Adrenergics - Non-Catecholamines

Question 1

Are adrenergic non-catecholamines direct or indirect acting? Are they agonists or antagonists?

Answer 1

Direct

Agonists

Question 2

What is the route of administration for phenylepherine? What are two exceptions?

Answer 2

Can be given orally
IV - when treating shock (hypotention)
Nasal decongestant comes in a nasal spray

Question 3

What receptor does phenylepherine act on?

Answer 3

A1 only

Question 4

What are the therapeutic effects of phenylepherine?

Answer 4

Increase BP (systolic and diastolic), decrease blood flow, decreases heart rate b/c of reflex from increased BP

Question 5

What are the therapeutic uses of phenylepherine? (4) Which is the most significant and why?

Answer 5

Opthalmic - dilate pupil, decrease hemorrhage, conjunctivial decongestion
W/ local anesthetics to increase duration of action
Treatment of hypotention (in cases of shock) -> in this case would give IV
Nasal decongestant - most significant b/c OTC and is in an oral or nasal spray

Question 6

What receptor does clonidine act on?

Answer 6

A2 - selective to CNS

Question 7

What are the therapeutic effects of clonidine?

Answer 7

Decrease BP (prolonged)
Decrease peripheral resistance, HR, and CO

Question 8

What are the therapeutic uses of clonidine?

Answer 8

reduce sympathetic outflow (HTN)

Question 9

What is the route of administration of clonidine?

Answer 9

can be given orally

Question 10

What is the effect of clonidine when not in the CNS? and Why?

Answer 10

NOT AFFECTIVE!! It is a direct agonist of A2 receptors in the CNS and will not produce those effects outside of CNS. Works in post synaptic neurons in the CNS.

Question 11

What are the side effects of clonidine?

Answer 11

Sedation, dry mouth, edema, rebound HTN with sudden discontinuation

Question 12

What receptor does albuterol act on?

Answer 12

B2

Question 13

What is the duration of action of albuterol?

Answer 13

3-6 hours - short acting

Question 14

What is the major therapeutic effect and use of albuterol?

Answer 14

Bronchodilation in acute asthma attacks

Question 15

What is the route of administration of albuterol?

Answer 15

Inhalation mainly

Also available as oral tablets

Question 16

What are the side effects of albuterol?

Answer 16

Tachycardia, tremor, anxiety

Question 17

What greatly reduces the side effects of albuterol?

Answer 17

Administration by inhalation

Question 18

What are the significant substitutions to the chemical compound and why are they significant (2)?

Answer 18

CH2 b/f one of the OH groups -> not absorbed by catechol-methyltransferase so is relatively longer acting
Substitution on amine allows for selectivity of B2 over B1

Question 19

What receptor does Salmeterol act on?

Answer 19

B2

Question 20

What is the effect of salmeterol?

Answer 20

bronchodilation

Question 21

What are the major therapeutic uses of salmeterol?

Answer 21

COPD, nocturnal asthma, persistent asthma

Question 22

What is the duration of action of salmeterol? Why?

Answer 22

12h
Substitution on amine makes it very lipophilic -> means it hangs out in the lungs longer -> prevents metabolism
Not degraded by catechol-methylstransferase (b/c same substitution)

Question 23

Is Salmeterol useful for acute asthma attacks?

Answer 23

No b/c slow onset of action

Question 24

What is the mode of administration of salmeterol?

Answer 24

Inhalation