Diclofenac rectal suppositories 50mg №6×1

Name:
Diclofenac supp rect 50mg in cont. cell pack. No. 6×1 Farmaprim MOLDOVA
Description:
White or white with a yellowish tint suppositories of cylindrical-conical shape. On the cut, the presence of an air and porous rod and a funnel-shaped recess is allowed. The main active ingredient Diclofenac sodium Product form Suppositories Dosage 50 mg Pharmacodynamics Diclofenac inhibits the activity of cyclooxygenase, the main enzyme in the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. The analgesic effect is due to two mechanisms: peripheral (indirectly, through the suppression of prostaglandin synthesis) and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system). Suppresses platelet aggregation. In rheumatic diseases, the anti-inflammatory and analgesic properties of the drug cause a weakening of such symptoms as pain (at rest and during movement), morning stiffness, swelling of the joints. It has a pronounced analgesic effect with moderate and severe pain of a non-rheumatic nature. In inflammatory processes that occur after operations and injuries, it quickly alleviates both spontaneous pain and pain during movement, reduces inflammatory edema at the wound site. In primary dysmenorrhea, relieves pain and reduces bleeding. Pharmacokinetics Absorption is fast and complete, the time of onset of Cmax with rectal administration is 30-40 minutes. The concentration of the drug in plasma is linearly dependent on the size of the administered dose. C max is 0.5-1 µg/ml. Subject to the recommended interval between doses, the drug does not accumulate. Communication with plasma proteins is about 99%. Diclofenac penetrates into the synovial fluid, where its maximum concentration is reached 2 to 4 hours later than in the blood plasma. Metabolized in the liver. The elimination half-life from plasma is 2 hours, from synovial fluid – 3-6 hours. About 60% of the administered dose is excreted as metabolites via the kidneys; less than 1% is excreted unchanged, the rest is excreted as metabolites in the bile. Indications for use Diseases that require rapid anti-inflammatory and / or analgesic effects: inflammatory rheumatic diseases (rheumatoid arthritis, spondyloarthritis, chronic juvenile arthritis and arthritis of other etiologies); degenerative rheumatism of the musculoskeletal system (arthrosis, spondylosis); microcrystalline arthritis (gouty arthritis, pseudogouty arthritis); extra-articular rheumatism (periarthritis, bursitis, myositis, tendinitis, synovitis); other inflammatory diseases of the musculoskeletal system, accompanied by pain. As an analgesic, diclofenac is used for soft tissue injuries, in the postpartum period in the absence of breastfeeding, for primary and secondary dysmenorrhea, in dentistry and after surgical interventions. If you need more information about your condition, ask your doctor for advice. Dosing and Administration Rectally. Adults: 100 mg once a day, 50 mg twice a day. The maximum daily dose is 150 mg. Children over 14 years old: 50 mg 1-2 times a day. Use during pregnancy and lactation If you are pregnant or breastfeeding, if you suspect that you are pregnant or do not exclude the possibility of pregnancy, inform your doctor. Pregnancy Suppression of prostaglandin synthesis can adversely affect the course of pregnancy and intrauterine development of the fetus. Data from epidemiological studies indicate an increased risk of miscarriage and / or the development of heart defects and gastroschisis after taking prostaglandin synthesis inhibitors in early pregnancy. It is believed that the risk increases with increasing dose and duration of therapy. Diclofenac should not be given during the first two trimesters of pregnancy unless the benefit outweighs the risk to the fetus. If diclofenac sodium is used by a woman planning a pregnancy, or in the first and second trimesters of pregnancy, then the dose of the drug should be minimal, and the treatment time should be as short as possible. In the third trimester of pregnancy, diclofenac is contraindicated. Lactation Period Like other NSAIDs, diclofenac is excreted in breast milk in small amounts. Thus, in order to avoid the manifestation of undesirable effects in a child, diclofenac should not be used during breastfeeding. Impact on fertility Like other NSAIDs, diclofenac can lead to impaired female fertility, so it is not recommended for women planning a pregnancy. In women who have difficulty conceiving or who are being tested for infertility, discontinuation of the drug should be considered. Precautions General precautions regarding the use of systemic NSAIDs Gastrointestinal ulcers, bleeding or perforation may occur at any time during NSAID treatment, regardless of COX-2 selectivity, even in the absence of warning signs. To minimize this risk, treatment should be initiated at the lowest effective dose for a short period. Placebo-controlled studies have shown an increased risk of thrombotic