fluticasone/vilanterol

General

Pronunciation:
floo-tik-a-sone vye-lan-ter-ol


Trade Name(s)

  • Breo Ellipta

Ther. Class.

bronchodilators

Pharm. Class.

corticosteroids

adrenergics

Indications

  • Maintenance treatment of COPD.
  • Maintenance treatment of asthma.

Action

  • Fluticasone: decreases airway inflammation.
  • Vilanterol: relaxes bronchial smooth muscle.

Therapeutic Effect(s):

  • Improved airflow and ↓ exacerbations in COPD.
  • Reduction in asthma exacerbations.

Pharmacokinetics

Fluticasone

Absorption: 15.2% systemically absorbed from lungs following inhalation; minimal absorption from swallowing (swallowed drug undergoes extensive first-pass hepatic metabolism).

Distribution: Unknown.

Protein Binding: 99.6%.

Metabolism and Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme to inactive metabolites; primarily excreted in feces.

Half-life: 24 hr.

Vilanterol

Absorption: 27.3% systemically absorbed from lungs following inhalation; minimal absorption from swallowing (swallowed drug undergoes extensive first-pass hepatic metabolism).

Distribution: Unknown.

Protein Binding: 93.9%.

Metabolism and Excretion: Primarily metabolized by the CYP3A4 isoenzyme to inactive metabolites. Primarily excreted in urine (70%), with 30% excreted in feces.

Half-life: 21.3 hr.

TIME/ACTION PROFILE (bronchodilation)

ROUTEONSETPEAKDURATION
Fluticasone/vilanterol (inhaln)within 1 hr1–2 hr24 hr

Contraindication/Precautions

Contraindicated in:

  • Hypersensitivity to any components or severe hypersensitivity to milk proteins;
  • Acute attack of asthma or COPD (onset of action is delayed);
  • Patients not receiving a long-term asthma-control medication (e.g., inhaled corticosteroid);
  • Patients whose asthma is currently controlled on low- or medium-dose inhaled corticosteroid therapy.

Use Cautiously in:

  • Moderate to severe hepatic impairment (↑ fluticasone levels may lead to systemic corticosteroid effects);
  • Cardiovascular history;
  • Glaucoma or cataracts;
  • History of seizures, thyrotoxicosis, diabetes mellitus, or ketacidosis;
  • OB:   Safety not established in pregnancy;
  • Lactation:  Use while breastfeeding only if potential maternal benefit outweighs potential risk to infant;
  • Pedi:  Safety and effectiveness not established in children <18 yr (COPD) or <5 yr (asthma);
  • Geri:  Older adults may be more sensitive to effects.

Exercise Extreme Caution in:

Concurrent use of MAO inhibitors or tricyclic antidepressants.

Adverse Reactions/Side Effects

EENT: cataracts, glaucoma, nasopharyngitis, oral candidiasis

Endo: adrenal suppression, ↓ growth (in children), hyperglycemia

F and E: hypokalemia

MS: ↓ bone mineral density

Neuro: headache

Resp: ↑ risk of pneumonia, paradoxical bronchospasm, upper respiratory tract infection

Misc: HYPERSENSITIVITY REACTIONS (including anaphylaxis, angioedema, and urticaria)

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

Route/Dosage

COPD

Inhaln (Adults): One inhalation (fluticasone 100 mcg/vilanterol 25 mcg) once daily.

Asthma

Inhaln (Adults): One inhalation of either fluticasone 100 mcg/vilanterol 25 mcg or fluticasone 200 mcg/vilanterol 25 mcg once daily (base decision on severity of asthma); not to exceed dosage of one inhalation of fluticasone 200 mcg/vilanterol 25 mcg once daily.

Inhaln (Children  12–17 yr): One inhalation (fluticasone 100 mcg/vilanterol 25 mcg) once daily.

Inhaln (Children  5–11 yr): One inhalation (fluticasone 50 mcg/vilanterol 25 mcg) once daily.

