Foster aerosol for inhalation 120 doses
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Active ingredients
Beclomethasone + Formoterol
Release form
Spray
Composition
Beclomethasone dipropionate 100 mcgformoterol fumarate 6 mcg
Pharmacological effect
Foster contains beclomethasone dipropionate and formoterol, which have different mechanisms of action and exhibit an additive effect in reducing the frequency of exacerbations of bronchial asthma. Beclomethasone dipropionate is an inhalation GCS, in recommended doses it has an anti-inflammatory effect, reduces the severity of symptoms of bronchial asthma, and reduces the incidence of asthma and reliance. lower frequency of side effects than systemic corticosteroids. Formoterol is a selective β2-adrenoreceptor agonist, causing relaxation e smooth bronchial muscles in patients with reversible airway obstruction. Bronchodilatory effect occurs quickly, within 1-3 minutes after inhalation, and lasts for 12 hours after a single dose inhalation. Adding formoterol to beclomethasone dipropionate reduces the severity of asthma symptoms, improves the performance of external respiratory function (LFD) and reduces the frequency of exacerbations of the disease. In the course of a clinical study, it was shown that the effect on FER of a fixed combination of Foster corresponds to that of the combination of beclomethasone monopreparations and formoterol and exceeds The action of beclomethasone dipropionate.
Pharmacokinetics
Pharmacokinetic indicators for the respective drugs were comparable after administration of beclomethasone dipropionate (BDP) and formoterol as monodrugs and as part of a combined preparation. For beclomethasone dipropionate, when given as part of the combined preparation AUC for its active metabolite, beclomethasone-17-monopropionate and Cmax value slightly lower, and absorption is faster than that of beclomethasone dipropionate monopreparation. For formoterol, when administered as part of a combined preparation arata Cmax in plasma coincided with that for a monodrug, and the systemic effect was slightly higher than that of a monodrug. Data on pharmacokinetic or pharmacodynamic interaction between BDP and formoterol were not obtained: BDP turns into an active metabolite, beclomethasone-17-monopropionate (B- 17 MP). The inhalable BDP is rapidly absorbed by the lungs; its absorption is preceded by an intense conversion of BDP into its active metabolite beclomethasone-17-monopropionate (B-17 MP).Systemic bio-potency (B-17 MP) is provided by 36% at the expense of the lungs, as well as by absorption by the gastrointestinal tract by the swallowed part of the inhalation dose. The bioavailability of the ingested BDP is negligible, however, the presystemic conversion of BDP to B-17 MP leads to the fact that 41% of BDP is absorbed by the body as B-17 MP. There is almost a linear increase in systemic effects with increasing inhalation dose. Absolute bioavailability after inhalation is about 2% and 62% of the nominal dose in relation to unchanged BDP y and B-17 MP, respectively. Binding to plasma proteins is quite high. Metabolism of BDP is characterized by a very high clearance rate from the large circulation through the esterase, present in most tissues. The main product of BDP metabolism is the active metabolite B-17 MP. The less active metabolites are beclomethasone 21 monopropionate (B-21 MP) and beclomethasone (VON), which are also formed as a result of metabolism, but their role in the systemic effects of BDP is very small. ExcretionThe main part of BDP is excreted with feces in the form of polar metabolites. Renal excretion of BDP and its metabolites is negligible. T1 / 2 BDP and B-17 MP is 0.5 and 2.7 h, respectively. Pharmacokinetics in special clinical situations. Hepatic failure does not alter the pharmacokinetic properties and safety profile of BDP due to the fact that the latter undergoes rapid metabolism to the B-21 MP polar metabolites. , VON and B-17 MP under the action of enzymes present in the gastrointestinal tract, plasma, lungs and liver. The pharmacokinetic properties of BDP in patients suffering from renal failure have not been studied. Taking into account that both the BDP and its metabolites are practically not excreted in the urine, there is no reason to suggest an increase in the systemic