Release form, composition and packing
Aerosol metered dose for inhalation as a clear, colorless solution; aluminum inhaler must be hermetically sealed with a metering valve and have no signs of corrosion. 1 dose of beclomethasone dipropionate 50 micrograms. Other ingredients: glycerol, ethanol, anhydrous, norfluran (HFA-134a).
Aerosol metered dose for inhalation as a clear, colorless solution; aluminum inhaler must be hermetically sealed with a metering valve and have no signs of corrosion. 1 dose of beclomethasone dipropionate 250 mcg. Other ingredients: glycerol, ethanol, anhydrous, norfluran (HFA-134a).
Clinico-pharmacological group: corticosteroids for inhalation.
Pharmacological action
Corticosteroids for inhalation use. Beclomethasone dipropionate is a prodrug with weak tropic to GCS receptors. Under the action of esterases, it is converted into an active metabolite - beclomethasone-17-monopropionat, which has a pronounced local anti-inflammatory effect.
Pharmacokinetics
Suction
Inhalation method of administration (via metered-dose inhaler) are absorbed unchanged beclomethasone dipropionate into the systemic circulation through the lungs with negligible absorption of swallowed drug. Even before the intake occurs predominantly rotation beclomethasone dipropionate in its active metabolite beclomethasone-17-monopropionat. Systemic absorption occurs from the lungs and from the gastrointestinal tract by ingested part of the drug. The absolute bioavailability of beclomethasone-17-monopropionat from the lungs is approximately 60% of normal dose. Beclomethasone dipropionate is rapidly absorbed, its Cmax plasma levels observed after 0.3 h. The plasma concentration of beclomethasone-17-monopropionata grows slowly, Tmax was 1 hour
Increasing doses of inhaled accompanied by almost linear increase in systemic drug concentrations. Bioavailability of beclomethasone dipropionate by ingestion is negligible, but the bioavailability is formed in the digestive tract of beclomethasone-17-monopropionata is 40%.
Metabolism
Beclomethasone dipropionate is rapidly metabolized esterases that are present in most tissues. The main product of metabolism is the active metabolite beclomethasone-17-monopropionat. Form and inactive secondary metabolites beclomethasone-21-monopropionat and beclomethasone, but they are not an essential part of system maintenance drug.
Distribution
In equilibrium, Vd beclomethasone dipropionate is an average of 20 liters, beclomethasone-17-monopropionata much higher - 424 liters. Binding to plasma proteins is relatively high - 87%.
Breeding
The elimination of beclomethasone dipropionate and beclomethasone-17-monopropionata characterized by high plasma clearance (150 l / h and 120 l / h, respectively), with T1 / 2 0.5 h and 2.7 h, respectively.
If ingestion of approximately 60% of the dose of beclomethasone dipropionate is excreted in feces mainly in the form of free and conjugated polar metabolites within 96 hours with urine output of approximately 12% of the dose in the form of free and conjugated polar metabolites. Renal clearance of beclomethasone dipropionate and its metabolites is negligible.
Statement
basic therapy of bronchial asthma in adults and children over 4 years.
Dosing regimen
Bekotid intended only for inhalation use. Bekotida dose should be set individually.
Adults and children older than 12 years: the drug is prescribed in the initial dose, which depends on the severity of the disease. Bronchial asthma, lung flow - 200-600 mg / day in divided doses. Bronchial asthma, moderate flow - 600-1000 mg / day in divided doses.
Bronchial asthma is severe - 1000-2000 mg / day in divided doses. Depending on the individual response dose can be increased or reduced to optimum effect. Children aged 4 years and older: 400 mcg / day in divided doses.
Bekotid children should receive the initial dose, corresponding to the severity of their condition. Depending on the individual patient response, dose may be increased or reduced to optimum effect. The maximum daily dose is 500 mcg. Elderly patients and patients with renal or hepatic impairment dose adjustment is required.
Patients should be aware of the preventative action of the drug and the need for its regular use even in the absence of asthma symptoms. If a patient believes that short-acting bronchodilators are less effective or it needs more inhalations than usual, he should consult a doctor. If patients find it difficult to coordinate pressing the canister dispensing inhaler with inhalation, can be inhaled via a spacer Bekotid.
