Nasarel;Nasalide;Flunisolide Hemihydrate;6-FLUORO-11,16ALPHA,17,21-TETRAHYDROXYPREGNA-1,4-DIENE-3,20-DIONE 16,17-ACETONIDE;Lunis;Nisolid;RS 3999;Synaclyn;Bronalide;Aerobid M
Synthetic fluorinated corticosteroid related to Prednisolone (P703740). Antiasthmatic.
일반 설명
The portion of a flunisolide (AeroBid,Nasarel) dose that is swallowed is rapidly converted to the6β-hydroxy metabolite after first-pass metabolism in theliver. The 6β-hydroxy metabolite is approximately as activeas hydrocortisone itself, but the small amount produced usuallyhas limited systemic effects. Water-soluble conjugatesare inactive.
Clinical Use
Flunisolide is an acetone ketal (acetonide) with a 6α-fluoro group and a free C-21 hydroxyl
group. The acetonide decreases mineralocorticoid activity, and the 6α-fluoro group increases
glucocorticoid activity. It is not a prodrug, because it has the free hydroxyl group at C-21.
Flunisolide has approximately 20% of the receptor affinity as budesonide, and approximately 40%
of the inhaled dose is systemically bioavailable.
신진 대사
When administered intranasally or by inhalation, flunisolide is rapidly absorbed
from nasal or lung tissue(94). This corticosteroid is efficiently metabolized by the liver to inactive
metabolites with no apparent effects on adrenal function with long-term therapy. Flunisolide that is swallowed undergoes extensive first-pass metabolism in the liver, and that which is absorbed directly from the
nasopharyngeal mucosa or lung bypasses this initial metabolism. It is not known if the drug undergoes
metabolism in the GI tract.
Flunisolide is rapidly hydroxylated by CYP3A4 at the 6β position, followed by
elimination of the 6α-fluoro group to its more polar 6β-hydroxy metabolite, which attains plasma concentrations
that usually are greater than those for flunisolide.
