Pharm - Asthma Drugs

Question 1

Parasympathetic nerves control what 2 structures in lungs?

Answer 1

Bronchial smooth muscle, mucosal glands

Question 2

Mucosal cells have what type of muscarinic receptors?

Answer 2

M1, M3

Question 3

Bronchial SM has what type of muscarinic receptors?

Answer 3

M2, M3

Question 4

Besides bronchial SM, where else can M2 receptors be found? What is their purpose here?

Answer 4

M2 receptors can be found at pre ganglionic nerve terminal, inhibit release of Ach into synapse of neuromuscular junction

Question 5

Besides muscarinic receptor at parasympathetic pre ganglionic nerve terminal, what other receptor is present? What is released from it?

Answer 5

Nicotinic receptors, release Ach

Question 6

The only receptor (if you block it) at presynaptic ganglion terminal that blocks ganglionic signal (blocks the release of Ach from the nerve terminal) is?

Answer 6

nicotinic receptor

Question 7

In asthma exacerbation, what neurotransmitter is released via post ganglionic parasympathetic nerves, worsening the asthma?

Answer 7

Ach released into NMJ, worsening bronchoconstriction

Question 8

In asthma, what does the accumulation of eosinophils at the parasympathetic post ganglionic synapse cause?

Answer 8

Eosinophil accumulation will inhibit M2 receptors at NMJ, allowing Ach to be released, worsening the asthma exacerbation

Question 9

Sympathetic innervation of lung primarily along what? What receptors here?

Answer 9

blood vessels, alpha 1,2, beta2

Question 10

Adrenergic receptor density highest in what part of lungs?

Answer 10

bronchioles

Question 11

Muscarinic receptor density highest in what part of lungs?

Answer 11

Trachea, upper airways

Question 12

Which is more effects, B2 agonists or muscarinic antagonists? Why

Answer 12

B2 agonists, because of location of B2 receptors. They are in the bronchioles vs muscarinic receptors being in the trachea and upper airways.

Question 13

Norepi stimulates what receptors?

Answer 13

alpha 1, alpha 2, beta 1

Question 14

Beta 2 receptors can only be stimulated by what adrenergic neurotransmitter?

Answer 14

Epinephrine. not norepi

Question 15

Nonspecific beta agonists?

Answer 15

• Epinephrine
• Ephedrine
• Isoproterenol

Question 16

B2 specific, quick onset-short acting drugs?

Answer 16

• Albuterol
• Xopenex (Levalbuterol)
• Terbutaline

Question 17

B2 specific, slow onset- long acting drugs?

Answer 17

• Salmeterol
• Salmeterol + Fluticasone (Advair)
• Formoterol
• Formoterol + Budesonide (Symbicort)
• Formoterol +Mometasone

Question 18

Sympathomimetics relation with cAMP?

Answer 18

B2 agonists increase rate of cAMP synthesis, which causes bronchodilation

Question 19

B2 agonists increase cAMP levels via what mechanism

Answer 19

stimulate adenylyl cyclase to increase production of cAMP

Question 20

MOA of Theophylline

Answer 20

B2 agonist. PDE-inhibitor, prevents breakdown of cAMP to AMP, allowing increased cAMP levels = bronchodilation

Question 21

Adenosine and Acetylcholine on bronchial tone?

Answer 21

bronchoconstriction

Question 22

Major adverse effect of beta agonists?

Answer 22

hypokalemia- QT prolongation = fatal arrhythmias (be careful with drugs causing hypokalemia like Loop/Thiazide Diuretics)

Question 23

Antimuscarinic drugs?

Answer 23

Atropine
Ipratropium
Tiotropium
Umeclidinium

Question 24

MOA of antimuscarinics?

Answer 24

Compete with acetylcholine for muscarinic receptor binding

Question 25

Adverse effect of antimuscarinics?

Answer 25

Contact with medication and touching eye can cause pupillary dilation and cycloplegia

Question 26

What is the mechanism of Cromolyn?

Answer 26

Inhibit mast cell degranulation, inhibit the inflammatory response, reduces bronchial hyperactivity

Question 27

Mechanism of action of Glucocorticoids?

Answer 27

combines with GRa in the cytosol–> inhibits NF-kB–>inhibits transcription of inflammatory genes

Question 28

What effect do glucocorticoids have on Th2 cells?

Answer 28

Competes with GATA-3 for translocation to the nucleus to prevent transcription of IL-4, IL-5, and IL-13

Question 29

ADE of glucocorticoids?

Answer 29

oral candidiasis, decreased bone density in premenopausal women, decreased growth rate of children, glucose intolerance, increase blood pressure/weight, immunosuppresion

Question 30

What is Lipocortin? What is the effect of glucocorticoids on it?

Answer 30

It suppresses phospholipase a2, glucocorticoids up regulate transcription of Lipocortin–> decrease inflammation

Question 31

What is Cushingoid Syndrome?

Answer 31

Cushing like syndrome seen in chronic glucocorticoid therapy, especially in children; Weight gain, moon face, buffalo hump, acanthosis

Question 32

Which has more of a role in acute bronchoconstriction, Leukotrienes of histamine?

Answer 32

Leukotrienes are 1000x more potent

Question 33

What are the 2 LTD4 receptor antagonists?

Answer 33

Zafirlukast and Monteleukast

Question 34

What kind of asthma CAN leukotriene modifiers be fairly effective in?

Answer 34

ASA induced asthma

Question 35

Name the Leukotriene synthesis blocker

Answer 35

Zileuton

Question 36

What does Zileuton do?

Answer 36

Inhibit syntehsis of LTB4, C4, D4, E4; Decreases smooth muscle contraction and blood vessel permeability, reduced leukocyte migration to the affected area

Question 37

Main ADE of Zileuton?

Answer 37

Causes elevation of hepatic enzymes–> Check LFTs

Question 38

What is the IgE monoclonal antibody?

Answer 38

Omalizumab

Question 39

Efficacy of Bupropion in treatment of COPD?

Answer 39

Anti-depressant that helps to block nicotinic receptors

Question 40

Possible role of Theophylline in COPD therapy?

Answer 40

Theophylline recruits histone deacetylase II–> inhibits transcription of inflammatory genes–> less damage to lung parenchyma

Question 41

Beta agonists effective in early, late, or both phases of an asthma attack?

Answer 41

Early phase (bronchoconstriction); don’t really play a role in the late phase (inflammatory)