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77 Cards in this Set
- Front
- Back
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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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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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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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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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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 - Intranasal |
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Budesonide
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- Corticosteroid
- MDI, DPI - Intranasal |
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Triamcinolone
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- Corticosteroid
- MDI |
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Prednisone
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- Corticosteroid
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Ciclesonide
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- Corticosteroid
- MDI, prodrug, decreased systemic effects? - Intranasal |
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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 - Decongestant |
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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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Isoniazid (INH)
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- 1st line TB
- Inhibits synthesis of mycolic acids (mycobacterial cell wall component) - Well absorbed from GI tract - Metabolism: Genetically controlled (Fast vs Slow acetylators) - Side Effects: Causes relative pyridoxine deficiency - Rash, Hepatotoxicity (minor elevation in ALT/AST; risk increases w/ age--> hepatitis), peripheral neuropathy (occurs in slow acetylators, responds to Vit B6 (pyridoxine)) |
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Rifampin
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- 1st line TB
- Binds to beta subunit of bacterial DNA dependent RNA polymerase (inhibits bacterial RNA synthesis) - Gram + and Gram - cocci, some Gram - rods, mycobacteria, legionella, chlamydia - NEVER USE ALONE in active case --> resistance (point mutation only): use with INH (6-9 months) - Penetrates well into cells - Bactericidal for M. TB - Alternative for latent TB (4 months, alone) - W/ other antibiotics for staphlococcal prosthetic valve endocarditis (and some others) - AE's: induces CYPs --> may increase metabolism of other drugs |
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Pyrazinamide
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- 1st line TB
- Penetrates cells well, but MOA not known - Used w/ INH and Rifampin for 1st 2 mo. --> reduced course from 12-18 to 6 months - AE's: Hepatotoxicity, hyperuricemia |
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Ethambutol
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- 1st line TB
- Inhibits mycobacterial arabinosyl transferases & blocks cell wall formation - Used to treat TB until susceptibility testing completed/or strain resistant to INH or rifampin - Used due to fears of resistance - Well absorbed from GI tract - Adjust for renal failure - AE's: Retrobulbar neuritis (loss of visual acuity and color blindness) NEED TO FOLLOW VISION |
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Amphotericin B
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- Polyene antifungal w/ broadest spectrum
- IV - MOA: Binds to ergosterol forming pores in fungal cell membrane - AE's: substantial toxicity including acute reactions (fever, chills) and chronic reactions (nephrotoxicity, electrolyte disturbances) - Lipid-based preparations have less toxicity but are expensive - note - nephrotoxicity of normal prep drives up cost - Used w/ 5-Flucytosine against cryptococcus |
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Nystatin
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- Similar to amphotericin B but only available topically
- cream, powder, ointment, vaginal tablet, swish & swallow |
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5-Flucytosine
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- DNA/RNA synthesis inhibitor
- Used w/ AmB against cryptococcus |
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Azoles
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- Inhibit lanosterol 14 alpha-demethylase (P450 enzyme) which converts lanosterol to ergosterol
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Fluconazole
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- Azole
- Excellent safety and pharmacology - high bioavail, water soluble, good tissue distribution, long 1/2 life - Generic - Not active against molds (Aspergillus) - 24+; renal; Oral, IV - Candida, Cryptococcus, Coccidiodes - Penetrates to CSF (meningitis) |
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Itraconazole
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- Azole
- Broader spectrum (relative to Fluconazole) - Absorption problems and drug-drug interactions (P450) can result in inadequate drug levels or toxicity - 24+; Hepatic; IV, Oral - Candida, aspergillus, HISTOPLASMOSIS, BLASTOMYCOSIS, SPOROTRICHOSIS, ONYCHOMYCOSIS |
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Voriconazole
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- Azole
- Broader spectrum (relative to Fluconazole) - Absorption problems and drug-drug interactions (P450) can result in inadequate drug levels or toxicity - Invasive aspergillosis - Reversible visual disturbances common after 1st dose - 6; Hepatic; Oral, IV |
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Posaconazole
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- Azole
- Broader spectrum (relative to Fluconazole) - Absorption problems and drug-drug interactions (P450) can result in inadequate drug levels or toxicity - Broadest spectrum (P.O. only) - Fungal prophylaxis in high risk patients (neutropenia, stem cell transplant) - Only Azole w/ activity against Zygomycosis - 24+; Fecal; Oral |
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Terbinafine
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- Inhibits ergosterol synthesis (diff. from azoles)
- tx superficial mycoses - Oral (Rx); Topical (OTC) - oral used mostly for onychomycosis and tinea pedis (athlete's foot) - Rare hepatotoxicity |
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Echinocandins (micafungin, caspofungin, anidulafungin)
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- Inhibit glucan synthase of Candida and Aspergillus spp. Preventing formation of Beta 1,3 glucan
- No activity against Cryptococcus - IV only - Low toxicity (mostly hepatic), long 1/2 life, few drug-drug interactions - Cyclic lipopeptide structure - All considered therapeutically equivalent |
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Griseofulvin
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- Oral drug used to treat dermatohyte infections
- Inhibits fungal microtubules - Infrequently used |
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Azithromycin
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- macrolide group, inhibits protein synthesis by binding to 23S subunit of bacterial ribosome
- Urinary Excretion --> No dose adjustment needed in renal/hepatic failure - One time dosing for STD; weekly to prevent Mycobacterium avium complex infection in AIDS - SE's: - GI, rash, hepatotoxicity, reversible ototoxicity, long QTc syndrome - Legionella, Chlamydia (intracellular CAP pathogens), OR Mycoplasma (extracellular but lacks cell wall), Hemophilus, moraxella - More resistance in Group A Streptococcus and S. pneumoniae - Other uses: Atypical mycobacterial infections, traveller's diarrhea, pharyngitis, otitis media - Resistance: Efflux pump, Mutated 23S, modifying enzyme |
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Ceftriaxone
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- Beta lactams inhibit final steps in peptidoglycan synthesis leading to cell wall formation
- 3rd gen cephalosporins stable against most plasma-encoded beta-lactamases, but not extended spectrum or AmpC beta-lactamases - 50/50 urinary and biliary excretion - Rash (stevens johnson syndrome) - 10-20% PCN allergy also allergic - avoid rechallenge w/ beta-lactams w/ anaphylaxis - Streptococci, MSSA, enteric gram negative (E. coli, Klebsiella, hemophilus, moraxella, salmonella, shigella) - enterobacter, pseudomonas, acinetobacter, citrobacter, stenotrophomonas and serratia considered resistant - Resistance: beta lactamases, altered PBPs (MRSA), altered permeability/efflux |
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Oseltamivir
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- Neuraminidase Inhibtor --> viral maturation/release inhibitor - blocks neuraminidase trimming of sialic acid residues required for release from cell membrane and disaggregation of virus
- Active against Influenza A and B - Tamiflu - H275Y produces resistance to Oseltamivir (not Zanamivir) - Oral; converted to active carboxylate by hepatic enzymes; renal excretion - Shortens cold by ~24 hrs in healthy people |
