Module 2.2.1 (Pharmacology of the drug treatments for COPD) Flashcards
What is the definition of COPD?
Chronic Obstructive Pulmonary Disease (COPD) is a common, preventable and treatable disease that is characterised by persistent respiratory symptoms and non-reversible airflow limitation that is due to airway and/or alveolar abnormalities usually caused by significant exposure to noxious particles or gases.
- Presence of cough and sputum production for at least 3 months in 2 consecutive years
What are the differences between ASTHMA and COPD
Asthma = bronchoconstriction and airway hyperresponsiveness
COPD = small airway fibrosis and alveolar destruction
What are the drugs used to treat COPD –> 6 different types
- Smoking cessation drugs
- Short acting bronchodilators
> Short acting beta agonists (SABAs)
> Short acting muscarinic agents (SAMAs)
- Long acting bronchodilators
> Long acting beta agonists (LABAs)
> Long acting muscarinic agents (LAMAs)
- Xanthines
- Corticosteroids
- Antibacterials
For the drugs used to treat COPD, provide examples for the following
A) Short acting beta agonists (SABAs)
B) Long acting beta agonists (LABAs) –> 5 types
C) Short acting muscarinic agents (SAMA) –> 1 type
D) Long acting muscarinic agents (LAMAs) –> 4 types
E) Xanthines –> 1 type
F) Corticosteroids –> 6 types
A)
- Salbutamol
- Terbutaline
B)
- Formoterol (eformoterol)
- Indacaterol
- Salmeterol
- Vilanterol (combination only)
- Olodaterol (COPD only)
C)
- Ipratropium
D)
- Aclidinium
- Glycopyrronium (glycopyrrolate)
- Tiotropium
- Umclidinium
E)
- Theophylline
F)
- Beclomethasone
- Budesonide
- Ciclesonide
- Fluticasone propionate
- Fluticasone furoate
- Oral prednisolone
Why is smoking cessation so important? What treatment to use?
- First line treatment for COPD
Treatments for nicotine dependence may be necessary
> Nicotine replacement therapy (NRT)
> Bupropion
> Varenicline
What is the MOA of SAMA and LAMAs?
Clue: involves parasympathetic nervous system
Parasympathetic nervous system regulates bronchomotor tone
- ACh as a neurotransmitter in the respiratory system → bronchoconstriction and mucous secretion
> SAMAs and LAMAs are competitive antagonists of endogenous ACh at muscarinic receptors → bronchodilation and ↓ mucous secretion
> Inflammatory stimuli (TNF-α) can also → ↑ production and release of ACh from other cells (e.g. epithelial cells)
For Short-acting muscarinic agent (SAMA);
A) What is an example?
B) Indication
C) MOA
D) Dose of adult with COPD
E) Severe acute asthma dose
A)
- Ipratropium is available as a MDI and nebulizer solution
B)
- Symptom relief of COPD and (asthma – rarely used )
C)
- Promotes bronchodilation by inhibiting cholinergic motor tone (by blocking muscarinic actions of acetylcholine)
D)
- MDI 42mcg – 2 inhalations 3 or 4 times a day when required
E)
- 8 inhalations (168mcg) via spacer or 500mcg neb given every 20 minutes for 3 doses (with salbutamol)
For Long-acting muscarinic agent (LAMA);
A) Provide FOUR examples
B) MOA
C) Indication (3 reasons)
A)
- aclidinium
- glycopyrronium
- tiotropium
- umeclidineum
B)
- Anticholinergic bronchodilators with a longer duration of action – taken once daily
- aclidinium – twice daily
C)
- Long term maintenance treatment of bronchospasm and dyspnoea of COPD
- Preferred to regular ipratropium for stable COPD
- Add on therapy in patients with asthma taking high dose ICS and LABA
What are some examples of LAMBA/LABA combinations?
- Spirolto Respimat® = Tiotropium and oldaterol
- Brimica Genuair® = Aclidinium and formoterol
- Ultibro Breezhale ® = Indacaterol and glycopyrronium
- Anoro Ellipta® = Umclidinium and vilanterol
ICS/LAMA/LABA Trelegy Ellipta® = Fluticasone furoate and umclidinium and vilanterol
For anticholinergics (SAMA and LAMA);
A) Is it more or less effective than B2 agonists in COPD? How does improve exercise tolerance in COPD?
B) Is it more or less effective than B2 agonists in asthma?
A)
- May be as effective or more effective than β2 agonists
- Vagal tone is not necessarily increased in COPD but may be the only reversible element of airway obstruction in COPD
- Anticholinergic drugs ↓ air trapping and improve exercise tolerance in COPD
B)
- Less effective than β2 agonists & less efficient protection against bronchial challenges
- Add on therapy when LABA not effective or tremor from β2 agonists is problematic
Precautions with SAMA and LAMAs?
Use with caution in patients with:
- Narrow angle glaucoma
> Watch for warning signs such as burred vision or visual halos
- Prostatic hyperplasia, or bladder neck obstruction
- Recent MI (<6 months), any unstable or life-threatening cardiac arrhythmia requiring intervention or drug therapy change in the last year, hospitalization of HF (NYHA class II or IV) within last year
- Severe renal impairment (CrCl ≤ 50mL/min)
- Do not allow mist of solution to enter the eyes
- Stopping inhaled anticholinergics – Small rebound ↑ in airway responsiveness
What are the common and rare adverse effects of SAMA and LAMA?
don’t take SAMA and LAMA together
Common: Bitter taste (ipratropium), dry mouth (can cause dental caries), throat irritation, inhalation induced bronchospasm, blurred vision, dizziness (common for ipratropium), urinary retention
Rare: constipation, acute angle-closure crisis, palpitations, allergy (urticaria, rash, angioedema, anaphylaxis)
For corticosteroids in COPD;
A) What is the main role for it? What drug is used to treat and what is the dose?
B) What reduces exacerbations? When is it used?
C) When is ICS/LABA + LAMA used?
D) What does ICS used in COPD result in an increased risk of?
A)
The main role of oral CSs in COPD is to treat exacerbations
- 30–50 mg of oral prednisolone typically for a period of 5-10 days
B)
Regular inhaled corticosteroids reduce exacerbations
- Used at a later stage of stepped treatment in COPD compared to asthma and in higher doses (1.e fluticasone 1000mcg/day)
C)
- Initiate ICS/LABA + LAMA at FEV1 < 50% predicted and 2 exacerbations in the previous 12 months – trial ICS for 3-6 months and continue ICS only if objective benefit
D)
- Increased risk of pneumonia
- Vaccination important
What are the doses of ICS (+LABA) used in COPD?
A) Budesonide + formoterol
B) Fluticasone furoate + vilanterol: 100mcg + 25mcg, once daily
C) Fluticasone propionate + salmeterol: 250 or 500mcg + 50mcg, twice daily
A)
- 400mcg + 12mcg, twice daily
B)
- 100mcg + 25mcg, once daily
C)
- 250 or 500mcg + 50mcg, twice daily
Why are antibacterials used in COPD? What are examples of the bacteria?
There are strong data implicating bacterial infection as a precipitant of a substantial portion of exacerbations
Frequently implicated in COPD exacerbations:
- Streptococcus pneumoniae, Haemophilus influenzae, and Moraxella catarrhalis
- Mycoplasma pneumoniae or Chlamydia pneumoniae are found in 5–10% of exacerbations
