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Therapeutics I > Therapeutics I Exam VII (Pharmacology of Asthma and COPD Medications) > Flashcards

Therapeutics I Exam VII (Pharmacology of Asthma and COPD Medications) Flashcards

Pharmacology of Asthma and COPD Medications (127 cards)

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1
Q

Define asthma.

A

Asthma is defined as airway hyperactivity. A trigger will enter the bronchioles and in an asthmatic person, the bronchial tubes tighten and thicken, making the air passages become inflamed and mucus filled.

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2
Q

What are triggers for asthma?

A

Allergens, airborne particles, drugs (beta antagonists), infection, exercise, stress, and cold temperature.

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3
Q

Define COPD.

A

COPD is chronic obstructive pulmonary disease. It is the progressive and irreversible disease of limited airflow. There are two types of COPD; chronic bronchitis and emphysema.

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4
Q

What are some causes of COPD?

A

Smoking, pollution, and genetic predisposition

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5
Q

What is chronic bronchitis COPD?

A

This is COPD characterized by cilia damage and mucus not longer being sweep upward to clear the airway.

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6
Q

What is emphysema COPD?

A

This is COPD characterized by alveoli walls being permanently destroyed which leaves spaces too large to produce enough tissue surface area for proper oxygen exchange.

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7
Q

What genetic predisposition/ deficiency is linked to COPD development?

A

alpha-1-antitrypsin deficiency has been show to increase the risk for COPD.

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8
Q

T or F: Pneumonia is a case/risk factor for COPD.

A

False

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9
Q

Which 4 classes of drugs are used to relieve bronchial tone/obstruction via direct action on airway smooth muscle?

A
  1. Beta receptor agonists (mainly B2 agonists)
  2. Phosphodiesterase inhibitors
  3. Adenosine A2B antagonists
  4. M3 muscarinic acetylcholine receptor antagonists
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10
Q

What are the 5 classes of anti-inflammatory drugs that are used to reduce inflammation/obstruction/ bronchial tone?

A
  1. Phosphodiesterase inhibitors
  2. Corticosteroids
  3. Mast cell degranulation inhibitors
  4. Leukotriene modifiers
  5. Anti-IgE and Anti-interleukine antibodies and antagonists
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11
Q

How does muscarinic activation alter bronchial smooth muscle?

A

Muscarinic receptor activation in bronchial smooth muscle primarily leads to contraction (bronchoconstriction) and increased mucus secretion through the release of acetylcholine from parasympathetic nerves, activating post junctional muscarinic receptors.

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12
Q

How does muscarinic inhibition/antagonism alter bronchial smooth muscle?

A

Muscarinic receptor antagonism in bronchial smooth muscle leads to bronchodilation and decreased mucus secretion.

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13
Q

How does phosphodiesterase inhibition alter bronchial smooth muscle?

A

Phosphodiesterase 4 is the enzyme that breaks down cGMP in the body which decrease the ability for the bronchial to dilate. When we inhibit this enzyme, levels of cGMP are increased which will causes bronchodilation.

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14
Q

In the treatment of asthma and COPD, selective beta 2 agonists are typically used as they are much more selective for the lungs. However, it what situation would non-selective beta agonists like epinephrine and isoproterol be used?

A

Epinephrine would be used in situation of an emergency wheezing attack. It agonizes B1, B2, and some B3. Isoproterol is a B1 and B2 agonist that is used for rapid reversal of bronchospasms under anesthesia.

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15
Q

What is the MOA for isoproterol (Isoprenaline)?

A

B1 and B2 agonist

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16
Q

What is the brand name for isoproterol?

A

Isoprenaline

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17
Q

What is the indication for use of isoproterol (Isoprenaline)?

A

Rapid reversal of bronchospasms under anesthesia

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18
Q

What is the MOA of epinephrine?

A

B1, B2, and some B3 agonist

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19
Q

What is the indication for use of epinephrine in terms of asthma and COPD?

A

Emergency wheezing attack

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20
Q

What is the main issue with using agents like epinephrine and isoproterol chronically for asthma and COPD?

A

These are short-acting medications and we prefer long-acting medications for chronic treatment of asthma and COPD. Additionally, these medications will cause tachycardia.

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21
Q

Explain beta adrengeric receptor activiation.

