Flunisolide

Janssen, P.A.J. U.S. Patent 3,773,939 November 20, 1973 assigned to Janssen Pharma-ceutica N.V. 

Chemical Name 16a,17a-lsopropylidenedioxy-6Q -fluoro-1,4-pregnadiene-11, 21-diol-3,20-dione 

20- dione 15 mg of crystalline 6Qi-fluoro-11j3,16a,17a,21-tetrahydroxy-1,4-pregnadiene- 

20- dlone [60 -fluoro-160 -hydroxyprednlsolone described in U.S. Patent 2338,546 and prepared as described in (a) above] Is dissolved in 2 ml of acetone and 0,02 ml of 70% perchloric acid is added. The solution Is allowed to stand 1 hour. Then 0.5 ml of saturated sodium bicarbonate solution is added and the solution concentrated under reduced pressure to about 

The solution is allowed to stand overnight and the crystals which form are filtered, washed with ether and recrystallized from acetone-hexane. The crystals are the 16a,17a-iso-propylidene derivative of 6Ql-fluoro-16Q -hydroxyprednisolone. 

Trade Name Manufacturer Country Year Introduced 

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Alprenolol HCl Bromelain Ciprofibrate Clortermine HCl Desonide Fenofibrate Flucloronide Flunisolide Fluocinonide Flurandrenolide Glucagon Gramicidin Hetacillin potassium I proniazid Kebuzone Methyltestosterone Niaprazine Probucol Relaxin Somatotropin Triamcinolone acetonide Acetonitrile... 

Narcotan - Halothane Narco26p Flunitrazepam Nardeizine Phenelzine sulfate Nardil - Phenelzine sulfate Narest Valethamate bromide Narigix Nalidixic acid Narsis - Medazepam Nasafarma - Oxymetazoline HCI Nazalide Flunisolide Nasal Yer Naphazoline Nasin Tetrahydrozoline HCI Nasivin - Oxymetazoline HCI Nasky Inositol niacinate Nasmil - Cromolyn sodium Nasophen - Phenylephrine HCI Natacillin - Hetacillln potassium Natacyn - Natamycin Natam - Flurazepam... 

Inhaled steroids (commonly used are beclomethasone, budesonide, triamcinolone, fluticasone, flunisolide) appear to attenuate the inflammatory response, to reduce bronchial hyperreactivity, to decrease exacerbations and to improve health status they may also reduce the risk of myocar dial infar ction, but they do not modify the longterm decline in lung function. Whether- steroids affect mortality remains unclear. Many patients appear to be resistant to steroids and large, long-term trials have shown only limited effectiveness of inhaled corticosteroid ther apy. Certainly, the benefit from steroids is smaller in COPD than in asthma. Topical side-effects of inhaled steroids are oropharyngeal candidiasis and hoarse voice. At the normal doses systemic side-effects of inhaled steroids have not been firmly established. The current recommendation is that the addition of inhaled gluco-coiticosteroids to bronchodilator treatment is appropriate for patients with severe to veiy sever e COPD. 

C24H33FOfi 1524-88-5) see Flunisolide flufenamic acid potassium salt (C14H9F3KNO2 35982-11-7) see Etofenamate flumetasone acetate... 

Currently, six intranasal corticosteroids—beclomethasone, budesonide, flunisolide, fluticasone, mometasone, and triamcinolone—are available commercially. Although all... 

Intranasal steroids are considered to have a slow onset of action (12-24 hours). Some patients may experience relief within a few days. Maximum treatment response may take up to several weeks to be observed.9,10,12 To achieve optimal effects, use at regular intervals is recommended.15 With the exception of beclomethasone and flunisolide, which are administered twice daily, the recommended doses for the intranasal corticosteroids are one to two sprays in each nostril once daily.15... 

Intranasal corticosteroids are the most effective anti-inflammatory agents used in pediatric patients with allergic rhinitis. Although fewer studies have been conducted in children, results demonstrate that intranasal corticosteroids are effective and well tolerated, with an adverse-effect profile similar to placebo. Mometasone is indicated for children as young as 2 years of age, fluticasone is indicated for children 4 years of age and older, and beclomethasone, budesonide, flunisolide, and triamcinolone are indicated for children 6 years and older.15 Because concerns regarding effect of intranasal steroids on growth exist, the growth of pediatric patients prescribed intranasal steroids should be monitored routinely via stadiometry. 

Corticosteroids (e.g., beclomethazone, flunisolide, triamcinolone) have anti-inflammatory and immunosuppressant actions. These drugs are used prophylactically to prevent the occurrence of asthma in patients with frequent attacks. Because they are not useful during an acute attack, corticosteroids are prescribed along with maintenance bronchodilators. These drugs are also administered by inhalation. Cromolyn is another anti-inflammatory agent used prophylactically to prevent an asthmatic attack. The exact mechanism of action of cromolyn is not fully understood however, it is likely to involve the stabilization of mast cells. This prevents the release of the inflammatory mast cell mediators involved in inducing an asthmatic attack. Cromolyn has proven effective in patients with exercise-induced asthma. 

Flunisolide — A steroid having marked anti-inflammatory activity,... 

Flunisolide is a fast-acting corticoid designed for the treatment of allergic rhinitis, asthma, and other allied respiratory disorders in humans. As the quantum of drug delivered by inhalation (/. e., the usual route of administration of the drug), is invariably small, the plasma-levels attained can also be fairly small. Hence, there is a dire need for a sensitive method of plasma concentration evaluation which is satisfied by radioimmunoassay. 

Flunisolide standards required for the preparation of the standard curve are obtained by dilution of a stock solution of 10 mg of it in 10 ml of ethanol,... 

An ethanolic solution of 3H-Flunisolide is diluted with tris-(hydroxymethyl)-aminomethane/hydro-chloric acid buffer and 0.1% gelatin such that 0.1 ml portion contains 8,000 to 10,000 cmp activity,... 

RIA is conducted by mixing together various dilutions of antiserum, buffer solution, 3H-Flunisolide and various dilutions of flunisolide standard solutions in a set of test tubes,... 

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