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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
What stimulates the effector organ of the parasympathetic system?
- Acetylcholine (ACh) - Pilocarpine - Physostigmine - Neostigmine - Methacholine
26
What inhibits the effector organ of the parasympathetic system?
Atropine
27
What inhibits stimulation of the presynaptic sympathetic nerve?
Hexamethonium | Mecamylamine
28
What stimulates the presynaptic sympathetic nerve?
Nicotine & Acetylcholine
29
What stimulates the post synaptic sympathetic nerve?
- Tyramine - Amphetamine - Ephedrine - Metaraminol
30
What inhibits the post synaptic sympathetic nerve?
- Reserpine | - Guanethidine
31
What stimulates the effector organ of the sympathetic system?
- NE - EPI - Isoproterenol - Ephedrine - Phenylephrine - Metaraminol
32
What inhibits the effector organ of the sympathetic system?
- Phentolamine - Phenoxybenzamine - Propranalol
33
What are the two parasympathetic receptors?
1. Nictoinic receptor | 2. Muscarinic receptor
34
Where is the parasympathetic nicotinic receptor? What does it cause?
Located on postsynaptic surface of postganglionic nerve. | Causes activation of postganglionic nerve.
35
What does the parasympathetic muscarinic receptor cause?
All end-organ responses by activating phospholipase C or suppressing adenylyl cyclase activity.
36
What are the major functions of the sympathetic system?
- Constrict vasculature in most beds (alpha1 receptor) | - Dilate bronchioles via Beta2 receptor stimulation
37
What are the major functions of the parasympathetic system?
Constrict bronchioles --> reduces airflow and increases resistance - Uses muscarinic recpetors - Also increases secretions
38
How do decongestants work?
They constrict vasculature via alpha1 receptor.
39
What is the primary endogenous agent causing dilation of bronchioles?
Epinephrine (via beta2 receptor stimulation)
40
What does a person exposed to an anti-cholinesterase (pesticide toxicity) look like?
- Sweating a lot - Incompetence - Pin point pupils
41
What are seven drugs that influence the pulmonary system?
1. Beta2 agonists 2. Epinephrine 3. Isoproterenol 4. Indirectly acting agents 5. Alpha1 agonists 6. Muscarinic receptor antagonists 7. Phosphodiesterase inhibitors
42
What two toxins will activate Gsalpha (G protein linked receptor)?
- Cholera | - Pertussis
43
What does the activation of all G proteins result in?
Functional response (Contraction, Relaxation, Secretion, Cell Growth)
44
What does Gialpha lead to?
- Ion channels - Inhibition of cAMP - Phospholipases
45
What does Gsalpha lead to?
-Increased cAMP
46
What does Gqalpha lead to?
- Increased DAG - IP3 - Ca2+ - --Eventual muscle contraction
47
What does G12,13alpha lead to?
-Activates Rho
48
What does gamma beta protein do in G protein-linked receptors?
- Ion channels - PI3K - Phospholipases - Adenylylayclases - Receptor kinases
49
What is the most effective acute bronchospasm therapy?
Beta2 agonists
50
What beta2 agonists do you need to know?
- Metaproterenol - Terbutaline - Albuterol - Salmeterol (long-acting)
51
How is Metaproterenol administered?
Inhalation or oral
52
How is Terbutaline administered?
Inhalation or Injection
53
How is Albuterol administered?
Inhalation
54
How is Salmeterol administered? How is it used?
Inhalation. It is a long-acting bronchodilator given by inhalation. Prophylactically.
55
What is the most common side effect of Beta2 Agonists?
Tachycardia
56
What are the long-acting beta2 agonists used for asthma or COPD?
- Formoterol - Arformoterol - Salmeterol
57
What are the major side effects of Beta 2 agonists?
- Tachycardia and palpitations (beta1 stimulation) - Tremor (skeletal muscle beta2 stimulation) - Headache
58
If a patient has well controlled asthma, how often should they use short acting beta2 agonists?
Twice per week (not counting uses for exercise)
59
What does over use of beta2 agonists cause?
