Budesonide

Glucocorticoid for local use, has anti-inflammatory and anti-allergic effects. It increases the production of lipocortin , which is an inhibitor of phospholipase A2, inhibits the release of arachidonic acid , inhibits the synthesis of arachidonic acid metabolism products - cyclic endoperoxides and Pg . Prevents marginal accumulation of neutrophils , reduces inflammatory exudation and cytokine production , inhibits macrophage migration, reduces the intensity of infiltration and granulation processes, the formation of chemotaxis substance (which explains the effectiveness in the "late" allergy reactions); inhibits the release of inflammatory mediators from mast cells (“immediate” allergic reaction), which plays a significant role in the occurrence of nasal symptoms of allergic genesis and the development of chronic rhinitis . It is well tolerated with long-term treatment, does not have ISS activity, practically does not have a resorptive effect . The therapeutic effect develops after 2-21 days.

Quickly absorbed from the lungs and gastrointestinal tract . With intranasal administration, it is very little absorbed from the mucous membrane of the nasal cavity (only 20% enters the systemic circulation). After inhalation, about 25% of the dose enters the alveoli . The part that got into the gastrointestinal tract is almost completely (90%) destroyed (inactive metabolites are formed) during the “first passage” through the liver . Bioavailability is 10% of the amount received in the stomach , 25-30% of the budesonide received in the alveoli is absorbed. Cmax in the blood is reached 15-45 minutes after inhalation and intranasal administration. Plasma protein binding is 88%. It has a high systemic clearance (84 l / h). T _1/2 from plasma - 2.8 hours. Excreted in the urine , partially with bile in the form of metabolites.

After ingestion, the values ​​of Cmax and Tmax are variable (Tmax in individual patients - from 30 to 600 minutes). Systemic availability after a single dose is higher in patients with Crohn's disease in comparison with healthy volunteers (21% and 9%, respectively), but approaches that of healthy volunteers after repeated doses. About 90% of the absorbed budesonide is metabolized during the first passage through the liver with the participation of microsomal enzymes (mainly CYP3A4 ) to 2 main metabolites - 6-beta-hydroxy-budesonide and 16-alpha-hydroxyprednisolone (glucocorticoid activity of metabolites is less than 1/100 of budesonide activity , of the remaining amount, about 90% binds to albumin and is in an inactive state.

Budesonide has pronounced lipophilic properties and is rapidly absorbed in the intestine due to good tissue permeability. Compared to classic corticosteroids, budesonide has a very high degree of receptor affinity. Due to these properties, it has a targeted local action ^[1] .

• For spray: Seasonal and perennial allergic rhinitis . For spray (optional) - vasomotor rhinitis; prevention of nasal polyp growth after polypectomy ; non-infectious inflammatory processes in the nasal cavity.
• For capsules: Crohn's disease (mild and moderate forms involving the ileum and / or ascending colon).
• For ointment: Allergic dermatitis , psoriasis , eczema ; lichen planus , atopic dermatitis .
• For inhalations: Bronchial asthma (as a basic therapy; with insufficient effectiveness of beta2-adrenostimulants, cromoglycelic acid and ketotifen ; to reduce the dose of oral corticosteroids ), chronic obstructive pulmonary disease .
• For ampoules: With saline solution for washing the nasal cavity.

Hypersensitivity , for inhalation use: active form of pulmonary tuberculosis , fungal infections of the respiratory system; for oral use: infections of the gastrointestinal tract (bacterial, fungal, amoebic, viral), severe dysfunction of the liver, children's age; for intranasal use: fungal, bacterial and viral infections of the respiratory system, tuberculosis of the respiratory system.

Caution

For oral use: tuberculosis, arterial hypertension , diabetes mellitus , osteoporosis , peptic ulcer , glaucoma , cataracts , a burdened family history of diabetes or glaucoma.

