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CRRAB II Week 7 > Autonomic Pharmacology of Respiratory System > Flashcards

Autonomic Pharmacology of Respiratory System Flashcards

1
Q

What class of drugs are often used for COPD? What do they do within the lungs?

A

Muscarinic antagonists

Decrease secretions!!

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2
Q

What structures are involved in the Parasympathetic response?

A
  • Medulla oblongota

- Vagus nerve

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3
Q

What structures are involved in the Sympathetic response?

A
  • Solar plexus

- Chain of sympathetic ganglia

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4
Q

What effects does the Parasympathetic Nervous System have on the body?

A
  • Constricts pupil
  • Stimulates flow of saliva
  • Slows heartbeat
  • Constricts bronchi
  • Stimulates peristalsis and secretion
  • Stimulates release of bile
  • Contracts bladder
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5
Q

What effects does the Sympathetic Nervous System have on the body?

A
  • Dilates pupil
  • Stimulates flow of saliva
  • Accelerates heartbeat
  • Dilates bronchi
  • Inhibits peristalsis and secretion
  • Conversion of glycogen to glucose
  • Secretion of adrenaline and noradrenaline
  • Inhibits bladder contraction
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6
Q

What are the three sympathetic receptors?

A
  • Nicotinic receptor
  • Alpha1 receptor
  • Beta2 receptor
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7
Q

What binds the nicotinic receptor?

A

Acetylcholine, Nicotine

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8
Q

Where is the nicotinic receptor located?

A

On Post-ganglionic Nerve of the Adrenal Medulla.

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9
Q

What does the nicotinic receptor do when it’s stimulated?

A

Acts as a pore for sodium, thus activating the medulla. It causes release of Epinephrine.

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10
Q

What is the mechanism for Varenicline? What is it used for? What is its trade name?

A

Nicotine Agonist. Chantix. It is a great drug for smoking cessation.

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11
Q

How much of COPD is caused by smoking?

A

85%

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12
Q

What is the mechanism of both Trimethaphan & Hexamethonium?

A

Nicotine antagonists

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13
Q

What are the potencies of three main drugs for the Alpha1 receptor?

A

EPI = NE&raquo_space; Isoproterenol

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14
Q

What do alpha1 agonists do?

A

Stimulate phospholipase C —> Generates inositol trisphosphate –> Inc. Ca2+ concentrations –> Contraction of vascular smooth muscle (through alpha1)

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15
Q

Where are alpha1 receptors located?

A

Vascular Smooth Muscle (not on bronchioles)

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16
Q

What is a negative side effect associated with Beta-2 blockers (heart drugs)?

A

Bronchoconstriction!!

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17
Q

What are the potencies of three main drugs for the Beta2 receptor?

A

Isoproterenol > EPI&raquo_space; NE

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18
Q

What do Beta2 agonists do?

A

Activate adenylyl cyclase —> glycogenolysis and relaxation of bronchial smooth muscle

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19
Q

What is a natural stimulus for beta2 receptor activation in the lung?

A

EPINEPHRINE

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20
Q

Why shouldn’t diabetics take beta-blockers?

A

When they take insulin, hypoglycemia is a major risk. If they are taking a beta blocker, they can’t increase glucose through the simplest pathway (sympathetic pathway)

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21
Q

What inhibits stimulation of the presynaptic parasympathetic nerve?

A

Hexamethonium

Mecamylamine

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22
Q

What stimulates the presynaptic parasympathetic nerve?

A

Nicotine & Acetylcholine

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23
Q

What inhibits the post synaptic parasympathetic nerve?

A

Botulinum toxin

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24
Q

What stimulates the post synaptic parasympathetic nerve?

A

Nothing

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25
Q

What stimulates the effector organ of the parasympathetic system?

A
  • Acetylcholine (ACh)
  • Pilocarpine
  • Physostigmine
  • Neostigmine
  • Methacholine
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26
Q

What inhibits the effector organ of the parasympathetic system?

A

Atropine

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27
Q

What inhibits stimulation of the presynaptic sympathetic nerve?

A

Hexamethonium

Mecamylamine

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28
Q

What stimulates the presynaptic sympathetic nerve?

A

Nicotine & Acetylcholine

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29
Q

What stimulates the post synaptic sympathetic nerve?

A
  • Tyramine
  • Amphetamine
  • Ephedrine
  • Metaraminol
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30
Q

What inhibits the post synaptic sympathetic nerve?

