Mesalazine is a drug for the basic treatment of ulcerative colitis, a mild form of Crohn's disease in some localizations, as well as a number of other diseases.
According to its chemical structure,
mesalazine is 5-aminosalicylic acid (5-ASA) , which has a local anti-inflammatory effect.
The drug affects the synthesis of pro-inflammatory prostaglandins and leukotrienes, slows down the migration, degranulation and phagocytosis of neutrophils, reducing the severity of inflammatory processes. Mesalazine has an antioxidant effect due to the binding of its molecules to free radicals. The drug is taken orally (orally) in the form of tablets, MMX tablets or granules, used in the form of an aerosol (rectal foam), suspension (microenemas) and suppositories. The anti-inflammatory effect of mesalazine is predominantly local (on the intestinal mucosa), so the concentration of the drug in contact with the intestinal wall and the time of this contact are important. Concentrations of the drug in the blood are usually minimal and do not affect its effectiveness.
The active ingredient in all these drugs is the same, but mesalazine is released in the intestinal lumen in different ways. This depends on the form of the drug, its shell and structure.
Below is a description of the main mesalazines registered in the Russian Federation.
Brief characteristics of mesalazine preparations
"Salofalk"
Production (Germany). In Russia it is presented in the form of tablets, granules, rectal foam, rectal suspension and suppositories.
A. Salofalk tablets
Salofalk tablets are coated with a protective enteric coating of Eudragit L, which provides pH-controlled release of mesalazine. The shell does not dissolve in gastric juice. But when it enters the intestine, where the pH level is ≥6.0, it is destroyed, and the active substance of the drug ends up in the intestinal lumen. In the terminal ileum, 15-30% of the drug is released, in the colon - 60-75%.
The release of mesalazine from Salofalk tablets begins in the terminal ileum 110-170 minutes after taking the drug, and after 4-5 hours, dissolution is completed in the descending colon. The release of mesalazine is not affected by changes in pH due to other medications or food intake.
About 10% of mesalazine is absorbed into the bloodstream, where it is quickly transformed into an inactive form and excreted from the body by the kidneys.
Forms of release and method of application
Salofalk tablets are available in doses of 250 mg and 500 mg. Take them in the morning, afternoon and evening 1 hour before meals. The tablets are swallowed without chewing and washed down with a sufficient amount of liquid.
b. Granules "Salofalk"
Salofalk granules are a two-component dosage form that combines pH-controlled release of mesalazine with long-term continuous release of the drug from a core based on an original polymer matrix. The enteric protective coating provides a pH-dependent release (at pH values ≥6.0) of the active substance, starting in the terminal ileum and continuing in the underlying intestine. The loss of the active substance to the ileum is minimal. The polymer matrix core ensures long-term continuous release of the active substance throughout the colon, right down to the rectum.
A large number of granules (3 g of Salofalk contain about 3500 granules) ensures a uniform and effective distribution of the active substance and, due to the very large surface area, maintains the effect even with diarrhea.
The drug reaches the ileocecal region after about 3 hours, and the ascending colon after 4 hours (faster than when taking Salofalk tablets). Approximately 80% of the oral dose reaches the colon, sigmoid and rectum. The amount of the drug that enters the blood and is excreted in the urine as a metabolite is less than when using Salofalk tablets.
Forms of release and method of application
Salofalk granules are available in doses of 500 mg and 1000 mg. The granules should be placed on the tongue and swallowed without chewing, with plenty of liquid. The prescribed dose of Salofalk in granules should be taken once a day, regardless of food intake.
V. Rectal foam (aerosol) “Salofalk”
Rectal foam (aerosol) “Salofalk” is a dosage form for rectal use, which allows for optimal contact of the active substance with the surface of the intestinal mucosa. Highly effective for active ulcerative colitis localized in the rectum, as well as for left-sided and widespread ulcerative colitis as part of combination therapy. When foam is administered through the rectum, mesalazine acts directly on the mucous membrane of the final sections of the colon. Due to the high adhesive ability of Salofalk foam, the drug can “stick” to the mucous membrane, which ensures long-term contact of mesalazine with the inflamed area of the intestine. And the duration of contact (exposure) increases the effectiveness of the drug.
