Asthma IV: Pharmacotherapy Flashcards
asthma goals of pharmacotherapy (1 main, 3 small)
maintain asthma control with the minimum amount of medication (lowest effective dose) necessary and
result in the least amount of side effects.
• Prevent or minimize asthma symptoms
• Restore lung function to best resultspossible
• Minimize risk of asthma-related death
Short-Acting β2-Agonists (SABAs)
Type / Class of Medication
AE (3)
- Bronchodilators
- Used as relievers
- Tremors or shakiness
- Nervousness
- Tachycardia / palpitations
Short-Acting β2-Agonists (SABAs)
Purpose / MOA
• Relaxes the muscles around the bronchi to relieve
bronchoconstriction.
• Work within ~20 minutes, last ~4-6 hrs
• Provides temporary relief of symptoms, including cough, chest tightness, dyspnea, and wheeze.
- prophylactically for physical activity, cold air
- 10 min before exposure of known triggers (sign of poorly controlled asthma)
Short-Acting β2-Agonists (SABAs)
additional notes
what is it intended for?
overuse associated with?
SABA-only treatment is no longer recommended, even in well controlled asthma
• Intended for PRN use only; regular use is not recommended and is an indication of poorly- controlled asthma
Regular use (overuse) is associated with
• Increased tolerance
• Airway sensitivity
• Morbidity / mortality
Short-Acting β2-Agonists (SABAs)
drugs
name 4
Ventolin® salbutamol - MDI, diskus, nebules, tabs (discont’d)
Airomir® salbutamol - MDI
Bricanyl® terbutaline - turbuhaler
orciprenaline - syrup (less common)
Inhaled Corticosteroids (ICSs)
Type / Class of Medication
AE (5)
- Anti-inflammatories
- Used as controllers
- Mild fungal infections of the mouth / throat
- “Thrush” or “oral candidiasis”
- Voice changes / hoarseness that are reversible
- Sore throat / sore mouth
- Possible adrenal crisis (rare!)
- With high doses, systemic side effects:
- Osteoporosis, cataracts, skin thinning, growth reduction in children (~1 cm by adult age)
Inhaled Corticosteroids (ICSs)
Purpose / MOA
- Treats airway inflammation
- Treats mucus production
- ICS are first-line controller therapy for all ages
- ICS therapy takes up to 8 weeks before full clinical effect, although usually some benefit after 1 week
- Helps prevent/minimize symptoms
- Minimizes need for reliever therapy
Inhaled Corticosteroids (ICSs)
additional notes
which has less side fx
- Ciclesonide is a prodrug that is biologically inert until activated by esterases in the lung to the active medication; it may have fewer topical side effects (thrush)
- Requires daily use to control symptoms (reduce severe exac by 44%)
- The risks associated with uncontrolled asthma are greater than risks associated with possible side effects
Inhaled Corticosteroids (ICSs) drugs
Alvesco® Ciclesonide - MDI
Arnuity® fluticasone Furoate - Ellipta
- Note: More potent and longer action than propionate
Flovent® fluticasone propionate - MDI, diskus
QVAR® Beclomethasone dipropionate - MDI
Pulmicort® Budesonide - turbulaher, nebules
- preferred in preg
Asmanex® mometasone - twisthalers
Long-Acting β2-Agonists (LABAs)
Type / Class of Medication
AE (4)
- Bronchodilators
- Used as controllers
- Never on their own!!
- Tremors
- Tachycardia
- Irritability
- Insomnia
Long-Acting β2-Agonists (LABAs)
Purpose / MOA
• Longer duration of action than SABAs
• Indicated for patients whose asthma is not well-controlled on an ICS alone or…
• Indicated in ICS/LABA combination for those who
present with severe disease
• In either case, may reduce number of exacerbations
Long-Acting β2-Agonists (LABAs)
Additional notes
- Not to be used as monotherapy
* May increase risk of asthma related death
Long-Acting β2-Agonists (LABAs)
drugs
Oxeze® *formoterol - turbuhaler
Note: Rapid onset, can be used as a reliever (prn) with ICS
Serevent® salmeterol - diskus
Combination ICS / LABAs
Type / Class of Medication
AE (4)
- Combination bronchodilator and anti-inflammatory
- Used as controller medications
- Tremors
- Palpitations
- Mild fungal infections in the mouth and throat
- Voice changes / hoarseness
Combination ICS / LABAs
Purpose / MOA
• Treats airway inflammation and relaxes muscles around the bronchi
• As mentioned, LABAs should only be used as add-on therapy (in combination) with ICS- controller
therapy
• formoterol can be used as an immediate reliever.
