Budostera - instructions for use, dose, side effects, contraindications

Dextrose 2.38 mg, Avicel (microcrystalline cellulose and carmellose sodium 9: 1 ratio) 0.63 mg, potassium sorbate 0.06 mg, polysorbate 80 0.01 mg, disodium edetate 0.005 mg, hydrochloric acid up to pH 4.5 , purified water 47.85 mg

Each dose (one spray) of the drug 100 μg in a dose contains:

Active substance:

Budesonide 100 mcg.

Excipients:

Description:

White or almost white homogeneous suspension.

Pharmacotherapeutic group:Glucocorticosteroid for topical application

ATX: & nbsp

R.03.B.A.02 Budesonide

Pharmacodynamics:Budesonide is a synthetic glucocorticosteroid drug with a pronounced anti-inflammatory, antiallergic effect.

When used in therapeutic doses, it practically does not exert a resorptive effect. It does not have mineralocorticoid activity, it is well tolerated with long-term use. The drug has an inhibitory effect on the release of mediators of the inflammatory reaction, increases the synthesis of anti-inflammatory proteins,reduces the number of mast cells and eosinophilic granulocytes, prevents marginal neutrophils, reduces inflammatory exudation and production of cytokines. Budesonide reduces the release of toxic proteins from eosinophils, free radicals from macrophages and lymphokines from lymphocytes. It also reduces the binding of adhesive molecules to endothelial cells, thus reducing the flow of leukocytes to the site of allergic inflammation. Budesonide increases the number "active" βadrenoreceptors on the surface of the membrane of the smooth muscle cells of the vessels, thus increasing the sensitivity to decongestants.

The drug inhibits the activity of phospholipase A2, which leads to inhibition of the synthesis of prostaglandins, leukotrienes and platelet activation factor inducing an inflammatory response. Budesonide also inhibits the synthesis of histamine, which leads to a decrease in its level in the mast cells. Improvement of the condition is noted on the second - third day after the start of treatment.

Budesonide reduces the severity of symptoms in allergic rhinitis, suppresses the late and early phases of an allergic reaction, and reduces inflammation in the upperrespiratory tract.

Pharmacokinetics:

Suction

After topical application of 400 mcg of budesonide, the maximum concentration of C_m_Oh in blood plasma is reached after about 30 minutes and is 1 nmol / l. Only about 20% of the administered dose enters the systemic circulation.

Distribution

Due to a good distribution in tissues and binding to plasma proteins, the volume of distribution is 301 liters. The binding with blood plasma proteins, mainly with albumin, is 86 - 90%.

Metabolism

Systemic bioavailability of budesonide is low, as more than 90% of the absorbed drug is inactivated during the "first pass" through the liver. Glucocorticoid activity of metabolites does not exceed 1%.

Excretion

Metabolites are excreted mainly by the kidneys (70%) and through the intestine (10%). The half-life (T_1/2) is 2 hours. Concentration of budesonide in blood plasma is increased in patients with liver disease.

Indications:

- Prevention and treatment of seasonal and all-year-round allergic rhinitis;

- prevention and treatment of vasomotor rhinitis;

- polyps of the nose.

Contraindications:

- Hypersensitivity to budesonide or any other component of the drug;

- active form of pulmonary tuberculosis;

- children's age till 6 years.

Carefully:

Fungal and viral infections of the respiratory tract, a latent form of pulmonary tuberculosis (continuous monitoring of the patient's condition and specific therapy), recent surgical interventions in the nasal cavity, recent nose trauma, neurotropic viral infections, incl. shingles), pregnancy, cirrhosis, glaucoma, hypothyroidism.

Pregnancy and lactation:

Pregnancy

The results of prospective epidemiological studies, as well as the use of budesonide in the postmarketing period throughout the world, are not revealed an increased risk of congenital malformations due to the use of inhaled and nasal forms of budesonide in the early stages of pregnancy.

The use of Budoster ® during pregnancy is allowed only if the expected benefit for the mother exceeds the possible risk to the fetus.

Breast-feeding

The drug is able to penetrate into breast milk. However, when therapeutic doses of budesonide are applied to a baby who is breastfeeding, it is not expected. Budesonide can be used during breastfeeding.

Supportive asthma therapy with inhaled budesonide (at a dosage of 200 mg or 400 mg) in lactating women results in a minimal effect of the drug on the infant breastfed.

