Term
Antibiotics are substances produced by some microorganisms capable of
a. destroying/killing (bacteri_____) or
b. inhibiting the growth (bacteri______) |
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Definition
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Term
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Definition
| IC 50 – where 50% of bacteria cells are killed or where 50% 0f the host cells are killed |
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Term
| trimethoprim: order of effectiveness against human, protozoal, and bacterial cells |
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Definition
most effective against bacteria (0.005)
intermediate effective against protozoa (0.07)
least effective against human cell (260) |
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Term
| pyrimethamine: order of effectiveness against human, protozoal, and bacterial cells |
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Definition
most effective against protozoal (0.0005)
intermediate effective against human cell (0.7)
least effective against bacteria (2.5) |
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Term
| methotrexate: order of effectiveness against human, protozoal, and bacterial cells |
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Definition
most effective against human cell (0.001)
intermediate effective against protozoa (~0.1)
inactive against bacteria |
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Term
| One measure, which relates the dose of a drug required to produce a desired effect to that which produces an undesired effect, is the _____ |
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Definition
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Term
| Therapeutic index is defined by ____/_____ |
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Definition
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Term
Toxic dose (TD50): means what?
Effective dose (ED50): means what? |
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Definition
Dose required to produce a particular toxic effect in 50% of animals
Dose at which 50% of individuals exhibit a specified therapeutic effect |
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Term
| High therapeutic index: _____ TD50 and ____ ED50 |
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Definition
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Term
| the > the therapeutic index, the > the _____ of a drug |
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Definition
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Term
| In general, agents that are active against the _____ are “cidal” |
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Definition
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Term
| Cidal agents required for ________ patients and those with _______, _______, and infections in ______ cancer patients |
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Definition
immunocompromised
endocarditis
meningitis
neutropenic |
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Term
Concentration-dependent killing (bacteriocidal):
Rate and extent of killing depends on drug _____
Examples: _______,_______ |
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Definition
concentration
Aminoglycosides, quinolones |
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Term
Time-dependent killing (bacteriocidal):
Drug concentration must be maintained above a ______
Examples: _____,______ |
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Definition
minimum bacteriocidal concentration (MBC)
Beta-lactams, vancomycin |
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Term
| with Concentration-dependent killing, the rate of bacterial killing _______ as the conc. of drug increases |
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Definition
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Term
| with Time-dependent killing, the rate of bacterial killing _________ as the conc. of drug increases |
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Definition
| does not significantly increase |
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Term
| In general, ____ synthesis inhibitors are bacteriostatic (but _______ are Bactericidal) |
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Definition
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Term
“Cidal” versus”static is relative
Example: penicillin is only bacterio_____ versus enterococci. When combined with an aminoglycoside like gentamicin, bacterio______ activity results. Due to increased _____ of gentamicin. Conversely, gentamicin is ineffective against enterococci in the absence of penicillin. This drug-drug enhancement is called ______. |
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Definition
bacteriostatic
bacteriocidal
permeability
synergism |
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Term
| Bacterial or tumor sensitive implies that the tumor or bacterial cell is ..... |
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Definition
| readily inhibited by the concentration of drug. |
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Term
| Bacterial or tumor resistance refers to the ability of a cell to ...... |
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Definition
grow in the presence of an antibiotic or cancer chemotherapeutic agent.
Resistant cells have a
growth advantage!!!!!! |
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Term
| Combinations of antimicrobrial agents can be (3) |
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Definition
a. synergistic
b. additive
c. antagonistic |
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Term
example:
A penicillin and an aminoglycoside may kill enterococcus more effectively than either component alone because inhibition of cell wall synthesis by penicillin allows passage of the aminoglycoside to its target in the cell.
This is an example of a _________ combination |
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Definition
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Term
example:
The inhibition of growth by bacteriostatic agents can prevent the lethal activity of penicillin because it is effective only on dividing cells. Therefore, bacteriostatic and bactericidal agents are not used together.
