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Therapeutics Spring 2015 > Asthma/COPD drugs > Flashcards

Asthma/COPD drugs Flashcards

1
Q

Albuterol

A

Ventolin

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2
Q

What class of drug is Abuterol?

A

Beta-2 Adrenergic Agonist

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3
Q

By what pathway does albuterol cause bronchodialation?

A

Stimulates Gs and Adenyl Cyclase –> increase cAMP–>activated PKA—>which phosphorylates myosin LC kinase causing bronchodialation

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4
Q

Terbutaline

A

Brethine

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5
Q

What class of drug is terbutaline?

A

Beta-2 adrenergic agonist

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6
Q

What is the rate of onset of albuterol?

A

inhalation–> 5 min

oral –> 30 min

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7
Q

What is the duration of albuterol?

A

inhalation –> 3-4 hours

oral –> 3-8 hours

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8
Q

What is the rate of onset of terbutaline?

A

inhalation –> 5 min

oral –> 30 min

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9
Q

What is the duration of action of terbutaline?

A

Inhalation –> 3-6 hours

oral –> 3-8 hours

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10
Q

Salmeterol

A

Severent

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11
Q

what class of drugs does salmeterol belong too?

A

Beta-2 adrenergic agonists

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12
Q

what is the rate of onset of salmeterol?

A

inhalation–> > 20 min

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13
Q

What is the duration of action of salmeterol?

A

12 hours

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14
Q

Formoterol

A

foradil, brovana

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15
Q

What class does formoterol belong too?

A

Beta-2 adrenergic agonists

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16
Q

What is the rate of onset of formoterol?

A

<10 min

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17
Q

What is the duration of action of formoterol?

A

> 12 hours

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18
Q

Which B2 agonists are only for use in combination with glucocorticoids?

A

Salmeterol and formoterol

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19
Q

What are ADE associated with B2 adrenergic agonists?

A
  • Skeletal muscle tremors
  • Tachycardia & palpitations
    ( less with B2 selective agents)
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20
Q

by what mechanism does B2 adrenergic agonists cause tachycardia and palpitations?

A

High doses can stimulate B1 receptors in the heart

Reflex tachycardia from baroreceptors (caused by drop in BP due to vaso/bronchodialation)

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21
Q

True or False?

Salmeterol and formoterol are contraindicated as monotherapy?

A

True

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22
Q

LABAs

A

Salmeterol/formoterol

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23
Q

SABAs

A

Albuterol/terbutaline

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24
Q

What is the mechanism of glucocorticoids?

