Beclate Inhaler

Pharmacodynamics

Beclomethasone is hormone-glucocorticosteroid of anti-inflammatory and anti-allergic action.

It has an inhibitory effect on inflammatory mediators release, increases lipomodulina production – phospholipase «A» inhibitor, reduces arachidonic acid release, inhibits prostaglandins synthesis.

It prevents neutrophils boundary accumulation, thereby reducing inflammatory exudate formation and lymphokines production. Beclomethasone inhibits macrophages migration, which leads to slowing infiltration and granulation processes.

Beclomethasone reduces number of mast cells in bronchial mucosa, epithelium swelling and mucus secretion by bronchial glands. It causes bronchial smooth muscles relaxation, reduces their hyperactivity and improves respiratory function.

The drug increases number of active beta-adrenoreceptors, restores patient’s response to bronchodilators, thereby allowing to reduce frequency of their use.

The drug has no mineralocorticoid activity.

Usually, in therapeutic doses beclomethasone has no side effects characteristic of systemic glucocorticosteroids.

Therapeutic effect usually develops after 5 – 7 days of beclomethasone course.

At external and local application the drug has anti-edemic, anti-allergic and anti-inflammatory effect.

Pharmacokinetics

When inhaled the drug penetrates deep into lungs. In lungs beclomethasone dipropionate is hydrolyzed to beclomethasone monopropionate, which is further hydrolyzed to beclomethasone.

Active substance is bound to blood plasma protein by 87%.

Beclomethasone half-life period when administered intravenously is 30 minutes. Metabolites are excreted up to 64% with feces and to 14% with urine within 96 hours.

Indications

For inhalation use: bronchial asthma treatment (including lack of bronchodilators and / or sodium cromoglycate efficacy, as well as severe hormone-dependent bronchial asthma heavy at adults and children).

For intranasal use: year-round and seasonal allergic rhinitis prevention and treatment, including rhinitis with hay fever and vasomotor rhinitis.

For external and local use: in combination with antimicrobial agents – skin and ear infectious and inflammatory diseases.

Contraindications

This drug is not used in the following cases:

• hypersensitivity;
• age up to 6 years.

Inhalation use is not practiced:

• at acute bronchospasm;
• at status asthmaticus – not used as first-line means;
• at non-asthmatic bronchitis.

Intranasal use is not practiced:

• at hemorrhagic diathesis;
• at systemic infections (bacterial, fungal);
• at acute respiratory diseases;
• at frequent nasal hemorrhages;
• at herpetic eye disease.

Note that there are restrictions for intranasal use. These are recent surgery in nasal cavity, nasal septum ulcerations, recent nose injury, glaucoma, amoebiasis, hypothyroidism, severe liver failure. The drug should be used with caution after recent myocardial infarction.

With Caution

• At moderate and severe bronchial obstruction 15-20 minutes before inhalation it is recommended to use bronchodilators.
• Used with caution at patients with hypothalamus-pituitary-adrenal insufficiency symptoms. It is necessary to continue inhalations, monitoring basal cortisol level in blood plasma. The same control is needed when using high doses of beclomethasone (1500 g or more).

Pregnancy and Lactation Period

The drug is strictly contraindicated during I trimester pregnancy.

Application during II and III trimester pregnancy is possible only when expected benefits to the mother outweigh potential risk to the fetus. Newborn children, whose mothers received beclomethasone during pregnancy should be carefully examined for adrenal dysfunction.

If necessary to use the drug during lactation period, patients should discuss issue of breastfeeding termination with doctor.

Dosage

At inhalation, average dosage for adults is 400 mg/day, frequency of application – 2 – 4 times/day. Dosage may be increased up to 1 g/day, if necessary. For children, single dose is 50 – 100 mg, frequency of application – 2 – 4 times/day.

For intranasal administration, dosage is 400 mg/day, frequency of application 1 – 4 times/day.

For external and local application, dosage depends on indications and drug pharmaceutical form.

Overdose

Symptoms: nausea, vomiting, insomnia, euphoria, agitation, depression.

Treatment: on the background of gradual drug withdrawal – vital functions maintenance, electrolyte balance correction, antacids, phenothiazines, Li drugs; at Cushing’s syndrome – aminoglutethimides.

Prolonged treatment with high drug doses may cause osteoporosis, high blood pressure and other hypercorticoidism symptoms (including Cushing’s syndrome).

Side Effects

During inhalations there are possible the following side effects:

• throat irritation;
• hoarseness;
• coughing and sneezing;
• eosinophilic pneumonia;
• paradoxical bronchospasm;
• allergic reactions;
• during long-term treatment – oral and upper respiratory tract candidiasis (disappears at antifungal treatment, does not require therapy withdrawal).

Systemic adverse effects can manifest when taking means at high doses (greater than 1,5 mg/day).

When applied intranasally there are possible the following side effects:

• nasal mucosa irritation and dryness;
• throat and nasal pains;
• nasal hemorrhages;
• nasopharyngeal infections, provoked by fungal flora;
• nasal septum perforation;
• rhinorrhea;
• nasal mucosa ulceration.

At prolonged drug use in high doses (more than 1500 mcg/day) systemic side effects may develop. As systemic effects manifestations there are possible: dizziness, headaches, eyes pains, drowsiness, increased intraocular pressure, blurred vision, conjunctival hyperemia, sense of taste distortion, allergic reactions, myalgia. If the drug is used for a long time, there may be growth retardation at children.

Drug Interactions

• At simultaneous reception, beta-agonists influence increases. Beta-agonists enhance beclomethasone anti-inflammatory effect, increasing degree of penetration into distal bronchial areas.
• Ephedrine activates beclomethasone metabolism process.
• Beclomethasone efficacy is lowered by microsomal oxidation enzyme inducers.
• When combined, estrogen, methandienone, theophylline, beta2-agonists, oral glucocorticoids activate beclomethasone effect.

Special Instructions

• Drug contact with eyes should be avoided.
• Inhalations should be carried out before meals and after each inhalation patients should rinse mouth to minimize risk of oropharyngeal candidiasis.
• Do not use this drug with purpose of relief acute asthma attacks. If, in response to beclometasone acute asthma attack develops, you should immediately cancel this treatment.
• Basal cortisol content in blood plasma should be monitored, if high doses of beclomethasone are used for treatment.
• At allergic rhinitis with severe symptoms treatment drug effectiveness increases, when used in combination with vasoconstrictors.
• People with steroid-dependent asthma need to use higher doses of the drug.
• Patients with asthma should gradually replace glucocorticoids of systemic action with inhaled beclomethasone. You should not reduce dosage abruptly.

Application at Childhood

Preparations for inhalation use, containing 250 mcg of beclomethasone in 1 dose, are not intended for children under the age of 12 years.

Reviews about Beclomethasone

Comments about this medicine suggests that in most cases it allows to improve patients condition. There is information about certain side effects manifestations, but reviews about the drug are generally positive.