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Pulmonary Drugs

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Question
Answer
Spacers   Increased delivery of drug to lungs; use especially w/ corticosteroids due to risk of thrush  
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Metered Dose Inhalers   Small, hand held, pressurized devices, hand-lung coordination. 10% reaches lung, 80% hits oropharynx and is swallowed  
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Dry Powder Inhalers   Breath activated, no hand lung coordination, 20% gets to lung  
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Nebulizers   Converts liquid to mist. Face mask or mouthpiece used; med delivers over several minutes; same amount of med as in one puff  
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Glucocorticoids   Vancenase, Pulmicort, Flovent/Flonase, Nasonex, Nasocort  
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Nasonex & Nasocort   Intranasal. S/E: drying of nasal mucosa, burning/itching, sore throat, epistaxis, not as effective if nasal congestion present  
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Corticosteroids   Inhaled = 1st line of therapy for asthma. Oral use for severe asthma; when symptoms not controlled with inhalation and bronchodilators  
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Vancenase, Pulmicort, Flovent/Flonase, Nasonex, Nasocort   S/E w/ chronic use: adrenal suppression & bone loss, oropharyngeal candidiasis and dysphonia. Prevent by gargling after admission, use spacer. Prevent bone loss by using lowest dose possible, adequate Ca+, Vit D, & wt bearing exercises  
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Leukotriene Modifiers   Compounds that promote bronchoconstriction, inflammation, mucus production and edema. -- Effects are not immediate  
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Name the Leukotriene Modifiers   Zyflo & Singulair  
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Zyflo   Blocks leukotriene synthesis, used for adults and children >12 yrs; hepatotoxic, monitor ALT, competes with theophylline & coumadin (increases drug levels)  
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Singulair   Leukotriene receptor blocker. Use prophylactically and maintenance; Prevention of exercise induced bronchospasm; relief of allergic rhinitis; not immediate, not hepatotoxic, does not increase drug levels  
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Methylxanthines   Theophylline  
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Theophylline   Causes bronchodilation; narrow therapeutic range; only given PO. Used w/ chronic, stable asthma to decrease frequency and severity of attacks. Wide variations in metabolic rates  
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Theophylline (2)   Dosage based on individual and therapeutic range 5-15. Levels 20-25 = nauseau, vomiting, restleness. Levels >30 dysrhythmias (Vfib), seizures, avoid w/ caffeine  
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Cromolyn (Nasalcrom, Intal)   Used for seasonal allergy attacks and exercise induced bronchospasm - give 15 minutes before.  
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Nasalcrom   Given intranasal for allergic rhinitis  
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Intal   Given inhalation  
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Nasalcrom & Intal   Decrease bronchial inflammation, not a bronchodilator. Used prophylactically, not quick relief, no systemic effects, may be used instead of steroids  
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Beta 2 Adrenergic Agonist (Bronchodilators)   Albuterol, Levalbuterol, Serevent, Advair  
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Beta II Adrenergic Agonist   Provides symptomatic relief but does not address underlying cause; most need w/ long term steroid. Most effective for relieving acute bronchospasm  
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Activate Beta 2 receptors   In smooth muscle of lungs causing bronchodilation suppressing histamine release in lung and increase ciliary motility. Available PO or inhalation. PO = long acting  
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Short Acting Beta 2 Adrenergic Agonist   Albuterol, Levalbuterol  
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Albuterol & Levalbuterol   Given by inhalation. Begin Immediately; peak 30-60 min, persist for 3-5 hrs. Used to abort an attack but not effective for long term prophylaxis  
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Short Acting (albuterol & levalbuterol)   Exercise induced bronchospasm - take 15 minutes before. Available MDI, DP, nebs, inhalers  
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Long Acting Beta 2 Adrenergic Agonist   Serevent  
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Serevent   Takes effect in 10-30 minutes.  
