Fluticasone (systemic, oral inhalation) (monograph)

Fluticasone (systemic, oral inhalation) (monograph)

introduction

Uses for fluticasone (systemic, oral inhalation)

asthma

Fluticasone is used for the long-term prevention of bronchospasm in patients with asthma.

In corticosteroid-dependent patients, fluticasone may allow a significant reduction in the daily maintenance dose of systemic corticosteroid and gradual discontinuation of the maintenance corticosteroid dose.

The fixed combination fluticasone/salmeterol is used only in asthma patients who do not respond adequately to long-term therapy for asthma control (e.g. inhaled corticosteroids) or whose severity clearly warrants initiation of treatment with both an inhaled corticosteroid and a long-acting β2-adrenergic agonist.

Once asthma control is achieved and maintained, assess the patient periodically and reduce therapy (e.g., discontinue fluticasone/salmeterol), if possible without loss of asthma control, and place the patient on long-term asthma control therapy (e.g., inhaled corticosteroids).

Do not use fluticasone/salmeterol in patients whose asthma is adequately controlled by low or moderate doses of inhaled corticosteroids.

COPD

The fixed combination with salmeterol as a powder for oral inhalation (Advair Diskus) is used for the maintenance treatment of airway obstruction in patients with COPD, including chronic bronchitis and/or emphysema; Also used to reduce COPD exacerbations in patients with a history of exacerbations.

Fluticasone/salmeterol is not indicated for the relief of acute bronchospasm.

Dosage and administration of fluticasone (systemic, oral inhalation).

Generally

• Carefully adjust dosage to individual needs and response.

• Once a satisfactory response is achieved, gradually reduce the dosage to the lowest dosage that maintains an adequate clinical response. Aim for the lowest effective dosage, especially in children, as inhaled corticosteroids may impair growth.

asthma

• The recommended starting and maximum doses for oral inhalation of fluticasone are based on previous asthma therapy.

• Recommended starting dose of fluticasone in fixed combination with salmeterol (Advair Diskus) oral inhalation powder based on the patient's asthma severity.

• Recommended starting dose of fluticasone in fixed combination with salmeterol (Advair HFA), an oral inhalation aerosol, based on the patient's current asthma therapy.

• If asthma is not adequately controlled after 2 weeks of fluticasone therapy alone or in fixed combination with salmeterol at the initial dose, replace the current strength with a higher strength.

Switching to oral inhalation therapy in patients receiving systemic corticosteroids

• When switching from systemic corticosteroids to oral inhaled fluticasone, asthma should be reasonably stable before initiating oral inhalation treatment.

• Initially, administer fluticasone by oral inhalation concurrently with the maintenance dose of systemic corticosteroid. After at least one week, gradually discontinue the systemic corticosteroid.

• The decrease in systemic corticosteroid should generally not exceed 2.5 to 5 mg of prednisone (or its equivalent) per week in patients receiving fluticasone for oral inhalation. Once oral corticosteroids are discontinued and asthma symptoms are controlled, titrate the fluticasone dose to the lowest effective amount.

• Patients requiring oral corticosteroids should be slowly withdrawn from systemic corticosteroid use after switching to fluticasone/salmeterol (Advair Diskus) oral inhalation powder. Prednisone dose reduction can be achieved by reducing the daily prednisone dose by 2.5 mg per week during therapy with fluticasone/salmeterol oral inhalation powder.

• Do not use fluticasone/salmeterol oral inhalation aerosol (Advair HFA) to convert patients from systemic corticosteroid therapy.

• Some people have died because systemic corticosteroids were discontinued too quickly. (See Discontinuation of Systemic Corticosteroid Therapy under Precautions.)

Administration

Administer by oral inhalation.

Oral inhalation

Administer fluticasone alone or in fixed combination with salmeterol (Advair HFA) as a microcrystalline suspension by oral inhalation using an oral aerosol inhaler with hydrofluoroalkane (HFA; not a chlorofluorocarbon) as the propellant.

Administer inhalation powder in fixed combination with salmeterol using a special oral inhaler (Advair Diskus) that delivers the medicine from foil-wrapped blister packs.

