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PHRM 5001 > 1. Sympathomimetic Bronchodilators > Flashcards

1. Sympathomimetic Bronchodilators Flashcards

1
Q

what are the 2 autonomic nerve fibers?

and what do they communicate with?

A

cholinergic and adrenergic

communicate with neurotransmitters

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2
Q

what are the 2 main autonomic neurotransmitters? what are they released by?

A

acetylcholine (released by cholinergic fibers) and norepinephrine/noradrenaline (released by adrenergic fibers)

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3
Q

what area of the spinal cord innervates the SNS?

A

thoracolumbar

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4
Q

length of pre vs post ganglionic fibers in the SNS

A

short pre, long post

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5
Q

what is the general action of alpha receptors?

A

vasoconstriction/vasopressor effects

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6
Q

what is the general action of beta 1 receptors?

A

increased myocardial conductivity, HR, and contractile force

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7
Q

what is the action of beta 2 receptors? Where are they found?

A

bronchodilation, inhibition of inflammatory mediator release, stimulation of mucociliary clearance, found throughout the tracheal tree and in the smaller airways

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8
Q

adrenergic bronchodilators are agents that stimulate which fibers?

A

sympathetic nervous fibers

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9
Q

what is the action of catecholamines (adrenergic bronchodilators) at the cellular level?

A

G protein couples the adrenergic receptor to the effector enzyme, initiates cell response (relaxation of airway smooth muscle)

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10
Q

B-adrenergic activate a _______ messenger system, list the steps.

A

secondary

  1. adenylyl cycles induction
  2. increase in intracellular cAMP
  3. inactivation of protein kinases
  4. decrease in intracellular calcium
  5. smooth muscle relaxation
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11
Q

what is the mechanism of action for indirect-acting sympathomimetics?

A

promote the accumulation of NE at the synapse…leads to nonspecific adrenceptor activity in the post-synaptic cell

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12
Q

what is the mechanism of action for direct-acting sympathomimetics? what are the results?

A

acts like NE, binds with adrenoceptors (creates complexes)

increased HR, airway smooth muscle relaxation, increased BP, glycogenolysis, skeletal muscle tremor, CNS stimulation

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13
Q

what are the components of a basic catecholamine structure?

A

catechol nucleus (benzene ring + 2 hydroxyl groups) and amine side chain

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14
Q

the keyhole theory of Beta 2 specificity states that…

A

addition of complex groupings to amine side chains increase beta 2 specificity
allows sympathomimetic drug to conform more closely to beta 2 receptors on airway smooth muscle (activation of secondary messenger system)

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15
Q

where does metabolism of catecholamines occur by MAO? mechanism of action?

A

in the neurons, oxidative deamination (removal of NH2)

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16
Q

where does metabolism of catecholamines occur by COMT? mechanism of action?

A

in non-neuronal tissues (kidney/liver), methylation to the OH- at carbon 3

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17
Q

what special consideration should be taken to prevent quick breakdown of catecholamines by COMT?

A

avoid oral administration

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18
Q

stereoisomers are also known as…

A

enantiomers or isomers

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19
Q

dextrorotatory (d, +) = _-epinephrine

A

S

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20
Q

levorotatory (l, -) = _-epinephrine

A

R

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21
Q

what are the physiological effects on (R) isomer/levo-isomer vs. (S) isomer/dextro-isomer

A

(R) isomer/levo-isomer produces bronchodilation

(S) isomer/dextro-isomer less active on adrenergic receptors

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22
Q

what is the ratio of a racemic mixture of both isomers?

A

50:50

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23
Q

list some clinical indications of adrenergic bronchodilators.

A

reversible airflow obstruction: asthma, chronic bronchitis, emphysema, bronchiectasis, cystic fibrosis, etc.

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24
Q

what are the 3 ways to classify bronchodilators?

A

rate of onset, peak effect, duration of action

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25
Q

what is the duration of ultra-short acting adrenergic bronchodilators? give an example.

