Beconase Aqueous

Beclometasone dipropionate.

BECONASE Aqueous Nasal Spray is a presentation of an aqueous suspension of microfine beclometasone dipropionate delivered by a metering, atomising pump. Each 100 mg spray delivered by the nasal applicator contains 50 micrograms beclometasone.
Excipients/Inactive Ingredients: Microcrystalline cellulose, Carboxymethylcellulose sodium, Glucose anhydrous, Polysorbate 80, Purified water, Benzalkonium chloride, Phenylethyl alcohol, Hydrochloric acid.

Pharmacology: Pharmacodynamics: Following topical administration beclometasone 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 beclometasone-17-monopropionate (B-17-MP), which has high topical anti-inflammatory activity.
BECONASE 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.
Pharmacokinetics: 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 concentrations 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, 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 is moderately high (87%).
Elimination: The elimination of BDP and B-17-MP are characterised by high plasma clearance (150 and 120L/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. The renal clearance of BDP and its metabolites is negligible.

Prophylaxis and treatment of perennial and seasonal allergic rhinitis and vasomotor rhinitis.

BECONASE is for administration by the intranasal route only.
Adults and children over 6 years of age: The recommended dose is two applications into each nostril twice daily.
A dosage regimen of one application into each nostril three or four times daily may be preferred.
Total daily administration should not normally exceed 8 puffs (400 micrograms).
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.

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 overdose occurs, the patient should be treated supportively with appropriate monitoring as necessary. The only harmful effect that follows inhalation of larger 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.

BECONASE Aqueous Nasal Spray is contraindicated in patients with a history of hypersensitivity to any of its components.

Infections of the nasal passages and paranasal sinuses should be appropriately treated but do not constitute a specific contraindication to treatment with BECONASE Aqueous Nasal Spray.
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.
Systemic effects with nasal corticosteroids have been reported, 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. If recommended doses of intranasal beclometasone are exceeded or if individuals are particularly sensitive or predisposed by virtue of recent systemic steroid therapies, systemic effects may occur including reduction in growth velocity. Visual disturbance has been reported, including cataract, glaucoma or central serous chorioretinopathy.
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.
Effects on Ability to Drive and Use Machines: None reported.

(Pregnancy Category C): Administration of drugs during pregnancy should only be considered if the expected benefit to the mother is greater than any possible risk to the foetus.
There is inadequate evidence of safety of BECONASE in human pregnancy. In animal reproduction studies adverse effects typical of potent corticosteroids are only seen at high systemic exposure levels; direct intranasal application ensures minimal systemic exposure.
The excretion of beclometasone dipropionate in milk has not been studied in animals. It is reasonable to assume that beclometasone dipropionate is secreted in milk but at the dosages used for the intranasal application, there is low potential for significant levels in breast milk.
BECONASE should only be used in a nursing mother if the expected benefit justifies the risk to the infant.

Adverse reactions are listed as follows by system organ class and frequency. Frequencies are defined as: very common (≥1/10), common (≥1/100 and <1/10), uncommon (≥1/1,000 and <1/100), rare (≥1/10,000 and <1/1,000) and very rare (<1/10,000) including isolated reports. Very common, common and uncommon reactions were generally determined from clinical trial data. Rare and very rare reactions were generally determined from spontaneous data. In assigning adverse reactions 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.
Immune system disorders: Very rare: Hypersensitivity reactions including rashes, urticaria, pruritis, erythema and angioedema, anaphylactoid/anaphylactic reactions, bronchospasm.
Nervous system disorders: Common: Unpleasant taste, unpleasant smell.
Eye disorders: Very rare: Glaucoma, raised intraocular pressure, cataract.
Respiratory, thoracic and mediastinal disorders: Common: Epistaxis, nasal dryness, nasal irritation, throat dryness, throat irritation.
Very rare: Nasal septal perforation.

None reported.

Incompatibilities: None reported.

Store below 30°C.

Instructions for Use: Shake before use.
Your BECONASE spray has a dust cap which protects the nozzle and keeps it clean. Remember to take it off before using the spray.
A new spray, or one which has not been used for a few days, may not work the first time. You may need to 'prime' the bottle by pumping the spray a few times until a fine mist is produced.
To do this hold the bottle. Put your forefinger and middle finger on the collar either side of the nozzle and your thumb underneath the bottle.
Keeping your thumb still, press down with your fingers to pump the spray.
Hold the nozzle pointing away from you while you are doing this.
If the spray still doesn't work and you think it may be blocked, clean it as described as follows.
NEVER try to unblock it or enlarge the tiny spray hole with a pin or other sharp object because this will destroy the spray mechanism.
Using the spray: 1. Shake the bottle and remove the dust cap.
2. Blow your nose gently.
3. Close one nostril and put the nozzle in the other nostril. Tilt your head forward slightly and keep the bottle upright. Hold the bottle as previously described.
4. Start to breathe in slowly through your nose. WHILE YOU ARE BREATHING IN squirt a spray of fine mist into your nostril by pressing down firmly on the collar with your fingers.
5. Breathe out through your mouth. Repeat step 4 to take a second spray in the same nostril.
6. Remove the nozzle from this nostril and breathe out through your mouth.
7. Repeat steps 3 to 6 for the other nostril.
AFTER USING THE SPRAY Wipe the nozzle carefully with a clean tissue or handkerchief, and replace the dust cap.
To clean the spray: 1. Take the dust cap off.
2. Pull upwards on the white collar to remove the nozzle.
3. Soak the nozzle and dust cap in warm water for a few minutes, and then rinse under a running tap.
4. Shake off the excess water and allow to dry in a warm, NOT HOT, place.
5. Re-fit the nozzle.
6. 'Prime' the bottle if necessary by pumping the spray a few times until the fine mist is produced.
Your nasal spray should be cleaned at least once a week or more often if it gets blocked.

Nasal Decongestants & Other Nasal Preparations

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

E-D