After each treatment, rinse your mouth thoroughly with water without swallowing.

Inhalation powder

Administer fluticasone in fixed combination with salmeterol using a special oral inhaler (Advair Diskus). Administer twice daily (morning and evening) approximately 12 hours apart.

Hold the Diskus device in one hand, place the thumb of the other hand on the thumb grip and squeeze the thumb grip until the mouthpiece appears and clicks into place.

Push the lever away from the case until you hear a click. The lever pierces the foil blister and releases the powdered medication into an outlet opening. Do not tilt or close the discus device, do not play with the lever, or advance the lever more than once at this time. Each time you press the lever, a dose counter advances.

Breathe out slowly and completely and, with your lips closed, insert the inhaler mouthpiece well into your mouth. After inhaling the dose through your mouth, hold your breath for 10 seconds and exhale slowly.

Do not breathe out into the Diskus device. Do not use an additional dose of the Diskus device if the patient does not feel or taste the medication.

Rinse your mouth after inhaling fluticasone/salmeterol. Slide the thumb grip toward your body to close the Diskus device and reset the device for the next dose. Do not wash or disassemble the inhaler.

Do not use fluticasone/salmeterol with a spacer.

Inhalation aerosol

Shake well (5 seconds) immediately before first use. Operate the fluticasone aerosol inhaler four times before first use. Before first use, spray the aerosol inhaler containing fluticasone in solid combination with salmeterol (Advair HFA) into the air (away from the face) four times and shake well for 5 seconds before each spray.

Operate the fluticasone inhaler once before use if it has not been used for more than a week or if the inhaler has been dropped. If the Advair HFA aerosol inhaler will not be used for more than 4 weeks or the inhaler has been dropped, test spray the inhaler into the air (away from the face) twice and shake well for 5 seconds before each spray.

Breathe out slowly and completely and, with your lips closed, insert the inhaler mouthpiece well into your mouth. Breathe in slowly and deeply through your mouth while using the inhaler. Hold your breath for 10 seconds, pull out the mouthpiece and exhale slowly.

Allow 30 seconds to pass between subsequent inhalations with the aerosol inhaler.

Rinse your mouth thoroughly after each treatment.

Clean the fluticasone inhaler at least once a week after the evening dose by removing the mouthpiece cap from the inhaler and washing the mouthpiece with moistened cotton. Allow the drive to air dry overnight.

Clean the Advair HFA aerosol inhaler by wiping the opening through which the medicine sprays from the metal container and mouthpiece with a dry cotton swab or damp cloth at least once a week after your evening dose. Allow the drive to air dry overnight.

If the dose indicator on the aerosol inhaler for fluticasone alone or in fixed combination with salmeterol (Advair HFA) reads “020,” we recommend that the patient contact the pharmacy for a refill or consult a physician to determine whether a refill is necessary. Discard the aerosol inhaler when the dose counter reads “000.” Never modify or remove the dose counter from the canister.

dosage

Unless otherwise stated, the dose of fluticasone propionate administered as an aerosol via a metered dose inhaler is expressed as the amount delivered by the inhaler actuator per metered actuation.

Fluticasone propionate aerosol for oral inhalation delivers 50, 125, or 250 mcg from the valve and 44, 110, or 220 mcg from the actuator per metered spray. The 10.6 or 12 g canister delivers 120 metered sprays.

The doses of fluticasone propionate and salmeterol in the fixed combination oral inhalation powder (Advair Diskus) are expressed as nominal (labeled) doses contained in each foil-wrapped blister pack. The amount of drug powder delivered to the lungs depends on factors such as the patient's inspiratory flow.

Each actuation of the Advair HFA oral aerosol inhaler delivers 50, 125, or 250 mcg of fluticasone propionate and 25 mcg of salmeterol from the valve. Advair HFA dosages are expressed in terms of the drug delivered through the mouthpiece. Each time the inhaler is actuated, 45, 115, or 230 mcg of fluticasone propionate and 21 mcg of salmeterol are delivered from the mouthpiece.

