Pharmacological properties
Pharmacodynamics.
mechanism of action. Asacol tablets and suppositories contain mesalazine, which is a 5-pascal compound that has an anti-inflammatory effect. the mechanism of action has not yet been fully elucidated. mesalazine inhibits the migration of polymorphonuclear leukocytes, resulting in relief of inflammation in the intestine by limiting the migration of macrophages to inflamed areas. as a result, the synthesis of anti-inflammatory leukotrienes (ltb4 and 5-hete) in macrophages of the intestinal wall is inhibited. Recent studies have found that mesalazine activates ppar-γ receptors, which counteract the nuclear activation of inflammatory reactions in the intestine. Pharmacodynamic effects. During studies, it was found that mesalazine also inhibits the action of COX, and therefore the release of thromboxane B2 and prostaglandin E2, but the clinical significance of this effect has not yet been established. Mesalazine inhibits the synthesis of platelet activating factor. In addition, mesalazine is also an antioxidant: it reduces the synthesis of substances containing active oxygen and binds free radicals.
Data from a meta-analysis of 9 studies (3 cohort studies, 6 case-control studies) involving 1932 patients with ulcerative colitis (334 cases of colorectal cancer and 140 cases of dysplasia) confirmed a 49% reduction in the risk of developing colorectal cancer in those patients who regularly took mesalazine. This effect was absent in patients with ulcerative colitis who did not receive mesalazine or took it irregularly.
Clinical efficacy and safety. Induction of remission in patients with proctitis or proctosigmoiditis of mild to moderate severity.
Maintenance treatment in remission in patients with mild or moderate proctitis.
Clinical studies of Asacol suppositories included: one comparative bioavailability study, one small-scale tolerability study and four double-blind clinical studies. Bioavailability study data confirmed an acceptable profile compared with another licensed mesalazine suppository product. During tolerability studies and clinical studies, data were obtained confirming the safety and effectiveness of this drug. Evidence of clinical effectiveness consists of a statistically significant improvement in clinical, sigmoidoscopic and histological parameters of the disease.
When administered orally, mesalazine acts predominantly locally on the intestinal mucosa and on the submucosal tissue from the intestinal cavity. Therefore, it is important that mesalazine is available in areas of inflammation. Systemic bioavailability and plasma concentration are not essential for the therapeutic effect, but most likely act as a safety factor.
Pharmacokinetics. Absorption. Only part of the mesalazine contained in the suppository is absorbed and circulates in the systemic circulation. The mechanism of action of mesalazine is local and not systemic. After administration of one Asacol suppository at a dose of 500 mg in healthy volunteers, the average Cmax and Tmax values were 211 ng/ml and 2.0 hours for mesalazine and 443 ng/ml and 3.0 hours for N-acetyl-mesalazine, respectively. Mesalazine and N-acetyl-mesalazine bind to plasma proteins by 43 and 78%, respectively.
Distribution. Low concentrations of mesalazine and its metabolite N-acetyl have been found in human breast milk. The clinical significance of this phenomenon has not been determined.
Biotransformation. Mesalazine is metabolized in the intestinal mucosa and liver, resulting in the formation of the inactive metabolite N-acetyl-mesalazine.
Excretion of mesalazine occurs mainly in feces and urine in unchanged form and in the form of the N-acetyl metabolite. After using one Asacol suppository at a dose of 500 mg in healthy volunteers, the biological T½ of mesalazine and N-acetyl-mesalazine were 4.97 and 8.32 hours, respectively.
Asacol tablets, enteric-coated, are resistant to gastric juice. The polymer shell of the tablets ensures the release of the active substance, depending on the pH of the environment, in the lower ileum and large intestine, which are the main sites of inflammation. The composition of the tablets is selected in such a way as to minimize the absorption of mesalazine in the digestive tract. Absorption of mesalazine is highest in the proximal intestine and lower in the distal intestine. Absorption after oral administration is about 24%. Accordingly, 76% of the administered dose remains in the lower ileum and colon, as well as in the rectum, providing a local anti-inflammatory effect.
Linearity/nonlinearity. No special studies have been conducted.
Relationship between pharmacokinetic/pharmacodynamic data. No special studies have been conducted.
