Pulmonary Med Chem: Asthma

Question 1

What is the term for a ligand that can induce conformational change in the receptor leading to max effect?

Answer 1

Full agonist

Question 2

What is the term for a ligand that induces some degree of receptor activation, but not a maximal response?

Answer 2

Partial agonist

Question 3

What is the difference between an inverse agonist and antagonist?

Answer 3

An inverse agonist is used when a receptor is constitutively active to turn it off while an antagonist competes with other substrates of a binding site

Question 4

What is the preferred drug delivery route for asthma and COPD treatment?

Answer 4

Inhaled

Question 5

Define asthma

Answer 5

Chronic inflammatory obstructive reversible disease of the airway characterized with bronchoconstriction, bronchial mucosal edema, and mucus plugging

Question 6

What 3 drug classes are commonly used to treat asthma?

Answer 6

Bronchodilators, mucolytic and anti-inflammatory drugs

Question 7

Which compartment of the autonomic nervous system has adrenergic effects and which compartment has cholinergic effects?

Answer 7

Sympathetic- adrenergic
Parasympathetic- cholinergic

Question 8

Adrenergic drugs stimulate _____ or _______ receptors and anti-adrenergic drugs block receptors of these same ligands

Answer 8

Norepinephrine, epinephrine

Question 9

Cholinergic drugs stimulate _____ receptors and anti-cholinergic drugs block receptors of the same ligand

Answer 9

Acetylcholine

Question 10

Sympathetic receptors present in lungs

Answer 10

Beta 1, Beta 2 and alpha receptors

Question 11

True or false: Stimulation of beta 2 receptors in lungs causes bronchoconstriction

Answer 11

False. Bronchodilation

Question 12

True or false: Stimulating alpha receptors in lungs causes vasoconstriction and vasopressor effect

Answer 12

True

Question 13

True or false: Blocking beta 1 receptors in the lungs causes increased heart rate

Answer 13

False. Stimulation of these receptors causes these effects

Question 14

Beta 2 adrenergic drugs (increase/decrease) cAMP levels which (activates/inhibits) adenylyl cyclase and (activates/inhibits) phosphodiesterase activity

Answer 14

Increase, activates, inhibits

Question 15

Parasympathetic receptors present in the lungs

Answer 15

Nicotinic and muscarinic

Question 16

Stimulation of which muscarinic receptor in the airway causes bronchoconstriction and increased airway secretion

Answer 16

M3 receptor

Question 17

Which of the following catecholamines acts on alpha 1, alpha 2, beta 1 and beta 2 receptors?
a. ephedrine
b. epinephrine
c. norepinephrine
d. isoproterenol

Answer 17

b. epinephrine

Question 18

Which of the following is a long acting, full agonist?
a. Formoterol
b. Salmeterol
c. Levalbuterol
d. Albuterol

Answer 18

a. Formoterol

Question 19

What characteristic of albuterol makes it more selective for beta 2 receptors?

Answer 19

Tertiary butyl group

Question 20

Levalbuterol is the (R/S) isomer of racemic albuterol

Answer 20

R isomer

Question 21

What makes LABAs more long lasting than SABAs?

Answer 21

High lipophilicity due to long R chain and anchoring due to phenyl group

Question 22

Which of the following is not a PDE4 inhibitor?
a. Caffeine
b. Cromolyn
c. Theobromine
d. Theophylline

Answer 22

b. Cromolyn

Question 23

Methylxanthine MOA

Answer 23

Bronchodilation of smooth muscle

Question 24

Drug classification and MOA of ipratropium

Answer 24

Anti-muscarinic agent. Blocks vagus nerve mediated acetylcholine effects on airway smooth muscle muscarinic receptors

Question 25

True or false: Cromolyn is mast cell stabilizer that relaxes bronchial muscles

Answer 25

False. Cromolyn does NOT relax bronchial or other smooth muscles

Question 26

Inhaled corticosteroid MOA

Answer 26

Anti-inflammatory properties; they do not relax airway smooth muscle but reduce reactivity and reduce their frequency of asthma exacerbation; inhibition of infiltrates by lymphocytes, eosinophils and mast cells in asthmatic airway

Question 27

Leukotriene receptor antagonist MOA

Answer 27

Inhibits 5-lipoxygenase and inhibits binding of LTD4 to its receptor tissue

Question 28

Which of the following leukotriene receptor antagonists is not commercially available in the U.S.? a. Montelukast b. Zileuton c. Zafirlukast

Answer 28

b. Zileuton