Drugs for Obstructive Lung Dz Flashcards
SABA
Albuterol- DOC
pirbuterol
terbutaline
Levobuterol
SABA- MOA
stim Beta 2 of bronchial tree –> inc cAMP/ decrease intracellular Ca –> relax SM
SABA- physiologic effects
bronchodilation
inc mucocilliary clearance
dec immune mediators
SABA- use
all asthma pts should have as a recue inhaler
Asthma- PRN during an attack, before exposure to trigger
COPD- part of initial tx as a scheduled drug
SABA- AE
tachycardia, anxiety
prolonged QT interval
tremor, hypoK, hypoglycemia
SABA- route of admin and AE
injected > oral > inhaled
SABA- mortality AE
causes down reg of Beta 2 in response to overstimulation –> inc mortality
Anticholinergic drugs
Ipratropium Bromide, Tiatropium
Atropine
Anticholinergics- MOA
competitive antagonist for Gq linked Ach receptor –> dec cytoplasmic Ca –> dec vagal tone and cause brochodilation
SABA need to know
beta agonist –> bronchodilation
(asthma): DOC- recue inhaler (PRN during attack), pre exposure
(COPD):initial tx, scheduled med
AE: tachycardia, anxiety
risk: inc mortality b/c of down- regulation of beta 2 receptors from overstimulation
Anticholinergic axn
Bronchodilation, dec vagal tone
Anticholinergics use
COPD- DOC as scheduled med
Asthma- add to Beta 2 agonist and steroid in status asthmaticus
emotionally triggered asthma if cant tolerate SABA
Iptratropium bromide and tiatroium
quaternary anticholinergics= less systemic absorption and NO CNS penetration= no systemic effects
15 min onset
Atropine
tertiary anticholinergic can cause- blurred vision, tachy, and urinary retention
Anticholinergics-shouldnt be sprayed where
IN THE EYES
Anticholinergics need to know
block Ach binding --> bronchodilation COPD- DOC as scheduled med status asthmaticus (3rd drug) emotionally triggered asthma (if cant tol SABA) quaternary- no systemic AE Atropine- does have systemic AE
Systemic Corticosteroids- drugs
Prednisone
Methylprednisone
hydrocortisone
prednisolone- pediatrics
Systemic corticosteroids- MOA
inhibit NfKb –> stop the inflammation
Systemic corticosteroids- uses
Exacacerbations that are not responsive to SABA = bust therapy= non tapered 3-10 days with 2 asymptomatic nights and FEV1 at 80% of the max
Systemic Corticosteroids- burst therapy and growth
doesn’t effect growth
Systemic corticosteroids- NTK
most effective
inhibit NfKb –> stop inflammation
used in Burst therapy
dont inhibit growth
Daily meds for pts with persistant asthma
ICS- DOC for all persistent asthma pts
Systemic corticosteroids- dont want to use these
ICS- drugs
fluticosone budenoside beclamethasone flunisolide triamcinolone
ICS- use, advantages
daily med for pts with persistent asthma
advantages- dec asthma related deaths and stop remodeling
ICS- MOA
suppress inflammatory cytokines
prevent epithelial destruction and airway remodeling
block Eos recruiting
ICS- and beta agonists
inc response to beta agonists by inhibiting beta receptor downregulation
ICS- AE
normally well tolerated
hoarseness, dysphonia, oral candidiasis
high dose: glaucoma, skin thinning, dec bone density.