Asacol instructions for use
The drug Asacol is an anti-inflammatory drug used for intestinal diseases. The mechanism of the anti-inflammatory action of mesalazine (5-aminosalicylic acid) is unknown. Research results indicate that mesalazine suppresses the migration of polymorphonuclear leukocytes and inhibits the activity of lipoxygenase, as a result of which the synthesis of anti-inflammatory leukotrienes in macrophages of the intestinal wall is inhibited. There is also evidence of the effect of mesalazine on the concentration of prostaglandins in the intestinal mucosa. Mesalazine can bind free radicals. When administered orally, mesalazine acts predominantly locally on the intestinal mucosa and on the submucosal tissue from the intestinal cavity. Therefore, it is important that mesalazine is available in areas of inflammation. Systemic bioavailability and plasma concentration are not essential for the therapeutic effect, but are most likely a safety factor. Pharmacokinetics. Asacol tablets, enteric-coated, resistant to gastric juice. The polymer shell of the tablets ensures the release of the active substance, depending on the pH of the environment, in the lower ileum and large intestine, which are the main cells of inflammation. The composition of the tablets is selected in such a way as to minimize the absorption of mesalazine in the digestive tract. Absorption of mesalazine is highest in the proximal intestine and lower in the distal intestine. Absorption after oral administration is about 24%. Accordingly, 76% of the administered dose remains in the lower ileum and colon, as well as in the rectum, exhibiting local anti-inflammatory effects. Mesalazine is metabolized in the liver and intestinal mucosa to form the inactive metabolite N-acetyl-5-aminosalicylic acid. The binding of mesalazine and its metabolite to plasma proteins is 43% and 78%, respectively. Excretion occurs mainly in feces and urine, unchanged and as a metabolite. Indications for use: The drug Asacol is used in the treatment of mild to moderate ulcerative colitis; maintenance treatment in remission, Crohn's disease.
Directions for use: Adults Ulcerative colitis. When treating the disease in the acute phase, the dose is selected individually and is up to 4 g of mesalazine per day, divided into several doses. For maintenance treatment in remission, the recommended dose is up to 2 g of mesalazine once a day, selected individually. It is also possible to distribute the dose over several doses. Crohn's disease. When treating the disease in the acute phase and maintenance therapy, the dose is selected individually and is up to 4 g of mesalazine per day, divided into several doses. Elderly patients do not require dose adjustment unless renal function is impaired. Children over 6 years of age When treating ulcerative colitis and Crohn's disease in the acute stage, the dose is selected individually, starting from 30-50 mg/kg/day, divided into several doses. The maximum dose is 75 mg/kg/day, divided into several doses. The total daily dose should not exceed 4 g of mesalazine. During maintenance therapy, the dose is selected individually, starting from 15-30 mg/kg/day, divided into several doses. The total daily dose should not exceed 2 g of mesalazine. Typically, children weighing up to 40 kg are prescribed half the adult dose, and children weighing more than 40 kg are prescribed the full adult dose. Asacol tablets should be taken whole, without chewing, with a sufficient amount of liquid, 1:00 before meals. Both during exacerbation of the disease and during maintenance treatment in remission, Asacol tablets should be taken regularly and continuously to achieve the desired therapeutic effect. The duration of use is determined by the doctor. Typically, exacerbations of ulcerative colitis and Crohn's disease subside after 8-12 weeks.
Side effects: From the hematopoietic and lymphatic systems: infrequently - anemia, isolated cases - aplastic anemia, methemoglobinemia, agranulocytosis, granulocytopenia, pancytopenia, neutropenia, leukopenia, thrombocytopenia, eosinophilia, suppression of bone marrow function. From the nervous system: very often - headache; often - dizziness; infrequently - paresthesia, tinnitus, fatigue; very rarely - peripheral neuropathy. From the gastrointestinal tract: often - abdominal pain, nausea, vomiting, diarrhea, dyspepsia; infrequently - flatulence; isolated cases - worsening symptoms of colitis, pancolitis, acute pancreatitis. From the digestive system: isolated cases - hepatotoxicity (including hepatitis, including cholestatic, cholestasis, increased levels of liver enzymes and bilirubin, liver cirrhosis, liver failure). From the skin and subcutaneous tissues: often - rash, infrequently - urticaria, itching, skin rash; isolated cases - alopecia. From the musculoskeletal system: often - arthralgia; infrequently - myalgia. From the respiratory system: isolated cases - shortness of breath, eosinophilic pneumonia, interstitial pneumonia, chest pain, cough. From the immune system: very rarely - hypersensitivity reactions, such as allergic rashes, drug fever, bronchospasm, myocarditis, allergic alveolitis; isolated cases - lupus-like syndrome, accompanied by symptoms of pericarditis and pleuropericarditis. From the cardiovascular system: isolated cases - myocarditis, pericarditis. From the urinary system: isolated cases - nephrotic syndrome, interstitial nephritis, renal failure (reversible). From the reproductive system: very rarely - oligospermia (reversible). Laboratory indicators: isolated cases - increased creatinine levels in blood plasma, decreased creatinine clearance, increased concentrations of amylase, lipase, increased erythrocyte sedimentation rate, decreased body weight.