effect of the drug on the organism of patients suffering from renal failure. Formoterol Absorption and distribution Inhalable formoterol is absorbed in the lungs and gastrointestinal tract. The part of the inhalation dose that is swallowed depends on the type of inhalation device. and inhalation techniques. So when using a multi-dose metered-dose inhaler, it can be up to 90%. Therefore, the swallowed fraction must be considered when injecting the drug. Not less than 65% of the oral dose of frmoterol is absorbed through the gastrointestinal tract, while 70% of this volume is subjected to systemic metabolism.Cmax of unchanged formoterol in plasma is observed within 0.5–1 h after oral administration. Communication with plasma proteins in formoterol is 61-64%, while the affinity to albumin - 34%. In the range of therapeutic doses, affinity saturation is not observed. With peroral intake, T1 / 2 is 2-3 hours. With inhalation of 12-96 μg of formoterol fumarate, absorption of formoterol is linear. Metabolism Formoterol metabolism is carried out, in particular, by direct conjugation of the phenol-hydroxyl group. Glucuronic acid conjugates are not active. The second significant metabolic pathway of formoterol is O-dimethylation via conjugation at the level of the phenol-2-hydroxyl group. Cytochrome P450 enzymes CYP2D6, CYP2C9, CYP2C19 is involved in O-demethylation of formoterol. There is reason to assume that the metabolism of formoterol is carried out mainly in the liver. Formoterol does not inhibit CYP450 enzymes in therapeutically significant concentrations. Injection The total renal excretion of formoterol after a single dose inhalation through a metered dose powder inhaler increases linearly in the dose range of 12-96 μg. Excretion rates of unchanged and total formoterol, on average, are 8% and 25%, respectively. Based on measurements of plasma concentrations of formoterol after its single inhalation at a dose of 120 μg in 12 healthy volunteers, T1 / 2 was determined, which was 10 hours. The ratio of (R, R) - and (S, S) -enantiomers of the unchanged drug with renal excretion is respectively, 40% and 60%. The relative ratio of these 2 indicators does not change in the range of studied dosages; there is no evidence of accumulation of one enantiomer relative to another after administration, repeated dose. In healthy volunteers after oral administration (40-80 mcg), 6-10% of the dose was found in the urine as an unchanged drug; 8% of the dose was present in the form of glucuronides. Only 67% of the oral dose of formoterol is excreted by the kidneys (mainly in the form of metabolites), the rest of the dose — through the intestine. Renal clearance of formoterol is 150 ml / min.
Indications
Basic therapy of bronchial asthma, which involves the appointment of combination therapy (inhaled GCS and long-acting β2-adrenergic mimicking): - patients, symptoms of the disease that are not sufficiently controlled by inhaled GCS and short-acting β2-adrenomimetics; long-acting adrenergic mimetics.
Contraindications
- children's age up to 12 years; - hypersensitivity to the components of the drug. With caution: pregnancy, lactation, pulmonary tuberculosis, fungal, viral or bacterial respiratory infections, thyrotoxicosis, pheochromocytoma, diabetes, uncontrolled hypokalemia, idiopathic hypertrophic subaortic stenosis, AV - III degree blockade, severe arterial hypertension, aneurysm of any localization or other severe cardiovascular diseases (acute myocardial infarction, ischemic heart disease, tachyarrhythmia, decompensiro ƈ This chronic heart failure, elongate QTs interval (reception formoterol can cause elongation of QTc interval).
Precautionary measures
During treatment, psoriasis may worsen. During pheochromocytoma, propranolol can only be used after taking an alpha blocker. After a long course of treatment, propranolol should be discontinued gradually, under the supervision of a physician. during anesthesia, you must stop taking propranolol or find a remedy for anesthesia with minimal negative inotropic effects. The impact on the ability to drive vehicles and control mechanisms of patients whose activities require increased attention, the question of the use of propranolol on an outpatient basis should be addressed only after evaluating the individual response of the patient.