A
  • Reserpine

- Guanethidine

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31
Q

What stimulates the effector organ of the sympathetic system?

A
  • NE
  • EPI
  • Isoproterenol
  • Ephedrine
  • Phenylephrine
  • Metaraminol
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32
Q

What inhibits the effector organ of the sympathetic system?

A
  • Phentolamine
  • Phenoxybenzamine
  • Propranalol
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33
Q

What are the two parasympathetic receptors?

A
  1. Nictoinic receptor

2. Muscarinic receptor

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34
Q

Where is the parasympathetic nicotinic receptor? What does it cause?

A

Located on postsynaptic surface of postganglionic nerve.

Causes activation of postganglionic nerve.

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35
Q

What does the parasympathetic muscarinic receptor cause?

A

All end-organ responses by activating phospholipase C or suppressing adenylyl cyclase activity.

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36
Q

What are the major functions of the sympathetic system?

A
  • Constrict vasculature in most beds (alpha1 receptor)

- Dilate bronchioles via Beta2 receptor stimulation

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37
Q

What are the major functions of the parasympathetic system?

A

Constrict bronchioles –> reduces airflow and increases resistance

  • Uses muscarinic recpetors
  • Also increases secretions
38
Q

How do decongestants work?

A

They constrict vasculature via alpha1 receptor.

39
Q

What is the primary endogenous agent causing dilation of bronchioles?

A

Epinephrine (via beta2 receptor stimulation)

40
Q

What does a person exposed to an anti-cholinesterase (pesticide toxicity) look like?

A
  • Sweating a lot
  • Incompetence
  • Pin point pupils
41
Q

What are seven drugs that influence the pulmonary system?

A
  1. Beta2 agonists
  2. Epinephrine
  3. Isoproterenol
  4. Indirectly acting agents
  5. Alpha1 agonists
  6. Muscarinic receptor antagonists
  7. Phosphodiesterase inhibitors
42
Q

What two toxins will activate Gsalpha (G protein linked receptor)?

A
  • Cholera

- Pertussis

43
Q

What does the activation of all G proteins result in?

A

Functional response (Contraction, Relaxation, Secretion, Cell Growth)

44
Q

What does Gialpha lead to?

A
  • Ion channels
  • Inhibition of cAMP
  • Phospholipases
45
Q

What does Gsalpha lead to?

A

-Increased cAMP

46
Q

What does Gqalpha lead to?

A
  • Increased DAG
  • IP3
  • Ca2+
  • –Eventual muscle contraction
47
Q

What does G12,13alpha lead to?

A

-Activates Rho

48
Q

What does gamma beta protein do in G protein-linked receptors?

A
  • Ion channels
  • PI3K
  • Phospholipases
  • Adenylylayclases
  • Receptor kinases
49
Q

What is the most effective acute bronchospasm therapy?

A

Beta2 agonists

50
Q

What beta2 agonists do you need to know?

A
  • Metaproterenol
  • Terbutaline
  • Albuterol
  • Salmeterol (long-acting)
51
Q

How is Metaproterenol administered?

A

Inhalation or oral

52
Q

How is Terbutaline administered?

A

Inhalation or Injection

53
Q

How is Albuterol administered?

A

Inhalation

54
Q

How is Salmeterol administered? How is it used?

A

Inhalation. It is a long-acting bronchodilator given by inhalation. Prophylactically.

55
Q

What is the most common side effect of Beta2 Agonists?

A

Tachycardia

56
Q

What are the long-acting beta2 agonists used for asthma or COPD?

A
  • Formoterol
  • Arformoterol
  • Salmeterol
57
Q

What are the major side effects of Beta 2 agonists?

A
  • Tachycardia and palpitations (beta1 stimulation)
  • Tremor (skeletal muscle beta2 stimulation)
  • Headache
58
Q

If a patient has well controlled asthma, how often should they use short acting beta2 agonists?

A

Twice per week (not counting uses for exercise)

59
Q

What does over use of beta2 agonists cause?

A

Down regulation of beta2 in the lungs –> not as effective

60
Q

How do beta2 agonists cause headache?

A

They vasodilate arteries —> increases pulse pressure —> causes headache

61
Q

How does Epinephrine act? How is it administered?

A

It acts to relax bronchioles. Parental (anaphylaxis), intracellular or inhaled.

62
Q

What metabolizes Epinephrine?

