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100 mg of diclofenac rectal suppository 10s




The instruction for medical use of DICLOFENAC medicine the Trade name Diclofenac the International unlicensed name Diclofenac Dosage Form Suppositories rectal, 50 mg or 100 mg Structure One suppository contains active agent – diclofenac of sodium of 50 mg or 100 mg excipients – cetyl alcohol, solid fat the Description suppositories of a tsilindrokonichesky form, White or white with a yellowish shade. On a cut the existence of an air and porous core and funneled deepening is allowed. Pharmacotherapeutic group Anti-inflammatory and antirheumatic drugs. Non-steroidal anti-inflammatory drugs. Derivatives of acetic acid. Diclofenac. The code of automatic telephone exchange of M 01AB 05 Pharmacological Pharmacokinetics Absorption properties fast, but more slowly, than at use of tablets with an enterosoluble covering. After use of suppositories Diclofenac in a dose of 50 mg its maximum concentration in blood plasma (Cmax) is reached in 1 h, but Cmax on unit of a dose makes near ⅔ from concentration in blood after use of tablets with an enterosoluble covering (1.95± 0.8 mkg/ml (1.9 mkg/ml =5.9 µmol/l)). Bioavailability. As well as in case of use of oral dosage forms of drug, area size under a curve concentration time (AUC) makes about a half from the value received at use of a parenteral dose. After repeated use of drug its pharmacokinetics does not change. Cumulation of drug is not observed at observance of the recommended dosing intervals. Distribution. Linking of diclofenac with proteins of blood plasma makes 99.7%, mainly with albumine – 99.4%. Diclofenac gets into synovial fluid where its Cmax is reached on 2-4 h later, than in blood plasma. The seeming elimination half-life (T½) makes 3-6 h of synovial fluid. In 2 h after achievement of Cmax in blood plasma the concentration of diclofenac in synovial fluid remains to higher, than in blood plasma, this phenomenon is observed during 12 h. Diclofenac is revealed in low concentration (100 ng/ml) in breast milk. The expected amount of drug which gets to an organism of the baby with breast milk is equivalent to a dose of 0.03 mg/kg/days. Metabolism. Diclofenac is metabolized partially by a glyukuronization of not changed molecule, but mainly – by single and multiple hydroxylation and a metoksilirovaniye that leads to formation of several phenolic metabolites most of which part forms conjugates with glucuronic acid. Two of these phenolic metabolites are biologically active, but in much less degree, than diclofenac. Removal. The general system clearance of diclofenac is 263±56 ml/min. of blood plasma (average value ± variate). Final T½ from blood plasma makes 1-2 h T½ of blood plasma of 4 metabolites, including two active, is also short and makes 1-3 h. About 60% of a dose are removed with urine in the form of a glyukuronidny conjugate of an intact molecule and in the form of metabolites, the majority of which also turns into glyukuronidny conjugates. In not changed look less than 1% of diclofenac are removed. The rest of the applied dose of drug is removed in the form of metabolites through bile, with a stake. Pharmacokinetics at separate groups of patients. Influence of age of the patient on absorption, metabolism and removal of drug was not observed. At the patients with a renal failure receiving therapeutic doses the accumulation of not changed active agent was not revealed. At patients with clearance of creatinine less than 10 ml/min. estimated equilibrium concentration of hydroxylated metabolites in blood plasma were about 4 times higher, than at healthy faces. However, finally, all metabolites are removed with bile. At patients with chronic hepatitis or the compensated cirrhosis the indicators of pharmacokinetics and metabolism of diclofenac are similar to that at patients without liver diseases. The pharmacodynamics Diclofenac is non-steroidal anti-inflammatory drug (NPVP) with the expressed anesthetic and anti-inflammatory action. It inhibits activity of cyclooxygenase and, therefore, synthesis of prostaglandins. In vitro sodium diclofenac in concentration, equivalent to those which are reached at treatment of patients does not suppress biosynthesis of proteoglycans of cartilaginous tissue. The indications of Bol of any type and inflammation accompanying various states: – Joint syndrome: a pseudorheumatism, the osteoarthritis ankylosing a spondylitis, gout (gouty arthritis). – Acute defeats of a musculoskeletal system: a periarthritis (for example, in freezing injury), a