Contraindications: Contraindications to the use of the drug Asacol are: hypersensitivity to the active substance, to any other component of the drug or to salicylates; severe impairment of liver and kidney function (creatinine clearance <30 ml/min); peptic ulcer of the stomach and duodenum; hemorrhagic diathesis.
Pregnancy: There is insufficient data on the use of Asacol in pregnant women. Limited data indicate no adverse effects of mesalazine on pregnancy or the health of the fetus and/or newborn. However, anecdotal evidence suggests an increased risk of preterm birth and low birth weight. In one case, renal failure was reported in a newborn after prolonged use of high doses of mesalazine (2-4 g per day) during pregnancy. Thus, the drug can be prescribed during pregnancy only when the expected benefit to the mother outweighs the potential risk to the fetus. N-acetyl-5-aminosalicylic acid and, to a lesser extent, mesalazine are excreted into breast milk. To date, there is only limited experience with the use of the drug during breastfeeding. Hypersensitivity reactions such as diarrhea cannot be excluded. So, Asacol® tablets can be used during breastfeeding only when the potential benefits of use outweigh the possible risks. If a nursing infant develops diarrhea, breastfeeding should be stopped.
Interaction with other drugs: With simultaneous use of sulfasalazine and digoxin, the absorption of digoxin is reduced. There are no data on the interaction between mesalazine and digoxin. When mesalazine is used together with coumarin-type anticoagulants, the anticoagulant effect may be potentiated (increased risk of intestinal bleeding). There are isolated reports of changes in the international normalized index (INI) in the case of simultaneous use of warfarin with mesalazine. When used simultaneously with mesalazine, the immunosuppressive activity of azathioprine and 6-mercaptopurine may be enhanced (promoting the development of leukopenia). Patients should be closely monitored for signs of infectious diseases or immunosuppression. With combination therapy, it is possible to weaken the uricosuric effect of probenecid and sulfinpyrazone and reduce the diuretic effect of furosemide and spironolactone. It is possible that the side effects of glucocorticoids on the gastrointestinal tract may increase when used together with mesalazine. When used simultaneously with drugs that have a nephrotoxic effect, such as NSAIDs, azathioprine or methotrexate, the risk of adverse reactions from the kidneys may increase. When used with a sulfonylurea, the hypoglycemic effect may be enhanced. When used with rifampicin, the tuberculostatic effect may be weakened.
Overdose: So far, no cases of intoxication with Asacol have been reported. If necessary, infusion of electrolytes is carried out (forced diuresis).
Storage conditions. Store at a temperature not exceeding 25 ° C in the original packaging. Keep out of the reach of children.
Release form: Asakol - 400 mg tablets: 10 tablets in a blister, 10 (10 × 10) blisters in a cardboard box Asakol - 800 mg tablets: 10 tablets in a blister, 5 (10 * 5) or 6 ( 10 * 6) blisters in a cardboard box.
Composition: 1 tablet Asacol contains 400 mg or 800 m mesalazine. Excipients: lactose, sodium starch (type A), magnesium stearate, talc, povidone. Shell: methacrylate copolymer (type B), talc, dibutyl phthalate, iron oxide yellow (E 172), iron oxide red (E172), macrogol 6000.