Release form and method of application
Salofalk foam is produced in an aerosol can containing 14 applications of the drug, 1 g each, the set is equipped with 14 disposable soft applicators for insertion into the rectum. It is recommended to administer the drug before bedtime (preferably after a bowel movement), however, if there are frequent nighttime bowel movements, the attending physician may prescribe a different time.
Excerpt from the instructions for use of Salofalk rectal foam:
- At the time of administration, the drug should be at room temperature (20–25 °C)
- Place the applicator firmly on the cylinder head
- Shake the can for 20 seconds
- When using for the first time, remove the protective tab from the base of the dosing head.
- Turn the cap so that the semicircular cutout on the safety ring is in line with the nozzle. Place your index finger on the cap and turn the can upside down.
- Insert the applicator into the rectum as deeply as possible. It is best to place your foot on a chair or stool. In order to administer the first part of the dose of the drug, press the cap all the way and slowly release it. To administer the second dose of the drug, press the cap again and release slowly. Wait 10–15 seconds, then slowly remove the applicator from the rectum
- After introducing the foam, remove the applicator and throw it away in a plastic bag. For each new dose of the drug, a new applicator should be used.
- After the procedure, wash your hands. Try not to have a bowel movement until the next morning.
g. Rectal suspension "Salofalk" (microenema)
Rectal suspension "Salofalk" (microenema) is a ready-made suspension in a bottle with disposable applicators. The drug reaches the left (splenic) corner of the colon. In some patients, the drug reaches the transverse colon and even the ascending colon. When mesalazine is used in microenemas, low absorption of the drug is observed.
Forms of release and method of application
Microclysters "Salofalk" are available in doses of 2 g/30 ml and 4 g/60 ml. Smaller volume microenemas are suitable for patients who find it difficult to hold large volumes of suspension. The entire volume of microenemas is injected into the rectum at night (preferably after bowel movements), however, if there are frequent nighttime bowel movements, the attending physician may prescribe a different time.
d. Rectal suppositories "Salofalk"
Rectal suppositories "Salofalk" are suppositories intended for insertion into the rectum. They are used to achieve the highest concentration of mesalazine in this section of the intestine.
Forms of release and method of application
Rectal suppositories "Salofalk" are available in doses of 250 mg, 500 mg and 1000 mg (this dose is not registered in Russia). Suppositories are inserted into the rectum 1-2 times a day as prescribed by a doctor (preferably after bowel movements). It is usually recommended to administer the suppository at night, however, depending on the prescribed frequency of administration, combination with other local forms of therapy, as well as for nighttime bowel movements, the attending physician may prescribe a different time.
Due to the small size of the granules (about 1 mm), which facilitates unhindered passage through the stomach, they can be taken regardless of meals.
"Pentasa"
Production (Denmark). Presented in the Russian Federation in the form of tablets, granules and suppositories.
A. Pentasa tablets
Pentas tablets are enteric-coated. After administration, it disintegrates into microgranules coated with ethylcellulose. Microgranules act as independent forms of the drug with a slow release. This provides a therapeutic effect throughout the duodenum to the rectum, regardless of pH. The microgranules reach the duodenum within an hour after taking the tablet, regardless of food intake. The average passage time for the drug through the small intestine is 3-4 hours. About 30-50% of the dose taken is absorbed in the small intestine.
Release form and method of application
Pentasa tablets are available in doses of 500 mg. It is recommended to take after meals without chewing in 2-3 doses. The tablet can be split into several pieces or dissolved in water to make it easier to swallow.
b. Pentas granules
Pentas granules are microgranules coated with ethylcellulose. They act as independent forms of the drug with a slow release, which provides a therapeutic effect throughout the entire length from the duodenum to the rectum, regardless of pH. Microgranules reach the duodenum within an hour, regardless of food intake. The passage time of the drug through the small intestine is on average 3-4 hours.
