QVAR REDIHALER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for QVAR REDIHALER (QVAR REDIHALER).
Beclomethasone dipropionate is a prodrug that is hydrolyzed by esterases to the active metabolite beclomethasone-17-monopropionate (17-BMP). 17-BMP is a glucocorticoid receptor agonist that binds to the glucocorticoid receptor, leading to modulation of gene expression involved in inflammatory pathways, including inhibition of pro-inflammatory cytokines, reduction of eosinophil survival and migration, and suppression of mast cell mediators.
| Metabolism | Beclomethasone dipropionate is extensively metabolized in the liver and extrahepatic tissues (including lung and plasma) by esterases to the active metabolite beclomethasone-17-monopropionate (17-BMP) and inactive metabolites. CYP3A4 may also contribute to metabolism but to a minor extent. |
| Excretion | Primarily hepatic metabolism via CYP3A4; metabolites are excreted in feces (~64%) and urine (~12%). |
| Half-life | 1.5-2.0 hours (terminal half-life) after inhalation; supports twice-daily dosing. |
| Protein binding | 87-90%; primarily to albumin. |
| Volume of Distribution | 0.3-0.5 L/kg; indicates distribution primarily into lung tissue and central compartment. |
| Bioavailability | Inhalation: approximately 30% systemic bioavailability due to first-pass metabolism; oral: <1%. |
| Onset of Action | 1-2 weeks for maximal therapeutic effect; some improvement within 24 hours. |
| Duration of Action | Up to 12 hours after inhalation; clinically dosed twice daily. |
Inhalation: 40-80 mcg twice daily; maximum 320 mcg twice daily.
| Dosage form | AEROSOL, METERED |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No formal studies; use with caution in severe hepatic impairment (Child-Pugh C) due to potential increased systemic exposure. |
| Pediatric use | Children 4-11 years: 40 mcg twice daily; maximum 80 mcg twice daily. Children 12 years and older: same as adults. |
| Geriatric use | No specific dose adjustment needed; monitor for local adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for QVAR REDIHALER (QVAR REDIHALER).
| Breastfeeding | Beclomethasone dipropionate is excreted in human breast milk in low concentrations; M/P ratio unknown. Considered compatible with breastfeeding due to minimal systemic absorption from maternal inhalation. Use lowest effective dose. |
| Teratogenic Risk | No teratogenic effects demonstrated in human studies. Inhaled corticosteroids (ICS) like beclomethasone dipropionate are not associated with major congenital malformations. First trimester: no increased risk. Second/third trimester: potential for fetal growth restriction with high doses, but benefit of asthma control outweighs risk. |
■ FDA Black Box Warning
None
| Serious Effects |
["Primary treatment of status asthmaticus or other acute episodes of asthma where intensive measures are required","Hypersensitivity to beclomethasone dipropionate or any ingredient in the formulation"]
| Precautions | ["Localized oral and pharyngeal candidiasis","Increased risk of adrenal insufficiency during transfer from systemic corticosteroids","Potential for growth suppression in pediatric patients","Paradoxical bronchospasm","Need for monitoring of asthma control; not for acute bronchospasm","Possible systemic corticosteroid effects with high doses or prolonged use"] |
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| Fetal Monitoring | Monitor maternal asthma control (symptom scores, peak expiratory flow rate). Ultrasound for fetal growth if high-dose ICS used long-term. Assess for maternal hypothalamic-pituitary-adrenal axis suppression if using >1000 mcg/day. |
| Fertility Effects | No evidence of impaired fertility in animal or human studies. Unlikely to affect reproductive function due to low systemic bioavailability. |