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65 Cards in this Set
- Front
- Back
abx known
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1. spectrum of activity: abx coverage of bacteris
2. MOA 3. Adverse effects and toxicities 4. Tissue penetration |
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abx
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-kill bacteria without harming the host (selective toxicity)
-empiric therapy (best guess) broad spectrum to cover most likely infecting agents (choose based on site, gram stain) -narrow focused therapy is begun ASAP after getting results of C&S from infected site (minimize resistance to broad spectrum agents) |
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bactericidal vs. bacteriostatic
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1. kills bacteria
2. abx inhibit growth of actively replicating; ok with a mild infx in an immunocompetent host- not good for immunocompromised |
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gram positive cocci
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1. Streptococci
-pneumococci 2. Staphylococci -normally inhibit skin and cause: abscesses 3. Empiric tx is: -Nafcillin, dicloxacillin -cephalexin, cefazolin 4. Enteroccoci- (usually in colon or perianal) innately resistant to many abx |
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penicilins and cephalosporins
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-inhibit formation of peptide bridges in petidoglycan of gram + and gram - bacteria
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gram negatives
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-encased by an outer membrane with LPS and protein channels
1. Enterics: E.coli, shigella, salmonella, serratia (inhospitalized pts cause pneumonia), proteus, enterbacter, klesiella 2, Haemophilus influenzae 3. **Pseudomonas- resistance so requires specific therapy-veryy difficult to treat |
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neisseria
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-gram neg dipploccus
-gonorrhea and meningitis |
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anaerobes
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-no O2, foul-smelling deep tissue infections
1. Bacteriodes fragilis- most common (internal abcesses) 2. Clostridia spp. (gangrene) 3. Prevotella (gingival pockets) 4. Peptostretococcus 5. need special abx: Clindamycin, Metronidazole |
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common syndromes of anaerobic infxs
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1. bite infxs
2. oral or dental infx 3. aspiration penumonia, lung abscess 4. appendicitis |
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probiotics
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-live, friendly organisms in intestine which may balance pathogenic organisms that cause diarrhea and yeast infections
(Bifidobacteria, lactobacillus, saccaromyces)-avail as cultures in yogurts, capsules, tables, packets -may help IBS, IBD, certain diarrhea and recurrent yeast infxs -abx can hurt these |
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Beta- lactam Abxs
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-Transpeptidase and penicillin binding proteins (PBPs) crosslink units of petidoglycan cell wall
-PCNs and cephalosporins are beta-lactam abx that bind and inactivate transpeptidases and PBPs and trigger autolysis--> destroy cell wall -PCN nucleus and side chains = R |
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Natural penicillins (PCN G (iv) and VK (po)
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-susceptible to beta lactamases produced by resistant bacteria
-Coverage- gram POSITIVE (best), gram negative, few anaerobes, treponema, streptococci, pneumococci, meningococci, listeria monocytogenes -PCN VK oral form for strep throat (TID) |
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Benzathine PCN
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IM formulation version of natural PCN
-depot --> deposited slowly in muscle -used for strep throat and syphillis |
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beta lactamases
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-variety of different enzymes that make bacteria--> destroy beta-lactam ring
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PCNs- Anti-staphylococcal
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-resistant to hydrolysis by staphylococcal beta lactamases
-MOND: 1. Methicillin (nephrotoxic- not used anymore) 2. Oxacillin 3. Nafcillin (IV, IM) 4. Dicloxacillin (po)- for mild skin infx, mastidis -Used for beta lactamase + staph infections! -Problem: Methicillin resistant staph aureus (MRSA) |
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Extended-spectrum PCNs
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-greater gram - coverage
1. Ampicillin po/IV 2. Amoxicillin po 3. Ticarcillin- pseudomonas 4. Piperacillin – pseudomonas -extended spectrum into gram - realm (also cover gram positives) |
