Respiratory/MSK Flashcards
Salmeterol
Long-acting B2-agonist
Inhaled
Manage moderate persistent and severe asthma
Never used alone in monotherapy; always with glucocorticoid
2-4 hour onset with 12 hour duration (never for acute relief)
Tremor, tachycardia and hypokalemia at high doses
Albuterol
Short-acting B2-agonist
Inhaled
Treat acute bronchospasm/Symptomatic relief
1-5 minute onset with 2-6 hour duration
Fluticasone
Inhaled glucocorticoid
Mainstay for chronic asthma
Weeks to months required for best effects
Candida, bone density loss, skin thinning and dysphonia (dose-dependent)
Nasal sprays and topical preps for allergic rhinitis and skin conditions
Prednisone
Systemic glucocorticoid
Manage chronic, severe asthma and episodes requiring hospitalization
6-12 hour duration
Little toxicity unless used long-term
Cromolyn Sodium
Inhibit mast cell degranulation MOA unknown Inhaled Rare side effects Less effective than glucocorticoids
Montelukast
Leukotriene inhibitor
Competitive antagonist of CysLT1 receptor
Oral
Liver metabolism
Less effective than glucocorticoids and B-agonists
Zileuton
Leukotriene inhibitor
5-lipoxygenase antagonist
Oral
Liver metabolism - associated with liver toxicity
Less effective than glucocorticoids and B-agonists
Theophylline
Bronchodilator Methylxantine (CNS stimulant) MOA?? = cAMP PDE and adenosine receptor antagonist Oral Many side effects (caffeine-like) 2nd or 3rd line asthma therapy Very inexpensive
Omalizumab
Anti-IgE
Humanized monoclonal Ab against Fc region
Reduces free IgE more than 95%
Used for moderate to severe persistent asthma
Reduce dependency on corticosteroids and decrease episodes
Treat other allergic disorders (rhinitis and food allergies)
SubQ injection every 2-4 weeks
Rare side effects - Injection site reactions, anaphylaxis and malignancy
Expensive
Histamine
H1 - Immediate hypersensitivity reactions
H2 - Gastric acid secretion
Rapid breakdown in serum (short term local effects)
H receptors have basal activity (antagonists = inverse agonists)
Diphenhydramine
First generation H1 competitive antagonist
CNS penetration
Treat hypersensitivity reactions, motion sickness and urticaria
Sedation, GI effects, and antimuscarinic effects
Loratadine
Second generation H1 antagonist
Better specificity with fewer side effects
No drowsiness or antimuscarinic effects
Treat hypersensitivity
Cromolyn
Inhibition of mast cell activation
Prophylaxis for allergic bronchial asthma
Take weeks for effectiveness
Not useful for many individuals
Ranitidine
Competitive H2 antagonist
Treat gastric ulcers and GERD
Rare side effects (diarrhea, dizziness, muscle pain, rash, gynecomastic, CNS effects)
Effects on acid secretion changes F/absorption for other drugs
Isoniazid
Most active anti-TB drug
Pro-drug activated by mycobacterial catalase
Inhibits fatty acid elongation (two enzymes) and DHFR
Acetylated in liver - bimodal distribution of half-life (high rate dominant)
Neurological toxicity - competes with B6 metabolism
Hepatic toxicity