leukotriene modifiers, methylxanthines, and anti-IgE Flashcards
montelukast brand
singulair
montelukast (singulair) dosage form
tablets (chewable) - 4mg, 5mg, and 10mg
granule packets - 4mg
zafirlukast brand
accolate
zafirlukast (accolate) dosage form
10 or 20 mg
zileuton brand
zyflo CR
zileuton (zyflo cr) dosage forms
IR tablets - 600 mg
ER tablets - 600 mg
leukotriene modifiers
block the production of leukotrienes
montelukast (singulair)
zafirlukast (accolate)
zileuton (zyflo)
montelukast (singulair) dosing in 0-4 yos
approved for 1 to 5 yos
4 mg qhs
montelukast (singulair) dosing in 5-11 yos
approved for 6 to 14 yos
5mg qhs
zafirlukast (accolate) dosing in 5-11 yos
10 mg bid
montelukast (singulair) dosing in adults
10mg qhs
zafirlukast (accolate) dosing in adults
20 mg bid
zileuton (zyflo cr) dosing in adults
IR - 600 mg qid
ER - 1200 mg bid
adverse effects of leukotriene modifiers
neuropsychiatric events (agitation, anxiety, abnormal dreams, hallucinations, depression, suicidal thinking)
churg-strauss syndrome (rare)
increases transaminases (specifically zafirlukast and zileuton)
clinical pearls of leukotriene modifiers
less effective than low dose ICS and ICS/LABA combos in asthma
have not been adequately trialed in COPD
montelukast (singulair) clinical pearls
minor substrate of CYP2C8/9 and 3A4
not for acute relief of symptoms
boxed warning for neuropsychiatric events
zafirlukast (accolate) clinical pearls
take at least 1 hour before or 2 hours after meals
can increase INR
major substrate, minor inhibitor of CYP 2C9
zileuton (zyflo cr) clinical pearls
weak cyp1A2 inhibitor
take with food
methylxanthines
bronchodilation through inhibition of PDE 2 and 4
theophylline (theochron)
theophylline brand
theochron
theophylline (theochron) dosage form
ER 12H tabs - 100, 200, 300, 400, and 450 mg
ER 24H tabs - 400 and 600 mg
ER 24H Caps - 100, 200, 300, and 400 mg
Liquid - 80mg/15mL
theophylline (theochron) acute exacerbation dosing in adults
loading dose typically given IV as aminophylline
followed by maintenance IV infusion
theophylline (theochron) chronic management dosing in adults
smokers - 16mg/kg/day divided
nonsmokers - 13mg/kg/day divided
theophylline (theochron) dosing in adults
doses based on serum concentrations and treatment of acute exacerbations or chronic management
target range 5-15mcg/mL
toxic is greater than 20 mcg/mL
adverse effects of theophylline (theochron)
insomnia
gastrointestinal upset
hyperactivity
hypotension (PDE 3 inhibition)
tremor
dose related toxicity of theophylline (theochron)
tachycardia (PDE 3 inhibition)
nausea (PDE 3 inhibition)
vomiting
headache
seizures
arrhythmias
contraindications of theophylline (theochron)
peptic ulcer disease
arrhythmias
seizure disorders
drug interactions of theophylline (theochron)
major substrate of cyp3a4, 1a2, and 2e1
increase concentration - cimetidine, erythromycin, clarithromycin, ciprofloxacin, ticlopidine
decrease concentration - phenobarbital, phenytoin, carbamazepine, rifampin (and smoking)
anti-IgE drugs
inhibit IgE binding to receptors on mast cells and basophils
inhibit mediator release and attenuation of early and late phase allergic response
omalizumab (xolair)
omalizumab brand
xolair
omalizumab (xolair) dosage forms
150mg/1mL prefilled syringe
75mg/0.5mL prefilled syringe
150mg/1.2mL after reconstitution with 1.4mL of sterile water for injection
omalizumab (xolair) dosing in 5-11 yos
approved for over 6 yos
150 to 375 mg sq every 2 to 4 weeks depending on body weight and pretreatment serum IgE levels
omalizumab (xolair) dosing in adults
150 to 375 mg sq every 2 to 4 weeks depending on body weight and pretreatment serum IgE levels
adverse effects of omalizumab (xolair)
headache
injection site reactions
arthralgias
thrombocytopenia
pharyngitis
sinusitis
upper respiratory tract infections
boxed warning for omalizumab (xolair)
anaphylaxis
clinical pearls of omalizumab (xolair)
do not give more than 150mg per injection
monitor for anaphylaxis before and after injection
FDA approved for moderate to severe persistent asthma in patients with a positive skin test or reactivity to a perennial aeroallergen and symptoms that are inadequately controlled with ICS