Buy Beclomethasone inhalation spray 250 mcg/dose, 200 doses
  • Buy Beclomethasone inhalation spray 250 mcg/dose, 200 doses

Beclomethasone

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2019-09-19
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Clinical Pharmacology

Beclomethasone dipropionate is a prodrug and has a weak tropism for GCS receptors. Under the action of esterases, it turns into an active metabolite, beclomethasone-17-monopropionate (B-17-MP), which has a pronounced local anti-inflammatory effect. Reduces inflammation by reducing the formation of chemotaxis substance (the effect on late allergy reactions), inhibits the development of an “immediate” allergic reaction (due to inhibition of arachidonic acid metabolite production and a decrease in inflammatory mediators from mast cells) and improves mucociliary transport. Under the action of beclomethasone, the number of mast cells in the bronchial mucosa decreases, the epithelium edema decreases, secretion of mucus by the bronchial glands, bronchial hyperreactivity, regional accumulation of neutrophils, inflammatory exudate and production of lymphokines, macrophage migration is inhibited, intensity of infiltration and granulation processes decreases. Increases the number of active beta-adrenergic receptors, restores the patient's response to bronchodilators, and reduces the frequency of their use. Practically no resorptive effect after inhalation.
It does not relieve bronchospasm, the therapeutic effect develops gradually, usually after 5-7 days of course application of beclomethasone dipropionate.
In the lung tissue of beclomethasone, dipropionate is rapidly hydrolyzed to beklomethasone monopropionate, which in turn is hydrolyzed to Beklokamethasone. The portion of the dose that is accidentally swallowed is largely inactivated by the “first pass” through the liver. In the liver, beclomethasone dipropionate is converted to beclomethasone mono-propionate and then to polar metabolites. Plasma protein binding of an active substance in the systemic circulation is 87%. The main part of the drug (35-76%) is excreted within 96 hours of the gastrointestinal tract, mainly in the form of polar metabolites, 10-15% - by the kidneys.

Indications

Basic therapy of various forms of asthma in adults and children over 4 years old.

Composition

1 dose contains:
Active ingredient: beclomethasone dipropionate - 0.25 mg (in terms of 100% substance)
Excipients: ethanol 96% 10.5 mg, norfluran (tetrafluoroethane) 74.4 mg.
Each inhaler contains 200 doses.

Beclomethasone is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Beclomethasone inhalation spray
Beclomethasone-Aeronative Nativa Russia inhalation spray
Clenil®UDV Chiesi Pharmaceutical SpA Italy ampoules
Beclazone Eco Teva Israel inhalation spray
Beclazone Eco Light Breath Ayvaks Pharmaceuticals Czech inhalation spray
Nasobec® Teva Israel spray

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Beclomethasone

Dosage and Administration

Beclomethasone is for inhalation use only.

Beclomethasone is used regularly (even in the absence of symptoms of the disease), the dose of beclomethasone dipropionate is selected taking into account the clinical effect in each particular case.

With mild bronchial asthma, forced inspiratory volume (FEV) or peak expiratory flow rate (PSV) make up more than 80% of proper values ​​with a spread of PSV values ​​of less than 20%.

With a moderate course of FEV or PSV is 60-80% of the proper values, the daily variation of PSV is 20-30%.

In case of severe FEV or PSV, 60% of the required values, the daily variation of PSV values ​​is more than 30%.

When switching to a high dose of inhalation beclomethasone dipropionate, many patients receiving systemic glucocorticosteroids will be able to reduce their dose, cancel them altogether.

The initial dose of beclomethasone is determined by the severity of bronchial asthma. The daily dose is divided into several doses.

Depending on the patient's individual response, the dose of the drug can be increased until the clinical effect appears or reduced to the minimum effective dose.

Children aged 4 to 12 years

The initial dose is 50 mg 2 times a day. If necessary, the initial dose can be increased to 100 μg 2 times a day. The maximum single dose of 200 micrograms.

The maximum daily dose is 400 micrograms. The daily dose is divided into 2-4 doses.

Adults and children aged 12 and over:

Recommended initial doses of the drug:

  • bronchial asthma of the lungs - 200-600 mg / day;
  • moderate bronchial asthma - 600-1000 mcg / day;
  • severe bronchial asthma - 1000-2000 mcg / day.

