Budesonide + Salbutamol (Budesonidum + Salbutamolum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Beta-adrenomimetics

Included in the formulation
  • Biasten
    powder d / inhal. 
    PULMOMED, ​​CJSC     Russia
    • АТХ:

    R.03.A.K.04   Salbutamol and sodium cromoglycate

    Pharmacodynamics:

    Combination preparation containing glucocorticosteroid for topical use (budesonide) and selective beta2-adrenomimetic (salbutamol hemisuccinate).

    Budesonide - inhalation glucocorticosteroid, at recommended doses has anti-inflammatory effect (has a lower incidence of side effects than systemic glucocorticosteroids).

    The anti-inflammatory effect of budesonide is due to several factors.

    1. The drug induces the synthesis of lipocortin, inhibiting the activity of phospholipase A2. Inhibition of phospholipase A mediated2 hydrolysis of membrane phospholipids of damaged tissues prevents the formation of arachidonic acid. The disruption of the formation of arachidonic acid actually means inhibition of the synthesis of prostaglandins, since arachidonic acid is a substrate for further metabolism along the cyclooxygenase pathway, and also along the lipoxygenase pathway, with appropriate inhibition of leukotriene synthesis.

    2. The anti-inflammatory effect of the drug is potentiated by its ability to inhibit the expression of COX-2 genes,which also leads to a decrease in the synthesis of prostaglandins in the inflammatory focus, including pro-inflammatory prostaglandins E2 and I2.

    3. Budesonide inhibits the expression of molecules of intercellular adhesion in the endothelium of blood vessels, violating the penetration of neutrophils and monocytes into the focus of inflammation.

    In addition, the drug inhibits the release of mediators of allergies, and also reduces the hyperreactivity of the smooth muscles of the bronchi.

    Salbutamol is a selective stimulant beta2-adrenergic receptors. Provides bronchodilating effect, prevents and stops bronchospasm, reduces resistance in the airways, increases vital capacity of the lungs. Prevents the release of histamine and leukotrienes from mast cells. In therapeutic doses, it practically does not have chronotropic and inotropic effects.

    Pharmacokinetics:The therapeutic effect of budesonide develops gradually over 7-10 days. The bronchodilator effect of salbutamol occurs rapidly, within 1-3 minutes after inhalation, and persists for 5-7 hours after taking a single dose.
    Indications:Bronchial asthma.
    ICD-10

    X.J40-J47.J45   Asthma

    Contraindications:Hypersensitivitypulmonary tuberculosis (active phase), fungal, viral, bacterial infections of the respiratory system, pregnancy (I-II trimester), threatened miscarriage, children's age (under 16 years).
    Carefully:Arrhythmias (especially tachyarrhythmias), myocarditis, heart disease (including aortic stenosis), hypokalemia, arterial hypertension, acute heart failure, diabetes mellitus, thyrotoxicosis, glaucoma, pregnancy, breast-feeding.
    Pregnancy and lactation:

    Combination Budesonide + Salbutamol: the category of FDA recommendations is not defined. Adequate and well-controlled studies on humans have not been conducted.

    Salbutamol: FDA recommendations in category C. In studies on mice, the intake of salbutamol was accompanied by the development of cleft palate in the fetus in 4.5-9.3% of cases, depending on the amount of the dose taken. It can cause tachycardia and hyperglycemia in a pregnant woman and a fetus; affects the contractile function of the uterus (delaying the onset of labor). Cases of arterial hypotension, pulmonary edema, paralysis of the heart and maternal death are described.

    Budesonide: recommendations of the FDA category C. A means of choice during pregnancy in the US due to the large clinical experience of its use. Standard doses of inhalation glucocorticosteroids, as a rule, do not cause violations on the part of the fetus. Adequate and well-controlled studies on humans have not been conducted. In pharmacological doses can cause placental insufficiency, deficiency of fetal body weight, stillbirth. Teratogenic effect is not confirmed. Studies in animals have revealed an increase in the incidence of cleft palate, placental insufficiency, spontaneous abortion and intrauterine growth retardation of the fetus. In newborns whose mothers received inhalation glucocorticosteroids during pregnancy, it is necessary to exclude adrenal insufficiency.

    There is no information on the penetration into breast milk. However, analogues of these drugs penetrate into breast milk.

    Dosing and Administration:

    Inhalation. Selection of the dose of medicines included in the composition of the drug occurs individually, depending on the severity of the disease. The recommended dose is 1 inhalation 3 times a day or 2 inhalations 2 times a day.

    After achieving optimal control of the symptoms of bronchial asthma on the background of taking the drug, it is possible to reduce the daily dose to a minimally effective maintenance dose, up to once a day.

    Side effects:Irritation of the mucous membrane of the mouth and pharynx, cough, hoarseness of voice (dysphonia) and aphonia, candidal stomatitis and pharyngitis, dryness and unpleasant taste in the mouth, nausea, vomiting. Anxiety, tremor of skeletal muscles, headache, decreased blood pressure, collapse, palpitations, paradoxical bronchospasm, skin rash, irritability, depression, sleep disorders, behavioral disorders, systemic side effects glucocorticosteroids.
    Overdose:Tachycardia, weakness, lowering of blood pressure, tremor. Treatment: symptomatic, the introduction of cardioselectivebeta blockadetorus.
    Interaction:

    Inhibitors of the enzyme of the cytochrome CYP3A4 system (ketoconazole, ritonavir): possible development of systemic action budesonide.

    Non-selective beta-blockers: incompatibility.

    The derivatives of xanthine, diuretics, glucocorticosteroids: risk of hypokalemia.

    Special instructions:

    It is not intended for initial selection of therapy at the first stages of treatment of bronchial asthma.

    Hoarseness, cough, resulting from the sedimentation of the drug in the oropharynx as a result of improper technique of inhalation, usually occur after a reduction in the dose of the drug.

    Local infections caused by yeast-like fungi are quickly stopped by local antifungal treatment without the need for interruption of drug treatment.

    To avoid the development of local candidiasis of the oral cavity and pharynx, it is necessary to rinse the mouth thoroughly with water after inhalation without swallowing.

    Transition from system glucocorticosteroids on inhalation of the drug may cause allergic reactions such as rhinitis and eczema, which were previously suppressed by systemic glucocorticosteroids. When these symptoms appear, it is necessary to prescribe antihistamines.

    During the transition from system glucocorticosteroids on inhalation patients may experience increased fatigue, headache, arthralgia and myalgia, and sometimes nausea and vomiting.

    Budesonide - an inhaled glucocorticoid for the prevention of asthma attacks, salbutamol - beta2-adrenomimetic for their cupping. Therefore, the combination of an inhaled glucocorticoid with beta2-adrenomimetics of short-acting is inexpedient and is not used in world practice.

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