Commercially available Advair HFA inhalation aerosol delivers 60 or 120 metered sprays per 8 or 12 g canister, respectively.

Pediatric patients

asthma

Fluticasone

Oral inhalation aerosol

Children 4-11 years of age: The starting and maximum dose is 88 mcg twice daily.

Children ≥ 12 years previously receiving bronchodilators alone: ​​Initially, 88 mcg twice daily. If asthma control is inadequate after two weeks of therapy at the initial dose, a higher strength may provide additional asthma control. If necessary, the dosage can be increased to a maximum of 440 mcg twice daily. For children with inadequate asthma control, consider a starting dose of >88 mcg twice daily.

Children ≥ 12 years who have previously received inhaled corticosteroids: Initially, 88 to 220 mcg twice daily. If necessary, the dosage can be increased to a maximum of 440 mcg twice daily. In patients receiving inhaled corticosteroids at the upper end of the dosage range, initial doses of >88 mcg twice daily should be considered.

Children ≥ 12 years who have previously received oral corticosteroids: Initially, 440 mcg twice daily; The maximum dosage is 880 mcg twice daily.

Fluticasone/salmeterol fixed combination

Oral inhalation aerosol

Children ≥ 12 years: 90, 230, or 460 mcg fluticasone propionate and 42 mcg salmeterol (2 inhalations) twice daily approximately 12 hours apart (morning and evening); The recommended starting dose is based on the patient's current asthma therapy.

If asthma control is inadequate after 2 weeks of therapy with the initial dose, replacing the current fixed-dose combination strength with a higher strength (higher strengths contain only higher doses of fluticasone) may provide additional asthma control.

Oral inhalation powder

Children aged 4-11 years: 100 mcg fluticasone propionate and 50 mcg salmeterol (1 inhalation) twice daily approximately 12 hours apart (morning and evening).

Children ≥ 12 years: 100, 250, or 500 mcg fluticasone propionate and 50 mcg salmeterol (1 inhalation) twice daily approximately 12 hours apart (morning and evening); The recommended starting dose depends on the severity of the patient's asthma.

If asthma control is inadequate after two weeks of therapy with the initial dose, replacing the current strength with a higher strength (higher strengths only contain higher doses of fluticasone) may provide additional asthma control.

Adult

asthma

Fluticasone

Oral inhalation aerosol

Previous use of bronchodilators alone: ​​Initially 88 µg twice daily. If necessary, the dosage can be increased to a maximum of 440 mcg twice daily. In adults with inadequate asthma control, consider a starting dose of >88 mcg twice daily.

If you have previously received inhaled corticosteroids: Initially 88-220 mcg twice daily. If necessary, the dosage can be increased to a maximum of 440 mcg twice daily. In patients receiving inhaled corticosteroids at the upper end of the dosage range, initial doses of >88 mcg twice daily should be considered.

If you have previously received oral corticosteroids: The starting and maximum dose is 880 mcg twice daily.

If asthma control is inadequate after two weeks of therapy at the initial dose, a higher strength may provide additional asthma control.

Fluticasone/salmeterol fixed combination

Oral inhalation aerosol

90, 230, or 460 mcg fluticasone propionate and 42 mcg salmeterol (2 inhalations) twice daily approximately 12 hours apart (morning and evening); The recommended starting dose is based on the patient's current asthma therapy.

If asthma control is inadequate after two weeks of therapy with the initial dose, replacing the current strength with a higher strength (higher strengths only contain higher doses of fluticasone) may provide additional asthma control.

Oral inhalation powder

100, 250, or 500 mcg fluticasone propionate and 50 mcg salmeterol (1 inhalation) twice daily approximately 12 hours apart (morning and evening); The recommended starting dose depends on the severity of the patient's asthma.

If asthma control is inadequate after two weeks of therapy with the initial dose, replacing the current strength with a higher strength (higher strengths only contain higher doses of fluticasone) may provide additional asthma control.

COPD

Fluticasone/salmeterol fixed combination

Oral inhalation powder

250 mcg fluticasone propionate and 50 mcg salmeterol (1 inhalation) administered twice daily, approximately every 12 hours (morning and evening).