The treatment of bronchial asthma is based on a stepwise approach - the therapy is started according to the degree corresponding to the severity of the disease. Inhalation GCS is prescribed for the second stage of therapy.

Stage 2. Basic therapy.

Beclomethasone dipropionate 100-400 mcg 2 times a day.

Stage 3. Basic therapy.

Apply inhaled GCS in a high dose or in a standard dose, but in combination with inhaled long-acting p-2 adrenomimetics.

Beclomethasone dipropionate in a high dose - 800-1600 mg / day, in some cases, megadoses up to 2000 mg / day.

Step 4. Severe asthma.

Beclomethasone dipropionate in a high dose - 800-1600 mg / day, in some cases, megadoses up to 2000 mg / day.

Step 5. Severe asthma.

Beclomethasone dipropionate in a high dose (see steps 3 and 4).

Special patient groups

There is no need to adjust the dose of beclomethasone in the elderly, in patients with renal or hepatic insufficiency.

Skip taking one dose of the drug

In case of accidental omission of inhalation, the next dose should be taken at the appropriate time in accordance with the treatment regimen.

Instructions for the patient to use the inhaler

Check the operation of the inhaler before using it for the first time, and also if you have not used it for a while, or if the bottle was cooled to a low temperature, and then you warmed it to room temperature. To check, remove the protective cap from the nozzle inhaler, turn the balloon upside down, putting your index finger on the bottom of the bottle and your thumb on the top of the nozzle inhaler, shake the cartridge up and down and make 2 presses with your thumb and forefinger, pointing the nozzle outlet -ingulator aside. After the appearance of the aerosol spray after the second pressing, proceed as described below, beginning with the words: “Ensure that there is no dust and dirt in the outlet tube”.

With regular use of the drug should do the following:

  • Remove the protective cap from the nozzle inhaler. Make sure there is no dust or dirt in the outlet tube.
  • Hold the bottle upright with the bottom facing up, with your index finger on the bottom of the bottle and your thumb on the top of the inhaler tip. Shake the can up and down.
  • Exhale as deeply as possible (without tension). Clamp the inhaler nozzle outlet tightly with your lips.
  • Take a slow deep breath. At the moment of inhalation by pressing your thumb and forefinger, release a dose of the drug. Keep breathing slowly.
  • Remove the inhaler tube from your mouth and hold your breath for 10 seconds or as much as you can without tension. Exhale slowly.
  • If more than one dose of medication is required, wait for about a minute and then repeat steps from step 2. Put the protective cap back on the inhaler tip.

Do not rush through steps 3 and 4. At the time of release of a dose of medicine, it is important to breathe in as slowly as possible. First practice in front of the mirror. If you notice steam coming out of the corners of your mouth, then start again from step 2.

Cleaning the inhaler.

The inhaler cap should be cleaned at least once a week. Remove the nozzle inhaler from the bottle and rinse it and the protective cap with warm water. Do not use hot water. Dry thoroughly, but do not use heating devices for this. Put the protective cap back on the nozzle inhaler, and its - on the balloon. Do not dip the balloon in water.

Adverse reactions

Adverse reactions are listed depending on the anatomical and physiological classification and occurrence.
Infections: very often - candida of the mouth and pharynx. The use of a spacer and rinsing the mouth and throat with water after inhalation reduces the likelihood of these side effects.
On the part of the immune system: infrequently - skin reactions of hypersensitivity, including rash, urticaria, itching, redness and swelling of the eyes, face, lips and mucous membranes of the mouth and pharynx; very rarely - angioedema, anaphylactic reactions.
On the part of the endocrine system: systemic effects are possible: very rarely - suppression of the function of the adrenal cortex, growth retardation in children and adolescents, cataracts, glaucoma.
On the part of the respiratory system: often dysphonia (hoarseness of the voice) or irritation of the mucous membrane of the pharynx, very rarely - paradoxical bronchospasm, which must be stopped immediately with the help of inhalation [3-2-adrenostimulyator of short action. In the event of a paradoxical bronchospasm, it is necessary to immediately discontinue the use of the drug in inhalation, assess the patient's condition, carry out the necessary examination and prescribe the necessary treatment.
On the part of the skin and subcutaneous fat: often - bruising, thinning of the skin.

