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Respiratory Medicine > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What are the 3 main category of drugs used in asthma and COPD and what are their subcategories?

A
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2
Q

What are the advantages and disadvantages of inhalation administeration of drugs?

A

Direct effect on airways , particulary for Asthma and COPD

The major advvantage is that the doses are much more effective with a decrease risk of systemic side effects

Bronchodilators also have rapid onset when administered orally

Can be used in combination with other drugs to have synergistic effects (LABA and ICS)

Disadvantages are that a mucus plug or airway obstruction could block adminsteration

If in an intense asthma attack may be hard for someone to hold their breath

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3
Q

What are the advantages and disadvantages of oral route administeration of drugs?

A

Can be used if there is airway obstruction or patient is in servere asthma and cannot function properly enough to coordinate inhalation

Disad: dose much higher than the inhaled dose requuired to achieve same effect as inhalation.

There are also increase systemic side effects

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4
Q

What are the 3 types of bronchodilators?

A

B2 adrenergic agonists

Anticholinergic agents

Methylxanthines

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5
Q

What is the mechanism of action for B2 adrenergic agonists?

A

Action of B2 receptor Gs-adenylyl cyclase –> increases cAMP-PKA pathway which leads to relaxation via phosphorylative events

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6
Q

What are the 4 effects of B2 adrenergic agonists?

A

Prevents mediator release from mast cells

prevents microvascular leakage and thus decreases development of oedema

Enhances mucocillary clearance

Reduces neutrotransmission (inhibits ACh release)

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7
Q

What are the 2 types of B2 adrenergic agonists you can have?

A

SABA and LABA

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8
Q

Which bronchodilator is specifically best for treating acute severe asthma?

A

SABA

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9
Q

Why must SABA’s be used in moderation?

A

overuse of SABA will cause desensitisation of the receptors

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10
Q

Are LABA’s used in COPD and are they used in combination with other drugs?

A

yes they are used in COPD and can be used alone or with combination of anticholinergics or ICS

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11
Q

Are LABAs prescribed alone to treat asthma? and if so why or why not?

A

Should never be used alone!!!! Do not treat the underlying chronic inflammation, and this may increase the risk of life-threatening and fatal asthma exacerbations

always used in combination with ICS

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12
Q

What does comibining a LABA and ICS result in?

A

Increased synergistic actions in treatment for COPD and asthma

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13
Q

What are the adverse effects of B2 adrenergic agonists?

A

Muscle tremor from stimulation of B2 receptors in skeletal muscle

Tachycardia and palpitations from stimulation of atrial B2 receptors and myocardial B1 receptors

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14
Q

What are the 2 broad actions of B2 agonists?

A

Bronchodilation and stabilise the mast cells membrane (decrease oedema mucus etc)

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15
Q

What is the mechanism of action for muscarinic cholinergic antagonists?

A

Inhibit M3 – Gq –PLC receptor which inhibits IP3 (prevents the increase in intracellular calcium) and DAG from stimulating PKC which prevents stimulation of Calcium sensitisation latch bridge

Inhibits only ACh-mediated bronchoconstriction

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16
Q

Describe the effectiveness of muscarinic cholinergic antagonists in Asthma and COPD patients

A

Less effective as bronchodilators than B2 agonists (used as an addition to bronchodilator) so not as effective as beta 2 agonists

Effective or suprerior to B2 agonists in COPD

They decrease gas trapping and increase exercise tolerance. This is because they prevent relieve bronchoconstriction and bronchoconstriction is the only reversible symptom of COPD. B2 agonists are just unecessary as have extra effects of mast cells????

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17
Q

What are the adverse effects of muscarinic cholinergic antagonist? (x2)

A

Dry mouth and bitter taste of inhaled

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18
Q

What are the 2 broad effects of anticholinergics on airways?

A

Effect just the bronchioles which produce just bronchdilation and reduce mucus secretion

19
Q

What is the mechanism of action for methylxanthines?

A

They bypass the action of extracellular receptors (adrenergic or cholinergic) and prevent the degradation of cAMP. –> results in smooth muscle and relaxation

20
Q

What is the contraindication of methylxanthines (in regards to its mechanism of action

A

lacks specificity – smooth muscle cells are not the only ones to use cAMP as a 2nd messenger

21
Q

Why are methylxanthines still used despite its adverse effects?