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Oral Antihistamine drugs   Chlor-Trimeton, Benadryl, Tavist, Zyrtec, Allegra, Claritin, Clarinex  
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First Generation Oral Antihistamines   Chlor-Trimeton, Benadryl, Tavist  
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Second Generation Oral Antihistamines   Zyrtec, Allegra, Claritin, Clarinex  
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Oral Antihistamines   Relieve rhinorrhea, sneezing, nasal itching but not congestion, most effective when taken prophylactically on a regular basis  
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1st Generation Oral Antihistamines   S/E: sedation, dry mouth, urinary hesitancy, constipation due to anticholinergic effects  
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2nd Generation Oral Antihistamines   NO SEDATION, few side effects  
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Sympathomimetics   Neosynephrine, Sudafed, Dristan, Atrovent, Spiriva  
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Sympathomimetics (Decongestants)   Activating alpha adrenergic receptors, decrease nasal congestion by vasoconstriction, shrinks, swollen membranes  
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Sudafed   Can be converted to methamphetamine, must be kept behind counter, sign a log, no more than 9 g/month or 3.6 g at one time  
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Neosynephrine, Sudafed, Dristan   Allergic rhinitis to relieve stuffiness, lower congestion of sinusitis and coid. S/E: rebound congestion, increase dose for symptom relief, limit 3-5 days of use, may need steroid, CNS excitation, restless, anxiety, systemic vasoconstrict, watch heart pts  
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Atrovent   Onset 30 sec, max 3 min, last up to 6 hrs. S/E: dry mouth, irritation pharynx, avoid if peanut allergy, contains soya lectithin. 10% anaphylaxis. Combo w/ aluterol is called duoneb  
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Atrovent & Spiriva (anticholinergic)   Block muscarinic receptors in bronchi causing dilation, used on COPD, off label use for asthma. Inhalation only  
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Spiriva   Long acting, onset 30 min, peak 3 hrs, last 24 hrs, given 1x daily. S/E: dry mouth, DPI, additive benefits w/ Beta 2; two different ways to dilate  
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Drugs for Coughing   Codeine, Dextromethophan, Mucinex, Mucomyst  
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Antitussives   Codeine & Dextromethophan  
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Expectorants & Mucolytics   Mucines & Mucomyst  
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Codeine   Decreases frequency and intensity of cough; low dose; 1/10 of dose used for pain; potential for abuse  
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Dextromethophan   Non-opioid antitussive; taken at high doses can cause euphoria and can be abused for this purpose  
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Expectorant   Stimulates flow of respiratory secretions  
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Mucolytics   Breaks up mucus  
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Mucomyst   Given by inhalation; watch for bronchospasm, contains sulfur  
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Selective Toxicity   Ability of drug to injure a target cell or organism without injuring other cells; without causing injury to host  
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Inhibition of Enzyme   Unique to bacteria; ex) folic acid - bacteria make folic acid which is needed for bacterial survival  
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Disruption of protein synthesis   Ribosomes in bacteria are different than ribosomes of mammalian cells  
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Bactericidal   Directly lethal to bacteria  
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Bacteriostatic   Slows bacterial growth but does not cause cell death. Elimination of bacteria must be accomplished by host immune defenses  
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Penicillins & Cephalosporins   Inhibit bacterial cell wall synthesis or activate enzymes to disrupt cell wall  
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Increase cell membrane permeability   Amphotericin B - causes leakage of intracellular material  
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Aminoglycosides   Lethal inhibition of protein synthesis  
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Non-lethal inhibition of protein synthesis   Tetracyclines - only slow bacterial growth  
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Inhibit bacterial synthesis of DNA/RNA   Binds directly to nucleic acids or enzymes that make nucleic acids: rifampin, metronidazole, fluorquinolones  
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Antimetabolites   Disrupt specific biochemical reactions: Trimethoprim & Sulfonamides  
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Suppress viral replication   inhibit specific enzymes  
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Microbial Mechanism   Decrease drug concentration at its site of action (intracellular), ease active uptake, increase active export. Produce drug metabolizing agent.  
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Microbial Mechanism 2   Change structure or receptor site or target molecules (ribosomes). Produces compound that antagonizes drug action  
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Acquired Resistance   Spontaneous (random) mutation. Conjugation: combining of 2 bacterial DNA; common in gram (-) bacteria; could use normal flora  
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Antibiotic Use   Normal flora competes w/ each other. When used, normal flora changes, bacterial flourish. Broad spectrum antibiotics increase chance of resistance  
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Antibiotic Use (2)   Nosocomial infections are among the most difficult to treat; more exposure to antibiotics  
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Vaccinate   Prevents infections  
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Disconnect invasive lines, catheters   Leading cause of nosocomial infections  
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Target the pathogen   Use only antibiotics the bacteria is sensitive to  
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Expert   Consult infectious disease specialist; right antibiotic for right amount of time  
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Antimicrobial control   Standing orders for bacteria/infections; evaluate effectiveness  
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Treat bacteria not colonization   Just because bacteria is present doesn't mean it is an infection  
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Gram (+)   PCN can easily penetrate thick cell wall and reach the PCN binding proteins on cytoplasmic membrane  
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Gram (-)   Most PCN's cannot penetrate outer membrane  
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Beta Lactamases   Enzymes that break down Beta lactam ring; can be produced by both gram (+-) bacteria.  
