Aerobid, Aerobid M
Flunisolide has demonstrated marked anti-inflammatory and anti-allergic activity in classical test systems. It is a corticosteroid that is several hundred times more potent in animal anti-inflammatory assays than the cortisol standard. The molar dose of each activation of flunisolide in this preparation is approximately 2.5 to 7 times that of comparable inhaled corticosteroid products marketed for the same indication. The dose of flunisolide delivered per activation in this preparation is 10 times that per activation of Nasalide® (flunisolide) nasal solution. Clinical studies have shown therapeutic activity on bronchial mucosa with minimal evidence of systemic activity at recommended doses.
After oral inhalation of 1 mg flunisolide, total systemic availability was 40%. The flunisolide that is swallowed is rapidly and extensively converted to the 6/3-OH metabolite and to water-soluble conjugates during the first pass through the liver. This offers a metabolic explanation for the low systemic activity of oral flunisolide itself since the metabolite has the low corticosteroid potency (on the order of the cortisol standard). The inhaled flunisolide absorbed through the bronchial tree is converted to the same metabolites. Repeated inhalation of 2.0 mg of flunisolide per day (the maximum recommended dose) for 14 days did not show accumulation of the drug in plasma. The plasma half-life of flunisolide is approximately 1.8 hours.
The following observations relevant to systemic absorption were made in clinical studies. In one uncontrolled study a statistically significant decrease in responsiveness to metyrapone was noted in 15 adult steroid-independent patients treated with 2.0 mg of flunisolide per day (the maximum recommended dose) for 3 months. A small but statistically significant drop in eosinophils from 11.5% to 7.4% of total circulating leucocytes was noted in another study in children who were not taking oral corticosteroids simultaneously. A 5% incidence of menstrual disturbances was reported during open studies, in which there were no control groups for comparison.
Aerosol administration of flunisolide 2.0 mg twice daily for one week to 6 healthy male subjects revealed neither suppression of adrenal function as measured by early morning cortisol levels nor impairment of HPA axis function as determined by insulin hypoglycemia tests.
Controlled clinical studies have included over 500 patients with asthma, among them 150 children age 6 and over. More than 120 patients have been treated in open trials for two years or more. No significant adrenal suppression attributed to flunisolide was seen in these studies.
Significant decreases of systemic steroid dosages have been possible in flunisolide- treated patients. Recommended doses of flunisolide appear to be the therapeutic equivalent of an average of 10 mg/day of oral prednisone. Asthma patients have had further symptomatic improvement with flunisolide treatment even while reducing concomitant medication.
Last reviewed on RxList: 5/8/2008
This monograph has been modified to include the generic and brand name in many instances.
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