A

A beta agonist will bind to the its g-protein coupled receptor with activates adenylyl cyclase which increase intracellular cAMP and activates protein kinase A.

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22
Q

What are LABAS?

A

LABAS are long-acting beta-2 receptor agonists

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23
Q

What is the typically dosing regimen for LABAS?

A

Twice daily dosing

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24
Q

What are the 2 LABAS we need to know?

A

Salmeterol (servent) and Formoterol (Perforomist)

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25
What is unique about the LABAS, salmeterol?
It has a 12 hour duration of action even though it has a 2-3 hour half-life.
26
LABAS and SABAS are poor substrates for what 3 reuptake/breakdown enzymes?
COMT, NET, and DAT This allows these medications to stay active for longer.
27
Salmeterol is a _____________ drug.
Lipophilic
28
What is the brand name for salmeterol?
Servent
29
What is the brand name for formoterol?
Perforomist
30
What is the half-life of formoterol?
10-12 hours
31
Salmeterol is a ________ _________ of the beta 2 receptor, allowing it to have a slower onset of action
Partial agonist
32
What is a unique characteristic of highly lipophilic inhaled medications?
They can leave their receptor and lurk in the lipid bilayer until they can reactivate the receptor.
33
What are the 2 ultra-LABAS we need to know?
Vilanterol and Olodaterol (Striverdi Respimat)
34
What is the daily dosing for ultra-LABAS?
Once daily dosing
35
What are the 3 SABAS we need to know?
Albuterol, pirbuterol, and terbutaline
36
What is the definition of a SABAS?
Short-acting beta 2 receptor agonists
37
What is the indication for use of SABAS?
Reversal of asthma symptoms and to provide protection against asthma triggers.
38
What are some possible side effects associated with SABAS?
Muscle tremors, tachycardia, and hypokalemia
39
What are the two brand names associated with albuterol?
Ventolin and Proventil
40
T or F: Corticosteroids are bronchodilators that augment SABAS and LABAS by upregulating the transcription of beta 2 receptors.
False. Corticosteroids do do this, but they are NOT bronchodilators.
41
Corticosteroids increase the transcription of what receptor?
Beta 2 receptors
42
What are the 2 adenosine A2B receptor antagonists we need to know?
Theophylline and aminophylline. These drugs are called methylxanthines.
43
Which medication is more efficacious for asthma and COPD; LABAS, corticosteroids, or adenosine A2B receptor antagonists like theophylline?
LABAS and corticosteroids are more efficacious compared to adenosine A2B receptor antagonists.
44
The adenosine A2B receptor antagonists, theophylline and aminophylline, are called ________________.
Methylxanthines
45
Why can adenosine A2B receptor antagonists be used in asthma and COPD?
These drugs block the adenosine A2B receptor so adenosine can not trigger smooth muscle bronchconstriciton.
46
What are LAMAS?
Long-acting muscarinic receptor antagonists
47
What are SAMAS?
Short-acting muscarinic receptor antagonists
48
What are the 3 LAMAS we need to know?
Tiotropium (Spiriva), Umeclidinium (Incruse), and Aclidinium (Tudorza)
49
LAMAS and SAMAS are less effective compared to LABAS and SABAS for _________ but more effective in _________.
Asthma COPD
50
What is the brand name for the LAMA, tiotropium?
Spiriva
51
What is the brand name for the LAMA, Umeclidinium?
Incruse
52
What is the brand name for the LAMA, Aclidinium?
Tudorza
53
What is the one SAMAS we need to know?
Ipratropium (Atrovent)
54
What is the brand name for the SAMAS, Ipratropium?
Atrovent
55
What phosphodiesterase subtype is inhibited for asthma and COPD treatment?
Subtype 4
56
What is the one long-acting PDe4 inhibitor we need to know?
Roflumilast (Daliresp)
57
What is the brand name for the PDE-i4 inhibitor, Roflumilast?
Daliresp
58
T or F: Roflumilast is a prodrug.
False. It is an active drug when taken but does become more active once converted to roflumilast N-oxide.
59
