Fluticasone Propionate | Prescribing Information

September 22, 2023 Prescribing Information 103 Views

Fluticasone propionate is a steroid medication. When inhaled it is used for the long-term management of asthma and COPD. In the nose, it is used for hay fever and nasal polyps. It can also be used for mouth ulcers. It works by decreasing inflammation.

Fluticasone propionate was patented in 1980 and approved for medical use in 1990. It is available as a generic medication. In 2020, fluticasone was the 23^rd most commonly prescribed medication in the United States, with more than 24 million prescriptions.

Indications

Fluticasone Propionate HFA is an inhaled corticosteroid (ICS) indicated for the maintenance treatment of asthma as prophylactic therapy in patients aged 4 years and older.

Fluticasone Propionate Nasal Spray is indicated for

The prophylaxis and treatment of seasonal allergic rhinitis including hay fever and perennial rhinitis.
It has potent anti-inflammatory activity on the nasal mucosa without detectable systemic activity.

Fluticasone Propionate Nebuliser Suspension is indicated for-

Adults and adolescents over 16 years of age: Prophylactic management in severe asthma (patients requiring high dose inhaled or oral corticosteroid therapy).

Children and adolescents from 4 to 16 years of age: Treatment of mild to moderate acute exacerbations of asthma.

Fluticasone Propionate (Topical) is indicated for the relief of inflammatory and pruritic manifestations of corticosteroid-responsive eczema/dermatitis.

Pharmacology

Fluticasone propionate is a synthetic trifluorinated corticosteroid with anti-inflammatory activity. Fluticasone propionate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor that is 18 times that of dexamethasone, almost twice that of beclomethasone-17-mono propionate (BMP), the active metabolite of beclomethasone dipropionate, and over 3 times that of budesonide. Data from the McKenzie vasoconstrictor assay in man are consistent with these results. The clinical significance of these findings is unknown.

Inflammation is an important component in the pathogenesis of asthma. Corticosteroids have been shown to have a wide range of actions on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) involved in inflammation. These anti-inflammatory actions of corticosteroids contribute to their efficacy in asthma.

Though effective for the treatment of asthma, corticosteroids do not affect asthma symptoms immediately. Individual patients will experience a variable time to onset and degree of symptom relief. Maximum benefit may not be achieved for 1 to 2 weeks or longer after starting treatment. When corticosteroids are discontinued, asthma stability may persist for several days or longer.

Trials in subjects with asthma have shown a favorable ratio between topical anti-inflammatory activity and systemic corticosteroid effects with recommended doses of orally inhaled fluticasone propionate. This is explained by a combination of a relatively high local anti-inflammatory effect, negligible oral systemic bioavailability (<1%), and the minimal pharmacological activity of the only metabolite detected in man.

Following topical administration into the nasal mucosa, Fluticasone propionate produces anti-inflammatory and vasoconstrictor effects. The exact mechanism of these actions remains unknown but may involve a reduction in the following: number of mediator cells (basophil, leukocytes, and mast cells) at the epithelial level, number of eosinophils, the sensitivity of sensory nerves to mechanical stimuli, secretory response to cholinergic receptor stimulation, and fibroblast activity. Other mechanisms may involve – inhibition of capillary dilation and permeability, stabilization of lysosomal membranes, and subsequent prevention of release of proteolytic enzymes.

Dosage

Inhaler-

Adult and adolescent patients aged 12 Years and older: The starting dosage is based on previous asthma therapy and asthma severity, including consideration of patients’ current control of asthma symptoms and risk of future exacerbation. The recommended starting dosage for patients aged 12 years and older who are not on an inhaled corticosteroid (ICS) is 88 mcg twice daily, approximately 12 hours apart. For other patients, and for patients who do not respond adequately to the starting dosage after 2 weeks of therapy, higher dosages may provide additional asthma control. The maximum recommended dosage for patients aged 12 years and older is 880 mcg twice daily.

Pediatric patients aged 4 to 11 years: The recommended dosage for patients aged 4 to 11 years is 88 mcg twice daily, approximately 12 hours apart.

