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Therapeutics > Hazbun lecture 2 > Flashcards

Hazbun lecture 2 Flashcards

1
Q

3 main treatment strategies in asthma

A

bronchodilation
anti-inflammation
inhibition of mast cell degranulation

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2
Q

3 types of drugs for bronchodilation

A

B2 adrenergic agonist
methylxanthines
anticholinergic

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3
Q

2 types of drugs for anti-inflammation

A

Glucocorticoids
anti-leukotriene agents

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4
Q

2 types of drugs for inhibition of mast cell degradation

A

cromolyn type drugs
Omalizumab (xolair)

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5
Q

B2- adrenergic agonist (sympathomimetic amines) primary and secondary activity.

A

Primary- bronchodilation of smooth muscle
secondary- inhibition of release of mediators from mast cells.

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6
Q

How does the inhibition of release of mediators from mast cells affect the body?

A

it increases microciliary transport to mucus and inhibits microvascular leakage

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7
Q

What are the steps to muscle contraction?

A

LTC4 or LTD4 interacts with CYSLT-1R (or histamine interacts with H1R)

This activates the GQ pathway and PLC, which leads to an increase in IP3

This leads to an increase in calcium, which binds to calmodulin

Leads to activation of myosin LC kinase (phosphorylates myosin LC)

myosin interacts with actin, after phosphorylation. It contracts

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8
Q

Steps to muscle relaxation (B2 agonist effect)

A

B2 agonist activates G2 protein, increasing cyclase

This decreases calcium and increases cAMP

PKA gets activated and phosphorylates myosin LC kinase

leads to muscle relaxation

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9
Q

recognize SABA chemical structures and chemical properties

A

Has a ter-butyl group
has a salicylic alcohol group in the middle
has an alcohol phenyl ring on the far left

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10
Q

contraction vs relaxation of the muscle difference in MLCK (myosin LC kinase)

A

In contraction the MLCK activates myosin LC, phosphorylating it. It then interacts with actin

in relaxation, activation of PKA phosphorylates MLCK and muscle relaxes

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11
Q

name of 2 SABAs and their differences

A

Albuterol and terbutalin.
Albuterol has optimal B2 selectivity, terbutalin has more potent B2 selectivity (but has increased palpitations)

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12
Q

LABA chemical structures and properties

A

Has CH2 chains in between two phenyl rings.

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13
Q

Name two LABA s and explain their differences

A

Formoterol and Salmeterol
Formoterol has the highest receptor affinity, it has increased lipophilicity and is resistant to MAO and COMT. LOOK UP STRUCTURE AND REMEMBER

Salmeterol has greater water solubility and moderate lipophilicity. It has long CH2 groups sandwiched between two phenyl rings
Also resistant to MAO and COMT

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14
Q

When are LABAs contraindicated?

A

you CAN NOT use LABAs as a monotherapy, being deaf is a side effect

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15
Q

why do LABAs act longer than SABAs

A

SABAs are resistant to COMT with a slight MAO resistance
LABAs are resistant to COMT and MAO

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16
Q

why is inhalation the route of choice for acute attacks

A

drug delivery directly to the site of action and fewer adverse effects compared to B2 agonists given orally

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17
Q

Adverse effects of B2 adrenergic agonists

A
  1. tachycardia and palpitations
    a) Less of this if the drug is more selective for B2
    b) High doses of B2 selective agents may stimulate B1 receptor in heart
    C) There may be some reflex tachycardia due to vasodilation by B2
  2. Skeletal muscle tremors
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18
Q

effect of glucocorticoids on bronchial smooth muscle

A

decreases hyperresponsiveness of bronchial smooth muscle that occurs in asthma

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19
Q

What infection risk is associated with taking glucocorticoids

A

Candidiasis (fungal infection) thrush

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20
Q

Risk of systemic side effects for gllucocorticoids? Why?

A

Low, this is because it is inhaled, oral has a lot of systemic side effects

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21
Q

example of ICS+LABA combination

A

Advair- Fluticasone+salmeterol

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22
Q

Does theophyline cause bronchoconstriction or relaxation? How?

A

Theophyline inhibits PDE4 in the muscle contraction/relaxation pathway. This increases levels of cAMP
leads to relaxation
Theophyline antagonizes the broncho-constriction produced by adenosine by blocking the adenosine 1 receptor

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23
Q

Why is theophyline not used anymore?

A

Narrow therapeutic range and lots of drug-drug interaction

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24
Q

How does cromolyn treat asthma

A

Inhibits mast cell degranulation

25
Q

Compare the structures of the two cromolyns Cromolyn sodium (intal) and nedocromil sodium (tilade)

A

Cromolyn sodium (Intal) has 4 phenol rings, an OH in the middle with an Na+ on each side

nedocromil sodium (tilade) has 3 phenol rings with an Na+ on each side

26
Q

Are cromolyn drugs inhaled or orally administered?

