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The Respiratory System > Drugs Used to Treat Asthma and COPD > Flashcards

Drugs Used to Treat Asthma and COPD Flashcards

1
Q

What are the 6 drug groups used in the treatment of asthma and COPD

A
  • Beta 2 agonists
  • Anti-muscarinic drugs
  • Xanthines
  • Mast cell stabilising drugs
  • Leukotrine antagonists
  • Corticosteroids.
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2
Q

What is an example of a beta 2 agonist

A

Salbutamol

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3
Q

What is an example of an anti-muscarinic drug

A

Ipratropium bromide

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4
Q

What is an example of a xanthine

A

Theophylline

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5
Q

What is an example of a leukotriene antagonist

A

Montoleukast

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6
Q

What is an example of a corticosteroid

A

Prednisolone

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7
Q

What is the role of beta 1 adrenoceptors

A

These are found in the heart and increase the force and rate on contraction

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8
Q

What is the role of beta 2 adrenoceptors

A

These are found in the lungs and the blood vessels where they bring about smooth muscle relaxation resulting in vasodilatation in the blood vessels and bronchodilation in the airways.

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9
Q

What is the result of agonism of beta 2 receptors in the lungs

A

This causes dilatation of the bronchi and bronchioles which increases their diameter, resistance to airflow is decreased and the ventilation of the alveoli increases which improves gas exchange.

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10
Q

What endogenous substances do beta adrenoceptors respond to

A

Adrenaline and other catecholamines secreted more locally in the lung.

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11
Q

What happens to the lungs if adrenaline is present

A

The smooth muscle in the lungs relaxes and the airways become less resistant to airflow leading to better ventilation of the alveoli.

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12
Q

Which drug type should patients with asthma or COPD not be given and why

A

Beta adrenoceptor antagonists (beta blockers) such as atenolol and bisoprolol because these are not entirely selective for beta 1 receptors in the heart and can act on beta 2 receptors in the lung to bring about bronchoconstriction.

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13
Q

What is the effect of beta 2 agonists on smooth muscle in the heart, lungs, uterus, bladder, GI tract etc.

A

Beta 2 agonists bind to beta-2 adrenoceptors leading to an increase in the secondary messenger cAMP and bringing about relaxation of the muscle.

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14
Q

What is the effect of beta 2 agonists in the vasculature (arteries and veins)

A

Beta 2 agonists bring about relaxation of the smooth muscle of the vasculature and bring about vasodilatation.

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15
Q

What effect to beta 2 agonists have on mast cells

A

To some extent, beta 2 agonists stabilise mast cells and reduce inflammatory mediators such as histamine from these cells.

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16
Q

What effect do beta 2 agonists have on skeletal muscle and therefore what is one side effect asthmatics often experience when using emergency treatment

A

Beta 2 agonists cause tremor in skeletal muscle.

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17
Q

Why are beta agonists sometimes also used to treat people with hyperkalaemia

A

Beta agonists act on cell membranes to increase the uptake of potassium into the cell leading to a rapid reduction of potassium in the blood. This is why they are sometimes used to treat hyperkalaemia.

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18
Q

What is the name of a short acting beta agonist

A

Salbutamol

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19
Q

What is the name of a long acting beta agonist

A

Salmeterol

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20
Q

What are the main actions of salbutamol

A

To increase cAMP production in the smooth muscle on the airways leading to relaxation and bronchodilation.

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21
Q

What are the indications for use of salbutamol

A
  • For prophylaxis in patients with acute asthma or COPD
  • Used in emergencies in nebulised form to allow a higher dose
  • Hyperkalaemia.
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22
Q

What are the possible adverse effects of salbutamol

A
  • Tremor (due to action on beta receptors in skeletal muscle)
  • Tachycardia and palpitations (due to action on beta-1 receptors in the heart)
  • Hypokalaemia (due to the increased uptake of potassium by cells)
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23
Q

What type of drug reactions come about from treatment with salbutamol

A

Type A adverse drug reactions. This means they are entirely predictable knowing the pharmacology of the drug.

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24
Q

What type of receptors do anticholinergic drugs act on

A

Muscarinic receptors, M1, M2 and M3 located in the airways.

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25
Q

What naturally acts on muscarinic receptors

A

Acetylcholine

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26
Q

What type of neurotransmitter is acetylcholine and what action does this have on the airways

A

Acetylcholine is a parasympathetic neurotransmitter released from the nerve endings of the vagus nerve to bring about bronchoconstriction and airways narrowing,

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27
Q

What do cholinergic agonists do

A

Act on muscarinic receptors to bring about airway narrowing and bronchoconstriction as well has increased mucus secretion.

28
Q

What do cholinergic antagonists do

A

Bring about bronchodilatation and reduced mucus production.

29
Q

What is an example of a short acting anticholinergic drug

A

Ipratropium bromide

30
Q

What is an example of a long acting anticholinergic drug

A

Tiotropium

31
Q

What type of drug reactions do anticholinergic drugs tend to bring about

A

Type A adverse reactions - those which are very predictable knowing the pharmacology of the drug.

32
Q

What are some examples of adverse drug reactions of anticholinergic drugs

A
  • Reduced secretions from other glands in the body leading to a dry mouth and scratchy throat
  • Reduced smooth muscle contraction leading to constipation and urinary retention
  • Reduced cholinergic effect on the heart leading to tachycardia
  • Headaches.
33
Q

How do you minimise the systemic effects of anticholinergic drugs

A

If they can be delivered in an inhaled form to where they are required.

