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. |
| Molecular Weight | 521 |
| Action Class | Inhaled Corticosteroid |
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 | Inhaled corticosteroids like beclomethasone are preferred for asthma in pregnancy. No teratogenicity in animal studies; human data minimal. Use if benefit > risk. |
| 2nd trimester | Safe for use; no known fetal harm. Maintain asthma control to avoid maternal hypoxia. |
| 3rd trimester | Safe; continued use recommended for asthma control. No adverse fetal effects reported. |
Clinical note
Comprehensive clinical and safety monograph for QVAR REDIHALER (QVAR REDIHALER).
| Placental transfer | Minimal; inhaled corticosteroids have low bioavailability. Beclomethasone dipropionate is extensively metabolized in liver; active metabolite beclomethasone-17-monopropionate may cross placenta in small amounts. |
| Breastfeeding | Beclomethasone dipropionate is inhaled; systemic absorption minimal. Excretion into breast milk is likely negligible. Considered compatible with breastfeeding. |
■ FDA Black Box Warning
None
| Common Effects | Headache, Pharyngitis, Sinusitis, Cough, Hoarseness (dysphonia), Throat irritation, Upper respiratory tract infection |
| Serious Effects | Adrenal insufficiency (with prolonged use or high doses), Oropharyngeal candidiasis, Paradoxical bronchospasm, Increased risk of pneumonia in patients with COPD, Growth suppression in children, Osteoporosis with long-term use, Cataracts and glaucoma |
Hypersensitivity to beclomethasone dipropionate or any excipient in QVAR RediHalerUntreated systemic infections (e.g., tuberculosis, fungal, bacterial, viral)
| 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 |
Loading safety data…
| Lactation Rating | L2: Limited data - probably compatible |
| 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. |
| 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. |
| Food/Dietary |
| No known clinically significant food interactions. Grapefruit juice does not affect beclomethasone metabolism. However, if oral candidiasis develops, avoid sugary foods which may exacerbate fungal overgrowth. |
| Clinical Pearls | QVAR REDIHALER (beclomethasone dipropionate HFA) is a breath-actuated inhaled corticosteroid (ICS) for maintenance asthma therapy. Unlike traditional pMDIs, it does not require hand-breath coordination; the device actuates automatically upon inspiration. Advise patients to rinse mouth with water after each use to reduce oropharyngeal candidiasis and dysphonia. Not for acute bronchospasm; use a rescue inhaler (SABA) for acute symptoms. Titrate to lowest effective dose; high doses may cause adrenal suppression. Monitor for increased asthma symptoms, which may indicate need for additional therapy. |
| Patient Advice | Use exactly as prescribed; do not use for sudden breathing problems. · Rinse mouth with water and spit after each use to prevent thrush. · Do not wash or soak the inhaler; keep it dry. · Shake the inhaler well before each use. · Breathe in deeply and forcefully through the mouthpiece for optimal drug delivery. · Keep track of the dose counter; replace inhaler when it reaches zero. · Avoid exposure to the propellant if allergic; seek medical help if severe reaction occurs. |