T or F: The PDEi4, Roflumilast, is effective in both COPD and asthma.
True
60
Explain corticosteroid binding.
Corticosteroids binds to their receptor and enter the nucleus, binding to CREB binding protein. The dimer complex between the ICS and its receptor inhibit the CREB binding protein HAT activity meaning the histone is not acetylated so it does not unwind and therefor the inflammation gene is not transcribed. Corticosteroids suppress inflammation mainly by switching off multiple activated inflammatory genes through reversing histone acetylation via the recruitment of histone deacetylase 2 (HDAC2).
61
ICS-GR binds what two things?
1. CREB binding protein- stops inflammatory gene expression 2. Histone deacetylase enzyme (HDAC2)- shuts down inflammation
62
What are the 5 big things that inhaled corticosteroids do to airway inflammation and structural cells?
- Inhibit inflammatory cytokine formation and release - Induce eosinophil apoptosis - Inhibit inflammatory gene expression in epithelial cells - Reverse vascular permeability and reduce edema - Decrease mucus secretion (NO EFFECT ON AIRWAY SMOOTH MUSCLE OR MAST CELL RELEASE OF MEDIATORS)
63
What 2 things do inhaled corticosteroids not do?
They do NOT have any effect on airway smooth muscle AND it has NO effect on mediator release from mast cells.
64
What percentage of inhaled drug actually makes it to the lungs?
Only 10-20%. The other 80-90% is actually just swallowed.
65
What are the two inhaled corticosteroid prodrugs we need to know?
Beclomethasone propionate (QVAR) and Ciclesonide (Alvesco)
66
What is the brand name for the ICS, beclomethasone propionate?
QVAR
67
What is the brand name for the ICS, ciclesonide?
Alvesco
68
The two ICS prodrugs rely on what enzyme in the lungs to become activated?
Lung esterases
69
Which ICS was discontinued, but was the first one of its kind on the market?
Beclomethasone propionate (QVAR)
70
What is the active metabolite of the ICS ciclesonide?
Des-ciclesonide
71
Is ciclesonide (Alvesco) categorized as a short or long-acting ICS?
Long-acting (6-7 hour half-life)
72
What are the 4 other inhaled corticosteroids we need to know that are not prodrugs?
Budesonide (Pulmicort), Fluticasone (Flovent), Momentasone (Asmanex), and Triamcinolone (Azmacort)
73
What is the half-life of the ICS budesonide?
3 hours
74
What is the half-life of the ICS fluticasone?
12 hours
75
What is the half-life of the ICS Momentasone?
6 hours
76
What is the half-life of the ICS triamcinolone?
2 hours
77
Rank the half-life of the ICSs from longest to shortest.
1. Fluticasone (12hr) 2. Ciclesonide (6-7hr) 3. Momentasone (6hr) 4. Budesonide (3hr) 5. Triamcinolone (2hr)
78
Systemic corticosteroids are reserved for ________ cases of asthma and COPD.
Severe
79
What are the 3 systemic corticosteroids commonly used long-term for those with severe asthma and/or COPD?
Prednisone (Deltasone), methylprednisolone (Medrol Dosepak), and hydrocortisone (Solu-Cortef)
80
What are the adverse effects of long-term systemic corticosteroid use?
Bone loss, cataracts, thinning of the skin, HYPOKALEMIA, hyperglycemia, insomnia, weight gain, and stunted growth in children
81
What is the brand name for prednisone?
Deltasone
82
What is the brand name for Methyprednisolone?
Medrol Dosepak
83
What is the brand name for hydrocortisone?
Solu-cortef
84
Which of the 3 systemic corticosteroids is administered via IV?
Hydrocortisone
85
What is the brand name for the combination inhaler ipratropium and albuterol?
Combivent Respimat Ipratropium (SAMA) Albuterol (SABA)
86
What is the brand name for the combination inhaler olodaterol and tiotropium?
Stiolto Respimat Olodaterol (LABA) Tiotropium (LAMA)
87
What is the brand name for the combination inhaler budesonide and formoterol?
Symbicort Budesonide (Short acting corticosteroid) Formoterol (LABAS)
88
What is the brand name for the combination inhaler fluticasone + salmeterol?
Advair Fluticasone (long-acting) Salmeterol (LABAS)
89
What is the brand name for the combination inhaler fluticasone and vilanterol?
Breo Ellipta Fluticasone (long-acting) Vilanterol (LABAS)
90
