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Anti-Asthma Drugs Flashcards

1
Q

what do chemokine do in mast cells

A

attract inflammatory mediators to the area

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2
Q

what are the types of bronchodilators

A

beta2 adrenergic receptor agonists
theophylline
muscarinic receptor antagonists
leukotriene receptor antagonists

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3
Q

where are beta2 receptor also found apart from on smooth muscle cells

A

mucous glands in the bronchiole wall and on ciliated epithelial cells that line the lumen of the bronchioles - stimulates mucus secretion and increases the beat frequency of cilia which together increases mucucillary clearance

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4
Q

what kind of receptors are beta2 adrenergic receptors

A

G protein coupled receptors

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5
Q

what are G protein coupled receptors mediated by

A

signalling cascades that are activated downstream of aGTP binding protein (G protein)

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6
Q

what is the G protein involved in the beta2 adrenergic receptor mechanism

A

the Gs protein

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7
Q

what enzyme does the Gs protein activate

A

adenylate cyclase

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8
Q

what are the natural agonists of the beta2 receptors

A

noradrenaline released from sympathetic nerve terminals or adrenaline

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9
Q

what does the endogenous agonist binding to the receptor site cause

A

a conformational change in the receptor protein

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10
Q

what does adenylate cyclase catalyse

A

the conversion of ATP into the second messenger, cAMP

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11
Q

what does cAMP bind to

A

protein kinase A causing it to be activated

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12
Q

what does protein kinase A do

A

phosphorylates several proteins that promote the relaxation of smooth muscle

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13
Q

what is the enzyme that metabolises cAMP called

A

phosphodiesterase which hydrolyses phosphodiester bonds to generate cAMP

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14
Q

how can the activity of phosphodiester be blocked

A

drugs known as phospohodiester inhibitors, resulting in an elevation of cAMP levels and stimulation of downstream events in the pathway

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15
Q

what is an example of a phosphodiesterase inhibitor

A

theophylline

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16
Q

how does a beta2 adrenergic antagonist work

A

when the beta blocker is bound to the receptor it does not interact with the Gs protein and stimulate the signalling cascade. compete with the beta2 agonist for binding to the receptor site and when they are bound they prevent the agonist from binding and having an effect.

