Beta-adrenergic bronchodilators Flashcards

(64 cards)

1
Q

what can airway receptors be found

A
  • airway smooth muscle

- Mucosa

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2
Q

What are 2 types of receptors

A
  • sympathetic (adrenergic)

- parasympathetic (cholinergic) receptors

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3
Q

What decrease airway calibre

A
  • ->edema
  • ->inflammation
  • ->muscle contraction
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4
Q

What is the clinical indicator for adrenergic Bronchodilators

A

Relaxation of smooth airway muscle in the presence of airflow obstruction

in these disease:
•Asthma
•Bronchitis
•Emphysema
•Cystic Fibrosis
•Bronchiectasis
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5
Q

What does SNS innervate

A

adrenal medulla using Norepinephrine

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6
Q

What is the effect of adrenergic stimulation of Beta 2 receptor in airway

A

bronchodilation

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7
Q

What does PNS innervate

A
  • Smooth airway muscle
  • Mucous glands
  • Pulmonary vasculature

uses Acetylcholine

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8
Q

What is the effect of cholinergic stimulation in these receptors

A
  • Bronchospasm

- Increased mucous production and thickness

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9
Q

What is agonists

A

stimulate receptors

“mimetics”

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10
Q

What is Antagonists

A

blocks receptors

“lytics”

***Drugs can stimulate or block SNS and PNS

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11
Q

What are the receptors of adrenergic ?

A

alpha 1(smooth muscle of peripheral blood vessels): Vasoconstriction/vasopressor effect

beta 1(heart)
Increased HR and contractile force
beta 2(airway)
Relaxation of bronchial smooth muscle
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12
Q

where are the muscarinic or cholinergic receptors

A

M3 cholinergic

  • Bronchial smooth muscle
  • Sub mucosal bronchial glands
  • Pulmonary, bronchial & peripheral blood vessels

M2 cholinergic
-Heart

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13
Q

What is the function of MAO and COMT

A

recycles/degrades norepinephrine

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14
Q

What are 2 types of beta-agonists

A

Direct Acting

Indirect Acting

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15
Q

What is the deal with Direct Acting beta-agonists

A

chemically similar to neurotransmitter NE

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16
Q

What is the deal with InDirect Acting beta-agonists

A
  1. COMT, MAO inhibitor

- ->increase NE available at synaptic cleft

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17
Q

What is the Primary messengers of SNS

A

NE

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18
Q

What is the secondary messengers of SNS

A

Second” messengers are responsible for specific cellular responses:

  • cAMP
  • bronchodilation, decreased secretions
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19
Q

What is the Primary messengers of PNS

A

cGMP

- bronchoconstriction, increased secretions, histamine release

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20
Q

what is the end action of cAMP after drug bind to beta 2 receptor

A
  • inactivates myosine light chain kinase
  • decrease intracellular Ca
  • -> lead to smooth muscle relaxation
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21
Q

how does salmeterol work

A

its hydrophilic so once it gets into the cell, it will anchors itself with the G protein, therefore increases the concentration of cAMP(cyclic AMP)–>continue bronchodilation

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22
Q

What is the result of drug binding to beta receptor

A

1 activation of G (guanine nucleotide) linked protein receptors

  1. G protein subunit attaches to enzyme adenyl cyclase & ATP to produce secondary messenger cAMP\
  2. lead to
    - -> inactivation of the enzyme kinase so no actin-myosin cross linkages
    - ->reduction in intracellular calcium
    - ->decrease histamine release and glandular secretions
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23
Q

