Autonomic Pharmacology of the Respiratory System - Trachte Flashcards
What is the autonomic innervation of the lung, including neurotransmitters and receptors?
-
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
What is the major function of sympathetics on the respiratory system?
- 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
What is the major function of parasympathetics on the respiratory system?
- Constrict bronchioles via Muscarinic receptors (ACh)
- Also increases secretions → plugs airways
- that’s why we use muscarinic antagonists to decrease secretions (mucus)
What are the general categories of drugs that affect the Pulmonary System?
- Beta-2 antagonists
- Epinephrine
- Isoproterenol
- Indirectly acting agents
- Alpha-1 agonists
- Muscarinic receptor antagonists
- Phosphodiesterase inhibitors
What is the most effective acute bronchospasm therapy?
Beta-2 Agonists:
- Metaproterenol
- Albuterol
- Terbutaline
- Salmeterol
What Beta-2 Agonist is a long-acting bronchodilator given by inhalation and used prophylactically?
Salmeterol
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?
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
How often should Beta-2 Agonists be used?
If asthma is well controlled, should only use short-acting Beta-2 agonists twice per week.
(not counting uses for exercise)
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?
Epinephrine
How is Epinephrine metabolized?
MAO and COMT
(monoamine oxidase and catechol-O-methyl transferase)
What major Respiratory System drug is a synthetic catecholamine stimulating Beta receptors and could be used to relax bronchioles (Beta-2)?
Isoproterenol
How is Isoproterenol metabolized?
MAO and COMT
(monoamine oxidase and catechol-O-methyl transferase)
What are the two Indirectly Acting Agents used for respiratory system treatments?
Ephedrine and Pseudoephedrine
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?
Ephedrine
(increased NE → stimulates Alpha-1/Beta-2 → constricts vasculature)
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)
Pseudoephedrine