This is an example of _______ combination |
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Definition
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Term
| Combination Pharmacotherapy, even if it is additive, is important because it decreases the probability of the emergence of a _______. |
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Definition
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Term
| If you don’t know causative organism, agent with a _____ spectrum of activity is usually required |
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Definition
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Term
Don’t put bacteriocidal & bacteriostatic together. Static will stop growth, but for cidal agent to work, there has to be a growing cell so if w/ a static, a cidal cannot work
Ex. Don’t give an aminoglycoside w/ tetracycline |
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Definition
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|
Term
| MIC-minimum inhibitory concentration?.... |
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Definition
| The lowest concentration of antibiotic that will inhibit the growth of an organism |
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Term
| Organism is usually considered “susceptible” if blood levels of drug ___-___ times the MIC can be attained without appreciable side effects |
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Definition
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Term
| MBC–minimum bactericidal concentration or minimum lethal concentration (MLC)?... |
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Definition
| lowest conc. of drug that kills 99.9% of bacteria |
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Term
| Susceptibility Testing: Kirby-Bauer disk diffusion test?... |
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Definition
A culture plate is seeded with a bacterial isolate.
Disks are placed containing different antibiotics.
Clear zones around disks indicate bug is susceptible & antibiotic is effective. |
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Term
| ____ spectrum: Only specific types of bacteria inhibited or killed. Example: only gram (+) cocci |
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Definition
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Term
| _____ spectrum: Many different types of bacteria are inhibited and/or killed. Example: gram (+) cocci, and bacilli, and many gram (-) bacteria |
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Definition
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Term
| inhibitors of metabolism: (2) |
|
Definition
Sulfonamides
Trimethoprim
These are competitive inhibitors of the enzyme involved in folate synthesis. -> important nutrient for pregnant women |
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Term
| Inhibitors of cell wall synthesis: (2) |
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Definition
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Term
| Inhibitors of protein synthesis: (5) |
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Definition
tetracyclines
aminoglycosides
macrolides
clindamycin
cloramphenicol |
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Term
| inhibitors of nucleic acid function or synthesis (2) |
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Definition
|
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Term
| inhibitors of cell membrane function (2) |
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Definition
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Term
| Penicillin G is what type of drug? |
|
Definition
| Natural Penicillin (100% resistant to Staphylococci) |
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Term
| Penicillin V is what type of drug? |
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Definition
| Natural Penicillin (100% resistant to Staphylococci) |
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Term
| Benzathine or procaine Penicillin G is what type of drug? |
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Definition
| Natural Penicillin (100% resistant to Staphylococci) |
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Term
| Methicillin is what type of drug? |
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Definition
| Antistaphylococcal Penicillins |
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Term
| nafcillin is what type of drug? |
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Definition
| Antistaphylococcal Penicillins |
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Term
| dicloxacillin is what type of drug? |
|
Definition
| Antistaphylococcal Penicillins |
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Term
| Oxacillin is what type of drug? |
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Definition
| Antistaphylococcal Penicillins |
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Term
| cloxacillin is what type of drug? |
|
Definition
| Antistaphylococcal Penicillins |
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Term
| floxacillin is what type of drug? |
|
Definition
| Antistaphylococcal Penicillins |
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Term
| Ampicillin is what type of druG? |
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Definition
| Extended Spectrum Penicillin |
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Term
| Amoxicillin is what type of drug? |
|
Definition
| Extended Spectrum Penicillin |
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|
Term
| Carbenicillin is what type of drug? |
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Definition
| Anti-Pseudomonal Penicillin |
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|
Term
| piperacillin is what type of drug? |
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Definition
| Anti-Pseudomonal Penicillin |
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Term
| ticarcillin is what type of drug? |
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Definition
| Anti-Pseudomonal Penicillin |