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Extended-spectrum PCNs uses
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1. susceptible sinusitis
2. respiratory infx 3. otitis media 4. pseudomonas infxs |
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beta-lactamase inhibitors
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-chemicals given with beta lactam abx to inhibit beta lactamases
1. Clavulanic acid + amoxicillin = augmenten (PO)- sinusitis, recurrent otitis media; diarrhea common AE 2. Sulbactam + ampicilin = Unasyn (IV, IM): for bite 3. Tazobactam + piperacilin --> Zosyn (IV)- pseudomondas infxs -Ticaricillin + clavulinic acid- severe pesudomonas infxs |
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pharmacology of the PCNs
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-poor CNS penetration except when meninges are inflammed (combined with something else)
-Category B |
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PCNs AE
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1. hypersensitivity rxns: rash
2. Interstitial nephritis 3. GI intolerance & diarrhea 4. rash with EBV mononucleosis (amox and amp) |
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Beta lactams- Cephalosporins and Cephamycins (10-15% x-reactivity with PCNs)
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-more stable than PCNs to B-lactamases produced by several bacteria
-1st gen: better G+ activity -2nd gen: inc activity against G - -3rd gen: G- rod, some pseudomona; less G+ -4th gen: inc stability to B lactamases and more extended spectrum than 3rd gen |
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1st generation cephalosporins
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1. Po Cephalexin (Keflex)
2. IV Cefazolin (ancef) (used for most surgical prophylaxis unless it is GI/ pelvic procedure then use Cefotetan-esp orthopedics) -Used for staph skin infections, soft tissue infections such as furuncle and to prevent infection -MRSA is resistant to these |
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Second generation cephalosporins and cephamycins
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1. IV: cefotetan, cefuroxime, cefoxitin (PID)
2. Po: cefaclor, cefuroxime axetil (Ceftin)**, cefmetazole, cefprozil -Cefoxitin, cefotetan are active against anaerobes (cephamycins) uses: Po OM, sinusitis, lower resp. tract infxs, communit. aquired pneumonia IV: gyn, surgical prophylaxis |
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3rd Generation Cephalosporins
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1. PO: cefixime (gone now), ceftibuten, cefpodoxime, CEFdinir
2. IV: Ceftriaxone, cefotaxime --> meningitis cross BBB!! 3. Pseudomonas coverage: Ceftazidime*, cefoperazone 4. Moxalactam and ceftizoxime cover B. fragilis |
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Fourth Generation Cephalosporins
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1. Cefepime IV only
-More resistant to hydrolysis by enterobacter’s beta lactamases but otherwise similar role to 3rd generation - |
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Cephalosporins- Basic Pharmacology
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-renal excretion
-variable CNA penetration -pregnancy category B |
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cephalosporins AE
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1. Hypersensitivity reactions
2. Renal nephritis 3. Platelet dysfunction 4. Superinfection esp. with broad spectrum agents (infx caused by abx) |
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Monobactam --> aztreonam
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-type of beta lactam
-only for gram neg rods -IV only -gram - sepsis AE: skin rash and increased LFTs |
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Carbapenems*
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-all IV
-Imipenem (+Cilistatin) -also meropenem and ertapenam (Invanz) -Doripenam (best against peudomonas of this group) -BROAD SPECTRUM BIG GUN -used for complicated infxs -covers gram +, - and anerobes AE: N/V and rarely seizures |
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Vancomycin
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-BIG GUN-use prudently; IV and PO (C.diff)
-MOA:cell wall inhibitor -use: fro gram + positive -MRSA, sepsis and endocarditis -enterococcus infxs (issues: VRE and VISA resistance to vanco) -resistant pneumococcal meningitis |
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vancomycin AE
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1. Local reactions
2. Fever, chills 3. Oto and nephrotoxicity 4. RED MAN syndrome (red neck and head after infusion)* |
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Fosfomycin
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-cell wall inhibitor
-used for uncomplicated UTI -3 g oral sachet -category B AE: Gi intolerance (diarrhea, nausease and dyspepsia) |