A

< 3 hours

ex. epinephrine

26
Q

what is the duration of action of short-acting adrenergic bronchodilators? give an example.

A

4-6 hours

ex. salbutamol

27
Q

what is the duration of action of long-acting adrenergic bronchodilators? give an example.

A

12 hours

ex. salmeterol

28
Q

what is the duration of action for ultra-long acting adrenergic bronchodilators? give an example.

A

24 hours

ex. indacaterol

29
Q

epinephrine and adrenaline stimulate which receptor(s)? what systemic effects should you expect?

A

both A and B receptors, will expect to see cardiac stimulation and vasoconstriction

30
Q

Epinephrine:

onset of action? peak effect? degraded by? routes of administration? adverse effects? special considerations?

A

3-5 min
5-20 min
COMT
inhalation, injection (parenteral/IM)
tachycardia, increase BP, tremor, headache, insomnia
readily inactivated by heat, light, or air

31
Q

Racemic epinephrine:

receptor activity? degraded by? typically used to relieve what? duration of action? dose?

A 
equivalent A and B activity (lack selectivity)
rapid inactivation by MAO/COMT
used to relieve upper airway swelling
0.5-2 hours
2.5-5mg of 1mg/ml solution
32
Q

at which 2 carbon groups is an OH removed to form a resorcinol agent? what does this prevent? what is the outcome?

A

4 and 5
prevents inactivation by COMT
lengthens duration of action

33
Q

Metaproterenol:

type? onset of action? peak effect? duration?

A

short-acting
1-5 min
30-60 min
4-6 hours

34
Q

terbutaline:

type? selective B2 activity? resists methylation? classified as?

A

short-acting
yes (bulky terminal N-butyl group on amine side chain)
yes, resists COMT
SABA

35
Q

at which carbon is an OH substituted in the cathechol nucleus to create saligenin bronchdilators? what does this prevent? active on which receptor? type?

A

carbon 3
prevents inactivation by COMT
B2 preferential effects
short and long acting

36
Q

Salbutamol:

type of saligenin? receptor activity? onset of action? peak effect? duration of action? special considerations?

A

short-acting
B2 preferential activity
15 min
30-60 min
4-6…up to 12 hours (with extended release)
prepared as racemic mixture (d and l isomers)

37
Q

list the delivery forms of salbutamol

A

extended release oral tablets, MDI (100mcg), DPI (200mcg), IV solution (1000mcg/ml)

38
Q

what are the current dosages for nebulized treatments of salbutamol?

A

inhalation solution: 5.0mg/ml diluted with NaCl

pre-mixed nebules: 2.5mg diluted in 2.5ml of NaCl or 5.0mg diluted in 2.5ml of NaCl

39
Q

salbutamol is the drug of choice for relieving ____ airflow obstruction.

A

acute

40
Q

what effect does salbutamol have on K+ levels in the body? special considerations?

A

decreases serum potassium levels (pushes extracellular K+ into intracellular spaces)

can be used to shift k+ in patients with hyperkalemia and should be used with caution in patients with hypokalemia

41
Q

what are the doses of salbutamol dependent on? what are the appropriate doses for regular use? what are the appropriate doses for relief of an exacerbation?

A

age
1-2 puffs via MDI with spacer Q4-6H, not exceeding 4-8 puffs per day
3-6 puffs via MDI with spacer Q15-30min OR 2.5-5.0mg nebulized

42
Q

what is salbutamol known to interact with?

A

MAOI, some beta-blockers (propanolol), other bronchodilators (terbutaline), diuretics, digoxin

43
Q

levosalbutamol:

type of saligenin? what type of isomer? receptor activity? how does it compare to salbutamol?

A

short-acting
R-isomer
100X more affinity for B2 receptor than d-isomer
mixed studies say you’re able to give lower doses and that it lasts longer (3-8 hours)

44
Q

long-acting saligenins aim for a duration of ____ hours and are classified as ____. What is the purpose?

