the aggregation of thrombocytes induced by ADF and collagen.
Symptomatic treatment of pain and inflammation at:
– acute arthritises (including gout attacks)
– chronic arthritises, in particular, in a pseudorheumatism (chronic polyarthritis)
– an ankylosing spondylitis (Bekhterev’s disease) and other inflammatory diseases of a backbone of the rheumatic nature
– painful sensitivity of fabrics in arthroses and spondylarthroses
– inflammatory diseases of the rheumatic nature with defeat of soft tissues
– hypostases with a pain syndrome or posttraumatic inflammations
Due to the slowed-down release of active ingredient from the Dikloberl capsules retard this drug is not suitable for initial therapy of diseases in which fast approach of action is required.
The route of administration and doses
the Dosage of diclofenac is established depending on disease severity.
The recommended dose at adults makes 1 Dikloberl capsule retard the prolonged action in day (that is equivalent to 100 mg of diclofenac of sodium).
Dikloberl retard it is necessary to accept inside entirely, without chewing and to wash down with a large amount of liquid. The patient with chronic diseases of a stomach Dikloberl retard at meal time is recommended to accept.
Therapy of rheumatic diseases can demand prolonged use of the drug Dikloberl retard. The issue of duration of use of drug is resolved by the attending physician.
Side effects of Dikloberl retard can be reduced by purpose of a minimal effective dose of drug during shorter period necessary for stopping of symptoms of a disease.
When prescribing drug no correction of a dose is required to elderly patients. Due to the profile of possible side effects at elderly patients it is necessary to exercise especially careful control of the state of health.
Patients with renal failures:
When prescribing drug with disturbances of renal function easy to moderate severity of a dose decline it is not required to patients.
Patients with abnormal liver functions
When prescribing drug with abnormal liver functions easy to moderate severity of a dose decline it is not required to patients.
Children and teenagers
It is contraindicated for use of drug for children and teenagers.
concerning the following side reactions on reception Dikloberl of a retard should be taken into account that development and intensity of these reactions generally depend on a dose and have individual character.
Very often (1/10)
– nausea, vomiting and a diarrhea and also insignificant gastrointestinal bleedings which in some cases can lead ment of anemia
Often (from 1/100 to & lt, 1/10)
– a headache, dizziness, excitement, irritability or increased fatigue
– dyspepsia, a meteorism, spasms in a stomach, lack of appetite and also formation of gastrointestinal ulcers (sometimes followed by bleeding and perforation)
– reactions of hypersensitivity, such as skin rash and skin itching. Patients have to be informed that in cases of emergence of hypersensitivity reactions at them they should report about it immediately to the doctor and to stop administration of drug
– increase in level of transaminases in blood
Sometimes (from 1/1000 to & lt, 1/100)
– a hematemesis, a tar-like chair or a bloody diarrhea, colitis, including gemmoragichesky colitis, exacerbation of ulcer colitis and Crohn’s disease
– developing of hypostases, especially at the patients having an arterial hypertension or a renal failure
– an alopecia
– a small tortoiseshell
– damage of a liver, especially at long therapy, the acute hepatitis which is followed or not followed by jaundice (the fulminantny hepatitis which is very seldom passing into a lightning form, even in the absence of symptoms harbingers)
In this regard at long administration of drug it is necessary to carry out regular control of functional indicators of a liver
Very seldom: & lt, 1/10.000
– the strengthened heartbeat, hypostases, heart failure, a myocardial infarction
– hemopoiesis disturbances (anemia, a leukopenia, thrombocytopenia, a pancytopenia, an agranulocytosis), hemolytic anemia. Fever, pain and inflammation in a throat, superficial ulcers in a mouth, influenzal states, the significant fatigue and also nasal and skin bleedings can be the first signs of these states. When performing long therapy by drug it is necessary to make regular observation of a picture of blood.
