Glucocorticoids flunisolide

Beclomethasone dipropionate, and several other glucocorticoids—primarily budesonide and flunisolide and mometasone furoate, administered as aerosols—have been found to be extremely useful in the treatment of asthma (see Chapter 20). 

Topical administration to the nose The safety of nasal glucocorticoids in the treatment of allergic rhinitis has been reviewed (434,435). The local application of glucocorticoids for seasonal or perennial rhinitis often results in systemic adverse effects. The use of nasal sprays containing a glucocorticoid that has specific topical activity (such as beclomethasone dipropionate or flunisolide) seems to reduce the systemic adverse effects, but they can nevertheless occur, even to the extent of suppression of basal adrenal function in children (436). Local adverse effects include Candida infection, nasal stinging, epistaxis, throat irritation (437), and, exceptionally, anosmia (438). 

Beclomethasone dipropionate and several other glucocorticoids—primarily budesonide and flunisolide and mometasone furoate, administered as aerosols—have been found to be effective in the treatment of asthma (see Chapter 20 Drugs Used in Asthma). The switch from therapy with systemic glucocorticoids to aerosol therapy must be undertaken with caution, since manifestations of glucocorticoid deficiency will appear if adrenal function has been suppressed. In such patients, a slow, graded reduction of systemic therapy and monitoring of endogenous adrenal function should accompany the institution of aerosol administration. 

The equivalence of inhaled glucocorticoids based on equipotent (cortisol suppression) effects has been studied by the Asthma Clinical Research Network (ACRN). Six different inhaled glucocorticoids and matched placebos (beclomethasone chlorofluorocarbon, budesonide dry powder inhaler, fluticasone dry powder inhaler, fluticasone chlorofluorocarbon metered-dose inhaler, flunisolide chlorofluorocarbon, and triamcinolone chlorofluorocarbon) were compared by measuring their systemic effects (18). 

There are three aerosolized corticosteroid preparatioias available in MDI formulation for administration to horses via the Equine AeroMask beclometasone dipropionate, fluticasone propionate and flunisolide (Table 16.2). In terms of the relative potency, fluticasone is more potent than beclometasone, which is more potent than flunisolide, which is equipotent to triamcinolone. Using dexamethasone as the standard (1.0), the relative glucocorticoid receptor affinity of the common corticosteroids is flunisolide 1.9, triamcinolone 2.0, beclometasone (active metabolite) 13.5 and fluticasone propionate 22.0 (Barnes et al 1998). The pulmonary residence time of the aerosolized corticosteroids is determined by the lipophilicity of each drug. Flunisolide has intermediate water solubility (lOmg/ml), simitar to... 

Albuterol is used to relieve and prevent bronchospasm in patients with reversible obstructive airway disease and in individuals with exercise-induced bronchospasm. The onset of action of albuterol is 5 to 15 minutes, peak of action is 0.5 to 2 hours, and duration of action is 3 to 6 hours. Albuterol does not cross the blood-brain barrier. It must be used cautiously in patients with hyperthyroidism, diabetes mellitus, coronary insufficiency, and hypertension. The concomitant use of albuterol with monoamine oxidase inhibitors or tricyclic antidepressants should be discouraged. Glucocorticoids (beclomethasone, dexametha-sone, flunisolide, or triamcinolone) may be used 15 minutes after inhalational albuterol. 

Flunisolide, a glucocorticoid with antiinflammatory and antiasthmatic properties (two inhalants b.i.d.) is used in steroid-dependent asthma (see also Table 14). 

Flunisolide is an extremely potent synthetic fluorinated glucocorticoid. It is administered by metered dose inhaler. 

Flunisolide is an acetone ketal (acetonide) with a 6a-fluoro group and a free C-21 hydroxyl group. The acetonide decreases mineralocorticoid activity, and the 6a-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. Flunisolide is quickly metabolized by CYP3A4 to the 6p-hydroxy metabolite, which has less than 1% of the activity of the parent compound. This,... 

Glucocorticoids (steroids) can be administered orally, via aerosol inhalation, intramuscularly, and intravenously. Glucocorticoids used for aerosol inhalation use beclomethasone (Beconase, Vanceril), dexamethasone (decadron), flunisolide (Aerobid, NasaMd), or triamcinolone (Azmacort, Kenalog, Nasacort). 

Unextracted calibrator for glucocorticoids Prepared in methanol by adding prednisone, prednisolone, cortisone, hydrocortisone, 6a-methylprednisolone, fluocortolone, fludrocortisone, dexamethasone, triamcinolone, beclomethasone, flumethasone, desonide, budesonide, flunisolide, fluticasone propionate, and carvedilol, each at 1.5 pg/mL 17a-methyltestosterone at... 

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