Additionally: Asacol tablets are not prescribed to children under 6 years of age, because there is insufficient experience with the drug in this age group. The drug is not prescribed to patients with severe renal impairment. Mesalazine should be used with caution in patients with elevated plasma urea concentrations and proteinuria. It is recommended to monitor renal function for all patients before starting treatment with Asacol, as well as during treatment according to the regimen: 14 days after the start of therapy, then 2-3 more times at 4-week intervals. In the absence of signs of renal dysfunction, tests are repeated every six months, and after 5 years of therapy - once a year. Impaired renal function during treatment with mesalazine may be a manifestation of its nephrotoxic effect, so the drug should be discontinued immediately. Blood dyscrasia Cases of blood dyscrasia have been reported very rarely. Before starting and during treatment, blood tests should be carried out - it is recommended to carry out monitoring 14 days after the start of treatment, then 2-3 more times at 4-week intervals. If the test results are normal, routine checks are sufficient to be carried out every 3 months. If other additional symptoms develop, tests must be done urgently. It is especially important to monitor the blood picture if the patient develops the following symptoms during treatment: bleeding of unknown origin, hematoma, purpura, anemia, increased body temperature that persists for a long time, as well as complaints of sore throat. In such cases, treatment must be stopped immediately and the patient must be provided with the necessary medical care. Hypersensitivity to sulfasalazine If a patient has hypersensitivity to sulfasalazine, treatment is carried out only under constant medical supervision and is immediately stopped if signs of acute intolerance to the drug develop, such as convulsions, abdominal pain, fever, severe headache, skin rash. Impaired liver function It is possible to increase the level of liver enzymes during mesalazine therapy, so patients with liver damage should use Asacol with caution. Hypersensitivity reactions from the heart Asacol is not recommended for use if there is a history of hypersensitivity reactions to mesalazine from the heart (myo- or pericarditis). The drug is used with caution in patients with a history of allergic myocarditis or pericarditis, regardless of which drug caused such a reaction. Stomach or duodenal ulcer If the patient has a stomach or duodenal ulcer, the use of Asakol is contraindicated. Presence of tablets in stool There are isolated reports of the presence of whole tablets in stool. In the vast majority of cases, these are remnants of the tablet shell. After the tablet enters an environment with an acidity of 7.0, cracks form in its shell sufficient to release mesalazine. From this moment on, the process of release of the active substance becomes irreversible, regardless of the acidity of the intestinal environment. If tablets (tablet shells) are frequently detected in stool, the patient should consult a doctor. Patients with pulmonary diseases, in particular asthma, should be under medical supervision during treatment with mesalazine. In elderly patients, the drug is prescribed with caution only if normal renal function is maintained. The drug contains lactose, so it should not be prescribed to patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome. The ability to influence the reaction rate when driving vehicles or other mechanisms. There was no effect on the ability to drive a car or operate machinery, but the possibility of such an adverse reaction as dizziness should be taken into account.
Indications
Pills. nonspecific ulcerative colitis of mild to moderate severity; maintenance treatment in remission. Crohn's disease.
Suppositories. This medicine is intended for use in adults:
- for the treatment of proctitis and proctosigmoiditis of mild or moderate severity;
- in severe forms of total ulcerative colitis, which affects the rectum or rectosigmoid rectum, as an additional therapy to oral treatment.
Reviews
Asakol is in demand among patients suffering from Crohn's disease and ulcerative colitis. The advantages of the drug include proven effectiveness, minimal side effects, and the possibility of use from the age of two.
You can read reviews about the drug at the end of the article. If you have had experience using Asakol, share it with other site visitors.
Application
Pills
Adults. Ulcerative colitis. When treating the disease in the acute phase, the dose is selected individually and is up to 4 g of mesalazine per day, which is divided into several doses.
For maintenance treatment in remission, the recommended dose is up to 2 g of mesalazine once a day, selected individually. It is also possible to divide the dose into several doses.
Crohn's disease. When treating the disease in the acute phase and maintenance therapy, the dose is selected individually and is up to 4 g of mesalazine per day, which is divided into several doses.
Elderly patients do not require dose adjustment unless renal function is impaired.
Children over 6 years of age
In the treatment of ulcerative colitis and Crohn's disease in the acute stage, the dose is selected individually, starting from 30–50 mg/kg/day, and is divided into several doses. The maximum dose is 75 mg/kg/day, divided into several doses. The total daily dose should not exceed 4 g of mesalazine.
During maintenance therapy, the dose is selected individually, starting from 15–30 mg/kg/day, divided into several doses. The total daily dose should not exceed 2 g of mesalazine.
