Anti-inflammatory drugs Flashcards
Anti-inflammatory drugs
Mast cell stabilizers
Leukotriene receptor antagonists
Corticosteroids
Prednisone
Mast Cell stabilizers
cromolyn sodium (intal, inhaler), nedocromil (Tilade, inhaler), omalizumab (Xolair, SQ)
Kinetics of Mast Cell stabilizers
Low oral absorption, good resp absorption (inhaler/SQ)
Excreted unchanged in feces
2-4 weeks for therapeutic effect
MOA of Mast Cell stabilizers
Exact mechanisms unknown Inhibits mast cells from rupture Inhibits release of inflammtory mediators from mast cells - histamines and leukotrines Not a bronchodilator Never use as a rescue drug
Cautions with Mast Cell stabilizers
Do not use for acute brochospasm or status asthmaticus - Use only for prophylaxis
CV patienrs
Lactose intolerant patients
Adverse effect with Mast Cell stabilizers
Cough, bad taste, irritation of oropharnx
Headache, dizziness, nausea, rhinitis, eosinophilic pneumonia
Brochospasms (Rebound effect with increase use or abrupt d/c)
Education with Mast Cell stabilizers
Not used for managing acute symptoms - prophylaxis only
Must take daily if have symptoms or not
Take 15-20 min before activity that will induce bronchospasms or exposure to antigens
Leukotreine receptor antagonists
Most effective for long term control of asthma
zafirlukast (Accolate): take orally on empty stomach (best absorption)
montelukast (Singulair): chewable and regular tablets (take at night for best absorption)
zileuton (Zyflo): oral (BID, TID, QID d/t short halflife)
MOA of a Leukotreine receptor antagonists
NOT A BRONCHODILATOR
Zafirlukast and montelukast
- Block receptors for leukotreines bound to amino acid cysteine (Bronchoconstrictor)
zileutron
- inhibit first enzyme in lipoxygense pathway = Decrease production of leukotrienes = decrease inflammation
Cautions with Leukotreine receptor antagonists
Liver disease patients (montelukast is the best choice)
Psych hx
Adverse effects with Leukotreine receptor antagonists
Increased LFT’s (zafirlukast and zileuton), increased psych events (BB warning)
Fever, rash, anaphylaxis, headache, and dizziness (zafirlukast)
Drug interactions with Leukotreine receptor antagonists
zafirlukast
- increased effects of warfarin
- Theophyline and erythromycin decrease levels of zafirlukast
Zileuton
- Increase effects of warfarin, theophylline and propranolol
montelukast
- decreased effectiveness when taken w/ phenobarbital and rifampin
Corticosteroids
last resort tx d/t side effects
flunisolide: MDI
fluticasone: MDI
beclomethasone (Vanceril): MDI and nasal inhaler
prednisone: oral
methylprednisone (Solu-Medrol, Medrol): IV or oral
Kinetics of Corticosteroids
Good absorption thru GI and resp tract Highly protein bound Liver metabolism, some renal clearance Need to be continuously used to maintain effect NOT DILATORS, NOT USED FOR ACUTE ATTACKS
MOA of Corticosteroids
Suppresion of cytokine, leukotriene and prostoglandin production
Suppression of airway eosinophil recruitment
Suppression of release of inflammatory mediators
- All lead to decreased capillary dilation = decreased migration/activation of WBC’s = decreased inflammation
Increases number of beta receptors (Increased sensitivity to beta meds)