Budesonide is an inhaled corticosteroid used for the maintenance treatment of asthma, including in young children (from 12 months of age). It works by reducing airway inflammation. It is not intended to relieve an acute asthma attack — rapid-relief bronchodilators are used for that. It must be used regularly, as prescribed.
Also known as: Pulmicort, Budelin, budesónido
Clarithromycin may increase systemic exposure to inhaled budesonide, potentiating corticosteroid effects.
Budesonide (inhaled or oral) is metabolised in the liver by CYP3A4; clarithromycin, a potent inhibitor, can increase its systemic exposure and potentiate corticosteroid effects (Cushing's syndrome, hyperglycaemia, adrenal suppression, osteoporosis), especially with prolonged use and high inhaled doses. Monitor for corticosteroid excess signs, consider reducing the budesonide dose and prefer another antibiotic when possible.
Budesonide + clarithromycin: clarithromycin increases systemic budesonide exposure (CYP3A4 inhibition), with risk of corticosteroid effects. Monitor for corticosteroid excess signs.
Clarithromycin inhibits CYP3A4, which metabolises budesonide.
Monitor bruising, blood glucose and signs of adrenal suppression in at-risk patients.
Cushing's syndrome, adrenal suppression.
Monitor for signs of corticosteroid excess with prolonged use of the combination.
DailyMed (FDA) — approved Budesonide label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ae1105cd-69fc-4c15-937f-c535304341c2 ; approved Clarithromycin label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d836ae7e-fdbf-4dcb-a90d-ede1dcbc3e67 — additional reference: Prontuário Terapêutico do INFARMED (11th ed., 2012)
Alcohol may potentiate the GI risk of corticosteroids.
Limit alcohol intake.
EMC-UK (MHRA) — approved Budesonide SmPC: https://www.medicines.org.uk/emc/product/9715/smpc
Grapefruit (juice) inhibits CYP3A4 and increases budesonide exposure.
Avoid grapefruit juice during treatment.
EMC-UK (MHRA) — approved Budesonide SmPC: https://www.medicines.org.uk/emc/product/9715/smpc
Inhaled corticosteroids may mask or worsen respiratory infections, including tuberculosis.
Monitor and treat intercurrent infections; consider prophylaxis per local guidelines.
EMC-UK (MHRA) — approved Budesonide SmPC: https://www.medicines.org.uk/emc/product/9715/smpc
The FDA RHINOCORT AQUA label (nasal budesonide) documents in section 5.7: "Glaucoma and cataracts: Close monitoring is warranted". Intranasal corticosteroids may increase intraocular pressure in susceptible patients, including those with pre-existing open-angle glaucoma; the rise in intraocular pressure may go undetected without tonometry, so periodic ophthalmological monitoring is recommended during prolonged use, especially in patients with a history of glaucoma or cataracts.
Periodic ophthalmological monitoring (intraocular pressure and lens) in patients with glaucoma or cataracts on prolonged nasal budesonide; watch for symptoms such as eye pain, blurred vision or visual changes.
DailyMed/FDA (NIH/NLM) — approved Budesonide nasal spray RHINOCORT AQUA label (Physicians Total Care), section 5.7 Glaucoma and cataracts: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ffca32a2-fbef-40bb-b0f0-73f63e18e747
The FDA RHINOCORT AQUA label documents in section 5.3 (Immunosuppression) the potential worsening of infections: "Potential worsening of infections (e.g., existing tuberculosis, fungal, bacterial, viral, or parasitic infections; or ocular herpes simplex). Use with caution in patients with these infections". Nasal corticosteroids may suppress local and systemic immune responses, favouring the spread of active infections; patients with untreated fungal, bacterial, viral or parasitic infections (and ocular herpes simplex) should use the drug with caution. Active or latent tuberculosis is already covered by its own dimension (tuberculose) — this dimension covers the remaining infections.
Use with caution in patients with active infection (fungal, bacterial, viral, parasitic or ocular herpes simplex); treat the infection before starting or during nasal budesonide use and monitor for worsening.
DailyMed/FDA (NIH/NLM) — approved Budesonide nasal spray RHINOCORT AQUA label (Physicians Total Care), section 5.3 Immunosuppression: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ffca32a2-fbef-40bb-b0f0-73f63e18e747
Inhaled budesonide is the corticosteroid of choice in pregnancy, with low systemic exposure.
Can be used in all trimesters when asthma requires it.
Excreted in small amounts into breast milk; compatible with breastfeeding.
No specific additional contraception.
EMC-UK (MHRA) — approved Budesonide SmPC: https://www.medicines.org.uk/emc/product/9715/smpc ; Prontuário Terapêutico do INFARMED (11th ed., 2012) — Annex 2, Drugs and Breastfeeding: See Corticosteroids.
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Inhaled corticosteroid with high affinity for the glucocorticoid receptor, with potent local anti-inflammatory action in the airways and low systemic bioavailability — indicated for asthma maintenance in children (12 months-8 years).
Binds the cytoplasmic glucocorticoid receptor, modulating gene transcription: increases synthesis of anti-inflammatory proteins (lipocortin-1, IκB) and inhibits pro-inflammatory cytokines, chemokines and inflammatory enzymes (COX-2, iNOS) — reduced airway inflammation and bronchial hyperresponsiveness.
After nebulisation, total systemic bioavailability (lung + oral) is ~6% of the dose; plasma peak ~20 min after a 1 mg nebulised dose (2.6 nmol/L); protein binding 85-90%; volume of distribution 3 L/kg.\n\nNasal route (RHINOCORT AQUA, 128 mcg): mean peak plasma concentration of ~0.3 nmol/L about 0.5 h post-dose; approximately 34% of the delivered intranasal dose reaches the systemic circulation, mostly absorbed through the nasal mucosa (FDA label).
Rapid, extensive hepatic metabolism by CYP3A4 to 16α-hydroxyprednisolone and 6β-hydroxybudesonide (activity <1% of the parent); high systemic clearance (~0.5 L/min in children); urinary (~60% IV) and faecal excretion as metabolites; no unchanged budesonide in urine.
Terminal half-life ~2.3 h after nebulisation in children with asthma; systemic clearance ~0.5 L/min (≈50% higher than in adults).
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