cardiovascular and cerebrovascular events with certain selective COX-2 inhibitors. Whether this risk is directly related to COX-1/COX-2 selectivity of individual NSAIDs is not known. Currently, there are no clinical trial data available regarding long-term treatment with the maximum dose of diclofenac; the possibility of a similar increased risk cannot be ruled out. Until such data become available, a careful assessment of the benefit/risk ratio regarding the use of diclofenac in patients with clinically confirmed coronary heart disease, cerebrovascular disorders, peripheral arterial disease, or significant risk factors (for example, arterial hypertension, hyperlipidemia, diabetes mellitus, smoking) should be carried out. In this regard, the minimum effective dose should be used for a short period. Renal effects of NSAIDs include fluid retention with edema and/or hypertension. Therefore, diclofenac should be used with caution in patients with cardiac dysfunction and other conditions that lead to fluid retention. It is necessary to monitor the condition of patients using concomitant diuretics or angiotensin-exceeding enzyme inhibitors, as well as those who have an increased risk of hypovolemia. The consequences tend to be more severe in the elderly. If gastrointestinal bleeding or ulcers occur in patients taking diclofenac, the drug should be discontinued. Skin reactions In connection with the use of NSAIDs, including diclofenac, very rarely reported serious skin reactions, some of them fatal, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. A higher risk of these reactions is noted at the beginning of therapy, and these reactions develop in most cases in the 1st month of treatment. At the first manifestations of skin rash, ulcers of the mucous membranes or any other manifestations of hypersensitivity, diclofenac should be discontinued. In rare cases, as with other NSAIDs, allergic reactions, including anaphylactic/anaphylactoid reactions, may occur even without prior exposure to diclofenac. Effect on infection Due to its pharmacodynamic properties, diclofenac, like other NSAIDs, may mask the signs and symptoms of infection. General cautions regarding the use of diclofenac sodium The simultaneous use of diclofenac with systemic NSAIDs, such as selective COX-2 inhibitors, should be avoided due to the lack of any evidence regarding a synergistic effect, and due to potential additive side effects. Caution is required when used in the elderly. In particular, it is recommended to use the minimum effective dose in debilitated elderly patients or with low body weight. History of asthma Patients with asthma, seasonal allergic rhinitis, chronic obstructive pulmonary disease, or chronic respiratory infections (especially those associated with allergic rhinitis-like symptoms) are more likely to experience reactions to NSAIDs, such as exacerbation of asthma (so-called analgesic intolerance). / analgesic asthma), Quincke’s edema or urticaria. In this regard, such patients are recommended special precautions (readiness for emergency care). This also applies to persons with allergic reactions (eg skin rash, itching, urticaria) to other substances. Influence on the gastrointestinal tract When using NSAIDs, including diclofenac, in patients with symptoms suggestive of disorders of the gastrointestinal tract or with a history suggesting the presence of a stomach or intestinal ulcer, bleeding or perforation, careful medical supervision and special care is necessary. The risk of gastrointestinal bleeding increases with increasing dose and in patients with a history of ulcers, especially with complications in the form of bleeding or perforation, and in the elderly. To reduce the risk of such toxic effects on the gastrointestinal tract, treatment is started and maintained at the minimum effective dose. For such patients, as well as those requiring concomitant use of drugs containing low doses of acetylsalicylic acid or other drugs that are suspected to increase the risk of undesirable effects on the gastrointestinal tract, combination therapy with protective agents (for example, inhibitors) should be considered. proton pump or misoprostol). Patients with a history of gastrointestinal toxicity, especially the elderly, should report any unusual abdominal symptoms (especially gastrointestinal bleeding). Caution is also required for patients receiving concomitant drugs that may increase the risk of ulcers or bleeding, such as systemic corticosteroids, anticoagulants, antithrombotics, or selective serotonin reuptake inhibitors. Effects on the liver Careful medical supervision is required when diclofenac is prescribed to patients with impaired liver function, as their condition may worsen. When using NSAIDs, including diclofenac, the activity of one or more liver enzymes may increase. This fact was noted in clinical studies (about 15% of patients), but it was very rarely accompanied by clinical symptoms (0.5%). In most cases, the activity