Use during pregnancy and lactation
There is no clinical data on the use of Foster during pregnancy. In animal studies, no embryotoxic or teratogenic effects have been identified. In pregnancy, Foster should be used only in cases where the benefits of using the drug outweigh the potential risk to the fetus. It is recommended to prescribe a minimum dose that provides effective control of symptoms of bronchial asthma. There is no data on the penetration of Foster into the breast milk of women. Foster can be administered to lactating women only in cases where the expected therapeutic effect for the mother outweighs the potential risk to the baby.
Dosage and administration
Foster is not intended for the initial treatment of bronchial asthma.Selection of the dose of drugs that are part of Foster, occurs individually and depending on the severity of the disease. This must be considered not only when starting treatment with combined preparations, but also when changing the maintenance dose of the preparation. In the event that an individual requires a different combination of doses of active ingredients than in Foster, β2-adrenomimetics and / or GCS in separate inhalers should be prescribed. For adults and patients over 12 years old: 1-2 inhalations 2 times / day. Patients should be under the constant supervision of a physician for adequate selection of the dose of Foster. The dose should be reduced to the lowest, against which the optimal control of the symptoms of bronchial asthma is maintained. When achieving complete control over the symptoms of bronchial asthma on the background of the minimum recommended dose of the drug, in the next stage, you can try the appointment of monotherapy with inhaled GCS. There is no need for special selection of the drug dose for elderly patients. on the use of the inhaler. The patient must be taught how to use the inhaler correctly and periodically check the inhalation technique. Before the first use By inhalation of the inhaler or 3 days or more after a break in its use, the first dose must be sprayed into the air to make sure that it works. Take the inhaler with your thumb and forefinger. Remove the protective cap from the inhaler mouthpiece. Take the mouthpiece in your mouth, tightly clasping his lips, and completely exhale through the nose. Make a long deep breath, while simultaneously pressing the tip of the cartridge with your index finger.5. After inhaling, hold your breath for as long as possible. Then remove the mouthpiece from the mouth and continue to breathe normally. To receive the second dose: hold the inhaler upright, wait about 30 seconds and then repeat steps 3 through 5. After using the cap tightly close the mouthpiece. When performing steps 3 and 4, you should not hurry . Inhale as slowly as possible, immediately before pressing the valve on the inhaler. If the gas partially comes out of the upper part of the inhaler or from the corners of the patient’s mouth, repeat the procedure from step 3. It is more convenient for patients with weak hands to hold the inhaler with two hands.Therefore, the upper part of the inhaler should be held with two index fingers and its lower part with the thumbs. After inhalation, it is recommended to rinse your mouth with water. To keep the mouthpiece clean, it is recommended to rinse it with warm water as it is contaminated. There are no clinical data on the use of Foster with a spacer; therefore, the recommended dosage of the drug is given in view of the fact that an inhaler without a spacer with a standard activator is used. It should be borne in mind that when using Foster with a spacer, it may be necessary to adjust the dose.
