Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

D. Respiratory Drugs > 2. Drugs used in respiratory disorders > Flashcards

2. Drugs used in respiratory disorders Flashcards

1
Q

Pharmacotherapeutics for asthma

A
  1. Bronchodilators to reverse bronchoconstriction

2. Anti-inflammatory

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Types of bronchodilators for asthma

A
  1. SABA (relievers) (first-line)
  2. LABA (controllers) (first-line)
  3. Muscarinic receptor antagonists (second-line)
  4. Theophylline (second-line)
  5. Leukotriene receptor antagonists (weak) (second-line)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Types of anti-inflammatory for asthma

A
  1. Glucocorticoids (corticosteroids/steroids) (first-line)
  2. Mast cell stabilisers - Cromoglicic acid
  3. Leukotriene pathway inhibitors / receptor antagonists
  4. Anti-IgE antibody
  5. Anti-interleukin 5 / interleukin-4 signalling antibodies
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

MOA of beta2-adrenoceptor agonists

A
  1. Airway smooth muscle relaxation → bronchodilation
  2. Mast cell stabilisation
  3. Decrease microvascular leakiness
  4. Increase mucociliary clearance
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Examples of beta2-adrenoceptor agonists

A
  1. Epinephrine (IV/SC in emergency)
  2. Salbutamol (3-6h SABA, fast acting) → IV in emergency
  3. Fomoterol (12h LABA, fast acting 2-3 mins)
  4. Salmeterol (12h LABA, slow-acting)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Adverse effects of beta2-adrenoceptor agonists

A

beta2-adrenoceptor-mediated sympathomimetic effects:

  1. Tremor and muscle cramps
  2. Peripheral vasodilation (e.g. flushing)
  3. Palpitations & tachycardia (nonselective beta-agonism leading to beta1-adrenoceptor effects)
  4. Hypokalemia / Hyperglycaemia
  5. Beta2-adrenoceptor tolerance → increased risk of asthma-related death
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What must be given together with LABAs

A

Glucocorticoids → upregulate beta2-adrenoceptor expression

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Example of muscarinic receptor antagonists

A

Ipratropium bromide → SAMA

Tiotropium bromide → LAMA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

MOA of mscarinic receptor antagonists

A
  1. Inhibit M3 receptor-mediated bronchoconstrictions

2. Reverse vagal-nerve mediated bronchospasm & mucus secretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Uses and efficacy of muscarinic receptor antagonists

A
  1. Adjunct to inhaled beta2 agonists and inhaled glucocorticoids
  2. Patients intolerant to beta2 agonists
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Adverse effects of muscarinic receptor antagonists

A
  1. Limited systemic side effects as not well absorbed into systemic circulation when taken by inhalation
  2. Unpleasant taste
  3. Typical parasympatholytic effects
    - Dry mouth
    - Urinary retention (in elderly)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Examples of methylxanthines

A
  1. Theophylline

2. Aminophylline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

MOA of methylxanthines

A
  1. Inhibits phosphodiesterases
  2. Blocks adenosine receptors
  3. Increase adrenaline release from adrenal medulla
  4. CNS stimulant action on respiration
  5. Not used as an anti-inflammatory but has some anti-inflammatory effects
    - Effects on mast cells and T-cells
    - Decrease microvascular leakiness
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Uses and efficacy of methylxanthines

A
  1. Can be administered IV in acute severe asthma

2. Less effective bronchodilators than beta2 agonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Adverse effects of methylxanthines

A
  1. Narrow therapeutic window
  2. Many drug-drug interactions → caution for potential drug interactions
  3. GI: nausea, vomiting, abdominal discomfort, anorexia
  4. CNS: nervousness, tremor, anxiety, insomnia, seizures
  5. CVS: arrhythmias
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Example of cysteinyl-leukotriene receptor antagonists

A

Montelukast

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Uses of CysLT receptor antagonists

A
  1. Adjunct therapy for mild to moderate asthma

2. Not used alone as reliever to rescue asthma attack

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Efficacy of CysLT receptor antagonist

A
  1. Relaxes airways in mild asthma (about 1/3 as effective as salbutamol, additive effects with beta2-adrenoceptor agonist)
  2. Effective in aspirin-sensitive asthma
  3. Effective in exercise-induced asthma
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Uses of MgSO4

