Asthma, COPD AND Rhinitis Medications Flashcards

1
Q

What is Theophylline?

A

BRONCHODIALTOR - ASTHMA - A methylxanthine drug with bronchodilator and anti-inflammatory action. Has many side effects and drug interactions.

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2
Q

What is Fexofenadine?

A

ANTI-HISTAMINE - RHINITIS - A competitive H1 receptor antagonist used to treat allergic rhinitis.

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3
Q

What is Ipratropium?

A

SAMA - RHINORRHOEA A short acting drug that blocks acetylcholine receptors non-selectively. Can be delivered intranasally to treat rhinorrhoea.

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4
Q

What is Tiotropium?

A

LAMA - COPD -An anticholinergic drug, selective for M3 receptors with a long half life.

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5
Q

What is Monteleukast?

A

BRONCHODILATOR - ASTHMA AND RHINITIS - A cysteinyl leukotriene receptor antagonist used to treat asthma and allergice rhinitis.

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6
Q

What is Beclometasone?

A

CORTICOSTEROID - ASTHMA, COPD, RHINITIS -An INHALED corticosteroid often used in combination with a beta-2 adrenoceptor agonist. It is used as a monotherapy or combination in asthma but only as a combination in COPD.

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7
Q

What is Rofumilast?

A

ADDITIONAL TREATMENT - COPD -An inhaled corticosteroid. Used in combination with a beta-2 adrenoceptor agonist, particularly in frequent exacerbations of COPD.

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8
Q

What is Sodium Chromoglicate?

A

MAST CELL STABILISER - ASTHMA AND RHINITIS -A drug that acts as a mast cell stabiliser, used in asthma and allergic rhinitis.

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9
Q

What is Prednisolone?

A

STERIOD - RHINITIS, ASTHMA AND COPD - An oral steroid, used in severe or intractable rhinitis, acute asthma or an exacerbation of COPD. Low therapeutic ratio therefore side effects are common.

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10
Q

What are relievers?

A

They act as bronchodilators. They include -
Short Acting Beta 2 Adrenoreceptor Agonists (SABA)
Long Acting Beta 2 Adrenoreceptor Agonists (LABA)
Cysteinyl Leukotriene 1 Receptor Agonists

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11
Q

What are controllers/preventers?

A

They act as anti-inflammatory agents that reduce airway inflammation. They include -
Glucocorticoids
Chromoglicate
Humanised monoclonal IgE antibodies

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12
Q

What are Methylxanthines?

A

Thy are anti-oxidants. They are both preventers and relievers.

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13
Q

How do beta 2 adrenoreceptor agonists work?

A

They bind to the B2 adrenoreceptors and cause the relaxation of smooth muscle

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14
Q

Describe the use of SABAs in asthma

A

They are a first line treatment for mile intermittent asthma and are taken when required. They increase mucus clearance and decrease inflammatory mediator release from the mast cells.

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15
Q

Describe the use of LABAs in asthma

A

They are not used for acute relief of bronchospasm. They are useful for nocturnal asthma. They shouldnt be used as a monotherapyas they can worsen asthma and increase likelihood of astmatic death, and must always be administered with a glucocorticoid

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16
Q

How do cysteinyl leukotriene receptor antagonists work?

A

They act competitively at the CysLT1 receptor only used in asthma as an anti inflammatory. The CysLTs are derived from mast cells and infiltrating inflammatory cells to cuase smooth muscle contraction, mucous secreation and oedema. By blocking thins mechanism, asthma is relieved

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17
Q

What are some examples of CysLT1 inhibitors?

A

Montelukast and Zarifirlukast

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18
Q

Describe the use of CysLT1 receptor antagonists in asthma.

A

They are a 2nd line add on therapy in mild persistant asthma OR used in combination with medications such as ICS in severe asthma. They are administered orally and are therefore not recommended for relief of acute severe asthma attack.
They can also be useful for EIB and allergic rhinitis (w/ anti-histamine).