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17
Q

examples of SABA

A

salbutamol and terbutaline

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18
Q

how long do SABA drugs work for

A

3-5 hours

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19
Q

how often do you use SABA

A

as needed

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20
Q

examples of LABA

A

salmeterol and formoterol

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21
Q

how long do LABA work for

A

8-12 hours

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22
Q

how often are LABA given

A

twice daily

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23
Q

examples of Ultra LABA

A

vilanterol and indacaterol

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24
Q

how long to ultraLABA work for

A

around 24 hours

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25
how often are ultraALABA used for
once daily
26
what drugs can be combined with a corticosteroid
ultra LABAs
27
side effects of beta2 agonists
tremor caused by activation of the skeletal muscles rise to headaches lowers blood pressure and triggers a reflex tachycardia
28
what is aminophylline made by
combining theophylline with ethylene diamine and is more water soluble and used when the drug is given intravenously
29
what is theophylline
a phosphodiesterase inhibitor
30
what is adenosine
produced in all cells as the final product of ATP extracellular conc is highly regulated but can be increased dramatically when the energy demand of a cell increases in cases such as inflammation In the long term thought to contribute to athsma
31
where are adenosine receptors found
airway smooth muscle and they evoke bronchocontriction and on inflammatory cells including mast cells that regulate degranulation
32
what is aminophylline used to treat
status asthaticus and given by slow intravenous infusion
33
what are the unwanted effects of theophylline
tremor vasodilation cardiac stimulation GI tract stimulation
34
what do muscarinic receptor antagonists do
bind to muscarinic receptors on bronchiole smooth muscle and prevent the binding of acetylcholine and that is released from parasymthpathetic nerves
35
what is the neurotransmitter for parasympathetic neurones
acetylcholine
36
what kind of receptors are muscarinic receptors
G protein coupled receptors so agonist binding to the receptor results in the activation of a G protein
37
how do muscarinic receptor antagonists work
they bind to the receptor but also only reduce the level of bronchoconstriction as still allow some receptors to bind as normal
38
what is main muscarinic antagonist drug
ipratropium because it is hydrophilic and poorly absorbed from the airways into the systemic circulation
39
what is the side effect of ipratropium - muscarinic antagonist
dry mouth
40
how long to ipratropium last
3-5 hours and act quickly
41
where are leukotrienes derived from
part of the plasma membrane of cells
42
what are leukotrienes generated by
cytosolic enzyme
43
lipoxygenase pathway
44
mechanism of the cysteinyl leukotriene receptor anatagonists
45
what are leukotriene receptor antagonists used with
an anti-inflammatory corticosteroid
46
when are leukotriene receptor antagonists used
as an add on for uncontrolled mild-moderate asthma - additive with beta2 receptor agonists
47
what kind of asthma are leukotriene receptor antagonists more effective against
asthma induced by exercise or sensitive to aspirin
48
what are the examples of leukotriene receptor antagonist drugs and how often are they taken
montelukast - x1 daily | zafirlukast - x2 daily
49
what do glucocorticoids reduce the production of
cytokines spasmogens leukocytes chemotaxis
50
where do glucocorticoids bind to their receptor
in the cytosol
51
what is the main anti-inflammatory protein
lipocortin
52
what are the two effects of glucocorticoids
increase the transcription of anti-inflammatory proteins and reduce the transcription of pro-inflammatory proteins
53
what is the target of lipcortin
phospholipase A2 which it inhibits
54
what is the consequence of lipocortin inhibiting phospholipase A2
stops cleavage of phospholipid to generate arachidonic acid. it inhibits all of the downstream pathways that employ arachidonic acid as the precursor, including all the lipoxygenase and xcyxlo-oxygenase pathways. much more effective than leukotriene antagonists as anti-inflammatory drugs.
55
examples of glucocorticoids and when they are given
``` beclometasone - 2x daily fluticasone - 2x daily budesonide - 1x daily mometasone - 1x daily ciclesonide - 1x daily ```
56
how are glucocorticoids given
by inhaler
57
what can be given by intravenous injection to treat patients with acute exacerbations of asthma
prednisolone may be given orally and hydrocortisone by injection
58
what drugs are anti-inflammatory but weaker than glucocorticoids
cromoglicate and nedocromil
59
what are the beneficial effects of cromoglicate and nedocromil
mast cell stabilisation reduction of neuronal reflexes inhibition of cytokine release from T cells inhibition of inflammatory cells and mediators
60
who are C and N most effective in
children
61
what are the unwanted effects of C and N
mainly irritation to the upper respiratory tract | hypersensitivity reactions
62
what does omalizumab target
targets IgE
63
what does mepolizumab target
targets IL5
64
what does reslizumab target
IL5
65
what does benralizumab target
IL5 receptor
66
what is IL5
one of the cytokines released from mast cells; activates and recruits eosinophils in the Airways
67
what do mepolizumab and reslizumab do
bind to IL5 and prevent it from binding to its receptor on eosinophils
68
what is the mechanism for benralizumab
acts downstream of these drugs by binding to the IL5 receptor and preventing it from being activated by endogenous IL5
69
what asthma are IL5 activity inhibitors good at treating
severse asthma known as eosinphilic asthma
70
route and frequency of biological drugs
they are proteins and usually delivered by subcutaneous injection. drug is slowly released into circulation to reach a peak plasma concentration after a few days
71
what drugs are used in a mild asthmatic with rare attacks
inhaled beta2 agonist
72
mild asthma with more frequent attacks
glucocorticoid for prophylaxis (prevention) and beta 2 agonist when needed for acute attack
73
moderate to severe asthmatic
long acting beta 2 agonist with glucocorticoid combined inhaler
74
what does a blue inhaler contain
salbutamol
75
what does a brown inhaler include
beclometasone dipropionate. low strength steroid corticosteroid
76
theophylline mode of action
Theophylline relaxes the smooth muscle of the bronchial airways and pulmonary blood vessels and reduces airway responsiveness to histamine, methacholine, adenosine, and allergen. Theophylline competitively inhibits type III and type IV phosphodiesterase (PDE), the enzyme responsible for breaking down cyclic AMP in smooth muscle cells, possibly resulting in bronchodilation. Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction. In inflammatory states, theophylline activates histone deacetylase to prevent transcription of inflammatory genes that require the acetylation of histones for transcription to begin.

DRUGS (4 decks)

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