Cortiment enteric sustained release pills 9 mg, 30 pcs.

Composition

of 1 tab. – budesonide 9 mg. Auxiliary substances:stearic acid-10 mg, soy lecithin-10 mg, microcrystalline cellulose-156 mg, hydroxypropylcellulose-60 mg, lactose monohydrate-50 mg, colloidal silicon dioxide-2 mg, magnesium stearate-3 mg.

Shell composition:

methacrylic acid copolymer type A – 8 mg, methacrylic acid copolymer type B-8 mg, talc-7.9 mg, titanium dioxide-4.5 mg, triethyl citrate-1.6 mg

. Pharmacological action

The exact mechanism of action of budesonide in the treatment of ulcerative colitis is not fully established. Budesonide inhibits many inflammatory processes, including cytokine production, activation of inflammatory infiltrate cells, and expression of adhesive molecules on endothelial and epithelial cells. At doses that are clinically consistent with prednisone, budesonide causes significantly less suppression of the hypothalamic-pituitary-adrenal axis and has less effect on inflammatory markers.

Data from clinical pharmacological and pharmacokinetic studies indicate that the mechanism of action of Cortimentum tablets is based on local action in the intestine.

Pharmacodynamic effects

Budesonide is a corticosteroid with anti-inflammatory, anti-allergic, anti-exudative and decongestant properties.

The extended release MMC technology is characterized by a multi-matrix structure covered with a gastro-resistant membrane that dissolves in intestinal fluids with a pH level above 7.

When using a budesonide tablet, the gastroprotective layer protects it when passing through the stomach and duodenum to the lower part of the intestine. When the protective layer is dissolved, the intestinal fluid comes into contact with a matrix of hydrophilic polymers, which begins to swell to form a viscous gel matrix. The solvent that penetrates through the gel matrix releases the Active ingredient from the lipophilic matrices. Budesonide is then released into the intestines at a controlled rate as it travels through the entire colon.

Budesonide is a corticosteroid that is successfully used in the treatment of inflammatory bowel diseases. It has a stronger local anti-inflammatory effect compared to many other corticosteroids, but it does not reduce cortisol levels to the same extent as methylprednisolone, prednisolone, or hydrocortisone. Its affinity for the glucocorticoid receptor is approximately 200 times higher than that of hydrocortisone, and approximately 15 times higher than that of prednisone.

Pediatric population

Cortimentum has not been studied in the pediatric population.

Indications

-induction of remission in patients with mild or moderate active ulcerative colitis.

Use during pregnancy and lactation

Pregnancy

Data on the use of inhaled budesonide in a large number of women during pregnancy do not indicate any adverse events. Although there are no data on pregnancy outcomes after oral administration, bioavailability after oral administration is low. During experiments in animals, with a high degree of exposure, corticosteroids were found to be harmful. The drug Cortimentum should be taken during pregnancy only if absolutely necessary.

Feeding a pile of food

Budesonide is excreted in small amounts in breast milk. Given the rapid clearance of budesonide from the blood, it is expected that the impact on a breastfed child will be small. However, there is no supporting evidence. A decision should be made to stop breast-feeding or discontinue / refrain from budesonide treatment, taking into account the benefits of breastfeeding for the child and the benefits of treatment for the woman.

Reproductive function

There are no data on the effects of Cortimentine on human reproductive function. After treatment with budssonide, no effects on reproductive function were observed in rats.

Contraindications

-hypersensitivity to the Active ingredient or any of the excipients—

– lactose intolerance, lactase deficiency, glucose-galactose malabsorption—

– cirrhosis of the liver—

– infectious bowel diseases

— – breast-feeding period;

– age up to 18 years.

With caution

Use with caution in patients with diagnosed liver and kidney function disorders.

The most thorough assessment is made of the risks associated with the use of corticosteroids, including the drug Cortimentum, among patients with a potential risk of complications. related to the use of steroids (patients with diabetes, hypertension, gastrointestinal diseases, osteoporosis, glaucoma or cataracts). Before transferring patients from systemic steroids to Cortimentum, possible complications due to a decrease in systemic steroid levels should be considered and the feasibility of gradual withdrawal of systemic corticosteroids should be evaluated.

The use of Cortimentum may lead to an exacerbation of the inflammatory response in patients with infectious diseases, and a decrease in the immune response to vaccines.

With caution, it is prescribed to patients with concomitant verified mental disorders or in the presence of mental illnesses in relatives of the first degree.

