Flunisolide Explained

Verifiedfields:changed
Verifiedrevid:461101454
Iupac Name:(1S,2S,4R,8S,9S,11S,12S,13R,19S)-19-fluoro-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.0<sup>2,9</sup>.0<sup>4,8</sup>.0<sup>13,18</sup>]icosa-14,17-dien-16-one
Tradename:Aerobid, Nasalide, Nasarel, others
Routes Of Administration:Inhaled
Protein Bound:40% after inhalation
Elimination Half-Life:1.8 hours
Iuphar Ligand:7076
Cas Number:3385-03-3
Atc Prefix:R01
Atc Suffix:AD04
Pubchem:82153
Drugbank:DB00180
Chemspiderid:74144
Unii:78M02AA8KF
Kegg:D00324
Chebi:5106
Chembl:1512
C:24
H:31
F:1
O:6
Smiles:O=C\1\C=C/[C@]2(/C(=C/1)[C@@H](F)C[C@H]3[C@H]4[C@](C[C@H](O)[C@H]23)([C@@]5(OC(O[C@@H]5C4)(C)C)C(=O)CO)C)C
Stdinchi:1S/C24H31FO6/c1-21(2)30-19-9-14-13-8-16(25)15-7-12(27)5-6-22(15,3)20(13)17(28)10-23(14,4)24(19,31-21)18(29)11-26/h5-7,13-14,16-17,19-20,26,28H,8-11H2,1-4H3/t13-,14-,16-,17-,19+,20+,22-,23-,24+/m0/s1
Stdinchikey:XSFJVAJPIHIPKU-XWCQMRHXSA-N
Synonyms:6α-Fluoro-11β,16α,17,21-tetrahydroxypregna-1,4-diene-3,20-dione acetone cyclic 16,17-acetal

Flunisolide (marketed as AeroBid among others) is a corticosteroid often prescribed as a treatment for allergic rhinitis.[1] Intranasal corticosteroids are the most effective medication for controlling symptoms.[2]

Flunisolide's principal mechanism of action is to activate glucocorticoid receptors, indicating an anti-inflammatory action. The effects of topical corticosteroids are not immediate and must be used for at least a few days for noticeable relief. As-needed use is less effective than regular recommended use.[2] Flunisolide should not be used for nasal infections. It should not be continued if symptoms are not relieved after regular use for over two to three weeks.[3]

Patented in 1958 and approved for medical use in 1978,[4] it is on the World Health Organization's List of Essential Medicines.[5]

Side effects

Temporary nose and throat dryness, irritation, bleeding, or unpleasant taste or smell may occur.[6] Nasal septum perforation has been rarely reported.[2] Rare but localized infections of the nose and pharynx with Candida albicans have also been reported. Its long-term use may raise the chances of cataracts or glaucoma.

Flunisolide nasal spray is absorbed into the circulatory system (blood).[3] Corticosteroid nasal sprays may affect the hypothalamic-pituitary-adrenal axis function in humans.[7] After obtaining the desired clinical effect, the maintenance dose should be reduced to the smallest amount required to control the symptoms. The amount can be as low as one spray in each nostril daily. Utilizing the minimum effective dose reduces possibility of side effects.[7] Recommended amounts of intranasal corticosteroids are generally not associated with systemic side effects.

Corticosteroids inhibit wound healing, so corticosteroid nasal sprays should be used cautiously in patients who have experienced recent nasal septal ulcers, recurrent epistaxis, nasal surgery or trauma, until healing.[3] In pregnancy, recommended doses of intranasal corticosteroids are safe and effective.[2]

Notes and References

  1. Web site: Flunisolide . DrugBank .
  2. Wallace DV, Dykewicz MS, Bernstein DI, Blessing-Moore J, Cox L, Khan DA, Lang DM, Nicklas RA, Oppenheimer J, Portnoy JM, Randolph CC, Schuller D, Spector SL, Tilles SA . 6 . The diagnosis and management of rhinitis: an updated practice parameter . The Journal of Allergy and Clinical Immunology . 122 . 2 Suppl . S1-84 . August 2008 . 18662584 . 10.1016/j.jaci.2008.06.003 . free .
  3. Web site: Flunisolide Nasal Solution . DailyMed . U.S. National Library of Medicine .
  4. Book: Fischer J, Ganellin CR . Analogue-based Drug Discovery . 2006 . John Wiley & Sons . 9783527607495 . 486 . en.
  5. Book: ((World Health Organization)) . World Health Organization model list of essential medicines: 22nd list (2021) . 2021 . 10665/345533 . World Health Organization . World Health Organization . Geneva . WHO/MHP/HPS/EML/2021.02 . free .
  6. Web site: FLUNISOLIDE - NASAL (Nasalide, Nasarel) side effects, medical uses, and drug interactions . MedicineNet .
  7. Web site: Nasalide (Flunisolide (Nasal Spray)) Drug Information: Clinical Pharmacology - Prescribing Information . RxList .