– disturbances of sensitivity, disorder of taste, memory disturbance, a disorientation, spasms, a tremor
– disorders of vision (blurring of sight and doubling in eyes)
– sonitus, a passing hearing disorder
– stomatitis, a glossitis (inflammation of language), injury of a gullet, exacerbation of nonspecific ulcer colitis or Crohn’s disease, intestinal impassability, pancreatitis, diafragmopodobny strictures of intestines. Patients have to be informed that at appearance in them of severe pain in upper area of a stomach, a tar-like chair or a hematemesis they should stop immediately administration of drug and to see a doctor.
– defeat of renal fabric (interstitial nephrite, papillary necrosis) which can be followed by development of an acute renal failure, a proteinuria and/or a hamaturia, a nephrotic syndrome. In this regard at patients it is necessary to carry out regular control of function of kidneys.
– a dieback, eczema, an erythema, a photosensitization, a purpura (including an allergic purpura) and bullous reactions, including Stephens-Johnson’s syndrome and a toxic epidermal necrolysis (Lyell’s disease)
– arterial hypertension
– heavy generalized reactions of hypersensitivity. These reactions can be shown by edema of face, language, internal hypostasis of a throat with narrowing of airways, breath difficulty, a cardiopalmus and also falling of arterial blood pressure up to the shock posing a threat for life. In case of emergence any of above-mentioned symptoms which can arise even at the first use Dikloberl of a retard therapy by drug should be stopped immediately and the immediate help of the doctor is required.
– an allergic vasculitis and a pulmonitis (pneumonia)
– psychotic reactions, a depression, uneasiness, dreadful dreams
– the exacerbation of infectious inflammatory diseases (for example, development of a necrotizing fascitis) connected with system prescribing of non-steroidal anti-inflammatory drugs. In cases of emergence or aggravation of weight of symptoms of infectious diseases during use Dikloberl the retarda to patients is recommended to see a doctor immediately. It is necessary to resolve an issue of need of performing antibacterial therapy.
– the symptoms of aseptic meningitis including muscle tension of a nape, a headache, nausea, vomiting, fever and stupefaction. At the patients having autoimmune diseases (the hard currency, the mixed diseases of connective tissue), notes predisposition ment of aseptic meningitis.
– hypersensitivity to diclofenac or other components of drug
– at allergic reactions in the anamnesis (bronchospasm, asthma, rhinitis or a small tortoiseshell) to intake of acetylsalicylic acid or other non-steroidal anti-inflammatory drugs
– in an acute round ulcer and also a recurrence of a peptic ulcer or gastrointestinal bleedings in the anamnesis (two or more registered episodes of gastrointestinal ulcers or bleedings)
– in the gastrointestinal bleedings or perforation in the anamnesis connected with therapy by class NPVP drugs (non-steroidal anti-inflammatory drugs)
– in the presence of stomach ulcer or intestines in an aggravation phase with bleeding or perforation
– in cerebrovascular or other fresh bleedings
– in heavy abnormal liver functions or kidneys
– at the diagnosed heart failure (NYHA II-IV), coronary heart disease, a disease of peripheral arteries and/or disturbance of cerebral circulation
– a disease of the haematogenic system
– pregnancy and the period of a lactation
– children and teenagers up to 18 years
– treatment of postoperative pain after operation of coronary shunting or use of the cardiopulmonary bypass
Other drugs of class NPVP, including salicylates:
Co-administration of several drugs of class NPVP can result in the increased risk of developing ulcers and bleedings in digestive tract in connection with synergy effects. For this reason the simultaneous use of diclofenac and other drugs of class NPVP is not recommended.
Digoxin, Phenytoinum, lithium drugs:
Dikloberl of a retard and digoxin, Phenytoinum or drugs of lithium can lead co-administration to increase in concentration of these drugs in blood. In this regard, in appropriate cases, it is necessary to control concentration of lithium in blood and also it is recommended to exercise control of concentration of digoxin or Phenytoinum in blood.