Nasal Spray-

For adults & children over 12 years: 2 sprays in each nostril once a day preferably in the morning. In some cases 2 sprays into each nostril twice daily, not exceeding 4 sprays.

Children under 12 years (4-11 years): 1 spray in each nostril once a day. The maximum total daily dosage should not exceed 4 sprays. For perennial rhinitis in children, there is insufficient clinical data to recommend its use.

Children below 4 years: The safety and effectiveness of Fluticasone Propionate nasal spray in children below 4 years of age have not been established.

Patients should use Fluticasone Propionate Nasal Spray at regular intervals as directed since its effectiveness depends on its regular use. Or as directed by the physician.

Nebuliser Suspension-

Adults and adolescents over 16 years (prophylactic management in severe asthma): 0.5-2 mg twice daily. The recommended initial dose is 2 mg twice daily. The dosage should then be adjusted until control is achieved or reduced to the minimum effective dose according to the individual response.

Children and adolescents 4 to 16 years of age (treatment of acute exacerbations of asthma): 1 mg twice daily.

Topical-

Cream: Apply a thin layer of Fluticasone propionate cream to the affected skin areas once daily.
Ointment: Apply a thin layer of Fluticasone propionate Ointment to the affected skin areas twice daily.

Administration

Using an Inhaler seems simple, but most patients do not know how to use it correctly. If the Inhaler is used in the wrong way, less medicine can reach the lungs. Correct and regular use of the Inhaler will prevent or lessen the severity of asthma attacks.

Following simple steps can help to use Inhaler effectively (According to “National Asthma Guidelines for Medical Practitioners” published by Asthma Association):

Take off the cap.
Shake the inhaler (at least six times) vigorously before each use.
If the inhaler is new or has not been used for a week or more, shake it well and release one puff into the air to ensure it works.
Breathe out as completely as comfortably possible & hold the inhaler upright.
Place the actuator into the mouth between the teeth and close the lips around the mouthpiece.
While breathing deeply and slowly through the mouth, press down firmly and fully on the canister to release medicine.
Remove the inhaler from the mouth. Continue holding your breath for at least 10 seconds or as long as it is comfortable.
If the doctor has prescribed more than one inhalation per treatment, wait 1 minute between puffs (inhalations). Shake the inhaler well and repeat steps 4 to 7.
After use, replace the cap on the mouthpiece. After each treatment, rinse the mouth with water.
Check your technique in front of a mirror from time to time, if you see a white mist during the inhalation, you may not have closed your lips properly around the mouthpiece, or you may not be breathing in as you press the can. This indicates a failure of the technique. If this happens, repeat the procedure from step 4 carefully.

How to use the Nasal Spray-

Shake the bottle gently and remove the dust cover.
Hold the spray with your forefinger and middle finger on either side of the nozzle and your thumb underneath the bottle. Press down until a fine spray appears. If using it for the first time or if you have not used it for a week or more, press the nasal applicator several times until fine moisture comes out from the container.
Gently blow the nose to clear the nostrils.
Close one nostril and carefully insert the nasal applicator into the open nostril. Tilt your head forward slightly and keep the spray upright. Breathe in through your nose and while breathing in, press the white collar of the nasal applicator firmly down once to release a spray.
Breathe out through your mouth.
Repeat the above steps in the same/ other nostril for consecutive doses.

Instructions for Cleaning Nasal Spray: The nasal spray should be cleaned at least once a week. The procedures are as follows-

Remove the dust cover.
Gently pull off the nasal applicator.
Wash the applicator and dust cover in warm water.
Shake off the excess water and leave to dry in a normal place. Avoid applying additional heat.
Gently push the applicator back on the top of the bottle and re-fix the dust cover.

Instructions for Cleaning Inhaler: Clean your Inhaler at least once a week. Remove the canister and rinse the plastic actuator and cap in warm water but do not put the metal canister into water. Dry the actuator and cap thoroughly and gently replace the metal canister into the actuator with a twisting motion. Put the cap on the mouthpiece.

