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Phase 1b - Pharmacology & Therapeutics > Pharmacology of Asthma > Flashcards

Pharmacology of Asthma Flashcards

Beclomethasone diproprionate Budesonide Fluticasone Mometason Salbutamol Salmeterol Formoterol Montelukast Ipratropium Aclidinium Glycopyrronium Tiotropium

1
Q

What are the 4 main beta-2 adrenergic receptor agonists used to treat asthma?

A
  • Salbutamol (Short-acting)
  • Salmeterol (Long-acting)
  • Formoterol (Long-acting)
  • Vilanterol (Long-acting)
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2
Q

What is salbutamol used for?

A
  • Inhaled short-acting beta-2-adrenergic receptor agonist used as a bronchodilator in the management of asthma, COPD, bronchitis, as well as prevent exercise induced bronchospasms
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3
Q

What is the primary drug target of salbutamol?

A
  • Beta-2 adrenergic receptor
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4
Q

What is the drug target type of salbutamol?

A
  • Receptor agonist
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5
Q

What is the location of action of salbutamol?

A
  • Bronchial muscles
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6
Q

What is the mechanism of action of salbutamol?

A
  • Bind on beta-2 adrenergic receptors on airway smooth muscle
  • Activation of adenyl cyclase
  • Increase in intracellular concentration of cyclic-3’-5’-adenosine monophosphate
  • Ativation of protein kinase a
  • Decrease in phosphorylation of myosin
  • Decrease in intracellular ionic calcium concentrations
  • Bronchus relaxations
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7
Q

What are the main adverse effects of salbutamol (3)?

A
  • Palpitations
  • Tachycardia / Arrhythmia
  • Hypokalaemia
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8
Q

What is salmeterol used for?

A
  • Inhaled long-acting beta-2-adrenergic receptor agonist used as a bronchodilator in the management of asthma and COPD
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9
Q

What is the primary drug target of salmeterol?

A
  • Beta-2 adrenergic receptor
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10
Q

What is the drug target type of salmeterol?

A
  • Receptor agonist
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11
Q

What is the location of action of salmeterol?

A
  • Bronchial muscles
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12
Q

What is the mechanism of action of salmeterol?

A
  • Bind on beta-2 adrenergic receptors on airway smooth muscle
  • Activation of adenyl cyclase
  • Increase in intracellular concentration of cyclic-3’-5’-adenosine monophosphate
  • Ativation of protein kinase a
  • Decrease in phosphorylation of myosin
  • Decrease in intracellular ionic calcium concentrations
  • Bronchus relaxations
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13
Q

What is the long-acting mechanism of action of salmeterol?

A
  • Bind on beta-2 adrenergic receptors on airway smooth muscle
  • Hydrophilic tail of salmeterol binds to leucine residues in the exo-site of the receptor almost irreversibly
  • Salmeterol persists in the active site (reason for long duration)
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14
Q

What are the main adverse effects of salmeterol (5)?

A
  • Trembling (particularly in the hands)
  • Nervous tension
  • Headaches
  • Palpitations
  • Muscle cramps
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15
Q

What is formoterol used for?

A
  • Inhaled long-acting beta-2-adrenergic receptor agonist used as a bronchodilator in the management of asthma and COPD
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16
Q

What is the primary drug target of formoterol?

A
  • Beta-2 adrenergic receptor
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17
Q

What is the drug target type of formoterol?

A
  • Receptor agonist
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18
Q

What is the location of action of formoterol?

A
  • Bronchial muscles
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19
Q

What is the mechanism of action of formoterol?

A
  • Bind on beta-2 adrenergic receptors on airway smooth muscle
  • Activation of adenyl cyclase
  • Increase in intracellular concentration of cyclic-3’-5’-adenosine monophosphate
  • Ativation of protein kinase a
  • Decrease in phosphorylation of myosin
  • Decrease in intracellular ionic calcium concentrations
  • Bronchus relaxations
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20
Q

What is the long-acting mechanism of action of formoterol?

