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58 Cards in this Set
- Front
- Back
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Beta-2 agonists, short acting (SABAs)
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- rapid relief of contracted airways w/o modifying frequency or severity.
- "Short-term relievers" - MOA - promotes intracellular cAMP, increases rate of synthesis by adenylate cyclase (AC), which promote bronchodilation - 3-4 hrs, used for rescue -> effects begin 5-15 min, peak ~15-30 min - AE's: tremor, tachycardia/palpitations, dizziness, bronchoconstriction (paradoxical), heartburn, hypokalemia, hyperglycemia, prolonged QT, sudden cardiac death |
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Albuterol
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- SABA
- MDI, Nebulizer, tablets, syrup |
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Terbutaline
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- SABA
- Oral, injection |
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Levalbuterol
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- SABA
- MDI, Nebulizer -> dose = 1/2 RS |
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Beta-2 agonists, long acting (LABAs)
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- anti-inflammatory modify edema and cellular infiltration; reducing severity and frequency.
- "Long-term controllers" - MOA - promotes intracellular cAMP, increases rate of synthesis by adenylate cyclase (AC), which promote bronchodilation - 12-24 hrs - NOT FOR TX of ACUTE - AE's: tremor, tachycardia/palpitations, dizziness, bronchoconstriction (paradoxical), heartburn, hypokalemia, hyperglycemia, prolonged QT, sudden cardiac death |
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Salmeterol
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- LABA
- DPI, Slow onset (20-30 min b4 start of relaxation) - 1st approved - Highest sudden cardiac death concern |
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Formoterol
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- LABA
- DPI, Nebulizer - Not labeled for rescue, but very fast onset (~5 min) |
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Indacaterol
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- LABA
- Ultra long acting >24 hrs - Once a day approved in Europe, twice a day for COPD - Attaches to receptor for very long time |
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Antimuscarinics
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- rapid relief of contracted airways w/o modifying frequency or severity.
- "Short-term relievers" - MOA - Blocks Ach which normally causes bronchoconstriction - AE's: Urinary retention, glaucoma, blurry vision |
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Ipratropium bromide
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- Antimuscarinic
- MDI, Nebulizer, nasal spray - COPD - insoluble quaternary ammonium atropine derivative - fairly rapid onset, not for rescue, 2-4X day |
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Tiotropium bromide
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- Antimuscarinic
- Selective M1, M3 (dissociates quickly from prejunctional M2) - DPI; 1-2X daily |
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Methylxanthines
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- rapid relief of contracted airways w/o modifying frequency or severity.
- "Short-term relievers" - MOA - Adenosine receptor antagonist which normally causes bronchoconstriction. - Also PDE inhibitor (PDE4 and other isozymes). - Anti-inflammatory action (reg. of gene transcription?) - AE's: low TI (requires monitoring), CNS stim, tremor and seizure, decreased sensitivity to CO2, GERD/heartburn/nausea, muscle activity, diuresis |
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Theophylline
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- Methylxanthine
- Oral |
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Aminophylline
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- Methylxanthine
- IV, (theophylline ethylenediamine) |
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Phosphodiesterase type 4 inhibitors
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- MOA - Selective inhibitors for PDE4 which reduces breakdown of cAMP and also involved in regulating inflammation
- Does not cause bronchodilation |
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Roflumilast
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- PDE Type 4 Inhibitor
- Oral 1x daily, active metabolite, little drug interaction - Treats COPD - Does not cause bronchdilation - MOA - 1st selective inhibitor of PDE type 4 - inhibition increases cAMP in inflammatory cells --> inhibits cellular infiltration and release of inflammatory cytokines - AE's: weight loss, nausea, diarrhea, headache |
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Corticosteroids
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- anti-inflammatory modify edema and cellular infiltration; reducing severity and frequency.
- "Long-term controllers" - Effect - Improve indices of asthma control - MOA - Inhibit synthesis of PLA, IL-1, & other proinflammatory cytokines - Decrease number of exacerbations - AE's: Candidal infections, esophagitis, vocal cord changes; glaucoma, cataracts; adrenal suppression - Oral used for acute exacerbations, then replaced by inhaled. - Oral may be needed for severe asthma |
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Fluticasone
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- Corticosteroid
- MDI, DPI |
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Budesonide
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- Corticosteroid
- MDI, DPI |
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Triamcinolone
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- Corticosteroid
- MDI |
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Ciclesonide
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- Corticosteroid
- MDI, prodrug, decreased systemic effects? |
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Leukotriene modulatory agents
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- anti-inflammatory modify edema and cellular infiltration; reducing severity and frequency.
- "Long-term controllers" |
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Zieluton
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- Leukotriene Modulatory Agent
- MOA - Inhibits 5-lipoxygenase - SR oral, 2X daily - AE's: Hepatotoxicity, psychiatric, drug-interactions |
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Montelukast
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- Leukotriene Modulatory Agent
- MOA - LTD4 receptor antagonist - Inhibits leukotriene C4 conversion to D4 - Oral 1X daily, > 6 months old - Other uses - exercise induced asthma, allergic rhinitis - AE's: drowsiness, psychiatric, systemic eosinophilia - Caution: Pregnancy (Cat B), Aspirin sensitive pts |
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Zafirlukast
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- Leukotriene Modulatory Agent
- MOA - LTD4 receptor antagonist - Inhibits leukotriene C4 conversion to D4 - oral 2X daily, > 5 yrs old - AE's: drowsiness, psychiatric, systemic eosinophilia - Caution: Pregnancy (Cat B), Aspirin sensitive pts |
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Histamine Release Inhibitors
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- anti-inflammatory modify edema and cellular infiltration; reducing severity and frequency.
