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4 Pharma > Asthma & COPD > Flashcards

Asthma & COPD Flashcards

1
Q

Compared to epinephrine, this sympathomimetic drug has longer duration, less potency, and more pronounced central effects.

A

ephedrine

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2
Q

This sympathomimetic is valued in anaphylactic patients with acute vasodilation, shock, and bronchospam

A

epinephrine

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3
Q

LABAs have this structural property

A

longer side chain

can interact with multiple receptor sites

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4
Q

B2 agonist available as SC injection

A

terbutaline

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5
Q

LABAs:

A

salmeterol, formoterol

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6
Q

B2 agonists available in tablet form

A

albuteral/salbutamol, terbutaline

2-3x daily

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7
Q

Full LABA?

A

formoterol

F=Full

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8
Q

Partial LABA?

A

salmeterol

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9
Q

LABA are not recommended for monotherapy for asthma because:

A

They lack anti-inflammatory properties.

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10
Q

Ultra LABA

A

indacaterol

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11
Q

R-isomer of B2 agonists do what?

S-isomer?

A 
R-isomer = activate receptor
S-isomer = promotes inflammation
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12
Q

B2 selectives inhibit production of ____ (it decreases cAMP level) which was shown to be elevated in asthmatic subjects and patients with other inflammatory lung disorders

A

endothelin-1

inhibiting ET-1 therefore increases cAMP levels

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13
Q

How do B2 selectives INCREASE expression of glucocorticoid receptors?

A

Inc. cAMP –> activate PKa –> activate CREB –> DNA-level transcription

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14
Q

B2 receptor polymorphism associated with increased agonist-mediated responsiveness and less reactive airways.

A

Glu27

Less reactive asthma

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15
Q

B2 receptor polymorphism associated with enhanced agonist-mediated DESENSITIZATION

A

Arg16

Increased asthma severity, reduced response to bronchodilators

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16
Q

B2 receptor polymorphism associated with increased airway hyperreactivity, NOCTURNAL symptoms and more severe asthma

A

Gly16

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17
Q

R isomer of albuterol that is more active and produces greater bronchodilation over a longer period of time

A

levalbuterol

more affinity
higher profile of metabolism
does not contract airway smooth muscle

Remember that S isomers PROMOTE inflammation. However, lack of evidence as far as efficacy and patient outcomes.

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18
Q

Combination of active groups of salbutamol/albuterol with theophyline

A

reproterol

salbutamol increases cAMP
theophylline decreases cAMP breakdown by inhibiting PDE

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19
Q

B2 agonist that interacts with a receptor-specific auxiliary binding site

A

salmeterol

20
Q

B2 agonist with direct activation of receptor

A

albuterol

21
Q

B2 agonist taken up into a membrane depot to activate receptor

A

formoterol

22
Q

B2 agonists increase effects of (drug interaction)

A

TCA
MAOi
sympathomimetics

23
Q

In severely ill patients on B2 agonists, what must be monitored in order to prevent respiratory paralysis

A

hypokalemia

24
Q

First line drug for COPD

A

ipratropium

25
Q

MoA of ipratropium

A

blocks ACh in bronchial smooth muscle

inhibits stimulation of M1, M2, M3 –> decreased secretion, increased bronchodilation

26
Q

Anti-musc with subtype-selectivity M3, M1 > M2

A

tiotropium

27
Q

Anti-musc with less frequent adverse effects

A

tiotropium

28
Q

Anti-musc that can cause dyspepsia, vomiting, GERD

A

tiotropium

29
Q

Non-selective PDE inhibitor used for asthma

A

theophylline

30
Q

theophylline MoA

A

blocks PDE –> inc. cAMP (i.e., decreasing cAMP hydrolysis) –> ++ Ca influx –> epi release –> bronchodilation and anti-inflammation

Adenosine receptor blockage –> blocks Gq coupled receptor that causes bronchoconstriction

Basically: blocks PDE and adenosine

31
Q

Common theophylline ADR at 2-35 mcg/L

A

tachycardia

32
Q

Common theophylline ADR at >35

A

seizure

33
Q

theophylline is metabolized by

A

CYP450

34
Q

theophylline decreases levels of these drugs (via induction)

A 
barbiturates
carbamazepine
charcoal
rifampicin
ketoconazole
sympathomimetics
35
Q

theophyilline increases levels of these drugs

A 
allopurinol
B blockers
CCB
ciprofloxacin
INH
macrolides
36
Q

Theophylline’s effect on cor pulmonale

A

increases

37
Q

These drugs inhibit (virtually all) cytokine synthesis, inactivate NF-KB (a transcription factor that induces production of TNF-a), other inflammatory agents

A

corticosteroids

beclomethasone
prednisone
fluticasone

38
Q

Prodrug activated by cleavage of esterases in bronchial epithelial cells. Less unwanted effects and no interaction with skin, eye, bone (tightly bound to serum proteins)

A

ciclesonide

39
Q

How does cAMP prevent smooth muscle contraction

A

PKA phosphorylates myosin light chain kinase MLCK (inactivating) –> no contraction

40
Q

5-LOX pathway inhibitor

A

zileuton

blocks conversion of arachidonic acid to LTs

For prevention not reversal. Liver toxicity.

41
Q

Blocks leukotriene receptor. Less effective than ICS.

A

montelukast

also zafirlukast

42
Q

Widely used in aspirin-induced asthma

A

montelukast

43
Q

Prevents degranulation of MAST CELLS

A

cromolyn

Prevention not reversal.

44
Q

Cromolyn is more useful in the prevention of what?

A

allergic asthma

45
Q

Inhibits the binding of IgE to high-affinity IgE receptor on mast cells, basophils, dendritic cells

A

omalizunab

46
Q

B2 agonist + Inhaled CS combinations: (3 of them)

A

salmeterol + fluticasone

formoterol + budesonide

salbutamol + beclomethasone

47
Q

Gold standard of asthma gadgets

A

MDI

4 Pharma (7 decks)

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