Interaction

Inhibitors of Cytochrome P450 3A4: Fluticasone propionate is a substrate of CYP3A4. The use of strong CYP3A4 inhibitors (e.g., ritonavir, atazanavir, clarithromycin, indinavir, itraconazole, nefazodone, nelfinavir, saquinavir, ketoconazole, telithromycin) with Fluticasone Propionate HFA is not recommended because increased systemic corticosteroid adverse effects may occur.

Ritonavir: A drug interaction trial with fluticasone propionate aqueous nasal spray in healthy subjects has shown that ritonavir (a strong CYP3A4 inhibitor) can significantly increase plasma fluticasone propionate exposure, resulting in significantly reduced serum cortisol concentrations. During postmarketing use, there have been reports of clinically significant drug interactions in patients receiving fluticasone propionate and ritonavir, resulting in systemic corticosteroid effects including Cushing’s syndrome and adrenal suppression.

Ketoconazole: Coadministration of orally inhaled fluticasone propionate (1,000 mcg) and ketoconazole (200 mg once daily) resulted in a 1.9-fold increase in plasma fluticasone propionate exposure and a 45% decrease in plasma cortisol area under the curve (AUC), but did not affect urinary excretion of cortisol.

Contraindications

The use of Fluticasone Propionate Inhaler is contraindicated in the following conditions: Primary treatment of status asthmaticus or other acute episodes of asthma where intensive measures are required. Hypersensitivity to any of the ingredients.

Side Effects

The most common adverse reactions (incidence >3%) are upper respiratory tract infection or inflammation, throat irritation, sinusitis, dysphonia, candidiasis, cough, bronchitis, and headache.

Pregnancy & Lactation

There are insufficient data on the use of Fluticasone propionate HFA in pregnant women. There are clinical considerations with the use of Fluticasone propionate HFA in pregnant women. There are no available data on the presence of fluticasone propionate in human milk, the effects on the breastfed child, or the effects on milk production. Other corticosteroids have been detected in human milk.

Precautions & Warnings

Candida albicans infection of the mouth and pharynx may occur. Monitor patients periodically. Advise the patient to rinse his/her mouth with water without swallowing after inhalation to help reduce the risk.
Potential worsening of infections (e.g., existing tuberculosis; fungal, bacterial, viral, or parasitic infections; ocular herpes simplex). Use with caution in patients with these infections. More serious or even fatal courses of chickenpox or measles can occur in susceptible patients.
Risk of impaired adrenal function when transferring from systemic corticosteroids. Taper patients slowly from systemic corticosteroids if transferring to Fluticasone propionate HFA.
Hypercorticism and adrenal suppression may occur with very high dosages or at the regular dosage in susceptible individuals. If such changes occur, discontinue Fluticasone propionate HFA slowly.
Assess for the decrease in bone mineral density initially and periodically thereafter.
Monitor the growth of pediatric patients.
Glaucoma and cataracts may occur with long-term use of ICS. Consider referral to an ophthalmologist in patients who develop ocular symptoms or use Fluticasone propionate HFA long term.

Use in Special Populations

Pediatric Use: The safety and effectiveness of Fluticasone Propionate Inhalers in children aged 4 years and older have been established

Overdose Effects

Chronic overdosage may result in signs/symptoms of hypercorticism. Inhalation by healthy volunteers of a single dose of 1,760 or 3,520 mcg of fluticasone propionate CFC inhalation aerosol was well tolerated. Fluticasone propionate given by inhalation aerosol at dosages of 1,320 mcg twice daily for 7 to 15 days to healthy human volunteers was also well tolerated. Repeat oral doses of up to 80 mg daily for 10 days in healthy volunteers and repeat oral doses of up to 20 mg daily for 42 days in subjects were well tolerated. Adverse reactions were of mild or moderate severity, and incidences were similar in active and placebo treatment groups.

Storage Conditions

Store at room temperature between 20°C and 25°C.
Keep away from light & moisture.
Keep out of the reach of children.

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