tendinitis, a tendovaginitis, a bursitis. – A pain syndrome and inflammation after injuries, including in fractures, stretching, bruises of ligaments, sinews, dislocations, backbone pain, including a waist, and after operations, including orthopedic, dental and other small surgical interventions. The route of administration and doses Side effects can be minimized when using a minimal effective dose during the minimum period necessary for control over symptoms (see. Special instructions). Not to accept inside, only for rectal administration. Suppositories need to be entered into a rectum as it is possible more deeply, it is desirable after purgation. Adult: – suppositories on 50 mg 2-3 times a day, – suppositories on 100 mg of 1 times a day. To children 16 years are more senior: suppositories on 50 mg 1-2 times a day. The maximum daily dose of drug should not exceed 150 mg. If necessary therapy can be combined, appointing at the same time diclofenac orally (tablets on 25 mg or 50 mg) and suppositories, without exceeding the maximum daily dose. Duration of a course of therapy is established individually. Special groups of patients Patients of advanced age (65 years are also more senior): though at elderly people the pharmacokinetics of the drug Diclofenac does not worsen to any clinically significant degree, NPVP should be applied with care to such patients as they, as a rule, are more inclined ment of side effects. In particular, the weakened patients of advanced age or persons with insufficient body weight are recommended to use drug in low effective doses, also at treatment of NPVP of patients it is necessary to survey rather gastrointestinal bleedings. Patients with a renal failure. Diclofenac is contraindicated to patients with a heavy renal failure. As special researches at patients with a renal failure were not conducted, specific recommendations about correction of a dose cannot be given. It is recommended to be careful at use Diclofenac at patients with a slight and moderate renal failure. Patients with an abnormal liver function. Diclofenac is contraindicated to patients with a heavy liver failure. As special researches at patients with an abnormal liver function were not conducted, specific recommendations about correction of a dose cannot be given. It is recommended to be careful at use Diclofenac at patients with a slight or moderate abnormal liver function. Children: medicine is not recommended for use for children aged do16 years. Side effects the Following undesirable effects include the phenomena connected with administration of the drug Diclofenac suppositories rectal and/or other dosage forms of diclofenac of sodium at short-term and long reception. Often (≥ 1/100, & lt, 1/10) – a headache, dizziness – nausea, vomiting, diarrhea, dyspepsia, an abdominal pain, a meteorism, hyporexia – increase in level of transaminases – skin rash Seldom (≥ 1/10000, & lt, 1/1000) – hypersensitivity, anaphylactic and anaphylactoid reactions (including arterial hypotension and shock) – drowsiness, fatigue – bronchial asthma (including an asthma) – gastritis, gastrointestinal bleeding, a hematemesis, hemorrhagic diarrhea, a melena, stomach ulcers and intestines (followed or not followed by bleeding or perforation) – hepatitis, jaundice, an abnormal liver function – urticaria – the irritation in the injection site, hypostases – morbidity of mammary glands, disturbance of reproductive function at women is Very rare (& lt, 1/10000) – thrombocytopenia, a leukopenia, hemolytic anemia, aplastic anemia, an agranulocytosis – a Quincke’s disease (including a face edema) – a disorientation, a depression, insomnia, nightmares, irritability, mental disorders – paresthesias, dysmnesias, spasms – uneasiness, a tremor, disturbances of taste, aseptic meningitis, a stroke – disorders of vision, the illegibility of sight, a diplopia – hearing disorder, sonitus – a cardiopalmus, a stethalgia, heart failure, a myocardial infarction – arterial hypertension, arterial hypotension, a vasculitis – a pneumonitis – colitis (including hemorrhagic colitis and exacerbation of ulcer colitis or Crohn’s disease) – a constipation, stomatitis (including a stomacace), a glossitis – dysfunction of a gullet, a diafragmopodobny intestinal stenosis – pancreatitis – lightning hepatitis, hepatic necrosis, a liver failure – diseases of skin and hypodermic cellulose – bullous rashes, eczema, an erythema, a multiformny erythema – Stephens-Johnson’s syndrome, a toxic epidermal necrolysis (Lyell’s disease), exfoliative dermatitis – an alopecia, reactions of photosensitivity, purple, including