Salofalk granules of prolonged action 1000 mg N50
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Active ingredients
Mesalazine
Release form
Granules
Composition
1 sachet contains: Active substance: 500 mg of mesalazine. Auxiliary substances: microcrystalline cellulose 400 mg, hypromellose 36 mg, silica, anhydrous colloidal anhydrous 0.5 mg, NE4D eudrageen (dry matter 40% dispersion of methyl methacrylate copolymer and ethacrylate (2: 1) and 2% nonoxynol) 90 mg, magnesium stearate 15.5 mg, simethicone emulsion 33% - 1 mg (simethicone 92%, methylcellulose 7.7%, sorbic acid 0.3%). The composition of the inner shell: hypromellose - 4 mg, a copolymer of methacrylic acid and methyl methacrylate (1: 1) ( Eudragit L100) - 150 mg, triethyl citrate - 15 mg, talc - 40 m g, magnesium stearate - 10 mg, titanium dioxide - 25 mg. Composition of the outer shell: carmellose sodium - 30 mg, titanium dioxide - 10 mg, aspartame - 2 mg, anhydrous citric acid - 6 mg, vanilla flavoring - 4 mg, talc 11 mg, Povidone K25 - 10 mg.
Pharmacological effect
The drug has a local anti-inflammatory effect. The action of the drug is due to inhibition of neutrophilic lipoxygenase and the synthesis of prostaglandins and leukotrienes. Mesalazine slows the migration, degranulation, phagocytosis of neutrophils, as well as the secretion of immunoglobulins by lymphocytes. It has an antioxidant effect (due to the ability to bind to free oxygen radicals and destroy them). Mesalazine can also trap radicals formed from reactive oxygen compounds. The results obtained in in vitro studies indicate a possible role for lipoxygenase inhibition. The effect on prostaglandins in the intestinal mucosa is also shown. On oral administration, mesalazine exerts a predominantly local effect in the intestinal mucosa and the submucosal layer, acting from the intestinal lumen. Therefore, it is important that mesalazine is available in the area of inflammation. The ratio of systemic bioavailability and plasma concentration of mesalazine is not significant in terms of therapeutic efficacy, but rather is a factor affecting safety. The release of the active substance in the right place is assisted by the fact that the Salofalk granules are resistant to gastric juice and are pH-dependent (due to the coating in the form of Eudragit L) and delayed (due to the matrix structure of the granules) release of mesalazine.
Pharmacokinetics
Absorption Mesalazine occurs in the terminal section of the small and large intestine.Tablets begin to dissolve in the small intestine after 110-170 minutes and completely dissolve after 165-225 minutes after administration. The rate of dissolution is not affected by changes in the pH of the medium caused by the ingestion of food or other drugs. The release of mesalazine from the granules begins with a slowdown of 2-3 hours, Cmax in plasma is reached in about 4-5 hours. The systemic bioavailability of mesalazine after oral administration is approximately 15- 25%. Food intake slows absorption for 1-2 hours, but does not change the speed and extent of absorption. Food intake can slow the transit of the drug for 1-2 hours, while increasing Tlag values (time gap after which the content of mesalazine is first determined in the blood) and Tmax, however, due to the small size of the granules, this does not change the speed and extent of absorption. Food intake causes a slight increase in Cmax and AUC values. The total amount of mesalazine and N-acetyl-5-ASA excreted by the kidneys for 24 hours is equivalent to about 25-32%, respectively prescribed dose of granules and that Salofalk. Approximately 30% of this amount is absorbed in the ileocecal zone, and approximately 90% of the whole in the ileocecal zone and the ascending colon. Thus, about 80-90% of the prescribed dose 5-ASA is present in the descending colon, sigmoid and rectum, where their absorption rate is low. Distribution Due to the size of the granules (about 1 mm), the transit from the stomach to the small intestine occurs quickly. A combined pharmacological scintigraphic and pharmacokinetic