Antibacterial Drugs Flashcards
cephalosporin resistances in general
intrinsic: pseudomonas. enterococci; membrane permeability; altered PBPs; B-lactamases
cefoxitin activity
excellent anaerobic activity 2nd generation
ceftriaxone clinical use
community acquired pneumonia meningitis(penetrates CSF) UTI
Penicillin G. administration
IV
Nafcillin. administration
IV
piperacillin. administration
IV
piperacillin-tazobactam. administration
IV
Bacitracin. activity
GP only, topical
cephalexin. administration
PO
metronidazole adverse effects
metallic taste;
HA, vertigo, confusion, psychosis,
disulfram-like effect w/alcohol(vomit, flush)
Penicillin G. adverse effects
hypersensitivity reactions(rash. hives/anaphylaxis. serum sickness. immune mediated cytopenias. acute interstitial nephritis); seizures at high doses
clindamycin, mechanism, activity, adverse reaction
binds 50S subunit GP only! “above the diaphragm” classically some CA-MRSA adverse reaction is c. diff infection
Vancomycin resistance?
alteration of vancomycin binding site (vanA.B.C.D.E),VRE; thickened cell wall(VISA)
rifaximin use
traveler’s diarrhea enteric drug; does not absorb across gut
isoniazid mechanism, clinical use
inhibits mycolic acid cell-wall syntehsis via O2 dependent pathways used for mycobacterial infections
aztreonam activity, clinical use
GN only, used w/b-lactam allergy occasionally; limited immunogenic potential
amoxicillin. administration
PO
Polymyxin B. Colistin activity
GN bactilli only
Daptomycin. adverse effects
GI distress. HA. elevated CPK(creatine phosphokinase)/rhabdomyolysis(avoid statins)
ampicillin, amoxicillin activity
widens spectrum to some GN(H. flu. E. coli; NOT pseudomonas)
Daptomycin. activity
GP ONLY! MRSA activity; enterococci(including VRE). anaerobes
ceftazidime clinical use
pseudomonas activity; very broad GN
ceftriaxone penetration, half life
high degree of CSF penetration; EXTREMELY long t1/2. can q24h dose for outpatient IV
name the tetracyclines, mechanism and activity
doxycycline tetracycline minocycline reversibly bind 30S subunit blocking tRNA access to mRNA broad GN(no pseudo) staph, strep(some CA-MRSA) some anaerobic atyps: chlamydia, mycoplasma 4(tetra) minos by the dox
Nafcillin. Dicloxacillin clinical use
primarily used for methicillin-susceptible S. aureus
ceftaroline. administration
IV
Vancomycin oral
does not cross GI tract given orally; used for c. diff
Fosfomycin. clinical use
UTI only
Vancomycin. activity
GP ONLY! MRSA activity; enterococci if susceptible; anaerobes
Nafcillin. resistance?
altered PBP encoded by mecA–>PBP2a(MRSA); cant bind it anymore
adverse effects of TMP-SMX
common - HANV, rash
less - hyperkalemia, hepatitis, pancreatits
rare - SCAR, anemias, thrombocytopenias, separates drugs from albumin, kernicterus
ethambutol use
inhibits arabinogalactan, lipoarabinomannan synthesis used for mycobacterial infections
carbopenam. adverse effects
hypersensitivity(cross-reaction w/penicillin)
Nafcillin, dicloxacillin activity
GP ONLY; narrow specturm; think penicillin G with overcoming certain b-lactamases
Vancomycin. clinical use
only use instead of b-lactam if: empiric therapy for severe infection. resistant GP infection. allergy to b-lactam; used for C. diff via oral dose
cefepime activity
EXTREMELY GN active including pseudomonas; one of broadest spectrum agents available; still has GP activity; resistant to almost all b-lactamases 4th gen
anti-tubercular drugs
isoniazid, rifampin, streptomycin, ethambutol, pyrazinamide
name all the drugs with GP only activity
nafcillin dicloxacillin vancomycin daptomycin bacitracin mupirocin clindamycin linezolid tedezolid
aztreonam. administration
IV
Penicillin G. activity
GN: cocci only; GP: cocci and anaerobes; spirochetes. enterococci
name all the cephalosporins in order by generation
1st gen: cefazolin cephalexin(PO) 2nd gen cefoxitin 3rd gen ceftriaxone ceftazidime 4th gen cefepime 5th gen ceftaroline
name the macrolides, mechanism, and activity
azithromycin clarithromycin erythromycin binds 50S subunit, blocks translocation broad GN(no pseudo) GP: staph,strep, pneumo(if susc.) atyp: myco, legionella, chlamydia
carbapenem administration
IV
fidoxamicin mechanism, use
blocks RNA polymerase by not letting DNA open PO drug approved for c.diff infections does not cross GI; very narrow spectrum(only effects some GP in gut); preserves flora better than others
name all the drugs with pseudomonas activity
piperacillin/pip-tazo ceftazidime cefapime meropenem imipenem fosfomycin - UTI only aminoglycosides(gentamicin, amikacin, tobramycin, streptomycin)
metronidazole
mechanims, activity
diffuses into bacteria and produces free radicals
activity: ANAEROBES“below diaphragm”
includes b. fragilis; protozoa
Polymyxin B and colistin adverse effects
nephrotoxicity. neurotoxicity
cefazolin. administration
IV
tigecycline, mechanism, activity, problems
semi-synthetic tetracycline very broad spectrum GN(no pseudo) GP(MRSA and VRE) most anerobes resistance develops rapidly…limits use; also increased mortality w/pneumonia pts….