Diuretics, APF inhibitors and antagonists of angiotensin-II:
Non-steroidal anti-inflammatory drugs can reduce effect of diuretics and antihypertensives. At patients with the broken renal function (for example, the dehydrated or elderly patients) the concomitant use of APF inhibitors or antagonists of angiotensin-II with the drugs inhibiting cyclooxygenase of the 2nd type can lead to aggravation of disturbances of renal function, up to possible development of the acute renal failure which often have irreversible character. In this regard it is necessary to appoint the combinations of drugs mentioned above with care, especially at elderly patients. It is necessary to point out by the patient importance of reception of enough liquid. After the beginning of combination therapy the regular control of indicators of renal function is necessary. Dikloberl of a retard and kaliysberegayushchy diuretics can lead co-administration ment of a hyperpotassemia.
In this regard at the accompanying therapy the potassium level is recommended to control
The accompanying prescribing of glucocorticoid drugs increases risk of developing ulcers and bleedings in digestive tract.
Antiagreganta and inhibitors of the return serotonin reuptake (IRSR):
The accompanying use of antiagregant or drugs of class IOZS increases risk of developing ulcers and bleedings in digestive tract.
Dikloberl retard within 24 hours to or after reception of a methotrexate can lead administration of drug to increase in concentration of a methotrexate in blood and to increase in its toxic action.
Non-steroidal anti-inflammatory drugs (to which sodium diclofenac belongs) can lead to increase in toxic influence of cyclosporine at kidneys.
NPVP can strengthen effect of anticoagulants, such as warfarin.
Probenetsid and Sulfinpyrazonum:
The medicines containing probenetsid or Sulfinpyrazonum can slow down diclofenac removal.
of the Precautionary measure concerning digestive tract
It is necessary to avoid drug Dikloberl co-administration retard with other drugs of class NPVP, including selection inhibitors of cyclooxygenase of the 2nd type.
Side effects of Dikloberl retard can be reduced by purpose of a minimal effective dose of drug during shorter period necessary for stopping of symptoms of a disease.
At elderly patients the increased frequency of development of undesirable reactions to NPVP, in particular gastrointestinal bleedings and perforation which can lead to a lethal outcome is noted.
Gastrointestinal bleedings, ulcers and perforation:
At use of any drugs of class NPVP it was reported about cases of development of the gastrointestinal bleedings, ulcers and perforation capable to lead to a lethal outcome. These complications can arise at any stage of treatment with symptoms harbingers or without them and do not depend on existence of serious gastrointestinal violations in the anamnesis.
Risk of developing gastrointestinal bleedings, ulcers and perforation increases at increase in a dose of NPVP. Besides, the risk of emergence of these states is increased at patients with a digestive tract ulcer in the anamnesis, in particular the complicated bleeding or perforation and also at elderly patients. Such patients have to begin therapy with the minimum dose.
Concerning the category of patients stated above and also at the patients demanding additional therapy by acetylsalicylic acid in low doses or therapy by other drugs capable to increase risk of development of gastrointestinal complications it is necessary to consider the possibility of purpose of the combination therapy including the means protecting a mucous membrane of digestive tract (for example, mizoprostol or inhibitors of the protonew pump).
Patients at whom purpose of NPVP in the past made toxic impact on digestive tract in particular elderly patients, have to report about all unusual symptoms from digestive tract (first of all about gastrointestinal bleedings), especially in an initial phase of therapy.
At the patients receiving the accompanying therapy by the drugs increasing risk of developing an ulcer or bleedings of digestive tract such as oral corticosteroid drugs, anticoagulants (for example, warfarin), the selective serotonin reuptake inhibitors or drugs reducing aggregation of thrombocytes (for example, aspirin), Dikloberl retard it is necessary to appoint with care.
When developing gastrointestinal bleeding or ulcer of a GIT during administration of drug Dikloberl retard, therapy by this drug should be cancelled immediately.
At patients with digestive tract diseases in the anamnesis (nonspecific ulcer colitis, Crohn’s disease), NPVP should appoint therapy with care as it can lead to aggravation of these states.
Influence on warmly – vascular and cerebrovascular systems:
Patients with a hypertension and/or stagnant heart failure easy to moderate severity in the anamnesis demand the corresponding medical control and consultations as there are messages that in certain cases therapy of NPVP can lead to a liquid delay in an organism and to hypostases.