study showed that the drug reaches the ileocecal department in about 3 hours and the ascending colon in approximately 4 hours. The total transit time through the large intestine is about 20 hours. Approximately 80% of the accepted oral dose reaches a large, sigmoid and rectum. Metabolism Mesalazine is metabolized both by the presystemic route in the intestinal mucosa and systemically in the liver, turning into pharmacologically inactive N-acetyl-5-am nosalicylic acid (N-Ats-5-ASA). The nature of acetylation does not depend on the acetylating phenotype of the patient. To a small extent, acetylation can be carried out by the action of bacterial microflora of the colon. Communication with plasma proteins mesalazine and N-Ac-5-ASA is 43% and 78%, respectively. 0.1% of the dose penetrates into the mother's milk (as a metabolite). Excretion When taking mesalazine at a dose of 500 mg 3 times / day, the total elimination of mesalazine by the kidneys and N-Ac-5-ASA under conditions of saturating concentration was about 25%.The excretion of the non-metabolized part of mesalazine was less than 1% of the oral dose. T1 / 2 in this study was equal to 4.4 hours. Pharmacokinetics in special clinical situations. With a single oral administration of Salofalk granules at a dose of 20 mg / kg, 13 children with active inflammatory bowel disease (age from 5.9 to 15.8 years) had a pharmacokinetics of systemic exposure of the drug consistent with that adults. Salofalk was safe and well tolerated. Data on the pharmacokinetics of Salofalk in the elderly in its use, both in pills and in granules are not available.
Indications
Ulcerative colitis, Crohn's disease. Unapproved indications: diverticular disease (diverticulosis and colon diverticulitis), chemoprophylaxis of colorectal cancer.
Contraindications
blood diseases; - peptic ulcer of the stomach and duodenum; - hemorrhagic diathesis (with a tendency to bleeding); - severe renal failure; - severe hepatic insufficiency; - glucose-6-phosphate dehydrogenase deficiency; - phenylketonuria (for granules); 3 years (for pills); - children up to 6 years (for granules); - hypersensitivity to the components of the drug and other derivatives of salicylic acid.
Precautionary measures
Caution should be given Salofalk with mild to moderate renal / hepatic failure, lung diseases (especially bronchial asthma), during pregnancy (I term).
Dosage and administration
The dosage regimen for the treatment of acute ulcerative colitis depends on the clinical need and in each case is individual. Assign 1 sachet of 500-1000 mg of mesalazine 3 times / day or 3 sachets 1 time / day (corresponding to 1.5-3.0 g of mesalazine per day). To maintain remission of ulcerative colitis, 500 mg (1 pack) of mesalazine is prescribed 3 times / day or 3 sachets of 500 mg 1 time / day (corresponding to 1.5 g of mesalazine per day). For children over 6 years old and adolescents with exacerbation of the disease, depending on its severity, mesalazine is prescribed at a dose of 30-50 mg / kg body weight / day with distribution of daily dose in 3 doses or 1 reception. To maintain remission, mesalazine is prescribed in a dose of 15-30 mg / kt body weight / day, while the daily dose can be divided into 2 doses.Children with a body weight of up to 40 kg are usually recommended to give a half dose of adults, children weighing more than 40 kg should be given a dose of adults. Salofalk granules should not be chewed. The prescribed dose of Salofalk in granules should be taken in the morning, at lunchtime and in the evening or the entire dose once in the morning. Salofalk granules should be put on the tongue and swallowed without chewing, drinking plenty of fluids. As with the treatment of exacerbation of the inflammatory process, and with prolonged use to maintain remission, the granules should be taken regularly and consistently, which allows to achieve the desired therapeutic effect. Exacerbation of ulcerative colitis usually subsides after 8-12 weeks, after which the dose of mesalazine in most patients can be reduced to 1.5 g / day.