Release form and method of application
Pentasa granules are available in doses of 1000 mg and 2000 mg. It is recommended to take the granules after meals without chewing. Pour the contents of one sachet onto your tongue and wash it down with water or juice.
V. Rectal suppositories "Pentas"
Pentasa rectal suppositories are suppositories intended for insertion into the rectum. They are used to achieve the highest concentration of mesalazine in this section of the intestine.
Release form and method of application
Rectal suppositories "Pentasa" are available in doses of 1000 mg. Externally they look like oblong tablets. Suppositories are inserted into the rectum 1-2 times a day as prescribed by a doctor, preferably after bowel movements. It is usually recommended to administer the suppository at night, however, depending on the prescribed frequency of administration, combination with other local forms of therapy, as well as in case of frequent nighttime bowel movements, the attending physician may prescribe a different time.
The drug can be moistened with water for easier administration.
"Mezavant"
Production (USA). Presented in the Russian Federation in the form of MMX tablets. MMX Mezavant tablets have a core containing mesalazine in a multicomponent matrix. The core is surrounded by a shell of methacrylic acid copolymers of types A and B. Mesalazine is released in the intestine only when the pH reaches >7. Scintigraphy studies have shown that after a single dose of 1.2 g of the drug on an empty stomach to healthy volunteers, mesalazine quickly and unchanged passes through the upper gastrointestinal tract. Traces of 14C-labeled mesalazine were detected throughout the colon. Complete disintegration of the tablet and release of mesalazine was observed after approximately 17.4 hours. After a single dose of 2.4 or 4.8 g to healthy volunteers for 14 days, mesalazine absorption was 21–22% of the dose taken.
Release form and method of application
MMX Mezavant tablets are available in a dose of 1.2 g (1200 mg). The entire recommended dose is taken 1 time per day with meals. The tablets should not be crushed or chewed and should be swallowed whole.
"Mesakol"
Manufacturing (India). Presented in the Russian Federation in the form of tablets. Mesacol tablets are coated with an enteric coating of Eudragit-L and Eudragit-S, which dissolves at pH>7. The bulk of mesalazine (60-79%) is released in the colon.
Forms of release and method of application
Mesacol tablets are available in a dose of 400 mg. The recommended dose of the drug is taken in 2-3 doses. The tablets should be taken before meals without chewing.
"Asakol"
Production (Switzerland). Presented in the Russian Federation in the form of tablets. Asakol tablets are coated with an enteric coating of Eudragit-S. Drug release begins in the colon at pH>7.
Forms of release and method of application
Asakol tablets are available in doses of 400 mg and 800 mg. The recommended dose of the drug is taken in 2-3 doses. The tablets should be taken before meals without chewing.
"Kansalazin"
Manufactured by Canonpharma Production CJSC (Russia). Presented in the Russian Federation in the form of tablets. The results of a study of the bioequivalence of the drug Cansalazine to the original drug mesalazine (manufactured by Danish) confirmed the full correspondence of the dynamics and concentration of mesalazine in the intestines when taking Kansalazine and the original drug. Thus, the manufacturer considers Kansalazine tablets to be a drug that has the same effect as Pentasa tablets.
Release form and method of application
Kansalazine tablets are available in doses of 500 mg. The recommended dose of the drug is taken in 2-3 doses. It is recommended to take the tablets after meals without chewing.
Instructions for use SALOFALK® tablets
General properties of mesalazine
Suction
Mesalazine is absorbed most efficiently in the proximal intestine and least efficiently in the distal intestine.
Distribution
Plasma protein binding of mesalazine and N-Ac-5-ASA is 43% and 78%, respectively. Approximately 1% of an oral dose of mesalazine is excreted in breast milk, mainly as N-Ac-5-ASA.