34
Q

What are the main actions of anticholinergic drugs

A

They act at parasympathetic muscarinic receptors in the lungs to bring about bronchodilation and decreased mucus secretion.

35
Q

What are the indications for use of ipratropium bromide

A

In COPD but can also be used in bronchial asthma and rhinitis.

36
Q

What are the adverse effects of ipratropium bromide

A
  • Dry mouth
  • Nausea
  • Headache
37
Q

What are the main actions of theophylline

A

Theophyllines are phosphodiesterase inhibitors. This means they increase cAMP in smooth muscle and bring about relaxation.

38
Q

What is the action of phosphodiesterase in the body

A

It reduces the levels of cAMP by breaking it down into AMP, therefore preventing smooth muscle relaxation.

39
Q

Other than muscle relaxation due to increase cAMP, what else does theophylline do (as a phosphodiesterase inhibitor)

A

It activates PKA, inhibits TNF alpha and inhibits leukotriene synthesis.

40
Q

What are the indications for use of theophylline

A

Used principally in COPD.

41
Q

How is theophylline given

A

Orally

42
Q

What are the adverse effects of theophylline

A

Similar to beta 2 agonists -

  • Tachycardia
  • Palpitations
  • Nausea
43
Q

What is fairly unique about theophylline

A

It is one of few drugs that the plasma concentration is measured to give an idea whether the dosage regimen is achieving sufficient concentration.

44
Q

What are the three general approaches to bronchodilation

A
  • Beta 2 agonists
    Act on beta 2 adrenoceptors in the lungs to increase cAMP and bring about a sympathetic response and cause smooth muscle relaxation and bronchodilation.
  • Anticholinergic drugs
    Prevent parasympathetic action by acetylcholine on muscarinic receptors in the lungs to bring about smooth muscle relaxation and bronchodilation.
  • Theophyllines
    Inhibit phosphodiesterase to increase the levels of cAMP, bringing about relaxation and bronchodilation.
45
Q

What are corticosteroids

A

Powerful anti-inflammatory drugs

46
Q

What are the actions of corticosteroids

A
  • they reduce the recruitment of white cells and macrophages to the area of inflammation (the lung in COPD and asthma)
  • They reduce oedema by reducing the permeability of vascular membranes.
  • They reduce the release of mediators such as interleukins.
  • They increase anti-inflammatory mediator production such as IL-1 and IL-10
47
Q

In what form do corticosteroids tend to be given for asthma and COPD

A

In purple or brown inhalers.

48
Q

What are the adverse effects of corticosteroids

A
  • Hyperglycaemia (so tends to precipitate type 2 diabetes)
  • Osteoporosis (reduced bone density)
  • Proximal myopathy (weak muscles)
  • Skin thinning
  • Altered fat distribution (more central fat accumulates)
  • Hypertension due to a tendency to retain sodium
  • Weight gain due to fat deposition and fluid retention
  • Growth suppression in children
  • Increased susceptibility to infection due to immunosuppression.
49
Q

What is an example of an inhaled corticosteroid

A

Beclometasone

50
Q

What is an example of an oral corticosteroid

A

Prednisolone

51
Q

When may IV corticosteroids be given

A

For very unwell patients in emergency situations.

52
Q

What is the action of leukotriene antagonists

A

To block the effects of leukotrienes which gave been recognised to be important in the inflammatory activity in asthma.

53
Q

What are leukotrienes

A

Leukotrienes are synthesised from arachidonic acid. Their production is increased in allergic responses and inflammation. They tend to stimulate airways narrowing and increased mucus secretion.

54
Q

What is an example of a leukotriene antagonist

A

Monteleukast

55
Q

What are the adverse effects of leukotriene antagonists

A

Leukotriene antagonists tend to be well tolerated but some adverse effects that can arise are -

  • Increased infection risk
  • Muscle aches
  • Liver damage
  • Hypersensitivity
56
Q

What are the main actions of monteleukast

A

To reduce airway narrowing and reduce mucus secretion.

57
Q

What are the indications of monteleukast

A
  • Bronchial asthma, especially exercise induced
  • Seasonal allergic rhinitis
  • An additive effect when given with corticosteroids.
58
Q

What are the adverse effects of monteleukast

A
  • Abdominal pain
  • Thirst
  • Headache
  • Hyperkinesia
  • Hypersensitivity.
59
Q

What is the action of cromoglicate

A

Cromoglicate is used to stabilise mast cells found in the airways to reduce the release of histamine - an inflammatory mediator.

60
Q

What is an example of a similar drug to cromoglicate

A

Nedocromil.

61
Q

How is cromoglicate given

A

In inhaled form or occasionally for children in nebulised form.

62
Q

What are the indications for use of oxygen

A

Oxygen is give to patients with respiratory disease to increase the availability of alveolar oxygen. it is usually given in an emergency when patients have acute attacks of asthma or COPD.

63
Q

Which type of patients do you need to be carful with when giving oxygen and why

A

Patients with COPD because often they are chronically hypercapnic and so their drive to breathe no longer comes from having high CO2, but instead comes from being hypoxic. Giving oxygen solves the problem of hypoxia but can then subsequently take away the patients drive to breathe all together.

64
Q

What are the pros of aerosol delivery

A

Drugs go directly to the site where they are required, reducing the exposure of other parts of the body.

65
Q

What are the cons of aerosol delivery

A
  • Not all drugs are available in inhaled form

- Correct inhaler technique is required.

The Respiratory System (20 decks)

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