of enzymes was close to the upper limit of normal and slightly higher. The activity of liver enzymes increased by ?3 – <8 times from the upper limit of normal in 2.5% of cases, and in 1% of patients it increased significantly by ?8 times from the upper limit of normal. The increased activity of enzymes, as a rule, is restored after discontinuation of the use of the drug. During long-term treatment with diclofenac, regular monitoring of liver function and liver enzymes is necessary. If abnormal liver function persists or worsens, and if clinical signs or symptoms may be associated with progressive liver disease, or if other manifestations (eg, eosinophilia, rash) are noted, the drug should be discontinued. In very rare cases, severe, sometimes fatal, reactions may develop, including fulminant hepatitis, liver necrosis, and liver failure. It should be remembered that hepatitis can develop without prodromal symptoms. Caution is necessary when used in patients with hepatic porphyria, because. the drug can provoke attacks of porphyria. Effects on the kidneys Since prostaglandins play an important role in maintaining renal blood flow, long-term treatment with high doses of NSAIDs, including diclofenac, often (1-10%) leads to edema and hypertension. Particular care is needed in the treatment of patients with impaired cardiac or renal function, with a history of arterial hypertension, elderly patients, patients receiving therapy with diuretics or drugs that significantly affect kidney function, as well as patients with a pronounced decrease in extracellular fluid volume of any etiology (for example before or after major surgery). In such cases, regular monitoring of renal function is recommended as a precautionary measure. Termination of therapy usually leads to the restoration of renal function to the state that preceded treatment. Impact on the cardiovascular system Therapy with NSAIDs, including diclofenac, especially long-term therapy and therapy with the drug at high doses, may be associated with a slight increase in the risk of developing serious cardiovascular thrombotic events (including myocardial infarction and stroke). To reduce the risk of these complications, especially in patients with cardiovascular disease and risk factors, NSAIDs should be taken at the lowest effective dose for the shortest possible duration of treatment. In patients with significant risk factors for cardiovascular events (eg, hypertension, hyperlipidemia, diabetes mellitus, smoking), diclofenac should only be used after careful consideration. Due to the possible increased risk of cardiovascular events with long-term use or at a high dose of the drug, patients should be prescribed diclofenac at the lowest effective dose and for the shortest possible time necessary to reduce the severity of symptoms. The need for symptomatic relief and response to treatment should be re-evaluated periodically. Clinical studies and data from epidemiological studies indicate that the use of diclofenac increases the risk of thrombotic complications (for example, myocardial infarction or stroke), especially with prolonged use of this drug or at high doses (150 mg per day). Influence on hematological parameters With long-term use of diclofenac, like other NSAIDs, monitoring of peripheral blood parameters is recommended. Like other NSAIDs, diclofenac may temporarily inhibit platelet aggregation. Patients with impaired hemostasis should be carefully monitored. Use in pediatrics: the drug can be prescribed from 18 years of age. Excipients The drug contains cetyl alcohol, which can cause local skin reactions (contact dermatitis). The use of this drug is possible only after consulting a doctor! Do not stop taking DICLOFENAC without first consulting your doctor! If you have any doubts or questions, please contact your doctor. When treating, regardless of the number of dosage forms used (one or more), the total daily dose of diclofenac sodium should be taken into account, which should not exceed 150 mg. Patients who do not tolerate oral administration of suppositories in appropriate doses. The initial daily dose of diclofenac sodium is 100 mg or 150 mg (1 suppository containing 50 mg of diclofenac sodium 2-3 times a day), depending on the severity of the disease. The maintenance dose of diclofenac sodium is usually 100 mg per day (1 suppository containing 50 mg of diclofenac sodium 2 times a day). Side effects of the drug can be reduced by using the lowest effective dose for the shortest period necessary to relieve symptoms. The suppository should be injected deep into the rectum. Patients with impaired renal function The drug should be used with caution in patients with renal insufficiency. Patients with impaired liver function The drug should be used with caution in patients with hepatic insufficiency. Elderly patients The lowest effective dose is recommended. Children This dosage form is not intended for use in children. Instructions for rectal administration