Prescription Limits

Pediatric patients

asthma

Fluticasone

Oral inhalation aerosol

Children 4-11 years: Maximum 88 mcg twice daily.

Children ≥ 12 years previously receiving bronchodilators alone or inhaled corticosteroids: Maximum 440 mcg twice daily.

Children ≥ 12 years who have previously received oral corticosteroids: Maximum 880 mcg twice daily.

Fluticasone/salmeterol fixed combination

Oral inhalation aerosol

Children ≥ 12 years: Maximum 460 mcg fluticasone propionate and 42 mcg salmeterol (2 inhalations) twice daily.

Oral inhalation powder

Children 4-11 years of age: Maximum 100 mcg fluticasone propionate and 50 mcg salmeterol (1 inhalation) twice daily.

Children ≥ 12 years: Maximum 500 mcg fluticasone propionate and 50 mcg salmeterol (1 inhalation) twice daily.

Adult

asthma

Fluticasone

Oral inhalation aerosol

If you have previously received bronchodilators alone or inhaled corticosteroids: Maximum 440 mcg twice daily.

If you have previously received oral corticosteroids: Maximum of 880 mcg twice daily.

Fluticasone/salmeterol fixed combination

Oral inhalation aerosol

Maximum 460 mcg fluticasone propionate and 42 mcg salmeterol (2 inhalations) twice daily.

Oral inhalation powder

Maximum 500 mcg fluticasone propionate and 50 mcg salmeterol (1 inhalation) twice daily.

COPD

Fluticasone/salmeterol fixed combination

Oral inhalation powder

A maximum of 250 mcg fluticasone propionate and 50 mcg salmeterol (1 inhalation) twice daily. Using doses higher than recommended does not improve lung function.

Special populations

The following information relates to the dosage of fluticasone propionate in special patient populations. When fluticasone propionate is used in fixed combination with salmeterol, the dosage requirements for salmeterol should be taken into account.

Geriatric patients

Inhalation aerosol: Select the dosage with caution, taking into account the greater frequency of reduced liver function, the presence of concomitant diseases or other drug therapies.

Fluticasone/Salmeterol: Dosage adjustments based solely on age are not recommended.

Precautions for fluticasone (systemic, oral inhalation)

Contraindications

• Primary treatment of severe acute asthma attacks or status asthmaticus when intensive measures (e.g. oxygen, parenteral bronchodilators, IV corticosteroids) are required.

• Fluticasone in fixed combination with salmeterol: Primary treatment of status asthmaticus or other acute episodes of asthma or COPD when intensive measures are required.

• Known hypersensitivity to fluticasone or any of the ingredients (e.g. milk protein) in the formulation.

Warnings/Precautions

Warnings

Using fixed combinations

When used in fixed combination with salmeterol, precautions, cautions, contraindications and interactions associated with each drug should be taken into account.

Serious asthma-related events

Long-acting β2-adrenergic agonists such as salmeterol, a component of Advair, increase the risk of asthma-related death when used as monotherapy. Data from clinical trials suggest that monotherapy with long-acting β2-adrenergic agonists also increases the risk of asthma-related hospitalization in children and adolescents.

Use the fixed-dose combination of fluticasone and salmeterol only in asthmatic patients who have not responded adequately to long-term therapy for asthma control (e.g., inhaled corticosteroids) or whose severity clearly warrants initiation of treatment with both an inhaled corticosteroid and a long-acting β2-adrenergic agonist. (See Asthma using.)

Based on the review of 4 clinical studies (3 in adults and adolescents and 1 in children), the FDA concluded that there is no clinically meaningful increased risk of serious asthma-related events (e.g., asthma-related hospitalization, intubation, death) associated with the use of concomitant therapy with long-acting β2-adrenergic agonists and inhaled corticosteroids compared to sole use of inhaled corticosteroids to treat asthma. These studies also showed that fixed-combination therapy with long-acting β2-adrenergic agonists and inhaled corticosteroids was more effective in reducing the frequency of asthma exacerbations than the use of inhaled corticosteroids alone.

