Deletion of Glaxo Wellcome SA, Buros, Spain for all registered functions

In section 4.5 Interaction with other medicinal products and other forms of interaction, following wording has been updated. 

 

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.

4.1 Therapeutic Indications

Beconase Hayfever prevents and relieves nasal congestion, sneezing and a runny, itchy nose due to hayfever and other seasonal allergic conditions. Once nasal congestion is cleared the pressure and pain around the eyes is also reduced.

Beconase Hayfever is indicated for the prevention and treatment of allergic rhinitis, including hayfever, in adults aged 18 and over.

5.1 Pharmacodynamic properties

Pharmacotherapeutic group: Nasal preparations, corticosteroids. ATC code: R01AD01

Following topical administration beclomethasone 17,21-dipropionate (BDP) produces potent anti-inflammatory and vaso-constrictor effects.

BDP is a pro-drug with weak glucocorticoid receptor binding affinity. It is hydrolysed via esterase enzymes to the active metabolite beclomethasone-17-monopropionate (B-17-MP), which has high topical anti-inflammatory activity.

Beclomethasone dipropionate offers a preventative background treatment for hayfever when taken prior to allergen challenge. After which with regular use, BDP can continue to prevent allergy symptoms from re-appearing by reducing the sensitivity of nasal membranes.

Clinical studies carried out on patients with allergic rhinitis showed efficacy in nose symptoms, more specifically sneezing, rhinorrhea, itchy nose, and nasal congestion.

Clinical data suggests that BDP improves ocular symptoms associated with allergic rhinitis. In a 6 week randomized, double-blind, parallel study involving 44 patients treated with BDP, there was a statistically significant improvement in mean ocular symptom scores (p<0.01) after the 15-day study period.

BDP seems to provide relief from sinus discomfort associated with allergic rhinitis by preventing nasal obstruction, which allows a better drainage of sinuses subsequently. The precise mechanism of action is not known.

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Section 8 has changed to

PA 1186/008/001

Section 10 revision date has changed to January 2013

Excipients: Each 100mg spray contains benzalkonium chloride solution equivalent to benzalkonium chloride 20 micrograms.

For a full list of excipients, see section 6.1.

"in a plastic bottle fitted with a metering atomising pump and nasal applicator."

5.1                 Pharmacodynamic properties

Beclomethasone dipropionate (BDP) following topical administration produces potent anti-inflammatory and vasoconstrictor effects. It offers preventative background treatment of hayfever when taken a few days prior to allergen challenge.

Following topical administration beclomethasone 17,21- dipropionate (BDP) produces potent anti-inflammatory and vaso-constrictor effects.

BDP is a pro-drug with weak glucocorticoid receptor binding affinity. It is hydrolysed via esterase enzymes to the active metabolite beclomethasone-17-monopropionate (B-17-MP), which has high topical anti-inflammatory activity.

Beclomethasone dipropionate offers a preventative background treatment for hayfever when taken prior to allergen challenge. After which with regular use, BDP can continue to prevent allergy symptoms from re-appearing by reducing the sensitivity of nasal membranes.

5.2           Pharmacokinetic properties

Beclomethasone 17, 21-dipropionate (BDP) administered intravenously is cleared rapidly with a half-life of approximately 30 minutes.

BDP is bound to plasma proteins to the extent of 87%. Up to 14% of an intravenous dose of BDP is excreted in the urine in 96 hours, mainly as polar metabolites a proportion of which are conjugated. Up to 64% of the dose is excreted in faeces in this time, again primarily as free conjugated metabolites.

Following nasal administration of BDP an indefinable fraction is absorbed by the nasal mucosa, which does not result in measurable plasma concentrations of BDP (limit of quantitation 100pg/ml). The swallowed portion of the drug is absorbed from the gastro-intestinal tract and is rapidly metabolised.

The nasal mucosa is not known to contain any enzymes capable of metabolising BDP.

Absorption

Following intranasal administration of BDP, 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%

Following oral administration of BDP the systemic absorption was also assessed by measuring the plasma concentration of its active metabolite B-17-MP, for which the absolute bioavailability following oral administration is 41%

Metabolism

BDP is cleared very rapidly from the circulation and plasma concentrations are undetectable (<50 pg/ml) following oral or intranasal dosing. Metabolism is mediated via esterase enzymes found in most tissues. The main product of metabolism is the active metabolite (B-17-MP). Minor inactive metabolites, beclomethasone-21-monopropionate (B-21-MP) and beclomethasone (BOH), are also formed but these contribute little to systemic exposure.

Distribution

The tissue distribution at steady-state for BDP is moderate (201) but more extensive for B-17-MP (4241). Plasma protein binding is moderately high (87%).

Elimination

The elimination of BDP and B-17-MP are characterised by high plasma clearance (150 and 120 l/h) with corresponding terminal elimination half-lives of 0.5h and 2.7h. Following oral administration of trititated BDP, approximately 60% of the dose was excreted in the faeces 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. The renal clearance of BDP and its metabolites is negligible.