Side effects
Foster contains beclomethasone dipropionate and formoterol fumarate, and therefore it can be expected that it can cause side effects characteristic of these components. There is no evidence that their simultaneous use causes additional side effects. Side effects associated with the use of beclomethasone dipropionate and formoterol as a fixed combination (Foster) are presented below. From the side of the CNS: often - headache. From the side of the respiratory system: often - hoarseness; less often - rhinitis, dysphonia, cough, slight irritation in the throat, bronchospasm. On the cardiovascular system: less often - heartbeat, prolongation of the QT interval, ECG change. On the musculoskeletal system: tremor, muscle cramps. On the side of the system hematopoiesis: granulocytopenia, an increase in the number of platelets. On the part of the digestive system: dry mouth, burning sensation in the lips, dysphagia, dyspepsia, diarrhea. On the part of the immune system: allergic dermatitis; increase in C-reactive protein. Metabolic disorders: hypokalemia. Infections: pharyngitis, flu, candidiasis of the oral mucosa, pharynx and esophagus, vaginal candidiasis, gastroenteritis, sinusitis. Among the most frequent side effects associated with formoterol, such typical for beta2 adrenomimetic drugs such as hypokalemia, headache, tremor, palpitations, cough, muscle cramps, lengthening of the QTc interval. Side effects typical of beclomethasone dipropionate: candidiasis of the oral mucosa and hl otki, irritation in the throat. Like other inhalants,Foster may cause paradoxical bronhospazm.Drugie side effects typical of formoterol thrombocytopenia, angioneurotic edema, hyperglycemia, increased blood levels of insulin, free fatty acids, glycerol and ketone derivatives, sleep disorders, hallucination, fatigue, restlessness, changes in taste (dysgeusia ), tachycardia, tachyarrhythmia, ventricular premature beats, angina pectoris, atrial fibrillation, arterial hypertension, arterial hypotension, exacerbation of asthma, shortness of breath , Nausea, itching, skin rash, hives, rash, myalgia, nephritis, peripheral oteki.Sistemnye GCS effects (including beclomethasone dipropionate) occur at high doses for long time. They include: suppression of adrenal function, decrease in bone mineral density, growth retardation in children and adolescents, glaucoma, and cataracts. Hypersensitivity reactions include: itching, skin rash, erythema, and swelling of the eyes, face, lips, and throat.
Overdose
Symptoms: in case of overdose symptoms of formoterol caused by beta2-adrenergic mimics occur, such as nausea, vomiting, headache, tremor, drowsiness, heart palpitations, tachycardia, ventricular arrhythmia, lengthening of the QTc interval, metabolic acidosis, hypocholymia, metabolic acidosis, hypocholymia, rash, heart failure, tachycardia, ventricular arrhythmia, lengthening of the QTc interval, metabolic acidosis treatment. In severe cases, hospitalization. The use of cardioselective beta-blockers may be considered with caution, since the use of these agents may cause bronchospasm. It is necessary to monitor the level of potassium in the blood plasma. Inhibiting doses of beclomethasone dipropionate higher than recommended can cause a temporary inhibition of the function of the adrenal cortex. This usually does not require any emergency measures, since in most cases the normal function of the adrenal glands is restored within a few days. It is recommended to monitor the level of cortisol in the blood plasma. In case of chronic intake of excessive doses of beclomethasone dipropionate, its systemic effect may appear: there may be significant inhibition of the adrenal cortex until adrenal crisis.Acute adrenal crisis is manifested by hypoglycemia, accompanied by confusion and / or convulsions. The situations that can serve as trigger factors for acute adrenal crisis include trauma, surgery, infection, or a rapid reduction in the dose of beclomethasone, which is part of the Foster. In chronic overdose, it is recommended to monitor the reserve function of the adrenal cortex.
Interaction with other drugs
Beta-adrenoreceptor blockers can weaken the effect of formoterol. Foster should not be administered simultaneously with beta-blockers (including eye drops), except in forced cases. When co-administered with Foster and other beta-adrenergic drugs, the side effects of formoterol may increase. (terfenadine), MAO inhibitors and tricyclic antidepressants can prolong the QTc interval and increase the risk of ventricular arrhythmias. In addition, levodopa, levothyrox n, oxytocin and alcohol can reduce the tolerance of the heart muscle to beta2-adrenomimetikam. The joint appointment of MAO inhibitors, as well as drugs with similar properties, such as furazolidone and procarbazine, may cause an increase in blood pressure. preparations of halogenated hydrocarbons. As a result of the use of beta2-adrenermimetics, hypokalemia may occur, which may increase with the concomitant treatment of xanthine derivatives, a miner lnymi derivatives corticosteroids, diuretics. Hypokalemia may increase the susceptibility to the development of arrhythmias in patients taking cardiac glycosides. Due to the content of a small amount of ethanol, interaction may occur in hypersensitive patients taking disulfiram or metronidazole.
