General Medical Information

Nasal Glucocorticoid Preparations

Richard L. Mabry

The first nasal glucocorticoid introduced was dexamethasone, which was delivered with a fluorocarbon propellant and offered rapid onset of action. Dose-related systemic absorption occurs with this preparation, which has been withdrawn from the market in the United States.

Beclomethasone is available as a suspension delivered with a propellant and as an aqueous pump spray preparation. Each puff delivers approximately 42 µg of beclomethasone. The initial dosage is one spray in each nostril four times a day (suspension), two sprays in each nostril twice a day (aqueous), or two sprays in each nostril every day (double-strength aqueous), making a total daily dose of 336 µg. Published data indicate no adrenal suppression until a total daily dose of about 1,600 µg is reached. As with all nasal glucocorticoids, after improvement is noticed, dosage should be reduced to the lowest effective maintenance level. The maintenance dosage must be continued through the period of anticipated allergic symptoms. Effects can last for several days after the spray is discontinued.

Flunisolide nasal spray is contained in a polyethylene glycol base and is delivered with a pump spray. Each spray delivers about 25 µg of flunisolide, and the recommended initial adult dosage is two sprays in each nostril twice a day, making a total daily dose of 200 µg. About 50% of intranasally administered flunisolide is changed to a less active metabolite in the first pass through the liver. Endogenous cortisol production is suppressed at a flunisolide dosage of 700 µg/d.

Triamcinolone is delivered with either a propellant or a pump spray in an initial dosage of two puffs per nostril every day, for a total dose of 220 µg. Doses greater than 3,200 µg/d are needed to cause adrenal suppression. The vehicle of the aqueous form is said to be thixotropic, meaning it minimizes run-down into the pharynx after usage.

Budesonide is available in two forms delivered as a pressurized spray in an aqueous form. The metered-dose nasal spray is recommended at a dose of four puffs in each nostril for a total dose of 256 µg. The aqueous spray, at a recommended dose of one spray in each nostril once a day, delivers a total daily dose of 64 µg, which in this form appears to be clinically equivalent to the higher dose from the metered-dose spray. Dose-dependent suppression of endogenous cortisol has been reported after administration of 1,024 µg budesonide per day.

Fluticasone is a topically active glucocorticoid with poor gastrointestinal absorption and extensive first-pass hepatic metabolism. It is delivered with a pump spray, two sprays in each nostril every day, for a dose of 200 mg. No adrenal suppression has been found after regimens as high as 1,600 mg per day in initial studies. Both budesonide and fluticasone have been implicated in a small number of studies as producing evidence of systemic effects (suppression of serum cortisol and changes in peripheral lymphocyte markers and osteocalcitonin levels) at normal therapeutic doses. Debate continues about the implications of these studies.

Mometasone furoate is delivered in an aqueous pump spray once daily, providing a total daily dose of 200 mg. Because of near-total first-pass hepatic metabolism, this preparation is said to have a systemic bioavailability of less than 1%.
An additional means of administering glucocorticoids to relieve symptoms of allergic rhinitis while minimizing systemic effects is by means of intraturbinal injection of a repository form. This procedure was first reported in the medical literature in 1951. Its use was questioned in the 1960s because of reports of associated vision loss. In 1981, a thorough review of 10 documented cases indicated that the mechanism involved was reflex vasospasm or retrograde embolization into the retinal circulation. Suggestions for preventing these events have been widely published. When the proper technique is followed, the procedure is safe and effective. Safe intraturbinal glucocorticoid injection involves the following:

1. Pretreatment of the mucosa with a topical vasoconstrictor
2. Use of a repository glucocorticoid with small particle size, such as triamcinolone acetonide
3. Placement of the injection just beneath the mucosa of the anterior tip of the inferior turbinate
4. Gentle injection that avoids undue pressure

After it is determined that an injection is needed, a mixture of 0.5% phenylephrine and 2% lidocaine on cotton pledgets is placed on the mucosa along the anterior portions of the inferior turbinates. The procedure is explained to the patient both to gain informed consent and to forestall a vasovagal needle reaction. One milliliter of triamcinolone acetonide (40 mg) is drawn into a tuberculin syringe fitted with a 1.5-inch, 25-gauge needle. After removal of the pledgets, 0.5 mL of the glucocorticoid is gently injected just submucosally into the anterior tip of each inferior turbinate. If properly performed, the procedure is painless and causes slight white blanching of the mucosa around the injection site. The most important factor, that of avoiding undue pressure, sometimes necessitates turning the needle bevel or moving it slightly to facilitate infiltration. After each injection, a dry cotton pledget is applied momentarily to hold pressure on the injection site. The patient is warned to expect some blood-streaked nasal mucus. A few patients have facial flushing the next day. Injections are not repeated until symptoms return and never administered sooner than 4 to 6 weeks after the previous injection. Patients who need two or more intraturbinal glucocorticoid injections per year are candidates for definitive allergic rhinitis treatment (immunotherapy).