When treating young children for inhalation Bekotida more convenient to use a spacer "Baby-haler.
Side effect
The frequency of adverse reactions is presented in accordance with the following gradation: very common (≥ 10%), frequent (≥ 1% and <10%), sometimes (≥ 0.1% and <1%), rarely (≥ 0.01%, <0.1%) very rare (<0.01%).
Local reactions: very common - candidiasis of the mouth and throat (thrush), which increases the likelihood of the application Bekotida in doses exceeding 400 micrograms per day. Most likely to develop this complication in patients with high levels of antibodies to Candida in the blood, indicating that the pre-infection.
Some assistance in prevention could have a mouth rinse with water after each use of an inhaler. For the treatment of candidiasis during ongoing therapy Bekotidom antifungal properties can be used for topical application. Allergic reactions: sometimes - rash, urticaria, pruritus, erythema, very rare - swelling of the eyes, face, lips, pharynx.
On the part of the endocrine system: very rarely - Cushing's syndrome, Kushingoid appearance, suppression of the adrenal cortex, growth retardation in children and adults, reduced bone mineral density.
CNS: very rare - anxiety, sleep disturbances, behavior changes, including hyperactivity and irritability (predominantly in children).
Part of the respiratory system: often - hoarseness, throat irritation.
Some benefit in this case could have a mouth rinse with water immediately after inhalation. The use of a spacer reduces the likelihood of these side effects.
Very rare - a paradoxical bronchospasm, which manifests increased wheezing after ingalirovaniya drug. This state should be immediately docked by using fast-acting inhaled bronchodilator.
Application Bekotida should cease immediately and if necessary, appoint an alternative therapy.
On the part of the vision: cataract, glaucoma.
Contraindications
hypersensitivity to the drug.
Pregnancy and lactation
Use of the drug during pregnancy and lactation (breastfeeding) is possible only if the potential benefit to the mother outweigh the risks to the fetus or nursing child.
Use in hepatic dysfunction
Patients with hepatic impairment dose adjustment is required.
Use in renal impairment
Patients with renal impairment dose adjustment is required. Special instructions Bekotid not a means of relief of acute asthma attacks, and is used for regular treatment. Treatment of asthma should be conducted in accordance with the step program. Effect of treatment should be monitored clinically and by investigations of respiratory function.
Increased demand for acceptance of short β2-agonists adrenretseptorov to control symptoms indicate a worsening condition. In this case the patient's treatment plan should be reviewed.
In case of insufficient efficacy or severe exacerbation of asthma is necessary to increase doses of inhaled Bekotida and, if necessary, the appointment of systemic corticosteroids, and in the presence of infection - antibiotics. Sudden and progressive deterioration of asthma symptoms is a potentially life-threatening condition and requires increasing doses of corticosteroids. Necessary to verify implementation of patient inhalation technique, to be sure that pressing on the inhaler canister is synchronized with the breath and provides a smooth delivery of the drug into the lungs.
Systemic effects may occur when using any inhaled corticosteroids, especially for prolonged use at high doses. These effects were significantly more likely to develop in the appointment of oral corticosteroids. It is therefore particularly important to select the minimum dose of inhaled corticosteroids in control of the disease. Due to the possible dysfunction of the adrenal cortex of patients with the translation of treatment with oral forms of inhaled steroids on Bekotid should be under close medical supervision and regular monitoring of adrenal function.
With the addition of inhaled Bekotida discontinuation systemic steroids should be gradual, and ill recommend carry a warning card, which indicates that in stressful situations, the patient needs additional systemic corticosteroids. Sometimes translated from systemic corticosteroids to inhalation may lead to the appearance of previously repressed forms of allergy, such as allergic rhinitis or eczema.
Not recommended drastic cancellation Bekotida. As with the appointment of other inhaled corticosteroids, should be particularly careful when treating patients with active or inactive pulmonary tuberculosis. The product contains small amounts of ethanol and glycerol. In the range of therapeutic doses of the content of these substances is extremely low and poses no danger to patients. Daily administration of the propellant HFA-34a, which does not contain freon, different kinds of animals over 2 years showed that the substance used has no toxic effects even at very high concentrations far exceeding those that can be used by patients.