A

Decrease protein synthesis

  • causes decreased esinophils/macrophages/mast cells
  • decreased prostaglandin/leukotryine syntheses
  • decreased hyperresponsiveness of bronchiole smooth muscle
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25
How are inhaled glucocortocoids dosed?
One inhalation in the morning
26
What type of infection does glucocorticoid use perpetuate?
Fungal thrush infections
27
What class of drugs does Advair belong too?
Glucocorticoid Combo - inhaled steroid + LABA
28
Advair
Fluticasone + salmeterol combo
29
What are the doses of advair?
100,250,500 ug of fluticasone | 50 ug salmeterol
30
Symbicort
budesonide + formoterol
31
Dulera
mometasone + formoterol
32
What are 3 examples of methylxanthines?
caffeine theophylline theobromine
33
What is the mechanism of theophylline?
1. PDE4 inhibitor - increases cAMP -->PKA-->MLCK-PO4--> relaxation\ 2. Blocks Adenosine receptor - antagonizes bronchoconstriction
34
What is the therapeutic range pf theophylline?
10-15 ug/mL
35
What are some ADE/toxicities of theophylline?
N/V, nervousness, abdominal discomfort at 20 ug/mL Cardiac arrhythmias, hypotension, CNS stimulation > 25 Seizures/ Cardiac arrest --> 40-100 ug/mL
36
What is a caution of theophylline?
can aggravate pre-existing seizure disorders
37
What antacids will delay theophylline absorption?
magnesium/Al containing antacids
38
What condition increases the half life of theophylline?
CHF
39
What agents increase theophylline blood levels by competing for CYP450?
``` Cimetidine Allopurinol erythromycin fluoroquinolones (cipro) propranolol leukotryine inhibitors ```
40
What class of drugs does Cromolyn sodium belong too?
Mast cell degranulation inhibitors
41
What class of drugs does nedocromil sodium belong too?
Mast cell degranulation inhibitors
42
What dosage forms do mast cell degranulation inhibitors come in?
Adults-- metered dose inhaler | children- 1% aerosol solution
43
Omalizumab
Xolair
44
What dosage form does Xolair come in?
SC injection
45
Why does Xolair only come in injectable?
It is a humanized mouse anti-human IgE antibody
46
How does Xolair work?
It inhibits the binding of IgE antibodies to the FcER1 receptors on mast cells and basophils.
47
What is an ADE of Xolair?
Anaphylaxis Injection site rxns Increased incidence of infection immunogenicity
48
Zileuton
Zyflo
49
What class of drugs does Zileuton belong too?
leukotryine inhibtors
50
What is the mechanism of action of Zileuton?
5- lipoxygenase inhibitors
51
What is the role of 5 - lipoxygenase inhibitors?
It converts arachidonic acid to 5HPETE during the formation of the leukotryines
52
Can you use Zyflo for an acute attack?
No
53
What are ADE of Zyflo?
``` Doubles blood levels of theophylline Increases PT time of warfarin Headache Dyspepsia Some incidence of liver toxicity ```
54
Zafirlukast
Accolate
55
Montelukast sodium
Singulair
56
What class of drugs do Zafirlukast belong too?
Leukotryine inhibitors
57
What class of drugs do montelukast belong too?
Leukotryine inhibitors
58
How do montelukast and zafirlukast work?
Selective competitive inhibitor of CysLT-1 receptor
59
What is the role of CysLT-1 receptor?
It inhibits the PLC-->IP3--> Ca--> myosin--> contraction pathway
60
Can Zafirlukast and montelukast be used in children?
Yes
61
How are CysLT-1 antagonists metabolized?
The liver
62
Can Zafirlukast and montelukast be taken with food?
No, food reduces bioavailability and broken down by bile acids
63
Can Zafirlukast and montelukast be used in an acute attack?
No, but can be used with B2 agonists
64
Ipratropium
Altrovert
65
Tiotropium
Spiriva
66
what class of drugs do ipratropium and tiotropium belong too?
muscarinic antagonists (anticholenergics)
67
What is the dose regimen of ipratropium?
inhaled QID
68
what is the dose regimen of tiotropium?
Inhaled QD
69
is PRN dosing used for inhaled muscarinic agonists?
PRN is not used in quaternary ammonium compounds
70
Indacaterol
Arcapta
71
What is indacaterol used for?
COPD only
72
What are formoterol and salmeterol used for?
Asthma and COPD
73
What is the dose of indacaterol?
75 ug once daily
74
Is monotherapy with LABAs containdicated in COPD?
No, inflammatory damage already done.
75
What is the role of Alpha-1 anti-trypsin in COPD?
normally produced to inhibit proteases (like elastase)
76
What class of drugs does prolastin belong too?
Alpha-1 anti-trypsin replacement
77
What class of drugs does aralast belong too?
Alpha-1 anti-trypsin replacement
78
what class of drugs does zemaira belong too?
Alpha-1 anti-trypsin replacement
79
How are Alpha-1 anti-trypsin replacement drugs dosed?
IV 1x/week
80
What class of drugs does Ivacaftor belong too?
CFTR regulator
81
Ivacaftor
Kalydeco
82
How does ivacaftor work?
it holds CFTR in a favorable conformation for Cl- to flow through in response to cAMP
83
How is ivacaftor dosed?
orally BID
84
What class of drugs do Dornase alfa belong too?
Mucolytics for tx of CF
85
N-acetylcysteine
Mucomyst
86
What class of drugs does mucomyst belong too?
Mucolytics
87
What function does hypertonic saline have in CF?
mucolytics
88
what are 3 classes of drugs for CF?
Mucolytics Bronchodialators Antibiotics
89
What are 2 gram (-) antibiotics used in CF?
tobramycin | azithromycin
90
What kind of drug is Ataluren?
small molecule to suppress premature stop codons in CF (nonsense mutations) Not approved yet
91
VX-809 is what kind of drug?
small molecule chaperone for deltaF508 CFTR | prevents the deletion of phenylananine codon
92
what kind of drug is Bronchitol?
Inhaled mannitol solution- rehydrates the mucus

Therapeutics Spring 2015 (12 decks)

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