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45 Cards in this Set
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levofloxacin, moxifloxacin
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Fluoroquinolones
Inhibit DNA synthesis by inhibiting DNA gyrase → “CIDAL” Enhanced gram-positive activity, anaerobes [moxifloxacin] Clinical uses: pneumonia, UTIs, travelers diarrhea [cipro], osteomyelitis [great bone penetration], “mixed” infections [moxifloxacin] |
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Nitromidazoles
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Metronidazole [Flagyl] PO, IV
How it works: Bactericidal; Taken up by anaerobic bacteria, disrupts DNA structure → cell death Spectrum of activity: Gram-positive and gram-negative anaerobes ONLY Clinical uses: Drug of choice for C. difficile diarrhea; used for anaerobic infections, bacterial vaginosis, trichomoniasis, Crohn’s disease Side effects: GI, metallic taste, drug-induced seizures, peripheral neuropathy [rare], disfulfiram reaction with alcohol |
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Cell-wall synthesis inhibitors
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Beta-lactams [penicillins, cephalosporins, carbapenems, monobactams]
Glycopeptides [vancomycin] |
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Penicillin Facts
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Excreted by tubular secretion and can be blocked by probenecid
Dosage adjustment for renal insufficiency [exceptions?] Generally well-tolerated GI [diarrhea], rash Can give rise to allergic reactions - immediate, accelerated and late Most important adverse effect – hypersensitivity |
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Fluoroquinolones
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Side effects: GI, CNS [dizziness, seizures], Achilles tendon rupture
Severe cases of hyperglycemia with gatifloxacin [Tequin] – no longer manufactured Drug interactions: CYP450 inhibitor [cipro to greatest extent], antacids, iron Not to be used in children < 18 yo Have been used in patients with cystic fibrosis without sequelae |
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Protein synthesis inhibitors
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Tetracyclines, Aminoglycosides, Fluoroquinolones
Macrolides, Chloramphenicol, Clindamycin |
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Folate Antagonists (Trimethoprim-Sulfonamides
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Sulfonamides block incorporation of PABA
Trimethoprim blocks dihydrofolate reductase enzyme Spectrum of activity: Gram-positive, gram-negative bacteria; no activity against Group A streptococcus Agents: Sulfadiazine, sulfasalazine, sulfamethoxazole- trimethoprim [Bactrim] |
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Commonly used for UTIs
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Trimethoprim/Sulfamethoxazole
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Folate antagonists
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nflammatory bowel disease, UTIs, acute otitis media, Pneumocystis carinii pneumonia [AIDS], some MRSA infectionsI
Side effects: Rash, GI, thrombocytopenia Not to be used in patients with G-6-P-D deficiency Sulfadiazine, sulfasalazine, sulfamethoxazole- trimethoprim |
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First line agent in treatment of tuberculosis
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Rifamycins:Rifabutin & Rifampin
Extremely active against gram-positive cocci Moderate gram-negative activity (NOT Pseudomonas aeruginosa) |
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Cephalosporin Facts
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General rules of spectrum of activity:
As you move from 1st through 4th generation “Lose” gram-positive activity and “gain” gram-negative activity Cross BBB better No cephalosporin covers enterococcus – intrinsic resistance |
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Metronidazole
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Nitromidazoles
Dose adjusted for severe liver impairment Major side effects: Metallic taste, disulfiram reaction, drug-induced pancreatitis, drug-induced seizures DOC for C. difficile colitis |
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Excellent bone penetration
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Clindamycin, they bind 50S
Fluoroquinolones |
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Metronidazole
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Excellent activity against gram-negative anaerobes (B. fragilis) and gram-positive anaerobes (Clostridium sp.)