Metabolism
Mesalazine undergoes first-pass metabolism to form inactive N-acetyl-5-aminosalicylic acid (N-Ac-5-ASA), both in the intestinal mucosa and in the liver. The pattern of acetylation is independent of the patient's acetylation phenotype. Part of mesalazine is also acetylated due to the action of bacterial microflora of the large intestine.
Removal
Mesalazine and its metabolite N-Ac-5-ASA are excreted in excrement (most of it), kidneys (the amount varies from 20% to 50% depending on the route of administration, dosage form and mechanism of release of the active substance) and bile (minor part) . It is excreted by the kidneys mainly in the form of N-Ac-5-ASA.
Specific features of the drug Salofalk® in the form of tablets 250 mg
Distribution
A combined pharmacoscintigraphic/pharmacokinetic study demonstrated that when taken with food (breakfast test), enteric film-coated tablets dissolve in approximately 3-4 hours in the ileum. The average time for evacuation of gastric contents was approximately 3 hours. After approximately 7 hours, the tablets reached the colon. In a subsequent study in volunteers, the evacuation time from the duodenum to the ileum was approximately 3 hours, with the highest concentration of 5-ASA in the intestinal lumen observed 7-8 hours after co-administration of the tablets with a test breakfast. Approximately 75% of the mesalazine dose reaches the large intestine unmetabolized.
Suction
The release of mesalazine from Salofalk® 250 mg enteric film-coated tablets begins after a lag phase of approximately 3-4 hours. The highest plasma concentration is achieved after approximately 5 hours (in the ileum) and with the administration of mesalazine at a dose of 500 mg 3 times/day (3×2 tablets. Salofalk® 250 mg) under the condition of steady-state equilibrium is 2.1±1.7 µg/ml for mesalazine and 2.8±1.7 µg/ml for its metabolite, N-A4-5-ACK.
Removal
During long-term treatment with Salofalk® 250 mg enteric film-coated tablets at a daily dose of 500 mg mesalazine 3 times a day (assuming steady state), the total rate of renal excretion of mesalazine and N-A4-5-ACK was approximately 55% (value obtained within 24 hours after the last dose). The proportion of unmetabolized mesalazine was approximately 5%. T1/2 is 0.7-2.4 hours (on average 1.4±0.6 hours) when using mesalazine at a dose of 500 mg 3 times a day.
Specific features of the drug Salofalk® in the form of tablets 500 mg
Distribution
A combined pharmacoscintigraphic/pharmacokinetic study demonstrated that when taken with food (breakfast test), enteric film-coated tablets dissolve in approximately 3-4 hours in the ileum. After approximately 4-5 hours, the tablets reach the colon. The total transit time in the large intestine is about 17 hours.
Suction
The release of mesalazine from Salofalk® 500 mg enteric film-coated tablets begins after a lag phase of approximately 3-4 hours. The highest plasma concentration is achieved after approximately 5 hours (in the ileum) and with the administration of mesalazine at a dose of 500 mg 3 times/day, subject to steady state equilibrium, is 3±1.6 µg/ml for mesalazine and 3.4±1.6 µg/ml for its metabolite, N-Ac-5-ASA.
Removal
The total rate of renal excretion of mesalazine and N-Ac-5-ASA within 24 hours with repeated doses (1 tablet 500 mg 3 times a day for 2 days; and 1 tablet on the third control day) was approximately 60% ( value obtained within 24 hours after the last dose). The proportion of unmetabolized mesalazine was approximately 10%.
Indications for the use of mesalazine
Many patients with ulcerative colitis and Crohn's disease are familiar with this drug under various commercial names (Salofalk, Pentasa, Mezavant, Mesacol, Asacol, etc.).
Most often, these drugs are prescribed for inflammatory bowel diseases (IBD), primarily ulcerative colitis .
Mesalazine and ulcerative colitis
According to the Russian and European recommendations of 2021, mesalazine is a drug for basic therapy of ulcerative colitis of any localization. Clinical studies have shown that all commercial forms of mesalazine are equally effective in the treatment of ulcerative colitis.