In pharmacokinetic studies, the estimated daily dose received by the child was 0.3% of the maternal daily dose, and the average concentration in the blood plasma of the child was 1/600 of the concentration observed in the mother's blood plasma. Concentrations of budesonide in all blood plasma samples of children were below the detection limit.

Based on the data obtained for inhaled budesonide and the fact that budesonide has linear pharmacological properties when applying therapeutic doses nasally, inhalation, orally, rectally, it is unlikely that the effect on the infant breastfed will be unlikely.

Dosing and Administration:

Adults and children older than 6 years at the beginning of therapy at 100 mcg in each nasal passage 2 times a day. The usual maintenance dose is 50 mcg in each nostril 2 times a day or 100 mcg in each nostril once a day in the morning. The maintenance dose should be the lowest effective dose that eliminates the symptoms of rhinitis.

The maximum single dose is 200 μg (100 μg per each nostril), the maximum daily dose is 400 μg for no more than 3 months.

For the full therapeutic effect of the preparation Budostere®, regular and correct application is required.

If the dose was missed, it should be taken as soon as possible, but not less than 1 hour before the next regular dose.

Children use the drug under the guidance of adults.

Side effects:

According to the World Health Organization (WHO), adverse reactions are classified according to their frequency of development as follows: very often (≥ 1/10), often (≥ 1/100, <1/10), infrequently (≥ 1/1000, < 1/100), rarely (≥ 1/10000, <1/1000) and very rarely (<1/10000); frequency is unknown - according to available data, it was not possible to establish the frequency of occurrence.

Disturbances from the respiratory system, organs of the thorax and mediastinum:

often: irritation of the nasal mucosa, bloody discharge from the nose, nosebleeds, sneezing after the first application of the drug, dyspnoea, hoarseness of the voice, wheezing, pain in the nasal cavity.

At the beginning of therapy for a short period of time, the following phenomena can occur: rhinorrhea and the formation of crusts on the mucosanose.

rarely: ulceration of the mucous membrane of the nasal cavity, perforation of the nasal septum, dysphonia.

Immune system disorders:

infrequently: immediate and delayed hypersensitivity reactions type (including urticaria, rash, dermatitis, itching, angioedema);

rarely: anaphylactic reactions.

Disorders from the endocrine system:

rarely: signs and symptoms of systemic effects of glucocorticosteroids, including suppression of adrenal function and growth retardation.

Disorders from the side of the organ of vision:

frequency is unknown: cataract, glaucoma.

Disorders from the gastrointestinal tract (GI tract):

often: dryness of the oral mucosa.

Disturbances from the musculoskeletal and connective tissue:

infrequently: muscular spasm;

rarely: osteoporosis (with long-term treatment).

General disorders and disorders at the site of administration:

infrequently: Candidiasis of the nasal cavity and upper respiratory tract, with prolonged use - atrophy of the mucous membrane of the nasal cavity;

rarely: hemorrhage in the mucosa due to improper use of the device.

Some of the ENT symptoms can be masked due to the use of glaucocorticosteroids.

Overdose:

Accidental overdose of the drug Budostera® in the dosage form of nasal dosed spray does not cause any obvious symptoms.

Acute overdose is unlikely.

With prolonged use of high doses, as well as with the simultaneous administration of other glucocorticosteroids, symptoms of hypercorticism may appear. In this case, the drug should be stopped, gradually reducing its dose.

Interaction:

For budesonide, interactions with drugs used to treat rhinitis have not been demonstrated. In the metabolism of budesonide, the main role is played by isoenzyme CYP3A4. Inhibitors of this isoenzyme, such as ketoconazole and itraconazole, may increase the risk of systemic effects of budesonide several times. It is necessary to avoid the simultaneous use of budesonide with these drugs. If therapy with budesonide and these drugs is required, their use should be maximally time-separated. A dose reduction of budesonide may be required. Simultaneous use of Budoster ® with such potential inhibitors of isoenzyme CYP3A4, as ciclosporin and trolandomycin, can lead to a significant increase in the concentration of budesonide in blood plasma.

Simultaneous application of the preparation Budostera® with inducers of microsomal oxidation (phenobarbital, phenytoin, rifampicin) can reduce the effectiveness of the first.

