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  • Diclosafe 100mg 10 suppositories — Made in India — Free Delivery

Diclosafe 100mg 10 suppositories — Made in India — Free Delivery

(Diclosafe 100mg )
Diclosafe 100mg 10 suppositories — Made in India — Free Delivery
Diclosafe 100mg 10 suppositories — Made in India — Free Delivery
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Description Diclosafe 100mg 10 suppositories — Made in India — Free Delivery

Pharmacological properties

Pharmacodynamics. Diclofenac sodium - NSAID, which has a pronounced analgesic and anti-inflammatory effect. it is an inhibitor of prostaglandin synthetase (cog).
Pharmacokinetics. Suction. Absorption is fast, but slower than with enteric-coated tablets.
After the use of diclofenac sodium suppositories at a dose of 50 mg, the concentration per dose unit is about ⅔ the concentration achieved after using enteric coated tablets (1.95 ± 0.8 μg / ml (1.9 μg / ml = 5.9 μmol / l)).
Bioavailability. As in the case of the use of oral dosage forms of the preparation, the AUC is approximately half of the value obtained with the use of a parenteral dose. After repeated use of the preparation, its pharmacokinetics does not change. Cumulation of the preparation is not observed, provided that the recommended doses are observed.
Distribution. The binding of diclofenac to blood plasma proteins is 99.7%, mainly with albumin - 99.4%.
Diclofenac penetrates into the synovial fluid, where its Cmax is reached 2–4 hours later than in blood plasma. The apparent T1 / 2 from the synovial fluid is 3-6 hours. 2 hours after reaching Cmax in the blood plasma, the concentration of diclofenac in the synovial fluid remains higher than in the blood plasma, this phenomenon is observed within 12 hours.
Diclofenac was determined at a low concentration (100 ng / ml) in breast milk in one woman. The estimated amount of the preparation entering the infant's body with breast milk is equivalent to a dose of 0.03 mg / kg / day.
Metabolism. Diclofenac is metabolized in part by glucuronidation of an unchanged molecule, but mainly through single and multiple hydroxylation and methoxylation, which leads to the formation of several phenolic metabolites, most of which form conjugates with glucuronic acid. Two of these phenolic metabolites are biologically active, but significantly less than diclofenac.
Excretion. The total systemic clearance of diclofenac is 263 ± 56 ml / min (mean ± CO). The final T1 / 2 from blood plasma is 1–2 hours. The half-life in the blood of four metabolites, including two pharmacologically active ones, is also short and amounts to 1–3 hours. About 60% of the preparation dose is excreted in the urine in the form of conjugates with glucuronic acid of an intact molecule and as metabolites, most of which are also converted to glucuronide conjugates. 1% of diclofenac is excreted unchanged. The remaining doses of the preparation are excreted in the form of metabolites in the feces.
Pharmacokinetics in certain groups of patients. The effect of the patient's age on the absorption, metabolism and excretion of the preparation was not noted, except for the fact that in 5 elderly patients, a 15-minute infusion led to a 50% higher concentration of the preparation in the blood plasma than was expected in young healthy volunteers.
In patients with impaired renal function who received therapeutic doses, accumulation of unchanged active substance can not be expected, based on the kinetics of the preparation after a single use. In patients with creatinine clearance of 10 ml / min, the calculated equilibrium plasma concentrations of hydroxylated metabolites were approximately 4 times higher than in healthy volunteers. Ultimately, however, all metabolites were excreted in the bile.
Patients with impaired liver function. In patients with chronic hepatitis or compensated liver cirrhosis, the pharmacokinetics and metabolism of diclofenac are similar to those in patients without liver disease.

Indications

Inflammatory and degenerative forms of rheumatism: rheumatoid arthritis, juvenile rheumatoid arthritis, ankylosing spondylitis, osteoarthritis, including spondyloarthritis.
Pain syndromes from the spine.
Rheumatic diseases of extra-articular soft tissues.
Post-traumatic and postoperative pain syndromes accompanied by inflammation and edema, especially after dental and orthopedic operations.
Gynecological diseases accompanied by pain and inflammation, such as primary dysmenorrhea and adnexitis.
Migraine attacks.
Acute gout attacks.
As an adjuvant in severe inflammatory diseases of the ENT organs, accompanied by a painful sensation, for example, with pharyngotonsillitis, otitis media.
In accordance with general therapeutic principles, the underlying disease should be treated with basic therapy. Fever in itself is not an indication for the use of the preparation.