Availability

Powder for inhalation (contains lactose): fluticasone 50 mcg/vilanterol 25 mcg/inhalation in a two-strip blister per dose, fluticasone 100 mcg/vilanterol 25 mcg/inhalation in a two-strip blister per dose, fluticasone 200 mcg/vilanterol 25 mcg/inhalation in a two-strip blister per dose

Assessment

  • Monitor respiratory status, including lung sounds. Assess pulmonary function tests periodically during and for several months after a transfer from systemic to inhalation corticosteroids.
  • Assess for severe milk allergy prior to initiation; contains lactose.
  • Monitor for signs and symptoms of hypersensitivity reactions (rash, pruritus, swelling of face and neck, dyspnea) periodically during therapy.
  • Monitor ECG, BP, and HR periodically during therapy. May cause ↑ HR, ↑ BP, prolonged QTc interval, ST segment depression, supraventricular tachycardia, and extrasystoles.
  • Observe for paradoxical bronchospasm (wheezing, dyspnea, chest tightness) and hypersensitivity reaction (rash; urticaria; swelling of face, lips, or eyelids).  If bronchospasm or hypersensitivity reaction occurs,  hold therapy and support as clinically indicated.
  • Assess patients changing from systemic to inhalation corticosteroids for signs of adrenal insufficiency (anorexia, nausea, weakness, fatigue, hypotension, hypoglycemia) during initial therapy and periods of stress.  If signs of adrenal insufficiency appear, notify health care provider immediately; condition may be life-threatening.
  • Monitor for withdrawal symptoms (joint or muscular pain, lassitude, depression) during withdrawal from systemic corticosteroids.
  • Monitor bone mineral density in patients on prolonged therapy and/or with ↑ risk (prolonged immobilization, family history of osteoporosis, postmenopausal status, tobacco use, advanced age, poor nutrition, chronic use of drugs that can reduce bone mass [anticonvulsants, oral corticosteroids]) for fractures.

Lab Test Considerations:

May cause hypokalemia and hyperglycemia.

Implementation

  • Inhaln 

    Administer once daily at the same time each day. Do not open cover of inhaler until ready to use. Discard inhaler 6 wk after opening; inhaler is not reusable.

Patient/Family Teaching

  • Explain purpose and side effects of medication. Advise patient to read  Patient Information  before starting therapy and to follow instructions in Medication Guide for use of inhaler.
  • Advise patient to take medication as directed. If a dose is missed, take as soon as remembered unless almost time for next dose. Advise patient not to discontinue medication without consulting a health care provider; gradual ↓ is required.
  • Advise patient to rinse mouth with water without swallowing after administration to ↓ risk of oropharyngeal candidiasis.
  • Caution patient not to use medication to treat acute symptoms. A rapid-acting inhaled beta-adrenergic bronchodilator should be used for relief of acute asthma attacks. Notify health care provider immediately if symptoms worsen or more inhalations than usual are needed from rescue inhaler.
  • Advise patient to stop using medication and notify health care provider immediately if signs and symptoms of hypersensitivity reaction occurs.
  • Instruct patient not to use additional long-acting beta2  agonists.
  • Caution patient to avoid smoking, known allergens, and other respiratory irritants.
  • Advise patient to notify health care provider if signs and symptoms of pneumonia or sore throat or mouth occur.
  • Instruct patient to notify health care provider immediately if exposed to chickenpox or measles. Inform patients of potential worsening of existing tuberculosis; fungal, bacterial, viral, or parasitic infections; or ocular herpes simplex.
  • Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care provider before taking other Rx, OTC, or herbal products.
  • Advise patient to have regular eye examinations. Instruct patient to notify health care provider immediately if signs and symptoms of glaucoma (eye pain or discomfort, blurred vision, visual halos or colored images in association with red eyes from conjunctival congestion corneal edema) occur.
  • Rep:  Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.
  • Pedi:  Advise caretakers to have a health care provider monitor growth regularly during therapy and to titrate to lowest effective dose.

Evaluation/Desired Outcomes

  • Improved airflow and ↓ exacerbations in COPD.
  • Reduction in asthma exacerbations.