OLD Pharm Flashcards
two drug targets in asthma and COPD
inflammation and constricted airways (bronchodilators)
6 inhaled corticosteroids
beclomethasone, triamcinolone, flunisolide, fluticasone, budesonide, mometasone
IV corticosteroid
solumedrol
Oral corticosteroid
prednisone
LOX inhibitor
zileuton
leukotriene antag
motelukast, zafirlukast
omalizumab
IgE antibody
mepolizumab
IL-5 antibody
dupilumab
IL-4 antibody
PDE4 inhib
rolumilast
mast cell stabilizer
cromolyn
SABAs
albuterol, epi
LABAs
salmeterol, formoterol, indacaterol
SAMAs (short acting anti cholinergic)
ipratropium
LAMAs (long acting anti cholinergic)
tiotropium, aclinidium, umeclidinium, glycopyrronium
ANS regulation of bronchiole SM
PSNS: less O2 needed, M3 activation and constriction
SNS: more O2, B2 activatio and dilation
M3 agonist
methacholine
maintenance therapy for asthma
LABAs, LAMAs, SAMAs
indications for epi, target, delivery
hits all SNS receptors, for anaphylaxis
subQ
ITD for albuterol (indications, target, delivery)
B2, asthma acute, inhalation prn
why albuterol only for rescue?
receptor desensitization/ downregulation w/ regular use
differentiate LABAs salmeterol/formoterol from indacaterol w/ ITD
all are B2 selective
first two are indicated for asthma and COPD, second is only COPD
all orally inhaled twice daily except indacaterol is once daily
important toxicities of B2 agonists
mainly cardiac for cross agonism of B1 (tachycardia, angina, a fib, etc)
strength of B2 agonist on receptor
all partial except epi
3 variables for toxicities of inhaled drugs
how much is systemically (blood) absorbed?
clearance/metabolism
receptor selectivity
how is most inhaled drug absorbed
95% swallowed, some is indirectly from mucociliary clearance then swallowed, toxicites occur in systemic circulation
most cardiotoxic B2 agonists
epi, indacaterol, then formoterol is moderate
which 2 M3 antagonists are indicated for asthma in addition to COPD?
ipratropium (SAMA), tiotropium (LAMA)
toxicities of M3 antagonists
parasympathetic related (lowering rest and digest): dry mouth (xerostomia), constipation, tachycardia, Urinary retention (Umeclidinium)
except aclidinum?
two main aspects of inflammation inhibition from steroids
reduction of cells: eos, mast cells, dendritic cells
reduction of cytokines: from t lymphos, macros, epithelial cells, SM
consequence of chronic steroid use
infection susceptibility- thrush and pneumonia from oral inhalation
pregnancy risk for CS
inhaled options relatively safe, prednisone less so
CS combo drugs
why?
LABAs always combined w/ inhaled corticosteroids
LABAs alone had higher asthma death rate
CS effect on bronchiole SM
increases B2 receptors, higher responsiveness to bronchodilators
effect of leukotriene inhibs
reduce Sx of respiratory inflammation
zileuton target
LOX enzymes in mast cells and eos- inhibit LT production
-lukast target
LT receptors in bronchiole SM, prevent constriction, plasma exudation/mucus
CS effect on LK activity
stimulate lipocortin production which inhibts phospholipase A2 and thus all eicosanoids
indication for LK inhibs
allergic asthma
montelukast toxicities (2)
Churg Strauss syndrome (eosinophilic granulamatosis w/ polyangiitis, autoimmune vasculitis)
reports of neuropsych disturbances- suicide
(not FDA confirmed)
indication of omalizumab
IgE allergic asthma, given once every 4 weeks
indication of mepolizumab
severe eosinophilic asthma, once every 4 weeks
theophylline moa
bronchodilation: inhibits PDEs (allows for cAMP buildup and more more inhibition of contraction), competitive adenosine antagonist (adenosine causes contraction)
also has anti inflammatory mechanisms
theophylline toxicities
CNS- headache, seizures
cardiac- arrhythmias
GI- nausea, diarrhea
non selective PDE inhib, low therapeutic index
moa of cromolyn
stabilize mast cell and prevent release of inflammatory mediators (in response to IgE/allergen
roflumilast moa
PDE4 selective inhib- fewer toxicities than theophylline
indications/dosing of roflumilast
for COPD, oral