Application

The minimum effective dose should be applied for a short period, taking into account the treatment objectives of each individual patient.
Do not take orally, for rectal administration only.
Suppositories should be injected into the rectum as deep as possible, preferably after bowel cleansing.
The initial dose is usually 100-150 * mg / day. With unexpressed symptoms, as well as with long-term therapy, a dose of 75 * –100 mg / day is sufficient.
The daily dose is divided into 2-3 doses. To avoid night pain or morning stiffness, before taking the preparation during the day, prescribe diclofenac sodium in the form of rectal suppositories before bedtime (the daily dose should not exceed 150 * mg).
In primary dysmenorrhea, the daily dose should be selected individually, usually it is 50–150 * mg / day. The initial dose may be 50 * –100 mg / day, but if necessary, it can be increased over several menstrual cycles to a maximum of 200 mg / day.
The use of the preparation should be started after the onset of the first painful symptoms and continued for several days, depending on the dynamics of regression of symptoms.
For the treatment of migraine attacks, the course should be started at a dose of 100 mg when the first signs of the onset of an attack appear. If necessary, on the same day, it is possible to apply a second suppository (100 mg of diclofenac). If necessary, on the following days, treatment can be continued (the daily dose should not exceed 150 * mg, the dose should be divided into 2-3 doses).
* Apply at the appropriate dosage.
Elderly patients. Although the pharmacokinetics of diclofenac sodium do not deteriorate to any clinically significant degree in elderly patients, NSAIDs should be used with caution in such patients, since they are usually more prone to developing adverse reactions. In particular, the lowest effective dose is recommended for debilitated elderly patients or patients with a low body mass index; also, patients should be evaluated for gastrointestinal bleeding during NSAID treatment.
Method of using suppositories. Suppositories should be injected into the rectum as deeply as possible, preferably after bowel cleansing. Suppositories should not be divided into parts, since such a change in the method of administration of the preparation can lead to a violation of the distribution of the active substance.

Contraindications

Hypersensitivity to the active substance or any auxiliary component.
A history of bleeding or perforation of the gastrointestinal tract associated with previous treatment with NSAIDs.
Active gastrointestinal ulcer / bleeding or recurrent gastrointestinal ulcer / history of bleeding (2 or more separate episodes of established ulcer or bleeding).
III trimester of pregnancy.
Inflammatory bowel disease (such as Crohn's disease or ulcerative colitis).
Liver failure.
Renal failure
Congestive heart failure (NYHA II – IV), ischemic heart disease in patients with angina pectoris, myocardial infarction.
Cerebrovascular diseases in patients with stroke or with episodes of transient ischemic attacks.
Peripheral artery disease.
Proctitis.
Diclofenac sodium, like other NSAIDs, is contraindicated in patients who develop asthma attacks, urticaria, angioedema or acute rhinitis in response to acetylsalicylic acid or other NSAIDs.

