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Pharmacology > Bronchodilators and Antimuscarinics > Flashcards

Bronchodilators and Antimuscarinics Flashcards

1
Q

Which limb of the nervous system causes bronchodilation?

A

By stimulating the sympathetic or blocking the parasympathetc.

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2
Q

What is adrenergic stimulation?

A

Stimulation of the sympathetic nervous system.

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3
Q

What are beta-2 receptors?

A

G-protein receptors that are responsible for smooth muscle relaxation. SYMPATHETIC BRONCHODILATION.

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4
Q

How do beta-2 receptors cause bronchodilation?

A

They are G-proteins that when stimulated go on to stimulate adenyl cyclase which converts ATP into cAMP. cAMP increases activation of protein kinase A which prevents myosin and actin interaction, causing smooth muscle relaxation.

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5
Q

What are catecholamines?

A

A class of aromatic amines (neurotransmitters) like epinephrine and norepinephrine that cause sympathetic stimulation throughout the body.

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6
Q

What breaks down catecholamines?

A

catechol O-methyltransferase (COMT).

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7
Q

How do epinephrine and norepinephrine cause bronchodilation?

A

By stimulating SYMPATHETIC (beta-2) receptors.

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8
Q

How do we extend the half-life of catecholamine drugs?

A

Because they are metabolized by COMT, we can change the structure so that COMT cannot recognize and break down the drug.

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9
Q

What are SABA drugs and what are they used for?

A

Short acting beta adrenergics (agonists) and they are used as rescue or reliever drugs.

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10
Q

Which isomer of salbutamol is responsible for bronchodilation and how does that help us?

A

The R-isomer; there is an R-isomer only formula called levosalbutamol so that there are more molecules that are able to cause bronchodilation.

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11
Q

How long do LABA drugs last?

A

12-24 hours

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12
Q

What are some other names for muscarinic antagonists?

A
  • antimuscarinics
  • cholinergic blockers
  • parasympatholytics
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13
Q

What are the two primary effects of parasympathetic innervation?

A

Bronchoconstriction and an increase in mucous production.

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14
Q

What are the main parasympathetic neurotransmitters?

A

Acetylcholine (ACh) which stimulates muscarinic 3 (M3) receptors.

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15
Q

What enzyme terminates the action of ACh?

A

Acetylcholinesterase.

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16
Q

Which nerve innervates the lungs?

A

The vagus nerve.

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17
Q

What are the three muscarinic receptors and where are they found?

A

M1: parasympathetic ganglia
M2: heart and postganglionic parasympathetic nerves
M3: airway smooth muscle and submucosal glands.

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18
Q

What muscarinic receptor do we tend to target?

A

M3

19
Q

What happens when M3 receptors are stimulated?

A

A chain effect is set off, the end result of which is Ca2+ rushing into cells causing smooth muscle contraction.

20
Q

What is the afferent signal caused by irritants in the airway transmitted by?

A

C fibres

21
Q

What is the only common short acting muscarinic antagonist?

A

Ipratropium bromide (atrovent).

22
Q

Describe the duration, use, delivery, and MOA of Aclidinium (Tudorza Genuair).

A

12 hrs, step-up medication, DPI, LAMA

23
Q

Describe the duration, use, delivery, and MOA of Salbutamol (Ventolin)

A

<6 hrs, tx of acute issues, MDI, DPI, SVN, IV, oral, and is a SABA.

24
Q

What is levosalbutamol?

A

A form of salbutamol that contains only the R-isomer (active isomer; S-isomer is inactive).

25
Q

Describe the duration, use, delivery, and MOA of Terbutaline (bricanyl).

A

<6 hours, tx of acute issues, MDI, SABA

26
Q

Describe the duration, use, delivery, and MOA of Salmeterol.

A

12 hrs, chronic conditions, DPI, LABA.

27
Q

Describe the duration, use, delivery, and MOA of Formoterol (Oxeze, Foradil).

A

12 hrs, chronic conditions,

DPI, LABA.

28
Q

Describe the duration, use, delivery, and MOA of Indacaterol (Onbreze inhaler).

A

24 hrs, chronic conditions, DPI, LABA.

29
Q

Describe the duration, use, delivery, and MOA of Vilanterol.

A

24 hrs, chronic conditions, only as combo with Umeclidinium, LABA.

30
Q

Describe the duration, use, delivery, and MOA of Olodaterol (striverdi Respimat).

A

24 hrs, chronic conditions, SMI, LABA.

31
Q

Describe the duration, use, delivery, and MOA of Ipratropium bromide.

A

4-6 hrs, acute issues, MDI or SVN, SAMA.

32
Q

Describe the duration, use, delivery, and MOA of Aclinidium (Tudorza Genuair).

A

12 hrs, severe chronic conditions and step up, DPI, LAMA.

33
Q

Describe the duration, use, delivery, and MOA of Tiotropium bromide (Spiriva).

A

24 hrs, DPI or SMI, severe chronic conditions or step up, LAMA.

34
Q

Describe the duration, use, delivery, and MOA of Glycopyrronium bromide (Sebri breezehaler).

A

24 hrs, severe chronic conditions or step up, DPI, LAMA.

35
Q

Describe the duration, use, delivery, and MOA of Umeclidinium (Incruse Ellipta).

A

24 hrs, severe chronic conditions or step up, DPI, LAMA.

36
Q

What are the LABA/LAMA combinations?

A

Indacterol and Glycopyrronium, Vilanterol and Umeclidinium, Formoterol and Umeclidinium, and Olodaterol and Tiotropium.

37
Q

How are LABA/LAMA combinations used?

A

Generally for COPD tx when monodrug therapy is no longer effective. Taken routinely (ex. once daily) and not PRN.

38
Q

What is the Combivent Respimat?

A

The device name for the SMI that combines Atrovent and Ventolin.

39
Q

What are two indirect cholinergic stimulants?

A

Neostigmine and pyridostigmine.

40
Q

What are indirect cholinergic stimulants used for?

A

Reversal of paralysis inducing drugs, increasing muscle contraction in myasthenia gravis, and increasing gastric motility.

41
Q

What is the name of a direct acting cholinergic?

A

Methacoline, it mimics Ach

42
Q

How is methacholine administered?

A

via nebulizer.

43
Q

What does methacholine do and what is it used for?

A

Causes bronchoconstriction and is used to assess severity of asthma.

Pharmacology (10 decks)

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