As a rule, children weighing 40 kg are prescribed half the adult dose, and children weighing 40 kg are prescribed the full dose.
The tablets should be taken whole, without chewing, with a sufficient amount of liquid, 1 hour before meals. Both during exacerbation of the disease and during maintenance treatment in remission, Asacol tablets should be taken regularly and continuously to achieve the desired therapeutic effect. The duration of use is determined by the doctor. Typically, an exacerbation of ulcerative colitis and Crohn's disease disappears after 8–12 weeks.
Suppositories. Suppositories are intended for rectal use only.
Dosage. Adults. Induction of remission: 1 suppository 3 times a day after defecation.
In severe forms of total ulcerative colitis, which affects the rectum or rectosigmoid rectum, as well as in the case of a slow response to oral therapy, 1 suppository in the morning and evening as an additional therapy to oral treatment.
Maintenance treatment in remission: the dosage depends on the severity of the disease and can be reduced if the patient’s condition improves.
Elderly patients can use the usual adult dose if they do not have impaired renal function. No studies have been conducted in elderly patients.
Release form and composition
Dosage forms:
- tablets, enteric-coated (10 pieces in a blister pack: 400 mg in a cardboard box of 10 packages, 800 mg in a cardboard box of 1 or 5 packages);
- rectal suppositories: No. 20 (10 pieces in a blister, 2 blisters in a cardboard box);
- rectal suspension (100 ml or 50 ml in plastic bottles, 7 bottles in a cardboard box).
1 tablet contains:
- active ingredient: mesalazine (5-ASA) – 0.4 g or 0.8 g;
- auxiliary components: sodium starch glyconate, lactose monohydrate, povidone, talc, magnesium stearate;
- shell composition: methacrylic acid, methacrylate copolymer, dibutyl phthalate, macrogol 6000, yellow and red iron oxide dye, talc.
1 suppository contains:
- active ingredient: mesalazine – 0.5 g;
- excipients: solid fat.
In 100 ml of suspension the content of the active substance mesalazine is 4 g.
Side effects
The clinical trial database included 246 patients who used Asacol, 500 mg suppositories. The dose range of mesalazine ranged from 1.0 to 1.5 g/day, the duration of treatment ranged from 4 weeks to 12 months.
Organ-specific side effects have been reported with oral or combined oral and rectal mesalazine therapy, particularly in the heart, lungs, liver, kidneys, pancreas, skin and subcutaneous tissues. Most of these side effects were noted during oral therapy with mesalazine and did not occur in patients receiving monotherapy with Asacol, 500 mg suppositories. However, such effects cannot be excluded when using rectal monotherapy with mesalazine.
Treatment should be discontinued immediately if the patient shows signs of acute intolerance to sulfasalazine, such as abdominal cramps, acute abdominal pain, fever, severe headache or rash.
Adverse effects reported in two double-blind clinical studies and one open-label clinical study, as well as in spontaneous reports or literature sources, the occurrence of which may be associated with the use of mesalazine or cannot be excluded, are presented below according to the class of organ system: often ( ≥1/100, 1/10), uncommon (≥1/1000, 1/100), rare (≥1/10,000, 1/1000), very rare (1/10,000).
From the blood and lymphatic system: very rarely - abnormalities in blood tests (aplastic anemia, agranulocytosis, pancytopenia, neutropenia, leukopenia, thrombocytopenia).
From the immune system: very rarely - hypersensitivity reactions, such as allergic rashes, drug fever, systemic lupus erythematosus, pancolitis.
From the nervous system: rarely - headache, dizziness; very rarely - peripheral neuropathy.
From the cardiovascular system: rarely - myocarditis, pericarditis.
From the respiratory system, chest organs and mediastinum: very rarely - allergic and fibrotic reactions from the lungs (including shortness of breath, cough, bronchospasm, alveolitis, pulmonary eosinophilia, pulmonary infiltration, pneumonitis).
From the digestive system: rarely - abdominal pain, diarrhea, flatulence, nausea, vomiting; very rarely - acute pancreatitis.
From the hepatobiliary system: very rarely - impaired liver function (increased levels of transaminases and cholestasis parameters), hepatitis, cholestatic hepatitis.
From the skin and subcutaneous tissues: very rarely - alopecia.
