Elpesom

Beclometasone dipropionate.

White to almost white suspension.
Each 1 mL suspension contains: Active ingredients: Beclometasone dipropionate 0.555 mg (each dose contains 0.050 mg beclometasone dipropionate).
Excipients/Inactive Ingredients: Polysorbate 80, anhydrous glucose, dispersible cellulose (Avicel RC 591), benzalkonium chloride, sodium hydroxide solution (1M), hydrochloric acid solution (1M), purified water.

Pharmacotherapeutic groups: Topical corticosteroids for nasal route. ATC code: R01AD01.
Pharmacology: Pharmacodynamics: Following topical administration beclometasone 17,21-dipropionate (BDP) produces potent anti-inflammatory and vasoconstrictor effects.
BDP is a pro-drug with weak corticosteroid receptor binding affinity. It is hydrolyzed via esterase enzymes to the highly active metabolite beclometasone-17-monopropionate (B-17-MP), which has high topical anti-inflammatory activity.
Beclometasone dipropionate offers a preventative background treatment for hay fever when taken before the allergen challenge. After which with regular use, BDP can continue to prevent allergy symptoms from reappearing.
Pharmacokinetics: Absorption: Following intranasal administration of BDP in healthy males, the systemic absorption was assessed by measuring the plasma concentrations of its active metabolite B-17-MP, for which the absolute bioavailability following intranasal administration is 44% (95% CI 28%, 70%). After intranasal administration, <1% of the dose is absorbed by the nasal mucosa. The remainder after being cleared from the nose, either by drainage or mucociliary clearance, is available for absorption from the gastrointestinal tract. Plasma B-17-MP is almost entirely due to the conversion of BDP absorbed from the swallowed dose.
Following oral administration of BDP in healthy males, the systemic absorption was also assessed by measuring the plasma concentrations of its active metabolite B-17-MP, for which the absolute bioavailability following oral administration is 41% (95% CI 27%, 62%).
Following an oral dose, B-17-MP is absorbed slowly with peak plasma levels reached 3-5 hours after dosing.
Metabolism: BDP is cleared very rapidly from the circulation and plasma concentrations are undetectable (<50 pg/mL) following oral or intranasal dosing. There is rapid metabolism of the majority of the swallowed portion of BDP during its first passage through the liver. The main product of metabolism is the active metabolite (B-17-MP). Minor inactive metabolites, beclometasone-21-monopropionate (B-21-MP) and beclometasone (BOH) are also formed but these contribute little to systemic exposure.
Distribution: The tissue distribution at steady-state for BDP is moderate (20l) but more extensive for B-17-MP (424l). Plasma protein binding of BDP is moderately high (87%).
Elimination: The elimination of BDP and B-17-MP is characterized by high plasma clearance (150 and 120l/h) with corresponding terminal elimination half-lives of 0.5 h and 2.7 h. Following oral administration of tritiated BDP, approximately 60% of the dose was excreted in the feces within 96 hours mainly as free and conjugated polar metabolites. Approximately 12% of the dose was excreted as free and conjugated polar metabolites in the urine.

Indicated for the prophylaxis and treatment of perennial and seasonal allergic rhinitis including hay fever, and vasomotor rhinitis. Beclometasone dipropionate has a potent anti-inflammatory effect within the respiratory tract, with a lower incidence and severity of adverse events than those observed when corticosteroids are administered systemically.

Method of administration: Nasal spray.
Posology: Adults and children over six years of age: The recommended dosage is two sprays into each nostril twice daily (400 micrograms/day).
Once control has been established it may be possible to maintain control with fewer sprays.
A dosage regimen of one spray into each nostril morning and evening is efficacious in some patients. However, should symptoms recur, patients should revert to the recommended dosage of two sprays into each nostril morning and evening. The minimum dose should be used at which effective control of symptoms is maintained. Total daily administration should not normally exceed eight sprays.
For full therapeutic benefit, regular usage is essential.
The co-operation of the patient should be sought to comply with the regular dosage schedule and it should be explained that maximum relief may not be obtained within the first few applications.
Children under six years old: There are insufficient clinical data to recommend use.

The only harmful effect that follows inhalation of large amounts of the drug over a short period is suppression of Hypothalamic-Pituitary-Adrenal (HPA) function. No special emergency action needs to be taken. Treatment should be continued at the recommended dose. HPA function recovers in a day or two.
Further management should be as clinically indicated or as recommended by the National Poisons Centre, where available.
There is no specific treatment for an overdose of beclometasone dipropionate. If an overdose occurs, the patient should be treated supportively with appropriate monitoring as necessary.

