New Zealand - English - Medsafe (Medicines Safety Authority)
ELTAIR FORTE AQUEOUS nasal spray is a uniform, white, liquid suspension packed in a
12mL amber glass bottle fitted with a metered dose pump.
Budesonide is a non-halogenated corticosteroid. In investigations in animalsandman,
budesonide has shown a favourable relationship between local anti-inflammatory activityand
systemic glucocorticoid side effects overa wide dose range. This favourablerelationbetween
therapeuticeffectandsystemic side effects is due to budesonide's high glucocorticoid receptor
affinity and high first-pass metabolism with a short half-life.
The mechanism of action of intranasally administered budesonide has not yetbeencompletely
defined,however, budesonide has been shown to counteract the mainly IgE mediated lung
anaphylaxis in guinea pigs.
Pre-treatmentfor one week with intranasal budesonide 400mcg daily in asymptomatic patients
with seasonal rhinitis significantly inhibited the immediate reaction to allergen challenge.
Duetoextensivefirst pass metabolism in the liver, the oral bioavailability of budesonide is low
(approximately 10%). After nasal administration of a largedose(1mg)ofbudesonidefroma
metered dose aerosol the systemicallyavailable fraction is approximately 15%.
Negligible biotransformation occurs in human nasal mucosa.
Afternasalapplication of 100mcg, budesonide peak plasma concentrations of approximately
1nmol/L were observed with 45 minutes.
The volume of distribution of budesonide inadultmanis301.341.7L and in children is 3.1 to
4.8L/kg indicating a high tissue affinity. Plasma protein binding is 88.31.5% in humans.
Budesonide is metabolised in the liver to morepolarmetaboliteswithlowglucocorticoidactivity
(ie. 100 fold lower than the parent compound).
Theplasma half-life of budesonide in humans after nasal inhalation is 2.90.4 hours and the
plasma clearance of unchanged budesonide is 55.27.8L/hour.
Budesonide is indicated for the prophylaxis and treatment ofseasonalandperennialallergic
rhinitis, vasomotor rhinitis and symptomatic relief of nasal polyposis.
Adults and Children (6 years and older): Initially,total daily dose 400mcg given as 100mcg
into each nostril morning and evening, or as a single daily application of 200mcgintoeachnostril
in the morning. For patients with only mild symptoms, atotaldailydoseof200mcgmaybe
After a good therapeutic response has been achieved, the daily dosage may bereducedtoa
total daily dose of 200mcg.
In seasonal allergic rhinitis, treatment ideally should start before exposure to the allergen.
Patientsshouldbeadvisedtoclearnasal passages of secretions prior to use and not to exceed
For long-term treatment the lowest dose which keeps the patient symptom-free should be used.
Continuous long term use in children is not recommended.
Historyofhypersensitivity to preparations containing budesonide. Severe nasal infections,
especially candidiasis. Persons with recurrent nasal bleeding or haemorrhagic diatheses.
Warnings and Precautions
Clinical response: The full effect ofELTAIR FORTE AQUEOUSis not achieved until at least 2
to 3 days of treatment.
Unwanted effects: Systemiceffectsof nasal corticosteroids may occur particularly at high
doses prescribed for prolonged periods. These effects varybetweenpatientsanddifferent
corticosteroids.Theseeffectsare much less likely to occur than with oral corticosteroids and
may vary in individual patients and betweendifferentcorticosteroidpreparations.Potential
systemiceffects may include Cushing’s syndrome, Cushingoid features, adrenal suppression,
growthretardation in children and adolescents, cataract, glaucoma and more rarely a range of
psychological or behavioural effects includingpsychomotor hyperactivity, sleep disorders,
anxiety, depression or aggression (particularly in children).
Concomitant treatment: Concomitant treatment may sometimes be necessary to counteract
potential eye symptoms caused by the allergy.
Transfer from oral corticosteroids: Cautionshouldbe observed when transferring patients
previously treated with systemic corticosteroids toELTAIR FORTE AQUEOUS, particularly if
adrenal function deficiency may be present. During transfer patients mayneedsupplementary
systemic steroids during periods of stress.
Concomitant corticosteroid therapy: ShouldELTAIR FORTEAQUEOUSbe prescribed for
patients already using corticosteroids for oral inhalation, care should betakentoensurethatthe
combined daily intake via all routes of administration is consideredwhendeterminingtotaldaily
Intranasal corticosteroids may cause a reduction in growth velocity whenadministeredto
paediatric patients (See Paediatric Use)
Continuous, long termuse: In continuous, long term treatment, the nasal mucosa should be
inspected at least twice a year.
Severe nasal obstruction/congestion: In some patients with severe nasal obstruction and
congestion, concomitant treatment with local decongestants for 2-3 daysshouldbeconsidered,
eitherbefore commencing or together with, budesonide. Nasal polypectomy may be indicated
initially for patients with nasal obstruction due to nasal polyposis.
Tuberculosis: Whenevercorticosteroidadministrationis required in patients with quiescent or
activetuberculosis,therapeutic advantages should be weighed against possible undesirable
Infection: Ifinfectionoftherespiratorytract,nasal passages, or paranasal sinuses is present or
occurs during administration ofELTAIR FORTE AQUEOUS,adequate antibacterial therapy
should be promptly instituted.
