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30 Cards in this Set
- Front
- Back
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airway innervation
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muscarinic - M1 (small airway constrict), M3 (large airway constrict), M2 (modulate M1 & M3)
sympathetic - β2 bronchodilate SMC/wall thick increases in small airways --> greater affect in dz and in Rx |
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Cell Types in Astma & COPD
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Asthma - T cells, eos, mast, IgG B lymphocytes
COPD - neutrophils, alveolar macrophages, CD8+ lymphocytes |
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Inhaled drug delivery
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gets drugs to site of dz (1-5 um droplets)
more complicated than PO Metered Dose Inhalers (portable) Nebulizer (easier to take, needs compressed air) Dry powder inhaler - higher inspiratory flow rate needed High 1st pass metabolism + low bioavailability allow Rx to work at site of action, but decreases AE |
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Epinephrine
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Primatene (OTC, if they are taking it they are not plugged in to medical care, high risk pt!!!)
First bronchodilator, but non selective α and β stimulation causes HTN, tachycardia, tremor, arrhythmias, along with bronchodilation |
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Isoproterenol
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β1 and β2 stimulation, better than epi, but still causes tachycardia and arrhythmias
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Albuterol
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most commonly used β2 agonist, available as MDI, nebulizer, or PO
Q4-6 dosing |
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Pributerol
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just like albuterol
breath actuated MDI |
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Salmeterol
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Long acting β2 agonist, not for quick relief
Q12 |
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Formeterol
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β2 agonist, long acting, quicker onset than salmeterol, but still not for immediate relief
Q12 |
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Levabuterol
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R stereoisomer of albuterol
slightly less tachycardia, not more effective $$$ (just use albuterol) |
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Arfomoterol
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R,R stereoisomer of formeterol, no clear advantage
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MOA for β2 agonists
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activation of AC --> incr cAMP --> activated protein kinase A --> inhibits phosphorylation of myosin --> decr intracelluluar Ca++ --> decr muscle tone
hyperpolarization down regulation of receptors w/ chronic use Some Bronchoprotective effects |
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Side Effects of β2 Agonists
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cross reactivity or cardiac β2 receptors: tremor, tachycardia, nervousness
LONG ACTING SHOULD ONLY BE GIVEN AS CORTICOSTEROID ADD ON Hypokalemia |
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Glucocorticoids
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anti-inflammatory, most effective Rx, inhaled reduces side effects
Part of any treatment for worse that mild intermittent |
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Glucocorticoid MOA
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bind Glucocorticoid Response Elements that transcribe anti-inflammatory mediators
inhibit inflammatory mediators via histone acetyl transferase antagonize recruitment of histone deacetylases decreasing inflammatory gene transcription --> inhibit cytokine production by macrophages, T-lymphocytes, eos, airway epithelial cells |
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Glucocorticoid specific agents
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Beclomethasone Dipropionate, Budesonide (peds), ciclesonide, fluticasone, flunisolide, mometasone, triamcinolone acetonide
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Glucocorticoid Side Effects
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systemic admin: mood liability, loss of glycemic control, osteoporosis, PUD, cataracts (#1 according to Goljan), decreased growth velocity, HTN (Minimize w/ short duration burst therapy)
Inhaled admin: Dysphonia, Candidiasis, Pneumonia (wash mouth out after) |
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Leukotriene Modifiers
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decrease production of and binding to receptor by cysteinyl leukotrienes (cause bronchial contraction and recruit eos and basos)
add on to corticosteroids or steroid sparing agent large variability in pt response Receptor Antagonists (Montelukast & Zafirlukast) - safe, qd & bid respectively Synthesis inhibitor (Zileuton) - may increase liver enzymes, same effects as receptor antagonists |
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anticholinergics
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slow onset, useful in COPD, combo w/ β2s
AE - systemic: anticholinergic, inhaled: dry mouth, respiratory secretions Ipratropium Bromide qid Tiotropium Bromide qd Typically given in acute COPD or Asthma exacerbation w/ other Rx will decrease likelihood of admission |
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Cromolyn Sulfate
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mast cell stabilizer, outstanding safety
needs to be taken before exposure or chronically |
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Theophylline
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Its cheap, its oral, but it will make you sick ...
third line tx, anti-inflammatory, bronchodilatory, used in advanced COPD AE: nervousness, tremor, dyspepsia --> n/v, tachycardia, seizure |
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Omalizumab
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anti-IgE, sq admin, $$$
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etc asthma Rx
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antihistamines - don't help
Mg - acute exacerbation, brownie points on ER rotation Allergen immunotherapy - awesome if symptoms a result of an allergic rxn Influenza immunization - vaccines are dangerous in general, they give you guillan-barre and they kill babies (at least thats what the lady in whole foods told me) |
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PAH tx
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secondary - tx underlying dz
primary - mild/moderate: sildenafil or endothelin receptor antagonists, late stage: prostacyclin active agents |
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Phosphodiesterase Type 5 Inhibitors
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Sildenafil tid (viagra), Tadalafil qd
PDE5 in pulm and penile vasculature vasodilatory, antiproliferative, proapoptotic effects |
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Endothelin Receptor Antagonists
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prevents vasoconstriction
Bosentan - stabilizes, $$$, AE: liver damage Ambrisentan - not better than Bosentan, similar price |
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Prostacyclin Active Agents
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Epoprostenol - improve symptoms, lengthen time to transplant, vasodilatory, inhibits platelet aggregation, inhibits SMC prolif
Treprostinil - sq analog of prostacyclin, $$$$ Iloprotst - inhaled prostacyclin, AE: HOTN syncope |
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CCBs
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effective in 10% of pts w/ PAH, can cause dramatic HOTN in some pts
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Idiopathic Pulmonary Fibrosis tx
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prayer?
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Smoking cessation
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Nicotine replacement
Varenicline - best results, nausea in some pts Bupropion - antidepressant, good results |
