Beclomethasone

Pharmacological properties

beclomethasone dipropionate is a precursor of the active substance with a weak affinity for corticosteroids receptors. it is hydrolyzed by esterases with the formation of the active metabolite beclomethasone-17-monopropionate, which has a high local anti-inflammatory activity.

Pharmacokinetics In case of inhalation, systemic absorption of unchanged beclomethasone dipropionate occurs through the lungs with slight oral absorption of the dose that has entered the gastrointestinal tract. Before absorption, beclomethasone dipropionate is intensively converted to its active metabolite of beclomethasone-17-monopropionate. Systemic absorption of beclomethasone-17-monopropionate consists of absorption in the lungs and gastrointestinal tract. Absolute bioavailability with inhalation is approximately 60% of the administered dose for beclomethasone-17-monopropionate.

Beclomethasone dipropionate is very rapidly eliminated from the systemic circulation through metabolism involving esterases. The main product of metabolism is active beclomethasone-17-monopropionate.

The distribution volume of beclomethasone dipropionate in the plateau phase is moderate (20 L), however, for beclomethasone-17-monopropionate it is larger (424 l). Plasma protein binding is moderately high (87%).

Beclomethasone dipropionate and beclomethasone-17-monopropionate have a high plasma clearance (150 and 120 l / h), T_½ make up 0.5 and 2.7 hours. About 60% of the dose is excreted in the feces, 12% in the urine in the form of free and conjugated polar metabolites. The renal clearance of beclomethasone dipropionate and its metabolites is negligible.

Indications

Beclazone-eco, 100 mcg: prophylactic treatment for mild, moderate and severe chronic ba.

Beclazone-Eco, 250 mcg: treatment of severe asthma in adults, as well as the treatment of patients who need systemic steroids to adequately control asthma symptoms.

Application

The drug is prescribed only for oral inhalation. therapeutic effect is observed after treatment for several days and reaches a maximum after 2-3 weeks. when transferring a patient from other inhaled drugs to beclacone-eco, it is necessary to leave the same dose of beclomethasone dipropionate, which is then determined individually.

Beclazone-Eco, 100 mcg. For optimal results, Beklazon-Eco should be used regularly. The initial dose should correspond to the severity of the disease.

A minimum dose should be established at which effective BA control is ensured.

Adults and children over the age of 12 years: the initial dose is from 100 to 500 mcg / day (the maximum daily dose is 1000 mcg), depending on the severity of AD of the patient.

The maintenance dose is usually 200-400 mcg, evenly distributed throughout the day. If necessary, higher doses can be applied, up to 1000 mcg during the day.

Children aged 7–12 years: the initial dose is 100 mcg 2 times a day (the maximum daily dose is 200 mcg), depending on the severity of the patient’s AD.

If the symptoms of AD remain satisfactory, then the dose can be gradually reduced to the minimum effective dose, which provides effective control of AD.

Beclazone-Eco, 250 mcg. Patients should know that Beklazon-Eco should be used to prevent the disease and therefore it should be used regularly, even in the absence of asthma attacks.

The dose of the drug is corrected depending on the individual reaction.

If improvement after short-acting bronchodilators becomes less effective or requires more inhalations than usual, treatment should be reviewed.

The initial dose should correspond to the severity of the disease. For patients in need of a high dose of inhaled GCS, the initial dose should be 1000 mcg / day.The dose of the drug can then be corrected to achieve a control of AD symptoms or reduced to the minimum effective, depending on the individual response of the patient.

Adults and children over 12 years of age (including elderly patients): 1000 mcg / day; the dose can be increased to 2000 mcg / day. After stabilization of the patients condition, the dose can be reduced. The daily dose can be prescribed for 2; 3 or 4 doses.

For optimal results, Beklazon-Eco should be used regularly, even in the absence of symptoms.

Instructions for using inhalers

Check the operation of the inhaler before using it.

1. Remove the cap from the inhaler. Make sure that there is no dust or dirt in the outlet pipe.

2. Hold the can in an upright position with the index finger on the bottom, and the large one on top of the can. Shake the can up and down vigorously.

3. To exhale as fully as possible (without tension). Tightly hold the outlet tube of the spray can with your lips. Take a slow deep breath. At the beginning of the inhalation, press the index finger on the bottom of the spray can, releasing a dose of the medicine. Continue to inhale slowly and deeply.

4. Remove the inhaler tube from your mouth and hold your breath for 10 seconds or as long as you can do without tension. Exhale slowly.

5. If you need to take more than one dose of the medicine, wait about 1 minute and then repeat the action, starting from step 2. Put the cap on the inhaler again.

Do not rush while performing step 3. At the time of release of the dose, it is important to take a breath as slowly as possible.

Inhaler Care

1. Remove the aluminum can from the plastic case. Contact with water must be avoided.

2. Remove the protective cap.

3. Rinse the plastic case with the mouth applicator with hot water and dry well (without using direct heating).

4. After drying, put the can back into the plastic case, close the mouth applicator with a protective cap.

Wash the mouth applicator once a week.

Contraindications

Hypersensitivity to beclomethasone dipropionate or to any of the excipients.