allergic, an itching – an acute renal failure, a hamaturia, a proteinuria – a nephrotic syndrome, interstitial nephrite, renal papillary necrosis, urination disorder – impotence With an unknown frequency – confusion of consciousness, a hallucination – disturbance of sensitivity, a general malaise – an optic neuritis indicate Clinical trials and data of epidemiological researches that use of diclofenac increases risk of emergence of trombotichesky complications (for example, a myocardial infarction or a stroke), especially at prolonged use or in high doses (150 mg a day). Contraindications – hypersensitivity to active agent or to drug excipients – – stomach ulcer or intestines in aggravation stages, bleeding or perforation the postponed gastrointestinal bleedings or perforation connected with the previous reception of NPVP – an acute or recurrent peptic ulcer / bleeding (two or more episodes of the established ulcer or bleeding in the anamnesis) – the III trimester of pregnancy – heavy liver, renal or heart failure – to patients who have attacks of bronchial asthma urticaria, a Quincke’s disease, acute rhinitis are provoked by reception of an ibuprofen, acetylsalicylic acid or other NPVP – a proctitis – children’s age up to 16 years – the established stagnant heart failure (NYHA II-IV), coronary heart disease, diseases of peripheral arteries or cerebrovascular diseases Medicinal interactions the interactions Given below include those which were observed at reception of the tablets of diclofenac covered with an enterosoluble cover and/or other dosage forms of drug. Lithium: at combined use the increase in concentration of lithium in plasma is possible. Monitoring of levels of lithium in plasma is recommended. Digoxin: at combined use the increase in concentration of digoxin in blood serum is possible. Control of levels of digoxin in serum is recommended. Diuretics and hypotensive drugs: Diclofenac, as well as other NPVP, can slow down effect of diuretic and hypotensive drugs (beta-blockers, ATP inhibitors). To patients, especially elderly, it is necessary to appoint these combinations with care and to periodically control arterial blood pressure. Patients have to be adequately hydrated. After the beginning and periodically during treatment, especially when prescribing diuretics and APF inhibitors, it is necessary to control function of kidneys, because of the increased risk of nephrotoxicity. Medicines which, as we know, cause a hyperpotassemia: the concomitant use with kaliysberegayushchy diuretics, cyclosporine, takrolimusy or Trimethoprimum can lead to increase in level of potassium in blood plasma therefore monitoring of a condition of patients should be carried out more often. Anticoagulants and antitrombotichesky drugs: it is recommended to apply with care because of possible increase in risk of bleeding at joint reception. Though clinical trials do not demonstrate influence of diclofenac on activity of anticoagulants, there are separate data on increase in risk of bleeding at the patients receiving diclofenac and anticoagulants at the same time. Therefore careful monitoring of such patients is recommended. Other NPVP, including selection TsOG-2 inhibitors, and corticosteroids: the combined use of diclofenac and other system NPVP or corticosteroids can increase risk of gastrointestinal bleeding or ulcer. It is necessary to avoid simultaneous use of two or more NPVP. Selective Serotonin Reuptake Inhibitors (SSRI): joint purpose of system NPVP and SIOZS can increase risk of gastrointestinal bleedings. Antidiabetic drugs: clinical trials showed that diclofenac can be applied together with oral antidiabetic drugs without influence on their clinical action. However, separate messages about development in such cases, both the hypoglycemia, and a hyperglycemia demanding need of change of a dose of glucose-lowering drugs during therapy by diclofenac are known. Monitoring of level of glucose in blood is recommended as a preventive measure at a concomitant use. Methotrexate: the care at therapy of NPVP is necessary less than for 24 h to or after reception of a methotrexate as in such cases the concentration of a methotrexate in blood can increase and increase its toxic action. Cyclosporine: impact of NPVP on synthesis of prostaglandins in kidneys can increase nephrotoxicity of cyclosporine. In this regard, the dose Diclofenac at the patients receiving cyclosporine has to be lower, than at patients who do not accept cyclosporine. Takrolimus: at use of NPVP with takrolimusy increase in risk of nephrotoxicity is possible