Side effects

Blood and lymphatic system disorders: thrombocytopenia, leukopenia, anemia (hemolytic anemia, aplastic anemia), agranulocytosis.
From the immune system: hypersensitivity, anaphylactic and anaphylactoid reactions (including hypotension and shock), angioedema (including facial edema).
Mental disorders: disorientation, depression, insomnia, irritability, nightmares, psychotic disturbances.
From the nervous system: headache, dizziness, drowsiness, fatigue, paresthesia, weakness, memory impairment, convulsions, anxiety, tremor, aseptic meningitis, taste disturbances, stroke, confusion, hallucinations, impaired sensitivity, general malaise.
From the side of the organ of vision: visual disturbances, blurred vision, diplopia, optic neuritis.
On the part of the organ of hearing and the labyrinth of the ear: vertigo, ringing in the ears, hearing disorders.
From the side of the cardiovascular system: palpitations, chest pain, heart failure, myocardial infarction, hypertension, arterial hypotension, vasculitis.
From the respiratory system, chest and mediastinal organs: BA (including shortness of breath), bronchospasm, pneumonitis.
From the digestive system: nausea, vomiting, diarrhea, dyspepsia, epigastric pain, flatulence, gastritis, gastrointestinal bleeding, hematemesis, melena, hemorrhagic diarrhea, stomach and intestinal ulcers, accompanied or not accompanied by bleeding or perforation (sometimes fatal, especially in elderly patients), colitis (including hemorrhagic colitis and exacerbation of ulcerative colitis or Crohn's disease), ischemic colitis, constipation, stomatitis (including ulcerative stomatitis), glossitis, esophageal dysfunction, diaphragmatic bowel stenosis, pancreatitis.
From the hepatobiliary system: increased transaminase levels, hepatitis, jaundice, abnormal liver function, fulminant hepatitis, liver necrosis, liver failure.
Skin and subcutaneous tissue disorders: rash, urticaria, blistering rash, eczema, erythema, erythema multiforme, Stevens-Johnson syndrome, Lyell's syndrome (toxic epidermal necrolysis), exfoliative dermatitis, hair loss, photosensitivity, purpura, including allergic , itching.
On the part of the kidneys and urinary system: acute renal failure, hematuria, proteinuria, interstitial nephritis, nephrotic syndrome, papillary necrosis of the kidney.
General disorders and disorders at the injection site: irritation at the injection site, edema, abscess at the injection site, exacerbation of hemorrhoids.
On the part of the reproductive system and mammary glands: impotence.
Clinical studies and epidemiological data indicate an increased risk of thrombotic complications (for example, myocardial infarction or stroke) associated with the use of diclofenac, in particular in high therapeutic doses (150 mg / day) and with prolonged use.