ICS- how to prevent AE
rinse, gargle, spit
spacer
vaporizer
for high dose effects of dec Bone density - give Vit D and Ca supplements to post menopausal women
ICS- dosing
goal is to tx with stronger meds at less frequent intervals b/c better compliance
have steep dose response curve so as inc the dose may inc AE more than benefit
Fluticasone is strongest > budenoside > beclamethasone > flunisolide> triamcinolone
ICS- NTK
DOC as daily med in persistant asthma
suppress inflammatory cytokines and prevent epithelial destruction
AE of hoarseness, dysphonia, and oral candidiasis can be prevented with rinse/ gargle
DON’t stunt growth
work synergistically with SABA
Systemic Corticosteroids as persistent med- use
dont want to use them due to AE
used for asthma refractory to ICS and LABA
what do u do if using systemic corticosteroids for more than 14 days
taper the dose to alternate day
systemic corticosteroids- AE
Growth retardation Cushing syndrome Glucose intolerance cataracts osteoporosis HTN myopathy imparied wond healing PUD mood distrubances avascular necrosis of the hip hypokalemia depression
Systemic corticosteroids as daily med- NTK
dont use, bad effects
if using more than 14 days taper
ONLY TIME THESE CAUSE GROWTH RETARDATION
LABA- drugs
Salmeterol
Formoterol
Normally in combo w/ ICS
LABA- use
DOC for addition to ICS
LABA- MOA
same as SABA but take longer
improve responsiveness to ICS
LABA- CI
CI in use w/o an ICS b/c of excessive B2 down regulation
LABA- AE
Tachyphylaxis
LABA-dosages (esp in combo)
if on combo med and change the dose this only inc the dose of ICS, not LABA
PTS CANNOT INC DOSE BY DOUBLING UP ON SPRAYS B/C ALREADY MAXED OUT ON LABA
LABA- NTK
DOC for adding to ICS
CI if not added
AE- tachyphylaxis from B2 downregulation
cant inc by taking more sprays
Methylxanthies- drugs
Theophylline, Aminophylline
Methylxanthies- MOA
unknown
PDE inhibitors –> inc cAMP
antagonize adenosine
Methylxanthine- axn
mild bronchodilators
Methylxanthine- and adenosine
block anti arythmatic effect of adenosine
Methylxanthine- kinetics
They have a very narrow therapeutic dose
non linear kinetics = small dose inc –> big inc in serum concentration= saturation kinetics
MM kinetics
methylxanthines- uses
Add to ICS instead of LABA
mono tx in kids under 5
Metabolism
CYP450 3a4= drug interactions
CYP450 inducers= phenytoin, phenobarbital, carbimazapine
Inhibitors= Cimetidine, Ciprofloxacin, INH
Methylxanthine- elimination
quickest in younger pts
smoking
blackened food
slower in older pts and hepatic dysfunction
methylxanthines and smoking
smoking inc rate of metabolism so pt require a higher dose.
IF pts are going to stop smoking need to tell the doc so can dec dose.
drug reacts with the PCAs in the cig not the nicotine
methylzanthines- AE
lower dose- N/V HA, insomnia, tremor, tachycardia and palplatations
higher dose- hypoK, hyperG, seizure, hypoTN, arrythmia
Methylxanthins- NTK
have narrow therapeutic index- MM kinetics smoking (PCAs) inc rate of metabolism met slower by hepatic dysfunction can use instead of LABA to add to ICS can use as monto tx in pts under 5
Leukotriene modifiers- drugs
Zafirlukast
Motelukast
LT mods- MOA
block receptor site for LT –> bronchodilation
prevent chemotaxis of inflammatory cells esp eos
prevent mucus secretion and airway edema
LT mods- use
asthma- not everyone responds to this but if pt does very good
if pt can handle LABA use this PO
second line addn to ICS instead of LABA
Comorbid rhinitis, exercise induces asthma and ASA/NSAID induced asthma
Zafirlukast- AE, use
SEVERE HEPATOTOXICITY
potentiates Warfarin, potentiated by ASA dec in erythromycin
almost never used
Montelukast- AE and use
mild HA,
FDA approv for allergic rhinitis
ASA induced Asthma
LT mods- AE
depression, insomnia, anxiety
Omalizunab
anti IgE Ab
sub q
Omalizunab- MOA
binds free IgE in circulation and prevents it from binding to mast cells and basos- cant respond to allergens
Omalizunab- uses
asthma in pts >12 y/o with testing verified allergen and Th2 rxn.
must be in facility w/ EPI b/c anaphylaxis can happen
Anti Asthmatics in pregnancy
ICS add LABA
have SABA on hand
acute exacerbation in preg= prednisone
Tx Ashthma goals
prevent airway remodeling (ICS)
use inhaler less than 2x/ week
normal asymptomatic activity and normal PFTs
minimal chronic symptoms