Usage
Fluticasone furoate is prescribed for the treatment of allergic rhinitis (both seasonal and perennial) and asthma. It belongs to the pharmacological classification of corticosteroids, specifically glucocorticoids. It works by reducing inflammation in the nasal passages and airways.
Alternate Names
Fluticasone furoate is sometimes referred to simply as fluticasone. Brand names for fluticasone furoate include Avamys, Veramyst, and Furoate. Brand names for formulations containing fluticasone furoate in combination with other drugs include Breo Ellipta (with vilanterol) and Relvar Ellipta (with vilanterol).
How It Works
Pharmacodynamics: Fluticasone furoate exerts its anti-inflammatory action by binding to glucocorticoid receptors in the cytoplasm of target cells. This complex then translocates to the nucleus, where it modulates the transcription of various genes involved in the inflammatory response. Specifically, it inhibits the production of inflammatory mediators like cytokines, chemokines, and prostaglandins. It also inhibits the recruitment of inflammatory cells like eosinophils and neutrophils to the site of inflammation.
Pharmacokinetics: Following intranasal administration, fluticasone furoate exhibits minimal systemic absorption due to extensive first-pass metabolism in the liver and gut wall, primarily by the cytochrome P450 enzyme CYP3A4. It is typically not quantifiable in plasma after intranasal administration at recommended doses. When administered via inhalation, absorption is higher, resulting in measurable plasma concentrations. The elimination half-life is approximately 15 hours after intravenous administration. Excretion is mainly through feces, with a small amount excreted in urine.
Dosage
Standard Dosage
Adults:
Allergic Rhinitis: The recommended starting dose is two sprays (27.5 mcg/spray) in each nostril once daily (total daily dose, 110 mcg). After achieving symptom control, the dose can be reduced to one spray in each nostril once daily (55 mcg).
Asthma (inhalation): For adults and children 12 years and older: The recommended starting dose is 100 mcg once daily using a metered-dose inhaler. It can be increased to 200 mcg/day if needed. The maximum dose is 200 mcg once daily.
Children:
Allergic Rhinitis: For children aged 2 to 11 years, the recommended starting dose is one spray (27.5 mcg/spray) in each nostril once daily (total daily dose, 55 mcg). It can be increased to two sprays per nostril daily (110 mcg) if needed. For children under 2 years of age, safety and efficacy have not been established.
Asthma (inhalation): For children aged 5-11 years: 50 mcg inhaled orally every day. For children under 5, safety and efficacy not established.
Special Cases:
- Elderly Patients: No dosage adjustment is generally necessary.
- Patients with Renal Impairment: No dosage adjustment is necessary.
- Patients with Hepatic Dysfunction: No dosage adjustment is recommended for mild to moderate impairment. However, close monitoring is advised in patients with severe hepatic dysfunction.
- Patients with Comorbid Conditions: Consider underlying conditions, especially concurrent use of other corticosteroids.
Clinical Use Cases
Fluticasone furoate is not indicated for intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. Its use is primarily focused on long-term management of allergic rhinitis and asthma.
Dosage Adjustments
Dose adjustments should be individualized based on the patient’s response, disease severity, and the presence of any comorbid conditions. Always titrate to the lowest effective dose.
Side Effects
Common Side Effects:
- Headache
- Epistaxis (nosebleed)
- Nasal irritation (burning, stinging, dryness)
- Sore throat
- Cough
- Upper respiratory tract infection
Rare but Serious Side Effects:
- Allergic reactions (anaphylaxis, angioedema, urticaria)
- Nasal septal perforation
- Adrenal suppression (with prolonged use of high doses)
- Growth retardation in children (with prolonged use of high doses)
- Glaucoma and cataracts (with prolonged use)
Long-Term Effects:
- Osteoporosis (with prolonged use of high doses)
- Increased risk of infections (with prolonged use of high doses)
Adverse Drug Reactions (ADR):
Any signs of hypersensitivity reactions or severe nasal complications should prompt immediate discontinuation of the drug and appropriate medical intervention.
Contraindications
- Hypersensitivity to fluticasone furoate or any of its components.
- Active, untreated localized nasal infections (e.g., herpes simplex).
Drug Interactions
- Strong CYP3A4 Inhibitors: (e.g., ritonavir, ketoconazole) can increase systemic exposure to fluticasone furoate and may increase the risk of adverse effects. Concurrent use should generally be avoided or closely monitored.
Pregnancy and Breastfeeding
- Pregnancy: Fluticasone furoate is classified as Pregnancy Category C. Use only if the potential benefit justifies the potential risk to the fetus. Nasal administration results in minimal systemic exposure.
- Breastfeeding: While the amount of fluticasone furoate excreted in breast milk is unknown, it is likely small. Use with caution and monitor the infant for potential side effects.
Drug Profile Summary
- Mechanism of Action: Binds to glucocorticoid receptors, modulating gene transcription and reducing inflammation.
- Side Effects: Headache, epistaxis, nasal irritation, sore throat, cough. Rarely: allergic reactions, nasal septal perforation, adrenal suppression.
- Contraindications: Hypersensitivity, active untreated local nasal infection.
- Drug Interactions: Strong CYP3A4 inhibitors.
- Pregnancy & Breastfeeding: Use with caution; potential benefits must outweigh risks.
- Dosage: Rhinitis: Adults: 110 mcg/day initially, reduced to 55 mcg/day; Children (2-11 years): 55 mcg/day initially, up to 110 mcg/day. Asthma: Adults and Children ≥12 years: 100-200 mcg/day; Children 5-11 years: 50 mcg/day.
- Monitoring Parameters: Growth in children during long-term therapy, intraocular pressure, signs of adrenal suppression.
Popular Combinations
Fluticasone furoate is often combined with vilanterol (a long-acting beta2-adrenergic agonist) for the treatment of asthma and COPD. This combination provides synergistic bronchodilatory and anti-inflammatory effects.
Precautions
- General Precautions: Assess for pre-existing nasal conditions, infections, and concurrent corticosteroid use.
- Specific Populations: Monitor children for growth suppression. Evaluate patients on long-term therapy for adrenal suppression, glaucoma, and cataracts.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Fluticasone Furoate in allergic rhinitis?
A: Adults: 110 mcg/day initially, reduced to 55 mcg/day. Children (2-11 years): 55 mcg/day initially, up to 110 mcg/day.
Q2: What is the recommended dosage for Fluticasone Furoate in asthma?
A: Adults and children ≥ 12 years: 100 mcg/day inhaled, can be increased to 200 mcg/day if necessary. Children 5-11 years: 50 mcg/day.
Q3: What are the common side effects of Fluticasone Furoate?
A: Headache, epistaxis, nasal irritation, sore throat, cough.
Q4: What are the serious side effects of Fluticasone Furoate?
A: Allergic reactions, nasal septal perforation, adrenal suppression (with prolonged use of high doses).
Q5: Can Fluticasone Furoate be used during pregnancy?
A: It should be used only if the potential benefit justifies the potential risk to the fetus. Discuss with a specialist.
Q6: Can Fluticasone Furoate be used during breastfeeding?
A: Use with caution and monitor the infant for potential side effects. Discuss with a specialist.
Q7: What are the contraindications for Fluticasone Furoate?
A: Hypersensitivity to the drug or any of its components, active untreated localized nasal infections.
Q8: What are the important drug interactions with Fluticasone Furoate?
A: Strong CYP3A4 inhibitors (e.g., ritonavir, ketoconazole) may increase systemic exposure.
Q9: How does Fluticasone Furoate work?
A: It is a corticosteroid that binds to glucocorticoid receptors, reducing inflammation in the airways and nasal passages.
Q10: What should be monitored in patients taking Fluticasone Furoate long-term?
A: Growth in children, intraocular pressure, and signs of adrenal suppression.