Aerosol metered dose for inhalation as a clear, colorless solution; aluminum inhaler must be hermetically sealed with a metering valve and have no signs of corrosion. 1 dose of beclomethasone dipropionate 50 micrograms. Other ingredients: glycerol, ethanol, anhydrous, norfluran (HFA-134a).
Aerosol metered dose for inhalation as a clear, colorless solution; aluminum inhaler must be hermetically sealed with a metering valve and have no signs of corrosion. 1 dose of beclomethasone dipropionate 250 mcg. Other ingredients: glycerol, ethanol, anhydrous, norfluran (HFA-134a).
Clinico-pharmacological group: corticosteroids for inhalation.
Pharmacological action
Corticosteroids for inhalation use. Beclomethasone dipropionate is a prodrug with weak tropic to GCS receptors. Under the action of esterases, it is converted into an active metabolite - beclomethasone-17-monopropionat, which has a pronounced local anti-inflammatory effect.
Pharmacokinetics
Suction
Inhalation method of administration (via metered-dose inhaler) are absorbed unchanged beclomethasone dipropionate into the systemic circulation through the lungs with negligible absorption of swallowed drug. Even before the intake occurs predominantly rotation beclomethasone dipropionate in its active metabolite beclomethasone-17-monopropionat. Systemic absorption occurs from the lungs and from the gastrointestinal tract by ingested part of the drug. The absolute bioavailability of beclomethasone-17-monopropionat from the lungs is approximately 60% of normal dose. Beclomethasone dipropionate is rapidly absorbed, its Cmax plasma levels observed after 0.3 h. The plasma concentration of beclomethasone-17-monopropionata grows slowly, Tmax was 1 hour
Increasing doses of inhaled accompanied by almost linear increase in systemic drug concentrations. Bioavailability of beclomethasone dipropionate by ingestion is negligible, but the bioavailability is formed in the digestive tract of beclomethasone-17-monopropionata is 40%.
Metabolism
Beclomethasone dipropionate is rapidly metabolized esterases that are present in most tissues. The main product of metabolism is the active metabolite beclomethasone-17-monopropionat. Form and inactive secondary metabolites beclomethasone-21-monopropionat and beclomethasone, but they are not an essential part of system maintenance drug.
Distribution
In equilibrium, Vd beclomethasone dipropionate is an average of 20 liters, beclomethasone-17-monopropionata much higher - 424 liters. Binding to plasma proteins is relatively high - 87%.
Breeding
The elimination of beclomethasone dipropionate and beclomethasone-17-monopropionata characterized by high plasma clearance (150 l / h and 120 l / h, respectively), with T1 / 2 0.5 h and 2.7 h, respectively.
If ingestion of approximately 60% of the dose of beclomethasone dipropionate is excreted in feces mainly in the form of free and conjugated polar metabolites within 96 hours with urine output of approximately 12% of the dose in the form of free and conjugated polar metabolites. Renal clearance of beclomethasone dipropionate and its metabolites is negligible.
Statement
basic therapy of bronchial asthma in adults and children over 4 years.
Dosing regimen
Bekotid intended only for inhalation use. Bekotida dose should be set individually.
Adults and children older than 12 years: the drug is prescribed in the initial dose, which depends on the severity of the disease. Bronchial asthma, lung flow - 200-600 mg / day in divided doses. Bronchial asthma, moderate flow - 600-1000 mg / day in divided doses.
Bronchial asthma is severe - 1000-2000 mg / day in divided doses. Depending on the individual response dose can be increased or reduced to optimum effect. Children aged 4 years and older: 400 mcg / day in divided doses.
Bekotid children should receive the initial dose, corresponding to the severity of their condition. Depending on the individual patient response, dose may be increased or reduced to optimum effect. The maximum daily dose is 500 mcg. Elderly patients and patients with renal or hepatic impairment dose adjustment is required.
Patients should be aware of the preventative action of the drug and the need for its regular use even in the absence of asthma symptoms. If a patient believes that short-acting bronchodilators are less effective or it needs more inhalations than usual, he should consult a doctor. If patients find it difficult to coordinate pressing the canister dispensing inhaler with inhalation, can be inhaled via a spacer Bekotid.
