BECONASE AQUEOUS NASAL SPRAY

Active substance: BECLOMETHASONE DIPROPIONATE

View full screen / Print PDF » Download PDF ⇩

Transcript
SUMMARY OF PRODUCT CHARACTERISTICS

1

NAME OF THE MEDICINAL PRODUCT
Beconase Aqueous Nasal Spray

2.

QUALITATIVE AND QUANTITATIVE COMPOSITION
Beclometasone Dipropionate 50μg (as monohydrate, micronised)

3.

PHARMACEUTICAL FORM
Aqueous suspension for intranasal inhalation via metered dose atomising
pump.

4.

CLINICAL PARTICULARS

4.1.

Therapeutic indications
Beconase Aqueous Nasal Spray is indicated for the prophylaxis and treatment
of perennial and seasonal allergic rhinitis including hayfever, 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.

4.2.

Posology and method of administration
Beconase Aqueous Nasal Spray is for administration by the intranasal route
only.
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 has been shown to be 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.
For children under six years old, there are insufficient clinical data to
recommend use.

4.3

Contraindications
Beconase Aqueous Nasal Spray is contra-indicated in patients with a history of
hypersensitivity to any of its components.

4.4

Special warnings and precautions for use
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
behavioural 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 with the aim of reducing 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 paediatric
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
Beconase Aqueous 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 Beconase Aqueous
Nasal Spray.

Although Beconase Aqueous 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.

4.5.

Interactions with other medicinal products and other forms of interaction
Not applicable

4.6.

Pregnancy and lactation
There is inadequate evidence of safety in human pregnancy. Administration of
corticosteroids to pregnant animals can cause abnormalities of foetal
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 the foetal changes in animals occur after
relatively high systemic exposure. Beconase Aqueous Nasal Spray delivers
Beclometasone dipropionate directly to the nasal mucosa and so minimises
systemic exposure.
The use of Beclometasone dipropionate should be avoided during pregnancy
unless thought essential by the doctor.
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.

4.7.

Effects on ability to drive and use machines
Not applicable.

4.8

Undesirable Effects
Adverse events are listed below by system organ class and frequency.
Frequencies are defined as: very common (≥1/10), common (≥1/100 and
<1/10), uncommon (≥1/1000 and <1/100), rare (≥1/10,000 and <1/1000) and
very rare (<1/10,000) including isolated reports. Very common, common and
uncommon events were generally determined from clinical trial data. Rare
and very rare events were generally determined from spontaneous data. In
assigning adverse event frequencies, the background rates in placebo groups

were not taken into account, since these rates were generally comparable to
those in the active treatment group.
System Organ
Class
Immune system
disorders

Adverse Event
Hypersensitivity reactions including:
Rashes, urticaria, pruritis, erythema.

Frequency

Dyspnoea and/or bronchospasm
Anaphylactoid/anaphylactic reactions

Common
Very rare
Very rare
Very rare

Unpleasant taste, unpleasant smell.

Common

Glaucoma, raised intraocular pressure,
cataract.
Epistaxis, nasal dryness, nasal irritation,
throat dryness, throat irritation.
Nasal septum perforation.

Very rare

Oedema of the eyes, face, lips and throat
Nervous
system
disorders
Eye disorders
Respiratory,
Thoracic &
Mediastinal
disorders

Common
Very rare

As with other nasal sprays, dryness and irritation of the nose and throat, and
epistaxis have been reported. Nasal septal perforation has also been reported
following the use of intranasal corticosteroids.
Systemic effects of nasal corticosteroids may occur particularly when used at
high doses for prolonged periods.

4.9.

Overdose
The only harmful effect that follows inhalation of large amounts of the drug
over a short time period is suppression of Hypothalamic-Pituitary-Adrenal
(HPA) function. No special emergency action need be taken. Treatment with
Beconase Aqueous Nasal Spray should be continued at the recommended
dose. HPA function recovers in a day or two.

5.

PHARMACOLOGICAL PROPERTIES

5.1.

Pharmacodynamic properties
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
hydrolysed via esterase enzymes to the highly active metabolite

Beclometasone-17-monopropionate (B-17-MP), which has high topical antiinflammatory activity.
Beclometasone 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 reappearing.

5.2.

Pharmacokinetic properties
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 mucocilary
clearance, is available for absorption from the gastrointestinal tract. Plasma B17-MP is almost entirely due to 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 (< 50pg/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-21monopropionate (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 (201) but more
extensive for B-17-MP (4241). Plasma protein binding of BDP is moderately
high (87%).

Elimination
The elimination of BDP and B-17-MP are characterised by high plasma
clearance (150 and 1201/h) with corresponding terminal elimination half-lives
of 0.5h and 2.7h. Following oral administration of tritiated 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.

5.3.

Preclinical safety data
No clinically relevant findings were observed in preclinical studies.

6.

PHARMACEUTICAL PARTICULARS

6.1.

List of Excipients
Avicel RC 591 (Microcrystalline Cellulose And Carboxymethylcellulose
Sodium) US NF
Anhydrous Dextrose BP
Benzalkonium Chloride BP
Phenylethyl Alcohol USP
Polysorbate 80 BP
Purified Water BP

6.2.

Incompatibilities
Not applicable.

6.3.

Shelf Life
24 months when not stored above 30°C

6.4.

Special Precautions for Storage
Beconase Aqueous Nasal Spray should not be stored above 30°C. Keep
container in the outer carton. Do not refrigerate.

6.5.

Nature and Contents of Container
A 25ml amber neutral glass bottle fitted with a metering atomising pump, or a
30ml polypropylene bottle fitted with a tamper-resistant metering atomising
pump. The pumps are manufactured by: Valois S.A. Le Prieure BPG, 27110
Le Neubourg, France.
Pack size: 200 Metered Spray.

6.6.

Instructions for Use/Handling
Refer to Patient Information Leaflet.

7.

MARKETING AUTHORISATION HOLDER
Glaxo Wellcome UK Ltd.
Trading as Allen and Hanburys,
Stockley Park West,
Uxbridge
Middlesex, UB11 1BT

8.

MARKETING AUTHORISATION NUMBER
PL 10949/0104

9.
DATE OF FIRST AUTHORISATION/RENEWAL OF THE
AUTHORISATION
06 March 1995

10

DATE OF REVISION OF THE TEXT

07/09/2011

Expand view ⇕

Source: Medicines and Healthcare Products Regulatory Agency

Disclaimer: Every effort has been made to ensure that the information provided here is accurate, up-to-date and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. This information has been compiled for use by healthcare practitioners and consumers in the United States. The absence of a warning for a given drug or combination thereof in no way should be construed to indicate that the drug or combination is safe, effective or appropriate for any given patient. If you have questions about the substances you are taking, check with your doctor, nurse or pharmacist.

Hide
(web5)