of the drug When using rectal suppositories, abdominal cramps and the urge to defecate often occur, so before the procedure, perform a cleansing enema or empty the intestines naturally. Wash your hands thoroughly with soap. Prepare wet wipes or a handkerchief soaked in water in advance. Lie on your side with your knees pressed to your stomach. For the procedure, this position is the most convenient, as it allows you to minimize discomfort. Remove the candle from the package. The candle is taken with the thumb and middle fingers of the right hand in the middle of the widest part, the index finger rests on the blunt end of the candle. The candle is directed with the free end to the anus and pushed with the index finger into the anal canal until it is completely immersed to a depth of 2-3 cm. Carry out the procedure carefully, without exerting excessive pressure. Despite the fact that the suppository has a streamlined shape, careless use can injure the mucous membrane. Do not get out of bed for about 20 minutes. Wipe your hands with a pre-prepared damp cloth or handkerchief. If within 10 minutes after the introduction of a rectal suppository there is an urge to defecate, empty the intestines and introduce a new suppository. If more than 10 minutes have passed between the introduction of the suppository and a bowel movement, an additional dose of the drug is not required. Interaction with other drugs If you are currently or have recently taken other drugs, tell your doctor. The following interactions include those observed with diclofenac enteric-coated tablets and / or other dosage forms of the drug. Lithium: when used together, it is possible to increase the concentration of lithium in plasma. Monitoring of plasma lithium levels is recommended. Digoxin: when used together, it is possible to increase the concentration of digoxin in plasma. Monitoring of plasma levels of digoxin is recommended. Diuretics and antihypertensive drugs: Like other NSAIDs, diclofenac, when taken together with diuretics or antihypertensive drugs (eg, beta-blockers, angiotensin-converting enzyme inhibitors), may reduce their antihypertensive effect. Therefore, when combining these drugs, care should be taken, and patients, especially the elderly, should periodically monitor blood pressure. Due to the increased risk of nephrotoxicity, especially when diuretics and ACE inhibitors are co-administered, patients should drink adequate fluids, and consideration should be given to monitoring renal function after initiation of concomitant therapy and periodically during its continuation. Simultaneous use with potassium-sparing drugs can lead to an increase in the level of potassium in the blood plasma. Frequent monitoring of this indicator is required. Other NSAIDs and corticosteroids: Co-administration of diclofenac with other systemic NSAIDs or corticosteroids may increase the incidence of gastrointestinal adverse events. Anticoagulants and antiplatelet agents: It is recommended to use with caution due to a possible increase in the risk of bleeding when taken together. Despite the fact that clinical studies have not revealed the effect of diclofenac on the action of anticoagulants, there are separate reports of an increased risk of bleeding in patients receiving diclofenac and anticoagulants at the same time. Such patients should be under close medical supervision. Selective serotonin reuptake inhibitors (SSRIs): Concomitant use of systemic NSAIDs, including diclofenac, and SSRIs may increase the risk of gastrointestinal bleeding. Antidiabetic drugs: in clinical studies it was found that diclofenac does not affect the clinical effect of oral antidiabetic drugs. However, there are separate reports of both hypoglycemic and hyperglycemic effects that have necessitated a change in the dosage of antidiabetic drugs during treatment with diclofenac. Therefore, during concomitant therapy, as a precautionary measure, it is recommended to control the level of glucose in the blood. Methotrexate: Diclofenac may inhibit tubular renal clearance of methotrexate and thereby increase its level. Caution should be exercised when using NSAIDs, incl. diclofenac, less than 24 hours before or after taking methotrexate, since it is possible to increase the concentration in the blood of the latter and, consequently, increase its toxicity. Cyclosporine: Diclofenac, like other NSAIDs, due to its effect on renal prostaglandins, may increase the nephrotoxicity of cyclosporine. In such cases, it is recommended to prescribe diclofenac at doses lower than those that would be prescribed to patients not receiving cyclosporine. Quinolone antibacterials: There are isolated reports of seizures that may have been associated with the concomitant use of quinolones and NSAIDs. Phenytoin: With the simultaneous use of phenytoin and diclofenac, periodic monitoring of the concentration of phenytoin in the blood plasma is recommended due to its possible increase. Colestipol and