that can be mediated through renal antiprostaglandinovy effects of NPVP and inhibitor of a kaltsinevrin. Antibacterial hinolona: there are separate messages about development of spasms in patients which are at the same time accepting derivatives of hinolon and NPVP. It can be observed at patients as with epilepsy and spasms in the anamnesis, and without them. Thus, the patients who are already applying NPVP should show care at the solution of a question of use of hinolon. Phenytoinum: at joint intake of Phenytoinum and diclofenac the monitoring of concentration of Phenytoinum in blood plasma because of the expected increase in exposure of Phenytoinum is recommended. Kolestipol and holestiramin: the concomitant use can lead to delay or reduction of absorption of diclofenac. Therefore it is recommended to take diclofenac for 1 h to or from 4 to 6 h after reception of a kolestipola/holestiramin. Cardiac glycosides: simultaneous use of cardiac glycosides and NPVP for patients can strengthen heart failure, reduce glomerular filtration rate and increase the level of glycosides in blood plasma. Mifepristone: NPVP should not be applied within 8-12 days after mifepristone use as NPVP can reduce effect of mifepristone. Strong CYP2C9 inhibitors: it is recommended to be careful at a concomitant use of diclofenac and CYP2C9 of inhibitors (such as vorikonazol) which can affect significant increase in concentration of diclofenac in plasma because of inhibition of his metabolism. Special instructions the General to minimize side effects, it is necessary to apply a minimal effective dose during the shortest span. It is necessary to avoid simultaneous use of the drug Diclofenac and other NPVP, including selection TsOG-2 inhibitors, owing to lack of data on synergy medical effect and possible additive side effects. It is necessary to be careful when prescribing drug to elderly people. In particular, are recommended to apply the lowest effective dose the weakened patients of advanced age with insufficient body weight. At intake of diclofenac, as well as other NPVP which were earlier not taking the drug manifestation of allergic reactions, including anaphylactic/anaphylactoid reactions is in rare instances possible. On
obno other NPVP, in connection with features of pharmakodinamichesky properties, diclofenac can mask manifestations and symptoms of infectious diseases. Influence on a digestive tract At use of NPVP, including diclofenac, cases of gastrointestinal bleedings (hematemesis, a melena), an ulcer or perforation which can be fatal are registered and occur at any time in the course of treatment at existence or lack of precautionary symptoms or the previous anamnesis of the serious phenomena from a GIT. These phenomena usually have more serious consequences at patients of advanced age. In case of developing of gastrointestinal bleedings at the patients taking the diclofenac given medicine it is necessary to cancel. As well as at use of other NPVP, when assigning, Diclofenac, to patients with the symptoms demonstrating disturbances from a digestive tract obligatory is medical observation and extra care. The risk of developing of bleeding, ulcer or perforation in a GIT increases with increase in a dose of NPVP, including diclofenac, and at patients with existence is the ulcer in the anamnesis which is especially complicated by bleeding and also at elderly people. To reduce risk of such toxic impact on a GIT, treatment should be begun and supported by minimal effective doses. For such patients and also the patients needing the accompanying use of the medicines containing low doses of acetylsalicylic acid or other medicines which probably increase risk of undesirable action on a GIT it is necessary to consider a question of use of combination therapy using protective equipment (for example, inhibitors of the proton pump or a mizoprostol). Patients with gastrointestinal toxicity in the anamnesis, especially advanced age, have to report about any unusual abdominal symptoms (especially about bleeding from a GIT). The precaution is also necessary for the patients receiving at the same time medicines which can increase risk of an ulcer or bleeding, such as system corticosteroids, anticoagulants (for example, warfarin), selective serotonin reuptake inhibitors or antitrombotichesky means (for example, acetylsalicylic acid). During therapy by drug it is necessary to carry out careful medical observation and to be careful at patients with ulcer colitis or Crohn’s disease as their state can become aggravated. Influence on a liver Careful medical observation