anti-microbials
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- 7 bacteriocidal agents
-
beta lactams
aminoglycosides
vancomycin
fluorouinolones
rifampin
metronidazole
isoniazid - 6 bacteriostatic agents
-
macrolides
chloramphenicol
clindmycin
tetracylcin
sulfonamides
ethambutol - inhibitors of cell wall synthesis
-
beta lactams
vancomycin - beta lactams subtypes
-
penicilllins
cephalosporins
carbapenems
monobactams - inhibitor of transpeptidation reaction
- beta lactams
- mechanisms of resistance to penicillin and cephalosporins
-
autolytic enzyme deficiency
altered PBP
productions of beta lactamase
outer membrane - DOC for group a beta hemolytic strep, viridans strep, meningicoccus, treponema
- penicillin G
- penicillin A, D, M, E
-
A: penicillin G acid labile, V stable
D: wide, low concentratio in prostate, eye, CSF, 60% protein bound
M: not metablozid
E: rapid renal clearance, high concentration in urine - side effects of penicillin
-
skin rash, fever, bronchospasm, vasculiis, serum sickness, exf derm, steen johnson syndrom, anaphylaxis
all due hypersinsitivity antibodies against enicillinoic acid - penicillinase resistant penicillins (methicillin group)
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nafcillin
dicloxacillin - aminopenicillins
-
ampicillin
amoxicillin - antipseudomonal penicililns
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carbenicillin
indanyl carbenicilin (orally active compound for UTI) - extended spectrum penicillin
- piperacillin
- what is augmentin?
- amoxicillin/clavulinic acid
- first generation cephalosporin
-
cefazolin
cephalexin - first generation cephalosporins are used often for
- surgical prophylaxis (cefazolin)
- second generation ceph
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cefuroxime
cefuroxime axetil (orally active) - second generation ceph's are used for
- increased gram - actiity
- third generation ceph
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cefotaxime
ceftizoxime
ceftriaxone - cephalosporins with broad gm - activity
-
third generation
resistant to beta lactamases - ceftriaxone
-
third gen ceph with long half life 8 hrs
good cns penetration
used for meningitis, hospital cquired pneumonia, sepsis, outpt gonorrhea - cefepime
-
4th generation ceph
reistant to some beta lactamase
cleared by kidneys,
excellent cns penetration
NOT actie against MRSA
b fragilis
myco - ceftazidime
-
third generation ceph
increased antipseudomonal activity - meropenem
- broad spectrum carbapenem
- particularly usefull against mixed infections of nosocomial organisms nd has excellent activity against anaerobes P. aeruginosa
- meropenem
- beta lacam with spectrum that resembles aminoglycoside (good against gm -, poor against gm + and anaerobes)
- aztreonem
- beta lactam not associated with hypersensitivity
- aztreonem
- meropenem administration
- IV, cilastatin (peptidase inhibitor) not required
- beta lactamase inhibitors
-
tazobactam
sulbactam
clavulinic acid - although both can be used for antibiotic associated colitis due to c dif, you would use metronidazole or vancomycin
- metronidazole to reduce appearance of vancomycin-resistant srains
- vancomycin s/e
-
flushing
tach
thrombophlepb
ototoxicity - mechanism of resistance to vancomycin
- peptidoglycans wherein the pentapeptide terminates in d-ala-lactate and has lower affinity for vancomycin
- tetracylcin MOA
-
enter bacteria by energy dependant process
act at A site of 30s ribosome prevent binding of tRNA - tetracyclin/doxycyclin A,D,M,E
-
oral (30% T 100% D) but don't use dairy, antacids, or iron with T
binding to plasma proteins increases with inc lip sol
excretion is both urin and feces (kidney for T, hepatic for D) - side effects of tetracyclin
-
toxicity
photosensitivity
renal insufficiency irritation
fancony synrome
super infections - MOA of CAM
- inhibits synthesis at 70s ribosome and halts translation elongation
- Chloramphenicol A,D,M, E
-
oral
good penetration into CSF
hepatic met - gray baby syndrome is associated with
- Chloramphenicol
- CAM can cause what blood disorders
-
reversible bone marrow depression
rare aplastic anemia - DOC for typhoid
- CAM
- guidelines for cam use
-
life threatining infection
never prophylactically or mild infection
avoid prolonged use
discontinue if lekopenia occurs - aminoglycosides
- gentamicin, tobramycin, amikacin
- MOA of aminoglycosides, A,D,M,E
-
translational distortion or block based on concentration
poor oral availability, renal excretion, poor cns penetration - resistance to aminoglycosides
-
intrinsic due to low ph, hyperosmolarit, divalent cations,
acquired: ribosomal, decreased uptake,