cholestyramine: Concomitant use may slow down or decrease the absorption of diclofenac. Therefore, it is recommended to take diclofenac at least one hour before or 4 to 6 hours after taking colestipol/cholestyramine. Potent CYP2C9 inhibitors: It is recommended that diclofenac be used with caution in conjunction with potent CYP2C9 inhibitors (eg, sulfinpyrazone and voriconazole), as a significant increase in the maximum plasma concentration and exposure of diclofenac is possible due to inhibition of its metabolism. Contraindications Hypersensitivity to diclofenac or other components of the drug; intolerance to acetylsalicylic acid or other NSAIDs in combination (complete or incomplete) with bronchial asthma, nasal polyps and paranasal sinuses (including history); violation of hematopoiesis of unclear etiology; gastric and duodenal ulcer in the acute phase; inflammatory and erosive and ulcerative lesions of the gastrointestinal tract in the acute phase; active gastrointestinal bleeding, incl. rectal; established congestive heart failure (NYHA II-IV), ischemic heart disease, peripheral arterial disease, cerebrovascular disease, severe heart failure; active liver disease, severe liver failure; severe renal failure (CC less than 30 ml / min); confirmed hyperkalemia; proctitis, hemorrhoids in the acute stage; children under 18; III trimester of pregnancy; lactation period. Composition One suppository contains: active substance: diclofenac sodium 50 mg or 100 mg; excipients: cetyl alcohol, semi-synthetic glycerides. Overdose Symptoms: headache, dizziness, tinnitus, lethargy, convulsions; epigastric pain, nausea, vomiting, diarrhea, bleeding from the gastrointestinal tract; increased blood pressure, acute renal failure, hepatotoxic effect, respiratory depression, coma. Treatment: symptomatic therapy. Forced diuresis, hemodialysis are ineffective (due to a significant connection with proteins and intensive metabolism). Side effects If side effects occur, tell your doctor about it. This applies to all possible side effects, including those not described in this package insert. MedDRA convention for frequency Very common (≥1/10); frequent (?1/100, <1/10); infrequent (?1/1000, <1/100); rare (?1/10000, <1/1000); very rare <1/10000); with unknown frequency (cannot be estimated based on available data). Blood and lymphatic system disorders: very rare - leukopenia, agranulocytosis, thrombocytopenia, anemia (including hemolytic and aplastic). Immune system disorders: rare - hypersensitivity, anaphylactic and anaphylactoid reactions (including hypotension and shock); very rare - angioedema (including swelling of the face). Mental disorders: very rare - disorientation, depression, insomnia, nightmares, irritability, psychotic disorders. Nervous system disorders: common - headache, dizziness; rare - drowsiness; very rare - paresthesia, memory impairment, convulsions, tremor, aseptic meningitis, taste disorders, stroke; with an unknown frequency - confusion, hallucinations, malaise. On the part of the organ of vision: very rare - blurred vision, blurred vision, diplopia. Hearing disorders and labyrinth disorders: common - dizziness, very rare - tinnitus, hearing impairment. Cardiac disorders: very rare - palpitations, chest pain, heart failure, myocardial infarction. Vascular disorders: very rare - arterial hypertension, vasculitis. Respiratory, thoracic and mediastinal disorders: rare - bronchial asthma (including dyspnea), very rare - pneumonia. Gastrointestinal disorders: common - nausea, vomiting, diarrhea, dyspepsia, epigastric pain, flatulence, anorexia; rare - gastritis, gastrointestinal bleeding, hematemesis, bloody diarrhea, melena, stomach and intestinal ulcers (with or without bleeding or perforation), proctitis; very rare - colitis (including hemorrhagic colitis and exacerbation of ulcerative colitis or Crohn's disease), constipation, stomatitis (including ulcerative stomatitis), glossitis, dysfunction of the esophagus, diaphragm-like intestinal stenosis, pancreatitis, exacerbation of hemorrhoids. Violations of the liver and biliary tract: frequent - increased levels of transaminases; rare - jaundice, asymptomatic hepatitis, acute hepatitis, chronic active hepatitis, hepatocellular necrosis, cholestasis; very rare - fulminant hepatitis, liver necrosis, liver failure. Skin and subcutaneous tissue disorders: common - rash; rare - urticaria; very rare - bullous rashes, eczema, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, hair loss, photosensitivity reactions, purpura, including allergic, itching. Renal and urinary disorders: very rare - acute renal failure, hematuria, proteinuria, nephrotic syndrome, papillary necrosis, interstitial nephritis. General disorders and disorders at the injection site: frequent - irritation at the injection site; rare - edema. Storage conditions Store in a dry, dark place at a temperature of 15 - 25oC. Keep out of the reach of children. Buy Diclofenac rectal suppositories 50mg No. 6x1