A
  • Bind on beta-2 adrenergic receptors on airway smooth muscle
  • Hydrophilic tail of formoterol binds to leucine residues in the exo-site of the receptor almost irreversibly
  • Formoterol persists in the active site (reason for long duration)
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21
Q

What are the main adverse effects of formoterol (5)?

A
  • Trembling (particularly in the hands)
  • Nervous tension
  • Headaches
  • Palpitations
  • Muscle cramps
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22
Q

What is vilanterol used for?

A
  • Inhaled long-acting beta-2-adrenergic receptor agonist used combination with other bronchodilators in the management of COPD, including chronic bronchitis and/or emphysema
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23
Q

What is the primary drug target of vilanterol?

A
  • Beta-2 adrenergic receptor
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24
Q

What is the drug target type of vilanterol?

A
  • Receptor agonist
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25
Q

What is the location of action of vilanterol?

A
  • Bronchial muscles
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26
Q

What is the mechanism of action of vilanterol?

A
  • Bind on beta-2 adrenergic receptors on airway smooth muscle
  • Activation of adenyl cyclase
  • Increase in intracellular concentration of cyclic-3’-5’-adenosine monophosphate
  • Ativation of protein kinase a
  • Decrease in phosphorylation of myosin
  • Decrease in intracellular ionic calcium concentrations
  • Bronchus relaxations
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27
Q

What is the long-acting mechanism of action of vilanterol?

A
  • Bind on beta-2 adrenergic receptors on airway smooth muscle
  • Hydrophilic tail of vilanterol binds to leucine residues in the exo-site of the receptor almost irreversibly
  • Vilanterol persists in the active site (reason for long duration)
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28
Q

What are the main adverse effects of vilanterol (5)?

A
  • Trembling (particularly in the hands)
  • Nervous tension
  • Headaches
  • Palpitations
  • Muscle cramps
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29
Q

What are the 4 main inhaled corticosteroids used to treat asthma?

A
  • Beclomethasone dipropionate
  • Budesonide
  • Fluticasone
  • Mometasone
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30
Q

What is beclomethasone dipropionate used for?

A
  • Maintenance treatment in the prophylaxis of asthma attacks
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31
Q

What is the primary drug target of beclomethasone dipropionate?

A
  • Glucocorticoid receptor
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32
Q

What is the drug target type of beclomethasone dipropionate?

A
  • Receptor agonist
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33
Q

What is the location of action of beclomethasone dipropionate?

A
  • Lungs
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34
Q

What is the mechanism of action of beclomethasone dipropionate?

A
  • Bind on glucocorticoid receptors
  • Receptors dimerize & translocate into the nucleus
  • Bind to glucocorticoid response elements (GRE) on glucocrticoid responsive genes
  • Changes in transcription
  • Inhibit the expression of multiple genes that encode pro-inflammatory factors that are activated during chronic inflammation (i.e. cytokines, chemokines & adhesion molecules)
  • Increase transcritpion of genes coding for anti-inflammatory proteins (i.e. lipocortin-1 & IL-10)
  • Decrease eosinophilia
35
Q

What are the main adverse effects of beclomethasone dipropionate (5)?

A
  • Sore mouth or throat
  • Hoarse or croaky voice
  • Nosebleeds
  • Cough
  • Oral thrush
36
Q

What is budesonide used for?

A

Treatment of:

  • Crohn’s disease
  • Asthma
  • COPD
  • Hay fever and allergies
  • Ulcerative colitis
37
Q

What is the primary drug target of budesonide?

A
  • Glucocorticoid receptor
38
Q

What is the drug target type of budesonide?

A
  • Receptor agonist
39
Q

What is the location of action of budesonide?

A
  • Lungs
40
Q

What is the mechanism of action of budesonide?

