Qvar Redihaler
Qvar Redihaler
Generic Name
Qvar Redihaler
Mechanism
- Glucocorticoid receptor binding: Fluticasone propionate gains intracellular access, binds to cytosolic glucocorticoid receptors, complexes, and translocates to the nucleus.
- Transcriptional regulation: The complex recruits co‑activators or recruits co‑repressors, leading to:
- ↓ synthesis of pro‑inflammatory cytokines (IL‑5, IL‑13, TNF‑α)
- ↓ recruitment of eosinophils and neutrophils
- ↑ anti‑inflammatory proteins (lipocortin‑1).
- Reduced airway hyper‑responsiveness: Decreases airway smooth‑muscle hypertrophy and submucosal edema.
- Local airway immunosuppression: Limits episodic bronchoconstriction and inflammation.
Pharmacokinetics
| Parameter | Details |
| Administration | Dry‑powder inhalation via Redihaler puffer |
| Bioavailability | ~30 % systemic absorption; majority remains in the lungs |
| Distribution | Widely distributed in lung tissue; limited systemic distribution |
| Metabolism | Hepatic CYP3A4 → inactive metabolites |
| Elimination | Renal excretion (~70 %), biliary route |
| Half‑life | 7 h (lung residue) / 1 h (systemic) |
| CYP interactions | Strong inhibition of CYP3A4 (e.g., ketoconazole) ↑ systemic exposure |
Indications
- Persistent asthma (mild‑moderate to severe) requiring daily controller therapy.
- Used as monotherapy for stable asthma or as add‑on to short‑acting β₂‑agonists (SABA).
- Can be tapered when remission is achieved and symptoms are controlled.
Contraindications
- Contraindications
- Hypersensitivity to fluticasone propionate, propionate esters, or any component.
- Active systemic fungal infections (e.g., candidiasis) that may worsen.
- Warnings
- Growth suppression in children; monitor annually.
- Adrenal suppression with high cumulative doses or concurrent systemic steroids.
- Local candidiasis—use oral rinse after each use.
- Exacerbation of pneumonia in immunocompromised patients.
- Precautions
- Use with caution in patients on potent CYP3A4 inhibitors or inducers.
- Avoid in patients with a history of thymic malignancies or interstitial lung disease.
Dosing
| Age Group | Typical Dose (Adults/Adolescents) | Children (≥6 yrs) |
| Standard | 1 puff (50 µg fluticasone) *twice daily* (morning + evening) | 1 puff BID (50 µg) |
| Titration | Increase to 2 puffs BID (100 µg/day) if control inadequate. | Up to 2 puffs BID; monitor growth. |
| Max | 2 puffs BID (100 µg total/day) | 2 puffs BID |
*Administration notes:*
• Hold inhalation for 10 s after exhaling; breathe in slowly and deeply.
• Use a spacer or valved holding chamber if coordination is difficult.
• Rinse mouth post‑dose to reduce fungal risk.
Adverse Effects
| Common (Local) | Serious (Systemic) |
| Oral candidiasis (thrush) | Growth suppression in children |
| Throat irritation / dysphonia | Adrenal insufficiency |
| Upper airway cough | Osteoporosis with long‑term high dose |
| Dry mouth | Cataracts / glaucoma (rare, systemic exposure) |
| Nasal irritation | Hypersensitivity reactions |
Serious events are rare when used at recommended doses; monitor especially in pediatrics and if high cumulative exposure.
Monitoring
- Pulmonary function (FEV₁, peak expiratory flow) → baseline and every 3–6 months.
- Growth velocity in children → annually.
- Signs of systemic absorption: blood pressure, serum cortisol (if clinically indicated).
- Oral candidiasis: Inspect oral cavity at each visit.
- Adherence & technique: Review inhaler technique at each encounter.
Clinical Pearls
- Pre‑dose rinse: Rinsing the mouth or gargling with salt water after each puff dramatically reduces oral candidiasis—especially in school‑going kids.
- Spacer synergy: A valved holding chamber improves deposition in the lower airways and reduces oral deposition.
- Dose escalation in adolescence: Start at 50 µg BID; if symptoms persist, add a second puff only after failure of bronchodilators and rescue therapy for at least 1 month.
- Avoid abrupt withdrawal: Taper slowly when discontinuing after long‑term use to prevent adrenal crisis.
- Use as a proof‑of‑concept: For patients who cannot tolerate alternate inhaled steroids, Qvar Redihaler can serve as a high‑potency, low‑dose alternative—mono‑therapy up to 200 µg/day.
- Drug–drug interactions: Screen for potent CYP3A4 inhibitors (ketoconazole, ritonavir). If concomitant therapy is mandatory, consider reducing Qvar dose or switching to another controller.
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• Key take‑away: *Qvar Redihaler* delivers an effective, low‑systemic‑dose corticosteroid for stable asthma, but requires diligent inhaler technique, routine monitoring of growth (in children) and careful attention to potential local fungal infections.