Acute exacerbations of asthma or COPD

Do not initiate therapy with the fixed combination of fluticasone and salmeterol in patients with significantly worsening or acutely progressive asthma or acute COPD symptoms.

Failure to respond to a previously effective dose of fluticasone in fixed combination with salmeterol may indicate a significant deterioration of asthma or COPD that requires reevaluation.

Therapy with fluticasone in fixed combination with salmeterol should not be initiated in patients with acute asthma symptoms (e.g., unresponsiveness to usual medications, increasing need for inhaled short-acting β-agonists, significant increase in symptoms, recent visits to the emergency department, sudden or progressive deterioration in lung function).

If inadequate control of symptoms with adjunctive therapy with β2-agonist bronchodilators persists or there is a significant decline in pulmonary function (e.g. PEF), asthma therapy must be reassessed promptly. In such situations, additional/increased doses of salmeterol or other long-acting inhaled β2-agonists (e.g. formoterol) should not be used. Such reassessment may include increasing the strength of the fixed-dose combination (higher strengths contain only higher doses of fluticasone), adding additional inhaled corticosteroids, or introducing systemic corticosteroids. Do not increase the frequency of administration of the fixed combination.

Discontinue systemic corticosteroid therapy

Potential life-threatening exacerbation of asthma or adrenal insufficiency in patients switching from systemic corticosteroids to orally inhaled fluticasone.

Discontinue systemic corticosteroid therapy gradually and monitor for objective signs of adrenal insufficiency (e.g., fatigue, fatigue, weakness, nausea, vomiting, hypotension) during discontinuation of systemic therapy. Also carefully monitor pulmonary function (FEV1 or morning PEF), additional use of β2-adrenergic agonists, and asthma symptoms. Patients receiving ≥20 mg of prednisone (or equivalent) daily may be most susceptible to such adverse events, particularly in the later part of the transfer.

Corticosteroid withdrawal symptoms (e.g. joint pain, muscle pain, fatigue, fatigue, depression) may occur.

Carefully monitor for acute adrenal insufficiency when exposed to trauma, surgery, infection (especially gastroenteritis), or other conditions associated with acute electrolyte loss.

Monitor carefully for eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy associated with Churg-Strauss syndrome.

Pay careful attention to unmasking conditions previously controlled by systemic corticosteroid therapy (e.g., rhinitis, conjunctivitis, eczema, arthritis, eosinophilic disorders).

Do not use fixed-dose combination fluticasone and salmeterol as an oral inhalation aerosol (Advair HFA) when converting patients from systemic corticosteroid therapy.

Immunosuppressed patients

Increased susceptibility to infection in patients taking immunosuppressive medications compared to healthy individuals. Certain infections (e.g. chickenpox, measles) can have more serious or even fatal consequences in such patients, especially children.

Use particular caution to avoid exposure in susceptible patients. If exposure to chickenpox or measles occurs in susceptible patients, administration of varicella-zoster immunoglobulin (VZIG) or pooled immunoglobulin (IG), respectively, should be considered. Consider treatment with an antiviral if chickenpox occurs.

Effects on the respiratory system

Bronchospasm and/or wheezing may occur.

If bronchospasm occurs, treat immediately (e.g. with a short-acting β-adrenergic agonist) and discontinue fluticasone treatment.

Sensitivity reactions

Immediate hypersensitivity reactions (e.g. urticaria, angioedema, rash, bronchospasm, anaphylaxis) may occur.

Anaphylactic reactions have been reported in patients with severe milk protein allergy after oral inhalation of powder products containing lactose (e.g. Advair Diskus). (See “Contraindications” under “Warnings.”)

General precautions

Eye effects

Glaucoma, increased intraocular pressure and cataracts have been rarely reported. Consider regular eye exams.

Systemic corticosteroid effects

Administration of higher than recommended doses of orally inhaled fluticasone may result in manifestations of hypercorticism and suppression of HPA function. If such changes occur, reduce the fluticasone dosage slowly and in accordance with established practices for reducing corticosteroid dosage and treating asthma symptoms.