The risks of drug interactions should be considered when Cortimentum is co-administered with drugs that may enhance the systemic effects of budesonide tablets (ketoconazole, grapefruit juice, etc. ).

Side effects

Summary of side effects. Those registered in clinical trials are listed in the table below.

Occasionally, side effects typical of systemic corticosteroids may occur. These side effects depend on the dose, duration of treatment, concomitant or previous treatment with other corticosteroids, and individual sensitivity. Side effects of a class of steroids include:

From the side of the skin: allergic exanthema, red striae, petechiae, ecchymosis, steroid acne, delayed wound healing, contact dermatitis;

Musculoskeletal system, connective tissue and bone disorders:aseptic bone necrosis (femur and head of humerus).

From the side of the visual organs: glaucoma, cataracts.

Mental disorders: depressive syndrome, irritability, euphoria.

From the gastrointestinal tract: complaints from the stomach, duodenal ulcer, pancreatitis.

Metabolic and nutritional disorders: Cushing’s syndrome, moon-shaped face, torso obesity, decreased glucose tolerance, diabetes mellitus, sodium retention with edema, increased potassium release, inactivity and/or atrophy of the adrenal cortex, growth retardation in children, impaired sex hormone secretion (for example, amenorrhea, hirsutism, impotence).

From the cardiovascular system: hypertension, increased risk of thrombosis, vasculitis (withdrawal syndrome after long-term therapy).

From the immune system: impaired immune response (for example, increased risk of infection).

Interaction

Budesonide exhibits lower systemic bioavailability compared to other CORTICOSTEROIDS, so drug interactions may be reduced compared to many other drugs in this class. Patients at increased risk of drug interactions include the elderly and patients with impaired renal or hepatic function.

Budesonide is metabolized by cytochrome P4503A4 (CYP3A4), so inhibitors of this enzyme, such as ketoconazole, itraconazole, erythromycin, and grapefruit juice, may increase the systemic exposure of budesomide. Co-administration with ketoconazole resulted in an 8-fold increase in AUC, compared to budesonide alone. When consuming large amounts of grapefruit juice, a CYP3A4 inhibitor in the intestinal mucosa, the systemic exposure to budesonide is approximately doubled. Treatment with other known CYP3A4 inhibitors is expected to have a similar effect. Inhibition of the metabolism of other drugs by the CYP3A4 isoform under the action of budesonide is unlikely, since budesonide shows low affinity for this enzyme.

Agents that interact with corticosteroids, which can pose a significant risk in individual patients, include cardiac glycosides (increased effect due to a decrease in potassium levels) and diuretics (increased potassium excretion).

When co-administered with estrogens or oral contraceptives, elevated plasma levels and enhanced corticosteroid effects have been reported in women. However, a low-dose combined oral contraceptive that increased the plasma concentration of oral prednisone by more than 2 times did not significantly affect the plasma concentration of oral budesonide. Contraceptives containing ethinyl estradiol have been shown to affect the pharmacokinetics of budesonide.

Although no studies have been conducted, co-administration of colestyramine or antacids may reduce budesonide uptake, along with other medications. Therefore, such drugs should not be taken simultaneously, but at least at intervals of 2 hours.

At the recommended doses, omeprazole did not have any effect on the pharmacokinetics of oral budesonide, while cimetidine may lead to a slight increase in plasma budesonide levels, but this is clinically insignificant.

How to take, course of administration and dosage

Inside, in the morning, regardless of food intake. The tablet should be swallowed whole, washed down with water, without chewing or grinding.

Adults

The recommended daily dose for inducing remission is 1 tab.9 mg in the morning, for 8 weeks.

Do not abruptly stop taking the drug, it is necessary to gradually reduce the dose.

Advanced age

No dose adjustment is required. However, the experience of using the drug in elderly patients is limited.

Patients with impaired liver and kidney function

Cortimant has not been studied in patients with impaired liver and kidney function, therefore, caution should be exercised when using the drug and monitoring such patients.

Overdose

Due to the low systemic availability of Cortimentine tablets, it is not expected that acute overdose, even at very high doses, can lead to an acute clinical crisis. In the case of acute overdose, there is no specific antidote. Treatment consists of supportive and symptomatic therapy.

Special instructions

Cortimentol tablets should be used with caution in patients with infections, hypertension, diabetes mellitus, osteoporosis, gastric and duodenal ulcers, glaucoma or cataracts, or with a family history of diabetes or glaucoma, or with any other condition where the use of glucocorticoids may have undesirable effects.

