Drugs for COPD Flashcards
What is an example of a SAMA used in COPD?
Ipratropium bromide (6-8hrs)
What is an example of a SABA used in COPD?
Salbutamol (4-6hrs)
What is an example of a LAMA used in COPD?
1) Glycopyrronium bromide (12-24hrs)
2) Tiotropium bromide (24hrs)
What are 2 examples of LABAs used in COPD?
1) Salmeterol (12hrs)
2) Formoterol (12hrs)
3) Olodaterol (24hrs)
4) Indacaterol (24hrs)
How do muscarinic antagonists differ from ß-agonists in their regulation of bronchodilatory action in COPD treatment?
Muscarinic: inhibit M3 receptor-mediated bronchoconstriction
ß-agonist: Activate ß2 adrenoceptors to mediate bronchodilation
What is GOLD?
Global initiative for chronic obstructive lung diseases
What is given to a COPD px with a recent hospitalisation due to exacerbation?
Group E: LABA + LAMA (can include ICS if blood eos >300)
LABA:
- Glycopyronnium bromide (12-24 hours)
- Tiotropium bromide (24 hours)
LAMA:
- Salmeterol (12 hours)
- Formoterol (12 hours)
- Olodaterol (24 hours)
- Indacaterol (24 hours)
What is given to a COPD px with 1 moderate exacerbation (not leading to hospital admission) but mMRC dyspnoea scale 0-1, CAT<10?
Group A: SABA/SAMA
- Ipratropium bromide/salbutamol
What is given to a COPD px with 1 moderate exacerbation (not leading to hospital admission) but mMRC dyspnoea scale ≥2, CAT ≥10?
Group B: LABA + LAMA
LABA:
- Glycopyronnium bromide (12-24 hours)
- Tiotropium bromide (24 hours)
LAMA:
- Salmeterol (12 hours)
- Formoterol (12 hours)
- Olodaterol (24 hours)
- Indacaterol (24 hours)
What is the moa of Muscarinic Receptor Antagonists used in COPD?
1) Inhibit M3 receptor-mediated bronchoconstrictions
2) Reverses vagal nerve-mediated bronchospasm & mucus secretion
What are 2 AEs of Muscarinic Receptor Antagonists used in COPD?
1) Unpleasant taste
2) Parasympatholytic (xerostomia, urinary retention in elderly)
Limited systemic side effects as not well absorbed into systemic circulation when taken by inhalation
What is the moa of ß-agonists used in COPD?
1) ß2-adrenoceptor activation mediated bronchodilation
2) Increase in mucociliary clearance
LABAs used in COPD are often combined with ______________ to prolong effectiveness.
Glucocorticoid
What are the components of a triple inhaler?
LAMA + LABA + glucocorticoid
What are 3 AEs of using ß-agonists in COPD treatment?
1) Tremor (commonest side effect) and muscle cramps
2) Peripheral vasodilatation (e.g., flushing)
3) Palpitations & tachycardia (nonselective ß-agonism → ß1 agonist effects)
4) HypoK+/Hypergly
(usually transient and/or insignificant but beware of DDIs with other drugs causing hypoK+/hypergly)
5) ß2-adrenoceptor tolerance (caution in COPD patients who also have asthma)
What is the moa of ICS used in COPD treatment?
1) Anti-inflammation
2) upregulate ß adrenoceptor expression
What is the use of ICS in COPD treatment?
Combined with LABAs to counter downregulation of ß2adrenoceptors by LABAs
e.g. budesonide + formoterol, fluticasone + salmeterol
What are 4 AEs of ICS used in COPD?
1) Oropharyngeal candidiasis (due to localised immunosuppression)
2) Dysphonia (enfeebled voice due to localised muscle wasting)
3) Cough / throat irritation
4) Adrenal suppression (e.g., fluticasone)
5) Easy bruising (especially in elderly)
6) Posterior subcapsular cataracts
7) Osteoporosis
When should ICS NOT be added to bronchodilator COPD treament?
1) Repeated pneumonia events
2) Blood eosinophils <100 cells/uL
3) Hx of mycobacterial infection
How is theophylline administered for COPD treatment?
Oral-ER and IV
What is the moa of theophylline in COPD treatment?
Bronchodilator:
Methylxanthine →
1) inhibit phosphodiesterases
2) Block adenosine receptors
3) ↑adrenaline release from adrenal medulla
4) CNS stimulant on respiration
What are 3 AEs of theophylline in COPD treatment?
1) Narrow therapeutic window (therapeutic range: 5-20 mg/L)
2) Many DDIs
3) GI: Nausea, vomiting, abdominal discomfort, anorexia
4) CNS: Nervousness, tremor, anxiety, insomnia, seizures
5) CVS: Arrhythmias
What is an example of a PDE-4 inhibitor used in COPD treatment?
Roflumilast (oral)
What is the moa of Roflumilast?
Inhibition of PDE-4 prevents breakdown of cAMP:
1) Reduced inflammatory cell activity
2) Inhibition of fibrosis
3) Relaxation of smooth muscle
What is the use of PDE-4 inhibitors (eg. Roflumilast) in COPD treatment?
1) reduces episodes of exacerbation
2) Slows progress of fibrosis
What are 3 AEs of PDE-4 inhibitors (eg. Roflumilast) in COPD treatment?
1) CNS: Headaches, dizziness, insomnia
2) Systemic: diarrhoea, nausea, ↓appetite
3) Rare: anxiety, depression, suicidal ideation
4) Caution in px with hepatic impairment
What is the moa of Azithromycin used in COPD?
1) Macrolide antibiotic prevents bacteria from growing by interfering with protein synthesis
2) anti-fibrotic and airway smooth muscle relaxant
What are 2 AEs of Azithromycin in COPD?
Common: Diarrhoea, nausea, vomiting
Severe: Cardiac arrhythmia
Contraindicated history of cholestatic jaundice or hepatic dysfunction
What are 3 Mucolytics used in COPD treatment?
1) Acetylcysteine
2) Carbocisteine
3) Erdosteine
What are 3 antibiotics to reduce the risk of acute exacerbations in COPD px?
Prone to exacerbations: either
1) Azithromycin
2) Erythromycin
Chronic bronchitis/frequent exacerbation:
- Moxifloxacin pulse therapy
What are 4 vaccinations recommended for stable COPD?
1) Influenza
2) SARS-CoV2
3) PPSV23 + (PCV20/PCV15)
4) Tdap (if not alr vaxxed)
5) VZV (if >50 y/o)
What are 3 pharmacological interventions for smoking cessation?
Nicotinic agonists:
1) Nicotine replacement
2) Varenicline
Antidepressants:
3) Bupropion
4) Nortryptilline
