Respiratory

Question 1

Beta 2 Adrenoceptor
- MOA

Answer 1

GPCR (Gs)
- Increases cAMP

Question 2

Beta 2 Adrenoceptor Agonist
- MOA

Answer 2

• Dilate bronchi by acting on Gs Beta 2 Adrenoceptors
• Inhibit mediator release from mast cells
• Inhibit TNFa release from monocytes
• Increase mucus clearance by acting on cilia

Question 3

Beta 2 Adrenoceptor Agonist
- cAMP relationship to bronchi

Answer 3

Beta 2 Adrenoceptor activation = Increased cAMP

• More cAMP = Greater activation of PKA
  –> Reduces Ca2+ levels leading to bronchidilation

Question 4

Salbutamol

Answer 4

Beta 2 Adrenoceptor Agonist
- Oral/Injection
- Short Acting

Question 5

Terbutaline

Answer 5

Beta 2 Adrenoceptor Agonist
- Short Acting

Question 6

Salmeterol

Answer 6

Beta 2 Adrenoceptor Agonist
- Long Acting

Taken when asthma is not properly controlled by glucocorticoids

Question 7

Formoterol

Answer 7

Beta 2 Adrenoceptor Agonist
- Long Acting

Taken when asthma is not properly controlled by glucocorticoids

Question 8

Beta 2 Adrenoceptor Agonists
- Adverse Effects

Answer 8

• Tachycardia
• Dysrhythmias
• Tremor

Question 9

Theophylline/Aminophylline
- MOA

Answer 9

• Inhibits PDE
  –> Prevents breakdown of cAMP = Increase cAMP
• Inhibits Adenosine Receptors
• Inhibits intracellular calcium release
  –> Reduces smooth muscle contraction

Question 10

Theophylline/Aminophylline
- Adverse Effects

Answer 10

Dysrhythmia
Seizures

Question 11

Montelukast/Zafirlukast
- MOA

Answer 11

Cysteinyl Leukotriene Receptor Antagonist (CysLT1)

Antagonism reverses:
- Bronchoconstriction
- Hyperresponsive airways
- Mucosal edema
- Mucosa hypersecretion

Question 12

Montelukast/Zafirlukast
- Comparison to Beta 2 Adrenoceptor Agonist

Answer 12

Not as effective as Beta 2 Adrenoceptor Agonist

Question 13

Montelukast/Zafirlukast
- Route

Answer 13

Taken by mouth
Usually taken with inhaled corticosteroids

Question 14

Beclometasone

Answer 14

Glucocorticoid
- Given as an inhalation

Anti-inflammatory
- Treats acute severe asthma
- Prevent chronic asthma

Adverse Effect:
- Adrenal Suppression
- Oropharyngeal candidiasis

Question 15

Budenoside

Answer 15

Glucocorticoid
- Given as an inhalation

Anti-inflammatory
- Treats acute severe asthma
- Prevent chronic asthma

Adverse Effect:
- Adrenal Suppression
- Oropharyngeal candidiasis

Question 16

Fluticasone

Answer 16

Glucocorticoid
- Given as an inhalation

Anti-inflammatory
- Treats acute severe asthma
- Prevent chronic asthma

Adverse Effect:
- Oropharyngeal candidiasis

Question 17

Mometasone

Answer 17

Glucocorticoid
- Given as an inhalation

Anti-inflammatory
- Treats acute severe asthma
- Prevent chronic asthma

Adverse Effect:
- Oropharyngeal candidiasis

Question 18

Ciclesonide

Answer 18

Glucocorticoid
- Given as an inhalation

Anti-inflammatory
- Treats acute severe asthma
- Prevent chronic asthma

Adverse Effect:
- Oropharyngeal candidiasis

Question 19

Prednisolone

Answer 19

Glucocorticoid
- Given orally

Anti-inflammatory
- Used for patients with severe disease

Adverse Effect
- Risk of infection
- Osteoporosis

Question 20

Glucocorticoids
- General MOA

Answer 20

Controls Gene Expression

1. Binds intracellular receptor
2. Dimerizes
3. Complex translocates into the nucleus
4. Modifies Gene Transcription
   –> Transcription Factors

Question 21

Basic Transactivation

Answer 21

Ligands binds to Glucocorticoid Receptor Dimer
–> Upregulates Transcription

Question 22

Basic Transrepression

Answer 22

Ligands binds to Glucocorticoid Receptor Dimer
–> Complex binds to nGRE
–> Turns off transcription

Question 23

Glucocorticoids
- Asthma MOA

Answer 23

Reduces transcription of
IL-2
–> Inhibits proliferation of Th Cells
–> Reduces formation of Th cytokines
–> Decreases activation of eosinophils

Reduces transcription of
IL-5/IL-13

Reduces transcription of lgE and lgE receptors

Question 24

Glucocorticoids
- Adverse Effects

Answer 24

Oropharyngeal Candidiasis (Thrush)
Adrenal Suppression in Beclometasone and Budenoside

Systemic Side Effects are uncommon due to low systemic absorption and bioavailability from inhalation route of administration

Question 25

Glucocorticoids - Other Considerations

Answer 25

Are usually used in combination with Beta 2 Adrenoceptor Agonists for Chronic Asthma - Dilation of Bronchial smooth muscles enhance deliver of glucocorticoids to the airway - Glucocorticoids cause an increase in expression of Beta 2 Adrenoceptors in the airway

Question 26

Omalizumab

Answer 26

Humanized Monoclonal Anti-lgE antibody - Binds to free lgE and prevents it from interacting with

Question 27

Mepolizumab

Answer 27

Humanized Monoclonal Antibody - Binds to and inhibits IL-5 --> Prevents differentiation and recruitment of eosinophils Treats Eosinophilic Asthma

Question 28

Reslizumab

Answer 28

Humanized Monoclonal Antibody - Binds to and inhibits IL-5 --> Prevents differentiation and recruitment of eosinophils Treats Eosinophilic Asthma

Question 29

Ipratropium

Answer 29

Inhaled Anticholinergic (Muscarinic M1-M3 Antagonist) - Treats Underlying symptoms of COPD M3 Muscarinic Receptors - Parasympathetic stimulation of these receptors causes bronchoconstriction and bronchial secretions

Question 30

Tiotropium

Answer 30

Inhaled Anticholinergic (Muscarinic M3 Antagonist) - Treats Underlying symptoms of COPD M3 Muscarinic Receptors - Parasympathetic stimulation of these receptors causes bronchoconstriction and bronchial secretions

Question 31

Aclidinium

Answer 31

Inhaled Anticholinergic (Newer Longer Acting) - Treats COPD

Question 32

Umeclidinium

Answer 32

Inhaled Anticholinergic (Newer Longer Acting) - Treats COPD

Question 33

Glycopyrrolate

Answer 33

Inhaled Anticholinergic (Newer Longer Acting) - Treats COPD

Question 34

Roflumilast

Answer 34

Long-Acting Phosphodiesterase 4 Inhibitor - Prevents degradation of cAMP --> Increases cAMP --> Increase PKA --> Decrease Calcium --> Reduces Inflammation Combined with bronchodilators to treat COPD