Use particular caution when monitoring patients after surgery or during periods of stress for signs of inadequate adrenal response.

Effects on the musculoskeletal system

Long-term use may interfere with normal bone metabolism and lead to loss of bone mineral density (BMD).

The use of fluticasone in fixed combination with salmeterol may pose additional risks in patients with major risk factors for decreased BMD, such as tobacco use, advanced age, sedentary lifestyle, poor diet, family history of osteoporosis, or chronic use of medications that may reduce bone mass (e.g., anticonvulsants, corticosteroids).

Because patients with COPD often have multiple risk factors for decreased BMD, assess BMD before starting therapy and periodically thereafter. Consider the use of agents to treat or prevent osteoporosis if a significant reduction in BMD is observed and the use of fixed combination fluticasone and salmeterol is considered important for the treatment of COPD.

Infections

Localized Candida infections of the pharynx have been reported. If infection occurs, appropriate local or systemic treatment and/or discontinuation of therapy may be necessary.

Use with extreme caution, if at all, in patients with clinical or asymptomatic Mycobacterium tuberculosis respiratory tract infections; untreated fungal, bacterial or parasitic infections; or ocular herpes simplex or untreated, systemic viral infections.

Be alert for the possible development of pneumonia in patients with COPD receiving fluticasone in fixed combination with salmeterol (Advair Diskus) oral inhalation powder, as the clinical features of pneumonia and COPD exacerbations often overlap.

Lower respiratory tract infections (e.g., pneumonia) reported in patients with COPD receiving inhaled corticosteroids, including fluticasone alone or in fixed combination with salmeterol (Advair Diskus) oral inhalation powder.

Other effects

Unknown long-term, systemic and local effects of the drug in humans, particularly developmental or immunological processes in the mouth, throat, trachea and lungs.

Specific populations

pregnancy

Category C

lactation

Excreted in the milk of rats; It is not known whether it passes into breast milk.

There are also no data available on the effects of fluticasone on the breastfed child or on milk production.

Be careful with breastfeeding women.

Consider the benefits of breast-feeding along with the woman's clinical need for the drug and potential adverse effects of fluticasone or an underlying maternal condition on the breast-fed infant.

Pediatric use

The safety and effectiveness of oral fluticasone inhalation aerosol or oral inhalation powder containing fluticasone in fixed combination with salmeterol have not been established in children under 4 years of age.

The safety and effectiveness of the oral inhalation aerosol containing fluticasone in fixed combination with salmeterol (Advair HFA) have not been established in children under 12 years of age. The adverse reaction profile of Flovent HFA in pediatric patients (4-11 years of age) is generally similar to that observed in adolescents and adults.

With long-term use, the growth rate in children and adolescents slows down; Routinely monitor (e.g., using stadiometry) the growth and development of children receiving prolonged corticosteroid therapy. Weigh the benefits of corticosteroid therapy against the possibility of growth suppression and the risks associated with alternative therapies. Use the lowest possible dosage that effectively controls asthma.

Geriatric use

There are no significant differences in safety and effectiveness compared to younger adults, but increased sensitivity cannot be ruled out.

There is insufficient experience with fluticasone in fixed combination with salmeterol powder for oral inhalation in patients ≥ 65 years of age with asthma to determine whether geriatric patients respond differently than younger patients.

An increased incidence of serious adverse reactions has been reported in patients aged 65 years with COPD receiving fluticasone in fixed combination with salmeterol oral inhalation powder compared to younger adults; However, the distribution of side effects is similar in both groups. (See Geriatric Patients under Dosage and Administration.)

Liver dysfunction

Plasma concentrations may be increased. Monitor the patient closely.

Common side effects

Fluticasone aerosol for oral inhalation: Upper respiratory tract infection, upper respiratory tract inflammation, sinusitis, sinusitis, dysphonia, throat irritation, candidiasis, cough, bronchitis, headache.

