Fluticasone Propionate

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• Nasal Burning or Stinging: A transient sensation immediately after using the nasal spray.
• Nausea and Vomiting: Occasionally reported with systemic absorption or post-nasal drip of the medication.
• Dizziness: Some patients may feel lightheaded shortly after administration.
• Upper Respiratory Tract Infection: Increased susceptibility to minor viral colds or sinus infections.

• Nasal Septal Perforation: In rare cases, long-term use of nasal steroids can lead to a small hole in the wall between the nostrils. This is often preceded by crusting and severe dryness.
• Glaucoma and Cataracts: Increased intraocular pressure has been documented with long-term, high-dose use of both inhaled and nasal corticosteroids.
• Growth Retardation: While rare at standard doses, prolonged use in children may slightly slow the rate of growth. Healthcare providers monitor height regularly in pediatric patients.

> Warning: Stop taking Fluticasone and call your doctor immediately if you experience any of these serious reactions:

• Anaphylaxis or Severe Allergic Reactions: Symptoms include hives, swelling of the face, lips, or tongue, and difficulty breathing or swallowing.
• Candida Albicans (Oral Thrush): White patches in the mouth or throat, which indicate a fungal infection. This is a risk if the mouth is not rinsed after inhalation.
• Adrenal Suppression: Signs include extreme fatigue, muscle weakness, weight loss, and low blood pressure. This occurs when the body stops producing its own cortisol.
• Immunosuppression: Increased vulnerability to severe infections. If you are exposed to chickenpox or measles while on Fluticasone, contact your doctor immediately.
• Vision Changes: Blurred vision, eye pain, or seeing 'halos' around lights.

Prolonged use of Fluticasone, especially at higher-than-recommended doses, can lead to systemic steroid effects. These include a reduction in bone mineral density (increasing the risk of osteoporosis), thinning of the skin (atrophy), and easy bruising. In rare cases, patients may develop 'Cushingoid' features, such as a rounded face (moon face) and a fatty hump between the shoulders. Regular monitoring by a healthcare provider is essential for anyone using Fluticasone for more than several months.

No FDA black box warnings currently exist for Fluticasone propionate as a monotherapy. However, combination products containing Fluticasone and long-acting beta-agonists (LABAs) previously carried warnings regarding asthma-related death risks; however, the FDA removed these specific warnings in 2017 following large-scale safety trials that demonstrated no significant increase in serious asthma-related events when LABAs are used in combination with an inhaled corticosteroid like Fluticasone.

Report any unusual symptoms to your healthcare provider. You may also report side effects to the FDA at 1-800-FDA-1088.

Healthcare providers may require the following monitoring for patients on long-term Fluticasone therapy:

• Growth Monitoring: For pediatric patients, height should be tracked at every visit to ensure the drug is not impacting growth velocity.
• Bone Density: For patients at high risk for osteoporosis, periodic bone mineral density (BMD) scans may be recommended.
• Ocular Exams: Annual or bi-annual eye exams to check for increased intraocular pressure.
• HPA Axis Testing: In rare cases where high doses are used, a cosyntropin stimulation test may be performed to check adrenal function.

Fluticasone generally does not cause sedation or cognitive impairment. It is considered safe to drive or operate machinery while using this medication, provided you do not experience rare side effects like severe dizziness or blurred vision.

There are no known direct interactions between Fluticasone and alcohol. However, alcohol can sometimes trigger asthma or allergy symptoms in certain individuals, so moderation is advised.

Do not stop using Fluticasone abruptly, especially if you have been using it at high doses. While 'withdrawal' is less common than with oral steroids, a sudden stop can lead to a return of severe inflammatory symptoms. Your doctor will provide a tapering schedule if you need to stop the medication.

> Important: Discuss all your medical conditions, especially any history of tuberculosis, eye problems, or recent infections, with your healthcare provider before starting Fluticasone.

• Desmopressin: Corticosteroids can increase the water-retaining effect of desmopressin, potentially leading to low sodium levels (hyponatremia).
• Diuretics (Water Pills): Some diuretics can cause potassium loss; when combined with high doses of steroids, the risk of hypokalemia (low potassium) may increase, though this is rare with localized Fluticasone.

• Grapefruit Juice: Grapefruit is a known inhibitor of the CYP3A4 enzyme in the gut and liver. While the impact on inhaled Fluticasone is likely minimal, consuming large amounts of grapefruit juice could theoretically increase the systemic absorption of the drug.
• Dairy: Some dry powder inhalers (DPIs) contain lactose. While the amount is tiny, patients with severe milk protein allergies (not just lactose intolerance) should avoid these specific formulations and use MDIs instead.

