COPD (Pulmonary)

Question 1

b2-agonists

Answer 1

Example: Albuterol, salmeterol

MOA: Stimulate selectively b2 receptor
–> bronchial SM relaxation

AEs: Tachycardia
– Arrhythmias (overdose)
– Tremor
– Hypokalemia

PK:
SABA: Albuterol
LABA: Salmeterol
–must be combined with ICS

Question 2

Muscarinic antagonists

Answer 2

Example: Ipratropium, tiotropium

MOA: Blockade of muscarinic receptors on…
– bronchial smooth muscle –> decrease Bronchoconstriction
– secretory glands –> decrease Secretions

AEs: Minimal antimuscarinic adverse effects due to limited absorption (administered by inhalation)
– Dry mouth
– Increased body temp
– red, dry, hot skin
– CNS symptoms
– Decreased accommodation for near vision

PK:
SAMA: Ipratropium
LAMA: Tiotropium

Question 3

Methylanthines

Answer 3

Example: Theophylline

MOA:
Inhibits PDE in bronchial SM
–> increases cAMP –> increases relaxation of bronchial SM
– Blocks adenosine receptors –> decreases bronchoconstriction

AEs:
N/V
CNS effects: Headache, nervousness, insomnia
Tachycardia, SVT

– Narrow therapeutic index; monitoring of plasma levels is recommended
– Many drug interactions

Question 4

Glucocorticoids

Answer 4

Example: Fluticasone

MOA: Activate glucocorticoid receptor –> several effects on gene transcription

AEs:
– Oropharyngeal candidiasis
– Throat irritation
– Higher doses: Cushing’s syndrome

Question 5

PDE4 inhibitor

Answer 5

Examples: Roflumilast

MOA: Inhibits PDE4 in inflammatory cells increases cAMP –> decreases inflammation

AEs:
– GI adverse effects: Diarrhea, nausea, weight loss
– Psychiatric symptoms (insomnia, depression, anxiety)