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19
Q

How do methylxanthines work?

A

The mode of action is uncertain but it might involve the inhibition of isoforms of phosphodiesterases.

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20
Q

What are some examples of methylxanthines?

A

Theophylline and aminophylline

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21
Q

Describe the use of methylxanthines in asthma.

A

They are a second line drug used in combination with ICS and LABA/SABA. They are administered orally and have a very narrow therapeutic window. They inhibit inflammatory mediator release from mast cells, increase mucus clearance, increase diaphragmatic contractility and reduce fatigue.

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22
Q

What are corticosteroids?

A

Humans are able to synthesise two kinds of corticostreoids - glucocorticoids and mineralocorticoids.

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23
Q

What are glucocorticoids?

A

The main hormone in humans is CORTISOL. They decrease inflammatory and immunological responses and regulate other essential processes

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24
Q

What are mineralocorticoids?

A

The main one is aldosterone which regulates salt and water retention in the kidneys. These are less likely to be used in the treatment of asthma.

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25
Q

What are some synthetic derivatives of cortisol?

A

Beclomethasone, Budesonide and Fluticasone

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26
Q

How do glucocorticoids work?

A

They are lipophilic molecules which enter cells across the plasma membrane. They then alter the rate of synthesis of inflammatory mediator proteins.

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27
Q

What are the cellular effects of glucocoticoids?

A

Reduce inflammatory cell and cytokine numbers.

They reduce cytokine mediators, endothelial leakage, they increase B2-Receptors and decrease mucus secretions

28
Q

What are glucocorticoids used for to treat asthma?

A

The are preventers. they both prevent new inflammation and resolve established inflammation. They are short term and don’t alleviate bronchospasm caused by allergens or exercise

29
Q

How are glucocorticoids given in mild to moderate asthma?

A

They are given by metered dose inhaler and efficacy develops over several days. The drugs used are generally beclometasone, budesonide or fluticasone.

30
Q

How are glucocorticoids give in chronic, severe or worsening asthma?

A

They can be given as oral prednisolone and may be used in combination with an inhaled steroid to reduce the oral dose required and minimise systemic effects.

31
Q

What are cromones?

A

They are second line drugs used infrequently to treat allergic asthma, particularly in children. They are mast cell stabilisers. Sodium cromoglicate is an example.

32
Q

How is sodium cromoglicate given to patients with asthma?

A

It is delivered by inhalation to reduce an asthma attack. It is more effective in children and young adults however it is not used much now due to poor efficacy

33
Q

How are monoclonal antibodies used to treat asthma?

A

These bind to lymphocytes to prevent inflammatory responses. This is a very expensive treatment.

34
Q

Give some examples of monoclonal antibody therapy for asthma?

A

Omalizumab - directed against IgE

Mepolizumab - directed against IL-5

35
Q

Which types of drugs are used to treat COPD?

A

Short acting muscarinic receptor antagonists
Long acting muscarinic receptor antagonists
LABAs

36
Q

What are muscarinic receptor antagonists?

A

They bind to muscarinic receptors and prevent binding of acetyl choline and therefore prevent bronchoconstriction. They are based around the broad spectrum parasympathetic antagonist, ATROPINE.

37
Q

Name a SAMA.

A

Ipratropium - non-selective for a specific M receptor

38
Q

Name some LAMAs.

A

Tiotropium
Glycopyrronium
Aclidinium
Umeclidinium

39
Q

How are SAMAs and LAMAs administered to patients?

A

They are administered by inhalation

40
Q

How do LAMAs work for COPD?

A

They reduce bronchospasm, decrease mucous secretion although they have little effect of the progression of COPD.

41
Q

Why are M3 selective blockers superior to ipratropium

A

Because the block of M2 isn’t desirable because blocking it will increase the release of ACh from parasympathetic post-ganglionic neurons

42
Q

Describe muscarinic antagonist and B2 antagonist treatment for COPD.

