Pulmonary Pharmacology

Question 1

B2-agonists

Answer 1

Albuterol, Salmeterol

USE: asthma, COPD

MOA: stimulate b2
(SABA: 3-4 hr, LABA: 12 hr)

AE: tachycardia, arrhythmias, tremor, hypokalemia

Question 2

In the tx of asthma, B2 agonists must be used in combination with ___

Answer 2

Inhaled corticosteroid (ICS)

Salmeterol + Fluticasone [Advair®]

Question 3

Muscarinic antagonists

Answer 3

Ipratropium, tiotropium

USE: asthma, COPD

MOA: block M receptors
(SAMA: 2 hr, LAMA: 25 hr)

AE: minimal due to limited absorption

Question 4

Muscarinic antagonists: Intoxication

Answer 4

DRY as a bone
HOT as a stone
RED as a beet
MAD as a hatter
BLIND as a bat

Question 5

Methylxanthines

Answer 5

Theophylline VTANC

USE: asthma, COPD

MOA: inhibits PDE (increase cAMP), blocks adenosine receptors

AE: N/V, CNS (HA, nervous, insomnia), tachycardia/arrhythmias

Precautions:
-Narrow therapeutic index; monitoring of plasma levels is recommended
-Many drug interactions

Question 6

Zafirlukast, Montelukast

Answer 6

Leukotriene modifiers (cysLT1 antagonists)

USE: asthma

MOA: block cysLT1 receptor

AE: neuropsychiatric (rare)

Question 7

Zileuton

Answer 7

Leukotriene modifiers (5-lipoxygenase-inhibitors)

USE: asthma

MOA: inhibits 5-lipoxygenase (LOX)

AE:
-Hepatotoxicity (must monitor LFT)
-Neuropsychiatric (rare)

Question 8

Fluticasone

Answer 8

Glucocorticoid (OTC)

USE: asthma, COPD

MOA: activate glucocorticoid receptor, increase annexins, decrease cyto/chemokines

AE:
-Oropharyngeal candidiasis
-Throat irritation
-Higher doses: Systemic effects (Cushing’s)

Question 9

Cromolyns

Answer 9

Cromolyn

USE: asthma

MOA: mast cell stabilizer, decrease release of mediators from mast cells

AE: minimal

Question 10

Omalizumab

Answer 10

Anti-IgE-antibodies

USE: asthma

MOA: monoclonal antibody against IgE, decrease fixation of IgE on mast cells

AE: injection site rxn, anaphylaxis (rare)

Question 11

Roflumilast

Answer 11

PDE4 inhibitor

USE: COPD

MOA: inhibits PDE4, increase cAMP, decrease inflammation

AE: GI (dia, nau, weight loss), psych (insomnia, depression, anxiety)

Question 12

Endothelin receptor antagonists

Answer 12

Macitentan, Ambrisentan HHHP

USE: pulmonary HTN

MOA: block ET, vasodilation

AE: headache, hypotension, hepatotoxicity

CI: pregnancy

Question 13

Eicosanoids

Answer 13

Epoprostenol (PGI2)

USE: pulmonary HTN

MOA: stimulate IP, vasodilation

AE: hypotension, headache, GI, jaw pain/extremity pain

Question 14

NO and Riociguat

Answer 14

USE: pulmonary HTN

MOA: activate sGC, increase cGMP, vasodilation

AE: hypotension, headache

Question 15

PDE5 inhibitors

Answer 15

Sildenafil

USE: pulmonary HTN

MOA: inhibit PDE5, decrease cGMP, vasodilation

AE: hypotension, headache

CI: organic nitrates

Question 16

Calcium channel blocker (CCB)

Answer 16

DHP, Amlodipine

USE: pulmonary HTN

MOA: block LTCC = vasodilation

AE: hypotension, headaches