Universal reference book for medicines
Product name: BENACAP (BENACAP)

Active substance: budesonide

Type: GCS for intranasal administration

Manufacturer: АБСхим (Russia)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
GCS. With inhalation application has anti-inflammatory, antiallergic and antiexcadative effect, which leads to a decrease in bronchial obstruction. The mechanism of action is to inhibit the release of inflammatory mediators and allergies, as well as to reduce the reactivity of the airways to their action. In the process of treatment, the function of breathing improves, the severity and frequency of dyspnea, attacks of suffocation, coughing significantly decrease. The maximum clinical effect develops after 1-2 weeks of therapy.
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. In doses that clinically correspond to prednisolone, 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 budesonide upon ingestion is based on local action in the intestine.
PHARMACOKINETICS
When inhaled into the bronchioles penetrates 30-35% of the dose. Bioavailability when entering the lung is about 73%. 25-30% fall into the digestive tract. Bioavailability in the oral route of administration is 10.7%. Cmax budesonide in plasma is reached after 1.5-2 h. Budesonide is quickly excreted from the body. T 1/2 with inhalation is 2-3 hours. Plasma clearance is 55-85 l / h.
After ingestion in a special dosage form, approximately 90% of budesonide is metabolized by "first passage" through the liver and only about 10% is systemic accessibility. Budesonide has a significant V d (about 3 l / kg). Binding to plasma proteins is 85-90% on average. Budesonide undergoes extensive biotransformation in the liver with the formation of metabolites with low glucocorticoid activity. Glucocorticoid activity of the main metabolites (6? -hydroxybudesonide and 16? -hydroxprednisolone), does not exceed 1% of the activity of budesonide itself. The metabolism of budesonide is predominantly mediated by CYP3A isoenzymes. The rate of excretion of budesonide is limited by the degree of absorption. Budesonide is characterized by a high systemic clearance (about 1.2 l / min).
INDICATIONS
Bronchial asthma requiring maintenance therapy with glucocorticoids.
To induce remission in patients with mild to moderate active ulcerative colitis.
DOSING MODE
The dose is set depending on the indications, age, dosage form.
SIDE EFFECT
With inhalation, irritation of the mucous membranes of the pharynx, oral cavity, nose, candidiasis is possible; with increased sensitivity - bronchospasm.
When ingested occasionally, there may be side effects typical of systemic SCS. These side effects depend on the dose, duration of treatment, concomitant or prior treatment with other SCS and individual sensitivity. Side effects of the class of steroids include:
On the part of the skin: allergic exanthema, red striae, petechia, ecchymosis, steroid acne, delayed wound healing, contact dermatitis.
From the side of the musculoskeletal system: aseptic necrosis of the bone (femur and head of the humerus).
On the part of the organs of vision: glaucoma, cataract.
Mental disorders: depressive syndrome, irritability, euphoria.
From the digestive system: discomfort in the stomach, duodenal ulcer, pancreatitis.
Endocrine system: Cushing's syndrome, lunar face, obesity of the trunk, decreased glucose tolerance, diabetes mellitus, adrenal cortex deficiency, growth retardation in children, violation of the secretion of sex hormones (eg, amenorrhea, hirsutism, impotence).
From the side of metabolism: sodium retention with the formation of edema, increased release of potassium.
From the cardiovascular system: arterial hypertension, increased risk of thrombosis, vasculitis (withdrawal syndrome after long-term therapy).
On the part of the immune system: violation of the immune response (eg, increased risk of infection).
CONTRAINDICATIONS
For inhalation use: hypersensitivity to budesonide.
For oral administration: cirrhosis of the liver; infectious diseases of the intestine; lactation period (breastfeeding); children and adolescents under 18; hypersensitivity to budesonide.
PREGNANCY AND LACTATION
In the form of inglay, pregnancy use is possible when the intended benefit to the mother exceeds the potential risk to the fetus. If it is necessary to use during the lactation period, breastfeeding should be stopped, due to the lack of data on the isolation of budesonide with breast milk.
Contraindicated oral administration during pregnancy and lactation (breastfeeding).
APPLICATION FOR CHILDREN
The effectiveness and safety of budesonide in children under the age of 7 years has not been studied.
SPECIAL INSTRUCTIONS
For inhalation use
With caution apply in patients with pulmonary tuberculosis, as well as with chicken pox.
Budesonide is not intended for relief of acute attacks of asthma in bronchial asthma. It is not recommended for intermittent disease.
Replacement of systemic GCS by inhalation is carried out gradually.
The effectiveness and safety of budesonide in children under the age of 7 years has not been studied.
For oral administration
Use with caution in patients with diagnosed disorders of liver and kidney function, with diabetes mellitus, arterial hypertension, gastrointestinal diseases, osteoporosis, glaucoma or cataracts, with concomitant verified mental disorders or in the presence of mental illness in first-degree relatives.
The use of budesonide can lead to an exacerbation of the inflammatory response in patients with an infectious pathology, a decrease in the immune response to vaccines.
DRUG INTERACTION
Cimetidine and omeprazole have no clinically significant effect on the pharmacokinetics of budesonide when taken orally. However, under the influence of cimetidine, a slowdown in the metabolism of budesonide in the liver is possible.
Budesonide is characterized by lower systemic bioavailability compared to other GCS, so the drug interaction may be less pronounced than many other drugs in this class.
The risk of drug interactions may be increased in elderly people and in patients with impaired renal or hepatic function.
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