What are some alpha 1 agonist drugs

A

Phenylephrine

Epinephrine

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24
Q

What is the effect of drug binding to alpha 1

A
  1. activation of G protein linked
  2. phospholipase C
    - ->release of intracellular calcium stores
    - ->kinase activation
    - ->resulting in vascular smooth muscle contraction (in periphery and airway)
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25
What is ephedrine, pseudoephedrine?
- powerful alpha 1 stimulant | - ->mild bronchodilator
26
What is the indication of phedrine, pseudoephedrine?
nasal decongestion
27
What is the precaution of ephedrine
* diabetes * glaucoma * CAD, CHF * urinary retention
28
What is the indication of adrenergic agonist
alpha 1: vasoconstriction of blood vessels & upper airway passages
29
What are 3 ways of administering adrenergic agonist
Local: salbutamol Systemic: IV or IM
30
What are the Adrenergic Agents and Formulations?
1. Ultrashort acting - ->Epinephrine, Racemic Epinephrine - -> <3hrs 2. Short acting(SABA) - ->Salbutamol, Metaproterenol - ->4-6 hrs 3. Long Acting (LABA) - ->salmeterol, formoterol, vilanterol, indacaterol, olodaterol - ->12-24hrs
31
Wht are the 3 classess Adrenergics
1. Catecholamines 2. Resorcinols 3. Saligenins
32
Which adrenergic class do sympathomimetic bronchilators belong to
Catecholamine e.g. epinephrine
33
how does Sympathomimetic bronchodilators trigger adrenegic effect
- catecholamines | - derivatives of catecholamines that mimic epinephrine
34
features of Resorcinol agents and example?
Modification of catecholamine molecule e.g. Metaproterenol / orciprenaline: Alupent® Terbutaline: Bricanyl ®
35
What are the features of saligenin agents and example
Modification of catecholamine molecule Salbutamol – Ventolin®
36
What is the deal with Keyhole Theory of β2 Specificity, exmaple ?
The larger the catecholamine side chain (key), the more β2 specific e.g Epinephrine •Equal α and β Isoproterenol -Strong β, little α Salbutamol, salmeterol -β2 preferential
37
What are the ultra short acting adrenegics
epinephrine, isoproterenol - non-specific adrenergic receptor stimulant - ->strong alpha 1 and beta 1 unsuitable for oral administration: -->inactivate by COMT and MAO
38
What is the onset, peak , duration of epinephrine, isoproterenol
onset: 3-5 minutes peak: 5-20 minutes duration: 1-3 hours
39
What is the Indications of ultra short acting
* acute asthma * laryngeal/airway edema * cardiac stimulation & systemic vasoconstriction * anaphylaxis
40
contraindication for ultra short acting
pre-existing cardiac arrhythmias
41
features of epinephrine, example ?
for life threatening systemic allergic reactions (anaphylaxis), include asthma Epipen®, AllerjectTM Potent catecholamine bronchodilator
42
What the route/dose/frequency of epinephrine?
route: IV, IM, subcu, ETT (instil), intra-cardiac (LV) Dose anaphylaxis (sc or im) 0.2-1.0 mg at 10-15 minute intervals asthma (IV) 0.1-0.25 mg over 5-10 minutes, repeat every 5 - 15 mins Epi-pen every 10-20 minutes for anaphylaxis
43
How is Catecholamines metabolized
``` inactivated by COMT Inactivated in gut and liver(oral/enteral adminstration isn't good) •Heat •Light •Air ```
44
What is Racemic Epinephrine and its indication
synthetic epinephrine 1. control airway bleeding during bronchoscopy 2. reduce airway swelling
45
feature of SABA and example
metaproterenol/orciprenaline - Alupent® terbutaline - Bricanyl® *direct acting, B2 selectivity increased
46
what is the onset, peak, duration of SABA (resorcinol, saligenin)?
onset: 1-5 min peak: 30 -60mins duration: 4 - 8 hrs
47
What is the Indications: for SABA ?
acute bronchospasm
48
What is the contraindication SABA?
tachy-arrhythmias
49
What is the route/dose/frequency of SABA?
Route Inhaled (via pMDI*, DPI**, nebulizer solution) 1-2 puffs or 0.5-1.0 mg every four hours prn oral *syrup 10-20 mg tid to qid
50
features of example of Saligenin Bronchodilators ?
beta 2 specific indirect acting e.g. Salbutamol Ventolin albuterol (USA) Airomir Salbutamol HFA
51
what is the onset, peak, duration of Saligenin Bronchodilators?
* onset: 5-15 min. inhaled, up to 30 min for oral * peak: 30-60 min * duration: 3-6 hours
52
Indication of Saligenin Bronchodilators
acute bronchospasm
53
What is the Route/dose/frequency of Saligenin Bronchodilators?
Inhalation (pMDI, nebulizer sol’n, nebules), parenteral (injection/IV) - inhaled: 1-4 puffs or 1.25-5 mg q 20min-4h oral (syrup, tablets) - 2-4 mg tid to qid
54
Features of LABA
highly selective B2 agonist lipophilic side chain allows for continual activation of beta2 receptor **never montherapy with LABA as it can lead to asthma paradox
55
drugs of LABA
salmeterol (Serevent) formoterol (Oxeze®) vilanterol (Incruse®)
56
What is the indication of salmeterol
long term control of bronchospasm
57
What is precaution for salmeterol
- Not for use in asthma without appropriate steroid use | - Not for acute relief
58
What is the Route/dose/frequency of salmeterol
inhaled (pMDI, DPI) 25mcg: 2 puffs bid 50mcg: 1 inhalation bid
59
What is the indication of formoterol fumarate
- long term control of break through bronchospasm - acute relief of bronchospasm - protection re: exercise
60
contraindication of formoterol fumarate
anaphylaxis to milk protein
61
What is the Route/dose/frequency of formoterol fumarate
inhaled (DPI) 6, 12 mcg Oxeze® 1-2 inhalations bid (and prn)
62
An example of LABA and combination of ICS
Symbicort ® ICS+LABA --> SMART asthma drug: single reliever and maintenance
63
What is the clinical use of LABA
Maintenance therapy of asthma not adequately controlled by inhaled corticosteroids (ICS) and warrants initiation of Tx with LABA COPD needing daily bronchodilator Not recommended for rescue therapy Not recommended for treatment of breakthrough symptoms or without ICS
64
What are the Side Effects of LABA’s
``` Tremors (shakiness) Tachycardia Palpitations Irritability Insomnia ```