Antibacterials Flashcards
natural penicillins
penicillin G
penicillin V
B lactamase resistant penicillin
cloxacillin oxacillin dicloxacillin methicillin nefcillin
broad/extended spectrum penicillins
amoxicillin ampicillin ticarcillin carbenicillin piperacillin mezlocillin
penicillinase inhibitors
sulbactam
clavulanic acid
1st gen cephalosporins
cephalexin
cefazolin
what causes pseudomembranous colitis
c. difficile
what group of drugs are B-Lactams
penicillins
cephalosporins
carbapenins
aztreonam
what do B-Lactams do?
they bind to penicillin binding proteins and inhibit transpeptidaztion, the bacteria can’t make cell wall
what have baceteria developed to resist B lactams
B-lactamases
natural penicillins are derived from what
penicillin notatium
penicillin G given how
IV, cuz its hydrolyzed by the stomach acid
penicillin G characteristics
narror spectrum, mostly gram +
destroyed by B-Lactamase
penicillin V is given how
orally, acid stable. unpredictable absorption
T/F broad or extended spectrum penicillins are resistant to B-lactamases
false
how is amoxicillin given?
orally
contraindications with ampicillin
causes rash in patients with mononucleosis and other viral infections
what do penicillinase inhibitors do?
inhibit penicillinase (B-Lactamase) not an antibiotic
T/F you use penicillinase inhibitors in combination
true
S.E. of all penicillins
B lactam ring may inhibit GABA
high IV dose may induce seizures
allergic responses
structure of cephalosporins
have 2 R groups on B-lactam ring that can be used or changed
how many generations of cephalosporins are there
5
each generation of cephalosporin is better at what?
more gram - activity
more resistance to B lactamase
second generation cephalosporins
cefaclor
cefuroxime
cephamycins
third generation cephalosporins
ceftazidime
ceftiaxone
cefoperazone
4th generation cephalosporins
cefepime
5th generation cephalosporins
ceftaroline
S.E. of cephalosporins
some allergic cross reactivity with penicillin sensitive patients.
possibility of superinfection
is there a problem for a pt who is sensitive to penicillin to give them cephalosporin?
yes, some cross allergic responses.
carbapenems general characteristics
smaller penicillinase resistance B lactams
very broad spectrum
can enter CNS more readily- increase seizures
how are carbapenems given?
IV
2 carbapenems
imipenem
meropenem
imipenem is better for what
gram +
meropenem is better against what
gram -
S.E. of imipenem
metabolized to a nephrotoxic product, given with another drug that stops the toxic product
what is given with imipenem?
cilastatin
what does cilastatin do?
inhibits the metabolic enzyme in the kidney that produces the toxic product from imipenem
one of the monobactam drugs
aztreonam
aztreonam is given how?
IV or IM
is aztreonam affected by B lactamases?
no
what is aztreonam used for?
aerobic gram - bacteria like e coli.
T/F aztrenam is cross reactive with allergic patients?
FALSE, it is not.
S.E. of aztreonam
seizures
non B lactic cell wall inhibitors
vancomycin televancin dalbavancin bacitracin fosfomycin cycloserine
vancomycin MOA
binds to dialamine residues on subunits of the cell wall and prevents cross linking
vancomycin used for what
most gram + infections. and staphylococcal infections that are resistant to B lactamases
how is vancomycin given? and what is the exception
IV, given orally with c. difficile infection
S.E. of vancomycin
nephrotoxicity
ototoxicity
rapid IV causes histamine release, leads to flushing, rash, itching (red man syndrome)
what drug causes red man syndrome
vancomycin
T/F bacteria treated with vancomycin can become resistant by changing their dialamine residue to lactic acid
TRUE
televancin and dalbavancin are both what
lipoglycopeptides
MOA of televancin and dalbavancin
act both like vancomycin and as a disrupter of bacterial cell membrane
S.E. of dalbavancin
fetal damage
renal damage
metalic taste in mouth
dalbavancin is used to treat what
complex skin infections with gram + bacteria and hospital acquired infections.
bacitracin MOA
inhibits recycling of the bactoprenol carrier vs gram + cells,
bacitracin is given how, why?
topically, given orally causes nephrotoxicity
bacitracin especially useful against what
staph
fosfomycin MOA
blocks synthesis of n acetyl muramic acid
fosfomycin useful against what
aerobic gram - bacteria like e coli and for uncomplicated urinary tract infections
S.E. of fosfomycin
diarrhea
cycloserine MOA
inhibits incorporation of alumni into n acetyl muramic acid
cycloserine used against what
mycobaceterium tuberculosum
S.E. for cycloserine
CNS sedation, tremor, psychosis
antibiotics that inhibit bacterial protein synthesis
macrolides
aminoglycosides
tetracyclines
macrolides
erythromycin
clarithromycin
azithromycin
telithromycin
erythromycin (macrolides) MOA
reversibly binds to the 50s subunit and inhibits translocation of mRNA. inhibits binding of tRNA to the “p” site
S.E. of erythromycin
Gi upset- nausea, heat burn increase Gi activity by increasing motion inhibits P450 liver damage cardiac arrhythmias
erythromycin works against what
gram + like staph and strep
how do you take clarithromycin?