What is the brand name for the combination inhaler Fluticasone + Umeclidinium + Vilanterol?
Trelegy Ellipta Fluticasone (long-acting) Umeclidinium (LAMAS) Vilanterol (LABAS)
91
What is the brand name for the combination inhaler Umeclidinium and vilanterol?
Anoro Ellipta Umeclidinium (LAMAS) Vilanterol (LABAS)
92
What is the brand name for the combination inhaler Momentasone and formoterol?
Dulair Momentasone (Short-acting) Formoterol (SABA)
93
Corticosteroid binding reduces inflammation via what 3 routes?
- Activate Tristetraprolin (anti-inflammatory) - Activate Annexin A1 (anti-inflammatory) - Inhibit NK-FB (proinflammatory)
94
ICS also block the formation of ____________ and ___________ by indirectly blocking arachidonic acid formation.
Leukotrienes and autacoids
95
What enzyme cleaves arachidonic acid to make a platelet-activating factor?
Phospholipase A2
96
Explain COX formation from the plasma membrane.
Phospholipids are used to create arachidonic acid and it converted to LOX (leukotrienes), COX, and platelet-aggrevating factor via the phospholipase A2.
97
Which drug is a lipoxygenase inhibitor that blocks the formation of leukotrienes?
Zileuton
98
Which drugs antagonize the leukotriene 1 receptor?
Montelukast, Pranlukast, and Zafirlukast
99
What is the brand name for the 5-lipoxygenase inhibitor, Zileuton?
Zyflo
100
What is MOA of Zileuton (Zyflo)?
It stop the conversion of arachidonic acid to leukotrienes by inhibiting 5-lipoxygenase.
101
Zileuton (Zyflo) is associated with what side effect?
Hepatic problems
102
What is the brand name for montelukast?
Singulair
103
What is the brand name for Zafirlukast?
Accolate
104
What are the two adverse effects associated with the leukotriene cys-LT1 receptor antagonists like montelukast and zafirlukast?
Vasculitis and neuropsychiatric disorders
105
What are the 5 monoclonal antibodies that are used for severe asthma and COPD?
Benralizumab Mepolizumab Reslixumab Dupilumab Omalizumab
106
What is the main function of Omalizumab (Xolair)?
Anti-IgE mab. It blocks IgE from binding to its receptor which stops chronic inflammation.
107
What is the main function of Dupilumab (Dupixent)?
Anti-IL-4R alpha receptor mab. It blocks IL-4 and IL-13 activation of IL-4 receptor alpha which blocks B cell formation of IgE.
108
What is the main function of Mepolizumab (Nucala) and Reslizumab (Cinqair)?
These mabs bind and immobilize circulating IL-5 that would otherwise cause eosinophilic inflammation.
109
What is the main function of Benralizumab (Fasenra)?
Blocks IL-5 activation of IL-5 receptor alpha so eosinophils are not activated.
110
What is the brand name for Omalixumab?
Xolair
111
What is the brand name for Dupilumab?
Dupixent
112
What is the brand name for Mepolizumab?
Nucala
113
What is the brand name for Reslizumab?
Cinqair
114
What is the brand name for Benralizumab?
Fasenra
115
Recognize the structure for antimuscarinics.
116
Recognize the structure for leukotriene modifiers.
3 non-polar greasy molecules molecules
117
Recognize mast cell degranulation inhibitors.
118
Recognize methylxanthines.
119
What is unique about albuterol?
The meta OH can't participate in resonance
120
What is the difference in chemical structure between epinephrine and norepinephrine?
Epinephrine has a methyl group attached the a nitrogen while norepinephrine has two hydrogens at that spot.
121
Methylation of norepinephrine allows occurs at __________ position.
Methyl
122
T or F: The ring configurations for albuterol and formoterol ensure beta selectivity and COMT resistance to increase the duration of action.
True
123
What two things on albuterol makes it optimal for beta selectivity, COMT resistance, and slow MAO metabolism?
The t-butyl group and ring configuration
124
What thing on formoterol makes its beta selective, resistant to COMT, and slow metabolism by MOA?
Bulky R group
125
_________ on molecules makes drugs more lipophilic.
Flurine
126
To make an antagonist, the drug should look similar to the natural ligand but be ___________.
Bigger
127

Therapeutics I (14 decks)

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