Autonomic Pharmacology of the Respiratory System - Trachte Flashcards

1
Q

What is the autonomic innervation of the lung, including neurotransmitters and receptors?

A
  • Sympathetic Innervation ⇒ dilates bronchi
    • ACh → Nicotinic Receptors on postgangilionic nerve
    • Epi → Alpha-1 Receptors on vascular smooth muscle
    • Epi → Beta-2 Receptors on bronchial smooth muscle
  • Parasympathetic Innervation ⇒ constricts bronchi
    • ACh → Nicotinic Receptors on postsynaptic surface of postganglionic nerve
    • ACh → Muscarinic Receptors on lung
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2
Q

What is the major function of sympathetics on the respiratory system?

A
  • Constrict the vasculature in most beds via Alpha-1 receptor stimulation (Epi)
    • this is how decongestants work
  • Dilate bronchioles via Beta-2 receptor stimulation (Epi)
    • this is how bronchodilators work
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3
Q

What is the major function of parasympathetics on the respiratory system?

A
  • Constrict bronchioles via Muscarinic receptors (ACh)
  • Also increases secretions → plugs airways
    • that’s why we use muscarinic antagonists to decrease secretions (mucus)
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4
Q

What are the general categories of drugs that affect the Pulmonary System?

A
  • Beta-2 antagonists
  • Epinephrine
  • Isoproterenol
  • Indirectly acting agents
  • Alpha-1 agonists
  • Muscarinic receptor antagonists
  • Phosphodiesterase inhibitors
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5
Q

What is the most effective acute bronchospasm therapy?

A

Beta-2 Agonists:

  • Metaproterenol
  • Albuterol
  • Terbutaline
  • Salmeterol
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6
Q

What Beta-2 Agonist is a long-acting bronchodilator given by inhalation and used prophylactically?

A

Salmeterol

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7
Q

What major Respiratory System drugs are less likely to cause increased HR when they are inhaled, but have major side effects of tachycardia, palpitations, tremor, and headache?

How do you explain the side effects?

A

Beta-2 Agonists

  • Tachycardia & Palpitations → due to Beta-1 stimulation
  • Tremor → skeletal muscle Beta-2 stimulation
    • sensitize Beta-2 receptors to Epi
  • Headache → vasodilation of blood vessels in the brain due to Beta-2 stimulation
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8
Q

How often should Beta-2 Agonists be used?

A

If asthma is well controlled, should only use short-acting Beta-2 agonists twice per week.

(not counting uses for exercise)

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9
Q

What major Respiratory System drug is used to relax bronchioles (Beta-2), treat bronchospasm (Beta-2) and hypersensitivity reactions (Beta-2 and others), but should not be used for asthma due to severe side effects?

A

Epinephrine

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10
Q

How is Epinephrine metabolized?

A

MAO and COMT

(monoamine oxidase and catechol-O-methyl transferase)

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11
Q

What major Respiratory System drug is a synthetic catecholamine stimulating Beta receptors and could be used to relax bronchioles (Beta-2)?

A

Isoproterenol

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12
Q

How is Isoproterenol metabolized?

A

MAO and COMT

(monoamine oxidase and catechol-O-methyl transferase)

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13
Q

What are the two Indirectly Acting Agents used for respiratory system treatments?

A

Ephedrine and Pseudoephedrine

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14
Q

What Respiratory System drug releases norepinephrine by reversing the NE Transporter having direct effects on cardiovascular (increase BP) and respiratory (relaxes bronchioles), and is most commonly used as a nasal decongestant?

A

Ephedrine

(increased NE → stimulates Alpha-1/Beta-2 → constricts vasculature)

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15
Q

What Respiratory System drug releases norepinephrine by reversing the NE transporter consequently stimulating Alpha-1 receptors in the nasopharynx resulting in vasculature constriction of the blood vessels and decreased nasal congestion?

(Hint: stereoisomer of ephedrine)

A

Pseudoephedrine

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16
Q

What Respiratory System drug is an Alpha-1 Agonist that is used as a decongestant because it constricts vasculature?