orally
what is clarithromycin used against
helicobacter pylori, associated with ulcer formation
what drug inhibits P450
erythromycin
what is special about azithromycin?
longer halflife 3 days
telithromycin MOA
same as other macrocodes but induces less resistance because it is not as readily transported out of bacterial cell
S.E. of telithromycin
severe liver toxicity
blocks cholinergic receptors in muscle- worsens myasthemia gravis and inhibits cillary ganglion- decrease visual accomidation
what drug induces severe liver toxicity?
telithromycin
what drug has cholinergic effects, including eye affects
telithromycin
aminoglycosides
streptomycin gentamycin amikacin neomycin tobramycin kanamycin netilmicin
do all macrocodes have same MOA
YES
do all aminoglycosides have same MOA
YES
streptomycin (aminoglycoside) MOA
irreversibly bind to 30s subunit. can inhibit tRNA binding all along mRNA, including the initial site.
how do you give streptomycin?
IM, generally does not enter CNS
does streptomycin enter CNS?
no
S.E. streptomycin
NNOF
ototoxicity- both balance and hearing affected. hearing loss may be permanent
nephrotoxicity- lead to renal failure
high does leads to decrease Ach and receptors on muscle, neuromuscular blocade
fetal damage
targets of streptomycin
gram - aerobic bacteria
what drug has neuromuscular blocking side affects
streptomycin
gentamicin used for what
eye solution
neomycin used how?
topically or orally
nephrotoxic
tetracycline and other cycline MOA
reversibly bind to 30s subunit- bacteriostatic
inhibits binding of tRNA to the “a” site
how is tetracycline given?
orally or parenterally
S.E. of tetracycline
binds to cations like Ca deposited in storage site (teeth, bone) causes stains in teeth
preg category D
renal and hepatic toxic- degrades over time to toxic elements, why you don’t use pass expiration date
what drug do you definitely not want to use after expiration date and why?
tetracycline, turns into renal and hepatic toxins
targets of tetracycline
rickettsia
spirochetes
helicobacteria
legionella
advantages of “other” tetracyclines
less likely to bind to Calcium
tetracycline drugs
tetracycline
doxycycline
minocycline
tigecycline
chloramphenicol MOA
inhibits peptidyltransferase (enzyme inhibitor)
S.E. chloramphenicol
inhibits P450
can cause aplastic anemia
GREY BABY SYNDROME
what drug causes grey baby syndrome
chloramphenicol
what is grey baby syndrom
chloramphenicol is metabolized by phase 2. enzymes needed/used in phase 2 are not present in new borns so they can’t metabolize the drug, causes vasomotor collapse and baby turns blue, dies?
lincosamides
clindamycin
lincomycin
MOA of clindamycin/lincomycin
like erythromycin, inhibits translocation
S.E. of clindamycin/ lincomycin
severe superinfections with c. difficile
targets of clindamycin/ lincomycin
severe anaerobic infections like penetrating gut wound
used for dental prophylaxis in patients with heart valve problems
streptogramins
quinupristin + dalfopristin
quinupristin + dalfopristin MOA
inhibit A and P sites - quinupristin
inhibits P site- dalfopristin
S.E. of quinopristin and dalfopristin
muscle pains (beware of synergistic effects)
targets of quinupristin and dalfopristin
gram +
oxazolidinones
linezolid, tedizolid
linezolid MOA
inhibits binding of f methionyl tRNA to the P site, prevents initiation of the synthesis process
linezolid S.E.
anemia, pseudomembranous colitis
most powerful antibiotics causes this
pseudomembranous colitis
daptomycin is a _____
lipopeptide
daptomycin MOA
not cell wall or protein synthesis
acts by disrupting bacterial cell membrane. forms pores in the membrane
S.E. of daptomycin
muscle pain and weakness
pneumonia
careful with using with statins
what two drugs cause muscle pain and weakness
statins and daptomycin
targets of daptomycin and what is it used for
aerobic gram + only- strep, staph
used in skin and soft tissue infection or severe blood infection with staph Aureus.