Then what is their difference? Why do some patients benefit from pH-dependent release mesalazine granules, others from slow-release tablets, and some do not get better at all?
Undoubtedly, there are differences in the drugs. In the section with general characteristics of mesalazines, the mechanisms of release of the active substance from tablets and granules are discussed in sufficient detail. Sometimes the release and uniform distribution of the drug throughout the intestine is affected by the acidity (i.e., the same pH) in the intestine. In other cases, the release of mesalazine is independent of pH but is dependent on intestinal transit time. In pathological conditions, pH values can vary greatly and differ from the norm. Thus, according to the results of one study (on a limited group of healthy individuals), pH values did not reach 7 in any part of the gastrointestinal tract in 25% of cases. In 90% of cases (again, not in all study participants), the pH exceeded 6. That is, there is a possibility that in a number of patients with ulcerative colitis and Crohn's disease, mesalazines with a pH-dependent release system (Salofalk, Mesacol, Asacol, Mezavant) may be less effective than expected. When using pH-independent mesalazines (Pentasa, Canasalazine), researchers note that most of the drug begins to be released in the small intestine, which means there is a possibility that the concentration of mesalazine in the colon will be less than necessary to achieve an effect. In some cases, this probability can be reduced by increasing the dose of the drug.
The dose of mesalazine prescribed is another factor in the success or failure of IBD treatment. An insufficient dose of the drug leads to a poor response to therapy.
It is important to correctly assess the location of intestinal damage. It is this (proctitis, left-sided or widespread/total ulcerative colitis) that determines the choice of the dosage form of mesalazine (tablets, granules, foam, microenemas or suppositories). For example, suppositories can be used in first-line therapy for ulcerative colitis affecting the rectum.
Finally, mesalamines may not have the expected benefit due to high disease activity. In this case, they are combined with other drugs (including hormonal agents and immunosuppressants).
Summarizing the above, we can conclude:
Good knowledge of the mechanism of action of drugs and the capabilities of various dosage forms allows a gastroenterologist to select an individual treatment regimen for the patient.
Mesalazine and Crohn's disease
A few words about Crohn's disease and the effectiveness of mesalazine in its treatment. Until 2021, when the update of the European consensus on the diagnosis and treatment of Crohn's disease (3rd revision) was published, mesalazine was recommended for mild forms of the disease affecting the large intestine (Crohn's colitis) and small intestine (Crohn's ileitis). In the first case, the use of large doses of mesalazine (3-4 g per day) with a pH-dependent release system was recommended, in the second - mesalazine with a pH independent release system (Pentasa) at a dose of 4 g per day. Changes to the treatment strategy were made after publication of the consensus. This also influenced Russian recommendations related to the diagnosis and treatment of Crohn's disease. Mesalazine is found to be ineffective compared to placebo. However, clinical practice shows that for patients with mild disease, taking mesalazine helps, up to the healing of the mucous membrane.
Mesalazine can also be prescribed for chronic colitis of unknown or unspecified origin, radiation (radiation) colitis, diverticular disease of the intestine, etc.
Salofalk suppositories (Salofalk suppositories) 500 mg No. 30 - Instructions
Release form
Rectal suppositories 500 mg, 30 pieces per package.
Compound
Active substance: Mesalazine 500 mg. Additional substances: solid fat 1680 mg, cetyl alcohol 18 mg, sodium docusate 2 mg.