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Inhibitors of protein synthesis
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1. Tetracyclines
2. Chloramphenicol (rarely used) 3. Macrolides (z-pack) 4. Clindamycin 5. Streptogramins -Quinupristin-dalfopristin 6. linezolid |
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Chloramphenicol
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MOA: binds to 50S of bacterial ribosome & inhibits protein synthesis
-broad spectrum Clinical: Rarely used except in kids < 8 with severe rickettsial infections (RMSF) and pneumococcal PCN resistant meningitis with major hypersensitivity to PCNs AE: Toxic- GRAY BABY SYNDROME; Bone Marrow suppression & aplastic anemia |
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Tetracyclines
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MOA: bind to 30s unit
-Broad spectrum and includes G+(more) and G-, anaerobes, rickettsia, Borrelia, [Legionella, chlamydia, mycoplasma] --> (walking PNA) |
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types of tetracyclines
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1. Demeclocycline (not used)
2. Tetracycline 3. Doxycycline (IV and PO) (impt) 4. Minocycline (impt) |
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AE of tetracyclines
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1. GI symptoms
2. Photosenitivity (stay out of sun!) 3. Preg category D 4. Hepatotoxicity (more common in preg) 5. Nephrotoxicity (less w/doxy) (more when expired) 6. NOT to be used in kids <8 7. discoloration of teeth and abnl bone growth in young kids 8. Vestibular rxns: dizzy, vertigo (mino) |
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Tetracyclines pharmacokinetics
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-best PO absorption w/doxy and mino
-do not take w/antacids, dairy or metal Clinical: 1. Chlamydia infxs, 2. Mycoplasm, 3. Acne vulgaria, 4. Lyme disease (doxy), 5. RMSF |
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Tygacil (tigecyclines)
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-IV
-similar to tetras but designed to overcome resistance problems -approved for complicated intra-abd and skin infxs that need broad empirical coverage -covers many gram + and gram - bacteria and anaerobes. good for MRSA |
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Macrolides
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-erythromycin is prototype
-MOA: binds to 50s and prevents movement of tRNA alon ribosome -erythromycin, azithromcyin, clarithromycin -spectrum: primary gram +, also mycoplasma, legionella, chlamydia, H. pylori and Listeria (atypical PNAs); bordatella |
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Macrolides pharm
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-Azithromycin has high concentrations and penetration with prolonged half life of 40-68 hours (z pack- 5 day course of abx)
-Clarithromycin and erythromycin potential for drug interactions |
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Macrolides- clinical
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-Azithromycin used to treat chlamydia, mild and uncomplicated CAP, acute OM, pharyngitis in PCN allergic
-Clarithromycin --> CAP, MAC (mycobacterium avium complex-assoc with AIDS) -Emcyin various forms |
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Macrolides: AE and DI
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1. Epigastric distress
2. metallic taste 3. cholestatic hepatitis 4. E-mycin and clarithromycin can potentiate the effects of many drugs such as: Digoxin, Terfenabine, Warfarin |
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Ketek (telithromycin)
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-Ketolide class of abx (similar to macrolides)
-PO -MOA: binds to 2 diff sites on ribosome -Used for: Community-acquired PNA due to Streptococcus PNA and other usual suspects in CAP -AE: N/D, visual disturbances, drug interactions due to liver metabolism |
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Clindamycin
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-MOA: binds to 50s
-PO and IV (short half life) -Gram + anaerobics; staph, strep (esp is PCN allergic) and pneumococcus -Tx of anaerobic and mixed infections (severe) -Pelvic and abd. Abscesses, peritonitis, lung abscesses, aspiration pneumonia in combination with other agents such as aminoglycosides |
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Clindamycin Pharm and AE
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-excellent penetration into abscesses and intracellularly
AE: DIARRHEA - pseudomembranous colitis |
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Quinupristin-dalfopristin (Synecid)
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-IV
-binds to 50s -tx for VRE and complicated infxs caused by highly resistant staph and strep -$$ needs to be admin thru central line -AE: infusion related to pan and phlebitis, drug interactions and arthralgias |
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Linezolid (Zyvox)