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|
Term
| Mezlocillin is what type of drug? |
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Definition
| Anti-Pseudomonal Penicillin |
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|
Term
| azlocillin is what type of drug? |
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Definition
| Anti-Pseudomonal Penicillin |
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Term
| All penicillins are _____ antibiotics |
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Definition
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Term
| Penicillins have __-member b-lactam ring |
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Definition
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Term
| Cephalosporins have __-member b-lactam ring |
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Definition
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|
Term
| Carbapenem and monobactams have _____ rings |
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Definition
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Term
| _____ of the b-lactams determine stability to stomach acid, antimicrobial spectrum, and susceptibility to b-lactamases |
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Definition
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|
Term
Penicillins: Mechanism of Action:
Inhibit ___ step of bacterial ____ synthesis
Inhibit cross linking of ____
Exposes membrane to _____
This makes these drugs bacterio_____ |
|
Definition
last
cell wall
peptides
osmotic lysis
bacteriocidal |
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|
Term
| Penicillins are Inactive against organisms that lack a cell wall, e.g., (4) |
|
Definition
mycobacteria
protozoa
fungi
viruses |
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|
Term
| Gram + bacteria have a bigger _______ layer than gram - |
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Definition
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Term
| Penicillin better against gram___ b/c it doesn’t have an outer membrane, w/ gram__ would have to pass through lipid bilayer to get to the cell wall |
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Definition
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Term
| Gram ___ have an outer lipid membrane layer |
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Definition
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Term
| _______ are enzymes (transpeptidase) involved in cell wall synthesis |
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Definition
| Penicillin Binding Proteins (PBPs) |
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Term
| Penicillins bind to ____ and inhibit them |
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Definition
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Term
| Alterations (or mutations ) in ___ of Staphylococcus aureus confers resistance = Methicillin-resistant S. aureus (MRSA) |
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Definition
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Term
| Penicillin inhibits _____ by binding to PBP |
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Definition
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Term
| _______ are a group of enzymes that exist in all bacteria containing peptidoglycan. The peptidoglycan matrix is very rigid, so these enzymes break down the peptidoglycan matrix in small sections so that growth and division of cells can occur. In the presence of Penicillins, cell wall breakdown proceeds in the absence of cell wall synthesis, resulting in cell ____ |
|
Definition
|
|
Term
Penicillin G: Spectrum
Gram (__) organisms are usually susceptible
Acquired resistance can be a problem |
|
Definition
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|
Term
Penicillin G: Spectrum:
G(+) cocci – (4)
G (+) bacilli – (4) |
|
Definition
S. aureus, Strep. pneumoniae, Strep. pyrogenes, Strep. viridans
Bacillus anthracis (anthrax), Clostridium perfringens, Corynebacterium diphtheriae, Listeria monocytogenes |
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Term
| Penicilling G is not very effective against Gram (__) b/c they have outer lipopolysaccharide membrane that presents a barrier to water-soluble penicillins |
|
Definition
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Term
Penicillin G: Spectrum
Some Gram (-) have ____ in outer membrane that will allow some penicillins to enter
G(-) cocci – (2)
G(-) bacilli- most are _____ |
|
Definition
pores (porins)
Neisseria gonorrhoeae, N. meningitidis
resistant |
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|
Term
Penicillin G: Spectrum
Spirochetes susceptible: (1) |
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Definition
| Treponema pallidum - syphilis |
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Term
Resistance through Beta-lactamases:
B-lactamases are enzymes produced by some bacteria and are responsible for their resistance to beta-lactam antibiotics. This resistance Can be ____ or ____ through transfer of plasmid |
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Definition
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|
Term
Resistance through Decreased permeability to drug:
In gram(__) -> a drug's decreased ability to cross outer membrane causes resistance |
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Definition
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Term
Resistance through Altered Penicillin Binding Proteins:
Bacteria can develop and produce mutated forms of PBPs that have lower affinity for _____. Example? |
|
Definition
penicillins
MRSA=Methicillin Resistant Staph. aureus |
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Term
| _____ blocks tubular transporter in kidneys and elevates plasma levels of penicillin |
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Definition
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|
Term
Adverse reactions of B-lactams:
Hypersensitivity (Allergy):
____ of penicillins serves as hapten to cause immune reactions.
About __% of patients react.
