Autonomic Pharmacology of Lung

Question 1

Where are nicotinic receptors located?

Answer 1

Adrenal medulla

Question 2

MOA of nicotinic receptors?

Answer 2

Activation of medulla by acting as a sodium pore; releases EPI

Question 3

What NT do nicotinic receptors respond to?

Answer 3

Acetylcholine

Question 4

Nicotine agonist?

Answer 4

Varenicline (Chantix)

Question 5

Name 2 nicotine antagonists

Answer 5

Trimethaphan

Hexamethonium

Question 6

alpha 1 receptor affinities

Answer 6

Epi = norepi&raquo_space;» Iso

Question 7

MOA on an alpha 1 receptor?

Answer 7

Contraction of VSM by stimulating phospholipase C.
Generates inositol trisphosphate
elevates Ca concentration

Question 8

Are alpha 1 receptors in bronchioles?

Answer 8

Nope, so don’t give an alpha 1 agonist in an asthma attack.

Question 9

B2 receptor affinities

Answer 9

Iso > Epi&raquo_space;»> Norepi

Question 10

MOA of B2 receptors?

Answer 10

Relax bronchial smooth muscle (hyperpolarizes potassium channels)
Glycogenolysis by activating adenylyl cyclase

Question 11

What is the natural stimuli for B2 activation in the lung?

Answer 11

Epi

Question 12

Why are shakes a side effect in asthma?

Answer 12

B2 receptors are in skeletal muscle. They are sensitized to ACH and nictotinic receptors.

Question 13

Where are nicotinic receptors located?

Answer 13

Postsynaptic surface of postganglionic nerve (activates post ganglionic nerve)

Question 14

What type of channels are nicotinic receptors?

Answer 14

Sodium

Question 15

Muscarinic receptor MOA?

Answer 15

activate end organ response by activating phospholipase C (Gq) or suppressing adenylyl cyclase activity (Galpha).

Question 16

What does cholera toxin inhibit?

Answer 16

gs alpha - results in an increase in CAMP

Question 17

What does pertussis toxin inhibit?

Answer 17

gi - increase camp

Question 18

Sympathetics and alpha-1

Answer 18

results in constriction

How decongestants work

Question 19

Sympathetics and beta-2

Answer 19

dilation of bronchioles via epi

Question 20

Parasympathetics and bronchioles

Answer 20

results in constriction via muscarinic receptors

increases secretions

Question 21

Most effective bronchospasm therapy?

Answer 21

B2 agonists

Question 22

Name some B2 agonists (result in bronchodilation)

Answer 22

Metaproterenol
terbutaline
albuterol
salmeterol

Question 23

What are some side effects of B2 agonists?

Answer 23

Tachy and palpitations (due to b1 stimulation)
Tremor (skeletal muscle b2 stimulation)
Headache

Question 24

What metabolizes epi?

Answer 24

MOA

COMT

Question 25

Contraindications of epi?

Answer 25

hyperthyroidism hypertension halogen-hydrocarbon anesthetics

Question 26

Isoproterenol

Answer 26

Synthetic catecholamine that relaxes bronchioles via B2

Question 27

Metabolism of Iso?

Answer 27

COMT | Not MAO

Question 28

Ephedrine MOA?

Answer 28

releases NE | increases BP and relaxes bronchioles

Question 29

Pseudoephedrine MOA?

Answer 29

Similar to ephedrine; used to treat nasal congestion

Question 30

Alpha 1 agonist?

Answer 30

Phenylephrine | decongestant, constricts vasculature

Question 31

Name 2 muscarinic receptor antagonists

Answer 31

Ipratropium - bronchodilator for obstructive lung disease | Tiotropium - bronchodilator for COPD

Question 32

Roflumilast

Answer 32

Bronchodilator for COPD improves FEV1 by 11% Nausea reported in 11% of patients

Question 33

Define COPD

Answer 33

Inflammatory disease distinct from asthma that effects 15% of smokers 3rd most common cause of death by 2020

Question 34

Example of a short acting beta agonist?

Answer 34

albuterol

Question 35

Examples of long acting beta agonists?

Answer 35

Salmeterol; formoterol; aformoterol

Question 36

2 examples of glucocorticoids

Answer 36

fluticasone budesonide (questionable usage because of bone disease nad pneumonia)

Question 37

MOA of Roflumilast?

Answer 37

Phosphodiesterase 4 inhibitor

Question 38

Pulmonary side effect of alpha blockers?

Answer 38

Muscosal stiffness | Example drugs: Phentolamine; phenoxybenzamine; prazosin; terazosin

Question 39

Pulmonary side effect of beta blockers?

Answer 39

increase airway resistance; particularly in asthmatics | -any drug with olol at the end

Question 40

If there is an acute attack in an asthmatic patient what is the likely drug culprit?

Answer 40

B blocker

Question 41

Why is Labetalol different from other beta blockers? (think ALOL)

Answer 41

Nonspecific - both B1 and B2

Question 42

What are some NE depleting agents?

Answer 42

Guanethidine; Guanadrel; Reserpine | cause mucosal stiffness

Question 43

This muscarinic agonist can sometimes cause bronchoconstriction

Answer 43

Bethanecol

Question 44

Why are anticholinesterases problematic for the respiratory system?

Answer 44

potentiate ACH actions on muscarinic receptors to cause bronchoconstriction

Question 45

Examples of anticholinesterases?

Answer 45

``` Neostigmine Physostigmine Phyridostigmine Edrophonium Ecothiophate Parathion Malathion Chlorphyrifos Soman ```

Question 46

Why do ACE inhibitors give trouble in the respiratory system?

Answer 46

cause cough and angioedema by preventing the degradation of kinins and kinin like compounds (such as bradykinin) -ACE Inhibitors = -prils

Question 47

Succinylcholine

Answer 47

Typically a depolarizing skeletal muscle paralyzing agent | Causes bronchoconstriction by interacting with pulmonary muscarinic receptors

Question 48

3 drug classes you bronchodilate with?

Answer 48

``` B2 agonists (albuterol) Muscarinic antagonist (Ipratropium, Tiotropium) Phosphodiesterase inhibitor (roflumilast) ```

Question 49

2 drugs to decongest vasculature?

Answer 49

ephedrine | phylephrine

Question 50

Bronchoconstriction as a SE with these drug classes?

Answer 50

B blockers muscarinic agonists (bethanecol) Anticholinesterase (neostigmine)

Question 51

Mucosal congestion as a SE with these drug classes?

Answer 51

``` A1 antagonist (terazosin) NE depleting agents (guanethidine) ```

Question 52

This drug class causes cough and angioedema

Answer 52

ACE inhibitors