Inhaled Steroids

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Chapter: Essential pharmacology : Drugs for Cough and Bronchial Asthma

These are glucocorticoids with high topical and low systemic activity (due to poor absorption and/or marked first pass metabolism).


INHALED STEROIDS

 

These are glucocorticoids with high topical and low systemic activity (due to poor absorption and/or marked first pass metabolism).Beclomethasone dipropionate, Budesonide and Fluticasone have similar properties. Ciclesonide is a new addition. Because airway inflammation is present in early mild disease as well, and bronchial remodeling starts developing from the beginning, it has been suggested that inhaled steroids should be the ‘step one’ for all asthma patients. However, currently inhaled steroids are not considered necessary for patients with mild and episodic asthma. They are indicated when inhaled β2 agonists are required almost daily or the disease is not only episodic. Start with 100–200 μg BD, titrate dose upward every 3–5 days; max. 400 μg QID, beyond which no further benefit generally occurs.

 

Inhaled steroids suppress bronchial inflammation, increase peak expiratory flow rate, reduce need for rescue β2agonist inhalations and prevent episodes of acute asthma. However, they have no role during an acute attack or in status asthmaticus. Peak effect is seen after 4–7 days of instituting inhaled steroids and benefit persists for a few weeks after discontinuation. They can be started in patients who in past have required oral steroids as well as in those with no such history. Patients who are to be switched over from oral steroid should receive inhaled steroid in addition for 1–2 weeks before the former is tapered, otherwise steroid withdrawal may manifest (precipitation of asthma, muscular pain, lassitude, depression, hypotension). This confirms lack of systemic activity of inhaled steroids (at doses < 600 μg/day). Long term experience has shown that efficacy of inhaled steroids is maintained and reinstitution of oral steroids is seldom needed. Short courses of oral steroids may be added during periods of exacerbation. Some patients who remain well controlled for long periods can even stop inhaled steroids without worsening of asthma.

 

COPD: High dose inhaled steroids are beneficial only in advanced COPD with frequent exacerbations; should not be used in early/mild cases. There is no proof that they slow disease progression.

 

Hoarseness of voice, dysphonia, sore throat, asymptomatic or symptomatic oropharyngeal candidiasis are the most common side effects. These can be minimized by the use of a spacer, gargling after every dose (to wash off the drug deposited on oral and pharyngeal mucosa) and prevented as well as treated by topical nystatin/ clotrimazole. There is no evidence of mucosal damage or increased incidence of chest infections, even on prolonged use.

 

Systemic effects of long term inhaled glucocorticoids are clinically relevant only at doses 600 μg/day. The significant ones are—mood changes, osteoporosis, growth retardation in children, bruising, petechiae, hyperglycaemia and pituitary adrenal suppression; several reports of adrenal crisis have appeared, especially in children, during stress (of an infection, etc).

 

Inhaled steroids are safe during pregnancy.

 

Beclomethasone dipropionate

 

BECLATE INHALER 50 μg, 100 μg, 200 μg per metered dose, 200 doses inhaler, BECORIDE 50, 100, 250 μg per puff inhaler.

BECLATE ROTACAPS (with rotahaler) 100, 200, 400 μg powder per cap.

AEROCORT INHALER 50 μg/metered aerosol dose with salbutamol 100 μg.

AEROCORT ROTACAPS 100 μg with salbutamol 200 μg rotacaps (with rotahaler).

 

Intranasal spray (50 μg in each nostril BD–TDS) is effective in perennial rhinitis.

 

Budesonide A nonhalogenated glucocorticoid with high topical: systemic activity ratio; claimed to be better than beclomethasone. Small fraction that is absorbed is rapidly metabolized.

 

Dose: 200–400 μg BD–QID by inhalation in asthma; 200– 400 μg/day by intranasal spray for allergic rhinitis.

 

PULMICORT 100, 200, 400 μg/metered dose inhaler, BUDECORT 100 μg/metered dose inhalation. FORACORT: Formoterol 6 μg + Budesonide 100 μg/200 μg rotacaps.

RHINOCORT 50 μg per metered dose nasal spray; BUDENASE AQ 100 μg metered dose aqueous nasal spray; for prophylaxis and treatment of seasonal and perennial allergic or vasomotor rhinitis, nasal polyposis; initially 2 puffs in each nostril every morning, maintenance 1 puff in each nostril in the morning.

 

Nasal irritation, sneezing, crusting, itching of throat and dryness may occur, especially in the beginning. Contraindicated in presence of infection or nasal ulcers.

 

Fluticasone propionate This newer inhaled glucocorticoid has high potency, longer duration and negligible oral bioavailability. The dose swallowed after inhalation has little propensity to produce systemic effects. At high doses, systemic effects may be due to absorption from the lungs. The inhalational dose is 100–250 μg BD (max 1000 μg/day).

FLOHALE INHALER 25 μg, 50 μg, 125 μg per actuation.

FLOHALE ROTACAPS 50 μg, 100 μg, 250 μg rotacaps.

FLOMIST 50 μg per actuation nasal spray.

 

Flunisolide This topical steroid is available for prophylaxis and treatment of seasonal and perennial rhinitis.

 

SYNTARIS 25 μg per actuation nasal spray; one spray in each nostril 2–3 times daily.

 

Ciclesonide This inhalational steroid utilizes a novel approach to improve topical: systemic activity ratio. It is a prodrug that is cleaved by esterases in the bronchial epithelium to release the active moiety. Though it is absorbed from the lungs, oral bioavailability is <1%. In the circulation it is extensively bound to plasma proteins, further minimizing exposure of tissue cells to the free and active drug.

 

Dose: 80–160 μg by inhalation OD, preferably in the evening. CICLEZ 80 μg and 160 μg per metered dose inhaler with HFA propellant.

 

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