fidaxomycin is given how
orally, non systemically absorbed, used against c. difficle
fidaxomycin used against what
c. difficle infection
fidaxomycin MOA
c difficle RNA polymerase, (enzyme inhibitor)
Fluoroquinolines
“floxacin” 10 on the market
ciprofloxacin MOA
inhibits topoisomerase 2 and 4. (enzyme inhibitor)
T/F ciprofloxacin has an affect on mammalian topoisomerase as well as bacterial
FALSE, very specific for bacterial
S.E. of ciprofloxacin
damage developing cartilage- not for children or pregnant women
tendonitis, achilis tendon rupture
phototoxicity- rash in sun
worsens myasthenia graves
who is ciprofloxacin contraindicated in
children and preg women, affects developing cartilage
targets or ciprofloxacin
broad
gram -/+, acid fast
antimetabolites- sulfonamides
sulfisoxazole
sulfacetamide
sulfadiazine
trimethoprim
sulfisoxazole MOA
reversibly inhibit dihydropterate synthetase (inhibits enzyme)
what does dihydrojpterate synthase eventually create?
tetrahydrofolic acid, must be made by the bacteria
S.E. of sulfisoxazole
allergic whole body rash- stevens johnson syndrome
hemolytic anemia in G6PDH deficient pt’s.
megaloblastic anemia
what drug causes steven johnson syndrome
sulfisoxazole
sulfisoxazole is used for what
urinary tract infections. any drug with SUL or SULF is probably a sulfur drug.
trimethoprim MOA
inhibits dihydrofolate reductase (enzyme inhibitor)
trimethoprim is used in conjunction with what
sulfamethoxizole
S.E. of trimethoprim
megalobalstic anemia
can be avoided with use of leukovorin
magloblastic anemia caused by trimethoprim can be avoided with use of what
leukovorin
trimethoprim used for what?
gram (-) bacteria, urinary tract infections- concentrates in acidic prostate/ vaginal tissue
metronidazole is a _____ and converted to ____
prodrug, converted to free radical
how is metronidazole given
IV
what is metronidazole used for
anaerobic bacteria infection but mainly for
protozoan infections- trichimonas, gardia
what drug is used for protozoan infections?
metronidazole
nitrofurantoin is a _____
reduced by bacteria to highly reactive molecule, concentrates in urine
nitrofurantoin is used for what
UTI
S.E. of nitrofurantoin
cough, chest pain, brown colored urine
agents used only topically
polymixin B gramicidin neomycin retapamulin mupirocin
Polymixin B MOA
binds to negatively charged sites on LPS of gram - bacteria - Increases membrane permeability.
S.E. of polymyxin B
nephrotoxic
neurotoxic
ataxia
perioral parasthesia
mupirocin MOA
binds to bacterial isoleucyl tRNA synthesis
retapamulin MOA
inhibits pepitdyl transferase
retapamulin is used for what
topical treatment of skin staph or strep infections
antimycobacterial agents
isoniazid rifampin pyrazinamide ethambutol bedaquiline
all antimycobacterial agents are what
enzyme inhibitors
T/F you always use two or more antimycobacterial agents to prevent resistance
TRUE
antimycobacterial agents are a major problem in what kinds of people
immunosuppresive
antimycobacterial agents are different how?
cell wall different, live inside target cells can lay inside dormant
Isoniazid is a ____
prodrug
metabolism of isoniazid produces what
produces an inhibitor of multiple mycobacterial enzymes, inhibits cell wall synthesis
isoniazid is a bacterial____
static for dormant cells
T/F isonizid is used in combination and for prophylaxis
true
how is isoniazid metabolized
acetylation
S.E. of isoniazid
increase excretion of Vit B6 causes pyridoxime deficiency niacin deficiency - pellegra tumor optic neuritis hepatotoxicity peripheral neuropathy
rifampin MOA
inhibits DNA depend RNA polymerase- cidal
what is a big static antibacterial agents
isoniazid
rifampin S.E.
hepatic toxicity
body fluids TURN RED
induces P450 very strong (little surprise)
what drug is related to the “little surprise”
rifampin
pyrazinamide is a _____
prodrug
where is pyrazinamide converted and what is its MOA
converted in macrophages where TB lives. inhibits fatty acid synthesis by TB
S.E. of pyrazinamide
gout
hepatitis
ethambutol MOA
inhibits transferase, necessary for cell wall synthesis
S.E. ethambutol
optic neuritis
impared red/green discrimmination- decreases vision
how do you use bedaquiline
always used with at least 3 other antiTB drugs
bedaquiline MOA
inhibits mycobacterial ATP synthetase
S.E. bedaquiline
arrhythmias
dapsone related to what
sulfonamides, same MOA
dapsone is used for what
mycobacterium leprae
you can’t use _______ as antimycoplasma agents
any cell wall inhibitors
what two drugs will work as antimycoplasms
erythromycin
tetracycline