A

MAO or COMT

63
Q

What are contraindications for Epinephrine use?

A
  • Hyperthroidism
  • Hypertension
  • Halogen-hydrocarbon anesthetics
64
Q

What are the therapeutic uses for Epinephrine?

A
  • Bronchospasm (beta2) other than asthma

- Hypersensitivity reactions (beta2 and others)

65
Q

What is the mechanism of Isoproterenol?

A 
Synthetic catecholamine stimulating beta receptors. 
Relaxes bronchioles (beta2).
66
Q

How is Isoproterenol administered?

A

Parenteral

Aerosol

67
Q

How is Isoproterenol metabolized?

A

by COMT (not MAO)

68
Q

What is the therapeutic use for Isoproterenol?

A

Respiratory disease (beta2)

69
Q

What are two indirectly acting agents?

A
  • Ephedrine

- Pseudoephedrine

70
Q

What is the mechanism of Ephedrine?

A

Releases NE and has direct effects

  • -> cardio = increase bp (constricts vasculature)
  • -> respiratory = relaxes bronchioles (weak relaxer)
71
Q

How is Ephedrine administered?

A

Oral

72
Q

What is the toxicity of Ephedrine?

A

Similar to a combination of EPI and amphetamine

73
Q

What are the therapeutic uses of Ephedrine?

A

-Bronchospasm
-Allergy
-Narcolepsy
-Stokes-Adams Syndrome
(in medications for colds)

74
Q

What is Pseudoephedrine and what is it used for?

A
  • Stereoisomer of ephedrine commonly used to treat nasal congestion.
  • Similar to ephedrine.
75
Q

What alpha1 agonist should you know/the only one used clinically?

A

Phenylephrine

76
Q

What is Phenylephrine used for? What does it do?

A

It is used as a decongestant. It constricts vasculature.

77
Q

What two muscarinic receptor antagonists do you need to know? What do they end in?

A

Ipratropium, Tiotropium

-End in -tropium

78
Q

What is Ipratropium and what is it used for?

A

Muscarinic receptor antagonist

  • Bronchodilator for COPD
  • Inhalation
79
Q

What is Tiotropium and what is it used for?

A

Muscarinic receptor antagonist

  • Bronchodilator for COPD
  • Inhalation
80
Q

What is Roflumilast? What is it used for?

A

Phosphodiesterase 4 inhibitor

-Bronchodilator for COPD

81
Q

How does Roflumilast affect FEV? What is this drugs major side effect?

A
  • Improves FEV1 by 11%

- Major side effect is nausea (11% of patients)

82
Q

What is the exact mechanism behind phosphodiesterase 4 inhibitors?

A

They inhibit PDE4 –> increases cGMP –> increased NO –> relaxes bronchioles and smooth muscle –> reduces inflammation

83
Q

What is COPD defined as?

A

Inflammatory disease distinct from asthma

84
Q

How many smokers does COPD effect?

A

15% of smokers

-It is predicted to be the third most common cause of death by 2020

85
Q

What are the four main treatments for COPD?

A
  1. Short acting beta2 agonists (albuterol)
  2. Long acting beta2 agonists (salmeterol; formoterol;aformoterol)
  3. Long acting muscarinic antagonist (tiotropium)
  4. Glucocorticoids (fluticasone, budesonide)
86
Q

What are the two main drugs with pulmonary side effects?

A
  1. Alpha blockers (antagonists)

2. Beta blockers (antagonists)

87
Q

What pulmonary side effects do alpha blockers (antagonists) cause?

A 
Mucosal stuffiness (block alpha1 receptors in vasculature)
-patient feels like they have a cold
88
Q

What are examples of alpha blockers/antagonists?

A
  • Phentolamine
  • Phenoxybenzamine
  • PRAZOSIN
  • TERAZOSIN
89
Q

In what cases are you most likely to see alpha blockers used?

A

Treatment of prostatic hypertrophy (Terazosin!!)

90
Q

What pulmonary side effects do beta blockers (antagonists) cause?

A

Increase airway resistance, particularly in asthmatics (beta2 antagonism) –> potential bronchospasm

91
Q

What are examples of beta antagonists?

A
  • Propranolol
  • Timolol
  • Pindolol
  • Labetalol (alpha1 and beta antagonist)
  • Metoprolol
  • Atenolol
  • Esmolol

CRRAB II Week 7 (8 decks)

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