10 - Respiratory Pharmacology

Question 1

What is the rationale for using inhaled medications for pulmonary disease?

Answer 1

• lower doses
• faster onset of action
• minimizes side effects by limiting systemic absorption

Question 2

What are the types of inhaled medications? What meds are only available orally?

Answer 2

Inhaled:

• short/long acting beta agonists
• short/long acting muscarinic/cholinergic antagonists
• inhaled corticosteroids

Orally:
- leukotriene modifiers

Question 3

What is albuterol’s mechanism of action?

Answer 3

• short acting beta-2 agonist (SABA)
• via adenyl cyclate, increases cAMP –> increases Ca2+ efflux
• relaxes smooth muscles (bronchodilation)
• has some beta-1 effects that lead to side effects

Question 4

What are the side effects of albuterol?

Answer 4

Nonspecific Beta-1 side effects:

• tremor
• tachycardia
• hypertension

Question 5

What is albuterol’s onset of action and duration?

Answer 5

Rapid onset (10-20 minutes) and moderate duration (4-6 hours)

Question 6

Albuterol is a [short/long]-acting beta-2 agonist.

Answer 6

short

Question 7

Salmeterol has a [slow/fast] onset and [short/moderate/long] duration.

Answer 7

slow onset, long duration

Question 8

Formoterol has a [slow/fast] onset and [short/moderate/long] duration.

Answer 8

fast onset, long duration

Question 9

Sympathetic stimulation causes [bronchoconstriction/bronchodilation]

Answer 9

bronchodilation

Question 10

Because they are not anti-inflammatory, ___ should not be used as a monotherapy for asthma.

Answer 10

long acting beta-2 agonists

Question 11

Anticholinergics/antimuscarinics block [sympathetic/parasympathetic] receptors, leading to [bronchoconstriction/bronchodilation].

Answer 11

block parasympathetic –> bronchodilation

Question 12

What type of medication is ipratropium?

Answer 12

Short acting antimuscarinic (4-6 hours)

Question 13

What type of medication is tiotropium?

Answer 13

Long acting antimuscarinic (24 hours)

Question 14

What is the major side effect of antimuscarinics?

Answer 14

Dry mouth

Question 15

What are the effects of theophylline? Why isn’t it commonly used anymore?

Answer 15

• bronchodilator
• anti-inflammatory
• respiratory stimulant
• improves respiratory muscle function

Has a narrow therapeutic range, significant toxicity, and is metabolized by cytochrome P450 (drug interactions)

Question 16

How are leukotriene antagonists administered?

Answer 16

Orally

Question 17

In what 2 ways do leukotriene antagonists work?

Answer 17

• inhibit 5-lipoxygenase (from creating leukotrienes)

- block leukotriene receptors

Question 18

What are the effects of leukotriene antagonists? What type of asthma medication is it?

Answer 18

Mostly anti-inflammatory with some bronchodilating effects.

Used as a control medication to improve FEV1 and decrease airway eosinophils (also used in exercise-induced bronchospasm)

Question 19

What are the principal effects of inhaled corticosteroids?

Answer 19

anti-inflammatory agents (decreases the amounts of lymphocytes, mast cells, and eosinophils and associated cytokines)

Question 20

What is the mainstay anti-inflammatory medication for asthma?

Answer 20

Inhaled corticosteroids

Question 21

What is the effect of Roflumilast?

Answer 21

PDE-4 inhibitor (increases cAMP) –> weak bronchodilator

Question 22

What is the effect of Cromolyn?

Answer 22

block histamine and leukotriene release from mast cells

Question 23

What is the effect of Nedocromil?

Answer 23

blocks histamine and leukotriene release from mast cells; blocks mediator release from eosinophils, macrophages, platelets

similar to Cromolyn

Question 24

cAMP, which is formed using ___, leads to [bronchoconstriction/bronchodilation].

Answer 24

Adenylate cyclase creates cAMP from ATP –> bronchodilation

Question 25

How do beta 2 agonists lead to smooth muscle relaxation?

Answer 25

Stimulate adenylate cyclase, which creates cAMP from ATP. cAMP build up leads to bronchodilation

Question 26

What advantage does salmeterol have over albuterol in terms of administration?

Answer 26

It is inhaled as a dry powder, which is much easier than a spray (albuterol is a spray)

Question 27

How do corticosteroids reduce inflammation?

Answer 27

They block phospholipases, which are the enzymes needed to convert arachidonic acid into the various inflammatory molecules --> has a broad anti-inflammatory effect because it blocks the beginning of the inflammatory pathway

Question 28

What is the most common inhaled corticosteroid in the US?

Answer 28

Fluticasone propionate (Diskus)

Question 29

How do leukotriene modifiers reduce inflammation?

Answer 29

They block the formation of leukotrienes or block leukotriene-receptor binding --> reduce the effects of leukotrienes (bronchoconstriction, mucus secretion, edema, eosinophil recruitment)

Question 30

Acetylcholine leads to [bronchoconstriction/bronchodilation].

Answer 30

bronchoconstriction

Question 31

How do muscarinic antagonists reduce bronchoconstriction?

Answer 31

they block acetylcholine from binding to muscarinic receptors, blocking parasympathetic bronchoconstriction

Question 32

How does treatment differ for COPD and asthma?

Answer 32

Asthma requires corticosteroids/anti-inflammatory agents. COPD does not

Question 33

What respiratory illness are monoclonal antibodies used for?

Answer 33

allergic asthma

Question 34

What is the most important monoclonal antibody side effect?

Answer 34

hypersensitivity reaction, usually to humanized antibodies