• St. John's Wort: This herbal supplement is an inducer of CYP3A4. It may speed up the metabolism of Fluticasone, potentially reducing its effectiveness in controlling asthma or allergies.
• Echinacea: Some believe Echinacea may interfere with the immunosuppressive effects of corticosteroids, though clinical evidence for this interaction with Fluticasone is limited.

Fluticasone generally does not interfere with standard blood or urine tests. However, because it can suppress the HPA axis, it may interfere with tests designed to measure adrenal function, such as the ACTH stimulation test or urinary free cortisol tests.

Management Strategy

To manage these interactions, healthcare providers typically:

1. 1Review all current medications before prescribing Fluticasone.
2. 2Use the lowest effective dose of Fluticasone if a CYP3A4 inhibitor is necessary.
3. 3Monitor for 'red flag' symptoms like rapid weight gain, facial swelling, or extreme fatigue.

> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter allergy or cold medicines.

• Active Tuberculosis (TB): Because steroids suppress the immune response, they can allow TB to worsen or reactivate.
• Ocular Herpes Simplex: There is a risk of corneal perforation if steroids are used during an active infection.
• Recent Nasal Surgery or Trauma: Until the nose has fully healed, the use of nasal steroids can delay wound healing and increase the risk of septal perforation.
• Severe Hepatic Impairment: Patients with liver failure may accumulate higher levels of the drug, requiring very close monitoring for systemic side effects.

Patients who are allergic to other corticosteroids (such as budesonide, triamcinolone, or mometasone) may occasionally experience cross-sensitivity with Fluticasone. If you have had a skin rash or breathing difficulty with any other steroid, inform your doctor before starting Fluticasone.

> Important: Your healthcare provider will evaluate your complete medical history, including any past infections or surgeries, before prescribing Fluticasone.

Fluticasone is approved for use in children as young as 4 years old for both asthma and allergic rhinitis.

• Growth Effects: A primary concern in pediatrics is the potential for corticosteroids to slow growth. Clinical trials have shown that children using inhaled Fluticasone may experience a small reduction in growth velocity (approximately 1 cm per year). This effect is usually most pronounced in the first year of treatment and may not affect final adult height.
• Dosing: Pediatric patients should always use the lowest effective dose to minimize these risks.

In older adults, Fluticasone is generally safe and effective. However, the following concerns apply:

• Bone Health: Elderly patients are at higher risk for osteoporosis. Since long-term steroids can reduce bone density, calcium and Vitamin D supplementation may be recommended.
• Thinning Skin: Older patients using topical Fluticasone may experience skin tearing or bruising more easily.
• Polypharmacy: Older adults are more likely to be on multiple medications (like CYP3A4 inhibitors for heart disease), increasing the risk of drug interactions.

No dosage adjustments are needed for patients with kidney disease. The drug is not significantly cleared by the kidneys, and dialysis does not affect its concentration.

Since Fluticasone is metabolized by the liver, patients with Child-Pugh Class B or C hepatic impairment should be monitored for signs of hypercorticism (excessive steroid levels). The drug's half-life may be prolonged in these patients.

> Important: Special populations require individualized medical assessment to ensure the safest possible treatment plan.

Fluticasone has a high affinity for the glucocorticoid receptor—approximately 18 times greater than dexamethasone. The onset of action for the nasal spray is typically 12 hours, with peak effects seen after several days. For asthma, improvement in lung function may be seen within 24 hours, but maximum benefit usually requires 1 to 2 weeks of continuous therapy.

| Parameter | Value |

|---|---|

| Bioavailability | <2% (Nasal), 10-20% (Inhalation) |

| Protein Binding | 99% |

| Half-life | 7.8 to 10 hours |

| Tmax | 0.5 to 1 hour (Inhalation) |

| Metabolism | Hepatic (CYP3A4) |

| Excretion | Fecal (>95%), Renal (<5%) |

• Molecular Formula: C25H27F3O4S
• Molecular Weight: 500.5 g/mol
• Solubility: Practically insoluble in water; freely soluble in dimethyl sulfoxide (DMSO).
• Structure: A trifluorinated corticosteroid with a propionate ester group at the 17-alpha position, which enhances its lipophilicity and receptor binding.

Fluticasone is classified as a synthetic corticosteroid and a glucocorticoid receptor agonist. It is part of the 'Inhaled Corticosteroid' (ICS) class for respiratory health and 'Topical Corticosteroid' (Group II or III) for dermatology.