Hypersensitivity to beclomethasone dipropionate or any of the excipients in drug component.

Systemic effects of nasal corticosteroids may occur, particularly at high doses prescribed for prolonged periods. These effects are much less likely to occur than with oral corticosteroids and may vary in individual patients and between different corticosteroid preparations. Potential systemic effects may include Cushing's syndrome, Cushingoid features, adrenal suppression, growth retardation in children and adolescents, cataract, glaucoma, and more rarely, a range of psychological or behavioral effects including psychomotor hyperactivity, sleep disorders, anxiety, depression or aggression (particularly in children).
Growth retardation has been reported in children receiving nasal corticosteroids at licensed doses. It is recommended that the height of children receiving prolonged treatment with nasal corticosteroids is regularly monitored. If growth is slowed, therapy should be reviewed to reduce the dose of nasal corticosteroid, if possible to the lowest dose at which effective control of symptoms is maintained. In addition, consideration should be given to referring the patient to a pediatric specialist.
Treatment with higher than recommended doses may result in clinically significant adrenal suppression. If there is evidence for higher than recommended doses being used then additional systemic corticosteroid cover should be considered during periods of stress or elective surgery.
Care must be taken while transferring patients from systemic steroid treatment to nasal spray if there is any reason to suppose that their adrenal function is impaired.
Infections of the nasal passages and paranasal sinuses should be appropriately treated but do not constitute a specific contra-indication to treatment with beclomethasone dipropionate nasal spray.
Although beclomethasone dipropionate nasal spray will control seasonal allergic rhinitis in most cases, an abnormally heavy challenge of summer allergens may in certain instances necessitate appropriate additional therapy particularly to control eye symptoms.
Benzalkonium chloride: Each dose contains 0.09 mg benzalkonium chloride. Benzalkonium chloride may cause irritation or swelling inside the nose, especially if used for a long time.
Benzalkonium chloride may cause wheezing and breathing difficulties (bronchospasm), especially if the patient has asthma.
Visual Disturbance: Visual disturbance may be reported with systemic and topical corticosteroid use. If a patient presents with symptoms such as blurred vision or other visual disturbances, the patient should be considered for referral to an ophthalmologist for evaluation of possible causes, which may include cataract, glaucoma or rare diseases such as central serous chorioretinopathy (CSCR) which have been reported after use of systemic and topical corticosteroids.
Effects on Ability to Drive and Use Machines: There is no evidence of drug's effects on the ability to drive and use machines.

Pregnancy: There is inadequate evidence of safety in human pregnancy. Administration of corticosteroids to pregnant animals can cause abnormalities of fetal development including cleft palate and intra-uterine growth retardation. There may therefore be a very small risk of such effects in the human foetus. It should be noted, however, that fetal changes in animals occur after relatively high systemic exposure. The drug delivers beclometasone dipropionate directly to the nasal mucosa and so minimizes systemic exposure.
The use of beclometasone dipropionate should be avoided during pregnancy unless thought essential by the doctor.
Lactation: No specific studies examining the transference of beclometasone dipropionate into the milk of lactating animals have been performed. It is reasonable to assume that beclometasone dipropionate is secreted in milk but at the dosages used for direct intranasal administration there is low potential for significant levels in breast milk. The use of beclometasone dipropionate in mothers breast feeding their babies requires that the therapeutic benefits of the drug be weighed against the potential hazards to the mother and baby.

Terms and frequencies of adverse effects are determined as follows: Very common: R ≥1/10; Common: 1/10> R ≥1/100; Uncommon: 1/100> R ≥1/1,000; Rare: 1/1,000> R ≥1/10,000; Very rare: R <1/10,000; Not known: Cannot be estimated from the available data. (See table.)


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Systemic effects of nasal corticosteroids may occur particularly when used at high doses for prolonged periods.
Immediately notify a doctor or pharmacist of any adverse reactions that may be encountered when using the drug.

Beclomethasone is less dependent on CYP3A metabolism than some other corticosteroids, and in general interactions are unlikely; however, the possibility of systemic effects with concomitant use of strong CYP3A inhibitors (e.g. ritonavir, cobicistat) cannot be excluded, and therefore caution and appropriate monitoring is advised with the use of such agents.

Stored below 30°C, do not refrigerate or freeze.
Shelf Life: 36 months from manufacturing date.
This product should be used within 6 months after opening.

Nasal Decongestants & Other Nasal Preparations

R01AD01 - beclometasone ; Belongs to the class of topical corticosteroids used for prophylaxis and treatment of allergic rhinitis.