PULMICORT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PULMICORT (PULMICORT).
Glucocorticoid receptor agonist; inhibits inflammatory mediators, reduces airway edema and mucus secretion.
| Metabolism | Primarily hepatic via CYP3A4; extensive first-pass metabolism. |
| Excretion | Budesonide is primarily metabolized in the liver via CYP3A4 to inactive metabolites. Approximately 60% of the dose is excreted in urine as metabolites, and 40% in feces. Less than 10% of unchanged drug is excreted renally. |
| Half-life | The terminal elimination half-life of budesonide is approximately 2.0 to 3.6 hours in adults, with a mean of about 2.8 hours. This short half-life is consistent with its rapid clearance and lack of significant accumulation with once- or twice-daily dosing. |
| Protein binding | Budesonide is 85-90% bound to plasma proteins, primarily albumin. Binding is linear over the therapeutic concentration range. |
| Volume of Distribution | The volume of distribution of budesonide is approximately 2.5 to 3.0 L/kg (range 1.9-3.8 L/kg), indicating extensive tissue distribution. This large Vd reflects its lipophilic nature and penetration into tissues including lung parenchyma. |
| Bioavailability | Inhaled budesonide: Absolute bioavailability is approximately 11-15% for the dry powder inhaler (Pulmicort Flexhaler) and about 11-18% for the pressurized metered-dose inhaler. Oral bioavailability is low (<1%) due to extensive first-pass metabolism. Intranasal budesonide: Bioavailability is approximately 21-34% for the aqueous suspension (Rhinocort). |
| Onset of Action | For inhaled Pulmicort (budesonide), onset of clinical effect (improvement in asthma control) is typically observed within 24 hours to 1 week, with maximal benefit achieved after 1-2 weeks or longer. For intranasal administration, relief of allergic rhinitis symptoms may begin within 10-12 hours, with full effect in several days. |
| Duration of Action | The duration of action for inhaled budesonide is approximately 12 to 24 hours, supporting once-daily dosing in many patients. The effect persists for at least 12 hours after a single dose. For intranasal use, symptomatic relief lasts for about 24 hours with regular use. |
| Molecular Weight | 430.53 |
| Action Class | Inhalational Corticosteriods |
| Brand Substitutes | Budez 100mcg Inhaler, Bunase 100mcg Inhaler, Derinide 100 Inhaler CFC Free, Budecort 100 Inhaler, Sappal 200mcg Inhaler, Solbihale B 200mcg Inhaler, Budez 200mcg Inhaler, Pneumabud 200 Inhaler CFC Free, Breemax 200mcg Inhaler |
Inhalation: 200-800 mcg twice daily for maintenance; maximum 1600 mcg/day. Nebulization: 0.5-1 mg twice daily.
| Dosage form | POWDER, METERED |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No specific guidelines; use caution in severe hepatic impairment (Child-Pugh C) due to potential decreased clearance. No dose adjustment recommended. |
| Pediatric use | Inhalation: Children >6 years: 200-400 mcg twice daily; maximum 800 mcg/day. Children 1-5 years: 0.25-0.5 mg via nebulization once or twice daily. Infants <1 year: 0.25-0.5 mg via nebulization once or twice daily. |
| Geriatric use | No specific dose adjustment required; use lowest effective dose due to potential for increased systemic effects. Monitor for adrenal suppression and oral candidiasis. |
| 1st trimester | Inhaled budesonide is preferred for asthma control during first trimester due to minimal systemic absorption; no increased risk of major congenital malformations reported. |
| 2nd trimester | Considered safe; use lowest effective dose to maintain asthma control. No known fetal adverse effects at standard doses. |
| 3rd trimester | Safe; important to maintain asthma control to prevent maternal hypoxia. No association with preterm birth or low birth weight. |
Clinical note
Comprehensive clinical and safety monograph for PULMICORT (PULMICORT).
| Placental transfer | Budesonide undergoes partial placental metabolism (11β-HSD2) reducing fetal exposure. Inhaled budesonide results in low maternal plasma levels; placental transfer is minimal (<10% of maternal dose). |
| Breastfeeding | Very low oral bioavailability (<11% after inhalation) leads to negligible infant exposure. Budesonide is excreted in breast milk in amounts equivalent to <0.4% of maternal weight-adjusted dose. Monitor infant for potential growth suppression, though risk is minimal. |
■ FDA Black Box Warning
None
| Serious Effects | Adrenal insufficiency (especially with high doses or prolonged use), Increased risk of pneumonia in patients with COPD, Oropharyngeal candidiasis, Growth suppression in children, Osteoporosis with long-term use, Glaucoma and cataracts, Hypersensitivity reactions including anaphylaxis |
Hypersensitivity to budesonide or any component of formulation
| Precautions | May cause adrenal insufficiency during stress or withdrawal, Increased risk of pneumonia in COPD patients, Oropharyngeal candidiasis, Growth suppression in children, Hypothalamic-pituitary-adrenal axis suppression |
| Food/Dietary | No significant food interactions. Grapefruit may increase systemic budesonide levels; avoid large amounts of grapefruit or grapefruit juice. |
Loading safety data…
| Lactation Rating | L1 - Safest |
| Teratogenic Risk | PULMICORT (budesonide) is an inhaled corticosteroid. Based on human data, the risk of major congenital malformations, including orofacial clefts, is not significantly increased with inhaled budesonide during pregnancy. However, high-dose systemic corticosteroids are associated with an increased risk of oral clefts and fetal growth restriction. Budesonide has low systemic bioavailability after inhalation, minimizing fetal exposure. First trimester: No clear evidence of increased malformation risk; second/third trimester: No known specific fetal risks but monitor for potential adrenal suppression in neonates if high doses used. |
| Fetal Monitoring | Monitor maternal asthma control: peak expiratory flow (PEF) and symptoms. Assess fetal growth by serial ultrasound if chronic high-dose systemic corticosteroids are used (unlikely with inhaled budesonide). In neonates, monitor for signs of adrenal insufficiency if mother has received significant systemic corticosteroid exposure (rare with inhalation). |
| Fertility Effects | No known adverse effects on fertility in humans. Animal studies at high systemic doses showed fertility impairment, but clinical relevance is negligible due to low systemic exposure with inhaled budesonide. |
| Clinical Pearls | 1. Pulmicort (budesonide) is an inhaled corticosteroid for maintenance therapy of asthma; not for acute bronchospasm. 2. Rinse mouth after each use to prevent oral candidiasis and dysphonia. 3. Titrate to lowest effective dose to minimize systemic effects. 4. Monitor growth in children due to potential growth suppression. 5. Nebulized suspension can be mixed with albuterol or ipratropium if compatible. |
| Patient Advice | Use regularly as prescribed to control asthma; do not use for sudden breathing problems. · Rinse mouth with water after each use to prevent thrush and hoarseness. · Do not stop taking suddenly; consult doctor before discontinuing. · Keep track of symptoms and peak flow; report worsening to your doctor. · Shake inhaler well before use; use a spacer if prescribed. |