Antiasthmatics

Front 1

Asthma is a chronic inflammatory disorder that has a usually "____" airway obstruction. Which symptom of asthma is the most common and the most commonly overlooked? What is one major type of infiltrative cell?

Back 1

1. reversible
2. cough
3. Eosinophils

Front 2

Wheezing represents increased resistance in the ___ airways, and the bronchi which are the greatest site for resistance will __ their resistance. Rales represent alveoli popping and indicate a ___ airway process.

Back 2

1. Conducting
2. Increase
3. Lower airway

Front 3

The goals of asthma therapy include:
1. Prevent airway remodeling -- ___ b/c of chronic inflammation will cause irreversible damage
2. Min or no chronic sx day or night w/ infrequent use of quick relief meds-- less than __ times/wk
3. Maintain what level of activity?
4. Maintain ___ pulm fx

Back 3

1. Fibrosis
2. less than 2x/ wk
3. Normal
4. Normal pulm fx

Front 4

Non pharm tx of asthma includes avoidance of triggers including-- ___ sensitivity, sensitivity to ___containing foods, and Medical conditions including _____

Back 4

1. Med sensitivity-- aspirin, NSAIDs, B blockers
2. sulfite foods- dried fruits
3. GERD, Sleep Apnea, URI

Front 5

2/3 of asthma pts have responses mediated by what type of T cells?

Back 5

TH2

Front 6

Intermittent asthma:
Mild persistent:
Moderate persistent:
Severe persistent:
Long term control meds are necessary for all types of ___ asthma, which is defined by more than __ per wk in the day and @ night more than __ times per month

Back 6

1. Int- rescue inhaler PRN
2. Mild Per-- albuterol rescue inhaler PRN + ICS
3. Mod Per- albuterol rescue inhaler PRN, ICS, + LABA
4. Severe persistent: - albuterol PRN, systemic corticosteroids, and then ICS +LABA
- necessary for all persistent asthma
- more than 2x a week in daytime
- more than 2x a month at night

Front 7

Long term control meds of asthma help to ___ and ___ bronchial inflammation.
Quick relief medication are ___ agents

Back 7

1. inhibit and moderate bronchial inflammation
2. Bronchodilator meds which are used to reverse acute airflow obstruction

Front 8

Quick relief meds include:
1.
2.
3.

Back 8

1. SABA
2. Anticholinergics
3. Short burst of systemic corticosteroids (3-10 days)

Front 9

ICS: Use, MOA

Back 9

Use: used for all persistent asthma
MOA: suppression of inflammatory cytokines, prevents epithelial destruction and airway remodeling, increases responsiveness of beta receptors by reversing down regulation

Front 10

ICS: AE
How do you reduce AE?

Back 10

AE; hoarseness, dysphonia, and oral candidiasis
- at EXTREMELY HIGH doses will cause systemic SE-- glaucoma, skin thinning, decreased bone density. DOES NOT stunt growth
- minimize with spacer, gargle/rinse/spit

Front 11

Which of the ICS is most potent? What drug is best to use?

Back 11

Fluticasone, fluticasone b/c there is less frq dosing which increases compliance

Front 12

Which cell type do steroids suppress in asthma, but are not present in COPD as much? How long to ICS take to show full effect?

Back 12

eosinophils, neutrophils on the other hand are present in COPD but eosinophils are not
2-4 wks

Front 13

Systemic corticosteroids: Use

Back 13

Short term: 3-10 days
Long term: Only for very severe persistent asthma-- who cannot achieve adequate control wiht other agents-- try to do alternate day dosing

Front 14

Systemic steroids: AE

Back 14

- Lots of SE-- glu intolerance, cushings like, growth retardation, osteoporosis, htn, cataracts, skin thinning, myopathy, CNS effects (depression), impaired wound healing.
Chronic use requires tapering off if want to switch to ICS

Front 15

Mast cell stabilizer- not really used

Back 15

Cromolyn sodium

Front 16

LABA: MOA

Back 16

- directly stimulates B2 adrenergic rectprs which causes bronchial relaxation. will also effect mucociliary clearance and prevents release of histamines, LTs, and PGs from mast cells
- increases sensitivity to ICS

Front 17

LABA include ____, often given in combo with ____. Should not increase the amt of these combo products - dose of LABA is constant. To avoid tachyphylaxis what is the max dose of sal? of form?

Back 17

1. salmeterol
2. fluticasone
3. salmeterol= 100 mcg
4. formeterol- 24 mcg

Front 18

LABA: use

Back 18

ADD ON THERAPY! for moderate to severe persistent asthma and to enhance ICS
- prevents exercise induced bronchospasm
- regular schedule
- NOT a quick relief med

Front 19

Theophylline: MOA

Back 19

Unknown-- some SM relaxation from PDE inhibition
- increase diaphragm contractility and mucociliary clearance
- may decrease eosinophilic infiltration into bronchial mucosa

Front 20

Theophylline: PK, what is one notorious thing that will effect theophylline clearance?