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-last resort for VRE and severe infxs caused by resistant staph and strep
-MOA: prevents formation ribosome complex -slightly more cost-effective than synecid; avail IV and PO -AE: minor ARs, monitor plts |
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Aminoglycosides
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-IV only
-MOA: binds to 30s -Gentamycin, streptomycin tobramycin; amikacin -SOA: GRAM - AEROBES Tobromycin --> pseudomonas Amikacin has broadest spectrum BIG GUN and may be used for infections resistant to gentamycin and tobramycin |
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aminoglycosides pharm
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-IV, IM only
-fair penetration into brain -excellent penetration in renal cortex -synergy with beta lactams (do not mix in same tubing) -postabx effect-work when the abx is no longer in system -clinical: for severe gram - infxs (sepsis, PNA, UTIs) in combo with PCN |
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Aminoglycosides AE
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1. ototoxicity (tinnitus, hearing loss;vertigo)
2. Nephrotoxicity- more common with gentamycin > 5 days (pts must be well hydrated!) -serum drug concen monitored (high trough levels assoc with nephrotoxicity) |
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Sulfonamides and trimethoprim (TMP)
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-Sulfonamides are used with TriMethoPrim (TMP) to produce synergistic blocking of folic acid synthesis (diagram)
Forms: oral absorbable, oral nonabsorbable (acts locally in GI), IV (cross into CSF), topical |
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Sulfa and TMP drugs spectrum
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-some G+ and many G-, some protozoa like pneumocycstis (PNA in HIC pts) and toxoplasma
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Sulfa and TMP drugs spectrum clinical utility
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-topical agents for bacterial conjunctivitis and prevention of infx in burns
-PO and IV absorbable agents (sulfamethoxazole/Trimethoprim combination-Bactrum) 1. UTI and prostate infxs 2. PCP 3. Salmonella and shigella 4 chronic sinusitis |
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sulfa drugs and TMP other agents
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-nonabsorbable --> sulfazalazine (local action on gut) (used for IBD)
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sulfa and TMP AE
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1. allergic rxns: rash, fever, SJS
2. N/V/D 3. photosensitive 4. granulocytopenia and thrombocytopenia 5. avoid G6PD pts 6. category C and contraindicated near end of pregnancy |
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Fluoroquinolones
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MOA: inhibits DNA gyrase interfering with transcription and DNA synthesis
SOA: broad and varies b/t 4 generations; gram - > gram + aerobics incl peudomonas |
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Fluoroquinolones 2nd gen
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-Ciprofloxacin with mostly G- including pseudomonas and little G+
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Fluoroquinolones 3rd gen
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-Levofloxacin, IV and oral
-gram neg and some gram post (strep and staph) |
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Fluoroquinolones 4th gen
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-Gemifloxacin (factive)- strep, staphs and atypicals
-Moxifloxacin (avelox) IV, PO- broad w/anaerobic coverage |
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clinical use of Fluoroquinolones
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1. UTI esp. Ciprofloxacin
2. Gonococcal infxs (inc resistance) 3. Community acquired PNA esp Levaquin 4. Bacillus anthracis 5. Intrabdominal infxs |
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Fluoroquinolones pharm
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-PO = IV dosing
-mostly BID or qd -renal elimination |
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Fluoroquinolones AE
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1. C/in kids <18 due to possible damage to growing cartilage
2. C/I in preg 3. Tendonitis |
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Metronidazole (Flagyl)
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-useful for parasitic and anaerobic infxs
-Gold standard PO, IV, for anaerobic -amebae, Giardiasis, trichomoniasis, c.diff infxs SE: disulfiram-like rxn w/alcohol, metallic taste, dark urine (harmless) |
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Nitrofurantoin
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-for UTIs, PO
-MOA: broad activity against urinary pathogens -? in preg -AE: avoided in G6PD pts, pulmonary fibrosis in pts taking it everyday |