A

By combining these, there is a superior effect in increasing FEV1to simply administering both drugs separately. This is because the drugs are complimentary to cause smooth muscle relaxation

43
Q

Name a SABA used in COPD treatment.

A

Salbutamol - administered by inhaler every 4-6 hours

44
Q

Name LABAs used in COPD treatment

A

Salmeterol and Formeterol - administered by inhaler twice daily

45
Q

Name ultra-LABAs used in COPD treatment

A

Indacaterol and Olodaterol - not recommended for relief of acute bronchospasm, administered once daily

46
Q

What is rofumilast?

A

This is a phosphodiesterase inhibitor that supresses inflammation and emphysema in COPD

47
Q

What are triple inhalers for COPD?

A

This is where a SABA, LAMA and glucocorticoid are administered once daily for moderate to severe COPD

48
Q

What is rhinitis?

A

This is a common disease where there is a chronic inflammation of the nasal mucosa.

49
Q

What are the symptoms of rhinitis?

A

Rhinorrhoea - runny nose
Sneezing
Itching
Nasal congestion and obstruction

50
Q

What are the three kinds of rhinitis?

A

Allergic
Non-Allergic
Mixed

51
Q

What are the three classifications of allergic rhinitis?

A

Seasonal
Perennial
Episodic

52
Q

What is non-allergic rhinitis?

A

This is any rhinitis that does not involve IgE dependent events. This inculdes, infectious rhinitis, hormonal rhinitis, vasomotor rhinitis, nonallergic rhinitis with eosinophilia syndrome, drug induced rhinitis

53
Q

Describe glucocorticoids in the treatment of rhinitis.

A

They are used to reduce vascular permeability, recruitment and activity of inflammatory cells and release cytokines and anti-inflammatory mediators. They are mainly used to treat seasonal and perrenial rhinitis.

54
Q

How are glucocorticoids administered to rhinitis patients?

A

It is usually administered by topical spray to the nasal mucosa and are used as a monotherapy although they may be combined with antihistamies. They may also be administered orallyin sever cases.

55
Q

What are some examples of glucocorticoids for rhinitis?

A

Beclometasone, fluticasone or oral prednisolone

56
Q

What are some side effects of prednisolone?

A
Diabetes
Weight gain
Fat deposition
Hypertenstion
Cataracts
Proximal myopathy
Tendon ruptures
57
Q

What may be a side effect if corticosteroids in COPD?

A

May cause pneumonia due to local immune supression, impaired mucociliary clearance and altered microbiome.

58
Q

Why is beclomethasone good for eosinophilic asthma and COPD?

A

The reduces exacerbations in these patients.

59
Q

Why would a spacer be used on an inhaler?

A

It avoids coordination problems with a metered dose inhaler.
It reduces oropharyngeal and laryngeal side effects from ICS.
It reduces systemic absorption
Acts as a holding chamber for the aerosol
It reduces particle size and velocity
It improves lung deposition

60
Q

What is Omalizumab?

A

This is an anti-IgE monoclonal antibody given as an injection every 2-4 weeks to patients with sever persistent allergic asthma/

61
Q

What is the mechanism of Omalizumab?

A
  1. It inhibits the binding to the high-affinity IgE receptor.
  2. This inhibits the TH2 response.
  3. It also inhibits associated mediator release form basophils and mast cells.
62
Q

What is Mepolizumab and Benralizumab?

A

These are anti-IL5s. They are given by injection to patients with sever refractory eosinophilic asthma.

63
Q

How do mepolizumab and benralizumab work?

A

They block the effects of the TH2 cytokine, IL-5 which is responsible for eosinophilic inflammation in asthma.

64
Q

What is dupilumab?

A

This is and anti-IL4. It is given by injection to patients with severe asthma and either raised eosinophils or raised FeNO despite max therapy.

65
Q

How does duplimab work?

A

IT blocks IL-4 and IL-13 signalling.