Down regulation of beta2 in the lungs --> not as effective
60
How do beta2 agonists cause headache?
They vasodilate arteries ---> increases pulse pressure ---> causes headache
61
How does Epinephrine act? How is it administered?
It acts to relax bronchioles. Parental (anaphylaxis), intracellular or inhaled.
62
What metabolizes Epinephrine?
MAO or COMT
63
What are contraindications for Epinephrine use?
- Hyperthroidism - Hypertension - Halogen-hydrocarbon anesthetics
64
What are the therapeutic uses for Epinephrine?
- Bronchospasm (beta2) other than asthma | - Hypersensitivity reactions (beta2 and others)
65
What is the mechanism of Isoproterenol?
``` Synthetic catecholamine stimulating beta receptors. Relaxes bronchioles (beta2). ```
66
How is Isoproterenol administered?
Parenteral | Aerosol
67
How is Isoproterenol metabolized?
by COMT (not MAO)
68
What is the therapeutic use for Isoproterenol?
Respiratory disease (beta2)
69
What are two indirectly acting agents?
- Ephedrine | - Pseudoephedrine
70
What is the mechanism of Ephedrine?
Releases NE and has direct effects - -> cardio = increase bp (constricts vasculature) - -> respiratory = relaxes bronchioles (weak relaxer)
71
How is Ephedrine administered?
Oral
72
What is the toxicity of Ephedrine?
Similar to a combination of EPI and amphetamine
73
What are the therapeutic uses of Ephedrine?
-Bronchospasm -Allergy -Narcolepsy -Stokes-Adams Syndrome (in medications for colds)
74
What is Pseudoephedrine and what is it used for?
- Stereoisomer of ephedrine commonly used to treat nasal congestion. - Similar to ephedrine.
75
What alpha1 agonist should you know/the only one used clinically?
Phenylephrine
76
What is Phenylephrine used for? What does it do?
It is used as a decongestant. It constricts vasculature.
77
What two muscarinic receptor antagonists do you need to know? What do they end in?
Ipratropium, Tiotropium | -End in -tropium
78
What is Ipratropium and what is it used for?
Muscarinic receptor antagonist - Bronchodilator for COPD - Inhalation
79
What is Tiotropium and what is it used for?
Muscarinic receptor antagonist - Bronchodilator for COPD - Inhalation
80
What is Roflumilast? What is it used for?
Phosphodiesterase 4 inhibitor | -Bronchodilator for COPD
81
How does Roflumilast affect FEV? What is this drugs major side effect?
- Improves FEV1 by 11% | - Major side effect is nausea (11% of patients)
82
What is the exact mechanism behind phosphodiesterase 4 inhibitors?
They inhibit PDE4 --> increases cGMP --> increased NO --> relaxes bronchioles and smooth muscle --> reduces inflammation
83
What is COPD defined as?
Inflammatory disease distinct from asthma
84
How many smokers does COPD effect?
15% of smokers | -It is predicted to be the third most common cause of death by 2020
85
What are the four main treatments for COPD?
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
What are the two main drugs with pulmonary side effects?
1. Alpha blockers (antagonists) | 2. Beta blockers (antagonists)
87
What pulmonary side effects do alpha blockers (antagonists) cause?
``` Mucosal stuffiness (block alpha1 receptors in vasculature) -patient feels like they have a cold ```
88
What are examples of alpha blockers/antagonists?
- Phentolamine - Phenoxybenzamine - PRAZOSIN - TERAZOSIN
89
In what cases are you most likely to see alpha blockers used?
Treatment of prostatic hypertrophy (Terazosin!!)
90
What pulmonary side effects do beta blockers (antagonists) cause?
Increase airway resistance, particularly in asthmatics (beta2 antagonism) --> potential bronchospasm
91
What are examples of beta antagonists?
- Propranolol - Timolol - Pindolol - Labetalol (alpha1 and beta antagonist) - Metoprolol - Atenolol - Esmolol

CRRAB II Week 7 (8 decks)

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