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26 Cards in this Set
- Front
- Back
Quinolones |
Mech: quinolones inhibit gyrase, and Topoisomerase IV (@ higher conc)
-Broad spectrum, wide indications -excellent absorption & F -most are available in IV & PO form -all quinolone have poor CNS penetration -excretion in kidney
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Quinolones Use/Adverse Effects |
Use: UTI, bacterial diarrhea, gonococcal infection, legionellosis, respiratory infection, anthrax
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Spectrum of activity of quinolones |
2nd = ciprofloxacin ( aerobe), 3rd = levofloxacin (aerobe), 4th = moxifloxacin (anaeroe에도 효과적이다; spectrum넓어진 대신 pseudomonas에는 사용할 수 없다). 셋다 atypical에 어느정도 효과가 있다.
-Ciprofloxacin, levofloxacin: aerobic G(-) including P. aeruginosa -Moxifloxacin & gatifloxacin: broader antibac. spectrum, weak activity against pseudomonas -Gemifloxacin: most active against S. pneumoniae. MRSA에 대해 효과 있을수도, 없을수도. -Fluoroquinolones: active against certain atypical organisms; UTI & prostatis 에 사용 (except for moxifloxacin) -Ofloxacin & levofloxacin: pelvic inflammatory disease -Levofloxacin & moxifloxacin: community-acquired pneumonia |
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Tetracyclines 예 |
-Terramycin = oxytetracycline (코피났을 때 윤활/항균 효과) -Doxycycline -Minocycline |
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Tetracycline PK |
-PO: possible but various bioavailability; not with metal ions, less with food, better in fasting state -IV, IM: possible -half life: doxycycline + minocycline - 16 h. -Distribution: poor BBB penetration/secretion to placenta, milk (toxic to fetus), accumulation in liver, spleen, BM, bone, teeth *Doxycycline, minocycline: liver metabolism to feces |
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Tetracycline side effects |
1. GI irritaiton** -not with milk || antacids 2. Binding to Ca2+ tissues ** -yellow discoloration of teeth -not for <5 years old 3. superinfection (pseudomembranous colitis) 4. phototoxicity 5. Liver toxicity** (tetracycline, oxytetracycline - less toxic) 6. IICP
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Tetracycline Indicators |
1. Broad spectrum 2. Rickettsia 3. Mycoplasma 4. Chlamydia 5. STD (SBMCR 시발미친롬) |
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Chloramphenicol |
-targets 50 S (vs. 30S targeting: tetracycline) -blocks initation of translation/premature termination (이건 tetracycline과 유사) + chloramphenicol also inhibits mitochondrial ribosome -VERY BROAD. aerobic G+, G-; anaerobic G+, G-. |
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Indications of chloramphenicol |
-now obsolete; some rickettsial infection -distribution: CNS, CSF (good BBB penetration) -adverse reaction: GI & BM depression
**Gray baby syndrome (premature/new born with low hepatic function)
-antagonize b-lactam or AG. |
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Chloramphenicol indication |
first consider others (due to high toxicity)
Typhoid fever, meningitis, anaerobic infection, rickettsia & brucellosis
(B-A-R-T: 토해서 머리가 아프다 (meningitis)) 그리고 앞글자가 B로 시작하니깐 BM suppression이 부작용. |
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Macrolide (erythromycin, clarithromycin, azithromycin -외울 때: clathrin, zenith 연상하면 됨. zenith-꼭대기니깐 제일 반감기 김. --뒤로 갈수록 반감기 길어짐) |
-narrow: aerobic G+ alone -PO: destruction by gastric acid, so use acid stable enteric coated tablet. -well distributed but BBB 통과 잘 못함; -eliminated mainly in liver to bile, partly to kidney.
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Macrolide indication |
1. Mycoplasma 2. Legionellosis 3. Peptic ulcer due to H. pylori (clarithromycin-amoxicillin-omeprazole) 4. STD 5. Diphtheria, pertussis, tetanus 6. G+ infection 7. prophylaxis of rheumatic fever
(시팔로마 빨리뒤져 SPLMPDG) |
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Clindamycin/Lincomycin |
-50S binding, bacteriostatic -chloramphenicol, erythromycin, clindamycin: binds to the same site in 50S -lipid soluble structure; metabolized in liver. 하지만 BBB 통과 못한다.
Side Effect: 1. Pseudomembranous colitis (C. difficile) 2. Hypersensitivity 3. Neuromuscular blockade
Indication = anaerobic infection; in case of mixed infection (abscess) --with AG. (클린다와 링컨은 애를 안 낳음 (an-)) |
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Clindamycin, metronidazole |
-considered as agents of choice for anaerobic infections
-Most clostridium and bacteroides (anaerobe) are susceptible to clindamycin -Metronidazole is the preferred agent for the treatment of bacterial vaginosis and infections caused by Entamoeba spp. and T. vaginalis.
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Polymyxin |
-membrane destruction as PP detergent -topical use due to renal toxicity --> for superbug. -pseudomonas infection to ext. ear |
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Vancomycin |
-big molecule, not permeable to membrane -bind to cell wall precursor -effective to G+ only. -used for GI infection by drug-resistance strain = PO / systemic infection by drug resistance strain = IV -inner ear/kidney toxicities
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Vancomycin 내성 출현 |
D-ala has been replaced by D-lactate, so vancomycin cannot bind. |
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Bacitracin |
-big molecule, not permeable to membrane -inhibit wall synthesis -effective to G + only. -topical application |
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ESKAPE |
new drugs most urgently needed against ESKAPE pathogens |
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Superbug #1 = Enterobacteriaceae |
only collistin (오래된 polymyxin) is effective |
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serious g+ infection |
staphylococcus = nafcillin strep = penicillin G\ ceftriaxone entrrococcus, listeria = ampicillin |
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Highly resistant |
G+ = VRE, MRSA G- = pseudomonas, ESBL |
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Double coverage for pseudomonas |
b -lactam (pip/tazo, cefepime, carbapenem) + anti-pseudomonal quinolones or AG. |
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antibiotics for anaerobic bacteria |
metronidazole, carbapene,. b lactam + b lacatmase inhibitor, clindamycin. |
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vs. Clostridium difficle |
-just two effective antibiotics =metronidazole, vancomycin |
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for atypical bacteria |
macrolide, tetracycline, quinolones, chloramphenicol. |