Special instructions

General. to minimize side effects, the lowest effective dose should be used for a short period.
The simultaneous use of Diclosef with systemic NSAIDs, such as selective COX-2 inhibitors, should be avoided due to the lack of any evidence of synergistic action and association with potential additive side effects.
Caution is required when used in patients over the age of 65 years. In particular, it is recommended to use the lowest effective dose in debilitated elderly patients with low body weight.
In rare cases, as with the use of other NSAIDs, allergic reactions, including anaphylactic / anaphylactoid reactions, may occur, even without prior exposure to diclofenac. Due to its pharmacodynamic properties, the preparation Dicloseif, like other NSAIDs, can mask the signs and symptoms of infection.
Effects on the digestive tract. With the use of all NSAIDs, including diclofenac, cases of gastrointestinal bleeding (vomiting of blood, melena), ulceration or perforation have been reported, which can be fatal and occur at any time during treatment with or without warning symptoms or a previous history of serious events with sides of the digestive tract. These events usually have more serious consequences in elderly patients. If patients receiving diclofenac sodium experience symptoms of gastrointestinal bleeding or ulceration, the preparation should be discontinued.
As with other NSAIDs, including diclofenac, medical supervision and extreme caution are required for patients with symptoms suggestive of gastrointestinal (GI) disorders. The risk of bleeding, ulceration or perforation in the gastrointestinal tract increases with increasing doses of NSAIDs, including diclofenac, and in patients with a history of ulcers, especially those with complications such as bleeding or perforation, and in elderly patients.
Elderly patients have an increased incidence of adverse reactions to the use of NSAIDs, especially in relation to gastrointestinal bleeding and perforation, which can be fatal.
To reduce the risk of such toxic effects on the gastrointestinal tract, treatment should be started and maintained at low effective doses.
For such patients, as well as those who require the combined use of preparations containing low doses of acetylsalicylic acid (or other preparations that are likely to increase the risk of adverse effects on the gastrointestinal tract), the use of combination therapy with protective agents should be considered ( e.g. proton pump inhibitors or misoprostol). Patients with a history of gastrointestinal toxicity, especially the elderly, should report any unusual abdominal symptoms (especially gastrointestinal bleeding). Cautions are also needed for patients receiving concomitant medications that may increase the risk of ulcers or bleeding, such as systemic corticosteroids, anticoagulants (eg warfarin), antithrombotics (eg acetylsalicylic acid), or selective serotonin reuptake inhibitors.
Effects on the liver. Careful medical supervision is necessary if Diclosef is prescribed to patients with impaired liver function, as their condition may worsen.
As with other NSAIDs, including diclofenac, one or more liver enzymes may be elevated. During long-term use of diclofenac sodium, as a precautionary measure, prescribe regular monitoring of liver function. If liver dysfunctions persist or worsen and if clinical signs or symptoms may be associated with progressive liver disease, or if other manifestations are observed (for example, eosinophilia, rash), the use of Diclosafe should be discontinued. The course of diseases such as hepatitis can pass without prodromal symptoms. Cautions are required if Diclosef is used in patients with hepatic porphyria due to the likelihood of provoking porphyria attacks.
Effects on the kidneys. Since cases of fluid retention and edema have been reported during the treatment of NSAIDs, including diclofenac, special attention should be paid to patients with impaired cardiac or renal function, a history of hypertension, elderly patients, patients receiving concomitant therapy with diuretics or preparations that significantly affect renal function; and in patients with a significant decrease in extracellular fluid volume for any reason, such as before or after major surgery. In such cases, monitoring of renal function is recommended as a precautionary measure. Discontinuation of therapy usually results in a return to the state prior to treatment.
Effects on the skin. In connection with the use of NSAIDs, including diclofenac sodium, serious skin reactions (some of them fatal) have been reported in very rare cases, including exfoliative dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. In patients, a high risk of developing these reactions is observed at the beginning of the course of therapy: the appearance of a reaction is noted in most cases during the first month of treatment. The use of the preparation Diclosef should be discontinued at the first appearance of skin rashes, mucosal lesions or any other signs of hypersensitivity.
Systemic lupus erythematosus and mixed connective tissue diseases. Patients with systemic lupus erythematosus and mixed connective tissue diseases may be at increased risk of developing aseptic meningitis.
