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Drugs > 1MB Resp > Flashcards

1MB Resp Flashcards

1
Q

Salbutamol is?

A

Short acting B2 agonist

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2
Q

How do SABAs work?

A

Bind to B2 adrenoreceptors causing a cascade which causes MLCK to stay phosphorolysed as well as MLK and Ca2+ influx is decreased.

Relaxing ASM and causing Vasodilation

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3
Q

When would you use a SABA?

A

First line in asthma

Also used in COPD

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4
Q

What is formoterol and salmetorol examples of?

A

LABAs

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5
Q

What is the mechanism of action of formoterol and salmetorol?

A

They both act the same as SABAs (by binding to B2 adrenoreceptors) however their action lasts longer. (<12hrs)

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6
Q

Montelukast and zafirlukast are examples of?

A

CysLT1 receptor antagonists, otherwise known as leukotriene receptor antagonists.

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7
Q

How does montelukast work?

A

Stop the CysLTs that have been released from inflammatory cells (e.g. eosinophils) from acting on the CysLT1 receptor (will bind onto this receptor competitively) and so prevent bronconstriction, mucus production and pulmonary oedema.

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8
Q

When would you administer a drug such as montelukast?

A

Late add on therapy in mild persistent asthma, also in rhinitis and rhinorrhoea.

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9
Q

Give an example of a xanthine.

A

Menoxanthines such as aminophylline and theophylline.

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10
Q

How do Xanthines work?

A

Theophylline activates histone deacetylase (HDAC) which may potentiate the anti-inflammatory action of glucocorticoids.

It is a competitive non-selective phosphodiesterase inhibitor, increasing cAMP which activates pKA that inhibits TNF-alpha and leukotriene synthesis.

Reducing inflammation and causing bronchodilation

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11
Q

When to use a xanthine

A

They are second line in the treatment of asthma and should be used in conjunction with a B2 adrenoreceptor and glucocorticoid.

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12
Q

Side affects of xanthines

A

Frequently causes nausea, vomiting, abdominal discomfort and headache.

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13
Q

Side affects of xanthines

A

Frequently causes nausea, vomiting, abdominal discomfort and headache.

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14
Q

The side affects of montelukast and zafirlukast

A

Sometimes report of headache and gastrointestinal symptoms.

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15
Q

Where are glucocorticoids produced?

A

Zona fasiciulata (in the adrenal cortex beneath zona glomerulosa)

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16
Q

Give examples of glucocorticoids

A

Prednisolone, Beclometasone, Budesonide, Flucticasone

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17
Q

Mechanism of action of Glucocorticoids

A

Glucocorticoids signal via nuclear receptors (class 1), specifically GR glucocorticoids increase transcription of genes encoding anti-inflammatory proteins and decrease transcription of genes encoding inflammatory proteins.

Has an anti-inflammatory action

18
Q

When to use glucocorticoids

A

Mainstay of treatment in the prophylaxis of asthma and are preferably delivered by the inhalational route to minimise adverse systemic effects.

Mainstay in rhinitis and rhinorrhoea – however unlike in asthma, it is a topical nasal spray (note these can be used in combination with anti-histamines for moderate to severe rhinitis).

19
Q

What family of drugs does sodium cromoglicate belong to?

A

Cromones

20
Q

When to use sodium cromoglicate

A

Asthma, also can be used for maintenance treatment of allergic rhinitis (intra-nasal administration) with an onset of action of 4 to 7 days, but weeks may be required for full effect – not as effective as corticosteroids

21
Q

How do cromones work

A

Are often described as ‘mast cell stabilizers’ (i.e. agents that supress histamine release from mast cells).

A decrease in the sensitivity of irritant receptors associated with sensory C-fibres that trigger exaggerated reflexes and reduction of cytokine release are potential mechanisms.

Has an anti-inflammatory effect

22
Q

Example of Anti-IgE

A

Omalizumab (requires intravenous administration)

23
Q

How does omalizumab work?

A

Monoclonal antibody directed against IgE. Binds IgE via Fc to prevent attachment to Fc receptors – suppresses mast cell response to allergens Reduces the expression of Fc receptors on various inflammatory cells

24
Q

Mepolizummab is an example of?

A

Anti-IL5

25
Q

How does mepolizumab work?

A

Monoclonal antibody directed against IL-5

26
Q

When to use an Anti-IL5

A

Recently introduced treatment for asthma associated with severe eosinophilia – very expensive

27
Q

Name Anticholinergics

A

Short acting (3-5hrs): Ipratropium, oxitropium

Long acting (<10hrs): Tiotropium

28
Q

How do anticholingerics work?

A

They inhibit cholinergic receptors (M1/2/3) in airways which when stimulated cause muscle contraction and submucosal gland activation (mucus production).

They relax ASM and decrease mucus production

29
Q

What is the similarity and difference between tiotropium and oxitopium

A

Similarity - both M3 selective Difference - tiotropium is a LAMA, oxitopium is a SAMA

30
Q

When to use a SAMA/LAMA

A

Treatment of COPD

These also work in PAR and SAR (not non-allergic) – this is due to the blocking of post-ganglionic neurones reducing mucosal secretion (in non-allergic it is increased mucosal blood flow that leads to secretions not excess mucus production).

Note, this medication for rhinitis would be topical.

31
Q

Example of PDE4

A

Rofumilast

32
Q

How does rofumilast work?

A

A selective PDE4 inhibitor,

Suppresses inflammation and emphysema

33
Q

When to use a PDE4 such as rofumilast

A

Can use in severe COPD when accompanied by chronic bronchitis

34
Q

Effects of rofumilast

A

Can have very limiting adverse effects on the GI system

35
Q

Anti-histamine examples

A

Intranasal - azelastine

Oral - Loratidine, fexofenadine, cetirizine

36
Q

How do anti-histamines work?

A

Competitive antagonists of H1 receptors reduce effects of mast cell derived histamine that include: vasodilatation and increased capillary permeability, activation of sensory nerves, mucus secretion from submucosal glands.

Inhibit vasodilation and mucus secretion

37
Q

When to use anti-histamines

A

SAR, PAR and episodic AR, but less so for non-allergic rhinitis

38
Q

Why chose an oral anti-histamine like loratidine, instead of intranasal?

A

Due to reduced sedation (do not cross the blood brain barrier) and lack of anti-cholinergic effects

39
Q

What is oxymetazoline?

A

Vasoconstrictor

40
Q

Mechanism of oxymetazoline

A

Act as direct, or indirect, sympathomimetics to mimic the effect of noradrenaline. Produce vasoconstriction via activation of 1-adrenoceptors to decrease swelling in vascular mucosa.

Causes vasocontriction

41
Q

When to use a vasoconstrictor

A

Short term in rhinitis - to reduce congestion

Drugs (3 decks)

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