Pharmacological properties
Pharmacodynamics. The mechanism of anti-inflammatory action is unknown. In vitro results suggest that lipoxygenase inhibition may have a role. An effect on the concentration of prostaglandins in the intestinal mucosa has also been demonstrated. Mesalazine (5-aminosalicylic acid/5-ASA) may also act as a reactive oxygen radical scavenger. Mesalazine, when administered rectally, acts predominantly locally on the intestinal mucosa and on the submucosal tissue of the intestinal lumen. Pharmacokinetics Absorption. Mesalazine absorption is greatest in the proximal intestine and minimal in the distal intestine. Cmax in blood plasma of 5-ASA after a single dose, as well as during therapy for several weeks with 500 mg of mesalazine 3 times a day in the form of Salofalk suppositories varied from 0.1 to 1.0 μg/ml, while for the main metabolite N- Ac-5-ASA - from 0.3 to 1.6 μg/ml. In some cases, Cmax of 5-ASA in blood plasma was achieved within 1 hour after administration. Biotransformation. Mesalazine is metabolized both presystemically in the intestinal mucosa and in the liver into the pharmacologically inactive N-Ac-5-ASA. It is obvious that acetylation does not depend on the acetylator phenotype of the patient. Some acetylation also occurs due to the action of bacteria in the large intestine. The binding of mesalazine and N-Ac-5-ASA to proteins is 43 and 78%, respectively. Distribution. In scintigraphic studies with technetium-labeled Salofalk suppositories, it was found that the peak spread of the suppository, which dissolved at body temperature, occurs after 2–3 hours. The spread is limited primarily to the rectum and the retrosigma-like junction. Consequently, Salofalk suppositories are especially effective for the treatment of proctitis (ulcerative colitis of the rectum). Excretion. After a single use of 500 mg of mesalazine in the form of a Salofalk suppository, about 11% (within 72 hours) and after therapy for several weeks with 500 mg of mesalazine 3 times a day in the form of Salofalk suppositories, about 13% of the administered dose of 5-ASA was excreted in the urine. About 10% of the administered dose was excreted in bile. Mesalazine and its metabolite N-Ac-5-ASA are excreted in feces (the main part) and bile (a small part), and excreted by the kidneys (varies between 20 and 50% depending on the route of administration, dosage form and route of release of mesalazine, respectively). Renal excretion occurs predominantly in the form of N-Ac-5-ASA. About 1% of the total orally administered dose of mesalazine passes into breast milk mainly in the form of N-Ac-5-ASA. Indications for use of the Salofalk suppository Treatment for exacerbations and prevention of relapses of ulcerative colitis limited to the rectum.
Directions for use and doses
Rectally. For the treatment of exacerbations of ulcerative colitis: adults, 2 supp. 3 times a day (corresponds to 1500 mg of mesalazine per day). As maintenance therapy during remission: adults, 1 sup. 3 times a day (corresponds to 750 mg of mesalazine per day). The duration of treatment is determined by the doctor.
Contraindications
- hypersensitivity to the components of the drug and other salicylic acid derivatives;
- severe renal/liver failure.
- children under 18 years of age.
- peptic ulcer of the stomach and duodenum in the acute phase;
- hemorrhagic diathesis (with a tendency to bleed).
With caution: respiratory dysfunction (especially bronchial asthma); hypersensitivity to sulfasalazine; liver dysfunction; deficiency of glucose-6-phosphate dehydrogenase, renal dysfunction.
Adverse reactions
The following side effects, classified by organ system and frequency of occurrence, were observed with the use of mesalazine. The assessment of adverse events is based on the following classification: often (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10000; <1/1000); very rare (<1/10000). From the blood and lymphatic system: very rarely - pathological indicators of blood cells (aplastic anemia, agranulocytosis, pancytopenia, neutropenia, leukopenia, thrombocytopenia). From the nervous system: rarely - headache, dizziness; very rarely - peripheral neuropathy. From the heart: rarely - myocarditis, pericarditis. From the respiratory system, chest and mediastinum: very rarely - allergic and fibrotic reactions from the lungs (including shortness of breath, cough, bronchospasm, alveolitis, pulmonary eosinophilia, pulmonary infiltrates, pneumonitis). From the gastrointestinal tract: rarely - abdominal pain, diarrhea, bloating, nausea, vomiting; very rarely - acute pancreatitis. From the kidneys and urinary tract: very rarely - renal dysfunction, incl. acute and chronic interstitial nephritis, renal failure. From the skin and subcutaneous tissues: very rarely - alopecia. From the musculoskeletal system and connective tissue: very rarely - myalgia, arthralgia. From the immune system: very rarely - hypersensitivity reactions, for example allergic exanthema, drug fever, lupus erythematosus syndrome, pancolitis. From the liver and biliary tract: very rarely - increased activity of transaminases and cholestasis parameters), cholestatic hepatitis. From the reproductive system: very rarely - oligospermia (reversible).