Side effects
Reactions associated with hypersensitivity: skin rash, itching, erythema, fever, bronchospasm, pericarditis, myocarditis, acute pancreatitis, interstitial nephritis, nephrotic syndrome. Individual cases of allergic alveolitis and pancolitis were observed. Under certain conditions, mesalazine and drugs with a similar chemical structure can lead to the development of a syndrome similar to that of systemic lupus erythematosus. On the digestive system: diarrhea, nausea, abdominal pain, flatulence, loss of appetite, vomiting, increased levels of liver enzymes in blood, hepatitis. From the side of the central nervous system: headache, depression, dizziness, sleep disturbances, malaise, paresthesia, convulsions, tremor, tinnitus. From the side of the cardiovascular system: rarely - tachycardia, arterial hypertension or hypotension, pain behind the sternum, shortness of breath. From the musculoskeletal system: myalgia, arthralgia. From the hemopoietic system: in some cases - anemia, leukopenia, agranulocytosis, thrombocytopenia. From the blood coagulation system: in some cases - hypoprothrombinemia. side of the urinary system: in some cases - proteinuria, hematuria, crystalluria, oliguria, anuria.Other: in some cases - reduced production of tears, alopecia, reversible decrease in sperm motility. fine structure of the active ingredient can not exclude the possibility of increasing the level metgemoglobina.Pri occurrence of acute symptoms of intolerance to treatment should be stopped immediately.
Overdose
Symptoms: nausea, vomiting, gastralgia, weakness, drowsiness. Treatment: gastric lavage, the appointment of laxatives, symptomatic therapy. In cases of overdose, if necessary, an infusion of electrolyte solutions (forced diuresis) is performed.
Interaction with other drugs
With simultaneous use of Salofalk causes increased action of indirect anticoagulants (increased risk of gastrointestinal bleeding). With simultaneous use of GCS with Salofalk, it is possible to increase unwanted reactions from the gastric mucosa. With simultaneous use of Salofalk increases the toxicity of methotrexate. Salofalk may decrease uric acid excretion. When used simultaneously, Salofalk reduces diuretic the cue effect of spironolactone and furosemide. When used simultaneously with Salofalk, the tuberculostatic effect of rifampicin can be weakened. If used simultaneously, Salofalk enhances the hypoglycemic effect of sulfonylurea derivatives. caused by the metabolism of bacteria. In patients who simultaneously receive treatment with azathiop otherwise or 6-mercaptopurine should be aware of the possible strengthening of myelosuppressive effect of azathioprine and 6-mercaptopurine.
special instructions
Before and during treatment, it is necessary to determine the parameters of the functional state of the liver (such as ALT activity or ACT) and monitor urine tests (by immersing test strips). Monitoring is usually recommended 14 days after the start of treatment, then another 2-3 times with an interval of 4 weeks. If the test results are normal, control tests should be carried out every 3 months. If the appearance of additional symptoms is noted, control studies should be carried out immediately. Caution should be taken in patients with impaired liver function. Appointment of Salofalk is not recommended for patients with severe impaired renal function.If impaired renal function has developed during treatment, one should think about the nephrotoxic effect of mesalazine. When administering Salofalk to patients with lung diseases, in particular, bronchial asthma, careful monitoring should be carried out during treatment. containing sulfasalazine, should be closely monitored in the initial period of treatment Salofalk. If during the treatment with Salofalk, acute intolerance reactions occur, such as convulsions, acute abdominal pain, fever, severe headache and rash, the drug should be stopped immediately. in doses equivalent to the following amount of phenylalanine: 0.56 mg (Salofalk granules 500 mg), 1.12 mg (Salofalk granules 1 g). Patients who are slow acetylators have an increased risk of developing side effects. x effects. There may be staining of urine and tears in yellow-orange color, staining of soft contact lenses. If you miss a few doses, then, without stopping the treatment, the patient should see a doctor. Use in pediatricsSalofalk in granules should not be administered to children under 6 years , because the experience of using the drug in patients of this age group is very limited. Impact on the ability to drive motor vehicles and control mechanisms. Care should be taken when driving and potentially hazardous activities that require increased concentration of attention and quickness of the psychomotor reaction.