Budesonide (When ATH R01AD05)

When ATH:
R01AD05

Characteristic.

White or almost white, odorless powder, practically insoluble in water and heptane, sparingly soluble in ethanol, very soluble in chloroform. Distribution factor октанол/вода при pH 7,4 равен 1,6·103. Molecular weight 430,54.

Pharmacological action.
Glucocorticoid, anti-inflammatory, antiallergic.

Application.

Inhalation: bronchial asthma, chronic obstructive pulmonary disease.

Inside: Crohn's disease involving the ileum and / or ascending colon (for the induction of remission in mild to moderate forms).

Intranasal: seasonal and perennial allergic rhinitis.

Contraindications.

Hypersensitivity, for inhalation use: active pulmonary tuberculosis, fungal infections of the respiratory system; oral: GI infections (Bacterial, Fungal, amebic, Viral), severe liver, childhood; for intranasal use: Fungal, Bacterial and viral infections of the respiratory, pulmonary tuberculosis.

Restrictions apply.

For oral administration: tuberculosis, arterial hypertension, diabetes, osteoporosis, pepticheskaya ulcer, glaucoma, Cataract, family history of diabetes in relation or glaucoma.

Pregnancy and breast-feeding.

When pregnancy is possible only in case, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies on the use during pregnancy has not been conducted). Children, whose mothers during pregnancy received substantial doses of corticosteroids, It should be closely monitored (possible hypoadrenalism). In women of childbearing age before therapy should be possible pregnancy, and during treatment - used reliable methods of contraception. At the time of treatment should stop breastfeeding (unknown, whether budesonide penetrate into breast milk).

Side effects.

Inhalation: disfonija, sore throat, dryness or irritation of the mouth or throat, cough; less frequently - candidiasis of the oral mucosa, nausea, pharyngitis, paradoxical bronchospasm.

When taken orally

From the nervous system and sensory organs: depression, euphoria, irritability, glaucoma, Cataract.

Cardio-vascular system and blood (hematopoiesis, hemostasis): increased blood pressure, an increased risk of thrombosis, vasculitis (withdrawal after prolonged treatment).

From the digestive tract: epigastric pain, dyspepsia, duodenalynaya ulcer, pancreatitis.

On the part of the endocrine organs: Cushing's syndrome, incl. moon face, obese trunk; diabetes, reduced glucose tolerance, sodium retention with edema formation, kaliopenia, decrease in function or atrophy of the adrenal cortex, violation of secretion of sex hormones (amenorrhea, girsutizm, impotence).

On the part of the musculoskeletal system: muscular weakness, osteoporosis, aseptic necrosis of bone (femoral head and shoulder).

For the skin: an allergic rash, red striae, petechiae, ecchymosis, steroid acne, impaired wound healing, contact dermatitis.

Other: increased risk of infectious diseases.

Intranasal application: burning, irritation of the nasal mucosa, sneezing, kandidomikoz.

Cooperation.

Inhibitors of cytochrome P450 (incl. ketoconazole, Erythromycin, cyclosporine) can slow the metabolism and enhance the effect of glucocorticoid. Budesonide may increase the effects of cardiac glycosides (due to potassium deficiency); saluretics may enhance hypokalemia. Co-administration of cimetidine and budesonide may result in a slight increase in plasma levels of budesonide (clinical significance has not). Omeprazole (while the appointment) It has no effect on the pharmacokinetics of budesonide.

Overdose.

Symptoms of chronic overdose: manifestations of Cushing.

Treatment: cancellation of budesonide by gradual dose reduction.

Dosing and Administration.

Inhalation: Dose selected individually, taking into account the severity of the disease, maintenance dose glucocorticoid tablets; adults - 200-800 mg / day (to 1600 mg / day), in divided doses; children - depending on their age.

Inside: without chewing (in violation of the act of swallowing can open the capsule and swallow the pellets), drinking plenty of fluids (a full glass of water), for 30 minutes before eating, by 3 mg 3 once a day (morning, at noon and in the evening). The course of treatment - usually 8 Sun; usually, effect occurs within 2-4 weeks. The abolition of a gradually.

Intranasal: the dose and duration of treatment are chosen individually, taking into account the severity of the disease, adults and children over 18 years, a single dose - 2-3 drops in each nostril; usually, enough 2 single doses a day; the duration of the course - 10-14 days.

Precautions.

With prolonged use may develop candidiasis.

Budesonide can suppress the function of the hypothalamic-pituitary-adrenal system. Before surgery or exposure to other stressors recommended supplementation systemic glucocorticoids.

Cooperation

Active substanceDescription of interaction
ItraconazoleFKV. FMR. As an inhibitor of CYP3A4 slows the biotransformation and increases the effect.
KetoconazoleFKV. As an inhibitor of CYP3A slow biotransformation, Increases concentration of plasma, It increases the likelihood of toxic effects.
ClarithromycinFKV. FMR: synergism. As an inhibitor of CYP3A slow biotransformation and increases the effect.
ErythromycinFKV. FMR: synergism. As an inhibitor of CYP3A4 slows the biotransformation and increases the effect.


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