A
  • Bind on glucocorticoid receptors
  • Receptors dimerize & translocate into the nucleus
  • Bind to glucocorticoid response elements (GRE) on glucocrticoid responsive genes
  • Changes in transcription
  • Decrease in neutrophil apoptosis and demargination
  • Dcrease in NF-Kappa B and other inflammatory transcription factors
  • Promote anti-inflammatory genes (i.e. IL-10)
  • Decrease in phosphilase A2
  • Decrease formation of arachinoid and derivative
  • Decrease inflammation
41
Q

What are the main adverse effects of budesonide (7)?

A
  • Local side effects:
    • ​Hoarse voice
    • Opportunistic oral infections
  • Systemic side effects:
    • ​Growth retardation in children
    • Hyperglycaemia
    • Decreased bone mineral density
    • Immunosuppression
  • Effects on mood
42
Q

What is fluticasone used for?

A

Treatment of:

  • Corticosteroid responsive dermatoses
  • Asthma
  • COPD
43
Q

What is the primary drug target of fluticasone?

A
  • Glucocorticoid receptor
44
Q

What is the drug target type of fluticasone?

A
  • Receptor agonist
45
Q

What is the location of action of fluticasone?

A
  • Lungs
46
Q

What is the mechanism of action of fluticasone?

A
  • Bind on glucocorticoid receptors
  • Receptors dimerize & translocate into the nucleus
  • Bind to glucocorticoid response elements (GRE) on glucocrticoid responsive genes
  • Changes in transcription
  • Dcrease in NF-Kappa B
  • Decrease in IL-5
  • Decrease in eosinophilia
47
Q

What are the main adverse effects of fluticasone (7)?

A
  • Local side effects:
    • ​Hoarse voice
    • Opportunistic oral infections
  • Systemic side effects:
    • ​Growth retardation in children
    • Hyperglycaemia
    • Decreased bone mineral density
    • Immunosuppression
  • Effects on mood
48
Q

What is mometasone used for?

A
  • Treatment of asthma
49
Q

What is the primary drug target of mometasone?

A
  • Glucocorticoid receptor
50
Q

What is the drug target type of mometasone?

A
  • Receptor agonist
51
Q

What is the location of action of mometasone?

A
  • Lungs
52
Q

What is the mechanism of action of mometasone?

A
  • Bind on glucocorticoid receptors
  • Receptors dimerize & translocate into the nucleus
  • Bind to glucocorticoid response elements (GRE) on glucocrticoid responsive genes
  • Changes in transcription
  • Decrease in phospholipase A2 & lipocortins
  • Decrease in the synthesis of potent mediators of inflammation (i.e. prostaglandins & leukotrienes)
  • Decrease in inflammation
53
Q

What are the main adverse effects of mometasone?

A
  • Local side effects:
    • ​Hoarse voice
    • Opportunistic oral infections
  • Systemic side effects:
    • ​Growth retardation in children
    • Hyperglycaemia
    • Decreased bone mineral density
    • Immunosuppression
  • Effects on mood
54
Q

What is montelukast used for?

A
  • Montelukast is a leukotriene receptor antagonist used as part of an asthma therapy regimen, to prevent exercise induced bronchoconstriction, and to treat seasonal allergic rhinitis
55
Q

What is the primary drug target of montelukast?

A
  • Cysteinyl leukotienes (CysLT) receptor
56
Q

What is the drug target type of montelukast?

A
  • Receptor antagonist
57
Q

What is the location of action of montelukast?

A
  • Eosinophils / Mast cells of airways of smooth muscles
58
Q

What is the mechanism of action of montelukast?

A
  • Binds to CysLT receptors on airway smooth muscle
  • Block the actions of CysLT
  • No stimulation of airway macrophages / eosinophils
  • Decrease in inflammation
59
Q

What are the main adverse effects of montelukast (7)?

A
  • Mild side effects:
    • Diarrhoea
    • Fever
    • Headaches
    • Nausea
    • Vomiting
  • Serious side effects:
    • Mood changes
    • Anaphylaxis
60
Q

What are the 4 main anticholinergics used to treat asthma?

A
  • Ipratropium
  • Tiotropium
  • Achlidinium
  • Glycopyrronium
61
Q

What is ipratropium used for?