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What is #1 adverse effect of PCN's   Allergic reaction  
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PCN Binding Proteins   Receptor site for drug; only available during growth and division of bacteria cell; PCN's have no direct effect on cells of host b/c they don't have cell wall making them very safe. PCN breaks cell wall; cell takes up H2O and ruptures. PCN is bactericidal  
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Penicillins   Penicillin G, Pipracil, Piperacillin/tazobactam, Augmentin  
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Penicillin G   first PCN available; active against most gram (+) bacteria. Most gram (-) are resistant; given IM or IV, intra arterial injection can produce severe reactions. MUST AVOID  
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Pipracil   Broad spectrum, given IV, decrease dosing for impaired renal function  
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Piperacillin/tazobactam (Zosyn)   Contains tazobactam, a beta lactamase inhibitor (prevents the bacterias beta lactase enzyme from breaking down the antibiotic which is the piperacillin)  
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Amoxicillin/clavulante(Augmentin)   May be given orally. S/E: rash & DIARRHEA. Clavulante, a beta lactamase inhibitor protecting the antibiotic (amoxicillin) from the bacterias beta lactamase enzymes  
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Cephalosporin   Binds to PCN binding proteins; has a beta lactam ring, bactericidial; most effective against bacteria undergoing cell division and growth  
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Cephalosporins Resistance   Based on bacteria's ability to break down beta lactam ring  
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1st Generation Cephalosporin   Destroyed by beta lactamase enzymes; used for gram (+)  
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2nd Generation Cephalosporin   Less sensitive to beta lactamase enzymes; first and second generation do not reach CSF  
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3rd & 4th Generation Cephalosporin   Highly resistant to beta lactamases. Given IV. Reserved for active infections; strong antibiotics "big guns"  
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Cephalosporins Pharmacokinetics   PO absortion from GI tract; usually given IM/IV; most eliminated by kidneys, may need to decrease dose if renal impairment  
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Cephalosporins Adverse Effects   Hypersensitivity reactions: rash for several days after onset of use; risk of bleeding (interferes with vitamin K metabolism); thrombophlebitis  
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Cephalosporins Drug Interactions   Meds that promote bleeding; interacts with Probenecid (delays excretion)  
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Cephalosporin Drugs   Cefazolin, Cefzil, Ceftin, Rocephin, Maxipime  
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First Generation Cephalosporin (Drug & Routes)   Cefazolin: IM, IV  
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Second Generation Cephalosporins (Drugs & Route)   Cefzil, Ceftin, PO. Not typically used for active infections, used prophylactically w/ surgical pts  
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Third Generation Cephalosporin (Drug & Route)   Rocephin: IM, IV -- Do NOT mix w/ calcium containing IVF/IVPB  
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Fourth Generation Cephalosporin (Drug & Routes)   Maxipime: IM, IV  
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Carbapenems Drugs   Imipenem & Cilastatin  
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Cilastatin   Inhibits destruction of imipenem by renal enzymes  
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Carbapenems   Very broad spectrum antibiotic. IV only. Able to penetrate gram (-) outer membrane. S/E: N/V, diarrhea, hypersensitivity reactions  
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Vancomycin   Reserved for serious infections, does NOT contain beta lactam ring. Given IV except for infections of GI tract; excreted by kidneys. Uses: CDIFF, MRSA, allergy to PCN  
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Vancomycin S/E:   nephrotoxic, ototoxic (ringing in ears), loss of hearing, rapid infusion may cause "red man syndrome": flushing, tachycardia, hypotension, rash, pruritis. Monitor serum levels do peaks/troughs  
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Azactam   Binds to PCN binding proteins; not effective against anaerobes or gram (+) bacteria; only against gram (-). Highly resistant to beta lactamases  
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Azactam S/E: & Routes   Pain and thrombophlebitis at site of injection. Given IM/IV  
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Tetracycline Drugs   Tetracycline & Doxycycline = Suppress bacterial growth by inhibiting protein synthesis. Take w/ full glass of H2O, use straw if liquid formula (don't let touch teeth)  
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Tetracycline   Take on empty stomach, eliminated by kidneys, avoid w/ renal failure  
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Vibramycin   Can take w/ food, eliminated by liver, OK to use w/ liver failure  
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Tetracycline & Vibramycin S/E:   GI irritation, binds to salts, do not give w/ Ca+ supplements/dairy products/iron supplements/Mg containing antacids or laxatives (discolor teeth from yellow to brown). CDIFF is common  
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Macrolide Drugs   Biaxin & Zithromax  
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Macrolides   Broad spectrum antibiotics w/ BIG molecules, usually bacteriostatic; may be used as alternative to PCN; active against many gram (+) and some gram (-). Inhibits protein synthesis (binds to ribosomes)  
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Macrolide Uses   Pertussis, whooping cough, diptheria, chlamydia, some pneumonia. Feed decreased absorption; eliminated by liver  
