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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
What is the location of action of vilanterol?
* Bronchial muscles
26
What is the mechanism of action of vilanterol?
* 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**
27
What is the long-acting mechanism of action of vilanterol?
* 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)
28
What are the main adverse effects of vilanterol (5)?
* Trembling (particularly in the hands) * Nervous tension * Headaches * Palpitations * Muscle cramps
29
What are the 4 main inhaled corticosteroids used to treat asthma?
* Beclomethasone dipropionate * Budesonide * Fluticasone * Mometasone
30
What is beclomethasone dipropionate used for?
* Maintenance treatment in the prophylaxis of **asthma** attacks
31
What is the primary drug target of beclomethasone dipropionate?
* Glucocorticoid receptor
32
What is the drug target type of beclomethasone dipropionate?
* Receptor agonist
33
What is the location of action of beclomethasone dipropionate?
* Lungs
34
What is the mechanism of action of beclomethasone dipropionate?
* 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
What are the main adverse effects of beclomethasone dipropionate (5)?
* Sore mouth or throat * Hoarse or croaky voice * Nosebleeds * Cough * Oral thrush
36
What is budesonide used for?
Treatment of: * Crohn's disease * Asthma * COPD * Hay fever and allergies * Ulcerative colitis
37
What is the primary drug target of budesonide?
* Glucocorticoid receptor
38
What is the drug target type of budesonide?
* Receptor agonist
39
What is the location of action of budesonide?
* Lungs
40
What is the mechanism of action of budesonide?
* 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
What are the main adverse effects of budesonide (7)?
* **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
What is fluticasone used for?
Treatment of: * Corticosteroid responsive dermatoses * Asthma * COPD
43
What is the primary drug target of fluticasone?
* Glucocorticoid receptor
44
What is the drug target type of fluticasone?
* Receptor agonist
45
What is the location of action of fluticasone?
* Lungs
46
What is the mechanism of action of fluticasone?
* 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
What are the main adverse effects of fluticasone (7)?
* **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
What is mometasone used for?
* Treatment of asthma
49
What is the primary drug target of mometasone?
* Glucocorticoid receptor
50
What is the drug target type of mometasone?
* Receptor agonist
51
What is the location of action of mometasone?
* Lungs
52
What is the mechanism of action of mometasone?
* 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
What are the main adverse effects of mometasone?
* **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
What is montelukast used for?
* 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
What is the primary drug target of montelukast?
* Cysteinyl leukotienes (CysLT) receptor
56
What is the drug target type of montelukast?
* Receptor antagonist
57
What is the location of action of montelukast?
* Eosinophils / Mast cells of airways of smooth muscles
58
What is the mechanism of action of montelukast?
* Binds to CysLT receptors on airway smooth muscle * Block the actions of CysLT * No stimulation of airway macrophages / eosinophils * Decrease in inflammation
59
What are the main adverse effects of montelukast (7)?
* **Mild side effects:** * Diarrhoea * Fever * Headaches * Nausea * Vomiting * **Serious side effects:** * Mood changes * Anaphylaxis
60
What are the 4 main anticholinergics used to treat asthma?
* Ipratropium * Tiotropium * Achlidinium * Glycopyrronium
61
What is ipratropium used for?
* Ipratropium is an anticholinergic drug used in the control of symptoms related to bronchospasm in COPD
62
What is the primary drug target of ipratropium?
* Muscarinic acetylcholine receptor
63
What is the drug target type of ipratropium?
* Receptor antagonist
64
What is the location of action of ipratropium?
* Bronchial muscles
65
What is the mechanism of action of ipratropium?
* Binds on the receptor * Stops the activity of acetylcholine in the smooth muscle (generate bronchial secretions & constriction) * Prevent contraction & producing relaxed airways
66
What are the main adverse effects of ipratropium (10)?
* **Common:** * **​**Dry mouth * Constipation * Cough * Headaches * **Less common side effects** * Nausea * Palpitations * Heartburn * Throat irritation * Dysphagia * Difficulty urinating
67
What is tiotropium used for?
* Tiotropium is a long-acting bronchodilator used in the management of COPD
68
What is the primary drug target of tiotropium?
* Muscarinic acetylcholine receptor
69
What is the drug target type of tiotropium?
* Receptor antagonist
70
What is the location of action of tiotropium?
* Bronchial muscles
71
What is the mechanism of action of tiotropium?
* Binds on the receptor * Stops the activity of acetylcholine in the smooth muscle (generate bronchial secretions & constriction) * Prevent contraction & producing relaxed airways
72
What are the main adverse effects of tiotropium (10)?
* **Common:** * **​**Dry mouth * Constipation * Cough * Headaches * **Less common side effects** * Nausea * Palpitations * Heartburn * Throat irritation * Dysphagia * Difficulty urinating
73
What is aclidinium used for?
* Aclidinium is an inhaled long-acting anticholinergic used as a maintenance bronchodilator in patients with COPD
74
What is the primary drug target of aclidinium?
* Muscarinic acetylcholine receptor
75
What is the drug target type of aclidinium?
* Receptor antagonist
76
What is the location of action of aclidinium?
* Bronchial muscles
77
What is the mechanism of action of aclidinium?
* Binds on the receptor * Stops the activity of acetylcholine in the smooth muscle (generate bronchial secretions & constriction) * Prevent contraction & producing relaxed airways
78
What are the main adverse effects of aclidinium (10)?
* **Common:** * **​**Dry mouth * Constipation * Cough * Headaches * **Less common side effects** * Nausea * Palpitations * Heartburn * Throat irritation * Dysphagia * Difficulty urinating
79
What is glycopyrronium used for?
* Glycopyrronium is an anticholinergic agent used to treat hyperhidrosis, severe drooling, COPD, used with other medications to treat ulcers, and used in anesthesia
80
What is the primary drug target of glycopyrronium?
* Muscarinic acetylcholine receptor
81
What is the drug target type of glycopyrronium?
* Receptor antagonist
82
What is the location of action of glycopyrronium?
* Bronchial muscles
83
What is the mechanism of action of glycopyrronium?
* Binds on the receptor * Stops the activity of acetylcholine in the smooth muscle (generate bronchial secretions & constriction) * Prevent contraction & producing relaxed airways
84
What are the main adverse effects of glycopyrronium (10)?
* **Common:** * **​**Dry mouth * Constipation * Cough * Headaches * **Less common side effects** * Nausea * Palpitations * Heartburn * Throat irritation * Dysphagia * Difficulty urinating

Pharmacology & Therapeutics (11 decks)

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