A
  • Ipratropium is an anticholinergic drug used in the control of symptoms related to bronchospasm in COPD
62
Q

What is the primary drug target of ipratropium?

A
  • Muscarinic acetylcholine receptor
63
Q

What is the drug target type of ipratropium?

A
  • Receptor antagonist
64
Q

What is the location of action of ipratropium?

A
  • Bronchial muscles
65
Q

What is the mechanism of action of ipratropium?

A
  • Binds on the receptor
  • Stops the activity of acetylcholine in the smooth muscle (generate bronchial secretions & constriction)
  • Prevent contraction & producing relaxed airways
66
Q

What are the main adverse effects of ipratropium (10)?

A
  • Common:
    • ​Dry mouth
    • Constipation
    • Cough
    • Headaches
  • Less common side effects
    • Nausea
    • Palpitations
    • Heartburn
    • Throat irritation
    • Dysphagia
    • Difficulty urinating
67
Q

What is tiotropium used for?

A
  • Tiotropium is a long-acting bronchodilator used in the management of COPD
68
Q

What is the primary drug target of tiotropium?

A
  • Muscarinic acetylcholine receptor
69
Q

What is the drug target type of tiotropium?

A
  • Receptor antagonist
70
Q

What is the location of action of tiotropium?

A
  • Bronchial muscles
71
Q

What is the mechanism of action of tiotropium?

A
  • Binds on the receptor
  • Stops the activity of acetylcholine in the smooth muscle (generate bronchial secretions & constriction)
  • Prevent contraction & producing relaxed airways
72
Q

What are the main adverse effects of tiotropium (10)?

A
  • Common:
    • ​Dry mouth
    • Constipation
    • Cough
    • Headaches
  • Less common side effects
    • Nausea
    • Palpitations
    • Heartburn
    • Throat irritation
    • Dysphagia
    • Difficulty urinating
73
Q

What is aclidinium used for?

A
  • Aclidinium is an inhaled long-acting anticholinergic used as a maintenance bronchodilator in patients with COPD
74
Q

What is the primary drug target of aclidinium?

A
  • Muscarinic acetylcholine receptor
75
Q

What is the drug target type of aclidinium?

A
  • Receptor antagonist
76
Q

What is the location of action of aclidinium?

A
  • Bronchial muscles
77
Q

What is the mechanism of action of aclidinium?

A
  • Binds on the receptor
  • Stops the activity of acetylcholine in the smooth muscle (generate bronchial secretions & constriction)
  • Prevent contraction & producing relaxed airways
78
Q

What are the main adverse effects of aclidinium (10)?

A
  • Common:
    • ​Dry mouth
    • Constipation
    • Cough
    • Headaches
  • Less common side effects
    • Nausea
    • Palpitations
    • Heartburn
    • Throat irritation
    • Dysphagia
    • Difficulty urinating
79
Q

What is glycopyrronium used for?

A
  • Glycopyrronium is an anticholinergic agent used to treat hyperhidrosis, severe drooling, COPD, used with other medications to treat ulcers, and used in anesthesia
80
Q

What is the primary drug target of glycopyrronium?

A
  • Muscarinic acetylcholine receptor
81
Q

What is the drug target type of glycopyrronium?

A
  • Receptor antagonist
82
Q

What is the location of action of glycopyrronium?

A
  • Bronchial muscles
83
Q

What is the mechanism of action of glycopyrronium?

A
  • Binds on the receptor
  • Stops the activity of acetylcholine in the smooth muscle (generate bronchial secretions & constriction)
  • Prevent contraction & producing relaxed airways
84
Q

What are the main adverse effects of glycopyrronium (10)?

A
  • Common:
    • ​Dry mouth
    • Constipation
    • Cough
    • Headaches
  • Less common side effects
    • Nausea
    • Palpitations
    • Heartburn
    • Throat irritation
    • Dysphagia
    • Difficulty urinating

Phase 1b - Pharmacology & Therapeutics (12 decks)

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