Combination ICS / LABAs
Additional notes
• In terms of systemic side effects, they can be similar to those of oral steroids, but less severe
▫ At high doses, over a long period of time, SE include bone weakening, cataracts, glaucoma, and skin thinning
Generally, this would occur at >1000-1500mcg/day doses of beclomethasone or equivalent
Combination ICS / LABAs
drugs (4)
Advair® fluticasone propionate / salmeterol - MDI, disk
Symbicort® budesonide / formoterol - turbuhaler
The only combination product officially indicated for reliever use in patients >12
Breo® Vilanterol + Fluticasone furoate - Ellipta
Zenhale Formoterol + Mometasone - MDI
Combination ICS / LABAs
what is the SMART Strategy
single maintenance and reliever therapy
- Let’s say a patient is on a medium dose of controller medication for maintenance of their asthma
• i.e. Symbicort 200/6mcg ii puffs bid - During this winter’s cold snap, they began to experience poor control of their asthma symptoms
• The patient’s prescriber recommended they increase their Symbicort® use as follows:
• Add 1 additional puff prn to a maximum of 8 total inhalations perday
Long-Acting Muscarinic Antagonists
(LAMAs)
Type / Class of Medication
AE (5)
- Bronchodilator
- Controller medication
• Dry mouth - Rinse mouth to decr. dry mouth AE. • Tremors • Tachycardia / palpitations • Urinary retention • Increased intraocular pressure orblurred vision if in contact with the eye
Long-Acting Muscarinic Antagonists
(LAMAs)
additional notes
what is it not intended for
Not intended for use as a reliever medication for acute bronchospasm
Long-Acting Muscarinic Antagonists
(LAMAs)
drug (1)
Spiriva® tiotropium bromide - capsules for handihaler, respimat
Short-Acting Muscarinic Antagonists (SAMAs)
Type / Class of Medication
AE (2)
- Bronchodilator
- Used as relievers if only option
- Dry mouth
- Glaucoma possible if in direct contact with the eye
Short-Acting Muscarinic Antagonists (SAMAs)
Purpose / MOA
- May be used as add-on therapy to β2- agonists for acute exacerbations
- Compared to β2-agonists, SAMAs have a delayed onset of action but longer duration of action
- Useful for patients who do not tolerate SABA side effects
- unusually susceptible to tremor or tachycardia from beta2-agonist
Short-Acting Muscarinic Antagonists (SAMAs)
Additional Notes
- SAMAs are used more frequently for COPD
- less commonly used for true “reliever” because of their delayed onset of action
- useful in beta-blocker–induced bronchospasm
Short-Acting Muscarinic Antagonists (SAMAs)
drug (1)
Atrovent® ipratropium - MDI
Leukotriene Receptor Antagonists (LRTAs)
Type / Class of Medication
AE (3)
- Leukotriene receptor antagonists
- Used as a controller medication
Generally well tolerated
• Headache
• Abdominal pain
• Depression / nightmares
Leukotriene Receptor Antagonists (LRTAs)
Additional notes
May be used in individuals who cannot / will not
use ICSs
• Second-line
• Add-on, especially in those with comorbid
rhinitis
May provide protection against bronchoconstriction when taken before exercise or allergen / cold air exposure
risk of neuropsychiatric events, suicdality (montelukast)
Leukotriene Receptor Antagonists (LRTAs)
drug (1)
monteleukast Singulair® - granules or chew tabs
Oral Corticosteroids
Type / Class of Medication
AE (short term, long term)
- Anti-inflammatory
- Used as controllers
Short-term • Insomnia • GI upset • Mood swings / psychosis • High BP / BG • Fluid retention
Long-term • Ulcers • Impaired immune response • Acne, diabetes, hypertension • Increased fat production
Oral Corticosteroids
Additional notes
- Short-course therapy does not need to be tapered
- Canadian guidelines suggest prednisone 25-50mg qd x 7-14 days
- Minimizing the need for this treatment by optimizing other pharmacotherapy options is the goal
Oral Corticosteroids
drugs
prednisone - tabs, syrups
methylprednisolone - tabs
Dexamethasone - tabs
- reduces emesis vs prednisone
Immunotherapy
AE (3)
costly
- Dizziness
- Leg pain or fractures
- Injection site reactions: Pain, redness, irritation
- Not studied in children or pregnant / breastfeeding women
- Must be supervised by an asthma or respiratory specialist
Immunotherapy
drugs in Canada
• Omalizumab (Xolair®) a biologic.
• Used in allergic asthma. If IgE 30-700 IU/mL.
• Omalizumab is for patients aged 6 years and older with moderate to severe persistent Allergic Asthma who are uncontrolled on inhaled corticosteroids
(ICS).
• 150 – 375mg by subcutaneous injection every 2 to 4 weeks (dose based on patient factors)
Biologics
AE (5)
Additional notes
• These products have not been studied in unique populations
Mepolizumab, reslizumab, or benralizumab if
eosinophillic asthma e.g. eosinophils >300-400
cell/uL.
- Anaphylaxis
- Injection site reactions
- Headache, sore throat
- Fever and/or infections
- Back or abdominal pains
- May be used as add-on maintenance therapy for patients with severe eosinophilic asthma
- When patients are uncontrolled on medium- to high-dose ICS and LABA
- Patients with parasitic infections should be treated for that condition first
Biologics
Benralizumab
MOA
brand, formulation
Fasenra® - SC injection
anti IL-5
Eosinophils involved in the inflammatory process. This medication selectively binds to IL-5 receptors on eosinophils and basophils and induces apoptosis
Biologics
Mepolizumab
MOA
brand, formulation
Nucala® - SC injection
IL-5 inhibitors
This IgG1 antibody binds with high affinity to IL-5 and prevents it from binding to eosinophils, decreasing survivability of eosinophils
Biologics
Reslizumab
MOA
brand, formulation
Cinqair® - IV infusion
IL-5 inhibitors
Similar to mepolizumab, IgG4 antibodies bind to IL-5 and decrease survivability of eosinophils
Biologics
Reslizumab
MOA
brand, formulation
Dupixent® - SC injection
anti-IL-4 & 13 inhibitor
spacers
read for more
flu shots read slide
All children – kids aged under 4–5 years will need a mask attached
Other - Theophylline, azithromycin
when is it used?
AE for azithromycin
- Narrow therapeutic range, frequent adverse effects, & drug interactions limit use
- 4th line due to systemic toxicity & only mild bronchodilator activity; useful as ‘add on’ agent in some requiring high-dose corticosteroids
azithromycin may decrease ex in > 18 yrs
500mg x 3 time a wk
Risk of incr. QT, resistance, & ototoxicty