Maculopapular rash, angioedema, anaphylaxis
Cross-reactivity occurs with all ____ |
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Definition
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|
Term
Adverse reactions of B-lactams:
_____ from imbalance of GI flora
____ & ____ -> decreased agglutination of platelets |
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Definition
Diarrhea
Carbenicillin & ticarcillin |
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Term
| Ampicillin is what type of drug? |
|
Definition
| Extended Spectrum Penicillins |
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|
Term
| Amoxicillin is what type of drug? |
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Definition
| Extended Spectrum Penicillins |
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Term
| Extended Spectrum Penicillins are _____ sensitive |
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Definition
| Penicillinase (beta-lactamase) |
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Term
| Amoxicillin Can combine with ____ (____ inhibitor) to enhance spectrum |
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Definition
clavulanic acid
penicillinase |
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Term
| Amoxicillin + clavulanic acid = ____ |
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Definition
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|
Term
| Amoxicillin has _____ oral bioavailability |
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Definition
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Term
| Extended spectrum antibiotics affect these bacteria: (6) |
|
Definition
Haemophilus influenzae
E. coli
Listeria monocytogenes
Proteus mirabilis
Salmonella
enterococci
HELPS kill enterococci |
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Term
| Adverse Reactions of Extended Spectrum Antibiotics: (2) |
|
Definition
Hypersensitivity
Pseudomembranous colitis |
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|
Term
| For meningitis use ____ and do not use _____ due to resistance |
|
Definition
ceftriaxone
benzylpenicillin |
|
|
Term
Cephalosporins are Very valuable for many gram (__) infections
activity against ____
inactive against ____ & ____ |
|
Definition
-
Klebsiella
enterococci & methicillin-resistant staph. |
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Term
| Cefazolin is what type of drug? |
|
Definition
| 1st generation Cephalosporin |
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Term
| cephalexin is what type of drug? |
|
Definition
| 1st generation Cephalosporin |
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Term
| Cefuroxime is what type of drug? |
|
Definition
| 2nd generation Cephalosporin |
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|
Term
| Ceftriaxone is what type of drug? |
|
Definition
| 3rd generation Cephalosporin |
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|
Term
| Ceftazidime is what type of drug? |
|
Definition
| 4th Generation Cephalosporin |
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|
Term
| ___ generation Cephalosporin is effective to treat meningitis |
|
Definition
|
|
Term
| First generation Cephalosporins are Very active against gram (__) ____. Modestly active against gram (__) organisms. They ___ penetrate the CNS. Do no use for ____. |
|
Definition
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|
Term
| Second generation Cephalosporins are Moderately active against gram (__) organisms. They Have extended gram (__) coverage. They are Inactive against ____. Cefuroxime __ penetrate the CNS. |
|
Definition
+
-
Pseudomonas aeruginosa
does |
|
|
Term
Third and Fourth generation Cephalosporins are Less active against gram (__) bacteria than those of second generation.
Expanded gram (__) coverage.
They ___ penetrate the CNS.
Exceptions: _____ & ____
_____ has Adequate antipseudomonal activity
_____ has Activity against B. fragilis |
|
Definition
+
-
do
Cefoperazone & Cefixime
Ceftazidime
Ceftizoxime |
|
|
Term
1st Generation Cephalosporins:
______ ->(use IV)
______ & ______ -> (use PO)
______, _______, & _______ -> (IV,PO) |
|
Definition
Cefazolin
cephalexin & Cefadroxil
cephalothin, cephapirin, cephradine |
|
|
Term
| 1st Generation Cephalosporins affect Gram(+) cocci as well as... (3) |
|
Definition
Proteus mirabilis
E. coli
Klebsiella pneumoniae |
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|
Term
| ____ Generation Cephalosporins are Useful in skin and soft tissue infections S. pyrogenes and/or S. aureus |