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Sulfadiazine, sulfasalazine, sulfamethoxazole- trimethoprim
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Folate Antagonists (Trimethoprim-Sulfonamides
Sulfonamides block incorporation of PABA Trimethoprim blocks dihydrofolate reductase enzyme Spectrum of activity: Gram-positive, gram-negative bacteria; no activity against Group A streptococcus |
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Commonly used for GI surgical prophylaxis and abdominal infections
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Second Generation: Group 2 (Cephamycins)
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Very useful in “mixed “ infections
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-Lactam/-Lactamase Inhibitor Combinations
Most common side effect: GI (diarrhea) |
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DOC for enterococcus
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Ampicillin
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Methicilin IV
Oxacillin Nafcillin Cloxacillin Dicloxacillin PO |
DOC for MSSA infection
Dose adjusted for severe hepatic impairment Cross BBB adequately |
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Widely used for uncomplicated cellulitis, surgical prophylaxis
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First generation Cefazolin
Cephalexin Cefadroxil |
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DOC for MSSA infection
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Penicillinase -Resistant penicillins
Methicilin IV Oxacillin Nafcillin Cloxacillin Dicloxacillin PO |
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High Na content
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Ticarcillin,Carboxypenicillins
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Poor CSF penetration
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Cefazolin
Cephalexin Cefadroxil First generation |
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• Bacteriostatic
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– Inhibit growth and reproduction of bacteria without killing them
– Examples: tetracyclines, sulfonamides |
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Oral absorption decreased by di- and trivalent cations (milk, antacids, sucralfate
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Doxycycline
Minocycline Tetracycline |
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Useful in “mixed” infections
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Imipenem/cilastatin
Meropenem Ertapenem |
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Doxycycline
Minocycline Tetracycline |
Acne,
respiratory tract infections, Lyme disease, STD, select |
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Good substitute for aminoglycosides in patients at risk for toxicity
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Aztreonam
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• Bactericidal
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– “Destroy bacteria”
– Cause bacterial cell death – Examples: beta-lactams, vancomycin, aminoglycosides |
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Doxycycline
Minocycline Tetracycline |
Major toxicity: GI, phototoxicity
Minocycline: associated with vertigo Doxycycline: hepatic |
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: Dose adjusted for liver dysfunction
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Ceftriaxone, cefoperazone:
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Most broad spectrum agents available
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Carbapenems
• Broadest spectrum β-lactam class |
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Imipenem/cilastatin
Meropenem |
Polymicrobial coverage all in one agent
Useful in “mixed” infections |
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Ampicillin/sulbactam
Amoxicillin/clavulanic acid Ticarcillin/clavulanic acid Piperacillin/tazobactam |
-Lactam/-Lactamase Inhibitor Combinations
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Carboxypenicillins
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Carbenicillin
Ticarcillin |
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-Lactam/-Lactamase Inhibitor Combinations
Imipenem/cilastatin Meropenem |
Useful in “mixed” infections
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Piperacillin
Azlocillin Mezlocillin IV |
Ureidopenicillins
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Very active against MSSA, strep
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Group 1
Cefaclor Cefuroxime |
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– Drug of choice for MRSA
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Vancomycin
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Less activity against MSSA,
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2 group Cephamycins)
Cefoxitin Cefotetan Cefmetazole |
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Gram-positive activity ONLY
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Vancomycin
Clindamycin Penicillinase -Resistant penicillins |
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Very good against atypical pathogens
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Doxycycline
Minocycline Tetracycline 2.Erythromycin Clarithromycin Azithromycin Dirithromycin 3Fluoroquinolones |
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Telithromycin
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Macrolides/ they bind 50S Ketolides
Limit use to resistant S. pneumoniae |
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Erythromycin
Clarithromycin Azithromycin Dirithromycin toxicity |
Major toxicity: GI upset (major)(erythromycin), drug interactions
Azithromycin, erythromycin: hepatic elimination Clarithromycin Metallic taste Visual disturbances, liver failure |
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Clindamycin
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Good alternative for cellulitis in PCN-allergy
Excellent bone penetration Major toxicity: GI, pseudomembraneous colitis Dose adjusted for hepatic dysfunction Used in higher doses for gram-positive toxic shock syndromes |