Interactions with other medications

The following information addresses possible interactions with fluticasone. When used in fixed combination with salmeterol, the interactions associated with salmeterol must be taken into account. To date, no formal drug interaction studies have been conducted with the fixed combinations.

Metabolized by CYP3A4 isoenzyme.

Drugs affecting hepatic microsomal enzymes

Strong inhibitors of CYP3A4: Possible pharmacokinetic interaction (increased fluticasone propionate plasma concentrations).

Specific medications

Pharmacokinetics of fluticasone (systemic, oral inhalation).

absorption

Bioavailability

The effectiveness of orally inhaled fluticasone appears to be based on local action rather than systemic absorption. The plasma concentrations of drugs do not provide information about the therapeutic effect.

beginning

Fluticasone: Significant relief usually occurs within 1-2 days; However, continuous therapy of ≥ 1–2 weeks may be required for optimal effectiveness.

Fluticasone in fixed combination with salmeterol: Initial improvement in asthma control may occur within 30 minutes after oral inhalation; Optimal benefit occurs ≥1 week of continuous therapy.

Length of time

When corticosteroids are discontinued, asthma control remains stable for several days or longer.

Special populations

Gender does not affect systemic exposure of fluticasone in patients with asthma.

distribution

extent

Glucocorticoids, including fluticasone, cross the placenta and may be excreted in milk.

Binds weakly to erythrocytes.

Plasma protein binding

Average 91%; little or no binding to transcortin.

Elimination

metabolism

Metabolized to an inactive metabolite via CYP3A4.

Elimination route

Excreted in feces (approx. 95%) as unchanged active substance and metabolites and in urine (<5%) as metabolites.

Half-life

After intravenous administration approximately 7.8 hours.

Special populations

In patients with impaired liver function, plasma concentrations of the drug may be increased.

stability

storage

Oral inhalation

Aerosol

Fluticasone: 25°C (can be exposed to 15-30°C). Protect from excessive heat. Store the metered dose inhaler with the mouthpiece facing down.

Fixed combination with salmeterol: 25°C (can be exposed to 15-30°C) with mouthpiece facing down. Content under pressure; Do not puncture, use or store near heat or open flames, and do not throw into fire or incinerator. At temperatures above 49°C the canister may burst. Discard it when the dose counter reads “000.”

powder

Fixed combination with salmeterol: 20-25°C. Protect from light and excessive heat. Discard Advair Diskus one month after removal from the foil pouch or after each blister pack, whichever comes first.

Actions

• Strong glucocorticoid activity and minimal mineralocorticoid activity.

• Reduces the inflammatory asthmatic response by inhibiting multiple cell types (e.g. mast cells, eosinophils, basophils, lymphocytes, neutrophils).

• Inhibits the accumulation of macrophages in inflamed areas.

• Inhibits the production or secretion of mediators (e.g. eicosanoids, leukotrienes, cytokines, histamine) involved in the asthmatic response.

• Improves lung function (e.g. FEV1, morning peak expiratory flow).

Advice for patients

• When used in fixed combination with salmeterol, it is important to inform patients about important warnings about salmeterol.

• Include a copy of the manufacturer's patient information (Medication Guide) for fluticasone in fixed combination with salmeterol with each prescription. It is important to instruct patients to read the medication guide before starting therapy and each time a prescription is refilled.

• It is important to inform patients receiving the fixed-dose combination of fluticasone and salmeterol that monotherapy with long-acting β2-adrenergic agonists (e.g. salmeterol) increases the risk of asthma-related death and may increase the risk of asthma-related hospitalization in children and adolescents.

• It is important to instruct patients on the use of the oral inhaler and Diskus devices and to provide patients with a copy of the manufacturer's information.

• It is important that children receive oral fluticasone inhalation therapy under adult supervision.

• It is important to have an adequate understanding of proper storage, disposal, preparation and inhalation techniques, including the use of the inhalation systems.

• Importance of mouth rinsing after oral inhalation.

• It is important to advise patients that oral fluticasone inhalation must be administered at regular intervals to be therapeutically effective.

• It is important not to exceed the recommended dosage and to contact a doctor immediately if you experience asthma or COPD symptoms that do not respond to bronchodilators.