A

Used in developing countries because it is inexpensive

22
Q

what are the adverse effects of methylxanthines

A

nervous system overstimulation

anxiety, nervousness nause, vomitting

23
Q

Glucocorticoids potently suppress _______

A

inflammation

24
Q

What are the effects of corticosteroids on the inflammatory processes? (x4)

A

Inhibit the production of factors that are critical in generating the inflammatory response

decrease release of vasoactive and chemoattractive factors

diminished sedcretion of lipolytic and proteolytic enzymes

Reduce expresssion of pro-inflammatory cytokines

25
Q

What is the mechanism of action for corticosteroids?

A

Enter target cells and bind to glucocorticoid receptors (GR)

The GR complex moves into n ucleus and binds to target genes –> alters transcription of the gene

directly Inhibits acetylation and causes activates HDAC2 which causes deactylation

26
Q

Why are corticosteroids not effective in COPD?

A

This is because they work by activating HDAC2 which causes deactylation of gene expression

However in COPD there is a decrease in HDAC2 int he first place.

27
Q

What are the effects of the corticosteroids on the inflammatory cells in airways? (x4)

A

Decrease mast cell rupture

Decrease new antibody production

decrease activity of immune cells

decrease recruitment of inflammatory cells into airways

28
Q

What are the synergistic effects of corticosteroids and B2 agonists?

A

Corticosteroid effects of B2 adrenergic responsiveness:

Increase strength of effects of B2 agonists on smooth muscle

Prevent and reverse B receptor densitiation

Increase transcription of B2 receptor gene

B2 agonists effects on corticosteroid responsiveness

B2 agonists also increase the action of GRs

Increase binding of GRs

29
Q

What are the adverse effects of corticosteroids? (x3)

A

Susceptible to infection in the pharynx region due to supression of immune function

Controversy over whether it stunts growth in children

hoarse voice

30
Q

Comment on the timing of effects of the corticosteroids

A

ICS inhibits the late phase and inhibits the increase of hyper-responsiveness

has no effect on early stage (which is stimulation of mast cell and chemotaxines release)

only effects when the mediators are released and epitihelial damage and inflammation starts occuring etc….

31
Q

When is ICS given in asthma?

A

Give to people with persistent asthma

(basically anyone who needs to use B2 agonist inhaler for symptom control more than twice weekly)

32
Q

When are systemic steroids give in asthma?

A

If lung function is below 30% predicted

33
Q

When is ICS given in COPD patients?

A

Jokes lol, it never really is because it doesnt have much of an effect

COPD patients only occasionally respond to steroids –> these patients likely to have accompanying asthma

34
Q

Explain the mechanism of action for leuktriene receptor antagonists

A

leukotrienes are produced by inflammatory cells, particulary mast cells and eosinophils

The airways have receptors for leukotrienes, if these bind they trigger smooth muscle contraction, mucus secretion and odema.

These drugs block the receptor and thus decrease these effects

35
Q

What is the mechanism of action of monoclonal anti-IgE treatment?

A

Bind with free IgE and prevent these from binding with mast cells

used in severe atopic asthma

36
Q

Whats a drug that is used commonly in severe atopic asthma?

A

monoclony anti IgE

37
Q

Why is IV administeration of these asthmatic drugs bad?

A

Because increase number of systemic effects due to the increase abundance of these drugs in plasma

38
Q

Why ICS not given on its own?

A

Because it only acts upon the late phase, I.E it doesnt relieve bronchospasm

39
Q

Why is SABA first?

A

As they are quick acting relievers that are only meant to be used for asthma that is controlled and not persistent

Best for ‘sudden’ asthma

40
Q

Describe the stepwise approach to asthma therapy

A
41
Q

which medication is the colour white/blue or just blue?

A

SABA

42
Q

which medication is the colour light blue/white

A

LABA

43
Q

which medication is the colour red?

A

ICS/LABA combinations

44
Q

Why are muscarinic cholinergic antagonists used adjutant in asthma?

A

Not as much research surrounding LAMA

Respiratory Medicine (15 decks)

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