Selective B2 Agonists

Question 1

B2 agonists

Answer 1

Selectively agonize B2

Question 2

B2 receptors does what? Stimulate _______increase cAMP which in turn leads to _______(2)

Answer 2

Stimulated activity of adenylyl cyclase
Increase cAMP
1.Relaxation of bronchial smooth muscle/uterine smooth muscle
2. inhibitor of release of mediators of immediate hypersensitivity from cells (mast cells)

Question 3

*****Selectivity is _____ at high doses and may______

Answer 3

****lost at high doses / High concentration of the agents and they can cause stimulation of B1 receptors at higher doses

Question 4

One side effect of the heart seen with beta 2 agonists

Answer 4

Tachycardia.

Question 5

Routes of administration

Answer 5

IV, SC, oral, INH

Question 6

For bronchodilation effecs, which route is preferred? why?

Answer 6

Inhaled; it delivers the greatest concentration of drug to the lungs and minimizes systemic absorption

Question 7

What should never be used to treat acute asthma?

Answer 7

LABA

Question 8

Tocolytics means

Answer 8

To stop premature labor

Question 9

NEVER USED here in US

Answer 9

ritodrine.

Question 10

Ritodrine withdrawn in

Answer 10

1998

Question 11

The only FDA approved Beta2 agonists to use as tocolytics______But currently ______Is used as tocolytics (off label )

Answer 11

Ritodrine: Terbutaline

Question 12

3 Side effects of b2 adrenergic agonist

Answer 12

• Tremor- Beta 2 in skeletal muscles
• Tachycardia- Due to loss of B2 selectivity at high dosess
• Palpitations

Question 13

In acute severe asthma, B2 agonists may cause _________how to fix ?

Answer 13

cause a decrease in arterial oxygenation presumed to reflect relaxation of compensatory vasoconstriction
- Give supplemental oxygenation

Question 14

Beta 2 agonist will cause what in potassium

Answer 14

HYPOKALEMIA

Question 15

What does beta 2 do to the sodium potassium pump?

Answer 15

drives K intracellular by stimulatin B2 receptors on the Na+ K+ ATPase pump

Question 16

Drugs interactions

Answer 16

MAOis and TCAs (within 2 weeks of discontinuation)

Question 17

CLASSIFICATION , how many classes

Answer 17

2
Short acting (SABA) 
and long acting (LABA)

Question 18

Short acting B2-adrenergic agonist last?

Answer 18

Last for 6 hours

Question 19

SABA , onset of action

Answer 19

fast onset of action

Question 20

Albuterol has ________ and they are all

Answer 20

7 different names; short acting agents.

Question 21

Albuterol sulfate

Answer 21

Racemix mixture : R and S (50-50)

Question 22

R isomer of albuterol is the _______also called _______

Answer 22

active ; Levalbuterol

Question 23

Levalbuterol is the

Answer 23

active ISOMER

Question 24

Which is commercially available as MDI and solution for inhalation

Answer 24

R-enantiomer

Question 25

Is levalbuterol better than albuterol? Why?

Answer 25

NO; same bronchodilator effects.

Question 26

LABA duration of action is ______and is more ______ and _______than SABA

Answer 26

> 12 hours (more lipophilic, longer duration of action)

Question 27

LABA- They all end in

Answer 27

• erol

Question 28

Onset of action of LABA

Answer 28

<5minutes

Question 29

***Should never be used to treat acute attack why?

Answer 29

****LABAs

Increases risk of asthma-related deaths with the use of long-term asthma control meds

Question 30

Selective B3 adrenergic agonist

Answer 30

Myrbetriq

Question 31

Myrbetriq FDA approved ____Agonists use to treat

Answer 31

Beta 3 ; Used to treat overactive bladder

Question 32

Myrbetriq mechanism of action

Answer 32

Relaxes the detrusor smooth muscle during the storage phase of the urinary bladder fill-void cycle by activation of B3 receptors.

Question 33

Most common adverse of myrbetriq

Answer 33

Hypertension

Question 34

Midodrine is a (class)_______used to treat

Answer 34

Vasopressor/antihypotensive agent; orthostatic hypotension

Question 35

Midodrine is a _______meaning it is inactive.

Answer 35

prodrug

Question 36

Midodrine active metabolite activates

Answer 36

alpha 1 adrenergic receptors of the arteriolar and venous vasculature, producing an increase in vascular tone and elevation in BP

Question 37

For BOTH ________and _______Administering these medications in combination with ____,_____,_____ Increase risk of ______Hypertension when given with those agents? solution?

Answer 37

MIDODRINE AND DROXIDOPA,supine; NE, epinephrine and other vasopressors
Monitor BP closely

Question 38

Northera (droxidopa)

Answer 38

Oral only agent that is used for NEUROGENIC ORTHOSTATIC HYPOTENSION

Question 39

Synthetic amino acid precursor of norepinephrine

Answer 39

droxidopa

Question 40

Beta 2 agents have

Answer 40

Sustained duration of action because of resistance to metabolism by COMT.

Question 41

Is inhaled as effective as parenteral with SABA?

Answer 41

yes

Question 42

SABA is the treatment of choice for ________and is also use as a prophylaxis agent to

Answer 42

Acute episode of bronchospasm

Prevent exercise-induced bronchospasm.

Question 43

3 acute metabolic responses with B2

one rare adverse effect:

Answer 43

Hyperglycemia
Hypokalemia
Hypomagnesemia

Paradoxical bronchospasm.

Question 44

***What are the only INHALED SABAs currently available

Answer 44

Albuterol

Levalbuterol

Question 45

The effects of Albuterol and volatile anesthetics are bronchomotor tone are

Answer 45

Additive

Question 46

Explain Droxidopa mechanism of action

Answer 46

directly metabolized into Epinephrine by the enzymes DOPA-Decarboxylas and norepinephrine then increases BP by inducing peripheral and venous vasoconstriction.