Antibiotics Flashcards
resistant worries for Vancomycin
resistant gene on plasmid(means very mobile gene) being picked up by MRSA
Vancomycin
MRSA
penicilin resistant S. pneumo
susceptible enterococcal infections
Drug for vancomycin resistant Enterococci
Dancomycin
Target of beta lactam antibiotics
Peptidoglycan synthesis
Aerobic gram +
staph
strep
enterococci
listeria
anaerobes
clostridium actinomyces peptostreptococcus propionibacterium bacteroides fusobacterium prevotella
aerobic (facultative) gram negative
enterobacteriaceae
neisseria
pseudomonas
haemophilus
Atypical/intracellular bacteria
mycoplasma chlamydia legionella mycobacterium rickettsia spirochetes
Examples of Aminoglycosides
streptomycin
gentamicin
amikacin
toxicities of aminoglycosides
nephrotoxicity - see elevated creatinine
ototoxicity
Macrolides and Ketolides
Broad spectrum but not deep Erythomycin Clarithromycin Azithromycin (known as z pack) Telithromycin - ketolide
mechanism of Macrolides
bind 23S rRNA of the 50s ribosome
prevents protein elongation
Telithromycin
binds at 2 sites
ketolides
Erythromycin
can cause GI upset - makes pt nauseous
Azithromycin
longer half life
clinical uses for Macrolides
empiric therapy for community aquired pneumonia (CAP)
DOC for legionella, mycoplamsa, and chlamydia
Macrolides
Most aerobic gram neg rods are resistant to
Macrolides
Resistance to Macrolides
Efflux pump
Enzyme mediated methylation of binding site on 23S ribosome
Examples of Lincosamide
Clindamycin
Clidamycin active against
generally anaerobic drug
aerobic gram + including MRSA and s. pneumo
gram + and - anaerobes
some protozoans
mechanism of Tetracyclines
bind reversibly to 30s subunit
blocks binding of tRNA
What is clindamycin not useful for?
aerobic gram negatives
Tetracycline
broad range many aerobic gram pos and neg
anaerobes
Atypicals - especially useful
some protozoa
Adverse reactions to Tetracyclines
Not given to childern under 8
Not used in pregnancy
Cause photosensitization - bad sunburn
Fluoroquniolones
Ciprofloxacin - below the waist Gatifloxacin levofloxacin oflaxacin moxifloxacin
DNA gyrase inhibitor
Fluoroquinolones
clinical uses of fluoroquinolones
broad spectrum
aerobic, gram neg bacteria
active against strains of staph and strept and many atypical
toxicities of Fluoroquinolones
may damage growing cartilage - so no childern under 18 or pregnant women
Black box warning of tendon rupture
Anti folate drugs
TMP/SMX
sulfonamides
trimethoprim
anerobic drug
metronidazole
clindamycin
TMP/SMX mechanism and activity
broad spectrum interferes with folate synthesis by bacteria which is needed for nucleic acid synthesis aerobic gm pos (CA-MRSA) some aerobic gm neg non bacterial organisms
Clinical uses of TMP/SMX
UTI
RTI
prostate and vaginal infections
Toxicities of TMP/SMX
skin rash
GI upset
bacteriocidal antibiotics
antibiotics that target cell wall causing lysis of bacteria
beta lactams
vancomycin
daptomycin - cell membrane
Antibiotics that block protein synthesis
aminoglycosides 30s macrolides 50s tetracyclines 30s clindamycin 50s chloramphenical 50s linezolid 50s
Bacterostatic
antibiotics that inhibit growth and/or replication
Antibiotics that inhibit RNA synthesis
Rifamycin
Rifabutin
Antibiotics that target DNA or DNA synthesis
Quniolones
metronidazole
clofazimine
Antimetabolite antibiotics
Trimethoprimsuflamethoxazole (TMP/SMX)
dapsone
para-aminosalicylic acid
Empirical
treatment before receiving the test/cultures back
Beta lactams
Effective for certain Gr+ or Gr- Penicillins cephalosporins carbapenems monobactams
Antibiotics for Gram + cocci
Vancomycin
Daptomycin
TB drugs
Isonizad
Ethambutol
Pyrazinamide
Peptidoglycan synthesis and structure
Composed of alternating NAG and NAM units linked by transpeptidases (PBP) via D-Ala D-Ala units
Cyloserine
inhibits reactions involved in incorporation of alanine into cell wall percusor
Glycopeptides
bind to terminal D-ala-D-ala residues prevents incorporation of subunit into growing peptidoglycan
Bacitracin
prevents dephosphorylation of phospholipid carrier which prevents regeneration of carrier necessary for synthesis to continue in building peptidoglycan walls
Beta lactams
bind to end inhibit enzymes which catalyze this link
Mechanism of action of beta lactam antibiotics
transpeptidases catalyse crosslinking of peptidoglycan residues
beta lactam antibiotics bind transpep. and block this reaction resulting in weak cell walls and bacterial lysis if bacteria are actively growing
Bacteriocidal
Types of Penicillins
natural
anti-staph penicillins
aminopenicillins
extended spectrum
what is unique about the structure of Penicillin
B lactam ring
Thiazolidine ring - essential for activity
Natural penicillins
5 is oral G is IV or IM limited spectrum Most strept - GAS, GBS, viridians group NOT s. pneum Most gram + anaerobes N. meningitidis Treponema pallidum
Poor activity against aerobic and anaerobic gram neg rods and not active for intracellular bacteria
natural penicillin
Anti Staph Penicillin
Many staph make beta lactamases
this antibiotic have large side groups making resistant to lactamases
Naficillin and Oxacillin (IV)
Dicloxacillin (oral)
Anti Staph penicillin activity
MSSA
MSSE - methicillin resistant staph epidermidis
Not active against
MRSA
MRSE
How is methicillin resistance confered?
due to altered PBP