Beclometasone Inhaled

Beclometasone is an inhaled corticosteroid (ICS) and the longest established controller in asthma, also used in COPD in combination. It is a prodrug activated by esterases in the lung to beclometasone 17-monopropionate. Effect builds over days to weeks.

Classification. Inhaled corticosteroid, glucocorticoid.

Mechanism. Binds the glucocorticoid receptor, suppressing eosinophilic airway inflammation and cytokine gene transcription, reducing hyperresponsiveness and exacerbations.

Pharmacokinetics. Extrafine solution inhalers deposit about 50 to 60% of the dose in the lung, conventional particle inhalers much less. The swallowed fraction has low bioavailability. Elimination half-life of the active metabolite is about 2 to 3 hours. Clearance depends little on CYP3A4, so beclometasone is the ICS least affected by ritonavir and cobicistat.

First-line, persistent asthma. The dose is set by particle size, which differs between inhalers.

• Conventional particle inhaler, adults: low 200 to 500 micrograms daily, medium over 500 to 1000 micrograms daily, high over 1000 micrograms daily, in 2 divided doses. Usual start 200 to 400 micrograms twice daily; maximum 800 micrograms twice daily under specialist direction.

• Extrafine particle inhaler, adults: about half the conventional dose. Start 100 micrograms twice daily; usual maximum 400 micrograms twice daily.

• Children 5 to 11 years: 100 micrograms twice daily, adjusted to the lowest effective dose. Higher doses only under specialist direction.

First-line, asthma maintenance and reliever therapy. Extrafine beclometasone with formoterol 100/6 micrograms: 1 to 2 inhalations twice daily as maintenance plus 1 inhalation as needed. Maximum 8 inhalations in 24 hours.

COPD. Not used alone. Combined with a LABA, or with a LABA and LAMA, in patients with frequent exacerbations and blood eosinophils of 300 cells/microlitre or more. A count under 100 cells/microlitre argues against adding a corticosteroid.

Alternative. Another ICS with a LABA, or add-on tiotropium or montelukast.

Emergency. Not used. Systemic corticosteroid is needed.

Titration. Start at a dose matched to severity, step down by about 25 to 50% every 3 months once control holds. No loading dose.

Contraindications. Hypersensitivity. Use with caution in active or quiescent pulmonary tuberculosis and untreated chest infection.

Serious adverse effects. Adrenal suppression and Cushingoid effects at high long-term doses, reduced growth velocity in children, cataract, glaucoma, reduced bone density, pneumonia in COPD, paradoxical bronchospasm.

Common adverse effects. Oropharyngeal candidiasis, hoarseness, cough, throat irritation.

Interactions. Minimal pharmacokinetic interactions. Additive hypokalaemia with beta-2 agonists in combination products.

Common prescribing errors. Mixing up conventional and extrafine doses. Prescribing a high dose without a spacer or mouth rinse. Stopping the controller when symptoms settle.

Special groups.

• Pregnancy: acceptable and preferable to uncontrolled asthma. Breastfeeding: compatible.

• Children: measure height at least annually.

• Older adults: monitor bone health and eyes on high doses.

• Kidney impairment: no adjustment. Liver impairment: no adjustment in mild disease; exposure increases in severe disease.

• East Africa: exclude active tuberculosis in a patient with chronic cough and weight loss before labelling asthma or COPD. Beclometasone is a practical choice in people on ritonavir-boosted regimens.

Formulations. Inhaler 50, 100, 200 and 250 micrograms/actuation depending on product; extrafine inhalers; dry powder; fixed combinations with formoterol or formoterol and glycopyrronium.

Technique. Use a spacer with inhalers. Rinse the mouth and spit after each dose.

Baseline. Spirometry or peak flow, symptom control score, exacerbation history, height in children.

Monitoring. Symptoms, reliever use, exacerbations, spirometry at 3 to 6 months, technique, height, eyes and bone health on prolonged high doses. Consider an emergency steroid card above 1000 micrograms daily of conventional particle drug.

Stop and reduce rules. Step down when control holds for 3 months. Therapeutic drug monitoring is not used.

Referral and escalation. Refer when control fails on high-dose ICS with a LABA or when oral corticosteroids are needed repeatedly.