is required when assigning Diclofenac to patients with abnormal liver functions as their state can worsen. At use of NPVP including diclofenac, the activity of one or several enzymes of a liver can increase. During long-term treatment by diclofenac regular observation of function of a liver and level of liver enzymes as a precautionary measure is necessary. If abnormal liver functions remain or aggravated and if clinical signs, or symptoms can be connected with the progressing liver diseases or if other manifestations are noted (for example, an eosinophilia, rash), use of drug should be stopped. The course of diseases, such as hepatitis, can pass without prodromal symptoms. Cautions are necessary if Diclofenac is applied at patients with a hepatic porphyria, because of the probability of provoking of an attack. Influence on kidneys Therapy of NPVP, including diclofenac, can be connected with a delay of liquid or hypostasis. Special attention should be paid to patients with dysfunctions of heart or kidneys, with arterial hypertension in the anamnesis, to the patients of advanced age, patients receiving therapy by the diuretics or drugs significantly influencing function of kidneys and also to patients with the significant decrease in extracellular volume of liquid of any etiology (for example, to or after serious surgical intervention). In such cases as a precautionary measure it is recommended to carry out regular control of function of kidneys. The therapy termination usually leads to restoration of function of kidneys to a state which preceded treatment. Influence on skin Due to the use of NPVP, including Diclofenac, serious reactions from skin (some of them were fatal), including exfoliative dermatitis, Stephens-Johnson’s syndrome and a toxic epidermal necrolysis were seldom or never registered. At patients the high risk of these reactions was revealed at the beginning of a therapy course: emergence of reaction is noted in most cases within the first month of treatment. Use of the drug Diclofenac needs to be stopped at the first appearance of skin rash, damage of a mucous membrane or emergence of any other signs of hypersensitivity. The System Lupus Erythematosus (SLE) and the mixed diseases of connective tissue At patients with hard currency and the mixed diseases of connective tissue can be observed the increased risk of developing aseptic meningitis. Cardiovascular and cerebrovascular effects Patients with considerable risk factors of cardiovascular complications (for example, arterial hypertension, a lipidemia, diabetes, smoking) should appoint diclofenac only after thorough examination of such opportunity. Owing to possible increase in risk of development of the cardiovascular phenomena at prolonged use or in a high dose of drug the patients should appoint diclofenac in a minimal effective dose and to accept its shortest time necessary for reduction of expressiveness of symptoms. It is necessary to carry out periodically the repeated assessment of need of relief of symptoms and the response to the carried-out treatment. Patients with presence of arterial hypertension and/or stagnant heart failure of light or moderate severity in the anamnesis require carrying out the corresponding monitoring and providing recommendations as in connection with use of NPVP, including diclofenac, cases of a delay of liquid and hypostases were registered. Clinical trials and epidemiological data indicate that use of diclofenac increases risk of emergence of trombotichesky complications (for example, a myocardial infarction or a stroke), especially at prolonged use of this drug or in high doses (150 mg a day). Patients with uncontrollable arterial hypertension, stagnant heart failure, steady coronary heart disease, diseases of peripheral arteries and/or a cerebrovascular disease should appoint diclofenac only after careful assessment of a ratio risk/advantage. Influence on hematologic indicators At prolonged use of drug, as well as other NPVP, is recommended monitoring of a picture of peripheral blood. Diclofenac can temporarily inhibit aggregation of thrombocytes therefore it is necessary to control carefully a condition of patients with disturbance of a hemostasis, hemorrhagic diathesis or hematologic disturbances. Influence on a respiratory system (asthma in the anamnesis) At patients with asthma, seasonal allergic rhinitis, a rhinedema (for example: nasal polyps), chronic obstructive diseases of lungs or persistent infections of a respiratory path (especially with the manifestations similar to symptoms of allergic rhinitis) at reception