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Respiratory 1 > Pharmacology of the Treatment of Airway Diseases > Flashcards

Pharmacology of the Treatment of Airway Diseases Flashcards

1
Q

FEV green yellow and red

A

Green over 80

Yellow 50-79

Red under 50

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2
Q

Asthma patho

A

INflammation, edema, mucous secretion, thickened airway wall, obstruction

Bronchial hyperresponsiveness

IL5 is an important cytokine that activates eosinophils and neutrophils…they can migrate into the airways

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3
Q

Tx of asthma severity

A

Step 1 - intermittent tx

Persistent ashtma is anything above that

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4
Q

Topical application

A

Aersol delivery

Few side effects

Most pts can use

Spacer limits particle size

Slow deep breath for 5-10 seconds

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5
Q

MDI

Nebulizers
Dry powders

A

Cheap, portable and fast

No coordiination…good for young children or elderly…uses pressurized gas and takes 15 minutes

Latose or glucose powders…need high flow and powder irritating…not good for young children or elderly and temp and humidity probs

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6
Q

Relivers

Controllers

A

Quick relierf (bronchodilators)..B2-agonists (short acting) and anti-cholinergics

Controllers - inhibit late phase inflammatory response (all other and long acting B2-agonists)

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7
Q

B2-adrenergic agonist MOA

A

Stimule the B-adrenergic receptors on airway smooth muscle

Decrease airway resistance by increasing formation of cAMP…this increase protein kinase A and then smooth muscle relaxation

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8
Q

Onset of action SABA

A

Most effective, MDI or nebulizer

Albuterol

Drug of choice for acute asthma…works in 1-5 minutes for 2-6 hours

Used for step 1 (need less than 3X week) and acute exacerbations of ALL steps

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9
Q

Oral B2 adrenergics

A

Salbutamol

Works in 1-2 hours and durations is 4-8 hours

Young children under 5

Occassional wheezing from upper resp infections

More advers eeffects

Slow release and short acting..less efficacious

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10
Q

LABA B2 adrnergic agonists

A

INhaled and long acting

Salmeterol

Takes longer to act (NOT for acute)

Longer durations

Long side chain inserts into lipid bilayer and PM gradullary diffuses

Long duration masks worsening of inflammation..not good for monotherapy

NEVER use on own and use with corticosteroids (step 3-6)

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11
Q

Epinerphine

A

Ultra-short acting

Life therating

Unconscious or severe resp distress

Not the drug of choice

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12
Q

B2 adverse effects

A

Uncommon in inhaled

Cardiac - tachy, palps, arrythmias

CNS - nervousness, restless, anxiety

Skeletal , muscle tremors

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13
Q

Dangers of B2 agonist overutilization

A

INcrease hyper-responsiveness

Death from worsening dz

Inhaleer more than 3X a week…need anti-inflammatory therapy

Monitor dz

Death - use long-acting B2-inhaler for actue attack

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14
Q

Anticholinergic agents

A

Comp inhibit M3 receptors

Block contraction of airway smooth muscle

Lower and less nitense than B2 agonists

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15
Q

Ipratropium and tiotropium with SEs

A

Ip - inhaler or nebulizer…works for 6 hours

Tio - dry power, works for 24 hours…add on for Step 4 (over 12 y/o)

Can be combined with B2 agonists…albuterol and ipratropium

Little sys absorption…dry mouth, blurred visoion, urinary retention…glaucomoa in the elderly

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16
Q

CSs

A

First line ofr step 2-4

Fluticasone - inhaled

Prednison - oral

Prophylactic…6-12 hours to work

Prevent exacerbation recurrence

Dose-dependnet

Max improvement - several weeks

Do NOT relax airway smooth muscle directly

Inhibit the inflammation and reduce reactivity…restores sensitivity to B2 agonists

17
Q

Local and systemic adverse effects of CSs

A

Local (inhaled) - voice weakness, thrush, suppress hypothalamus, growth suppression, osteoporosis and cataracts

Systemic - fluid retention, weight gain, osteo, cataracts, diabetes, HYPA suppression…make sure to taper

18
Q

Advair

A

Long acting B-agonist with low/medium dose of ICS

Pts not adequately controlled by steroids alone (steps 3-6)

Advair - combination of almetrol and fluticasone

19
Q

Anti-IgE - omalizumab

A

Recom humanized monoclonal AB against IgE

MOA- IgE binds FCeRI receptor on mast cells

Allergen binds cell-bound IgE

Crosslinks receptor…histamine release

OMalizumab binds the free IgE

20
Q

PK and effects of Anti-IgE

A

Single sq injection every 2-4 weeks

Use in pts with severe asthma not controlled by std drugs (long acting B agonist and corticosteroid)
OR pts iwth IgE mediated sensitivity (skin prick test)

INjection site rxn…slight increast risk of circulatory effects…maybe allergic rxns?

21
Q

Mepolizumab

A

Pts with severe esosinophilic asthma

IV or SC

Neutrlizes IL-5

22
Q

Leukotrienes

A

Secreted by mast cells and eosinophils

Binds cys-LT1 receptor on smooth muscles

Potent bronchoconstrictors

23
Q

Montelukast

A

Oral leukotriene receptor antagonist

Competitive nihiborrs of cyc-LT1 receptor

Prophylactic

Some don’t respond

Less efficious than mod-high

Second line for Step 2

Use in combo iwth B2 agonists and steroids (step 3 and 4)

**8Better adherence

24
Q

PKs, adverse effects with singulair

A

Oral, 1X daily

Abnormal liver function tests

Suicide?? Mood changes/??

25
Q

Thophylline

A

Bronchodilator and antiflam

Activates histone deacetylases and decrease transcription of proinflam genes

Phopshodiesterase inhibitor…prevents conversion of cAMP to other things

Allows cAMP to promote bronchodilation

26
Q

Theophylline PKs, adverse effects and uses

A

Oral or IV

T1/2 increased - heart failure, PE, AB interations

Fatal intox if administered IV too fast…seizures often precede toxicity

Second line to low dose ICS (step 2)
Add-on (in addtion to ICS..step 3 and4)

Pts who can’t take ICS, aren’t adherent or don’t have insurance

Low dosage making a comeback

27
Q

Rofumilast

A

COPD - FDA approved
Trialse for allegens

PDE4 inhibitor which increases cAMP

Bronchodilator

Anti-inflam response (reduces esosinophil mirgrations)

More selective to aitrway than theophylinne

Adverse - weight loos, insomnia, mood

28
Q

Azithromycin

A

Severe asthma - high risk for exacerbations and infection

Non-esosinphilic - neutrophilic resistant to CSs

Anti-bac and anti-infolam

Frwquency of severe exacerbations is primary endpoint

29
Q

tx of COPD

A

Rofumilast

Salmetrol (long acting)

Long acting anti-cholinergic (tio)…if reversible

CSs - some respond to short course

Theo - effective for some…add to B2

Daily azih - prevent exacerbations

30
Q

Bronchodilator effects of drugs

A

Beta agonists increase AC…increase AMP…increases dialtion

Theophylline and rofumilast…inhibit PDE and decrease AMP

Theophylline and muscarinic antagonists both block bronchocontstriction

Respiratory 1 (28 decks)

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