Contraindications

Hypersensitivity to any component of the drug.
Pulmonary tuberculosis.
Children's age up to 4 years. Beclomethasone, containing 250 mcg in 1 dose, is not intended for use in pediatrics (ie, in children under 18).
Carefully
Apply with glaucoma, systemic infections (bacterial, viral, fungal, parasitic), osteoporosis, cirrhosis of the liver, hypothyroidism, pregnancy, during lactation.

Drug interactions

Beclomethasone restores the patient's response to beta-adrenomimetics, allowing you to reduce the frequency of their use.
When used together with inducers of microsomal oxidation (including phenobarbital, phenytoin, rifampicin, etc.), the effectiveness of beclomethasone may decrease.
With simultaneous use with methandienone, estrogen, beta2-adrenergic, theophylline, as well as systemic GCS, the effectiveness of beclomethasone increases.
With the simultaneous use of beclomethasone enhances the effect of beta-adrenermics.

Special instructions

Before the appointment of inhaled drugs, it is necessary to instruct the patient about the rules of their use, ensuring the most complete ingestion of the drug in the desired areas of the lungs. The development of oral candidiasis is most likely in patients with a high level of precipitating antibodies in the blood against Candida fungus, which indicates a previous fungal infection. After inhalation, rinse the mouth and throat with water.For the treatment of candidiasis, you can use local antifungal drugs while continuing therapy with Beclomethasone.
If patients take GCS orally, then Beclomethasone is prescribed while taking the previous dose of GCS, while patients should be in a relatively stable state. About 1-2 weeks later, the daily dose of oral GCS is gradually reduced. The dose reduction scheme depends on the duration of the previous therapy and on the magnitude of the initial dose of GCS. Regular use of inhaled corticosteroids allows, in most cases, abolishing oral corticosteroids (patients requiring no more than 15 mg of prednisolone can be fully transferred to inhalation therapy). At the same time, in the first months after the transition, the patient’s condition should be carefully monitored until his pituitary-adrenal system is restored sufficiently to ensure an adequate response to stressful situations (for example, trauma, surgery or infection).
When transferring patients from taking systemic corticosteroids to inhalation therapy, allergic reactions (for example, allergic rhinitis, eczema), which were previously suppressed by systemic drugs, can manifest themselves.
Patients with a reduced function of the adrenal cortex, transferred to inhalation treatment, should have a supply of corticosteroids and always carry a warning card, which should indicate that they need additional systemic corticosteroids in stressful situations (after eliminating the stressful situation, the dose of corticosteroids can again reduce). A sudden and progressive worsening of asthma symptoms is a potentially dangerous condition, not infrequently life-threatening to the patient, and requires an increase in the dose of GCS. An indirect indicator of the ineffectiveness of therapy is the more frequent use of 0-2-adrenostimulyatorov short-acting.
Beclomethasone dipropionate for inhalation is not intended to relieve seizures, but for regular daily use. For the relief of attacks, 3–2 short-acting adrenergic stimulants (for example, salbutamol) are used. With severe exacerbation of bronchial asthma or insufficient efficacy of therapy, the dose of inhalation beclomethasone dipropionate should be increased and, if necessary, systemic GCS and antibiotic should be administered during infection.
With the development of paradoxical bronchospasm, you should immediately stop the use of beclomethasone, assess the patient's condition, conduct an examination and, if necessary, prescribe therapy with other drugs. With prolonged use of any inhaled GCS, especially in high doses, systemic effects may occur (see “Side Effects”), but the probability of their development is significantly lower than when taking GCS orally. Therefore, it is especially important that when the therapeutic effect is achieved, the dose of inhaled GCS is reduced to the minimum effective dose controlling the course of the disease. At a dose of 1500 mcg / day, the drug in most patients does not cause significant suppression of adrenal function. In connection with possible adrenal insufficiency, special care should be taken and the indicators of the function of the adrenal cortex should be regularly monitored when transferring patients taking GCS orally for treatment with beclomethasone.
It is recommended to regularly monitor the growth of children receiving inhaled GCS for a long time.
The introduction can be carried out using special dispensers (spacers), which improve the distribution of the drug in the lungs and reduce the risk of side effects.
It is not recommended abrupt withdrawal of the drug Beclomethasone aerosol.
It is necessary to protect the eyes from getting the drug. Washing after inhalation can prevent damage to the skin of the eyelids and nose.
You cannot pierce, disassemble or throw into the fire even if it is empty. Like most other inhalants in aerosol packaging, Beclomethasone may be less effective at low temperatures. When cooling the cylinder, it is recommended to remove the inhaler attachment from it and warm it with your hands for a few minutes.
Influence on ability to drive vehicles and mechanisms
No data.