• It is important to advise the patient that if a dose of fluticasone alone or in a fixed combination with salmeterol is missed, the next dose should be taken at the regular time. the dose should not be doubled.

• It is important not to discontinue therapy with fluticasone in fixed combination with salmeterol without medical advice, as symptoms may recur.

• It is important to discontinue regular use of short-acting, oral or inhaled β2-adrenergic agonists at the start of therapy with fluticasone in fixed combination with salmeterol and to use short-acting, inhaled β2-adrenergic agonists only to relieve acute symptoms (e.g. shortness of breath).

• Importance of the availability of a short-acting, inhaled β2-adrenergic agonist for acute asthma symptoms. It is important to inform a doctor if a short-acting, inhaled β2-adrenergic agonist is not available for use.

• It is important to contact a doctor if acute symptoms result in reduced effectiveness of a short-acting β2-adrenergic agonist (requiring ≥4 inhalations on ≥2 consecutive days or 1 canister in 8 weeks).

• It is important to advise patients that although significant improvement may occur as early as the first day of therapy with fluticasone propionate, continued therapy may be required for ≥ 1 to 2 weeks to achieve optimal effects.

• It is important to advise patients using a fixed combination of fluticasone and salmeterol that ≥1 week of therapy may be required to achieve optimal effects. It is important to contact a doctor if asthma symptoms do not improve after a week of regular use of the fixed combination.

• It is important to inform patients receiving therapy with a fixed combination of fluticasone and salmeterol about common side effects associated with β2-adrenergic agonists such as palpitations, chest pain, rapid heartbeat, tremor or nervousness.

• It is important to inform patients that corticosteroids can reduce BMD.

• It is important to inform patients that long-term use of inhaled corticosteroids may increase the risk of developing cataracts or glaucoma.

• It is important to inform the doctor about heart problems, high blood pressure, seizures, thyroid disease, diabetes mellitus, liver disease, osteoporosis or immune disorders before starting therapy.

• It is important to advise patients that orally inhaled fluticasone should not be used as a bronchodilator and that the drug is not indicated for emergency use (e.g., relief of acute bronchospasm).

• It is important to seek emergency medical care if breathing problems worsen quickly.

• It is important to advise patients that when using the fixed-dose combination, additional salmeterol or other long-acting inhaled β2-adrenergic agonists should not be used for the prevention of exercise-induced bronchospasm, for the treatment of asthma or COPD, or for other reasons.

• It is important to advise patients switching from systemic corticosteroid therapy to oral fluticasone inhalation therapy to carry specific identification (e.g. card, wristband) indicating the need for additional systemic corticosteroids during periods of stress. It is important to advise such patients to immediately resume full therapeutic dosage of systemic corticosteroids during stressful periods (e.g., severe infection, severe asthma attack) and to contact their physician for further instructions.

• It is important to avoid infection with chickenpox or measles and, if infected, to consult a doctor immediately.

• It is important to inform patients with COPD who are receiving fluticasone in fixed combination with salmeterol oral inhalation powder (Advair Diskus) that they are at increased risk of pneumonia and to contact their doctor if they develop symptoms of pneumonia.

• It is important to inform physicians about existing or planned concomitant therapies, including therapy with prescription drugs, especially other orally inhaled corticosteroids or ritonavir, as well as over-the-counter drugs, vitamins or herbal supplements.

• It is important to inform doctors of allergies to fluticasone, salmeterol (in fixed combination), other medicines or foods.

• It is important for women to tell doctors if they are pregnant, plan to become pregnant, or want to breastfeed.

• It is important to inform patients of other important precautionary information. (See Precautions.)

More information

Fluticasone propionate (systemic, oral inhalation)

Preparations

Excipients in commercial drug preparations may have clinically significant effects in some individuals; Details can be found on the respective product labeling.

For information about shortages of one or more of these drugs, visit the ASHP Drug Shortages Resource Center.

Fluticasone propionate

Fluticasone propionate combinations

AHFS DI Essentials™. © Copyright 2024, Selected changes November 19, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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