Methandienone, estrogens and hormonal contraceptives enhance the action of budesonide. However, when budesonide and low-dose combined oral contraceptives no such effect was observed.

Special instructions:

It is recommended to avoid getting Budoster ® into the eyes!

With long-term administration of high doses of budesonide, the risk of systemic action of the drug can not be ruled out. The probability of systemic effects is much lower than when using oral corticosteroids. Individual differences are possible with the development of such effects. Potential systemic effects may include Cushing's syndrome, cushingoid symptoms, suppression of adrenal function, growth retardation in children and adolescents, decreased bone mineral density, hypo- or hypercorticoid symptoms, cataracts and glaucoma.Nausea, changes in taste, difficulty swallowing, anosmia, palpitations, nasal congestion, dizziness, headache, sore throat, conjunctival hyperemia, myalgia, drowsiness, coughing are also possible. There may be deviations in psychological and behavioral patterns, including psychomotor hyperactivity, sleep disturbance, anxiety, depression, or aggressiveness (especially in children).

When switching from treatment with systemic glucocorticosteroids to nasal spray treatment, due to the risk of developing adrenal insufficiency, caution is required for the recovery period functions of the hypothalamic-pituitary-adrenal system (GGNS) and gradual withdrawal of the drug (a gradual dose reduction for normalization of the function of the GGNS). At the stage of dose reduction, some patients may experience withdrawal symptoms of systemic glucocorticosteroids, such as muscle and / or joint pain, apathy and depression. If such symptoms are detected, a temporary increase in the dose of systemic glucocorticosteroids may be required, and subsequently - a further abolition at a slower rate.Because glucocorticosteroids slow the healing of wounds, caution should be exercised when prescribing Budostere® to patients who have recently undergone trauma or nose surgery. For a full therapeutic effect in allergic rhinitis, the drug should be used regularly. With prolonged therapy with Budostere®, an assessment of the nasal mucosa every 6 months is necessary. There were reported cases of growth retardation in children receiving glucocorticosteroids for nasal administration at therapeutic doses.

With prolonged use of glucocorticosteroids for nasal administration in children, it is recommended to carry out dynamic growth control. If the growth slows down, the pediatrician should reconsider the method of using the drug in order to reduce the dose and transition to a minimum therapeutic dose, at which control over the symptoms of the disease is possible.

The use of nasal glucocorticosteroids in doses exceeding the recommended ones can lead to a significant inhibition of adrenal function. In this case, the need for additional use of systemic glucocorticosteroids in the period of adrenal function reduction or planned surgery should be considered.

Violation of the function of the liver can lead to a decrease in the excretion of corticosteroids and contribute to an increased likelihood of systemic exposure.

Since the function of the adrenal glands can be reduced, the adrenocorticotropic hormone stimulation test to detect abnormalities in the pituitary gland may produce incorrect (underestimated) results.

Caution should be exercised when using Budostere®in patients with a latent form of tuberculosis, as well as in infections of fungal and viral etiology.

Patients taking the drug Budostere® should be informed that the full effect develops a few days after the start of the drug.

Effect on the ability to drive transp. cf. and fur:

The use of budesonide does not affect the ability to drive vehicles, mechanisms.

Form release / dosage:

Spray nasal dosed, 50 mcg in a dose and 100 mcg in a dose.

Packaging:

For 200 doses in a vial of dark glass with a metering valve, crimped aluminum ring, closed protective cap. Po 1 bottle in a pack of cardboard along with instructions for use.

Storage conditions:

2 years. After opening the bottle, the shelf life is 3 months.Do not use after the expiry date printed on the package.

Shelf life:

Store at a temperature not exceeding 25 ° C. Do not freeze. Keep out of the reach of children.

Terms of leave from pharmacies:On prescription

Registration number:LP-001115

Date of registration:03.11.2011 / 07.03.2017

Expiration Date:Unlimited

The owner of the registration certificate:Sentiss Pharma Pvt. Ltd.Sentiss Pharma Pvt. Ltd. India

Manufacturer: & nbsp

MIPHARM, S.P.A. Italy

Representation: & nbspSENTISS RUSS LLCSENTISS RUSS LLCRussia

Information update date: & nbsp06.06.2017

Illustrated instructions

Instructions

Budostere® (Budoster®)