Breo Ellipta

Uses

Fluticasone Furoate nasal spray is used for the treatment of the symptoms of seasonal and perennial allergic rhinitis in patients aged 2 years and older.

Breo Ellipta is also used to associated treatment for these conditions: Asthma, Bacterial Sinusitis, Chronic Obstructive Pulmonary Disease (COPD), Chronic Sinusitis, Perennial Allergic Rhinitis (PAR), Seasonal Allergic Rhinitis

How Breo Ellipta works

Fluticasone furoate works through an unknown mechanism to affect the action of various cell types and mediators of inflammation. In vitro experiments show fluticasone furoate activating glucocorticoid receptors, inhibiting nuclear factor kappa b, and inhibiting lung eosinophilia in rats.

Dosage

Breo Ellipta dosage

Adults & Children over 12 years: 2 sprays in each nostril once a day. In some cases 2 sprays into each nostril twice daily, not exceeding 4 sprays.

Children under 12 years (2-11 Years): 1 spray in each nostril once a day. Patients should use Fluticasone Furoate nasal spray at regular intervals as directed since its effectiveness depends on its regular use.

Children (under 2 years of age): There are no data to recommend use of Fluticasone Furoate Nasal Spray for the treatment of seasonal or perennial allergic rhinitis in children under 2 years of age.

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. If using for the first time or if you have not used it for a week or more, press the nasal applicator several times until a fine mist 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 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.

Side Effects

Eosinophilic conditions, adrenal insufficiency, growth retardation, Cushing's syndrome, decreased bone density, cataract, glaucoma. Rarely, psychological effects.

Toxicity

Fluticasone furoate administered nasally may be associated with adrenal suppression or an increase in QTc interval though the association has not been well demonstrated in studies. Fluticasone furoate requires no dosage adjustment in renal impairment but must be used in caution in hepatic impairment due to the elimination mechanisms. Fluticasone furoate is not associated with carcinogenicity, mutagenicity, or impairment of fertility. There are no well controlled studies in pregnancy or lactation though animal studies have shown teratogenicity and hypoadrenalism in the offspring of treated mothers and other corticosteroids are known to be excreted in breast milk. Generally, there are no reported adverse effects with fluticasone in pregnancy. Pediatric patients should be given the lowest possible dose and monitored for reduction in growth velocity. There is insufficient evidence to determine whether geriatric patients respond differently to other patients. Systemic exposure may be 27-49% higher in Japanese, Korean, and Chinese patients compared to Caucasian patients. Caution should be exercised in these patients and the benefit and risk should be assessed before deciding on a treatment.

Precaution

Patients taking Fluticasone Furoate nasal spray should be periodically monitored for signs of adverse effects on the nasal mucosa such as epistaxis, nasal ulceration and impaired wound healing. Avoid using the drug in patients with recent nasal ulcers, nasal surgery, or nasal trauma. Closely monitor patients with a history of increased intraocular pressure, glaucoma and hypersensitivity reactions (including anaphylaxis, angioedema, rash, and urticaria). Besides, potential worsening of existing fungal, bacterial, viral, or parasitic infections or ocular herpes simplex, hypercorticism and growth retardation may occur after the administration of Fluticasone Furoate nasal spray.

Interaction

Potent inhibitors of cytochrome P450 3A4 (CYP3A4) may increase exposure to Fluticasone Furoate. Coadministration of ritonavir is not recommended. Use caution with coadministration of other potent CYP3A4 inhibitors, such as ketoconazole.

Special instruction: Patients should be instructed that the device must be primed: before first use, and if the cap is left off or if the device does not seem to be working or if the nasal spray has not been used for 30 days or more. In order to prime the device, the nasal spray needs to be shaken vigorously for about 10 seconds with the cap on. The patient must then press the button firmly all the way in, approximately 6 times until a fine mist is seen. Once primed, the patient must shake the nasal spray vigorously each time before use.

Volume of Distribution

608L at steady state for intravenous administration of fluticasone furoate. Other reports suggest the mean volume of distribution at steady state is 661L. A study of 24 healthy Caucasian males showed a volume of distribution at steady state of 704L following intravenous administration.

Elimination Route

Intranasal exposure of fluticasone furoate results in patients swallowing a larger portion of the dose. However, absorption is poor and metabolism is high, therefore there is negligible systemic exposure with a nasal bioavailability of 0.50% and oral bioavialability of 1.26%. Inhaled bioavailability is 13.9%. A study of 24 healthy Caucasian males showed an inhaled bioavailability of 6.3-18.4%.

Half Life

15.1 hours for intranasal fluticasone furoate and 24 hours for the inhaled formulation. A study of 24 healthy Caucasian males showed a half life of 13.6 hours following intravenous administration and 17.3-23.9 hours followed inhalation.

Clearance

57.8L/h for fluticasone furoate. A study of 24 healthy Caucasian males showed a clearance of 71.8L/h following intravenous administration.

Elimination Route

Fluticasone furoate is eliminated ≥90% in the feces and 1-2% in the urine.

Pregnancy & Breastfeeding use

Pregnancy: Plasma Fluticasone Furoate concentrations were typically non-quantifiable and therefore potential for reproductive toxicity is expected to be very low.

Lactation: The excretion of Fluticasone Furoate into human breast milk has not been investigated.

Contraindication

Fluticasone Furoate nasal spray is contraindicated in patients with a hypersensitivity to any of its ingredients.

Special Warning

Pediatric use: The safety and effectiveness of Fluticasone Furoate in children younger than 2 years have not been established.

Geriatric use: In general, dose selection for the elderly patient should be cautious, keeping in mind the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Use in hepatic impairment: Use Fluticasone Furoate with caution in patients with severe hepatic impairment.

Use in renal impairment: No dosage adjustment is required in patients with renal impairment.

Storage Condition

• Store at a temperature not exceeding 30 °C.
• Do not refrigerate.
• Protect from light and moisture.
• Keep out of the reach of children.

Innovators Monograph

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