Results of clinical trials and epidemiological data indicate that diclofenac use, in particular in high doses (100 mg of a form retard in day) and at the big duration of therapy is connected with increase in risk of developing arterial thrombosis (for example, a myocardial infarction or a stroke).
Patients with significant risk factors of developing cardiovascular pathology (e.g., an arterial hypertension, a lipidemia, diabetes, smoking) need to appoint diclofenac only after careful assessment of their state.
As risk of developing cardiovascular pathology at intake of diclofenac can increase with increase in a dose and duration of reception, it is necessary to use drug in the smallest effective daily dose during the smallest possible time. It is periodically necessary to repeat assessment of need of the patient for performing symptomatic treatment and its treatment response.
Are available messages that seldom or never use of NPVP was connected with development of serious skin allergic reactions, including exfoliative dermatitis, Stephens-Johnson’s syndrome and a toxic epidermal necrolysis (scalded skin syndrome). Most likely, risk of development of toxic skin reactions is the highest during an initial stage of therapy as, in most cases, skin reactions develop within the first month of therapy. At emergence of the first symptoms of skin rash, damage of mucous membranes or other manifestations of hypersensitivity the therapy by the drug Dikloberl retard should be stopped immediately.
Influence on a liver
In a case the patients need to be careful with an abnormal liver function to prescribing of drug as at treatment by diclofenac their state can worsen. At long or repeated therapy by the drug Dikloberl retard regular control of function of a liver is necessary for precaution. At emergence of signs of disturbance of its function it is necessary to stop administration of drug immediately.
Dikloberl retard it is necessary to appoint other instructions only after the careful analysis of advantage/risk of therapy at the following states:
– at congenital disturbances of metabolism of porphyrine (for example, a sharp intermittent porphyria),
– at the system lupus erythematosus (SLE) and also at the mixed diseases of connective tissue.
Dikloberl retard it is necessary to apply under especially careful medical observation:
– at disturbances of renal function,
– in abnormal liver functions,
– directly after considerable surgical interventions,
– at the patients having hay fever (pollinosis), polyps of a nose or chronic obstructive respiratory diseases as at such patients the risk of development of allergic reactions is increased. Allergic reactions can be expressed in asthma attacks (so-called analgetikovy asthma), a Quincke’s edema or a small tortoiseshell,
– at the patients allergic reacting to other substances as at appointment of the drug Dikloberl as such patient retard there is also an increased risk of approach of reactions of hypersensitivity.
Very seldom at use of diclofenac the development of acute reactions of hypersensitivity was observed (for example, an acute anaphylaxis). At emergence of the first signs of development of reactions of hypersensitivity during reception of the Dikloberl capsules retard therapy by drug should be cancelled immediately. It is necessary to carry out urgent symptomatic treatment.
Diclofenac can suppress aggregation of thrombocytes reversibly. For this reason it is necessary to watch the patients suffering from fibrillation disturbances carefully.
Owing to the pharmakodinamichesky properties, diclofenac, as well as other drugs of class NPVP, can mask infection symptoms. At emergence or aggravation of symptoms of an infection during administration of drug Dikloberl retard is recommended to see a doctor urgently. It is necessary to resolve an issue of need of performing antibacterial therapy. At prolonged use of the drug Dikloberl retard regular control of function of kidneys and a picture of blood is necessary.
At long use of sedatives, headaches which it is impossible to treat the increased doses of these drugs can be observed.
In general, frequent intake of sedatives, in particular combinations of several soothing drugs, can cause the permanent damage of kidneys which is followed by risk of developing a renal failure (so-called analgetikovy nephropathy).
The accompanying alcohol intake can strengthen the side effects caused by active ingredients of drugs of class NPVP, in particular side effects from digestive tract and the central nervous system.
Drug contains sucrose. The patients suffering from rare hereditary intolerance of fructose, a sprue of glucose and a galactose and also insufficiency of enzymes of invertase or isomaltase should not take the drug Dikloberl retard.