When treating young children for inhalation Bekotida more convenient to use a spacer "Baby-haler.
Side effect
The frequency of adverse reactions is presented in accordance with the following gradation: very common (≥ 10%), frequent (≥ 1% and <10%), sometimes (≥ 0.1% and <1%), rarely (≥ 0.01%, <0.1%) very rare (<0.01%).
Local reactions: very common - candidiasis of the mouth and throat (thrush), which increases the likelihood of the application Bekotida in doses exceeding 400 micrograms per day. Most likely to develop this complication in patients with high levels of antibodies to Candida in the blood, indicating that the pre-infection.
Some assistance in prevention could have a mouth rinse with water after each use of an inhaler. For the treatment of candidiasis during ongoing therapy Bekotidom antifungal properties can be used for topical application. Allergic reactions: sometimes - rash, urticaria, pruritus, erythema, very rare - swelling of the eyes, face, lips, pharynx.
On the part of the endocrine system: very rarely - Cushing's syndrome, Kushingoid appearance, suppression of the adrenal cortex, growth retardation in children and adults, reduced bone mineral density.
CNS: very rare - anxiety, sleep disturbances, behavior changes, including hyperactivity and irritability (predominantly in children).
Part of the respiratory system: often - hoarseness, throat irritation.
Some benefit in this case could have a mouth rinse with water immediately after inhalation. The use of a spacer reduces the likelihood of these side effects.
Very rare - a paradoxical bronchospasm, which manifests increased wheezing after ingalirovaniya drug. This state should be immediately docked by using fast-acting inhaled bronchodilator.
Application Bekotida should cease immediately and if necessary, appoint an alternative therapy.
On the part of the vision: cataract, glaucoma.
Contraindications
hypersensitivity to the drug.
Pregnancy and lactation
Use of the drug during pregnancy and lactation (breastfeeding) is possible only if the potential benefit to the mother outweigh the risks to the fetus or nursing child.
Use in hepatic dysfunction
Patients with hepatic impairment dose adjustment is required.
Use in renal impairment
Patients with renal impairment dose adjustment is required. Special instructions Bekotid not a means of relief of acute asthma attacks, and is used for regular treatment. Treatment of asthma should be conducted in accordance with the step program. Effect of treatment should be monitored clinically and by investigations of respiratory function.
Increased demand for acceptance of short β2-agonists adrenretseptorov to control symptoms indicate a worsening condition. In this case the patient's treatment plan should be reviewed.
In case of insufficient efficacy or severe exacerbation of asthma is necessary to increase doses of inhaled Bekotida and, if necessary, the appointment of systemic corticosteroids, and in the presence of infection - antibiotics. Sudden and progressive deterioration of asthma symptoms is a potentially life-threatening condition and requires increasing doses of corticosteroids. Necessary to verify implementation of patient inhalation technique, to be sure that pressing on the inhaler canister is synchronized with the breath and provides a smooth delivery of the drug into the lungs.
Systemic effects may occur when using any inhaled corticosteroids, especially for prolonged use at high doses. These effects were significantly more likely to develop in the appointment of oral corticosteroids. It is therefore particularly important to select the minimum dose of inhaled corticosteroids in control of the disease. Due to the possible dysfunction of the adrenal cortex of patients with the translation of treatment with oral forms of inhaled steroids on Bekotid should be under close medical supervision and regular monitoring of adrenal function.
With the addition of inhaled Bekotida discontinuation systemic steroids should be gradual, and ill recommend carry a warning card, which indicates that in stressful situations, the patient needs additional systemic corticosteroids. Sometimes translated from systemic corticosteroids to inhalation may lead to the appearance of previously repressed forms of allergy, such as allergic rhinitis or eczema.
Not recommended drastic cancellation Bekotida. As with the appointment of other inhaled corticosteroids, should be particularly careful when treating patients with active or inactive pulmonary tuberculosis. The product contains small amounts of ethanol and glycerol. In the range of therapeutic doses of the content of these substances is extremely low and poses no danger to patients. Daily administration of the propellant HFA-34a, which does not contain freon, different kinds of animals over 2 years showed that the substance used has no toxic effects even at very high concentrations far exceeding those that can be used by patients.
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