Pulmonary Med Chem: Asthma Flashcards
What is the term for a ligand that can induce conformational change in the receptor leading to max effect?
Full agonist
What is the term for a ligand that induces some degree of receptor activation, but not a maximal response?
Partial agonist
What is the difference between an inverse agonist and antagonist?
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
What is the preferred drug delivery route for asthma and COPD treatment?
Inhaled
Define asthma
Chronic inflammatory obstructive reversible disease of the airway characterized with bronchoconstriction, bronchial mucosal edema, and mucus plugging
What 3 drug classes are commonly used to treat asthma?
Bronchodilators, mucolytic and anti-inflammatory drugs
Which compartment of the autonomic nervous system has adrenergic effects and which compartment has cholinergic effects?
Sympathetic- adrenergic
Parasympathetic- cholinergic
Adrenergic drugs stimulate _____ or _______ receptors and anti-adrenergic drugs block receptors of these same ligands
Norepinephrine, epinephrine
Cholinergic drugs stimulate _____ receptors and anti-cholinergic drugs block receptors of the same ligand
Acetylcholine
Sympathetic receptors present in lungs
Beta 1, Beta 2 and alpha receptors
True or false: Stimulation of beta 2 receptors in lungs causes bronchoconstriction
False. Bronchodilation
True or false: Stimulating alpha receptors in lungs causes vasoconstriction and vasopressor effect
True
True or false: Blocking beta 1 receptors in the lungs causes increased heart rate
False. Stimulation of these receptors causes these effects
Beta 2 adrenergic drugs (increase/decrease) cAMP levels which (activates/inhibits) adenylyl cyclase and (activates/inhibits) phosphodiesterase activity
Increase, activates, inhibits
Parasympathetic receptors present in the lungs
Nicotinic and muscarinic
Stimulation of which muscarinic receptor in the airway causes bronchoconstriction and increased airway secretion
M3 receptor
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
b. epinephrine
Which of the following is a long acting, full agonist?
a. Formoterol
b. Salmeterol
c. Levalbuterol
d. Albuterol
a. Formoterol
What characteristic of albuterol makes it more selective for beta 2 receptors?
Tertiary butyl group
Levalbuterol is the (R/S) isomer of racemic albuterol
R isomer
What makes LABAs more long lasting than SABAs?
High lipophilicity due to long R chain and anchoring due to phenyl group
Which of the following is not a PDE4 inhibitor?
a. Caffeine
b. Cromolyn
c. Theobromine
d. Theophylline
b. Cromolyn
Methylxanthine MOA
Bronchodilation of smooth muscle
Drug classification and MOA of ipratropium
Anti-muscarinic agent. Blocks vagus nerve mediated acetylcholine effects on airway smooth muscle muscarinic receptors
True or false: Cromolyn is mast cell stabilizer that relaxes bronchial muscles
False. Cromolyn does NOT relax bronchial or other smooth muscles
Inhaled corticosteroid MOA
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
Leukotriene receptor antagonist MOA
Inhibits 5-lipoxygenase and inhibits binding of LTD4 to its receptor tissue
Which of the following leukotriene receptor antagonists is not commercially available in the U.S.?
a. Montelukast
b. Zileuton
c. Zafirlukast
b. Zileuton