Cardiovascular and cerebrovascular effects. Clinical studies and epidemiological data indicate that the use of diclofenac, especially in high doses (150 mg / day) and with long-term treatment, may be associated with a slight increase in the risk of arterial thrombotic events (for example, myocardial infarction or stroke).
Prescribing diclofenac to patients with significant risk factors for cardiovascular events (for example, hypertension, hyperlipidemia, diabetes mellitus, smoking) can only be after a thorough clinical assessment. Since the cardiovascular risks of diclofenac may increase with increasing dose and duration of treatment, it should be used for the shortest possible period and at the lowest effective dose. The patient's need for diclofenac should be periodically reviewed to reduce the severity of symptoms and response to therapy.
Patients should be informed about the possibility of serious arterial thrombotic events (chest pain, shortness of breath, weakness, speech impairment) that can occur at any time. In this case, you should immediately consult a doctor.
Influence on hematological parameters. With prolonged use of diclofenac sodium, like other NSAIDs, monitoring of a complete blood count is recommended.
The preparation Dicloseif can reversibly inhibit platelet aggregation. Patients with hemostasis disorders, hemorrhagic diathesis or hematological disorders should be closely monitored.
History of asthma. Patients with AD, seasonal allergic rhinitis, nasal mucosa edema (i.e. polyps), COPD, or chronic respiratory tract infections (especially those associated with allergic rhinitis-like symptoms) are more likely to experience NSAID reactions such as exacerbation of AD (i.e. called analgesic intolerance / analgesic asthma), Quincke's edema, urticaria. In this regard, in relation to such patients, special measures are recommended (readiness to provide emergency care). This also applies to patients with allergic reactions to other substances, such as rash, itching, hives.
Like other preparations that suppress the activity of prostaglandin synthetase, diclofenac sodium and other NSAIDs can provoke the development of bronchospasm when used in patients with asthma or patients with a history of asthma.
Use during pregnancy and lactation. Pregnancy. In the first and second trimester of pregnancy, diclofenac sodium can be prescribed only if the expected benefit to the mother outweighs the potential risk to the fetus, and only in the minimum effective dose, the duration of treatment should be as short as possible. As in the case of the use of other NSAIDs, the preparation is contraindicated in the last 3 months of pregnancy (suppression of the contractility of the uterus and premature closure of the ductus arteriosus in the fetus are possible). Inhibition of prostaglandin synthesis can adversely affect pregnancy and / or embryo / fetal development. Data from epidemiological studies indicate an increased risk of developing heart defects and gastroschisis after using an inhibitor of prostaglandin synthesis in early pregnancy. The absolute risk of cardiovascular disease was increased from less than 1% to 1.5%. It is possible that the risk increases with the dose and duration of treatment. It was found that in animals the administration of an inhibitor of prostaglandin synthesis leads to an increase in pre- and post-implantation loss and mortality of the embryo / fetus.
In addition, in animals that received an inhibitor of prostaglandin synthesis during the period of organogenesis, an increased frequency of various malformations, including those of the cardiovascular system, was recorded. If diclofenac sodium is used by a woman who seeks to become pregnant, or in the first trimester of pregnancy, the dose should be as low as possible, and the duration of treatment should be as short as possible.
In the third trimester of pregnancy, when using inhibitors of prostaglandin synthesis, the following side effects may occur:
cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension);
impaired renal function, which can progress to renal failure with oligohydramnios.
In the mother and newborn, as well as at the end of pregnancy:
possible prolongation of bleeding time, antiplatelet effect, which can occur even at very low doses;
inhibition of uterine contractions, which leads to a delay or lengthening of labor.
Thus, diclofenac sodium is contraindicated in the third trimester of pregnancy.
Lactation. Like other NSAIDs, diclofenac passes into breast milk in small amounts. In this regard, diclofenac suppositories should not be used in women during breastfeeding in order to avoid unwanted effects on the infant.
Fertility in women. Like other NSAIDs, diclofenac sodium can negatively affect female fertility, therefore it is not recommended to prescribe it to women planning a pregnancy. In women who have problems with conception or are being examined for infertility, the feasibility of discontinuing diclofenac sodium should be considered.
The ability to influence the reaction rate when driving or working with other mechanisms. Patients who experience visual impairment, dizziness, drowsiness, central nervous system disorders, weakness or increased fatigue during diclofenac sodium therapy should not drive vehicles or operate machinery.