A
  1. Adjunct treatment of severe acute asthma
  2. Intravenous or nebulized
  3. Mechanisms incompletely understood
    - Relaxes airway smooth muscle
    - Modulates release of acetylcholine and histamine
    - Anti-inflammatory effect
  4. Adverse effects rarely reported
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Examples of inhaled corticosteroids

A

Budesonide, Fluticasone, Cicleosonide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Characteristics of inhaled corticosteroids

A
  1. High receptor binding affinity → very low dose required
  2. Extensive first pass metabolism → less systemic side effects
  3. High lipophilicity
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What is an example of “soft steroid”

A

Ciclesonide → prodrug that requires esterase activation in the lung thus avoiding systemic side effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Adverse effects of inhaled corticosteroids

A

Side effects rare due to limited systemic absorption

24
Q

Can inhaled corticosteroids be administered IV as well?

A

Yes, it can be administered IV in acute asthma attack but must be administered early as onset of action is slow

25
Q

MOA of inhaled corticosteroids

A
  1. Reduce pro-inflammatory mediators
    - decrease T cells, mast cells, eosinophils
    - decrease shedding of epithelial cells
    - decrease mucus secretion
    - decrease pro-inflammatory cytokines
    - decrease phospholipase A2
    - decrease COX2
    - decrease 5-LOX
    - decrease inducible nitric oxide synthase
  2. Increase anti-inflammatory mediators
    - increase annexin A1
    - increase beta2-adrenoceptors

i. Do not relax airway smooth muscles directly
ii. Decrease airway hyper-responsiveness in 4-6 weeks
iii. Decrease frequency of acute asthma exacerbation
iv. Possibly prevent airway wall remodelling
v. Decrease the need for beta2 agonist
vi. Decrease risk of death from asthma

26
Q

Uses of inhaled corticosteroids

A
  1. First line prophylactic for asthma treatment

2. For nocturnal asthma

27
Q

Adverse effects of inhaled corticosteroids

A

Largely limited by route of administration

  • Oropharyngeal candidiasis
  • Dysphonia
  • Cough / throat irritation
  • Adrenal suppression (e.g fluticasone)
  • Easy bruising (especially in elderly)
  • Posterior subcapsular cataracts
  • Osteoporosis
28
Q

Examples of leukotriene pathway inhibitors

A
  1. Montelukast - CysLT receptor antagonist

2. Zileuton - 5-LOX inhibitor

29
Q

Uses for leukotriene pathway inhibitors

A
  1. Prophylaxis & chronic treatment of asthma
  2. Aspirin-induced / NSAID exacerbated asthma
  3. Exercise-induced asthma
30
Q

Efficacy of leukotriene pathway inhibitors

A
  1. Less effective than glucocorticoids
  2. Decrease frequency of asthma attacks
  3. Decrease use of inhaled steroids
  4. Decrease use of beta2 agonist
  5. Decrease peripheral blood eosinophil levels
31
Q

Side effects of leukotriene pathway inhibitors

A

Few and mild, headache and GI disturbances

Caution: suicidal thinking and neuropsychiatric adverse effects in some patients

Associated with Churg-Straus syndrome → likely due to concomitant glucocorticoid withdrawal when prescribing leukotriene pathway inhibitors

32
Q

Example of mast cell stabiliser

A

cromoglicic acid

33
Q

MOA of cromoglicic acid

A
  1. Mast cell stabiliser
  2. Decrease mast cell degranulation induced by IgE-mediated FcεRI cross-linking
  3. Decrease secretion of inflammatory mediators from eosinophils, neutrophils and macrophages
  4. Controls chloride channels to inhibit cellular activation
  5. Increase secretion of annexin A1
    - Annexin A1 inhibits prostaglandin and leukotriene production
34
Q

Uses for cromoglicic acid

A
  1. Prophylactic control of asthma (by inhalation only)

