Inhaled Steroids Study Notes

Inhaled Steroids

Overview

  • Inhaled steroids are effective for:

    • Prevention and treatment of inflammation in the airway.

Approved Agents

  • The following agents are approved for use as inhaled steroids:

    • Beclomethasone (QVAR Redihaler)

    • Budesonide (Pulmicort Respules, Pulmicort Flexhaler)

    • Ciclesonide (Alvesco)

    • Fluticasone (Flovent Diskus, Flovent HFA)

    • Triamcinolone (generic)

  • Choice of agent depends on individual patient response; a patient may not respond to one agent but do well on another.

  • Recommended to try another preparation if the first is ineffective after 2-3 weeks.

  • Some agents available as nasal sprays to relieve allergic rhinitis symptoms.

  • Systemic corticosteroids are discussed in more detail in Chapter 36.

Fixed-Combination Drugs

  • Fixed-combination drugs merge different classes of medications for treating asthma and COPD, enhancing therapeutic efficacy. Examples include:

    • Advair Diskus / Advair HFA: Fluticasone (steroid) + Salmeterol (long-acting beta2-adrenergic agonist, LABA)

    • Combivent Respimat: Ipratropium (anticholinergic) + Albuterol (beta2-adrenergic agonist)

    • Symbicort: Budesonide (corticosteroid) + Formoterol (LABA)

    • Anoro Ellipta: Umeclidinium (anticholinergic) + Vilanterol (LABA)

    • Breo Ellipta: Fluticasone (corticosteroid) + Vilanterol (LABA)

    • Breztri Aerosphere: Budesonide (corticosteroid) + Glycopyrrolate (anticholinergic) + Formoterol Fumarate (LABA)

    • Bevespi Aerosphere: Glycopyrrolate (anticholinergic) + Formoterol Fumarate (LABA)

    • Duaklir Pressair: Aclidinium Bromide (anticholinergic) + Formoterol Fumarate (LABA)

    • Dulera: Mometasone (corticosteroid) + Formoterol (LABA)

    • Trelegy Ellipta: Fluticasone (corticosteroid) + Umeclidinium (anticholinergic) + Vilanterol (LABA)

    • Airduo Respiclick: Fluticasone (corticosteroid) + Salmeterol (LABA)

Therapeutic Actions and Indications

  • Inhaled steroids decrease inflammation in the airway, which results in:

    • Increased airflow

    • Facilitated respiration

  • Inhalation reduces systemic effects associated with steroid use by:

    • Decreasing effectiveness of inflammatory cells

    • Decreasing swelling from inflammation

    • Promoting beta-adrenergic receptor activity, enhancing smooth muscle relaxation, and inhibiting bronchoconstriction

Pharmacokinetics

  • Inhaled steroids are rapidly absorbed from the respiratory tract. However, effective levels take about 2-3 weeks to be reached.

  • Patients should continue taking the medications to reach and maintain effective levels.

  • Mostly metabolized by the liver and excreted in urine.

  • Glucocorticoids can cross the placenta and enter human milk.

Contraindications and Cautions

  • Inhaled steroids are not for emergency use or during an acute asthma attack or status asthmaticus.

  • Should not be used in pregnancy or lactation unless benefits outweigh risks.

  • Use with caution in patients with active infections of the respiratory system, as steroid use may depress the inflammatory response leading to serious illness.

Adverse Effects

  • Inhaled steroids typically cause fewer adverse effects compared to oral or parenteral administration. Some common adverse effects include:

    • Sore throat

    • Hoarseness

    • Coughing

    • Dry mouth

  • Serious adverse effects can include:

    • Laryngeal or pharyngeal fungal infections

    • Glaucoma (for long-term users)

    • Growth impairment in pediatric patients

    • Coma

    • Cataracts

    • Decreased bone mineral density

Clinically Important Drug-Drug Interactions

  • Currently, there are no known drug interactions with inhaled steroids.

  • Coadministration of fluticasone with ritonavir is not recommended due to increased plasma levels of fluticasone.

Prototype Summary: Budesonide

  • Indications:

    • Prevention and treatment of asthma

    • Treatment of chronic steroid-dependent bronchial asthma

    • Adjunct therapy for patients not controlled by traditional bronchodilators

  • Actions:

    • Decreases inflammatory response in the airway, increasing airflow and facilitating respiration.

  • Pharmacokinetics:

    Route

    Onset

    Peak

    Duration

    Inhalation

    Slow

    Rapid absorption

    8-12 h ( varies)

  • Half-life (T1/2): Approximately 2-3 hours; primarily metabolized in the liver and excreted in urine.

  • Adverse Effects:

    • Irritability

    • Headache

    • Rebound congestion

    • Hypersensitivity

    • Local infection.