Pregnancy and the period of a lactation
Suppression of synthesis of prostaglandins can adversely influence course of pregnancy and/or development of a germ/fruit. Results of epidemiological researches indicate the increased risk of misbirths (abortions), malformations of heart and not fusion of an anterior abdominal wall connected with use of inhibitors of synthesis of prostaglandins in the early period of pregnancy. It is considered that risk of development of side effects increases parallel to increase in a dose and duration of therapy.
In experiments on animals it was shown that prescribing of inhibitors of synthesis of prostaglandins led to increase in frequency of loss of fruits at a stage before implantation and also to increase in mortality of embryos/fruits. Besides, at the animals receiving inhibitors of synthesis of prostaglandins in the period of an organogenesis the increased frequency of various malformations, including defects of a cardiovascular system was noted.
It is not necessary to appoint diclofenac during the first and second trimesters of pregnancy, except for cases when the advantage exceeds risk. In cases of prescribing of diclofenac to the women planning pregnancy or at use of drug in the first and second trimesters of pregnancy the dose and duration of therapy have to be, whenever possible, minimum.
Prescribing of inhibitors of synthesis of prostaglandins in the third trimester of pregnancy can make the following adverse effects on a fruit:
& middot, toxic impact on heart and lungs (with premature closing of a botallov of a channel and development of hypertensia in the system of a pulmonary artery),
& middot, disturbance of renal function which development of a renal failure and an oligoamnios (oligogidramniya) can progress and cause,
– adverse effects concerning mother and the newborn when assigning at the end of pregnancy:
& middot, Possible lengthening of a bleeding time that is caused by inhibiting effect of drug on aggregation of thrombocytes which can be shown even when assigning very low doses,
& middot, Suppression of sokratitelny uterine activity that leads to late or long childbirth.
Therefore, prescribing of diclofenac in the third trimester of pregnancy is contraindicated.
diclofenac and products of its disintegration in insignificant quantities pass Active ingredient into maternal milk. As messages about negative consequences for the baby still did not arrive, at short-term use of drug of need for the feeding termination by a breast, as a rule, is not present. In cases of purpose of high doses or long therapy by drug for treatment of diseases of the rheumatic nature it is necessary to stop temporarily administration of drug during breastfeeding.
Dikloberl retard can lead fertility to disturbances of fertile function at women and, in this regard, prescribing of this drug is not recommended to the women trying to become pregnant. At the women experiencing difficulties with conception and also at the women undergoing inspection concerning infertility it is necessary to think of therapy cancellation by the drug Dikloberl retard.
Features of influence on ability of driving or potentially dangerous mechanisms
At drug Dikloberl use retard in high doses side effects from the central nervous system can take place, for example, fatigue and dizziness that can lead to decrease in reaction and disturbance of ability of driving. These disturbances are especially significant at a concomitant use Dikloberl of a retard with alcohol.
Symptoms: headache, dizziness, obscuring and loss of consciousness, abdominal pain, nausea and vomiting. Besides, gastrointestinal bleedings and also disturbances of functions of a liver and kidneys, development of arterial hypotonia, respiratory depression and cyanosis are possible.
Treatment: there is no specific antidote. The supporting and symptomatic therapy.
The form of release and packing
On 10 capsules place in blister strip packaging from a white film polypropylene – the cycloolefin copolymer-polypropylene welded with soft aluminum foil.
On the 2nd blister strip packagings together with the instruction for medical use in the state and Russian languages put in a pack cardboard.
To Store storage conditions at a temperature not over 25C.
To store out of children’s reach!
not to apply a period of storage after an expiration date!
According to the prescription
Proizvoditel Berlin-Hemi AG (Menarini Group) Gliniker Weg 125 12489 of Berlin, Germany
The owner of the registration certificate
Berlin-Hemi AG (Menarini Group) Gliniker Weg 125 12489 of Berlin, Germany
The Menarini-Fon Haden organization packer, Germany
the Address of the organization accepting in the territory of the Republic of Kazakhstan claims from consumers concerning quality of products (goods):
Representative office of joint-stock company Berlin-Hemi AG in RK
Ph.: +7 727 2446183, 2446184, 2446185
Fax: +7 727 2446180