of NPVP more often than other patients, have such side effects as exacerbation of asthma (so-called intolerance of analgetics or analgetic asthma), a Quincke’s edema or urticaria. In this regard special precautionary measures (readiness for rendering emergency aid) are necessary for such patients. Above stated also concerns patients with allergic manifestations at use of other drugs, for example rash, an itching or urticaria. Pregnancy and feeding by a breast Pregnancy Suppression of synthesis of prostaglandins can negatively affect a course of pregnancy and pre-natal fetation. If Diclofenac the woman planning pregnancy or in І applies a pregnancy trimester, the dose of drug has to be as low as possible, and treatment duration — as it is possible well. In ІІІ a pregnancy trimester inhibitors of synthesis of prostaglandins can influence: 1) on a fruit and to cause: cardiopulmonary toxicity (with premature closing of an arterial channel and pulmonary hypertensia) and a renal failure which can progress to a renal failure with oligogidramniony, 2) on mother, the newborn and also for the result of pregnancy: lengthening of a bleeding time, antiagregantny effect which can be observed even at very low doses, oppression of sokratitelny ability of a uterus that leads to a delay or increase in the period of childbirth are possible. Diclofenac is contraindicated in ІІІ a pregnancy trimester. The lactation As well as other NPVP, diclofenac in insignificant quantity gets into breast milk. In this regard suppositories Diclofenac should not be applied to women during feeding by a breast to avoid undesirable impact on the baby. The fertility at women As well as other NPVP, Diclofenac can negatively affect female fertility therefore the women planning pregnancy are not recommended to appoint drug. For women who have problems with conception or undergo inspection concerning infertility, it is necessary to consider expediency of drug withdrawal Diclofenac. Features of influence of medicine on ability to run the vehicle or potentially dangerous mechanisms during treatment reduction of speed of mental and motor reactions is possible. Patients who test disorders of vision, dizziness, drowsiness, disturbances from the central nervous system, fatigue at reception of NPVP have to abstain from control of vehicles or other mechanisms. The overdose of the Typical clinical picture characteristic of diclofenac overdose does not exist. The overdose can cause such symptoms as a headache, nausea, vomiting, pain in epigastric area, gastrointestinal bleeding, diarrhea, dizziness, a disorientation, excitement, a coma, drowsiness, sonitus, a syncope or spasms. In case of a serious poisoning the development of an acute renal failure and injury of a liver is possible. Treatment: symptomatic therapy. During 1 h after wrong oral administration of toxic amount of drug the gastric lavage, intake of activated carbon is recommended. In frequent or long spasms it is necessary in/in to enter diazepam. Taking into account a clinical condition of the patient other actions can be shown. Form of release and packing Suppositories the rectal, containing 50 mg of diclofenac: On 6 suppositories in blister strip packagings from a film polyvinylchloride laminated by polyethylene. On 1 blister strip packaging together with the instruction for medical use in the state and Russian languages put in a pack from cardboard. The rectal suppositories containing 100 mg of diclofenac: On 5 suppositories in blister strip packagings from a film polyvinylchloride laminated by polyethylene. On the 2nd blister strip packagings together with the instruction for use in the state and Russian languages put in a pack from cardboard. To Store storage conditions in the dry, protected from light place, at a temperature not over 25 s. Not to freeze. To store out of children’s reach! 3 years not to apply a period of storage after an expiration date. Prescription status According to the prescription the Producer of Ltd company to PHARMAPRY st. Krinilor, 5, the village Porumben, the area Kriulen, the Republic of Moldova, MD-4829 the Owner of the registration certificate of Ltd company PHARMAPRIM, the Republic of Moldova the Address of the organization in the territory of the Republic of Kazakhstan of the accepting claim (offer) from consumers on quality of medicine and responsible for post-registration observation of safety of medicine Representative office of PHARMAPRIM SRL in Republic of Kazakhstan, Almaty, Gogol St., 86, office 528, ph. 8-727-2796518

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