Back 20

- narrow theraputic index- low serum levels -- 5-10 mcg/ml
- follows michaelis mentin kinetics with NON LINEAR saturation- small increase in dose can greatly increase serum concentration
- metabolized by cytochrome p450 hepatic enzyme pathways- diff ages metabolize differently
- bbq foods, mary jane, caffeine can all change theophylline levels
- smoking cessation will decrease clearance and will greatly increase serum concentration of theophylline

Front 21

Theophylline: AE

Back 21

At serum levels > 20mcg/ml
- N & V, nervousness, tremors, tachycardia/ palpitations, headache, & insomnia occurs w/ increasing frequency
At serum levels > 30mcg/ml
- Cardiac arrhythmias (mostly atrial), hypokalemia, hyperglycemia, seizure, hypotension, & coma can occur
Monitoring serum [ ] is recommended, particularly w/ higher dose or if DI is suspected

Front 22

Theophylline: Use

Back 22

Added to ICS- used when pt cannot afford LABA
- can be used as single controller tx if pt greater than 5 y/o but less effective that ICS

Front 23

LT modifiers: MOA

Back 23

Block Lt receptor site-- LTD4 and LTE4. LTs cause chemotaxis of inflam cells esp eosinophils, cause bronchoconstrction, and production of mucus and cause edema of airway wall

Front 24

LT modifiers include the drugs

Back 24

- zafirluksat, montelukast (singulair)

Front 25

LT modifiers:
Zafirlukast: AE
Montelukast: AE

Back 25

Zafirlukast: severe hepatotoxicity
Montelukast: mostly none, RARE insomnia, agitation, anxiety, depression

Front 26

Zafirlukast- DI

Back 26

- P450 Cyp2c9 and 3A4 inhibitor, and may increase effects of warfarin
- zafirlukast concentration can be increased by aspirin and decreased by eythromycin

Front 27

Montelukast- DI

Back 27

- phenobarbital decreases AUC, and no one uses phenobarb so none really

Front 28

LT modifier- USE

Back 28

- 2nd line alternative tx to low dose ICS in MILD persistent asthma
- in 20-30% just as efficacious as ICS
- good for pts with ALLERGIES
- good to ADD on to therapy--esp if you want to reduce the dose of ICS
- good for NSAID/aspirin induced asthma

Front 29

Omalizumab-MOA

Back 29

- anti IgE antibody- monoclonal antibody that binds to free IgE in circulation and blocks its attachment to surface of mast cells and basophils, preventing them from responding to allergens.

Front 30

Omalizumab- AE

Back 30

- injection site rxn, urticaria, anaphylactic rxns (very rare- BLACK BOX WARNING- thus only administer in health care setting)
- URI, sinustis, pharyngitis

Front 31

Omalizumab- Use

Back 31

- In pts greater than 12 who have very allergen specific asthma. must have postive skin test. Very expensive
- also should not be well controlled w/ normal meds

Front 32

SABA- MOA

Back 32

- directly stimualte B2 adrenergic receptors which results in bronchial relaxation
- increase mucociliary clearance and decrease release of histamines, LTs, and PGS from mast cells
- are selective-- rapid onset, and last for 2-6 hrs

Front 33

What is wrong with the over the counter short acting beta agonists?

Back 33

- non selective and shorter duration of action

Front 34

When should parenteral or oral beta 2 agonists be used?

Back 34

only in the most severe attacks when inhaled beta 2 agonists cannot be used

Front 35

SABA- AE

Back 35

- for systemic beta 2 agonists- may have cardiac stimulation, muscle tremor, nervousness, hypokalemia, and hyperglycemia

Front 36

SABA- Use

Back 36

DOC for acute asthma symptoms- PRN
- DOC for prevention of exercise induced bronchospasm and prevention of bronchospasm from predictable triggers

Front 37

SABA- monitoring

Back 37

- freq use is predictive of mortality
- may lead to drug tolerance
- may need to initiate other therapy with too much use
- avoid beta blockers-- including topical for glaucoma

Front 38

Anticholinergics- MOA

Back 38

- competes w/ ach at muscarinic receptor site-- cause decreased vagal tone to the airway and bronchodilation

Front 39

Atropine- PK, Use

Back 39

- very limited b/c of anticholinergic SE, tertiary struc, systemically absorbed

Front 40

Ipratropium bromide inhaler- PK, Use

Back 40

- not FDA approved for asthma, but has quat struc so is not absorbed systemically
- helps to dx between COPD and asthma
- added to B2 agonist adn systemic corticosteroids in SEVERE asthma exacerbation
- alt if pts unable to handle SABA
- good for emotionally induced asthma

Front 41

Systemic corticosteroids- Use, Drugs

Back 41

- hydrocortisone, methylprednisone, prednisone
- use drugs w/ short half life
- short burst -- 3-10 days- can stop abruptly after 2 asx nights
- most effective drugs for pts completely unresponsive to SABA
- good for children in whom death may result otherwise

Front 42

Recommendation for asthma in pregnancy?

Back 42

- pregnancy may cause asthma
- inhaled steroids are now recommended
- LABA if moderate persistent
- albuterol
- if need oral corticosteroids-- prednisone is best but in 1st trimester may cause cleft palate