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PHRM 211 > Lecture 5 > Flashcards

Lecture 5 Flashcards

1
Q

Obstruction of airway flow in asthma is due to 3 things

A

airway inflammation
bronchial hyperresponsiveness
smooth muscle constriction

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2
Q

Asthma is

A

chronic long term inflammatory condition affecting the upper airways in the lungs

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3
Q

asthma is characterized by

A

reversible bronchoconstriction and SOB

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4
Q

COPD is

A

a chronic progressive respiratory disease

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5
Q

COPD causes

A

irreversible restricted airflow and breathing problems

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6
Q

restricted airflow is due to

A

destruction of parts of the lung including alveoli.
mucus blocking the airways
inflammation and swelling of the airway lining.

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7
Q

is COPD curable?

A

Not curable, but can be managed by medications.

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8
Q

benefits of inhaled drug deposition

A
  • effective use of smaller dose
  • lower incidence of unwanted systemic effects
  • rapid onset of action
  • controlled delivery
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9
Q

Name two common short acting beta agonists

A

salbutamol and terbutaline

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10
Q

name two common LABA

A

sameterol, formoterol

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11
Q

MOA of B2 agonists

A
  1. B2 agonists bind and stabilize the receptor in the activated stage.
  2. activates adenylate cyclase, increases generation of cAMP from ATP
  3. cAMP inhibits Ca, hyperpolarizes smooth muscle cells = bronchodilation
  4. cAMP also activates protein kinase A, incrasing protein phosphorylation, regulates smooth muscle tone, = bronchodilation
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12
Q

what happens with frequent use of B2 agonists

A
  1. enhance inflammatory pathways, downregulation of B2receptors and tolerance to bronchodilator effects
  2. receptors desensitize rapidly, so B2 agonists do not reduce airway inflammation.
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13
Q

SABA onset of action

A

5 minutes

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14
Q

SABA peak effect (max bronchodilation)

A

15-30 minutes

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15
Q

how long do SABA bronchodilation effect last until

A

2-6 hours

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16
Q

How are SABAs administered

A

Inhalation, salbutamol sometimes given with IV infusion.

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17
Q

When should SABAs be used and why

A

intermittently or as needed

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18
Q

LABA duration of action

A

up to 12 hours, more lipophilic than SABAs and bind to the lipid of the smooth muscle cell membrane.

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19
Q

Which LABA has slower onset compared to others

A

salmeterol

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20
Q

low efficacy agonist LABA

A

salmeterol (60% partial agonist activity)

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21
Q

high efficacy agonists LABA

A

formoterol and Indacaterol - full agonist activity

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22
Q

should LABAs be used alone in asthma

A

NO! should be used as an add on to ICS to control persistent symptoms in adults. It reduces the risk of exacerbations compared to ICS alone

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23
Q

should LABAs be used alone in COPD

A

Can be used alone or in combo with CIS or LAMA

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24
Q

what do LABAs do alone in COPD

A

improve symptoms and exercise tolerance by reducing both air trapping and exacerbations.

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25
ADRs of B2 agonists
muscle tremors, restlessness, headache, arrythmias and tachycardia. Hypokalemia in high doses
26
LABAS AND SABAS should be used with
Inhaled Corticosteroids for anti-inflammatory therapy
27
2 steps of Glucocorticoid receptors
1. bind GS and GR undergoes confirmational change, ebcomes activates and dissociates from multi-protein complexes 2. GR transolcates into the nucleus and regulates gene expression.
28
Which enzyme moves a gene to the active stage
histone acetyltransferases
29
which enzyme silences the genes
histone deacetylases
30
what genes do GCS turn on/off
Switch ON anti-inflammatory gene expression Switch OFF inflammatory gene expression
31
Do CS have any benefit in the initial stages
NO, not in an acute attack bc they are NOT bronchodilators just anti-inflammatory agents.
32
what do CS enable in asthma
less frequent use of bronchodilators
33
List 4 common systemic corticosteroids
prednisone, prednisolone, methylprednisolone, hydrocortisone
34
Name 6 inhaled corticosteroids
Beclomethasone, budenoside ciclesonide, fluticasone, mometasone, triamcinolone
35
When should ICS be used for asthma
drug of choice for regular controller therapy, should be used regularly
36
side effects local of ICS
hoarseness (dysphonia) caused by drug deposition on vocal cords throat irritation coughing thrush
37
ICS prolonged use SE
increased pneumonia risk cataracs HPA axis supression osteoporosis growth restriction skin thinning/bruising
38
benefits of LABA ICS therapy
adding a laba to an ICS is more effective than doubling ICS dose which also limits risk of side effects.
39
what does the M3 receptor in the airways do
bronchoconstriction, increased bronchial secretions
40
name a SAMA
ipratropium
41
name a LAMA
Tiotroprium
42
SAMA onset of action, peak, duration of action
15 mins, peak at 1-2 hours, duration of action 5-6 hours
43
Ipratropium SE
metallic/bitter taste when inhaled
44
LAMA MOA
functionally selective for M3 receptors due to faster disassociation from M2
45
Onset, peak, duration of action
30 mins, 3-4 hours, 24 hours
46
what is the dosing of a LAMA
once daily dosing
47
SE LAMA
dry mouth, tachycardia, urinary retentoin
48
why is tiotropium better than ipratropium?
more specific, longer duration of efficacy
49
are antimuscarinics more or less effective as bronchodilators than b2 agonists
less
50
role of antimuscarinics in COPD
release of ACh causes vagally-mediated bronchospasm, major reversible component of COPD
51
LABA + LAMA combo therapy
additive bronchodilator effect, not synergistic
52
PDE's roles
hydrolyze cAMP and cGMP, hence they deactivate their cAMP/cGMP mediated effects
53
which PDE is important for anti-inflammatory stuff
PDE 4
54
methylxanthines are ?
PDE inhibitors
55
Methylxanthines act to relax airways by
inhibit PDEs Antagonize Adenosine receptors activation of histone deacetylases
56
how do methylxanthines work on adenosine recepors
adenosine causes bronchocontriction and inflammation. Methylxanthines inhibit the receptors thus causing bronchodilation and anti-inflammatory effects
57
name two methylxanthines
theophylline and aminophylline
58
PDE4 inhibitor
roflumilast
59
Indication of Roflumilast
Patients with COPD with chronic bronchitis , with frequent exacerbations
60
can roflumilast be used alone
NO! only has anti-inflammatory effects, doenst work for relief of acute symptoms.
61
what is Roflumilast CI in
patients taking theophylline because it reduces roflumilast clearance
62
Leukotrienes are a family of ______
inflammatory lipid mediators
63
leukotrienes cause
narrowing and swelling of the airways in the lungs
64
name two leukotriene receptor antagonists
Montelukast and Zafirlukast
65

PHRM 211 (25 decks)

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