special instructions
If patients have such comorbidities as coronary artery disease, myocardial infarction, exacerbation of arterial hypertension, cardiac arrhythmias, chronic heart failure, diabetes, prostatic hypertrophy, glaucoma, special precautions should be taken when choosing a dose of Foster. treatment of patients with prolonged QTc interval (QTc> 0.44 sec.). Acceptance of formoterol may cause prolongation of the QTc interval.Foster can be used in patients with tachyarrhythmia only with special precautions, such as ECG monitoring. Special precautions should be observed in patients with unstable asthma who use short-acting bronchodilators to relieve seizures during exacerbation of severe bronchial asthma, because The risk of hypokalemia increases on the background of hypoxia and in other conditions, when the likelihood of the development of a hypokalemic effect increases. In such cases, it is recommended to control serum potassium. Inhalations of high doses of formoterol can lead to an increase in blood glucose levels. During the treatment period, blood glucose concentration should be monitored in patients with diabetes mellitus. If anesthesia is planned with drugs of halogenated hydrocarbons, it is necessary to warn the patient not to use Foster for 12 hours before starting anesthesia. of the respiratory system. Due to the danger of developing an exacerbation, treatment with Foster should not be abruptly stopped, the dose of the drug should be reduced gradually and under the supervision of a physician. GDA patients are undergoing this treatment (inhaled or oral corticosteroids), it is necessary to continue without any change, even if there is improvement simptomov.Sohranenie symptoms of asthma or the need to increase the dose of Foster could indicate a worsening of bronchial asthma and the need to review treatment. To relieve acute attacks of bronchospasm, patients are advised to constantly carry short-acting beta2-adrenomimetics. The treatment with Foster should not be prescribed during exacerbation of bronchial asthma. In this connection, it is necessary to discontinue Foster therapy, review treatment tactics and, if necessary, prescribe alternative therapy. Any inhalation GCS can cause systemic effects, especially with long-term use in high doses; It should be noted, however, that the likelihood of developing these symptoms is much lower than in the case of treatment with oral corticosteroids.Possible systemic effects include depression of adrenal function, growth retardation in children and adolescents, reduced bone mineral density, cataracts and glaucoma. Considering the above, the dose of inhaled corticosteroids should be titrated to the minimum, which will ensure the maintenance of effective control. When chronic intake of excessive doses of beclomethasone dipropionate, its systemic effect may occur: there may be significant inhibition of the adrenal cortex until the adrenal crisis. Adrenal crisis is manifested by anorexia, abdominal pain, weight loss, fatigue, headache, nausea, vomiting, hypotension, hypoglycemia, accompanied by confusion and / or convulsions. The situations that can serve as trigger factors for an acute adrenal crisis include trauma, surgery, infection, or a rapid reduction in the dose of beclomethasone, which is part of the Foster. In case of chronic overdose, it is recommended to monitor the reserve function of the adrenal cortex. If there is reason to believe that, against the background of previous systemic treatment of the GCS, the adrenal function was impaired, precautions should be taken when transferring patients to Foster. The advantages of inhalation therapy usually minimize the need administration of oral corticosteroids, however, in patients discontinuing therapy with oral corticosteroids, insufficient function may persist for a long time. eyeglass cases. Patients who in the past needed emergency high-dose GCS or received long-term treatment with high-dose inhaled GCS may also be in this risk group. It is necessary to provide for an additional appointment of GCS during stress or surgery. It is recommended to instruct the patient about the need to rinse your mouth with water after inhalation of maintenance doses in order to prevent the risk of developing candidiasis of the mucous membrane of the oral cavity and pharynx. The balloon is under pressure: do not exposed to heat, do not pierce, do not throw into the fire, even empty. Use within 3 months from the start of use.