Resp Drugs Flashcards

1
Q

What are the two classes of β2-adrenoceptors Agonists?

A
  • SABA (short acting beta agonist)

- LABA (long acting beta agonist)

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2
Q

What is the first line SABA used?

A

Salbutamol

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3
Q

What are the two types of LABA used?

A
  • Salmeterol

- Formoterol

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4
Q

What conditions are β2-adrenoceptors Agonists used to treat?

A
  • Asthma

- COPD

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5
Q

What is the mechanism of β2-adrenoceptors Agonists?

A
  • Coupled with G proteins
  • Binding stimulates adenylyl cyclase which then converts ATP to cAMP
  • Phsophodiesterase breaks down cAMP
  • So Ca++ levels are decreased, formation to protein kinase A is increased
  • Myosin light chain is phosphorylated by protein kinase A
  • Bringing about realxation of bronchi smooth muscle
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6
Q

What are the side effects of β2-adrenoceptors Agonists?

A
  • Fine tremor
  • Hypotension
  • Tachycardia
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7
Q

What are two examples of cysteinyl leukotriene receptor (CysLT1) antangonists?

A
  • Montelukast

- Zafirlukast

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8
Q

What are CysLT1 antagonists and mast cell stabilisers used to treat?

A
  • Asthma

- Rhinitis

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9
Q

What is the mechanism of CysLT1 Antagonists?

A

(CysLT) are derived from mast cells

  • Mast cells produce arachidonic acid through stimulating phospholipase A2
  • FLAP enzyme stimulates 5-lopoxygenase
  • Leukotrienes are released which bind to CysLT1
  • CAUSES muscle contraction, mucus secretion and oedema
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10
Q

What do CYsLT1 antagonists prevent from binding?

A

Leukotrienes (cause inflammation)

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11
Q

What are the side effects of CysLT1 antagonitss and mast cell stabilisers?

A
  • Abdominal Pain
  • Headaches

“on a boat, the mast can hit you in the head or the stomach”

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12
Q

What are two examples of xanthines?

A
  • Theophylline

- Aminophylline

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13
Q

What are xanthines used in the treatment of?

A

Asthma

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14
Q

What is the mechanism of xanthines?

A
  • Inhibit phosphodiesterase (breaks down cAMP)
  • Increase in cAMP levels
  • Decreases protein kinase A
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15
Q

Give an example of an inhaled corticosteroid?

A

Beclometasone

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16
Q

Give an example of an oral corticosteroid?

A

Predinsolone

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17
Q

What are corticosteroids used in the treatment of?

A
  • Asthma

- Rhinitis

18
Q

When would oral corticosteroids be used in the case of asthma?

A

When it is very severe

19
Q

What is the mechanism of action of corticosteroids?

A
  • Signalling via nuclear receptors GRα, where glucocorticoid binds to GRα and enters nucleus
  • Binds to promotor region
  • Either produces transactivation or transrepression of genes
20
Q

How do corticosteroids transactivate genes?

A
  • Annexin-1 inhibits synthesis of phospholipase A1
  • Decreases formation of arachidonic acid
  • Decreases production of leukotrienes, chemotaxins and spasmogens
21
Q

How do corticosteroids transrepress genes?

A
  • Cytokines used to decrease formation of IL4,5,7 and 13

- Eosinophils and plasma cells (IgE are not recruited)

22
Q

What are side effects of corticosteroids?

A
  • Thrush
  • Hoarse/weak voice
  • Restricts growth
  • Glaucoma
  • Diabetes
  • Cushing’s syndrome (weight gain, bruises, stretch marks)
23
Q

What is cromoglicate used for?

A
  • Allergic asthma

- Allergic rhinitis

24
Q

What is omalizumab used for?

A

Allergic asthma

25
Q

What is the mechanism of omalizumab?

A
  • Monoclonal antibody treatment against IgE
26
Q

What are the side affects of xanthines?

A
  • Nausea
  • Vomiting
  • Headache
27
Q

What are the two classes of Muscarinic Ach Antaognists of M3 Receptors?

A
  • SAMA (short acting muscarinic antagonist

- LAMA (long acting muscarinic antagonist)

28
Q

Give an example of a SAMA

A

Ipratropium (non-selective)

29
Q

Give an example of a LAMA

A

Tiotropium (selective for M3 receptors)

30
Q

What are muscarinic antagonists used for?

A
  • COPD (can be used in combo with inhalers)

- Rhinitis (decreases watery secretions)

31
Q

What is the mechanism of muscarinic antagonists?

A

Prevents binding of antagonists and gives the response…

  • Activated M3 acts on Gg coupled protein
  • Increases the formation of phospholipase C
  • Pip2 degrades phospholipase C into IP3
  • Releases calcium
  • Smooth bronchi muscle contracts
32
Q

What are the side effects of muscarinic antagonists?

A
  • Dry mouth
  • Dizziness
  • Thrush
  • Disturbes tase
33
Q

What are anti-histamines used to treat?

A

Allergic rhinitis

34
Q

Give an example of an anti-histamine

A

Loratadine

35
Q

What is the mechanism of anti-histamines?

A

Reduces effects of activation of mast cells

36
Q

What are the side effects of anti-histamines?

A
  • Drowsiness
  • Palpitations
  • Hypotension
37
Q

What are vasoconstrictors used for?

A

Rhinitis

38
Q

What do vasoconstrictors do?

A

Mimics effect of noradrenaline

39
Q

Give an example of a vasoconstrictor

A

Oxymetazoline

40
Q

What is roflumilast used for?

A

COPD

41
Q

How does rofumilast work?

A

Long acting PDE4 inhibitor