Controller Drug Class & Adverse Effects/Clinical Pearls Flashcards
inhaled corticosteroids (ICS)
prevent and control inflammation
AE: oral thrush (candidiasis), cough, dysphonia
Counseling tip: patients should rinse their mouth and spit after use to prevent oral thrush
- inhaled corticosteroids are the most effective long-term control therapy for asthma (improve quality of life, increase lung function, and reduce the risk of exacerbations)
- ICSs may increase the risk of pneumonia in patients with COPD
- titrate to lowest effective dose
- high doses increase the risk for systemic side effects
- Pulmicort Respules should use Jet Nebulizer and should not be mixed with other nebulizer medications
Long Acting Beta Agonist (LABA)
increase in cAMP -> bronchial smooth muscle relaxation and inhibit hypersensitivity mediators from mast cells (histamine and leukotrienes)
AE: tachycardia, headache, tremor, hypokalemia
Boxed warning for increased risk of asthma-related death for all monotherapy LABA use - should not be used alone for asthma management
Boxed warning for increasing hospitalizations in pediatric and adolescent patients
- prolonged QT seen with intentional overdoses
- not for acute symptoms
- may be helpful for exercise-induced bronchospasm
- Formoterol and indacaterol capsules should not be taken orally
- pediatric considerations: most children <4 YO cannot provide sufficient inspiratory flow for adequate lung delivery with a DPI
Long Acting Antimuscarinics (LAMA)
block the bronchoconstrictor effects of acetylcholine on M3 and M2 receptors
AE: dry mouth, dizziness, blurred vision, upper respiratory infections, paradoxical bronchospasms
- Tiotropium has been approved for use in asthma as an add-on option for children ages 12+
ICS/LABA Combo
AE: see individual products
- guidelines recommended combination LABA with ICS in asthma, as LABA should not be used as monotherapy
- combo products developed to create convenient packaging and assist with patient adherence
LABA/LAMA Combo
AE: see individual products
- not indicated for treatment of acute deteriorations
LABA/LAMA/ICS Combo
AE: see individual products
Mast Cell Stabilizer: cromolyn
AE: high incidence of unpleasant taste in mouth (>10%), rare cardiac arrhythmias, coughing, dyspnea, sore throat, N/V/D if absorbed systemically
- less effective than low-dose ICS
- prevents increase in bronchial hyperreactivity seen in allergy season
Leukotriene Modifiers
block the production of leukotrienes
AE: neuropsychiatric events (agitation, anxiety, abnormal dreams, hallucinations, depression, suicidal thinking), Churg-Strauss syndrome (rare), increased hepatic transaminases (zafirlukast & zileuton)
- less effective than low-dose ICS and ICS/LABA in asthma
- have not been adequately trialed in COPD
Montelukast
- minor substrate of CYP2C8/9 and 3A4
- not for acute relief of symptoms
- Boxed warning: neuropsychiatric events
Zafirlukast
- take at least 1 hour before or 2 hours after meals
- can increase INR (higher INR = thinner the blood/takes longer to clot)
- major substrate, minor inhibitor of CYP 2C9
Zileuton
- weak CYP1A2 inhibitor
- take with food
Methylxanthines: theophylline
bronchodilation through inhibition of PDE III and PDE IV
AE: insomnia, GI upset, hyperactivity, hypotension, tremor
Dose-related toxicity: tachycardia, nausea, vomiting, headache, seizures, arrhythmias
CI: peptic ulcer disease, arrhythmias, seizure disorders
DI: major substrate of CYP 3A4, 1A2. 2E1
- increase in concentration: cimetidine, erythromycin, clarithromycin, ciprofloxacin, ticlopidine
- decrease in concentration: phenobarbital, phenytoin, carbamazepine, rifampin, smoking
- PDE III inhibition likely cause for hypotension, tachycardia, and nausea
Anti-IgE: omalizumab
inhibit IgE binding to receptors on mast cells and basophils, inhibit mediator release and attenuation of early- and late-phase allergic response
AE: headache, injection site reactions, arthralgias, thrombocytopenia, pharyngitis, sinusitis, upper respiratory tract infections
Boxed warning: anaphylaxis
- monitor for anaphylaxis before and after injection
- do not give more than 150 mg per injection site
- FDA approved for moderate to severe persistent asthma in patients with a positive skin test or reactivity to a perennial aeroallergen and symptoms that are inadequately controlled with ICS
Anti-IL5: mepolizumab
blocks binding of IL-5 to the alpha chain of the IL-5 receptor complex, which results in reduced production and survival of eosinophils
AE: headache, injection site reactions, arthralgias, Herpes Zoster infection
Precaution: anaphylaxis
- monitor for anaphylaxis before and after injection
- available as an in-clinic or at-home injection
- indicated for add-on maintenance treatment of patients with severe asthma with an eosinophilic phenotype
Anti-IL5: reslizumab
blocks binding of IL-5 to the alpha chain of the IL-5 receptor complex, which results in reduced production and survival of eosinophils
AE: injection site reactions, myalgias, increased creatinine phosphokinase
Boxed warning: anaphylaxis, malignancies
- monitor anaphylaxis before and after injection
- indicated for add-on maintenance treatment of patients with severe asthma with an eosinophilic phenotype
Anti-IL5: benralizumab
blocks binding of IL-5 to the alpha chain of the IL-5 receptor complex, which results in reduced production and survival of eosinophils
AE: injection site reactions, antibody development, headache, pharyngitis, fever
Precaution: anaphylaxis
- available as an in-clinic or at-home injection
- indicated for add-on maintenance treatment of severe asthma in adults and children ages 12+ with an eosinophilic phenotype
- acts on IL-5 receptors while others act on IL-5
Anti-IL4/IL13: dupilumab
blocks binding of IL-4 to reduce eosinophil trafficking and IgE reactions while also blocking IL-13 to reduce mucus secretion and airway remodeling
AE: injection site reactions, antibody development, arthralgias, conjunctivitis
Precaution: anaphylaxis
- available in pre-filled syringe for in-office or at-home administration
- indicated as an add-on maintenance treatment in patients with moderate to severe asthma ages 12+ with an eosinophilic phenotype or with oral corticosteroid dependent asthma
Phosphodiesterase-4 Inhibitors: roflumilast
inhibits PDE4 leading to increase in cAMP
AE: HA, weight loss, diarrhea, nausea
Monitoring: liver function test, weight
DI: CYP3A4 (major), CYP1A2 (minor)
CI: Child-Pugh class B or C
