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. |
| 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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PULMICORT (PULMICORT).
| Breastfeeding | Budesonide is excreted into breast milk in low amounts. The milk-to-plasma (M/P) ratio is approximately 0.4. The estimated daily infant dose is about 0.3% to 1% of the maternal weight-adjusted dose, which is unlikely to cause adverse effects in the infant. Compatible with breastfeeding with caution; monitor infant for signs of adrenal suppression if mother is on high doses. |
| 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. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to budesonide or any component","Status asthmaticus or acute asthma attacks (not for primary treatment)"]
| 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"] |
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| 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. |