A

Phenylephrine

(Donatussin, Duo-Medihaler, Albatussin, Neosynephrine)

17
Q

What Respiratory System drugs are Muscarinic receptor antagonists that act as bronchodilators for chronic obstructive lung disease by taking the bronchiole tone away?

A

Ipratropium (Atrovent)

Tiotropium (Spiriva)

***Anything ending in “–tropium”

18
Q

What two Respiratory System drug classes act on parasympathetics?

A

Muscarinic receptor antagonists

&
Phosphodiesterase 4 inhibitors

19
Q

What Respiratory System drug is a Phosphodiesterase 4 Inhibitor and acts as a bronchodilator for chronic obstructive pulmonary disease by stopping the breakdown of cAMP/cGMP and thus preventing bronchoconstriction?

A

Roflumilast (Daliresp)

20
Q

What is the major side effect of Phosphodiesterase 4 Inhibitors?

A

Nausea

21
Q

What are the four drug classes used to treat COPD?

A
  1. Short acting Beta-2 agonists
    • Albuterol, etc.
  2. Long acting Beta-2 agonists
    • Salmeterol, formoterol, aformoterol
  3. Long acting Muscarinic antagonist
    • Tiotropium
  4. Glucocorticoids
    • Fluticasone, Budesonide
22
Q

What respiratory side effect is often experienced when taking Alpha-Blockers which block Alpha-1 receptors in vasculature?

(Examples: Phentolamine, Phenoxybenzamine, PRAZOSIN, TERAZOSIN, Tamsulosin (Flomax))

A

Mucosal stuffiness → feel like ya got a cold!

23
Q

What respiratory side effect is often experienced when taking Beta-Blockers?

(Examples: Propranolol, Timolol, Pindolol, Labetalol, Metoprolol, Atenolol, Esmolol)

A

Increased airway resistance

(particularly asthmatics)

24
Q

What respiratory side effect is often experienced when taking Norepinephrine-depleting agents?

(Examples: Guanadrel, Reserpine)

A

Mucosal stuffiness

(no vascular constriction in nasopharynx)

25
Q

What respiratory side effect is often experienced when taking Muscarinic agonists?

(Examples: Bethanecol)

A

Bronchoconstriciton

(stimulation of parasympathetic muscarinic receptors → constricts bronchi)

26
Q

What respiratory side effect is often experienced when taking Anticholinesterases?

(Examples: Neostigmine, Physostigmine, Pyridostigmine, Edrophonium, Ecothiophate, Parathion, Malathion, Chlorpyrifos (insecticide), Soman)

A

Potentiate acetylcholine actions on parasympathetic muscarinic receptors → cause bronchoconstriction

27
Q

What respiratory side effect is often experienced when taking Acetylcholine-like molecules such as Succinylcholine?

A

Succinylcholine = depolarizing skeletal muscle paralyzing agent

Interacts with pulmonoary muscarinic receptors (parasympathetic) → causing bronchoconstriction

28
Q

What respiratory side effect is often experienced when taking Angiotensin Converting Enzyme Inhibitors?

(Examples: Captopril, Enalapril, Lisinopril)

A

Cough and angioedema

(probably by preventing degradation of kinins and kinin-like compounds)

29
Q

What four specific respiratory system drugs can you bronchodilate with?

A
  • Albuterol = Beta-2 agonist
  • Ipratropium/Tiotropium = muscarinic antagonist
  • Roflumilast = phosphodiesterase inhibitor
30
Q

What two specific respiratory system drugs can you decongest vasculature with?

A

Ephedrine/Pseudoephedrine & Phenylephrine

(Releases NE & Alpha-1 agonist)

31
Q

What three drug classes cause bronchoconstriction as an adverse side effect?

A
  • Beta-Blockers (Propranolol)
  • Muscarinic Agonists (Bethanecol - mushrooms)
  • Anticholinesterases (Neostigmine)
32
Q

What two drug classes cause mucosal congestion as an adverse side effect?

A
  • Alpha-1 Antagonist (Terazosin)
  • Norepinephrine-depleting agents (Guanethidine)