PHARM: Drugs for Asthma/COPD Flashcards Preview

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Flashcards in PHARM: Drugs for Asthma/COPD Deck (56):
1

What do adrenergic agonists do? (broad)

Bronchodilator

2

List 3 non-specific adrenergic agonists.

Epinephrine (beta1, beta2, alpha)
Ephedrine (beta1, beta2, some alpha)
Isoproterenol (beta1, beta2)

3

List 2 beta-2 specific agonists with quick onset/short duration.

Albuterol
Xopenex
Terbutaline (IV)

4

List 2 beta-2 specific agonists with slow onset/long duration.

Salmeterol
Formoterol (used with steroids)

5

What do cholinergic antagonists do? (broad)

bronchodilator

6

Name 2 cholinergic antagonists.

Atropine
Ipratropium

7

What are methylxanthines?

bronchodilators with anti-inflammatory activity

8

Name 2 methylxanthines.

Aminophylline
Theophylline

9

Name 4 classes of drugs used for inflammation associated with asthma.

1) Cromolyns
2) Corticosteroids
3) Leukotriene receptor blockers
4) Leukotriene synthesis inhibitors

10

Name an example of a cromolyn.

Cromolyn sodium

11

Name some examples of corticosteroids.

Budesonide
Fluticasone
Prednisone (oral)
(ones, ides, or compined with "ols")

12

Name 2 leukotriene receptor blockers.

Monteleukast
Zafirlukast

13

Name a leukotriene synthesis inhibitor.

Zileuton

14

What is the anti-IgE antibody used for asthma/COPD treatment?

Omalizumab

15

Which class of drugs are used as "rescue medication"? How long is the duration?

selective, quick-onset beta-2 agonists with intermediate duration (3-6 hours)

16

What class of drugs are used only in combination with inhaled steroids? How long is the duration?

LABAs (long-acting beta2 agonists) that last for over 12 hours

17

List some LABA + steroid combinations.

Advair (salmeterol + fluticasone)
Symbicort (formoterol fumarate + Budesonide)

18

How do beta agonists lead to bronchodilation (help asthma)?

-Increase levels of cAMP
-Inhibit release of mediators from mast cells
-Inhibit microvascular permeability
-promote some mucociliary transport

19

How does increasing cAMP lead to bronchodilation?

Gs Pathway: cAMP activates PKA which inhibits myosin light chain kinase (along with decreased levels of calcium from activation of calcium-activated K+ channels) leading to relaxation

20

What is the "alternative signaling" pathway of beta2 agonists?

Gq pathway: Increased phospholipase C and input from beta-arrestin2 leads to increased inflammation

21

What are some adverse reactions to beta agonists?

-N/V
-Headache
-Decreased BP, Increased HR (cardiac arrhythmias)
-Decreased PaO2
-CNS effects (coma, convulsions, agitation, etc)

22

What is the MOA of antimuscarinics?

Block Ach receptors to reduce airway muscle constriction, decrease mucus secretion, and enhance beta2-mediated bronchodilation

23

What are some adverse effects of antimuscarinics?

Pupillary dilation
Cycloplegia (on contact)

24

What is interesting about ipratropium?

it is a tertiary compound (antimuscarinic) that is poorly absorbed and has no significant systemic effects

25

What is combivent?

combined anti-cholinergic and beta-2 agonist (albuterol + ipratropium bromide)

26

What is the indication for combivent?

COPD

27

Methylaxanthines are related to what chemical?

caffeine

28

What are the major actions of methylaxanthines?

-Increase levels of cAMP (bronchodilation)
-Decrease release of inflammatory mediators
-Block muscle adenosine receptors (prevent bronchoconstriction)

29

How do methylxanthines increase levels of cAMP?

they block the conversion of cAMP into AMP (breakdown)

30

The adverse effects of methylxanthines depend on what?

the serum levels

31

What adverse reactions occur with 5-10 microgram/mL serum levels of methylxanthines?

