Asthma drugs Flashcards

1
Q

What are the aims of drug treatment?

A

Reduce inflammation, prevent brochoconstriction, and restore airway calibre.

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2
Q

At what different stages are what drugs used?

A

Bronchodilator is used to treat the first asthma response- bronchospasm.
Anti-inflammatory drugs are used to treat the later response of inflammation.

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3
Q

What are the four types of bronchodilator?

A

B2 adrenergic receptor agonsits.
Theophylline
Muscarinic receptor agonists
Leukotriene receptor antagonists.

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4
Q

What are the actions of beta 2 adrenergic receptor agonists?

A

Act directly on the beta 2 adrenoreceptors in brochiole smooth muscle to relax the muscle.
Inhibit mediator release from mast cells and monocytes.
Can act on cilla to increase mucus clearance.

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5
Q

Explain the activation pathway of beta 2 adrenoreceptors.

A

Beta 2 agonists bind to the receptor on the G-protein. This activates the G protein which activates adenylate cyclase. This causes ATP to be converted to cAMP. This activated PKA which leads to protein phosphorylation. Causing muscle relaxation.

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6
Q

What are short acting beta 2 adrenergic receptor agonists.

A

Affects can be seen after 30 minutes and their effects last up to 4-6 hours.
Examples are salbutamol and tolbutamide.

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7
Q

What are the long acting beta 2 adrenergic receptor agonists?

A

Salmeterol
Last up to 12 hours.
Can be used twice daily with patients that aren’t on glucocorticoids.

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8
Q

What are the unwanted effects of beta 2 agonists?

A

Absorption into the systemic circulation
Tremor
Development of tolerance- however this can be resolved with glucocorticoids.

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9
Q

What is theophylline?

A

Bronchodilator used to treat the first phase of asthma.
Contains xanthine
Inhibits PDE
Second line drug- used when response to beta 2 is inadequate.

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10
Q

What are the unwanted side effects of theophylline?

A

CNS stimulant causing tremor and sleep disturbance.
Absorbed into the cardiovascular system stimulating heart causing vasodilation.
Absorption into the GI tract causing anorexia, nausea and vomiting.

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11
Q

What are muscarinic receptor antagonists?

A

Bronchdilators that are used when B2 agonists are insufficient.
Fast acting- 3-5 hours.
Administed by an aerosol- poorly absorbed so therefore few unwanted side effects.

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12
Q

List an examples of muscarinic receptors.

A

Iprotropium

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13
Q

What are the actions of muscular receptors

A

Bronchodilators
Inhibit mucus secretion
Increase clearance of bronchial secretions.
Block ACH at muscarinic receptors.

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14
Q

How does ACH causes bronchoconstriction with asthma.

A

People with asthma have raised levels of ACH. ACH binds to receptors in smooth muscle causing constriction. Blocking the receptors thus prevents bronchoconstriciton.

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15
Q

What are leukotriene receptor antagonists.

A

Bronchodilator.
Administered orally.
Used to prevent exercise induced and aspirin asthma.
Used in conjunction with beta 2.

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16
Q

What are examples of leukotriene receptor antagonists

A

Montelucast

Zarfirlukast.

17
Q

What are the actions of leukotrine antagonists?

A

Act on cysteinyl-leukotrine receptors.
Prevent the actions of LTC and LTD- the spasminogens that stimulate mucus secretion.
There are few unwanted side effects- headaches and GI disturbances.

18
Q

What are the main types of anti-inflammatory drugs?

A

Glucocorticoids- e.g beclometasone and budesonide.

19
Q

What are the actions of glucocorticoids?

A

Reduce production of inflammatory mediations, LTC and LTD spasminogens.
Therefore reduce bronchospasm and reduce the recruitment and activation of inflammatory cells.

20
Q

What are the clinical uses for glucocorticoids?

A

Used for patients receiving regular broncholiators.
Used for severe asthma.
Given IV as hydrocortisone and oral predisolone for acute exacerbations.

21
Q

What is a cromoglicate?

A

A cromoglicate can reduce both early and late phases of responses.
Reduces bronchial hyper-reactivity.
Effective against asthma caused by antigen, exercise and irritants.
However not all asthmatics respond.

22
Q

What is an example of a cromoglicate?

A

Nedocromil sodium

23
Q

What are the mechanisms of cromoglicate?

A

Mast cell stabiliser

Side effects cause irritation of URT and hypersensitivity.

24
Q

What are the clinical uses of cromoglicate?

A

Used in prophylactic to prevent both phases of an attack. Most effective in children.

25
Q

What are biologic agents?

A

A new development of recombinant DNA from IgG1.

26
Q

Give an example of a biologic agent.

A

Omalizumab

27
Q

What are the mechanisms of biologic agents?

A

Inhibit IgE

28
Q

What are the unwanted side effects of omalizumab?

A

Anaphylaxis

Malignancies.

29
Q

How would you treat mild asthma with rare attacks?

A

Beta 2 agonist as and when required.

30
Q

How would you treat mild asthma with more frequent attacks?

A

Glucocorticoid and beta 2.