special instructions
Before starting and during treatment, it is necessary to conduct blood tests (differentiated count of blood cells; liver function parameters, such as transaminases; creatinine content) and urine (level indicators) at the doctor's discretion. It is recommended to carry out monitoring 14 days after the start of treatment, then 2-3 times at intervals of 4 weeks. If the test results are normal, routine checks can be performed every 3 months. If other additional symptoms appear, tests must be done immediately. Particular attention when using Salofalk is necessary in case of liver dysfunction. Salofalk is not recommended for use in patients with impaired renal function. Before initiating treatment, attention should be paid to mesalazine-induced renal toxicity.
During pregnancy and breastfeeding
There is no sufficient data regarding the use of Salofalk in pregnant women. However, information about the use of the drug in a limited number of pregnant women indicates the absence of undesirable effects of mesalazine on the course of pregnancy or on the health of the fetus and/or newborn. In a single case, renal failure in the newborn was reported after long-term use of high doses of mesalazine (2–4 g orally) during pregnancy. Salofalk should be taken during pregnancy only when the potential benefits of use outweigh the possible risks. Breastfeeding 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 in women during breastfeeding. Hypersensitivity reactions such as diarrhea cannot be excluded. Therefore, Salofalk can be used during breastfeeding only when the potential benefit to the mother outweighs the likely risk to the fetus. If an infant develops diarrhea, breastfeeding should be stopped.
Children
Do not use in children under 18 years of age.
Impact on the ability to drive vehicles and operate other machinery
No effect on the ability to drive vehicles or use machinery was detected. However, if the patient experiences any symptoms from the central nervous system, he should stop driving vehicles or operating other mechanisms.
Interaction
No studies have been conducted on the interaction of Salofalk with other drugs. Patients receiving concomitant treatment with azathioprine, 6-mercaptopurine or thioguanine should be aware of the possible enhanced myelosuppressive effect of azathioprine and 6-mercaptopurine or thioguanine. The use of mesalazine together with anticoagulants, such as warfarin, may reduce the anticoagulant effect of the latter.
Overdose
No cases of overdose have been identified. In case of overdose, symptomatic treatment is carried out.
Storage conditions for the drug Salofalk
In a place protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children.
Shelf life of the drug Salofalk
3 years. Do not use after the expiration date stated on the package.
Conditions for dispensing from pharmacies
On prescription.
Side effects when using mesalazine
The side effects of mesalazine are described in sufficient detail in the official instructions for the drug, however, in general, the drug is well tolerated even in large doses and with long-term use (in 93-98% of patients).
Immediate allergic reactions (soft tissue swelling, Quincke's edema, anaphylaxis) when taking mesalazine range from 0.07 to 0.1% of cases.
The risk of allergic reactions generally increases in patients with bronchial asthma.
The drug is toxic to the liver, pancreas and bone marrow. Drug-induced liver damage and clinically insignificant changes in liver tests (increased ALT and/or AST) when taking mesalazine occur in 2.6-4% of cases. Toxic pancreatitis (inflammation of the pancreas) is observed even less frequently - less than 1% of cases.
Mesalazine, pregnancy and breastfeeding
In the article “Frequently Asked Questions on IBD,” we looked at the problem of conception, pregnancy and delivery in ulcerative colitis and Crohn’s disease.
These diagnoses are not a death sentence at all; patients with IBD can become pregnant and give birth. At the same time, the patient may need to continue taking mesalazine even during pregnancy.
The effect of mesalazine on conception
There is no data on the effect of mesalazine on the ability of men to conceive (unlike, for example, sulfasalazine).