From the musculoskeletal system and connective tissue: bone damage; very rarely - myalgia, arthralgia.
From the urinary system: very rarely - impaired renal function, including acute and chronic interstitial nephritis and renal failure.
From the reproductive system and mammary glands: very rarely - oligospermia (reversible).
Systemic disorders: infrequently - no effect of the drug.
Description of individual side effects. Some (the number is not established) of the above side effects are probably related to the underlying disease (inflammatory bowel disease) and not to the use of the drug Asacol. This is especially true for disorders of the digestive system.
Patients should be carefully monitored to avoid blood dyscrasias, which may be caused by bone marrow suppression.
Concomitant use of myelosuppressive drugs such as azathioprine, 6-mercaptopurine or thioguanine may cause leukopenia.
When used simultaneously with NSAIDs, azathioprine or methotrexate, the risk of adverse reactions from the kidneys may increase.
Children. There is limited safety data on the use of Asacol suppositories in pediatric practice. It is expected that in children the same organs as in adults (heart, lungs, liver, kidneys, pancreas, skin and subcutaneous tissues) may be affected.
Other special patient groups. Patients with impaired renal function. Rare reports of acute renal dysfunction have been received. The possibility of mesalazine-induced nephrotoxicity should be considered in patients who develop renal dysfunction during treatment. This nephrotoxicity usually resolves when treatment is stopped.
Patients with impaired liver function. There are reports of increased liver enzyme levels and hepatitis. In some patients, these symptoms disappeared after discontinuation of mesalazine.
Elderly patients. For elderly patients, Asacol suppositories are prescribed with caution. Asacol can be prescribed only when the patient does not have impaired renal function.
special instructions
Renal dysfunction. To assess your kidney function, your doctor may order a urine test (using a dipstick) before and during treatment. This drug should be prescribed with caution to patients with elevated plasma creatinine concentrations and proteinuria. If renal dysfunction occurs during treatment with mesalazine, this may be a manifestation of the nephrotoxic effect of mesalazine.
It is recommended to monitor renal function in all patients before starting treatment with Asacol, as well as during therapy. It is also recommended that follow-up tests be performed 14 days after the start of treatment and then every 4 weeks for the next 12 weeks. With the help of monitoring, which is performed at short intervals after the start of therapy with Asacol, it is possible to identify rare acute renal reactions. In the absence of acute renal reactions, the intervals between tests can be increased to 3 months, and then to once a year for the next 5 years. If there are additional laboratory or clinical signs of renal failure, these tests should be performed immediately. If there are signs of renal dysfunction, the patient should immediately stop therapy with Asacol and immediately consult a doctor.
Blood dyscrasia. Cases of severe blood dyscrasia are very rare. If dyscrasia is suspected or reliably occurs (signs of bleeding of unknown origin, bruising, purpura, anemia, persistent fever or sore throat), the patient should immediately stop treatment with Asacol and immediately consult a doctor. Before starting and during therapy, it is recommended to conduct hematological studies (counting certain types of leukocytes), the date of which is determined by the doctor. It is recommended to carry out control tests 14 days after the start of treatment, and then 2-3 more times at 4-week intervals. If the test results are normal, such tests are sufficient to be carried out every 3 months. If additional symptoms are present, these tests should be performed immediately.
Liver dysfunction. Among patients taking medications containing mesalazine, cases of increased liver enzyme levels have been reported. Asacol should be prescribed with caution to patients with impaired liver function. It is recommended to carry out blood tests (liver function parameters such as ALT or AST) before and during treatment. The time for these tests is determined by the doctor. It is recommended to carry out control tests 14 days after the start of treatment, and then 2-3 more times at 4-week intervals. If the test results are normal, such tests are sufficient to be carried out every 3 months. If additional symptoms are present, these tests should be performed immediately.
Hypersensitivity reactions from the heart. Cases of cardiac hypersensitivity reactions caused by mesalazine (myocarditis or pericarditis) are very rare in patients taking Asacol. In case of cardiac hypersensitivity reactions caused by mesalazine, patients should not use Asacol a second time. The drug is used with caution in patients with a history of allergic myocarditis or pericarditis, regardless of which drug caused such a reaction.
Lung diseases. Patients who have lung diseases, in particular asthma, should be closely monitored during treatment with Asacol.