Pregnancy and lactation

During pregnancy, it is possible only if the expected effect of therapy exceeds the potential risk to the fetus (adequate and strictly controlled studies on the use during pregnancy have not been conducted). Children whose mothers received significant doses of corticosteroids during pregnancy should be closely monitored ( adrenal hypofunction is possible). In women of childbearing age, a possible pregnancy should be excluded before the start of therapy, and reliable methods of contraception should be used during treatment. At the time of treatment, breast-feeding should be stopped (it is not known whether budesonide passes into breast milk ).

Inhalation

Dysphonia , sore throat , dryness or irritation of the oral cavity or pharynx , cough ; less often - candidiasis of the oral mucosa, nausea , pharyngitis , paradoxical bronchospasm .

When taken orally

• From the nervous system and sensory organs: depression , euphoria , irritability, glaucoma, cataract.
• On the part of the cardiovascular system and the blood system (hematopoiesis, hemostasis): increased blood pressure , increased risk of thrombosis, vasculitis (withdrawal syndrome after prolonged treatment).
• From the organs of the gastrointestinal tract: pain in the epigastric region , dyspeptic symptoms , duodenal ulcer , pancreatitis .
• From the endocrine organs: Cushing's syndrome , including a moon-shaped face, obesity of the body; diabetes mellitus, decreased glucose tolerance , sodium retention with the formation of edema , hypokalemia , decreased function or atrophy of the adrenal cortex , impaired secretion of sex hormones ( amenorrhea , hirsutism , impotence ).
• From the musculoskeletal system: muscle weakness, osteoporosis, aseptic necrosis of the bones ( femoral and humeral heads).
• From the skin: allergic exanthema , red striae , petechiae , ecchymosis , steroid acne , wound healing, contact dermatitis.
• Other: increased risk of infectious diseases.

Intranasal use

Burning, irritation of the nasal mucosa, sneezing, candidomycosis .

Overdose

Symptoms of chronic overdose: manifestations of hypercorticism .

Treatment: withdrawal of budesonide by gradually reducing the dose.

Cytochrome P450 inhibitors (including ketoconazole , erythromycin , cyclosporine ) can slow down the metabolism and enhance the glucocorticoid effect. Budesonide may enhance the action of cardiac glycosides (due to potassium deficiency); saluretics may increase hypokalemia . The simultaneous administration of cimetidine and budesonide can lead to a slight increase in the level of budesonide in the plasma (it does not have clinical significance). Omeprazole (with simultaneous administration) does not affect the pharmacokinetics of budesonide.

Theoretically, interaction with resins capable of binding steroids (e.g. cholestyramine), as well as antacids , cannot be ruled out. With the simultaneous administration of these drugs as a result of the interaction, the therapeutic effect of budesonide may decrease. In this regard, the above drugs should be taken with an interval of at least 2 hours ^[1] .

Inhalation: the dose is selected individually, taking into account the severity of the disease, supporting the dose of tablet glucocorticoids; adults - 200-800 mcg / day (up to 1600 mcg / day), in several doses; children - depending on age.

Inside: without chewing (in case of violation of the swallowing act, you can open the capsule and swallow all the granules), drinking plenty of fluids (a full glass of water) 30 minutes before meals, 3 mg 3 times a day (morning, noon and evening). The course of treatment is usually 8 weeks; as a rule, the effect appears after 2-4 weeks. Cancellation is carried out gradually.

Intranasally: the dose and duration of treatment are selected individually, taking into account the severity of the disease, for adults and children over 18 years of age, a single dose - 2-3 drops in each nasal passage; as a rule, 2 single doses per day are sufficient; course duration - 10-14 days.

With prolonged use, candidiasis may develop.

Budesonide can suppress the function of the hypothalamic-pituitary-adrenal system. Before surgery or exposure to another stress factor, the additional appointment of systemic glucocorticoids is recommended.

• Site of the Radar Drug Encyclopedia (rlsnet.ru). Description of the drug Budenofalk.
• Budesonide (Budesonide) - Encyclopedia of drugs and pharmaceutical products . Radar Patent. - Active substance.

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• Budenofalk in clinical practice