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iPTX > Pulmonary Med Chem: Asthma > Flashcards

Pulmonary Med Chem: Asthma Flashcards

1
Q

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

A

Full agonist

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2
Q

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

A

Partial agonist

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3
Q

What is the difference between an inverse agonist and antagonist?

A

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

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4
Q

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

A

Inhaled

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5
Q

Define asthma

A

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

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6
Q

What 3 drug classes are commonly used to treat asthma?

A

Bronchodilators, mucolytic and anti-inflammatory drugs

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7
Q

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

A

Sympathetic- adrenergic
Parasympathetic- cholinergic

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8
Q

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

A

Norepinephrine, epinephrine

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9
Q

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

A

Acetylcholine

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10
Q

Sympathetic receptors present in lungs

A

Beta 1, Beta 2 and alpha receptors

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11
Q

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

A

False. Bronchodilation

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12
Q

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

A

True

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13
Q

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

A

False. Stimulation of these receptors causes these effects

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14
Q

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

A

Increase, activates, inhibits

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15
Q

Parasympathetic receptors present in the lungs

A

Nicotinic and muscarinic

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16
Q

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

A

M3 receptor

17
Q

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

A

b. epinephrine

18
Q

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

A

a. Formoterol

19
Q

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

A

Tertiary butyl group

20
Q

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

A

R isomer

21
Q

What makes LABAs more long lasting than SABAs?

A

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

22
Q

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

A

b. Cromolyn

23
Q

Methylxanthine MOA

A

Bronchodilation of smooth muscle

24
Q

Drug classification and MOA of ipratropium

A

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

25
Q

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

A

False. Cromolyn does NOT relax bronchial or other smooth muscles

26
Q

Inhaled corticosteroid MOA

A

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

27
Q

Leukotriene receptor antagonist MOA

A

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

28
Q

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

A

b. Zileuton

iPTX (18 decks)

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