name the carbapenems
meropenem imipenem ertapenem doripenem(black boxed)
Vancomycin. administration
IV/PO PO for c.diff; not absorbed
cefepime. administration
IV
Penicillin G. clinical use
Grp A and B strep. and Streptococcus pneumoniae; anaerobic infections(dental abscess. human bites); syphilis
Daptomycin. administration
IV
cefoxitin clinical use
prophylaxis for intra-abdominal surgery 2nd gen
ampicilin. amoxicilin adverse effects
in addition to hypersensitivity�.GI distress is common; maculopapular rash if treating mono(100% of pts)
ceftazidime. administration
IV
cephalosporins activity
GN increases w/generations(except 5); most have som GP ; no good against enterococci; only 1 good against MRSA. not much anaerobe activity
Colistin(polymyxin E). administration
IV
ceftaroline activity
MRSA activity; broad GP activity. no enterococci; only some gram-neg activity. no pseudomonas�similar activity to that of gen3
cefoxitin. administration
IV
adverse effects of rifampin
orange secretions, hepatitis, GI and heme issues
Carbapenems resistance?
any weird acquired metallo-beta-lactamases. KPCs can still be resistant to carbapenems
Polymyxin B. Colistin clinical use
Serious resistant GN infections; inhaled resistant GN pneumonia
piperacillin-tazobactam. activity
adds S.aureus (not MRSA). B-lactamase producing GN and anaerobes; AND PSEUDOMONAS
Daptomycin. clinical use
complex GP infections(soft tissue; bacteremia/endocardidits)
ampicillin. administration
IV
Vancomycin. adverse effects
Red Man Syndrome; dose-related ototoxicity; nephrotoxicity(avoid co-administration with other agents)
cefazolin, cephalexin(1st gen) clinical use
surgical prophylaxis. soft skin/tissue infections(resistance limiting)
Polymyxin B. administration
IV
name the B-lactamase drug combos
ampicillin-sulbactam amoxicillin-clavanic acid piperacillin-tazobactam
Dicloxacillin. administration
PO
Fosfomycin. administration
PO/Powder
ceftriaxone, ceftazidime activity
excellent GN activity 3rd gen
Penicillin G. resistance?
B-lacatamases hydrolyze b-lactam ring; PBPs can be modified on transpeptidase; decreased perm.; efflux pumps
rifampin clinical use
prophylaxis for n. meningitidis, s. aureus mycobacterial infections
ceftriaxone. administration
IV
unique PK/PD of rifampin
p450 inducer; can decrease concentrations of other drugs in body
carbapenem activity
VERY BROAD SPECTRUM; GN w/pseudomonas; GP;Anaerobes ertapenem = no pseudo/acinetobacter spp.
name the aminoglycosides and their mechanism and activity
gentamicin amikacin tobramycin streptomycin binds 30S ribosome; stops protein synthesis only GN(w/pseudo) activity; cant’ penetrate GP wall w/out synergy
Fosfomycin resistance?
can develop rapidly on the transporter that brings the drug into the bacteria
Daptomycin cannot be used where?
inhibited by pulmonary surfactant. DON�T USE FOR PNEUMONIA; bactericidal
Carbapenems. clinical use
empiric treatment for serious infections and resistant infections
Penicillin V. administration
PO
ampicillin. amoxicilin clinical use
community acquired HEENT/upper resp infectsion; community acquired UTI
adverse effects of fluoroquinolones
Common - HANV(HA,nausea, vomiting) ab pain, dizzy
less common - long QT, tendon rupture, cartilage problems in kids, pregos can cause c.diff