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Apo-beclomethasone
nasal spray
Beclomethasone Dipropionate Aqueous Suspension 0.05% w/w
50 µg/metered spray
Corticosteroid for Nasal Use
Product Description
Apo-Beclomethasone (beclomethasone dipropionate) Nasal Spray is a suspension
of beclomethasone dipropionate in an amber glass bottle fitted with a
metered atomizing pump and a nasal applicator. Each spray delivered by the
nasal applicator contains 50 micrograms beclomethasone dipropionate.
Pharmacology
Pharmacodynamics:
Following topical administration beclomethasone 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
hay fever when taken prior to 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.
Metabolism: BDP is cleared very rapidly from the circulation and plasma
concentrations are undetectable (< 50µg/ml) following oral or intranasal
dosing.
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 characterized 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.
Indication
APO-BECLOMETHASONE (beclomethasone
dipropionate) 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.
Recommended Dose and Mode of Administration
Apo-Beclomethasone 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. A dosage
regimen of 1 spray into each nostril 3 or 4 times daily may be preferred.
Total daily administration should not normally exceed 8 sprays (400 mcg).
For full therapeutic benefit, regular usage is essential. The cooperation 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.
Contraindication
APO-BECLOMETHASONE is contra-indicated in patients with a history of
hypersensitivity to any of its components.
Warnings
Use in 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. APO-BECLOMETHASONE 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.
Use in children:
Apo-Beclomethasone Nasal Spray is not suitable for children.
Precautions
When prescribing Apo-Beclomethasone Nasal Spray, the importance of
continuous and regularity usage of the preparation should at all times be
highlighted to the patient. When systemic corticoid or ACTH therapy is
substituted by Apo-Beclomethasone Nasal Spray, the former medication should
be continued concurrently with Apo-Beclomethasone Nasal Spray for about a
week, hereafter the systemic drug can be progressively reduced. Any nasal
infections and sinusitis must be treated effectively.
When the systemic steroid is withdrawn, other allergic conditions may emerge
or weaken.
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System Organ Class |
Adverse Event |
Frequency |
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Immune system disorders |
Hypersensitivity
reactions including : |
|
|
Rashes, urticaria,
pruritis, erythema. |
Common |
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Oedema of the eyes, face,
lips and throat |
Very rare |
|
Dyspnoea and/or
bronchospasm |
Very rare |
|
Anaphylactoid/anaphylactic
reactions |
Very rare |
|
Nervous system disorders |
Unpleasant taste,
unpleasant smell |
Common |
|
Eye disorders |
Glaucoma, raised
intraocular pressure, cataract. |
Very rare |
|
Respiratory, thoracic &
Mediastinal disorders |
Epistaxis, nasal dryness,
nasal irritation, throat dryness, throat irritation. |
Common |
|
Nasal septum perforation. |
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.
Symptoms and Treatment of Overdose
When used in excessive dosages (above 600 micrograms or 12 applications of
Apo-Beclomethasone (beclomethasone dipropionate) Nasal Spray per day),
systemic steroid effects, such as hypercorticism and adrenal suppression,
may appear. Decreasing the dosage will abolish the side-effects.
Storage Conditions
Do not refrigerate. Store at room temperature (15-30°C). Protect from light.
Interactions with Other Medicaments
Not applicable.
Adverse 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.
Shelf-life
36 months from the date of manufacture.
Availability of Dosage Forms
Apo-Beclomethasone Nasal Spray is available in 200 metered spray (22g net
weight) bottles.
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