08.14 - ANS and Bronchial Tone (Sweatman) - Questions Flashcards

1
Q

Clinically, both ___ agonists and ___ antagonists are used to control bronchospasm

A

B2 agonists, Muscarinic Antagonists

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2
Q

Adrenergic receptors in the lung are found in

A

Airway SM, Epithelial Cells, Mast Cells, Type 2 alveolar cells

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3
Q

T/F: The SNS has no direct neural connection to bronchial SM

A

TRUE

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4
Q

How does SNS modulate bronchial SM tone

A

Modulate PNS, via hetero-receptors

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5
Q

Permeability advantages of lung drug delivery

A

More permeable to macromolecules than other; Most permeable to small molecules than GI tract

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6
Q

The less ionized a molecule, the __ it’s absorption rate

A

Faster - Fewer interactions with proteins and lipids that line the pore

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7
Q

What type of compounds can “dissove” in the lipid bilayer and rapidly be absorbed transcellular

A

Lipophilic

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8
Q

How do insoluble compounds traverse lung epithelium

A

Paracellular - Aqueous pores in intercellular tight junctions

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9
Q

What determes rate at which molecules pass through lung epithelium

A

MW and Degree of Ionization, and Lipophilicity

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10
Q

How does ionization affect absoprtion rate

A

Less ionized is absorbed more rapidly

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11
Q

Blockade of M2 Auto-receptors ___

A

increases release of endogenous ACh

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12
Q

Paradoxical actions of Atropine, Ipratropium

A

Decr bronchial SM tone via M3 blockade; But blocking M2 auto-recetpors actually increases release of enodgenous ACh –> bronchial SM contraction

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13
Q

M1 Receptor Locations

A

PG membrane; Nasal mucosa

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14
Q

Locations of M2 receptors

A

Inhibitory autoreceptors on pre-synaptic membrane of PG fibers; Bronchial SM

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15
Q

Selectivity of Atropine, Ipratopium

A

Non-selective: M2 and M3

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16
Q

Selectivity of Tiotropium

A

Functional selectivity for M1 and M3 receptors

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17
Q

Tiotropium

A

Functional selectivity for M1 and M3 receptors

18
Q

Most pervasive group with anticholinergic “side effects”

A

1st generation antihistamines

19
Q

Effect of Anticholinergics on secretions

A

Dry secretions

20
Q

Effect of Acetylcholinesterase inhibitors on secretions

A

Increase

21
Q

Which phase of atopic asthmatic response is Albuterol effective in?

A

Early (bronchospastic), not Late (Inflammatory)

22
Q

How might B2 agonists produce bronchoconstriction

A

Increasing PNS Tone

23
Q

Goblet Cells and Submucosal Glands receive primarily __ innervation

A

PNS

24
Q

Beta agonist effect on mucociliary clearance

A

Increase glycoportein composition; Incr cilia beat freq -> incr clearance

25
Q

Beta agonist effect on Vascular Endothelial Permeability

A

Decr microvascular leakage, Decr airways obstruction in asthma

26
Q

At high concentrations, B2 agonists produce (2):

A

CV stimulatory effects; QT prolongation (esp in hypoK)

27
Q

How does B2 agonism affect QT prolongation

A

Stimulation of Na/K pump decr serum K –> Hypokalemia –> Worsening QT prolongation

28
Q

Patients with whtat type of problems should be cautions with B2-agonists

A

Cardiovascular

29
Q

3 drug classes that also promote hypokalemia

A

Saquinavir; Loop and Thiazide Diuretics; Non-specific Beta Blockers

30
Q

Why should asthmatics not take beta-blockers

A

Can’t treat with B2 Agonists

31
Q

Beta-agonists activate G-proteins, which stimulate __

A

Adenylyl Cyclase

32
Q

Beta-Arrestin

A

Binds to phosphorylated domain on B-adrenergic receptor and blocks Gs binding -> Thereby decr AC activity; Endosomal localization

33
Q

M1 is coupled to what g protein

A

Gq

34
Q

M3 is coupled to what g protein

A

Gq

35
Q

M2 is coupled to what g protein

A

Inhibitory action via Gi/o

36
Q

Beta2 agonists activate what g protein

A

Gs

37
Q

Repeated stimulation of beta adrenergic receptor results in

A

Phosphorylation –> Beta-arrestin –> internalization

38
Q

Corticosteroid effect on b2 receptors

A

Transcriptional upregulation of beta-2 receptors

39
Q

4 off-target Beta2 actions

A

Cardiostimulation, Muscle Fasciculation, Hypokalemia (QT prolongation)

40
Q

B2agonist activity is exacerbated by

A

Metabolism inhibitors

41
Q

How can you restore beta 2 receptor density

A

Corticosteroid transcriptional upregulation