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Macrolide S/E:   GI upset, QT prolongation leading to TorSades and sudden cardiac death; avoid w/ antidysrhtymics and calcium channel blockers. Increases levels of theophylline and coumadin  
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Biaxin   Used for respiratory tract infections & H pylori  
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Zithromax   Used for respiratory tract infections, chlamydia; absorption increases w/ food  
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Cleocin   Severe group A streptococcal infections. Active against anaerobic bacteria (Gram + -). Usually bacteriostatic. Inhibits protein synthesis  
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Cleocin S/E:   Pseudomembranous colitis (CDIFF), abdominal pain, fever, leukocytosis; stools (+) for mucus & blood  
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Zyvox   Oxazolidinone; activity against multidrug resistant gram (+) bacteria, VRE, MRSA. Inhibits protein synthesis  
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Zyvox S/E:   myelosuppression AKA decreases WBC, RBC, platelet  
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Aminoglycosides - Drug   Gentamycin  
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Gentamycin   Disrupts protein synthesis, bactericidal d/to production of abnormal proteins  
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Gentamycin S/E:   ototoxic, nephrotoxic, monitor peaks and troughs  
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Gentamycin -- Uses & Routes   Aerobic gram (-) bacilli; cannot kill anaerobes, need O2 to transport medication across membrane. Given IV only, may give PO for bowel infection only; decrease dose or increase interval for renal pts  
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Fluoroquinolones - Drugs   Cipro & Levaquin  
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Cipro & Levaquin uses   Respiratory, Urinary, GI, bone/joint, skin, soft tissue infects. Absorption decreased w/ Al, Mg, Ca, Fe & dairy  
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Cipro & Levaquin S/E:   Tendon rupture (achilles), GI upset, candida inf of pharynx & vagina; CNS: dizziness, confusion (elderly), phototoxicity  
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Metronidazole Drug   Flagyl  
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Flagyl   Used for CDIFF, H Pylori, abdominal & vaginal surgery.  
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Flagyl S/E:   nausea, dry mouth, unpleasant metallic taste; darkening of urine; avoid alcohol, may need to decrease coumadin dose  
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Anti-fungal Drugs   Amphotericin B, Azoles (Sporonox, Diflucan, Vfend), Cancidas  
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Amphotericin B   Active against broad spectrum fungi, given IV. Used as last ditch effort, not common. BIG DANGEROUS DRUG!!!  
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Amphotericin B S/E:   Premedicate w/ Benadryl & Tylenol, corticosteriods. Phlebitis: change peripheral IV sites, give thru central line. Nephrotoxic: renal impairment occurs in almost all patients, avoid other nephrotoxic drugs. Bone marrow suppression  
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Azoles - Drugs   Sporonox, Diflucan, Vfend  
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Sporonox   Take w/ food NOT w/ antacids  
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Azoles action   Broad spectrum antifungal; lower toxicity than Ampho B, given PO. Increases membrane permeability  
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Sporonox, Diflucan, Vfend uses:   Blastomycosis, histoplasmosis, candidiasis  
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Azoles S/E:   Cardiosuppression & liver injury - use cautiously in cardiac & liver patients  
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Cancidas   Given IV, disrupts cell wall; Better tolerated than Ampho B, S/E: phlebitis. Used for aspergillus or candida only  
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TB Drugs   INH, Rifadin, PZA, Myambutol  
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INH   bactericidal to actively dividing organisms. Must take 6 mos, preferred 9.  
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INH S/E:   liver damage; excreted by kidneys, increase risk of liver damage w/ advancing age; peripheral neuropathy d/t lowered levels of vit B6  
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Rifadin   Bactericidal to TB. Take on empty stomach. Eliminated by hepatic metabolism; hepatotoxic  
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Rifampin S/E:   Red-orange discoloration of urine, tears, sweat & saliva  
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PZA   Bactericidal to TB, hepatotoxic, increases uric acid (inhibits excretion)  
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Myambutol   Bacteriostatic, may be used to treat TB resistant to INH or Rifadin  
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Myambutol S/E:   Optic neuritis (blurred vision, constriction of visual field, changes to color discrimination); inhibits uric acid excretion  
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Zovirax   Only active against herpes virus family (chicken pox, herpes, shingles) S/E: IV - phlebitis, nephrotoxic PO - N/V/D/HA not nephrotoxic  
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Chemo Agent Drugs   Carboplatin & Taxol  
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Carboplatin   Used for small cell lung cancer. S/E: bone marrow suppression, N/V, nephrotoxic. Watch for hearing loss  
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Taxol   Used for non-small cell lung cancer. S/E: severe hypersensitivity infusion reactions (hypotension, dyspnea, angioedema, urticaria-hives) premedicate w/ Benadryl, corticosteroids; bone marrow suppression; alopecia; bradycardia  
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