ENZYMES (most common method) - which aminoglycoside has widest spectrum
- ami > tobra > genta
- S/E of aminoglycosides
-
neurotoxicity
ototoxicity
renal - structural analog of folic acid and competes with FAH
- trimethoprim
- structural analog of p amino benzoic acid PABA
- sulfonamide
- treat nocardia
- sulfonamide (in combo with ampicillin)
- treat protozoal infections including p falciparum, toxoplasma, pneomcystic carinii
- sulfonamides
- drug of choice for leprosy
- dapsone
- sulfonamide A,D,M, E
- good oral absorbpion, wide distribution including CNS, acetylted andproduct remains toic, can precipitate in urine
-
cotrimaxazole
(cotrimazole) -
combo of sulfamethoxazle with FAH2 inhibitor trimethoprim used fr UTI
not effective against pseudomonas - trimethoprim A,D,M,E
-
well absorbed from gut
blood levels higher than other tissues
acetylated in liver and appears in urine - theoretical side effect of SMZ/TMP
- megaloblastic anemia in folate deficient patient
- inhibit topoisomerase IV and DNA gyrase
- fluoroquinolones
- second gen fuoroquinolone
- ciprofloxicin
- third generation fluoroquinolone
-
levofloxacin
moxifloxacin - resistance to fluoroquionolone
-
chromosomal mutation in DNA gyrase or topoisomerase genes or
increased efflux plasmid mediated - fluoroquionlone A,D,M,E
-
orally available
excellent tissue peneration, bone and prostate (CSF low, brain parenchyma high)
some excreted through urine unchanged (Levo), others undergo extensive hepatic met - meningococcal prophylaxis DOC
- ciprofloxicin
- macrolides
-
erythromycin
clarithromycin
azithromycin - binds 50s subunit of ribosome, inhibits protein translocation step
-
erythromycin
m - mot often used to treat mycoplasm pneuomniae
- erythromycin
- penicillin allergic individuals cn use this for strep and pneumococcal infections
- erythromycin
- DOC for C diptheriae
- erythromycin
- DOC for legionella
- Erythromycin
- erythromycin A,D,M,E
-
orally available, but acid labile
diffuses well into most body spaces except CSF unless inflamed
concentrated by liver
excreted in bile - ilosone
- acid resistant form of erythromycin
- S/E of erythromycin
- GI upset,, ilosone can cause cholestatic hepatitis, potentiation of other drugs by interfereing with cytochrome p45
- more effective than erythromycin against H flu
- claryithromycin or azithromycin
- partitions into acidic compartmens, such as acidic vesicle in phagocytic cells
- azithromycin
- anaerobes, anaerobes, anaerobes
- metronidizole
- effective against virtually al anaerobic gram - bacteria, including bacteriodes, nicararophilic protozoa, but ineffective agaisnt aerobic and facultative anaerobic
- metronidazole
- MOA of metronidazole
- interrupts electron transport process-- mutagen
- metronidazole A,D,M,E
- oral, 8 hour half life, vol of distribution is total body water, unchanged and oxidized are excreted in urine and penetrates all tissues
-
furry tongue, head ache, nausea, contraindicated with CNS disease, glossitis, stomatitis
disulfiram like effect - metronidazole
- anaerobe coverage best compounds
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metro, meropenem, CAM, amp/calv, ticarcilin/sulbactam, piperacillin/tazobacam
NOT CLINDAMYCIN - anti mycobacerial
- isoniazid, rifampin, pyrasinamide, ethambutol
- inhibits synthesis of mycolic acids
- isoniazid
- isoniazid A,D,M,E
- well absorbed from gut, well distrubted, acetylated and appears in urine, there are fast acetylaters and slow acetylaters that are determined geneticaly
- toxic effects of isoniazid
- hepatotoxicity, optic neuritis
- inh therapy includes administration of what to prevent symptoms of excitabillity (neurotoxicity)
- pyridoxine
- interacts with phenytoin to cause toxicity, lethargy, incoordination
- isoniazid
- binds to beta subunit of bacterial RUNA polymerase
- rifampin
- rifampin A,D,M,E
- well absorbed from gut, distributes widely, deacylated in liver, only 20% in uirne, cautin with compromised hepatic function
- why is rifampin no good for grm -
- doesn't penetrate outer membrane
- can be used for H flu prophylaxis
- rifampin, cipro is better
- rifampin side effects
-
hepatotoxicity
inducer cyp3a4 (cyt p450 enzyme - pyrazinamide
-
bacericidal for tubercle bacillus
absorbed from gut, widel distributed, excvreted by kidne - important part of short term 6 month TB treatment
- pyrasinamidr
- side effects of pyrazinamidr
-
hepatotoxicity
hyperuricemia - drug is taken up by diviiding mycobacteria and is tuberculostatic after 24 hrs
- ethambutol
- ethambutol
- well absorbed from gi tract, distributes widely, renal excretion
- s/e of ethambutol
- retrocular neuritis