A

12+ hours, LABAs

reduce frequency of administration, increases patient compliance, manages nocturnal symptoms

45
Q

Salmeterol:

onset of action? peak effect? length of action?

A

14-22 min
3-5 hours
12+ hours

46
Q

what is the lipophilic arrangement of salmeterol? why is this important? which inhibtor(s) does salmeterol resist?

A

lipophilic tail, hydrophilic head
contributes to increased duration of action, increased lipid solubility allows drug to access phospholipid bilayer, attaches to exosite anchor to provide sustained stimulation
non-catecholamine structure resists degradation by MAO and COMT

47
Q

Formoterol:

type of saligenin? onset of action? peak effect? duration of action? receptor activity?

A 
long acting
15 min
30-60min
12+ hours
fast/long acting B2 agonist
48
Q

what are 4 resulting isomers of the 2 asymmetric centers of formoterol?

A

SS, RR, SR, RS

49
Q

what allows formoterol to have some lipid solubility?

A

lipophilic tail allows for retention in cell membrane where it can be stored with sustained stimulation of B2 receptor

50
Q

Indacaterol:

classified as? duration of action? unique structure? dose?

A

LABA

24 hours

heterocyclic ring attached to saligenin nucleus + multi-ring structure attached to terminal amine (highly resistant to MAO/COMT)

75mcg capsule via DPI OD to control severe COPD

51
Q

list some precautions with adrenergic bronchodilators.

A

cardiac effects, tolerance, loss of bronchoprotection, CNS effects, fall in PaO2, metabolic disturbances, paradoxic bronchospasm, sensitivity to additives

52
Q

what are some specific cardiac effects related to adrenergic bronchodilators?

A

tachycardia, increased CO/O2 consumption, increased BP, palpitations

53
Q

what does the 20% rule state?

A

if HR increases by 20% or more, the treatment should be discontinued and another therapy should be considered

54
Q

down-regulation refers to…
In what types of drugs can this be seen?
How can it be reversed?

A

long term desensitization of B receptors to B2 agonists, caused by a decrease in the # of B receptors
SABAs and LABAs
reversed with concurrent corticosteroid use

55
Q

bronchoprotective effect refers to airway reaction to ________________.
Protective effect found to decline more rapidly than what? What does this lead to?

A

bronchoprovocation
bronchodilating effect
leads to bronchial hyper-responsiveness

56
Q

what are some specific CNS effects that can be seen with adrenergic bronchodilators?

A

headache, nervousness, irritability, anxiety, insomnia, tremors

57
Q

Why can a fall in PaO2 be seen when administering adrenergic bronchodilators?

A

regional alveolar hypoxia causes vasoconstriction and administration of B agonist can increase perfusion in under-ventilated lung regions (due to the vasodilation), which will worsen V/Q mismatch

58
Q

What are some specific metabolic disturbances that can be seen when administering adrenergic bronchodilators?

A

increased blood glucose and insulin levels (problematic for diabetics) and decreased serum potassium levels (concern for patients with cardiac disease)

59
Q

What is paradoxic bronchospasm related to? How long the bronchospasm last? If sensitivity exists, consider what?

A

related to propellants used in MDI
typically lasts < 3 min
consider DPI

60
Q

What are some specific additives that pose a concern when administering adrenergic bronchodilators?

A

sulfite preservatives, benzalkonium chloride (BAC), ethylenediamine tetra-acetic acid (EDTA - sulphite + acid pH = sulfurous acid and sulfur dioxide), and hydrochloric/sulfuric acids

61
Q

How should you monitor effectiveness of an adrenergic bronchodilator?

A

ongoing respiratory assessment (RR + pattern, SpO2, BS before/after, WOB, cardiac response (HR, BP), monitor flow rates (peak flow, bedside spirometry), capnography, ongoing pulse assessment (20% rule), ABGs, pulse oximetry

PHRM 5001 (12 decks)

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