Overdosage

Symptoms:
Acute overdose of the drug can lead to a temporary decrease in the function of the adrenal cortex, which does not require emergency therapy, since the function of the adrenal cortex is restored within a few days, which is confirmed by plasma cortisol concentration. In chronic overdose, persistent suppression of the function of the adrenal cortex can be observed.
Treatment:
In such cases, it is recommended to monitor the reserve function of the adrenal cortex. In case of overdose, treatment with beclomethasone dipropionate can be continued in doses sufficient to maintain a therapeutic effect.

  • Brand name: Beclomethasone
  • Active ingredient: Beclomethasone
  • Dosage form: Inhalation aerosol dosed 50 mcg / dose, 100 mcg / dose or 250 mcg / dose.
    For 200 doses in aluminum cylinders with a protective coating, sealed with a metering valve and equipped with a spray nozzle with a protective cap. Each cylinder with a spray nozzle and a protective cap, as well as instructions for use are placed in a pack.

  • Manufacturer: Ayvaks Pharmaceuticals

Studies and clinical trials of Beclomethasone (Click to expand)

  1. Effects of inhaled beclomethasone compared to systemic dexamethasone on lung inflammation in preterm infants at risk of chronic lung disease
  2. Decomposition of beclomethasone propionate esters in human plasma
  3. Beclomethasone relative availability of oral versus inhaled beclomethasone dipropionate from an HFA-134a metered dose inhaler
  4. Effects of early inhaled beclomethasone therapy on tracheal aspirate inflammatory mediators IL-8 and IL-1ra in ventilated preterm infants at risk for bronchopulmonary dysplasia
  5. Comparative kinetics of metabolism of beclomethasone propionate esters in human lung homogenates and plasma
  6. Beclomethasone dipropionate inhalation treatment for chronic hoarseness in rheumatic disease
  7. Activation of beclomethasone dipropionate by hydrolysis to beclomethasone-17-monopropionate
  8. Sensitive liquid chromatographic/tandem mass spectrometric method for the determination of beclomethasone dipropionate and its metabolites in equine plasma and urine
  9. Manipulation of beclomethasone–hydrofluoroalkane interactions using biocompatible macromolecules
  10. Effect of nanoprecipitation on the physicochemical properties of low molecular weight poly(l-lactic acid) nanoparticles loaded with salbutamol sulphate and beclomethasone dipropionate
  11. Experimental study of the GAS process for producing microparticles of beclomethasone-17,21-dipropionate suitable for pulmonary delivery
  12. Transient drug supersaturation kinetics of beclomethasone dipropionate in rapidly drying films
  13. Metered-dose inhalers I: drug content and particle size distribution of beclomethasone dipropionate
  14. Dose-dependent inhibitory effect of inhaled beclomethasone on late asthmatic reactions and increased responsiveness to methacholine induced by toluene diisocyanate in sensitised subjects
  15. Simultaneous quantification of beclomethasone dipropionate and its metabolite, beclomethasone 17-monopropionate in rat and human plasma and different rat tissues by liquid chromatography–positive electrospray ionization tandem mass spectrometry
  16. The measurement of beclomethasone dipropionate entrapment in liposomes: a comparison of a microscope and an HPLC method
  17. Nebulisation of rehydrated freeze-dried beclomethasone dipropionate liposomes
  18. Beclomethasone dipropionate 250 μg per dose metered dose inhalers: effect of Volumatic spacer on potentially respirable dose
  19. Pulmonary distribution and clearance of two beclomethasone liposome formulations in healthy volunteers
  20. The influence of lactose carrier on the content homogeneity and dispersibility of beclomethasone dipropionate from dry powder aerosols
  21. Beclomethasone dipropionate: absolute bioavailability, pharmacokinetics and metabolism following intravenous, oral, intranasal and inhaled administration in man
  22. Dose–response for adrenal suppression with hydrofluoroalkane formulations of fluticasone propionate and beclomethasone dipropionate
  23. Beclomethasone dipropionate enemas versus prednisolone sodium phosphate enemas in the treatment of distal ulcerative colitis
  24. The gastrointestinal passage and release of beclomethasone dipropionate from oral delivery systems in ileostomy volunteers

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