Interactions

The interactions observed with the use of diclofenac in the form of enteric tablets and / or in other dosage forms are indicated.
Lithium. Provided the simultaneous use of diclofenac can increase the concentration of lithium in the blood plasma. Monitoring of plasma lithium levels is recommended.
Digoxin. If used simultaneously, diclofenac can increase the concentration of digoxin in the blood plasma. Monitoring of plasma digoxin levels is recommended.
Diuretics and antihypertensive preparations. Like other NSAIDs, the simultaneous use of diclofenac with diuretics and antihypertensive agents (for example, β-adrenergic receptor blockers, ACE inhibitors) can lead to a decrease in their antihypertensive effect by inhibiting the synthesis of vasodilating prostaglandins. Thus, such a combination should be used with a reservation, and patients, especially the elderly, should be closely monitored for blood pressure. Patients should receive adequate hydration, and monitoring of renal function after initiation of concomitant therapy and on a regular basis after it is also recommended, especially with regard to diuretics and ACE inhibitors, due to an increased risk of nephrotoxicity.
Preparations that cause hyperkalemia. Concomitant treatment with potassium-sparing diuretics, cyclosporine, tacrolimus or trimethoprim may be associated with an increase in serum potassium levels, so patients should be monitored more frequently.
Anticoagulants and antiplatelet agents. Combined use can increase the risk of bleeding, so it is advisable to take precautions. Although clinical studies do not indicate the effect of diclofenac on the activity of anticoagulants, there are some data on an increased risk of bleeding in patients taking simultaneously diclofenac and anticoagulants. Therefore, to ensure that no changes in the dosage of anticoagulants are necessary, careful monitoring of such patients is recommended. Like other NSAIDs, high doses of diclofenac can temporarily suppress platelet aggregation.
Other NSAIDs, including selective COX-2 inhibitors and corticosteroids. The simultaneous use of diclofenac and other NSAIDs or corticosteroids may increase the risk of gastrointestinal bleeding or ulcers. The simultaneous use of two or more NSAIDs should be avoided.
Selective serotonin reuptake inhibitors. Concomitant use of NSAIDs and selective skerotonin reuptake inhibitors may increase the risk of gastrointestinal bleeding.
Antidiabetic preparations. Clinical studies have shown that diclofenac can be used together with oral hypoglycemic agents, which does not change their therapeutic effect. However, there are some reports of the development in such cases of both hypoglycemia and hyperglycemia, which necessitated a change in the dose of antidiabetic agents when using diclofenac. Therefore, it is recommended to control blood glucose levels in combination therapy.
Methotrexate. Diclofenac can suppress the renal tubular clearance of methotrexate, which leads to an increase in methotrexate levels. Caution should be exercised when prescribing NSAIDs, including diclofenac, less than 24 hours before using methotrexate, since in such cases the concentration of methotrexate in the blood may increase and its toxic effect may increase. Cases of severe toxicity have been reported when the interval between the use of methotrexate and NSAIDs, including diclofenac, was within 24 hours. This interaction is mediated due to the accumulation of methotrexate as a result of impaired renal excretion in the presence of NSAIDs.
Cyclosporine. The effect of diclofenac, like other NSAIDs, on the synthesis of prostaglandins in the kidneys may increase the nephrotoxicity of cyclosporin, therefore, diclofenac should be used in lower doses than in patients not using cyclosporin.
Tacrolimus. When using NSAIDs with tacrolimus, an increase in the risk of nephrotoxicity is possible, which may be mediated through the renal antiprostaglandin effects of NSAIDs and a calcineurin inhibitor.
Antibacterial quinolones. There are some data on the development of seizures in patients taking quinolone derivatives and NSAIDs at the same time. This can occur in patients with or without a history of epilepsy and seizures. Thus, caution should be exercised when deciding whether to use quinolones in patients already receiving NSAIDs.
Phenytoin. When using phenytoin simultaneously with diclofenac, it is recommended to monitor the concentration of phenytoin in the blood plasma in connection with the expected increase in the effect of phenytoin.
Colestipol and colestyramine. These preparations may delay or decrease the absorption of diclofenac. Therefore, it is recommended to prescribe diclofenac at least 1 hour before or 4–6 hours after the use of colestipol / colestyramine.
Cardiac glycosides. The simultaneous use of cardiac glycosides and NSAIDs in patients can increase heart failure, reduce the glomerular filtration rate and increase the level of cardiac glycosides in the blood plasma.
Mifepristone. NSAIDs should not be used within 8–12 days after using mifepristone, as NSAIDs may reduce the effect of mifepristone.
Potent inhibitors of CYP 2C9. Caution is recommended for the combined administration of diclofenac with potent inhibitors of CYP 2C9 (for example, with voriconazole), which can lead to a significant increase in plasma Cmax and exposure to diclofenac due to inhibition of diclofenac metabolism.

Overdose

Symptoms there is no typical clinical picture characteristic of diclofenac overdose. overdose can cause symptoms such as headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding, diarrhea, dizziness, disorientation, agitation, coma, drowsiness, tinnitus, and seizures. opn and liver damage are possible in case of severe intoxication.
Treatment. If necessary, treatment is symptomatic. Within 1 hour after using a potentially toxic amount of the preparation, the use of activated carbon should be considered. In addition, for adult patients, the possibility of gastric lavage within 1 hour after the use of a potentially toxic amount of the preparation should be considered. For frequent or prolonged convulsions, diazepam should be administered intravenously. Taking into account the clinical condition of the patient, other measures may be indicated.

Storage conditions

In its original packaging at a temperature not exceeding 25 ° C.

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