Pulmonary Pharmacology: Anti-inflammatory Rx Flashcards
What are the 4 general categories of anti-inflammatory drugs?
- ICS (1st & 2nd gen)
- Oral & IV corticosteroid
- Leukotriene pathway inhibitor
- Monoclonal antibodies
Why are there no drug interactions for monoclonal antibody drugs?
metabolized by antibodies
Hoarse voice and oropharyngeal candidiasis are common side effects of which class of drugs?
corticosteroids
What is the genomic vs. non-genomic mechanism of action for anti-inflammatory Rx?
genomic: decreases TH2 cytokines
non-genomic: inhibits arachidonic acid production
If a patient has perennial aeroallergen that is not well controlled w/inhaled corticosteroids, what would you recommend?
omalizumab
Which bronchodilator is used to treat nasal polyps that are not responding to nasal corticosteroids?
omalizumab
(costs up to $2,706 for one month’s supply)
Which bronchodilator blocks binding of IgE to FcERI on mast cells and basophils?
omalizumab
How does omalizumab provide extra protection after viral illness?
enhances type 1 IFN, reducing FCeRI
How is omalizumab dosed?
measure IgE + patient’s body weight
bronchospasm, hypotension, syncope, uticaria, angioedema of throat are symptoms of which condition?
anaphylaxis
(omalizumab, ipratropium & tiotropium may cause this)
Hoarse voice and oropharyngeal candidiasis are common side effects of which class of drugs?
corticosteroids
Dupilumab v. omalizumab: both decrease prevent the effects of IgE. How are they different?
Dupilumab: IL-4 Receptor blocker (prevents IgE synthesis)
Omalizumab: IgE binding
(decreasing production ineffective, MUST bind receptor)
When would you use omalizumab or Dupliumab?
severe asthma
symptoms inadequately controlled w/ICS
What is the main difference in the function of IL-4 and IL-5 as it pertains to respiratory inflammation?
IL-4 enhances IgE synthesis
IL-5 keeps eosinophils alive
“5 keeps eosinophils alive”
Which 2 drugs target IL-5 antibodies?
(prevents eosinophil survival)
- mepolizumab
- reslizumab
Which drug targets IL-5 receptor?
(prevents eosinophil survival)
Benralizumab
IL-5 inhibitors benefit the patient by decreasing the need for which therapies?
maintenance dose of ICS
(reduces exacerbations by 50%)
Which general class of medicine is indicated for severe asmtha, but NOT reducing COPD exacerbations?
IL-5 inhibitors
Which drug can treat severe asthma, atopic dermatitis and rhinosinusitis?
Dupilumab: IL-4 inhibitor
What is the treatment for aspirin-sensitivity asthma?
leukotriene pathway inhibitors
when COX-2 is inhibited, no arachidonic acid –> more leukotrienes
Which 3 medications are used for prophylaxis and maintenance therapy for asthma?
- zileuton
- zafirlukast
- monteleukast
(cromolyn = also prophylactic)
Which 3 respiratory medications are contraindicated for patients with liver disease?
- zileuton
- roflumilast
- theophylline
Zileuton is metabolized by which CYP enzymes?
1A2
3A4
2C9
Why does zileuton increase levels of theophylline, warfarin and propranolol when co-administered?
it has a high level-of plasma protein binding and so do the other drugs
Which medications can be given to patients 12 months and older to treat asthma?
montelukast
Which 2 medications also treats allergic rhinitis in addition to asthma?
- Montelukast
- Omalizumab
Montelukast is excreted exclusively through what?
bile
must monitor liver function
Which asthma medication has a black-box warning for suicidal thoughts as a side effect?
Montelukast
In addition to suicidal thoughts as a side effect, montelukast may also cause which side effects?
- upper respiratory infections
- churg-strauss
Which medication is a CysLT1 receptor antagonist?
monteleukast
Which medication is a selective and competitive antagonist of the leukotriene D4 and E4?
zafirlukast
Why is it particularly dangerous to combine Zafirlukast with warfarin (2)?
- Zafirlukast is metabolized by CYP2C9, which is inhibited by warfarin
- zafirlukast is almost 100% bound by plasma proteins
Vasculitic rash, eosinophilia and neuropsychiatric effects are side effects of which respiratory medication?
Zafirlukast
Which 4 medications are used as asthma prophylaxis?
- cromolyn
- zileuton
- zafirlukast
- monteluekast
(the first 3 are also used as maintenance therapy)
Cromolyn indication
asthma prophylaxis
Cromolyn mechanism of action
mast cell stabilizer by Ca2+ blockade
this inhibits immediate and non-immediate bronchoconstriction
Which antitussive (cough suppressant) inhibits mu receptors? which inhibits sigma?
both are opioid receptors in the medullary cough center
- codeine inhibits mu
- dextromehtorphan inhibits sigma
Which antitussive is a local anesthetic
respiratory use: lungs, pleura and respiratory passages
benzoate
Visual hallucinations is a side effects of which antitussive (cough suppressant)?
benzoate
Which 2 neuromodulators can be used as an antitussive?
for chronic idiopathic cough
- gabapentin
- pregabalin
somnolence and dizziness are side effects of which 2 antitussives?
- pregabalin
- gabapentin
Morphine and methadone are indicated for which condition?
intractable cough in bronchial carinoma
targets cough receptors in proximal airways
caution w/codeine
enzymatic polymorphisms: high levels of CYP 2D6 –> higher levels of morphine
dextromethorphan is a derivitive of which drug?
levorphanol
(codein analog)
codeine analog
dextromethorphan
In addition to activating sigma opioid receptors in cough center, dextromethorphan also acts as ______(2).
- NMDA antagonist
- oneirogen (pschadelic)
Adverse effects of dextromethorphan
- toxic psychosis
- serotonin syndrome
- dystonia
- blurred vision
- change in muscle reflexes