2. Prophylactic control of allergic rhinitis, allergic conjunctivitis, and vernal keratoconjunctivitis

35
Q

Efficacy of cromoglicic acid

A
  1. Prevents antigen, cold, dry air and exercise-induced bronchospasm
  2. Single-dose before antigen-challenge or exercise prevents bronchospasm
  3. ↓ bronchial hyper-reactivity in 4 weeks
  4. ↓ need for bronchodilator therapy
  5. But less effective than inhaled glucocorticoids
  6. Inter-individual variability in response → not possible to predict which patients will respond
36
Q

Side effects of cromoglicic acid

A
  1. Throat and nasal irritation, mouth dryness, cough

2. Unpleasant/Bitter taste

37
Q

An example of anti-IgE monoclonal antibody

A

Omalizumab

38
Q

Uses and MOA of Omalizumab

A
  1. Used for severe asthmatics with allergies and an elevated IgE level
  2. Depletes levels of free IgE in serum
  3. Decreases FcεRI expression on mast cells (basophils)
39
Q

Limitations of omalizumab

A
  1. Expensive
  2. Associated with small increase in risk of heart attack, transient ischaemic attacks (TIA) and blood clots
  3. Potential for anaphylaxis
40
Q

Example of Anti-IL-5/IL-4 signalling monoclonal antibodies

A

Reslizumab (IL-5)

41
Q

Limitation of reslizumab

A
  1. Expensive
  2. Oropharyngeal pain
  3. Potential for anaphylaxis
42
Q

Drugs used in the management of COPD

A
  1. Bronchodilators: SAMAs, SABAs, LAMAs and LABAs
  2. Anti-inflammatories: Inhaled corticosteroids
  3. Theophylline
  4. Phosphodiesterase-4 (PDE-4) inhibitors: roflumilast
  5. Azithromycin
  6. Mucolytics: erdosteine
  7. Antibiotics
  8. Vaccinations against respiratory infections
  9. Smoking cessation
43
Q

What is the ABCD of COPD?

A

Exacerbations per year: ≤ 1 (with no hospital admission) → Group A and B

Exacerbations per year: ≥ 2, ≥ 1 leading to hospital admission → Group C and D

44
Q

Treatment for Group A COPD

A

Any bronchodilator (SABA or LABA)

45
Q

Treatment for Group B COPD

A

A long acting bronchodilator (LABA or LAMA)

46
Q

Treatment for Group C COPD

A

LAMA

47
Q

Treatment for Group D COPD

A

LAMA or LAMA + LABA or ICS + LABA

48
Q

Example of phosphodiesterase-4 (PDE-4) inhibitors

A

roflumilast

49
Q

MOA of roflumilast

A

Inhibition of PDE-4 prevents breakdown of cAMP resulting in

  1. Reduced inflammatory cell activity
  2. Inhibition of fibrosis
  3. Relaxation of smooth muscle
50
Q

Uses and efficacy of roflumilast

A
  1. Reduces episodes of exacerbation

2. Slows progress of fibrosis

51
Q

Adverse effects of roflumilast

A
  1. Headaches, dizziness, insomnia
  2. Weight loss, diarrhoea, nausea, decreased appetite
  3. Rarely: anxiety, depression, and suicidal ideation
  4. Caution in patients with hepatic impairment
52
Q

MOA of azithromycin

A
  1. Macrolide antibiotic prevents bacteria from growing by interfering with their protein synthesis
  2. Additionally, anti-fibrotic and airway smooth muscle relaxant through mechanisms that are not completely understood
53
Q

Uses and efficacy of azithromycin

A
  1. Anti-fibrotic and airway smooth muscle effects reduces risk of exacerbations
  2. Prevention and treatment of exacerbations due to bacterial infection
54
Q

Adverse effects of azithromycin

A

Many adverse effects including:
• Common: Diarrhoea, nausea, vomiting
• Severe: Cardiac arrythmia
• Contraindicated history of cholestatic jaundice or hepatic dysfunction

55
Q

Vaccination for stable COPD

A

PPSV23 and PCV13 recommended for all patients ≥ 65 years old

PPSV23 recommend for younger COPD patients with significant comorbid conditions including chronic heart or lung disease

56
Q

Pharmacotherapy for smoking cessation

A
  1. Nicotinic
    - Nicotine replacement
    - Vareniciline (partial agonist)
  2. Antidepressant (NET/DAT inhibitors)
    - Bupropion
    - Nortryptiline

D. Respiratory Drugs (2 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions