Usage
Fluticasone propionate is a synthetic corticosteroid prescribed for the management of various inflammatory conditions, primarily affecting the respiratory system and skin. It is used to treat allergic rhinitis (hay fever), non-allergic rhinitis, nasal polyps, asthma, and certain skin conditions like eczema and psoriasis.
Pharmacological Classification: Corticosteroid, Anti-inflammatory, Immunosuppressant.
Mechanism of Action: Fluticasone propionate exerts its anti-inflammatory and immunosuppressive effects by binding to glucocorticoid receptors in the cytoplasm of target cells. This complex then translocates to the nucleus, modulating gene expression. It decreases the production of inflammatory mediators like cytokines, prostaglandins, and leukotrienes, reducing inflammation, swelling, and mucus production.
Alternate Names
Fluticasone propionate is also known as Fluticasone 21-propionate. Brand names include Flonase, Veramyst, Flovent, Cutivate, and Flixonase.
How It Works
Pharmacodynamics: Fluticasone propionate suppresses the inflammatory cascade by decreasing vascular permeability, reducing inflammatory cell migration, and inhibiting the release of inflammatory mediators. It also modulates the activity of the immune system by suppressing T-cell function and reducing antibody production.
Pharmacokinetics:
- Absorption: Fluticasone propionate, when administered intranasally, undergoes minimal systemic absorption, primarily due to extensive first-pass metabolism in the liver and gut. Inhalation results in higher systemic bioavailability. Topical application also results in minimal systemic absorption.
- Metabolism: Fluticasone propionate is primarily metabolized in the liver by the cytochrome P450 3A4 (CYP3A4) enzyme system to inactive metabolites.
- Elimination: It is primarily excreted in the feces, with a small amount excreted in the urine.
Mode of Action: Fluticasone propionate binds to glucocorticoid receptors in the cytoplasm. The drug-receptor complex translocates to the nucleus, where it interacts with DNA, modulating gene expression. This leads to decreased production of inflammatory mediators and suppression of immune cell activity.
Receptor Binding: Glucocorticoid receptors.
Elimination Pathways: Primarily hepatic metabolism by CYP3A4 enzymes, followed by fecal excretion.
Dosage
Standard Dosage
Adults (Nasal Spray):
- Allergic and Non-allergic Rhinitis: Initially, two sprays (50 mcg/spray) in each nostril once daily (200 mcg total daily dose). May reduce to one spray per nostril once daily for maintenance. Alternatively, one spray per nostril twice daily can be considered. The maximum dose is 200 mcg/day.
Children (Nasal Spray):
- Ages 4-11: Initially, one spray (50 mcg/spray) in each nostril once daily (100 mcg total daily dose). May increase to two sprays per nostril once daily if necessary. Maximum dose is 200 mcg/day.
- Under 4 years: Use is generally not recommended.
Adults (Inhalation):
- Asthma: Dosage varies depending on the specific product and disease severity. Please refer to the individual product’s prescribing information.
Children (Inhalation):
- Asthma: Dosage varies depending on the specific product and disease severity. Please refer to the individual product’s prescribing information.
Special Cases:
- Elderly Patients: Start at the lower end of the dosing range due to potential for decreased hepatic, renal, or cardiac function.
- Patients with Renal Impairment: No specific dosage adjustment is typically required.
- Patients with Hepatic Dysfunction: Use with caution as impaired metabolism may lead to drug accumulation. Close monitoring is recommended.
- Patients with Comorbid Conditions: Consider potential drug interactions and adjust accordingly.
Clinical Use Cases
Fluticasone propionate is not indicated for the use cases mentioned below. Its primary uses involve managing asthma and allergic rhinitis, typically administered via inhalation or nasal spray. These clinical use cases involve intravenous medications which are different from fluticasone propionate.
Dosage Adjustments
Dosage adjustments may be necessary based on patient response, disease severity, and the presence of hepatic dysfunction. Close monitoring for adverse effects is essential, especially with prolonged use or higher doses.
Side Effects
Common Side Effects:
- Headache
- Nasal irritation (burning, stinging, dryness)
- Sore throat
- Nosebleeds
- Sneezing
- Cough
Rare but Serious Side Effects:
- Allergic reactions (rash, itching, swelling)
- Nasal septal perforation
- Adrenal suppression (with prolonged or high-dose use)
- Glaucoma, cataracts (with prolonged use of nasal spray)
- Growth retardation in children (with prolonged use of inhaled formulations)
Long-Term Effects:
- Osteoporosis (with prolonged use of systemic corticosteroids)
- Increased risk of infections (with prolonged or high-dose use)
Adverse Drug Reactions (ADR):
- Angioedema
- Bronchospasm
- Anaphylaxis (rare)
Contraindications
- Hypersensitivity to fluticasone propionate or any of its components.
- Active systemic fungal infections.
- Untreated active or quiescent tuberculosis.
- Recent nasal surgery or trauma.
Drug Interactions
- CYP3A4 Inhibitors: Ritonavir, ketoconazole, itraconazole can increase plasma concentrations of fluticasone propionate, increasing the risk of systemic side effects.
- Other corticosteroids: Concurrent use may increase the risk of adverse effects.
Pregnancy and Breastfeeding
- Pregnancy: Fluticasone propionate should be used during pregnancy only if the potential benefit outweighs the potential risk to the fetus. There are limited data on its use in pregnant women.
- Breastfeeding: While limited data suggest that the amount of drug excreted in breast milk is low, caution is advised when administering to breastfeeding women.
Drug Profile Summary
- Mechanism of Action: Binds to glucocorticoid receptors, modulating gene expression, and reducing inflammation.
- Side Effects: Nasal irritation, headache, sore throat, nosebleeds, allergic reactions.
- Contraindications: Hypersensitivity, active systemic fungal infections, untreated tuberculosis.
- Drug Interactions: CYP3A4 inhibitors (ritonavir, ketoconazole), other corticosteroids.
- Pregnancy & Breastfeeding: Use with caution if benefits outweigh risks.
- Dosage: Varies based on formulation and indication. Consult prescribing information.
- Monitoring Parameters: Growth in children (inhaled formulations), intraocular pressure (nasal spray), cortisol levels (long-term or high-dose use).
Popular Combinations
Fluticasone propionate is often combined with salmeterol (a long-acting beta-agonist) for the treatment of asthma. This combination provides both anti-inflammatory and bronchodilatory effects.
Precautions
- Monitor for local and systemic side effects.
- Assess asthma control regularly.
- Caution in patients with hepatic impairment.
- Advise patients to rinse their mouths after using inhaled formulations to reduce the risk of oral candidiasis.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Fluticasone Propionate nasal spray?
A: For adults, the recommended starting dose is two sprays in each nostril once daily (200 mcg total). It can be reduced to one spray per nostril once daily for maintenance. For children aged 4-11 years, the starting dose is one spray in each nostril once daily (100 mcg total).
Q2: What are the common side effects of Fluticasone Propionate nasal spray?
A: Common side effects include nasal irritation, headache, sore throat, nosebleeds, sneezing, and cough.
Q3: Is Fluticasone Propionate safe during pregnancy?
A: Fluticasone propionate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult with an obstetrician for individualized advice.
Q4: Can I use Fluticasone Propionate while breastfeeding?
A: Caution is advised while breastfeeding. Limited data suggest the amount of drug excreted in breast milk is low. Discuss with a pediatrician or healthcare professional.
Q5: How does Fluticasone Propionate work for allergies?
A: It reduces inflammation in the nasal passages by suppressing the release of inflammatory mediators, thus relieving allergy symptoms.
Q6: What should I do if I miss a dose of Fluticasone Propionate?
A: Take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and continue with your regular dosing schedule. Do not double the dose to catch up.
Q7: How long does it take for Fluticasone Propionate to work?
A: It may take several days to experience full benefits. Some patients may notice improvement within a few days, while others may require up to two weeks.
Q8: Can Fluticasone Propionate interact with other medications?
A: Yes, it can interact with certain medications, particularly CYP3A4 inhibitors (e.g., ritonavir, ketoconazole), increasing the risk of systemic side effects. Inform your doctor about all medications you are currently taking.
Q9: Are there any long-term side effects of Fluticasone Propionate nasal spray?
A: While rare, long-term use of the nasal spray has been associated with glaucoma, cataracts, and nasal septal perforation. Regular monitoring is essential.