N/V
Nervousness
Headache
Insomnia

32

What adverse reactions occur with over 20 microgram/mL serum levels of methylxanthines?

Vomiting
Hypokalemia
Hyperglycemia
Tachycardia
Tremor
Seizures

33

Cromolyns may alter the activity of what type of channels?

chloride channels

34

What are the 4 major actions of cromolyns?

-Inhibit mast cell degranulation
-Inhibit inflammatory response (act on eosinophils)
-Inhibit cough (act on airway nerves)
-Reduce bronchial hyperactivity

35

What is a reason people may not be adherent to cromolyns?

they taste bad

36

List some adverse reactions to cromolyns.

COUGH and bronchospasm after inhalation (irritation of trachea)
Chest pain (rare)
Restlessness (rare)
Hypotension (rare)
N/V (rare)

37

List 4 actions of glutocorticoids.

1) Decrease production of inflammatory cytokines
2) Reduce mucus secretions
3) Reduce bronchial hyperactivity
4) Enhance effect of Beta-2 agonists (by increasing transcription of the receptors)

38

Which syndrome can result from use of glucocorticoids? List some symptoms.

Cushingoid Syndrome
-Weight gain (abdomen, buffalo hump, moon face)
-Thinning and leg/arm muscle weakness
-Thin skin
-Increased acne, facial hair growth, scalp hair loss in women
-Ruddy complexion
-Acanthosis (neck skin darkening)
-Child obesity and poor growth
-High BP

39

What is the role of LTB4?

neutrophil chemoattractant

40

Which leukotrienes mimic asthma symptoms (bronchial hyper-reactivity and constriction, mucosal edema, increased mucus secretion)?

LTC4
LTD4

41

What leukotriene receptor do Zafirlukast and Monteleukast block?

LTD4 receptors

42

Leukotriene receptor blockers are "effective in some patients" of what subtype of asthma?

aspirin-induced asthma

43

What are some adverse effects associated with zafirlukast?

GI problems
headache
elevation of liver enzymes (liver and bladder cancer in rodents)

44

What are some adverse effects associated with monteleukast?

GI problems
laryngitis/pharyngitis
nausea
otitis/sinusitis
viral infections increased
possible suicidal ideation*

45

What is the effect that leukotriene synthesis blockers have in asthma patients?

-Decrease smooth muscle contraction
-Decrease blood vessel permeability/leukocyte migration to damaged area

46

Which CYP is inhibited by (and a substrate for) Zileuton?

CYP1A2 (interacts with theophylline!)

47

What must be checked when on Zileuton?

LFTs are required, because it causes hepatic enzyme elevation

48

Use of Zileuton could be connected to what sort of conditions?

inflammation-related conditions like RA and acne

49

Omalizumab is used for what?

-Reduce severity/frequency of asthma attacks by decreasing the allergic response to triggers
-Reduce requirement for inhaled corticosteroids

50

What are some adverse effects of omalizumab?

-Serious allergic RXN
-Redness, warmth, itching, bruising in injection site
-Sore throat/cold symptoms
-Increase CV complications

51

How does the treatment approach differ for asthma and COPD?

corticosteroids do not help and bronchodilators are only partially helpful

52

What are the 3 main-lines of treatment for COPD?

1) Smoking cessation
2) Bronchodilators
3) Antimuscarinics

53

What 5 drug classes are contraindicated in airway diseases?

1) Sedatives
2) Beta-blockers
3) Aspirin
4) ACE Inhibitors
5) Local anesthetics with EPI

54

What is doxapram?

a short-acting respiratory stimulant given IV

55

What is the MOA of doxapram?

activates peripheral carotid receptors to increase respirations to treat acute hypercapnia in COPD or post-anesthesia respiratory depression

56

What is the "best" glucocorticoid? Why?

Ciclesonide
-High lipophilicity
-Rapidly cleared from mouth
-Good binding to receptor
-Good brinding to protein