Flunisolide

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Belgium: Syntaris; France: Nasalide; Germany: Syntaris; Italy: Aerflu, Aerolid, Asmaflu AD, Assolid, Astian, Careflu AD, Charlyn, Citiflux, Desaflu, Doricoflu, Eliosid, Euroflu, Fluminex, Flunigar, Flunisolide, Flunitop A, Forbest AD, Givair, Kaimil, Lunibron, Lunis, Multinebulgen, Nambrol, Nebulcort, Nebulgen, Nereflun, Nisolid AD, Nisoran, Plaudit AD, Pulmist, Saflineb, Syntaris; Luxembourg: Broncort, Syntaris; Netherlands: Syntaris; Greece: Bronalide.

North America

Canada: Flunisolide, Nasalide, Rhinalar; USA: AeroBid, Aerospan HFA, Flunisolide, Nasarel.

Asia

Japan: Synaclyn.

Drug combinations

Chemistry

Flunisolide: C~24~H~31~FO~6~ ½H~2~O. Mw: 443.51. (1) Pregna-1,4-diene-3,20-dione, 6-fluoro-11,21-dihydroxy-16,17-[(1-methylethylidene)bis(oxy)]-, hemihydrate, (6α,11 β,16α)-; (2) 6α-Fluoro-11β,16α,17,21-tetrahydroxypregna-1,4-diene-3,20-dione cyclic 16,17-acetal with acetone, hemihydrate. CAS-77326-96-6; CAS-3385-03-3 (anhydrous)(1974).

Pharmacologic Category

Hormones and Synthetic Substitutes; Adrenals. EENT Preparations; Anti-inflammatory Agents; Corticosteroids. (ATC-Code: R01AD04; R03BA03).

Mechanism of action

Flunisolide is a synthetic fluorinated glucocorticoid. Decreases inflammation by suppression of migration of polymorphonuclear leukocytes and reversal of increased capillary permeability. Does not depress hypothalamus.

Therapeutic use

Oral inhalation for long-term prevention of bronchospasm in asthma.

Pregnancy and lactiation implications

No data on crossing placenta or effects on fetus. Unknown whether flunisolide is distributed into milk. Caution if used in nursing women.

Unlabeled use

Contraindications

Hypersensitivity to flunisolide or any component of the formulation. Acute status asthmaticus. Viral, tuberculosis, fungal, or bacterial respiratory infections. Infections of the nasal mucosa.

Warnings and precautions

May cause hypercorticism or suppression of HPA axis, (may lead to adrenal crisis). Withdrawal and discontinuation should be carried out slowly. Bronchospasm may occur with wheezing after inhalation. Avoid nasal corticosteroid use in recent nasal septal ulcers, nasal surgery or nasal trauma until healing has occurred. Prolonged use may increase incidence of secondary infection, mask acute infection (including fungal infections), prolong or exacerbate viral infections, or limit response to vaccines. Exposure to chickenpox should be avoided; corticosteroids should not be used to treat ocular herpes simplex. Should not be used for cerebral malaria. Restrict use in active tuberculosis (only in conjunction with antituberculosis treatment). Prolonged treatment with corticosteroids associated with development of Kaposi’s sarcoma (case reports). Corticosteroid use may cause psychiatric disturbances, including depression, euphoria, insomnia, mood swings, and personality changes, and pre-existing psychiatric conditions may be exacerbated. Not to be used in status asthmaticus or for relief of acute bronchospasm. Use with caution in heart failure (long-term use may cause fluid retention and hypertension), diabetes mellitus (may alter glucose production/regulation leading to hyperglycemia), GI diseases (diverticulitis, peptic ulcer, ulcerative colitis), hepatic impairment, including cirrhosis (long-term use may cause fluid retention), or in myasthenia gravis (exacerbation of symptoms has occurred especially during initial treatment with corticosteroids). Use with caution following acute MI (corticosteroids may cause myocardial rupture). Use with caution in cataracts and/or glaucoma (increased intraocular pressure, open-angle glaucoma, and cataracts have occurred with prolonged use). Use with caution in osteoporosis (high doses and/or long-term use of corticosteroids associated with increased bone loss and osteoporotic fractures). Use with caution in renal impairment (fluid retention might occur). Use with caution in history of seizure disorder (seizures reported with adrenal crisis). Changes in thyroid status may occur (increased metabolic clearance of corticosteroids in hyperthyroidism and decreased in hypothyroidism). Orally-inhaled and intranasal corticosteroids may cause a reduction in growth velocity in pediatric patients. There have been reports of systemic corticosteroid withdrawal symptoms (e.g. joint/muscle pain, lassitude, depression) when withdrawing oral inhalation therapy.

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