Wound healing: Becauseof the inhibitory effect of corticosteroids on wound healing, patients
whohaveexperiencedrecentnasal septal ulcers, nasal surgery or trauma should not use a
nasal corticosteroid until healing has occurred.
Use in pregnancy: Administration during pregnancy should be avoided unless thereare
compelling reasons. In pregnant animals, administration of budesonide causesabnormalitiesof
foetal development. The relevance of these finding tomanhasnotbeenestablished.Iftreatment
with corticosteroids during pregnancy is unavoidable, inhaled corticosteroidsshouldbepreferred
becauseoftheirlowersystemiceffect compared with equipotent antiasthmatic doses of oral
Use during lactation: There is no information available on the passage of budesonide into
breastmilk.It is recommended, therefore, that breast-feeding be discontinued in women
Paediatric Use: ELTAIR FORTE AQUEOUS is not recommended for useinchildrenundersix
years of age.Controlled clinical studies have shown that intranasal corticosteroids may cause a
reductionin growth velocity in paediatric patients. This effect has been observed in the absence
oflaboratory evidence of hypothalamic-pituitary-adrenal (HPA) axis suppression, suggesting that
growthvelocity is a more sensitive indicatorof systemic corticosteroid exposure in paediatric
patients than some commonly used tests of HPA axis function.Thelong-termeffectsofthis
reductioningrowthvelocityassociatedwith intranasal corticosteroids, including the impact on
finaladultheight,areunknown.The potential for "catch up" growth following discontinuation of
treatmentwithintranasalcorticosteroidshasnot been adequately studied. The growth of
paediatricpatientsreceivingintranasal corticosteroids, should be monitored routinely (e.g. via
stadiometry). The potential growth effects of prolonged treatment shouldbeweighedagainst
clinical benefits obtained and the availability of safe and effective non corticosteroidtreatment
alternatives.Tominimizethesystemiceffects of intranasal corticosteroids, each patient should
be titrated to his/her lowest effective dose.
Carcinogenicity, Mutagenicity: Themutagenicpotential of budesonide was evaluated in 6
different test systems. No mutagenic or clastogenic properties were found.
Operation of motorised vehicle or machinery: Presumedto be safe or unlikely to produce an
effect on the ability to drive or use machinery.
Adverse local reactions following budesonide use are mild andusuallytransient.Systemic
corticosteroid side effects have not been reported during clinicalstudiesofbudesonidenasal
Adverse effects reported during studies with budesonide nasal presentations:
More Common (more than 1%):
Nose and throat: nasal irritation, haemorrhagic secretion or nose bleeding, dry mucous
membranes, sneezing after spraying, nasal crust.
Central Nervous System: Headache.
Uncommon (less than 1%):
Nose andthroat: itching, strong smell of spray, bad taste, itching of throat and larynx, sore
throat, dry mouth, earache.
Gastrointestinal: Loss of appetite, stomach disorder, nausea.
Skin and Appendages: Skin itching.
Central Nervous System: Tremor, tiredness, sedation.
Immune SystemDisorders :immediate or delayed hypersensitivity reaction (urticaria, rash,
itching, dermatitis, angioedema)
Rare (less than or equal to 0.2%):
Ear And Labyrinth Disorders : Ear itching
Musculoskeletal And Connective Tissue Disorders : joint aches, osteoporosis (with long term
Eye Disorders : glaucoma ( with long term treatment), cataract ( with long term treatment)
Veryrare (<0.01%): adrenal suppression
Laboratoryvariables: All changes in haematology, biochemistryandurinalysiswerewithinthe
normal range and were not considered clinically significant.
Budesonide is primarily metabolisedbytheenzymeCYP3A4, a subfamily of cytochrome P450.
The interaction between budesonide and inhibitors of CYP3A4 suchasketoconazoleand
itraconazole may result in increased systemic exposure to budesonide.
Inhibition of CYP3A4 increases the risk of Cushing’s syndrome, a condition due to
Budesonide 400mcg/day does not suppress the HPA axis as assessed by morning plasma
cortisol and synacthen tests. The dose of intra-nasal budesonide, which maycausesuppression
of the HPA axis, is not known. In the unlikely event of adrenal suppression duetopro-longed
excessive use of
ELTAIR FORTE AQUEOUS ,treatmentshouldbe discontinued, although normalisation of the
HPA-axis may be a slow process.
Store below 25 o C. Keep out of reach of children.
ELTAIR FORTE AQUEOUS: 100mcg/spray, 200 sprays.
Budesonide is 16,17-Butylidene bis (oxy)-11,21-dihydroxypregna-1,4-diene-3,20-dione.Ithasa
molecular formula and weight of C
and 430.55 respectively.
Other ingredients are: Purified water, Dispersible cellulose, Hydroxypropylmethylcellulose,
Sodium lauril sulphate, Polyethylene glycol 400, Butylated hydroxy Anisole, Sodium citrate, Citric
acid monohydate, Potassium sorbate and Disodium edetate.
Douglas Pharmaceuticals Ltd, P.O. Box 45-027, Auckland 0651
Ph: (09) 835-0660, Fax: (09) 835-0665
Date of Preparation
27 November 2012