Side effects

Infections and infestations: latent / opportunistic infections, candidiasis of the oral cavity and throat.

Disorders of the immune system: allergic reactions, including angioedema of the eyes, throat, lips and face; respiratory symptoms (dyspnea and / or bronchospasm with increased wheezing, cough) and anaphylactoid / anaphylactic reactions.

Disorders from the endocrine system: Cushings syndrome, cushingoid symptoms, inhibition of adrenal function (systemic effects), growth retardation in children and adolescents.

Disorders from the organ of vision: cataract, blurred vision, central serous retinopathy, glaucoma (systemic effect).

Respiratory system disorders: hoarseness, throat irritation, paradoxical bronchospasm.

Disorders from the skin and subcutaneous tissue: urticaria, rash, itching, erythema.

Disorders from the musculoskeletal system and connective tissue: a decrease in the mineral density of bone tissue (systemic effects).

Mental disorders: sleep disturbances, anxiety, depression, aggression, behavioral changes, including hyperactivity and arousal (mainly in children).

special instructions

Treatment for BA should be carried out according to a phased program, the patients condition should be regularly monitored both clinically and by determining indicators of external respiration function.

Increased frequency of administration / dose of bronchodilators (in particular, fast inhalation β₂agonists) in order to eliminate symptoms of asthma indicates a deterioration in asthma control. In these conditions, therapy must be reviewed.A sudden and progressive deterioration in asthma control is potentially life-threatening, therefore, the dose of corticosteroids should be increased. In patients at risk, peak flow measurement is required.

Beklazon-Eco is not intended for the relief of acute asthma attacks, but for long-term preventive treatment. To alleviate the condition in acute asthmatic attacks, fast and cortical inhaled bronchodilators should be used.

It is necessary to use the inhaler correctly in order to ensure that the drug enters the bronchi. Aerosol actuation should be synchronized with inhalation. An insufficient response to treatment or a severe exacerbation of AD requires an increase in the dose of Beklazon-Eco and, if necessary, the use of systemic steroids and / or antibiotics in the presence of infection.

When using inhaled corticosteroids, especially in high doses and for a long time, a systemic effect may occur, but significantly less than when taking oral steroids. A systemic effect can be manifested by Cushings syndrome, cushingoid symptoms, inhibition of the adrenal glands, growth retardation in children and adolescents, decreased bone mineralization, cataracts and glaucoma. Therefore, it is important that the dose of inhaled GCS be reduced to the minimum possible, which would support effective control of AD symptoms. In such patients, adrenal cortex function should be regularly monitored and the dose of the systemic steroid should be reduced with caution. Some patients experience malaise (i.e., headache, nausea, discomfort in the joints or muscles) during the phase of failure, despite maintaining or even improving respiratory function. They must be encouraged to further inhalation and to abandon the systemic steroid, unless there are objective signs of adrenal insufficiency. It is recommended to regularly monitor the growth of children using long-term treatment with inhaled GCS.

There is an individual hypersensitivity to inhaled corticosteroids.

The transfer of patients from oral corticosteroids to Beklazon-Eco requires special attention and constant monitoring of adrenal function, mainly because the restoration of adrenal cortex dysfunction caused by prolonged systemic treatment with steroids is slow. The patients condition should be moderately stable before starting Beklazon-Eco inhalation as an addition to the usual maintenance dose of a systemic steroid. After about 1 week, they begin the gradual withdrawal of the systemic steroid, reducing the daily dose by 1 mg of prednisolone or its equivalent for other corticosteroids, with at least weekly intervals.

Spirometric and clinical evaluation should be used for dose reduction during oral administration of GCS. Most patients can be successfully transferred to Beklazon-Eco while maintaining proper respiratory function, but special care is necessary in the first months after the transition, until the hypothalamic-pituitary-adrenal function is restored enough so that the patients body can cope with unforeseen cases, such as trauma , surgery or infection.

Due to the possibility of inhibition of adrenal function, the transfer of patients from oral GCS to Beklazon-Eco requires special attention and constant monitoring of adrenal function.

The process of switching to Beklazon-Eco and the termination of systemic therapy should be gradual and patients should have a special card with them warning about the need for additional administration of the systemic steroid during the stressful period, for example, in case of a severe asthmatic attack, severe intercurrent diseases, surgical interventions, injuries, they should also provide a supply of oral steroids for use in an unpredictable case, for example, with worsening AD symptoms due to infection, localization bathroom in the chest. The dose of Beclazone-Eco should be increased at this time, and after stopping the use of the systemic steroid, reduce it to a maintenance level.

Similarly, replacing systemic steroid therapy with inhalation can sometimes unmask allergic diseases such as allergic rhinitis or eczema, previously controlled by systemic steroid use. These allergic manifestations should be treated with antihistamines and / or topical drugs, including corticosteroids.

Treatment with Beklazon-Eco does not stop suddenly!

In patients with high levels of Candida precipitins in the blood, which indicate a history of infection, the development of candidiasis of the oral cavity and throat (candidal stomatitis) is more likely. For all patients, it may be helpful to rinse the mouth with water after using the inhaler.