Hypersensitivity to sulfasalazine. If the patient has hypersensitivity to sulfasalazine, treatment is carried out only under constant medical supervision. Treatment should be stopped immediately if there are signs of acute intolerance to the drug, such as abdominal colic, acute abdominal pain, fever, severe headache or rash.
Ulcer of the stomach and duodenum. Based on theoretical knowledge, treatment should be started with caution in patients with gastric or duodenal ulcers.
Elderly patients. The drug should be prescribed with caution to elderly patients and only if normal renal function is maintained and there is no severe renal dysfunction.
Children. The experience of using the drug in the pediatric group is insignificant, and therefore there is a limited number of documents on the effectiveness of the drug when used in children.
Use during pregnancy and lactation. Pregnancy. There is insufficient data on the use of Asacol in pregnant women. Limited data (627 pregnant women) indicate no adverse effects of mesalazine on pregnancy or the health of the fetus and/or newborn. However, some data indicate an increased risk of preterm birth and decreased birth weight in women receiving mesalazine during pregnancy. To date, no relevant epidemiological data are available.
One case of renal failure has been reported in a newborn whose mother used high-dose mesalazine (2–4 g orally) for a long time during pregnancy.
Data from animal studies on oral administration of mesalazine do not indicate its direct or indirect adverse effects on pregnancy and childbirth, embryofetal or postnatal development.
Thus, Asacol can be prescribed during pregnancy only when the expected benefit to the mother outweighs the potential risk to the fetus.
Breast-feeding. N-acetyl-5-aminosalicylic acid and, to a lesser extent, mesalazine are excreted into breast milk. The clinical significance of this excretion has not been established. To date, there is only limited experience with the use of the drug during breastfeeding. Hypersensitivity reactions such as diarrhea cannot be excluded in newborns. So, Asacol can be used during breastfeeding only when the potential benefits of use outweigh the possible risks. If the infant develops diarrhea, breastfeeding should be stopped.
Reproductive function. The effect on reproductive function has not been established.
The ability to influence reaction speed when driving vehicles or working with other mechanisms. Asacol does not affect or may have an insignificant effect on the ability to drive vehicles and operate machinery. If dizziness occurs during treatment, you should refrain from driving.
Contraindications
- severe forms of renal and/or liver dysfunction;
- age up to 2 years;
- peptic ulcer of the stomach and duodenum;
- hemorrhagic diathesis;
- last 4 weeks of pregnancy;
- breast-feeding;
- individual intolerance to the components of the drug.
Asacol should be prescribed with caution in case of liver and/or kidney failure, glucose-6-phosphate dehydrogenase deficiency, and in the first trimester of pregnancy.
Suppositories should not be prescribed to patients with confirmed hypersensitivity to salicylates.
The use of the suspension is contraindicated in patients with hypersensitivity to methylparaben and propylparaben.
Interactions
No drug interaction studies have been conducted.
There is some evidence of the possibility of reducing the anticoagulant effect of warfarin when used simultaneously with mesalazine.
Under the influence of mesalazine, the immunosuppressive activity of azathioprine, 6-mercaptopurine or thioguanine may increase. As a result, a life-threatening infection may develop. Patients should be closely monitored for signs of infectious diseases or immunosuppression. Before starting combination therapy, hematological parameters should be monitored, especially white blood cell, platelet and lymphocyte counts, with periodic blood tests (weekly) during treatment. If the white blood cell count remains stable over 1 month, the test can be performed at 4-week intervals for the next 12 weeks, and then at 3-month intervals.
When used simultaneously with drugs that have nephrotoxic effects, such as NSAIDs, azathioprine or methotrexate, the risk of adverse reactions from the kidneys may increase. However, side effects that provide evidence of such an interaction have not been reported.
Drug interactions
With simultaneous use of Asakol:
- sulfonylurea derivatives – enhance the hypoglycemic effect;
- glucocorticosteroids - increase side effects that cause disruption of the mucous membrane of the gastrointestinal tract;
- anticoagulants - enhance their effect;
- cyanocobalamin – slows down its absorption;
- methotrexate – increases toxicity;
- sulfonamides, spironolactone, rifampicin, furosemide - weaken their therapeutic effect;
- blockers of tubular secretion (uricosurics) – increase their effectiveness.
Note!
Description of the drug Asacol table. p/o 800 mg No. 60 on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