|
Definition
|
|
Term
| ___ Generation Cephalosporins are Useful for prophylaxis before surgery |
|
Definition
|
|
Term
| ________: 2nd Generation Cephalosporin that has activity against H. influenzae and is Used for community-acquired respiratory infections (otitis media, sinusitis, pneumonia) |
|
Definition
|
|
Term
| ____(3)____: 2nd Generation Cephalosporin With activity against Bacteroides fragilis. Used for mixed aerobic-anaerobic infections, usually intra-abdominal, or infected lower limb of diabetic |
|
Definition
| Cefmetazole, cefotetan, cefoxitin |
|
|
Term
| 3rd Generation Cephalosporins Have increased activity versus gram (__) bacilli, particularly ____ and _____ |
|
Definition
-
Enterobacteriaceae
H. influenzae. |
|
|
Term
| ___ Generation Cephalosporins are the Drug of choice for N. gonorrhea |
|
Definition
|
|
Term
| ____ Generation Cephalosporins Achieve adequate concentrations in CSF against major meningeal pathogens |
|
Definition
|
|
Term
| ____ Generation Cephalosporins Use for meningitis & serious infections such as nosocomial pneumonia due to aerobic Gram (-) bacilli |
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Definition
|
|
Term
| ________ is Stable to b-lactamase |
|
Definition
|
|
Term
| ______ Generation Cephalosporins are Active against Pseudomonas aeruginosa |
|
Definition
|
|
Term
Oral extended spectrum 3rd/4th generation cephalosporins
______ & _______ are Used to treat infections due to Enterobacteriaceae resistant to other oral b-lactams. They are Less active than other 3rd/4th generations for Gram (__) bacilli & _______ & _____ |
|
Definition
Cefixime & cefpodoxime
-
P. aeruginosa & S. aureus |
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|
Term
| Imipenem is what type of drug? |
|
Definition
|
|
Term
| Carbapenems are a class of ____ antibiotics with a ____ spectrum of antibacterial activity. |
|
Definition
|
|
Term
| Carbapenems Resists hydrolysis by most _____ |
|
Definition
|
|
Term
| Imipenem always given with ____(an inhibitor of ____) to decrease inactivation in renal tubules |
|
Definition
cilastatin
renal dihydropeptidase I |
|
|
Term
| ______: Drug of choice for Enterobacter |
|
Definition
| Carbapenems (Imipenem/cilastatin) |
|
|
Term
| Aztreonam is a synthetic monocyclic ____ antibiotic (a ___) |
|
Definition
|
|
Term
| Aztreonam is a monobactam resistant to ____ |
|
Definition
|
|
Term
| Mechanism of Action of Aztreonam? |
|
Definition
| Binds to PBPs and inhibits cell wall synthesis |
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|
Term
| Aztreonam is Synergistic with _____ |
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Definition
|
|
Term
| Aztreonam has No cross-reactivity with _____ |
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Definition
|
|
Term
| Aztreonam is Used for Gram (__) ____, Klebsiella, Pseudomonas, Serratia. |
|
Definition
|
|
Term
| Aztreonam is Not active vs. gram (__) or ____. |
|
Definition
|
|
Term
| What antibiotic is Used for penicillin-allergic patients and those with renal insufficiency who can’t tolerate aminoglycosides.? |
|
Definition
|
|
Term
| Clavulanic Acid is what type of drug? |
|
Definition
|
|
Term
| Sulbactam is what type of drug? |
|
Definition
|
|
Term
| Tazobactam is what type of drug? |
|
Definition
|
|
Term
| b-lactamase Inhibitors (3)... |
|
Definition
Clavulanic Acid
Sulbactam
Tazobactam |
|
|
Term
| b-lactamase Inhibitors have No significant ____ activity by themselves. They Bind to and _____ b-lactamases and therefore Protect co-administered _____. |
|
Definition
antibacterial
inactivate
antibiotic |
|
|
Term
| Vancomycin is a tricyclic _____ antibiotic (not a lactam) |
|
Definition
|
|
Term
| MEchanism of action of Vancomycin? |
|
Definition
| Inhibits cell wall mucopeptide formation |
|
|
Term
| Vancomycin is bacterio______ |
|
Definition
|
|
Term
| _____ is the antibiotic Used for serious gram (+) multidrug-resistant organisms including S. aureus, Clostridium difficile (pseudomembranous colitis) |
|
Definition
|
|
Term
What antibiotic has this Toxicity: nephrotoxic, ototoxicity, thrombophlebitis, diffuse flushing -> "red man
syndrome” |
|
Definition
|
|
Term
| _____ is the antibiotic used to treat methicillin-resistant Staph. Infection (MRSA); ____ can also be used |
|
Definition
|
|
Term
| With Drug resistant S. pneumoniae: ______ can be used for severely ill patients. |
|
Definition
|
|
Term
| For methicillin/vancomycin-resistant staph infection use ____ |
|
Definition
|
|