- "Long-term controllers" - MOA - inhibit early response to allergen challenge (mast cell degran), by altering funx of delayed Cl- channel - may also inhibit or alter funx of other inflam cells and airway nerves - Pretreament by inhalation (2-4 puffs, 2-4 X daily) - little systemic exposure - AE's: throat irritation, cough, dry mouth - SAE's: dermatitis, myositis, gastroenteritis - No longer used for Asthma |
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Cromolyn sodium
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- Mast Cell Stabilizer (Histamine Release Inhibitor)
- Nasal spray (OTC) for allergic rhinitides |
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Nedocromil
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- Mast Cell Stabilizer (Histamine Release Inhibitor)
- Ophthalmitic allergy (which can also resolve rhitides because of drainage into nasal cavity --> 2 for 1) |
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Monoclonal Antibody to IgE
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- anti-inflammatory modify edema and cellular infiltration; reducing severity and frequency.
- "Long-term controllers" - MOA - inhibits binding of IgE to mast cells, does not provoke degranulation |
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Omalizumab
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- Monoclonal Ab to IgE
- Subcutaneous injection 2-4 weeks - reduces plasma IgE levels - reduces both early and late phase bronchospasm by allergen - humanized mouse monoclonal Ab - dose adjusted to IgE levels - Pts w/ poor pulmonary funx, and uncontrolled asthma even at high levels of corticosteroids - VERY EXPENSIVE - AE's: Anaphylaxis, malignancy, fever, arthralgia, rash, helminth infection (lack of IgE), eosinophilia, vasculitis |
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Anti-Histamine Agents
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Tx:
- Acute allergies (seasonal and/or allergic rhinitis and conjunctivitis) - Allergic dermatoses (esp w/ acute uticaria) - Serum sickness and allergic drug reactions - Motion sickness and vertigo - Sedation AE's: - Sedation, fatigue, dizziness, tinnitus; blurred vision; dry mouth, GI distress; Weight gain; Excitation - Convulsions (overdose in children) - Drug allergy (topical application) |
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1st Generation H1 Receptor Antagoist
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- MOA: Competitive antagonists
- Prominent CNS sedative effects (Cross BBB) - Antimuscarinic effects (activity at other receptors) - Good prophylaxis for motion sickness (vertigo) - Some mast cell stabilization effect - AE's: Potential to affect hepatic metabolic enzymes (drug-drug interactions) |
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Chlorpheniramine
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- 1st Gen H1 antag
- Slight sedation - Anticholinergic activity + - common component of OTC "cold" meds |
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Diphenhydramine
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- 1st Gen H1 antag
- Benadryl - Anticholinergic activity +++ - Marked sedation - anti-motion sickness activity |
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Dimenhydrinate
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- 1st Gen H1 antag
- Dramamine - Anticholinergic activity +++ - Marked sedation - anti-motion sickness activity |
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Promethazine
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- 1st Gen H1 antag
- Marked sedation - Anticholinergic activity +++ - Antiemetic - alpha block |
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Cyproheptadine
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- 1st Gen H1 antag
- Moderate sedation - Anticholinergic activity + - Antiserotonin activity |
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Hydroxyzine
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- 1st Gen H1 antag
- Marked sedation - No anticholinergic activity - Injectable used as tranquilizer |
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Meclizine
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- 1st Gen H1 antag
- Slight sedation - Anticholinergic activity - - Anti-motion sickness activity |
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Doxepin
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- 1st Gen H1 antag
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2nd Generation H1 Receptor Antagoist
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- Less sedating than 1st gen (less BBB penetration), but can occur at high doses
- More selective - Prodrugs metabolized by CYP3A4 caused drug-drug interactions, Active metabolites did NOT cause long QT |
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Loratadine
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- 2nd Gen H1 antag
- Did not cause long QT - Longer t1/2 |
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Cetirizine
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- 2nd Gen H1 antag
- Active metabolite of hydroxyzine - sedative effects |
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3rd Generation H1 Receptor Antagoist
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- Less sedating than 1st and 2nd gen
- More selective - Generally active metabolites of 2nd gen |
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Desloratadine
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- 3rd Gen H1 antag
- Metabolite of loratadine |
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Fexofenadine
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- 3rd Gen H1 antag
- Acid metabolite of terfenadine (safer) |
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Levocetirizine
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- 3rd Gen H1 antag
- Active enantiomer of cetirizine |
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Decongestants
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- Older antihistamines
- several different mechanisms (alpha agonist, anticholinergics, mast-cell stabilizer, intranasal corticosteroids) - Tx: Rhinorrhea and nasal congestion - Cough from post-nasal drip - Viscous bronchial secretions |
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Phenylephrine
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- Decongestant
- alpha-agonist - oral, intranasal |
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Pseudoephedrine
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- Decongestant
- Alpha-agonist (sudafed) - Oral |
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Oxymetazoline
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- Decongestant
- Alpha-agonist - intranasal - HTN, hypotension, Rhinitis medicamentosa |
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Ipratropium
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- Decongestant
- Anticholinergic (atrovent) |
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Expectorant
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- Reduces viscosity
AE's (Rare): - nephrolithiasis, nausea |
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Guaifenesin
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- Expectorant
- Reduces viscosity AE's (Rare): - nephrolithiasis, nausea |
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Cough Suppressants
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- Inhibit brainstem cough reflex
- delta-opiod receptor - Efficacy is "?" AE's: - sedation, dizziness, hypersensitivity rxn, constipation - may impair driving (DUI) |
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Codeine
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- Cough Suppressant
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Dextromethorphan
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- Cough Suppressant
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Hydrocodone
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- Cough Suppressant
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