Treatment with Cortimentum tablets achieves lower systemic steroid levels compared to traditional oral glucocorticoid therapy. When switching from another steroid therapy, symptoms associated with changes in systemic steroid levels may occur. Replacing systemic glucocorticoids with drugs with low bioavailability, such as Cortimentum tablets, can unmask allergies such as rhinitis and eczema that were previously controlled with a systemic drug. Other symptoms associated with steroid withdrawal may also occur, such as benign intracranial hypertension. Therefore, monitoring of adrenal cortical function may be necessary in such patients, and the dose of systemic steroids should be reduced with caution.

Suppressing the inflammatory response and immune system increases susceptibility to infections and their severity. Clinical manifestations may be atypical, and serious infections, such as sepsis and tuberculosis, may be masked and go into an advanced stage before detection.

In patients receiving oral glucocorticoids, chickenpox and measles may be more severe. Special care should be taken to avoid exposure to patients who have not previously had these diseases. If an infection is detected or suspected in the patient, you should consider reducing the dose or discontinuing treatment and consult your doctor immediately. Passive varicella zoster immunoglobulin (VZIG) immunization is required in exposed non-immune patients who are receiving systemic corticosteroids or have used them for the previous 3 months; it should be performed within 10 days after exposure to the varicella zoster virus. If the diagnosis of chickenpox is confirmed, the disease requires urgent treatment under the supervision of a specialist. The use of corticosteroids should not be discontinued, and an increase in the dose may also be required. Immunocompromised patients who have had contact with koryo patients should receive normal immunoglobulin as soon as possible after contact.

Glucocorticoids can cause suppression of the hypothalamic-pituitary-suprarenal axis and decrease the stress response. When patients are undergoing surgery or other stressful conditions, additional treatment with a systemic glucocorticoid is recommended.

Deterioration of liver function may affect the elimination of glucocorticoids. Pharmacokinetics after oral budesonide administration changed in patients with impaired liver function, as evidenced by increased systemic availability in patients with moderate cirrhosis of the liver.

The risk of developing systemic adverse events is increased in patients with severe hepatic impairment (for example, with cirrhosis of the liver).

When discontinuation of treatment is necessary, a gradual dose reduction is recommended. Some patients may experience non-specific ill health during the drug withdrawal period, such as muscle and joint pain. A general lack of glucocorticoid effect should be suspected if, in rare cases, symptoms such as fatigue, headache, nausea and vomiting occur. In such cases, temporary use of systemic glucocorticoids may be required. Taking into account the available information about other drugs containing budesonide, sudden discontinuation of treatment is not recommended. A possible method of discontinuing the drug may be to take one tablet every other day for one week, after which the treatment may be discontinued.

Special care should be taken when considering the use of systemic corticosteroids in patients with severe affective states at the current time or in the patient’s own history or any of the first-degree relatives. This includes depressive syndrome or manic-depressive illness and prior steroid psychosis.

Systemic effects of steroids may occur, especially if high doses are prescribed and used for extended periods of time. Such effects may include Cushing’s syndrome, adrenal suppression, growth retardation, decreased bone mineral density, cataracts, glaucoma, and, very rarely, a wide range of psychiatric/behavioral effects.

In vivo studies have shown that oral administration of ketoconazole (an inhibitor of CYP3A activity in the liver and in the intestinal mucosa) increases the systemic effect of oral budesonide several times. If ketoconazole treatment is indicated in combination with budesonide, discontinuation of budesonide treatment should be considered in the event of side effects typical of systemic glucocorticoids.

After consuming significant amounts of grapefruit juice (which inhibits CYP3A activity mainly in the intestinal mucosa), systemic exposure to oral budesonide increased approximately 2-fold. As with other drugs that are primarily metabolized by CYP3A, it is necessary to avoid regular consumption of grapefruit or grapefruit juice at the same time as budesonide (other juices such as orange juice or apple juice do not inhibit the activity of CYP3A).

Since corticosteroids are known to have immunological effects, co-administration of Cortimentum tablets is likely to reduce the immune response to vaccines.

Influence on the ability to drive vehicles and mechanisms

No studies have been conducted to study the effect of the drug Cortimenton on the ability to drive vehicles and work with mechanisms. When driving vehicles or working with mechanisms, it should be taken into account that occasionally dizziness or fatigue may occur.

Form of production

Tablets enteric-soluble with prolonged release, film-coated white or almost white, round, biconvex, with the inscription “MX 9” on one side.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 30°C.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Budesonide

Conditions of release from pharmacies

Prescription

Weight

Weight: 27 gr.