A

Inhaled via microfine powder of aerosol

27
Q

Why can’t cromolyn drugs be taken orally

A

They are insoluble salts

28
Q

Cromolyn action compared to B2 adrenergic agonists

A

Cromolyn blocks bronchoconstriction, reducing symptomatic severity and bronchodilator use while B2 induces bronchodilation

29
Q

What are the wo types of inflammation associated with asthma and monoclonal-based therapy

A

Type 2 low inflammation and type 2 high inflammation

30
Q

What is the difference between type 2 high inflammation and type 2 low inflammation?

A

Type 2 low inflammation is neutrophilic and harder to treat and is likely to have adverse effects
Type 2 high is eosinophilic and easier to treat

31
Q

name the 5 major pathways targeted by biologics (monoclonal antibodies)

A

IgE antagonists- omalizumab (xolair)
IL-5 pathway- reslizumab &mepolizumab
IL-5 alpha receptor- benralizumab
IL-4 receptor alpha antagonist- dupliumab
thymic stromal lymphopoietin (TSLP)- tezepelumab

All approved for type 2 high inflammation

32
Q

rationale for xolairs (omalizumab) therapeutic use

A

causes a 96% reduction in free IgE

33
Q

How does xolair cause a reduction of IgE

A

Xolair inhibits binding of IgE antibodies to the FcER1 receptor on mast cells and basophils.

This inhibits mast cell degranulation, suppressing inflammation.

34
Q

Name two different anti-leukotriene drugs

A

ZYFLO (Zileuton)
Zafrilukast/montelukast (Accolate)

35
Q

explain the differences in the mechanism of action between zileuton and zafrilukast

A

zileuton is a selective inhibitor of 5-lipoxygenase
Zafrilukast/montelukast is a selective and competitive inhibitor of CysLT-1 receptor

36
Q

Remember the structures of Zafrilukast and Zileuton

A
37
Q

How does singulair work and how does its chemical structure contribute to its action?

A

Singulair has similar structure to LTD-4 so it mimics this LTD4 and binds CysLT-1 receptor, inhibiting the late phase of bronchoconstriction

38
Q

adverse effects of singulair and associated box warning

A

Box warning- agitation and mental health issues
headache, nausea, diarrhea

39
Q

difference between ipratropium and tiotropium

A

Ipratropium is a SAMA
Tiotropium is a LAMA

40
Q

Know the structure of Tiotropium and Ipratropium

A
41
Q

why is it useful the both ipratropium and tiotropium are quaternary ammonium compounds

A

Limits systemic absorption, decreasing side effects

42
Q

mechanism of action of tiotropium and ipratropium

A

Both ipratropium and tiotropium block the binding of AcH to muscarinic receptor, preventing contraction

43
Q

What drugs are allowed as monotherapy in COPD but not asthma

A

LABA (formoterol, salmeterol, indacterol)

44
Q

In COPD, neutrophils are activated and release proteases called

A

MMP9 and elastase

45
Q

WHat inhibits MMP9 and elastase

A

a-1 anti trypsin

46
Q

effect of a-1 anti trypsin deficiency

A

leads to excessive proteolytic damage to lung tissue

47
Q

How can we treat a-1 anti trypsin deficiency

A

We can treat this by replacement therapy

48
Q

What is a drug that can improve lung function in CF

A

Ivacaftor (kalydeco)

49
Q

Mechanism of action of kalydeco (ivakaftor)

A

Kalydeco helps potentiate the chloride current channel in CFTR, allowing the channel to function better

50
Q

What is the del 508 mutation? what does it lead to?

A

Del 508 mutation leads to CF and makes the protein unstable affecting protein traffic

51
Q

What are 3 drugs used to treat genotypes of cystic fibrosis

A

Orkambi
symdeco
trikafta

52
Q

Orkambi is used to treat what genotype of F508del

A

Homozygous for F508del

53
Q

Symdeco is used to treat what genotype of F508del

A

Homozygous for F508del or one F508del plus one 154 residual function mutation

54
Q

Trikafta is used to treat what genotype of F508del

A

One copy of F508del or atleast one copy of 177 mutations

55
Q

what drugs are used for alleviating complications/symptoms from CF

A

Mucolytics- reduce mucus thickness
bronchodilators (albuterol)
antibiotics

56
Q

Thick mucus in CF obstructs pancreatic enzyme flow, how do we treat this

A

PERT (Pancreatic enzyme replacement therapy)

57
Q

Asthma pulmonary targets for treatment

A

bronchodilation
anti-inflammation
inhibition of mast cell
inhibition of eosinophilia

58
Q

COPD pulmonary targets for treatment

A

bronchodilation
protease inhibitor

59
Q

CF pulmonary targets for treatment

A

Protein folding/channel corrections
PERT
bronchodilation and antibiotics

Therapeutics (46 decks)

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