As with other inhalation medications, a paradoxical bronchospasm may develop with rapidly growing shortness of breath after inhalation. In this case, you should immediately use fast-acting inhaled bronchodilators, immediately stop the inhalation of the drug Beklazon-Eco, conduct a patient examination and, if necessary, prescribe alternative therapy.

Patients should also be made aware that Beklazon-Eco will have to be used regularly to get the best results, even if they have no symptoms. Patients receiving treatment with Beklazon-Eco at 100 mcg / dose can be transferred directly to treatment with Beklazon-Eco at 250 mcg / dose (in the same total daily dose, if necessary, increase the dose to a maximum daily - 1000 mcg) . In most patients, there is no significant effect on the levels of free cortisone in blood plasma or urine until a dose of 1000 mcg / day is exceeded. Some patients who receive 2000 mcg / day of beclomethasone dipropionate have noted a decrease in the level of free cortisone in blood plasma or urine, although the short-term adrenal reserve remains unchanged. In any patient, the risk of developing adrenal suppression should be weighed against therapeutic benefits and measures should also be taken to provide support with systemic steroids in situations of prolonged stress.

As with other inhaled corticosteroids, special care is required when prescribing Beklazon-Eco to patients with active and latent pulmonary tuberculosis. GCS treatment can mask the symptoms of pulmonary tuberculosis and other bacterial, viral, and fungal infections of the respiratory tract. Possible reactivation of pulmonary tuberculosis. In the case of the appointment of the drug to patients with concomitant respiratory tract infections, they should be treated appropriately. With limitations, use the drug to treat patients with lung abnormalities, such as bronchiectasis and pneumoconiosis due to the possibility of fungal infection. After using the drug, rinse the oral cavity with water.

The drug should not be prescribed to patients with herpes simplex and asthmatic status. Particular care should be taken to minimize the use of local GCS in patients with immunosuppression.

The drug should be used with caution in patients with viral, bacterial and fungal infections of the eye or mouth, as well as the respiratory tract. In the case of a bacterial infection of the respiratory tract, the use of an appropriate antibiotic may be necessary.

Patients must be warned that the drug contains a small amount of ethanol. In therapeutic doses, the amount of ethanol is extremely small and does not pose a risk to patients.

The aerosol can contains liquid under the pressure of compressed gas, so it cannot be exposed to temperatures above 50 ° C, punch or break, even when it is probably empty. Do not refrigerate or refrigerate.

Medicines that are no longer needed should be disposed of in accordance with the internal regulations for the disposal of this type of product. These measures will help protect the environment.

Use during pregnancy or lactation. The safety of the drug Beklazon-Eco during pregnancy has not been fully established. Inhalation of beclomethasone may be accompanied by intrauterine growth retardation. When deciding on the use of beclomethasone during pregnancy, it is necessary to weigh the ratio of the expected benefits to the mother and the potential risk to the fetus.

Beclomethasone passes into breast milk, but in very small amounts. The purpose of the drug during lactation should be balanced taking into account the fact that the therapeutic benefit of using the drug should be greater than the possible risk to the fetus.

Children. Beklazon-Eco 100 mcg is not recommended for use in children under the age of 7 years due to insufficient data on its safety and effectiveness.

Beklazon-Eco 250 mcg is not recommended for children under 12 years of age.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. Does not affect.

Interactions

The simultaneous use of barbiturates, phenytoin or rifampicin can increase metabolism and reduce the effectiveness of oral glucocorticosteroids. the reaction to anticoagulants can be reduced and, in some cases, increased due to the action of oral glucocorticosteroids. the simultaneous use of oral glucocorticosteroids or diuretics that do not inhibit potassium, such as thiazides or furosemide, can cause excessive potassium loss. no interaction was reported with the use of beclacone-eco.

Beclazone-Eco contains a very small amount of ethanol, therefore, theoretically, in patients with hypersensitivity, interaction with simultaneous administration with disulfiram or metronidazole is possible.

Overdose

The acute toxicity of beclacone-eco is very low. the only harmful effect after inhalation of a large number of doses for a short time is the temporary inhibition of the hypothalamic-pituitary-adrenal function. in this case, special measures are not required. treatment should be continued at the recommended dose. restoration of the hypothalamic-pituitary-adrenal function occurs within 1-2 days.

However, when the drug is used in doses exceeding the recommended, for some time some suppression of adrenal gland function is possible in addition to inhibition of hypothalamic-pituitary-adrenal function. In such cases, it is necessary to check the adrenal gland reserve. The patient should be treated as steroid dependent and transferred to an appropriate maintenance dose of a systemic steroid such as prednisone. As soon as the patients condition stabilizes, he should be transferred to Beklazon-Eco by the method described in the SPECIAL INSTRUCTIONS section.

There is no specific treatment for an overdose of beclomethasone dipropionate. In case of overdose, maintenance therapy should be carried out with appropriate monitoring, if necessary. Further treatment - in accordance with the clinical condition or in accordance with local recommendations, if any.

Storage conditions

At a temperature not exceeding 25 ° c.